Sunday, September 30, 2012

Mepron


Generic Name: atovaquone (Oral route)

a-TOE-va-kwone

Commonly used brand name(s)

In the U.S.


  • Mepron

Available Dosage Forms:


  • Tablet

  • Suspension

Therapeutic Class: Antiprotozoal


Chemical Class: Ubiquinone


Uses For Mepron


Atovaquone is used to treat and to prevent Pneumocystis carinii pneumonia (PCP), a very serious kind of pneumonia. This particular kind of pneumonia occurs commonly in patients whose immune systems are not working normally, such as cancer patients, transplant patients, and patients with acquired immune deficiency syndrome (AIDS).


This medicine is available only with your doctor's prescription.


Before Using Mepron


In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:


Allergies


Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.


Pediatric


Appropriate studies have not been performed on the relationship of age to the effects of atovaquone in children 1 month to 13 years of age. Safety and efficacy have not been established .


Geriatric


Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of atovaquone in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems which may require an adjustment of dosage in patients receiving atovaquone .


Pregnancy








Pregnancy CategoryExplanation
All TrimestersCAnimal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding


There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.


Interactions with Medicines


Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.


Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.


  • Rifampin

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.


  • Indinavir

  • Rifabutin

  • Tetracycline

  • Warfarin

Interactions with Food/Tobacco/Alcohol


Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.


Other Medical Problems


The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:


  • Liver disease, severe or

  • Stomach or intestinal disorders—Atovaquone may not work properly in patients with these conditions .

Proper Use of Mepron


Make certain your doctor knows if you are on any special diet. This medicine must be taken with balanced meals so that it can work properly.


It is important that you take atovaquone with a balanced meal. This is to make sure the medicine is fully absorbed into the body and will work properly.


Atovaquone tablets may be crushed if necessary to make it easier to swallow.


Because atovaquone tablets and oral suspension do not produce the same amount of medicine in the blood, the tablets and the suspension cannot be switched and used in place of each other.


For patients taking the oral liquid form of this medicine:


  • Shake the bottle gently before using atovaquone.

  • This medicine is to be taken by mouth. Use a specially marked measuring spoon or other device to measure each dose accurately. The average household teaspoon may not hold the right amount of liquid.

  • Do not use after the expiration date on the label since the medicine may not work properly after that date. Check with your pharmacist if you have any questions about this .

To help clear up your infection completely, keep taking your medicine for the full time of treatment, even if you begin to feel better after a few days. If you stop taking this medicine too soon, your symptoms may return.


Atovaquone works best when there is a constant amount in the blood. To help keep the amount constant, do not miss any doses.


Dosing


The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.


The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.


  • For prevention of Pneumocystis carinii pneumonia (PCP):
    • For oral dosage form (suspension):
      • Adults and teenagers—1,500 milligrams (mg) or 10 milliliters (mL) once a day with a meal.

      • Children—Use and dose must be determined by your doctor .



  • For treatment of Pneumocystis carinii pneumonia (PCP):
    • For oral dosage form (suspension):
      • Adults and teenagers—750 milligrams (mg) or 5 milliliters (mL) taken with a meal two times a day for 21 days.

      • Children—Use and dose must be determined by your doctor .


    • For oral dosage form (tablets):
      • Adults and teenagers—750 milligrams (mg) taken with a meal three times a day for 21 days.

      • Children—Use and dose must be determined by your doctor.



Missed Dose


If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.


Storage


Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.


Keep out of the reach of children.


Do not keep outdated medicine or medicine no longer needed.


Ask your healthcare professional how you should dispose of any medicine you do not use.


Precautions While Using Mepron


It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood tests may be needed to check for unwanted effects .


If your symptoms do not improve within a few days, or if they become worse, check with your doctor.


Mepron Side Effects


Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.


Check with your doctor immediately if any of the following side effects occur:


More common
  • Cough or hoarseness

  • difficult or labored breathing

  • fever or chills

  • lower back or side pain

  • painful or difficult urination

  • shortness of breath

  • tightness in chest

  • wheezing

Incidence not known
  • Black, tarry stools

  • bleeding gums

  • bloating

  • blood in urine or stools

  • bluish-colored lips, fingernails, or palms

  • constipation

  • dark urine

  • dizziness or lightheadedness

  • fast heartbeat

  • headache

  • indigestion

  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs

  • light-colored stools

  • loss of appetite

  • nausea

  • noisy breathing

  • pains in stomach, side, or abdomen, possibly radiating to the back

  • pale skin

  • pinpoint red spots on skin

  • rapid heart rate

  • sore throat

  • unusual bleeding or bruising

  • unusual tiredness or weakness

  • vomiting

  • yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:


More common
  • Abdominal or stomach pain

  • diarrhea

  • lack or loss of strength

  • runny nose

  • skin rash

  • sleeplessness

  • sneezing

  • sore mouth or tongue

  • stuffy nose

  • sweating

  • trouble in sleeping

  • unable to sleep

  • white patches in mouth, tongue, or throat

Incidence not known
  • Blistering, peeling, or loosening of skin

  • eye irritation or redness

  • itching

  • joint or muscle pain

  • red skin lesions, often with a purple center

  • skin rash

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.


Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Mepron side effects (in more detail)



The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.


The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.


More Mepron resources


  • Mepron Side Effects (in more detail)
  • Mepron Use in Pregnancy & Breastfeeding
  • Drug Images
  • Mepron Drug Interactions
  • Mepron Support Group
  • 1 Review for Mepron - Add your own review/rating


  • Mepron Prescribing Information (FDA)

  • Mepron Concise Consumer Information (Cerner Multum)

  • Mepron Monograph (AHFS DI)

  • Mepron MedFacts Consumer Leaflet (Wolters Kluwer)

  • Atovaquone Professional Patient Advice (Wolters Kluwer)

  • Atovaquone and Proguanil Hydrochloride Monograph (AHFS DI)



Compare Mepron with other medications


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Saturday, September 29, 2012

Viread


Pronunciation: ten-OF-oh-vir
Generic Name: Tenofovir
Brand Name: Viread

Severe and sometimes fatal lactic acidosis (a buildup of lactic acid in the blood) and liver problems have occurred with this type of medicine. The risk may be greater in women, patients who are very overweight, or patients who have been taking nucleoside medicines (eg, emtricitabine, tenofovir) for a long time.


Tell your doctor right away if you develop symptoms of lactic acidosis (eg, unusual weakness or tiredness; unusual muscle pain; fast or difficult breathing; stomach pain with nausea and vomiting; feeling cold, especially in the arms and legs; dizziness or lightheadedness; fast or irregular heartbeat). Tell your doctor right away if you develop symptoms of liver problems (eg, yellowing of the skin or eyes, dark urine, pale stools, persistent loss of appetite, nausea, stomach pain).


Some patients with hepatitis B virus (HBV) infection who took Viread had severe worsening of HBV infection after they stopped taking it. Patients who have HBV infection need close medical follow-up to check for worsening liver problems for at least several months after they stop Viread. Keep all doctor and lab appointments. Do not stop taking Viread without checking with your doctor.





Viread is used for:

Treating HIV infection in combination with other medicines. It is also used to treat chronic hepatitis B infection. It may also be used for other conditions as determined by your doctor.


Viread is an antiviral reverse transcriptase inhibitor. It works to treat HIV infection by reducing the amount of HIV (the virus that causes AIDS) in the body by blocking the ability of the virus to multiply. It works to treat HBV infection by reducing the amount of HBV in the body by blocking the ability of the virus to multiply and infect new liver cells. Viread is not a cure for HIV or AIDS.


Do NOT use Viread if:


  • you are allergic to any ingredient in Viread

  • you have severe liver problems (eg, an enlarged liver) or lactic acidosis

  • you take adefovir or other medicines that contain tenofovir

  • you take a medicine that may harm your kidneys (eg, an aminoglycoside antibiotic [eg, gentamicin], amphotericin B, cyclosporine, a nonsteroidal anti-inflammatory drug [NSAID] [eg, ibuprofen], tacrolimus, vancomycin). Ask your doctor if you are not sure if any of your medicines might harm your kidneys

Contact your doctor or health care provider right away if any of these apply to you.



Before using Viread:


Some medical conditions may interact with Viread. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


  • if you are pregnant, planning to become pregnant, or are breast-feeding

  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

  • if you have allergies to medicines, foods, or other substances

  • if you have a history of bone problems or kidney problems (including dialysis treatment), or if you are overweight

  • if you have abnormal liver function tests or liver problems, including HBV infection

  • if you have HIV infection

Some MEDICINES MAY INTERACT with Viread. Tell your health care provider if you are taking any other medicines, especially any of the following:


  • Medicines that may harm the kidney (eg, aminoglycoside antibiotics [eg, gentamicin], amphotericin B, cyclosporine, NSAIDs [eg, ibuprofen], tacrolimus, vancomycin) because they may increase the risk of Viread's side effects. Ask your doctor if you are not sure if any of your medicines might harm your kidneys

  • Certain antiviral medicines (eg, acyclovir, cidofovir, ganciclovir) because they may increase the risk of Viread's side effects

  • Adefovir, HIV protease inhibitors (eg, atazanavir), lopinavir/ritonavir, or medicines that contain tenofovir because they may increase the risk of Viread's side effects

  • Didanosine because the risk of its side effects may be increased by Viread

This may not be a complete list of all interactions that may occur. Ask your health care provider if Viread may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.


How to use Viread:


Use Viread as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • An extra patient leaflet is available with Viread. Talk to your pharmacist if you have questions about this information.

  • Take Viread by mouth with or without food.

  • Continue to take Viread even if you feel well. Do not miss any doses.

  • Taking Viread at the same time each day will help you remember to take it.

  • Do not suddenly stop taking Viread without checking with your doctor. This may cause the virus to become less sensitive to this or other medicines. Some conditions (eg, hepatitis B) could become worse if you suddenly stop taking Viread.

  • If you miss a dose of Viread, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Viread.



Important safety information:


  • Viread may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Use Viread with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

  • If you have HIV infection, you should be tested for HBV infection before you start to take Viread. If you have HBV infection, you should be tested for HIV infection before you start to take Viread.

  • Keep a list of all the medicines that you take. Make a new list each time medicines are added or stopped. Find out about medicines that should not be taken while you are using Viread. Be sure that each of your health care providers know all the medicines that you are taking.

  • When your medicine supply is low, get more from your doctor or pharmacist as soon as you can. Do not stop taking Viread, even for a short period of time. If you do, the virus may grow resistant to the medicine and become harder to treat.

  • Viread is not a cure for HIV infection. Patients may still get illnesses and infections associated with HIV. Remain under the care of your doctor.

  • Viread does not stop the spread of HIV or HBV to others through blood or sexual contact. Use barrier methods of birth control (eg, condoms) if you have HIV infection. Do not share needles, injection supplies, or items like toothbrushes or razors.

  • If you have HBV infection, you will need close medical follow-up for several months after stopping treatment with Viread. Follow-up includes medical exams and blood tests to check for HBV infection that could be getting worse.

  • Viread may improve immune system function. This may reveal hidden infections in some patients. Tell your doctor right away if you notice symptoms of infection (eg, fever, sore throat, weakness, cough, shortness of breath) after you start Viread.

  • Check with your doctor to see if you should take a calcium and vitamin D supplement while you are taking Viread.

  • Changes in body fat (eg, an increased amount of fat in the upper back, neck, breast, and trunk, and loss of fat from the legs, arms, and face) may occur in some patients taking Viread. The cause and long-term effects of these changes are unknown. Discuss any concerns with your doctor.

  • Lab tests, including liver and kidney function and bone mineral density, may be performed while you use Viread. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • Use Viread with extreme caution in CHILDREN younger than 18 years old; safety and effectiveness in these children have not been confirmed.

  • PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Viread while you are pregnant. It is not known if Viread is found in breast milk. Mothers infected with HIV should not breast-feed. There is a risk of passing the HIV infection or Viread to the baby. Do not breast-feed while taking Viread.


Possible side effects of Viread:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:



Abnormal skin sensations; back pain; diarrhea; dizziness; gas; headache; indigestion; loss of appetite; nausea; sleeplessness; sweating; vomiting; weakness; weight loss.



Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); anxiety; bone pain; chest pain; fever, chills, or sore throat; mental or mood changes (eg, depression); numbness, burning, pain, or tingling in the hands or feet; pneumonia; severe or persistent nausea or vomiting; shortness of breath; stomach pain; symptoms of kidney problems (eg, increased or decreased urination, increased thirst); symptoms of lactic acidosis (eg, unusual weakness or tiredness; unusual muscle pain; fast or difficult breathing; stomach pain with nausea and vomiting; feeling cold, especially in the arms and legs; dizziness or lightheadedness; fast or irregular heartbeat); symptoms of liver problems (eg, yellowing of the skin or eyes; dark urine; pale stools; persistent loss of appetite).



This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


See also: Viread side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.


Proper storage of Viread:

Store Viread at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Do not use Viread if the seal over the bottle opening is broken or missing. Keep Viread in its original container and keep the container tightly closed. Do not keep medicine that is out of date or that you no longer need. If you throw any medicines away, make sure that children or pets cannot find them. Keep Viread out of the reach of children and away from pets.


General information:


  • If you have any questions about Viread, please talk with your doctor, pharmacist, or other health care provider.

  • Viread is to be used only by the patient for whom it is prescribed. Do not share it with other people.

  • If your symptoms do not improve or if they become worse, check with your doctor.

  • Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Viread. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Viread resources


  • Viread Side Effects (in more detail)
  • Viread Use in Pregnancy & Breastfeeding
  • Drug Images
  • Viread Drug Interactions
  • Viread Support Group
  • 2 Reviews for Viread - Add your own review/rating


  • Viread Prescribing Information (FDA)

  • Viread Monograph (AHFS DI)

  • Viread Advanced Consumer (Micromedex) - Includes Dosage Information

  • Viread Consumer Overview



Compare Viread with other medications


  • Hepatitis B
  • HIV Infection
  • Nonoccupational Exposure

Thursday, September 27, 2012

Cardene SR Sustained-Release Capsules


Pronunciation: nye-KAR-di-peen
Generic Name: Nicardipine
Brand Name: Cardene SR


Cardene SR Sustained-Release Capsules are used for:

Treating high blood pressure. It may be used alone or in combination with other high blood pressure medicines. It may also be used for other conditions as determined by your doctor.


Cardene SR Sustained-Release Capsules are a calcium channel blocker. It works by relaxing the blood vessels, which helps to lower blood pressure.


Do NOT use Cardene SR Sustained-Release Capsules if:


  • you are allergic to any ingredient in Cardene SR Sustained-Release Capsules

  • you are breast-feeding

  • you have advanced narrowing of your aorta (stenosis)

Contact your doctor or health care provider right away if any of these apply to you.



Before using Cardene SR Sustained-Release Capsules:


Some medical conditions may interact with Cardene SR Sustained-Release Capsules. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


  • if you are pregnant or planning to become pregnant

  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

  • if you have allergies to medicines, foods, or other substances

  • if you have angina (chest pain), congestive heart failure (CHF) or other heart problems, adrenal glad problems (eg, pheochromocytoma), liver or kidney problems, low blood pressure, or lung congestion associated with heart attack, or have had a stroke

  • you have CHF and you are taking a beta-blocker, or you are having beta-blocker withdrawal

Some MEDICINES MAY INTERACT with Cardene SR Sustained-Release Capsules. Tell your health care provider if you are taking any other medicines, especially any of the following:


  • Cimetidine because it may increase the risk of Cardene SR Sustained-Release Capsules's side effects

  • Cyclosporine or digoxin because the risk of their side effects may be increased by Cardene SR Sustained-Release Capsules

This may not be a complete list of all interactions that may occur. Ask your health care provider if Cardene SR Sustained-Release Capsules may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.


How to use Cardene SR Sustained-Release Capsules:


Use Cardene SR Sustained-Release Capsules as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • Take Cardene SR Sustained-Release Capsules by mouth with or without food, but do not take with a high-fat meal.

  • Swallow Cardene SR Sustained-Release Capsules whole. Do not break, crush, or chew before swallowing.

  • Do not eat grapefruit or drink grapefruit juice while taking Cardene SR Sustained-Release Capsules unless your doctor directs you otherwise.

  • If you miss a dose of Cardene SR Sustained-Release Capsules, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Cardene SR Sustained-Release Capsules.



Important safety information:


  • Cardene SR Sustained-Release Capsules may cause dizziness or fainting. These effects may be worse if you take it with alcohol or certain medicines. Use Cardene SR Sustained-Release Capsules with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

  • Patients being treated for high blood pressure often feel tired or run down for a few weeks after beginning therapy. Continue taking your medicine even though you may not feel quite "normal." Contact your doctor or pharmacist about any new symptoms.

  • Maximum lowering of blood pressure occurs approximately 1 to 2 hours after taking the medicine. Blood pressure should be taken 1 to 2 hours after the medicine has been taken.

  • Tell your doctor or dentist that you take Cardene SR Sustained-Release Capsules before you receive any medical or dental care, emergency care, or surgery.

  • Additional monitoring of your dose or condition may be necessary if you are using intravenous (IV) calcium.

  • Lab tests, including blood pressure, electrocardiogram (ECG) readings, and monitoring of heart rate, may be performed while you use Cardene SR Sustained-Release Capsules. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Cardene SR Sustained-Release Capsules while you are pregnant. Cardene SR Sustained-Release Capsules are found in breast milk. Do not breast-feed while taking Cardene SR Sustained-Release Capsules.

If you suddenly stop taking Cardene SR Sustained-Release Capsules, you may experience WITHDRAWAL symptoms including increased chest pain (angina) and more frequent chest pain.



Possible side effects of Cardene SR Sustained-Release Capsules:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:



Dizziness; headache; nausea; upset stomach; vomiting.



Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); calf pain, swelling, or redness; confusion; fainting; fast or irregular heartbeat; fever; increased chest pain; pounding in the chest; shortness of breath or wheezing; swelling of the feet, ankles, or hands; unusual bruising or bleeding.



This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


See also: Cardene SR side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include confusion; drowsiness; fast or slowed heart rate; flushing; slurred speech; weakness.


Proper storage of Cardene SR Sustained-Release Capsules:

Store Cardene SR Sustained-Release Capsules between 59 and 86 degrees F (15 and 30 degrees C) in a tightly closed container. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Cardene SR Sustained-Release Capsules out of the reach of children and away from pets.


General information:


  • If you have any questions about Cardene SR Sustained-Release Capsules, please talk with your doctor, pharmacist, or other health care provider.

  • Cardene SR Sustained-Release Capsules are to be used only by the patient for whom it is prescribed. Do not share it with other people.

  • If your symptoms do not improve or if they become worse, check with your doctor.

  • Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Cardene SR Sustained-Release Capsules. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Cardene SR resources


  • Cardene SR Side Effects (in more detail)
  • Cardene SR Use in Pregnancy & Breastfeeding
  • Drug Images
  • Cardene SR Drug Interactions
  • Cardene SR Support Group
  • 0 Reviews for Cardene SR - Add your own review/rating


Compare Cardene SR with other medications


  • Angina Pectoris Prophylaxis
  • Heart Failure
  • High Blood Pressure

Wednesday, September 26, 2012

Triprolidine Hydrochloride


Class: First Generation Antihistamines
ATC Class: R06AX07
VA Class: AH104
CAS Number: 6138-79-0
Brands: Allerfrim, Aprodine, Zymine

Introduction

First generation antihistamine; an alkylamine derivative.a


Uses for Triprolidine Hydrochloride


Allergic and Nonallergic Rhinitis


Symptomatic relief of seasonal (e.g., hay fever) or perennial (nonseasonal) allergic rhinitis or nonallergic (vasomotor) rhinitis.101 102


Used in fixed combination with other agents (e.g., pseudoephedrine) for symptomatic relief of rhinorrhea, sneezing, oronasopharyngeal itching, lacrimation, itching eyes, and/or other symptoms (e.g., sinus congestion) associated with seasonal or perennial allergic rhinitis or nonallergic rhinitis.102 103 104 105


Allergic Conjunctivitis


Symptomatic relief of allergic conjunctivitis caused by foods or inhaled allergens.101


Allergic Skin Disorders


Symptomatic treatment of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.101


Common Cold


Used in fixed combination with other agents (e.g., pseudoephedrine) for self-medication for symptomatic relief of sinus congestion and other symptoms associated with the common cold.103 104


Triprolidine Hydrochloride Dosage and Administration


Administration


Oral Administration


Administer orally as tablets or oral solution.101 102 103 104 a


Dosage


Available as triprolidine hydrochloride; dosage expressed in terms of the salt.101 102 103 104


Individualize dosage according to patient’s response and tolerance.a b


Fixed-combination preparations do not permit individual titration of dosages. When used in fixed combination with other agents (e.g., pseudoephedrine), select a dosage that is within the usual therapeutic range for each ingredient; dosage recommendations of triprolidine hydrochloride for adults and children when administered in fixed combinations are the same as when the drug is used as a single agent.a


Pediatric Patients


Allergic Conditions

Allergic and Nonallergic Rhinitis, Allergic Conjunctivitis, and Allergic Skin Disorders

Oral

Children 4 months to <2 years of age: 0.313 mg every 4–6 hours (as oral solution), not to exceed 1.252 mg in 24 hours.101 (See Pediatric Use Under Cautions.)


Children 2 to <4 years of age: 0.625 mg every 4–6 hours (as oral solution), not to exceed 2.5 mg in 24 hours.101


Children 4 to <6 years of age: 0.938 mg every 4–6 hours (as oral solution), not to exceed 3.75 mg in 24 hours.101


Allergic Rhinitis and Allergic Conjunctivitis

Self-medication in children 6 to <12 years of age: 1.25 mg every 4–6 hours (as tablets or oral solution), not to exceed 5 mg in 24 hours.103 104 105


Self-medication in children ≥12 years of age: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104 105


Common Cold

Oral

Self-medication in children 6 to <12 years of age: 1.25 mg every 4–6 hours (as tablets or oral solution), not to exceed 5 mg in 24 hours.103 104


Self-medication in children ≥12 years of age: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104


Adults


Allergic Conditions

Allergic Rhinitis and Allergic Conjunctivitis

Oral

Self-medication: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104 105


Common Cold

Oral

Self-medication: 2.5 mg every 4–6 hours (as tablets or oral solution), not to exceed 10 mg in 24 hours.103 104


Prescribing Limits


Pediatric Patients


Allergic Conditions

Allergic and Nonallergic Rhinitis, Allergic Conjunctivitis, and Allergic Skin Disorders

Oral

Children 4 months to <2 years of age: Maximum 1.252 mg in 24 hours.101


Children 2 to <4 years of age: Maximum 2.5 mg in 24 hours.101


Children 4 to <6 years of age: Maximum 3.75 mg in 24 hours.101


Allergic Rhinitis and Allergic Conjunctivitis

Self-medication in children 6 to <12 years of age: Maximum 5 mg in 24 hours.103 104 105


Self-medication in children ≥12 years of age: Maximum 10 mg in 24 hours.103 104 105


Common Cold

Oral

Self-medication in children 6 to <12 years of age: Maximum 5 mg in 24 hours.103 104


Self-medication in children ≥12 years of age: Maximum 10 mg in 24 hours.103 104


Adults


Allergic Conditions

Allergic Rhinitis and Allergic Conjunctivitis

Oral

Self-medication: Maximum 10 mg in 24 hours.105


Common Cold

Oral

Self-medication: Maximum 10 mg in 24 hours.103 104


Cautions for Triprolidine Hydrochloride


Contraindications



  • Use contraindicated in neonates and premature infants.102 a b (See Pediatric Use under Cautions.)




  • Women who are breast-feeding.102 (See Lactation under Cautions.)




  • Patients receiving MAO inhibitor therapy.102 (See Interactions.)




  • Patients with asthmatic attacks.b




  • Known hypersensitivity to triprolidine or any ingredient in the formulation.101 102



Warnings/Precautions


Warnings


Concomitant Diseases

Because of anticholinergic effects, use with extreme caution in patients with angle-closure glaucoma, pyloroduodenal obstruction, bladder-neck obstruction, and symptomatic prostatic hypertrophy.101 102 b


Use with extreme caution in patients with a history of bronchial asthma, increased IOP, hyperthyroidism, or cardiovascular disease (e.g., hypertension).101 102 b


CNS Effects

Risk of drowsiness.102 105 (See CNS Depressants under Interactions and also see Advice to Patients.)


Possible excitability (especially in children).105 (See Pediatric Use under Cautions.)


General Precautions


Use of Fixed Combinations

When used in fixed combination with other agents (e.g., pseudoephedrine), consider the cautions, precautions, and contraindications associated with all ingredients in the formulation.103 104 105 a


Duration of Therapy

When used for self-medication, discontinue therapy and consult a clinician if symptoms persist for >7 days or are accompanied by fever.105


Specific Populations


Pregnancy

Category C.101 102 106


Lactation

Distributed into milk.106 Some manufacturers suggest discontinuing nursing or the drug because of potential risk to nursing infants.101 102 a However, AAP considers triprolidine compatible with breast-feeding.106


Pediatric Use

Use not recommended in premature or full-term neonates.a b (See Contraindications.)


Possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), especially in children.b


Use in children <4 months of age not recommended. Children <6 years of age should receive triprolidine only under the direction of a clinician.103 104


Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established. Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.


Geriatric Use

Possible increased risk of dizziness, sedation, and hypotension in geriatric patients ≥60 years of age.102 b


Common Adverse Effects


Drowsiness,101 dry mouth,101 anorexia,101 nausea,101 vomiting,101 headache,101 dizziness,101 102 nervousness,101 blurred vision,101 polyuria,101 heartburn,101 dysuria,101 urinary retention.101


Interactions for Triprolidine Hydrochloride


Specific Drugs and Laboratory Tests















Drug or Laboratory Test



Interaction



Comments



CNS depressants (e.g., alcohol, hypnotics, sedatives, tranquilizers, tricyclic antidepressants)



Possible additive CNS depression101 102 105 b


Tricyclic antidepressants prolong and intensify anticholinergic effects of antihistamines101



Avoid concomitant use102 105



MAO inhibitors



MAO inhibitors prolong and intensify anticholinergic effects of antihistamines101 102 b



Avoid use with or for 2 weeks after discontinuance of MAO inhibitors105



Test, antigen or histamine



Inhalation-challenge testing with histamine or antigen: Possible suppression of test response


Antigen skin testing: Possible suppression of wheal and flare reactions


Triprolidine Hydrochloride Pharmacokinetics


Absorption


Bioavailability


Rapidly absorbed.102


Therapeutic concentration achieved rapidly and usually maintained for 4–8 hours.102


Distribution


Extent


Distributed into milk.106 (See Lactation under Cautions.)


Elimination


Half-life


3–3.3 hours.101 102


Stability


Storage


Oral


Tablets

Tight, light-resistant containers at 15–30°C in a dry place.a


Solution

Tight, light-resistant containers at 15–30°C in a dry place;101 102 105 a do not freeze.a


ActionsActions



  • Blocks H1-receptor sites, thereby preventing the action of histamine on the cell.101 102 b




  • Suppresses flare and pruritus that accompany the endogenous release of histamine.b




  • Has anticholinergic and sedative effects.102




  • Antihistamines do not block the stimulating effect of histamine on gastric acid secretion, which is mediated by H2-receptors of the parietal cells.b



Advice to Patients



  • Risk of drowsiness; avoid alcohol and use caution when driving or operating machinery.102 105




  • When used for self-medication, discontinue therapy and consult a clinician if symptoms persist for >7 days or are accompanied by fever.105




  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.101 102 Importance of patients already receiving another CNS depressant (e.g., sedative, tranquilizer) not undertaking self-medication without first consulting a clinician.




  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.101 102




  • Importance of informing patients of other important precautionary information.101 102 (See Cautions.)



Preparations


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.


* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name













Triprolidine Hydrochloride

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



Solution



1.25 mg/5mL*



Zymine Liquid



Vindex


* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
















































Triprolidine and Pseudoephedrine Hydrochlorides

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



Solution



1.25 mg/5 mL Triprolidine Hydrochloride and Pseudoephedrine Hydrochloride 30 mg/5 mL*



Allerfrim Syrup



Rugby



Aprodine Syrup



Major



Triprolidine and Pseudoephedrine Hydrochlorides Solution



1.25 mg/5 mL Triprolidine Hydrochloride and Pseudoephedrine Hydrochloride 45 mg/5 mL*



Triprolidine and Pseudoephedrine Hydrochlorides Solution



Zymine-D Liquid



Vindex



Tablets



2.5 mg Triprolidine Hydrochloride and Pseudoephedrine Hydrochloride 60 mg*



Allerfrim



Rugby



Aprodine



major



Triprolidine and Pseudoephedrine Hydrochlorides Tablets



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions November 01, 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.




References



101. Vindex Pharmaceuticals, Inc. Zymine (triprolidine hydrochloride) liquid prescribing information. Memphis, TN; 2005 Jul.



102. Vindex Pharmaceuticals, Inc. Zymine-D (triprolidine hydrochloride and pseudoephedrine hydrochloride) liquid prescribing information. Memphis, TN; 2005 Jul.



103. Major Pharmaceuticals. Aprodine (triprolidine hydrochloride and pseudoephedrine hydrochloride ) syrup product information. Livonia, MI. From Major Pharmaceutical website (). Accessed 2008 Jan 31.



104. Major Pharmaceuticals. Aprodine (triprolidine hydrochloride and pseudoephedrine hydrochloride ) tablets product information. Livonia, MI. From Major Pharmaceutical website (). Accessed 2008 Jan 31.



105. Rugby. Allerfrim (triprolidine hydrochloride and pseudoephedrine hydrochloride) syrup product information. Duluth, GA; 2004 Jul.



106. Triprolidine. In: Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005:1639-40.



a. AHFS Drug Information 2008. McEvoy GK, ed. Triprolidine Hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2008:24.



b. AHFS Drug Information 2008. McEvoy GK, ed. Antihistamines General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2008:1-8.



More Triprolidine Hydrochloride resources


  • Triprolidine Hydrochloride Side Effects (in more detail)
  • Triprolidine Hydrochloride Use in Pregnancy & Breastfeeding
  • Triprolidine Hydrochloride Drug Interactions
  • Triprolidine Hydrochloride Support Group
  • 1 Review for Triprolidine Hydrochloride - Add your own review/rating


  • Triprolidine Professional Patient Advice (Wolters Kluwer)

  • Triprolidine Suspension MedFacts Consumer Leaflet (Wolters Kluwer)

  • triprolidine Concise Consumer Information (Cerner Multum)

  • Tripohist Prescribing Information (FDA)

  • Zymine Syrup MedFacts Consumer Leaflet (Wolters Kluwer)



Compare Triprolidine Hydrochloride with other medications


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  • Eye Redness/Itching
  • Hay Fever
  • Rhinorrhea

Monday, September 24, 2012

Loron 520





1. Name Of The Medicinal Product



Loron 520 mg Film-coated Tablets.


2. Qualitative And Quantitative Composition



Each tablet contains 520 mg clodronate disodium (as the tetrahydrate).



Excipients:



Each tablet contains:



• 4.875 mg lactose monohydrate



• 3.6 mmol (83.4 mg) sodium, as clodronate disodium, sodium starch glycolate and sodium citrate.



For a full list of excipients, see section 6.1.



3. Pharmaceutical Form



Film-coated tablets for oral administration.



4. Clinical Particulars



4.1 Therapeutic Indications



Loron is indicated for the management of osteolytic lesions, hypercalcaemia and bone pain associated with skeletal metastases in patients with carcinoma of the breast or multiple myeloma. Loron is also indicated for the maintenance of clinically acceptable serum calcium levels in patients with hypercalcaemia of malignancy initially treated with an intravenous infusion of clodronate disodium.



4.2 Posology And Method Of Administration



Adults



The recommended dose is 2 tablets (1040 mg clodronate disodium) daily. If necessary, the dosage may be increased but should not exceed a maximum of 4 tablets (2080 mg clodronate disodium) daily.



The tablets may be taken as a single dose or in two equally divided doses if necessary to improve gastrointestinal tolerance. Loron tablets should be swallowed with a little fluid, but not milk, at least one hour before or one hour after food.



The oral bioavailability of bisphosphonates is poor. Bioequivalence studies have shown appreciable differences in bioavailability between different oral formulations of clodronate disodium, as well as marked inter and intra patient variability. Dose adjustment may be required if the formulation is changed.



Elderly



No special dosage recommendations.



Children



Safety and efficacy in children has not been established.



Use in renal impairment



In patients with renal insufficiency with creatinine clearance between 10 and 30ml/min, the daily dose should be reduced to one half the recommended adult dose. Serum creatinine should be monitored during therapy. Clodronate disodium is contra-indicated in patients with creatinine clearance below 10ml/min.



4.3 Contraindications



Hypersensitivity to clodronate disodium or to any of the excipients. Acute, severe inflammatory conditions of the gastrointestinal tract. Pregnancy and lactation. Renal failure with creatinine clearance below 10ml/min, except for short term use in the presence of purely functional renal insufficiency caused by elevated serum calcium levels. Concomitant use of other bisphosphonates.



4.4 Special Warnings And Precautions For Use



No information is available on the potential carcinogenicity of clodronate disodium, but patients have been treated in clinical trials for up to 2 years. The duration of the treatment is therefore at the discretion of the physician, according to the status of the underlying malignancy.



It is recommended that appropriate monitoring of renal function with serum creatinine be carried out during treatment. Serum calcium and phosphate should be monitored periodically. Monitoring of liver enzymes and white cells is advised (see side effects).



Osteonecrosis of the jaw, generally associated with tooth extraction and/or local infection (including osteomyelitis) has been reported in patients with cancer receiving treatment regimens including primarily intravenously administered bisphosphonates. Many of these patients were also receiving chemotherapy and corticosteroids. Osteonecrosis of the jaw has also been reported in patients with osteoporosis receiving oral bisphosphonates.



A dental examination with appropriate preventive dentistry should be considered prior to treatment with bisphosphonates in patients with concomitant risk factors (e.g. cancer, chemotherapy, radiotherapy, corticosteroids, poor oral hygiene).



While on treatment, these patients should avoid invasive dental procedures if possible. For patients who develop osteonecrosis of the jaw while on bisphosphonate therapy, dental surgery may exacerbate the condition. For patients requiring dental procedures, there are no data available to suggest whether discontinuation of bisphosphonate treatment reduces the risk of osteonecrosis of the jaw. Clinical judgement of the treating physician should guide the management plan of each patient based on individual benefit/risk assessment.



Orally administered, mainly nitrogen-containing, bisphosphonates may cause local irritation of the upper gastrointestinal mucosa. Because of these possible irritant effects and a potential for worsening of the underlying disease, caution should be used when clodronate disodium is given to patients with active upper gastrointestinal problems (e.g. known Barrett's oesophagus, dysphagia, other oesophageal diseases, gastritis, duodenitis or ulcers).



Adverse experiences such as oesophagitis, oesophageal ulcers and oesophageal erosions, in some cases severe and requiring hospitalisation, rarely with bleeding or followed by oesophageal stricture or perforation, have been reported in patients receiving treatment with oral bisphosphonates. The risk of severe oesophageal adverse experiences appears to be greater in patients who do not comply with the dosing instruction and/or who continue to take oral bisphosphonates after developing symptoms suggestive of oesophageal irritation. Patients should pay particular attention and be able to comply with the dosing.



Physicians should be alert to any signs or symptoms signaling a possible oesophageal reaction and patients should be instructed to discontinue clodronate disodium and seek medical attention if they develop dysphagia, odynophagia, retrosternal pain or new or worsening heartburn.



While no increased risk was observed in controlled clinical trials there have been post-marketing reports of gastric and duodenal ulcers with oral bisphosphonate use, some severe and with complications.



Owing to the presence of lactose monohydrate, patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.



4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction



No other bisphosphonate drugs should be given with Loron tablets.



The calcium-lowering action of clodronate disodium can be potentiated by the administration of aminoglycosides either concomitantly or one to several weeks apart. Severe hypocalcaemia has been observed in some cases. Hypomagnesaemia may also occur simultaneously. Patients receiving NSAID's in addition to clodronate disodium have developed renal dysfunction. However, a synergistic action has not been established. There is no evidence from clinical experience that clodronate disodium interacts with other medication, such as steroids, diuretics, calcitonin, non NSAID analgesics, or chemotherapeutic agents. Calcium rich foods, mineral supplements and antacids may impair absorption.



4.6 Pregnancy And Lactation



There are insufficient data either from animal studies or from experience in humans of the effects of clodronate disodium on the embryo and foetus. No studies have been conducted on excretion in breast milk. Consequently, clodronate disodium is contraindicated in pregnancy and lactation.



4.7 Effects On Ability To Drive And Use Machines



Clodronate disodium has no influence on the ability to drive and use machines.



4.8 Undesirable Effects



Adverse reactions are ranked under heading of frequency, the most frequent first, using the following convention:



Very common (



Common (



Uncommon (



Rare (



Very rare (<1/10,000)



Immune system disorders:



Rare:



Allergic reaction



Very rare:



Bronchoconstriction



Metabolic and nutritional disorders:



Rare:



Hypocalcaemia



Gastrointestinal disorders:



Common:



Nausea and diarrhoea (especially at beginning of treatment and at higher doses)



Renal and urinary disorders:



Rare:



Deterioration of renal function



Transient proteinuria immediately after intravenous infusion



Very rare:



Acute renal failure has been reported after intravenous injection



Investigations:



Very rare:



Decreased serum phosphate



Increased serum alkaline phosphatase



Increased serum lactate dehydrogenase



Increased serum parathormone



Increased serum transaminases



4.9 Overdose



Symptoms and signs: There is no experience of acute overdosage in humans. The development of hypocalcaemia is possible for up to 2 or 3 days following the overdosage.



Treatment: Serum calcium should be monitored and oral or parenteral calcium supplementation may be required. Acute overdosage may be associated with gastrointestinal symptoms such as nausea and vomiting. Treatment should be symptomatic.



5. Pharmacological Properties



5.1 Pharmacodynamic Properties



Pharmacotherapeutic group: Bisphosphonates, ATC code: M05BA02.



Clodronate disodium is a bisphosphonate which has a high affinity to bone. It is mainly the portion of the dose adsorbed to bone which is pharmacologically active. The pharmacological effect of clodronate disodium is to suppress osteoclast mediated bone resorption as judged by bone histology and decreases in serum calcium, urine calcium and urinary excretion of hydroxyproline, without adversely affecting mineralisation.



5.2 Pharmacokinetic Properties



Oral bioavailability is in the order of 2%.



Clodronate disodium is not metabolised. The volume of distribution is approximately 0.3L/kg. Elimination from serum is rapid, 75% of the dose is recovered unchanged in urine within 24 hours.



The elimination kinetics best fit a 3 compartment model. The first two compartments have relatively short half-lives. The third compartment is probably the skeleton. Elimination half life is approximately 12 - 13 hours.



5.3 Preclinical Safety Data



Clodronate disodium shows relatively little toxicity either on single oral administration or after daily oral administration for a period of up to 6 months. In rats, a dose of 200mg/kg/day in the chronic toxicity test is at the limit of tolerability. In dogs, 40mg/kg/day chronically is within the tolerated range.



On daily administration of 500mg/kg for 6 weeks to rats, signs of renal failure with a clear rise in BUN, and initial liver parenchymal reaction with rises of SGOT, SGPT and AP occurred. No significant haematological changes were found in the toxicological investigations.



Investigations for mutagenic properties did not show any indication of mutagenic potency.



Reproduction toxicology investigations did not provide any indication of peri and post natal disorders, teratogenic damage or disorders of fertility.



It is not known if clodronate disodium passes into the mother's milk or through the placenta.



6. Pharmaceutical Particulars



6.1 List Of Excipients



Tablet Core



Talc



Maize starch



Cellulose microcrystalline



Magnesium stearate



Sodium starch glycolate



Film Coat



Hypromellose



Polyacrylate dispersion 30%



Macrogol 10000



Lactose monohydrate



Talc



Titanium dioxide (E171)



Polysorbate 80



Sodium citrate



6.2 Incompatibilities



Not applicable.



6.3 Shelf Life



5 years.



6.4 Special Precautions For Storage



This medicinal product does not require any special storage conditions.



6.5 Nature And Contents Of Container



PVC/aluminium blister packs containing 10 or 60 tablets.



Not all pack sizes may be marketed.



6.6 Special Precautions For Disposal And Other Handling



No special requirements.



7. Marketing Authorisation Holder



Roche Products Limited



6 Falcon Way



Shire Park



Welwyn Garden City



AL7 1TW, United Kingdom



8. Marketing Authorisation Number(S)



PL 00031/0521



9. Date Of First Authorisation/Renewal Of The Authorisation









 
 


Date of first authorisation:




1 July 1999




Date of last renewal:




11 November 2003



10. Date Of Revision Of The Text



19 October 2011



11 LEGAL CATEGORY


POM



Loron is a registered trade mark




Sunday, September 23, 2012

Xolegel Gel


Pronunciation: KEE-toe-KON-a-zole
Generic Name: Ketoconazole
Brand Name: Xolegel


Xolegel Gel is used for:

Treating a skin condition called seborrheic dermatitis.


Xolegel Gel is an antifungal agent. It works by killing the fungus causing the skin condition.


Do NOT use Xolegel Gel if:


  • you are allergic to any ingredient in Xolegel Gel

Contact your doctor or health care provider right away if any of these apply to you.



Before using Xolegel Gel:


Some medical conditions may interact with Xolegel Gel. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


  • if you are pregnant, planning to become pregnant, or are breast-feeding

  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

  • if you have allergies to medicines, foods, or other substances

  • if you have a weakened immune system, liver problems, or the blood disease porphyria

Some MEDICINES MAY INTERACT with Xolegel Gel. Because little, if any, of Xolegel Gel is absorbed into the blood, the risk of it interacting with another medicine is low.


Ask your health care provider if Xolegel Gel may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.


How to use Xolegel Gel:


Use Xolegel Gel as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • An extra patient leaflet is available with Xolegel Gel. Talk to your pharmacist if you have questions about this information.

  • Wash your hands before and immediately after using Xolegel Gel.

  • Spread a thin layer of Xolegel Gel onto the affected area with the tips of your fingers. Gently rub it in. Be sure to cover the entire affected area and the healthy skin around it.

  • Do not touch your eyes or nose while you are applying Xolegel Gel.

  • Wait for at least 20 minutes after you apply Xolegel Gel before you apply makeup or sunscreen.

  • Do not wash the area where you applied Xolegel Gel for at least 3 hours after you apply it.

  • If you miss a dose of Xolegel Gel, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Xolegel Gel.



Important safety information:


  • Xolegel Gel is for external use only. Do not get it in your eyes, nose, or mouth. If you get it in your eyes, rinse at once with cool tap water. Do not get Xolegel Gel in your vagina.

  • Do not use Xolegel Gel for other skin conditions at a later time.

  • Xolegel Gel is flammable. Do not store or use near an open flame. Do not smoke during or right after use of Xolegel Gel.

  • Xolegel Gel should be used with extreme caution in CHILDREN younger than 12 years old; safety and effectiveness in these children have not been confirmed.

  • PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Xolegel Gel while you are pregnant. It is not known if Xolegel Gel is found in breast milk after topical use. If you are or will be breast-feeding while you use Xolegel Gel, check with your doctor. Discuss any possible risks to your baby.


Possible side effects of Xolegel Gel:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:



Mild burning at the application site.



Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blisters, irritation, pain, redness, or severe burning at the application site.



This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


See also: Xolegel side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.


Proper storage of Xolegel Gel:

Store Xolegel Gel at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do NOT store near an open flame. Keep Xolegel Gel out of the reach of children and away from pets.


General information:


  • If you have any questions about Xolegel Gel, please talk with your doctor, pharmacist, or other health care provider.

  • Xolegel Gel is to be used only by the patient for whom it is prescribed. Do not share it with other people.

  • If your symptoms do not improve or if they become worse, check with your doctor.

  • Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Xolegel Gel. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Xolegel resources


  • Xolegel Side Effects (in more detail)
  • Xolegel Use in Pregnancy & Breastfeeding
  • Xolegel Support Group
  • 3 Reviews for Xolegel - Add your own review/rating


Compare Xolegel with other medications


  • Cutaneous Candidiasis
  • Dandruff
  • Seborrheic Dermatitis
  • Tinea Corporis
  • Tinea Cruris
  • Tinea Pedis
  • Tinea Versicolor

Saturday, September 22, 2012

Cubicin


Generic Name: Daptomycin
Class: Cyclic Lipopeptides
VA Class: AM900
Chemical Name: N - Decanoyl - l - tryptophyl - l - asparaginyl - l - aspartyl - l - threonylglycyl - l - ornithyl - l - aspartyl - d - alanyl - l - aspartylglycyl - d - seryl - threo - 3 - methyl - l - glutamyl - 3 - anthraniloyl - l - alanine ε1-lactone
Molecular Formula: C72H101N17O26
CAS Number: 103060-53-3

Introduction

Antibacterial; cyclic lipopeptide antibiotic.1 3 5


Uses for Cubicin


Skin and Skin Structure Infections


Treatment of complicated skin and skin structure infections caused by susceptible Staphylococcus aureus (including methicillin-resistant S. aureus [MRSA; also known as oxacillin-resistant S. aureus or ORSA]), Streptococcus pyogenes (group A β-hemolytic streptococci), S. agalactiae (group B streptococci), S. dysgalactiae subsp. equisimilis, and Enterococcus faecalis (vancomycin-susceptible strains only).1


Concomitant use of another anti-infective may be indicated if documented or presumptive pathogens also include gram-negative or anaerobic bacteria.1


Bacteremia


Treatment of bacteremia (blood stream infection) caused by susceptible S. aureus (including MRSA).1


May be used for treatment of S. aureus bacteremia in patients with right-sided infective endocarditis.1 Efficacy not established in patients with left-sided infective endocarditis caused by S. aureus;1 limited data suggest a poor outcome in such patients despite daptomycin treatment.1


Concomitant use of another anti-infective may be indicated if documented or presumptive pathogens also include gram-negative or anaerobic bacteria.1


Persisting or relapsing S. aureus infection has been reported in some patients.1 (See Persisting or Relapsing Staphylococcus aureus Infection under Cautions.)


Has not been studied in patients with prosthetic valve endocarditis or meningitis.1


Cubicin Dosage and Administration


Administration


IV Infusion


Administer by IV infusion.1


Lyophilized powder for infusion must be reconstituted and diluted prior to administration.1


Vials are for single use only.1


Additives and other drugs should not be added to daptomycin solutions or infused simultaneously through the same IV line.1 If the same IV line is used for sequential infusion of different drugs, the line should be flushed with a compatible infusion solution (see Compatibility under Stability) before and after infusion of daptomycin.1


Do not use in conjunction with ReadyMed elastomeric infusion pumps; stability studies identified an impurity (i.e., 2-mercaptobenzothiazole) leaching from this pump system into the daptomycin solution.1


Reconstitution and Dilution

Reconstitute powder for infusion by adding 10 mL of 0.9% sodium chloride injection to vial containing 500 mg of daptomycin.1


Gently rotate vial to ensure that entire product is wetted.1 Allow vial to remain undisturbed for 10 minutes, then rotate or swirl for a few minutes (as needed) to obtain a completely reconstituted solution.1 To minimize foaming, avoid agitating or vigorously shaking vial during or after reconstitution.1


Reconstituted solution should be further diluted with 0.9% sodium chloride injection1 to a final concentration of ≤20 mg/mL.6


Use strict aseptic technique when preparing daptomycin solutions since the drug contains no preservatives.1


Rate of Administration

IV infusions are given over 30 minutes.1


Dosage


Adults


Skin and Skin Structure Infections

Complicated Infections

IV

4 mg/kg once every 24 hours for 7–14 days.1


Do not administer more frequently than once daily.1 (See Musculoskeletal Effects under Cautions.)


Bacteremia

IV

6 mg/kg once every 24 hours for at least 2–6 weeks.1 Base duration of treatment on clinical diagnosis.1 Limited safety data regarding use beyond 28 days; however, some patients in a clinical study received daptomycin for >6 weeks.1


Do not administer more frequently than once daily.1 (See Musculoskeletal Effects under Cautions.)


Special Populations


Hepatic Impairment


Dosage adjustment not necessary in adults with mild to moderate hepatic impairment;1 pharmacokinetics not evaluated in adults with severe hepatic impairment.1


Renal Impairment


Reduce dosage in adults with Clcr <30 mL/minute and in those undergoing hemodialysis or CAPD.1


For treatment of complicated skin and skin structure infections in adults with Clcr <30 mL/minute, reduce dosage to 4 mg/kg IV once every 48 hours.1


For treatment of bacteremia in adults with Clcr <30 mL/minute, reduce dosage to 6 mg/kg IV once every 48 hours.1


In hemodialysis patients, give dose on hemodialysis days following the procedure, if possible.1


Geriatric Patients


No dosage adjustments except those related to renal impairment.1 (See Renal Impairment under Dosage and Administration.)


Obese Patients


Dosage adjustment not warranted.1


Cautions for Cubicin


Contraindications



  • Known hypersensitivity to daptomycin.1



Warnings/Precautions


Warnings


Eosinophilic Pneumonia

Eosinophilic pneumonia reported in some patients receiving daptomycin.1 7 8 9 10 11 12 Patients generally developed fever, dyspnea with hypoxic respiratory insufficiency, and diffuse pulmonary infiltrates 2–4 weeks after the drug was initiated.1 7 8 9 10 11 12 Improvement or resolution of symptoms generally occurred when daptomycin was discontinued;1 7 8 9 10 11 12 most patient received treatment with systemic corticosteroids.1 7 8 9 10 11 12 Reinitiation of daptomycin has resulted in recurrence of eosinophilic pneumonia.1 7 8 11


FDA determined that there appears to be a temporal association between daptomycin and development of eosinophilic pneumonia.7 To date, there have been 7 probable and 36 possible cases of eosinophilic pneumonia reported in patients receiving daptomycin;7 some were receiving the drug for uses not approved by FDA.7 8 9 Consider that eosinophilic pneumonia can progress to respiratory failure and is potentially fatal if not quickly recognized and appropriately managed.7 8 9 11


Closely monitor for signs and symptoms of eosinophilic pneumonia (e.g., new onset or worsening fever, dyspnea, difficulty breathing, new pulmonary infiltrates).1 7 8 9 10 11 12


Immediately discontinue daptomycin if there are any signs or symptoms of eosinophilic pneumonia.1 7 8 9 10 11 12 Initiate prompt medical evaluation;1 7 8 9 10 11 12 treatment with systemic corticosteroids is recommended.1 8 9 10 11 12


Superinfection/Clostridium difficile-associated Colitis

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.1 Careful observation of the patient is essential.1 Institute appropriate therapy if superinfection occurs.1


Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile.1 13 14 15 16 C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) has been reported with nearly all anti-infectives, including daptomycin, and may range in severity from mild diarrhea to fatal colitis.1 Hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.1


Consider CDAD if diarrhea develops during or after therapy and manage accordingly.1 13 14 15 16 Obtain a careful medical history since CDAD may occur as late as 2 months or longer after anti-infective therapy is discontinued.1


If CDAD is suspected or confirmed, anti-infectives not directed against C. difficile should be discontinued.1 Manage moderate to severe cases with fluid, electrolyte, and protein supplementation, anti-infective therapy active against C. difficile (e.g., oral metronidazole or vancomycin), and surgical evaluation when clinically indicated.1 13 14 15 16


General Precautions


Persisting or Relapsing Staphylococcus aureus Infection

Treatment failure due to persisting or relapsing S. aureus infection has occurred in patients receiving daptomycin;1 fatalities reported.1 S. aureus isolates with reduced susceptibility or resistance to daptomycin have been reported and have emerged during therapy with the drug.1 19 20 21


In a clinical study in patients with bacteremia, 15.8% of daptomycin-treated patients and 9.6% of patients receiving a comparator anti-infective (vancomycin or a penicillinase-resistant penicillin) had persisting or relapsing S. aureus infections;1 some fatalities occurred.1 In vitro studies indicated isolates from some of these patients developed reduced susceptibility to the anti-infective during or following treatment.1 Most patients with persisting or relapsing infections had deep-seated infections and did not receive necessary surgical intervention.1


Perform repeat blood cultures in patients with persisting or relapsing infection or with poor clinical outcomes.1 If cultures are positive for S. aureus, perform in vitro susceptibility testing using standardized MIC procedures.1 Also perform diagnostic evaluation to rule out sequestered foci of infection.1 Surgical intervention (e.g., debridement, removal of prosthetic devices, valve replacement surgery) and/or a change in anti-infective regimen may be required.1


Musculoskeletal Effects

Increases in serum CK concentrations have been reported in patients receiving daptomycin.1 Occurs more frequently if the drug is given more frequently than once daily.1


Monitor for development of muscle pain or weakness, particularly of distal extremities.1 Determine serum CK concentrations weekly during daptomycin treatment;1 more frequent determinations are indicated in those who develop unexplained increases in serum CK concentrations and in those previously or concomitantly treated with an HMG-CoA reductase inhibitor (statin).1 In those with renal impairment, monitor serum CK concentrations and renal function more frequently.1


Discontinue daptomycin in patients with unexplained signs or symptoms of myopathy in conjunction with increases in CK >1000 U/L (i.e., approximately 5 times the ULN) or in patients without reported symptoms who have substantial increases in serum CK concentrations (i.e., >2000 U/L [≥10 times the ULN]).1


Consider temporarily discontinuing drugs associated with rhabdomyolysis (e.g., HMG-CoA reductase inhibitors) during daptomycin treatment.1 (See Specific Drugs under Drug Interactions.)


Nervous System Effects

Decreases in nerve conduction velocity and adverse effects (e.g., paresthesia, Bell’s palsy) possibly suggestive of peripheral or cranial neuropathy reported rarely.1


Be alert to possible manifestations of neuropathy.1


Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of daptomycin and other antibacterials, use only for treatment of infections proven or strongly suspected to be caused by susceptible bacteria.1


When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.1 In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.1


If documented or presumed pathogens include gram-negative or anaerobic bacteria, concomitant use of an anti-infective active against such bacteria may be indicated.1 (See Uses.)


Do not use for treatment of pneumonia.1


Safety and efficacy not studied in patients with prosthetic valve endocarditis or meningitis.1


Specific Populations


Pregnancy

Category B.


Lactation

Not known whether distributed into milk.1 Use with caution.1


Pediatric Use

Safety and efficacy not established in children <18 years of age.1


Geriatric Use

In clinical studies, success rates were lower and incidence of treatment-emergent adverse effects were higher in patients ≥65 years of age compared with younger adults.1


Consider age-related decreases in renal function when selecting dosage and adjust dosage if necessary.1 (See Renal Impairment under Dosage and Administration.)


Hepatic Impairment

Pharmacokinetics not altered in patients with moderate hepatic impairment (Child-Pugh class B);1 not studied in patients with severe hepatic impairment.1


Renal Impairment

Clearance decreased; AUC and half-life increased in patients with renal impairment.1


Monitor renal function and serum CK concentrations more frequently in patients with renal insufficiency.1


Dosage adjustment necessary in patients with Clcr <30 mL/minute.1 (See Renal Impairment under Dosage and Administration.)


Common Adverse Effects


Patients treated for complicated skin and skin structure infections: GI effects (constipation, nausea, diarrhea, vomiting), injection site reactions, nervous system effects (headache, insomnia, dizziness), rash, pruritus, abnormal liver function test results, CK elevations, infections (fungal, urinary tract), hypotension, renal failure, anemia, dyspnea, fever.1


Patients treated for bacteremia: GI effects (diarrhea, vomiting, constipation, nausea, dyspepsia, loose stools, abdominal pain), musculoskeletal and connective tissue disorders (pain in extremity, back pain), nervous system effects (headache, dizziness, insomnia, anxiety), respiratory disorders (pharyngolaryngeal pain, pleural effusion), infections (urinary tract, osteomyelitis, sepsis, bacteremia), peripheral edema, pyrexia, chest pain, edema, asthenia, rash, pruritus, erythema, increased sweating, CK elevations, hypertension, hyperkalemia, hypokalemia, anemia, hypotension.1


Interactions for Cubicin


Does not inhibit or induce CYP isoenzymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, or 3A4; pharmacokinetic interactions with drugs metabolized by these CYP isoenzymes unlikely.1


Specific Drugs and Laboratory Tests



























Drug



Interaction



Comments



Aminoglycosides



Tobramycin: Increased daptomycin plasma concentrations and AUC and decreased tobramycin plasma concentrations and AUC1


In vitro evidence of synergistic antibacterial effects against staphylococci and enterococci1 17 in studies using gentamicin and tobramycin;17 additive or indifferent antibacterial effects also reported, but antagonism did not occur17



Tobramycin: Clinical importance of pharmacokinetic interaction unclear; use concomitantly with caution1



β-Lactam anti-infectives



Aztreonam: Clinically important pharmacokinetic interactions unlikely1 6


In vitro evidence of synergistic antibacterial effects against staphylococci and enterococci1 17 in studies using penicillins (ampicillin, oxacillin, ampicillin and sulbactam, piperacillin and tazobactam, ticarcillin and clavulanate), cephalosporins (cefepime, ceftriaxone), aztreonam, or imipenem;17 additive or indifferent antibacterial effects also reported, but antagonism generally did not occur17



Aztreonam: Dosage adjustment not necessary if used concomitantly1



HMG-CoA reductase inhibitors (statins)



Potential pharmacologic interaction (risk of myopathy manifested as muscle pain or weakness in association with increased serum CK concentrations);1 increased serum CK concentrations reported in some patients previously or concomitantly treated with an HMG-CoA reductase inhibitor1


Simvastatin: No evidence of increased adverse effects when used concomitantly with daptomycin in healthy adults1



Experience with concurrent use is limited; consider temporarily discontinuing HMG-CoA reductase inhibitor during daptomycin treatment1



Probenecid



Clinically important pharmacokinetic interactions unlikely1 6



Dosage adjustment not necessary1



Rifampin



In vitro evidence of synergistic antibacterial effects against staphylococci and enterococci, including some vancomycin-resistant enterococci;1 17 additive or indifferent antibacterial effects also reported, but antagonism did not occur17



Tests, coagulation



Daptomycin causes concentration-dependent false prolongation of PT and elevated INR if certain recombinant thromboplastin reagents are used for these tests1



Interference with PT/INR may be minimized by drawing blood samples for coagulation tests near the time of daptomycin trough plasma concentrations; consider that trough plasma concentrations may still be high enough to interfere with these tests1


If abnormally elevated PT/INR results are reported in a patient receiving daptomycin, repeat coagulation testing using blood specimens drawn just prior to the next daptomycin dose (i.e., at trough concentrations);1 if results remain substantially elevated over what would otherwise be expected, consider alternative methods of measuring PT/INR and evaluate patient for other causes of abnormally elevated PT/INR1



Warfarin



No evidence of pharmacologic or pharmacokinetic interaction1



Experience with concurrent use is limited; closely monitor anticoagulant activity during the first several days if daptomycin is initiated in patients receiving warfarin 1


Cubicin Pharmacokinetics


Absorption


Bioavailability


Generally exhibits linear and time-independent pharmacokinetics at a dosage of 4–12 mg/kg IV once every 24 hours.1


Steady-state trough serum concentrations are achieved by the third daily dose.1


Distribution


Plasma Protein Binding


90–93% bound to plasma proteins, principally albumin.1


Elimination


Metabolism


In vitro studies indicate daptomycin is not metabolized by CYP isoenzymes.1 Inactive metabolites have been detected in urine; site and extent of metabolism have not been identified.1


Elimination Route


Eliminated principally by renal excretion; approximately 78 and 6% of a dose recovered in urine and feces, respectively.1


Half-life


Mean elimination half-life at steady state is 7.7–8.3 hours in adults.1


Special Populations


In geriatric adults ≥75 years of age, clearance is reduced approximately 35% and AUC is increased approximately 58% compared with younger adults (18–30 years of age).1


Pharmacokinetics not altered in adults with moderate hepatic impairment (Child-Pugh class B); pharmacokinetics not studied in adults with severe hepatic impairment.1


Clearance is decreased and AUC and half-life increased in adults with renal impairment compared with adults with normal renal function.1 Mean half-life is 10.75 hours in those with mild renal impairment (Clcr 50–80 mL/minute), 14.7 hours in those with moderate renal impairment (Clcr 30 to <50 mL/minute), or 27.83 hours in those with severe renal impairment (Clcr <30 mL/minute).1


In obese adults, plasma clearance of daptomycin normalized to total body weight is approximately 15% lower in those who are moderately obese and 23% lower in those who are extremely obese compared with nonobese adults.1 This difference is most likely the result of differences in renal clearance of daptomycin.1


Stability


Storage


Parenteral


Powder for Injection

2–8°C.1 Avoid excessive heat.1


Following reconstitution, stable in original vial for up to 12 hours at room temperature or up to 48 hours at 2–8°C.1 After further dilution, stable in infusion bag for 12 hours at room temperature or 48 hours when refrigerated.1 Combined storage time (vial and infusion bag) should be ≤12 hours at room temperature or ≤48 hours when refrigerated.1


Compatibility


For information on systemic interactions resulting from concomitant use, see Interactions.


Parenteral


Solution Compatibility

Not compatible with dextrose-containing solutions.1






Compatible



Ringer's injection, lactated1



Sodium chloride 0.9%1


ActionsActions and Spectrum



  • Lipopeptide antibiotic.1 3 5




  • Usually bactericidal in action.1 5 19




  • Binds to cell membranes in susceptible bacteria and causes rapid membrane depolarization leading to inhibition of protein, DNA, and RNA synthesis and cell death.1 5




  • Spectrum of activity includes many gram-positive bacteria;1 inactive against gram-negative bacteria.6




  • Gram-positive aerobes: Active in vitro and in clinical infections against Staphylococcus aureus (including methicillin-resistant S. aureus [MRSA; also known as oxacillin-resistant S. aureus or ORSA]),1 18 19 Streptococcus pyogenes (group A β-hemolytic streptococci),1 S. agalactiae (group B streptococci),1 S. dysgalactiae subsp. equisimilis,1 and Enterococcus faecalis (vancomycin-susceptible strains only).1 Also active in vitro against some strains of Corynebacterium jeikeium,1 E. faecalis (vancomycin-resistant strains),1 E. faecium (including vancomycin-resistant strains),1 S. epidermidis (including oxacillin-resistant strains),1 and S. haemolyticus.1




  • Reduced susceptibility to daptomycin has been produced in vitro by serial passage of S. aureus in the presence of increasing concentrations of the drug.2 In addition, daptomycin-resistant S. aureus strains have emerged in patients treated with the drug.1 20 21 Mechanism of resistance or transferable elements that might confer resistance to daptomycin not identified to date.1 19 21




  • Cross-resistance between daptomycin and other anti-infectives not clearly identified to date.1 2 Although further study is needed, there is some evidence that some strains of MRSA that develop resistance to daptomycin also may develop resistance or reduced susceptibility to vancomycin20 21 and that daptomycin-resistant MRSA may emerge during daptomycin therapy in some patients with prior exposure to vancomycin.20



Advice to Patients



  • Importance of patients immediately informing clinicians if they develop new or worsening fever, cough, shortness of breath, or difficulty breathing.7




  • Importance of contacting a clinician if muscle pain or weakness, particularly of the extremities, occurs.1




  • Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued.1 Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.1




  • Importance of reporting persistent or worsening symptoms of infection.6




  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1




  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1




  • Importance of informing patients of other important precautionary information. (See Cautions.)



Preparations


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.













Daptomycin

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Parenteral



For injection, for IV infusion



500 mg



Cubicin



Cubist



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions December 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.




References



1. Cubist Pharmaceuticals. Cubicin (daptomycin for injection) prescribing information. Lexington, MA; 2003 Sep.



2. Silverman JA, Oliver N, Andrew T. Resistance studies with daptomycin. Antimicrob Agents Chemother. 2001; 45:1799-1802. [PubMed 11353628]



3. Tally FP, DeBruin MF. Development of daptomycin for gram-positive infections. J Antimicrob Chemother. 2000; 46:523-6. [IDIS 454808] [PubMed 11020247]



4. Wise R, Gee T, Andrews JM et al. Pharmacokinetics and inflammatory fluid penetration of intravenous daptomycin in volunteers. Antimicrob Agents Chemother. 2002; 46:31-3. [IDIS 474163] [PubMed 11751107]



5. Silverman JA, Pelmutter NG, Shaprio HM. Correlation of daptomycin bactericidal activity and membrane depolarization in Staphylococcus aureus. Antimicrob Agents Chemother. 2003; 47:2538-44. [PubMed 12878516]



6. Cubist Pharmaceuticals, Lexington, MA: Personal communication.



7. US Food and Drug Administration. FDA Drug Safety Communication: Eosinophilic pneumonia associated with the use of Cubicin (daptomycin). 2010 Jul 29. From FDA website.



8. Miller BA, Gray A, Leblanc TW et al. Acute eosinophilic pneumonia secondary to daptomycin: a report of three cases. Clin Infect Dis. 2010; 50:e63-8. [PubMed 20420515]



9. Lal Y, Assimacopoulos AP. Two cases of daptomycin-induced eosinophilic pneumonia and chronic pneumonitis. Clin Infect Dis. 2010; 50:737-40. [PubMed 20121418]



10. Shinde A, Seifi A, DelRe S et al. Daptomycin-induced pulmonary infiltrates with eosinophilia. J Infect. 2009; 58:173-4. [PubMed 19046602]



11. Hayes D, Anstead MI, Kuhn RJ. Eosinophilic pneumonia induced by daptomycin. J Infect. 2007; 54:e211-3. [PubMed 17207858]



12. Kakish E, Wiesner AM, Winstead PS et al. Acute respiratory failure due to daptomycin induced eosinophilic pneumonia. Respir Med CME. 2008; 1:235–7.



13. Johnson S, Gerding DN. Clostridium difficile-associated diarrhea. Clin Infect Dis. 1998; 26:1027-36. [IDIS 407733] [PubMed 9597221]



14. Fekety R for the American College of Gastroenterology Practice Parameters Committee. Guidelines for the diagnosis and management of Clostridium difficile-associated diarrhea and colitis. Am J Gastroenterol. 1997; 92:739-50. [IDIS 386628] [PubMed 9149180]



15. American Society of Health-System Pharmacists Commission on Therapeutics. ASHP therapeutic position statement on the preferential use of metronidazole for the treatment of Clostridium difficile-associated disease. Am J Health-Syst Pharm. 1998; 55:1407-11. [IDIS 407213] [PubMed 9659970]



16. Wilcox MH. Treatment of Clostridium difficile infection. J Antimicrob Chemother. 1998; 41(Suppl C):41-6. [IDIS 407246] [PubMed 9630373]



17. Steenbergen JN, Mohr JF, Thorne GM. Effects of daptomycin in combination with other antimicrobial agents: a review of in vitro and animal model studies. J Antimicrob Chemother. 2009; 64:1130-8. [PubMed 19825818]



18. Mendes RE, Moet GJ, Janechek MJ et al. In Vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates. Antimicrob Agents Chemother. 2010; 54:2704-6. [PubMed 20385851]



19. Sader HS, Becker HK, Moet GJ et al. Antimicrobial activity of daptomycin tested against Staphylococcus aureus with vancomycin MIC of 2 microg/mL isolated in the United States and European hospitals (2006-2008). Diagn Microbiol Infect Dis. 2010; 66:329-31. [PubMed 20159377]



20. Hsu LY, Leong M, Balm M et al. Six cases of daptomycin non-susceptible Staphylococcus aureus bacteremia in Singapore. J Med Microbiol. 2010; :. [PubMed 20705729]



21. Lee CH, Wang MC, Huang IW et al. Development of Daptomycin Nonsusceptibility with Heterogeneous Vancomycin-Intermediate Resistance and Oxacillin Susceptibility in Methicillin-Resistant Staphylococcus aureus during High-Dose Daptomycin Treatment. Antimicrob Agents Chemother. 2010; 54:4038-40. [PubMed 20585116]



More Cubicin resources


  • Cubicin Side Effects (in more detail)
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  • Cubicin Support Group
  • 0 Reviews for Cubicin - Add your own review/rating


  • Cubicin Prescribing Information (FDA)

  • Cubicin Consumer Overview

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  • Bacteremia
  • Endocarditis
  • Methicillin-Resistant Staphylococcus Aureus Infection
  • Skin and Structure Infection
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