Share on Facebook Share on Twitter Email
Answers.com

Cilostazol

 
Drug Info: Cilostazol

Brand names: Pletal®

Chemical formula:



Cilostazol tablets

What are cilostazol tablets?

CILOSTAZOL (Pletal®) is a medication that reduces the symptoms of intermittent claudication. This condition causes pain in the legs during walking, and goes away with rest. Cilostazol helps blood flow more smoothly through the blood vessels; this action improves oxygen flow to the tissues of the body. By improving blood flow, cilostazol helps people with claudication walk longer distances without pain. In some cases cilostazol may be prescribed for other health conditions where improved blood flow through the blood vessels is needed. Generic cilostazol tablets are available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of the following conditions:
• angina
• bleeding disorder or hemophilia
• diabetes
• headaches
• history of heart failure, heart attack, or other heart disease
• low blood pressure
• an unusual or allergic reaction to cilostazol, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take cilostazol tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with plenty of water (at least a full glass) to avoid stomach upset. Take on an empty stomach, at least ½ hour before or 2 hours after a meal. Take your doses at regular intervals. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What drug(s) may interact with cilostazol?

• agents that prevent or treat blood clots (such as enoxaparin or warfarin)
• antiinflammatory drugs (NSAIDs, such as ibuprofen, naproxen, or ketoprofen)
• aspirin
• cimetidine (do not purchase non-prescription without prescriber advice)
clopidogrel
diltiazem
• erythromycin or clarithromycin
• fish oil (omega-3 fatty acids) supplements
• herbal medicines or dietary supplements like feverfew, garlic pills, ginger, gingko biloba, or horse chestnut
• grapefruit juice
omeprazole
pentoxifylline
• some medications for treating depression (examples: fluoxetine, fluvoxamine, nefazodone)
• some medications for treating fungal infections (examples: ketoconazole, fluconazole, itraconazole)
ticlopidine

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking cilostazol?

After you start to take cilostazol, it may take 2—4 weeks for you to notice improvement in your condition. In some people, it can take as long as 3 months for claudication (leg pain) to improve.

Visit your prescriber or health care professional for regular checks on your progress. Do not stop taking cilostazol except on your prescriber's advice. If you notice any unusual symptoms or side effects, contact your prescriber.

You may get dizzy, especially when you sit or stand up quickly. Do not drive, use machinery or do anything that needs mental alertness until you know how cilostazol affects you. To reduce dizzy spells, do not sit or stand up quickly, especially if you are an older patient. Alcohol can increase dizziness, so try to avoid alcoholic drinks.

Grapefruit juice can increase the levels of cilostazol in your body, which could increase the risk of unwanted side effects. Try to avoid drinking grapefruit juice while on this medicine.

Smoking tobacco may have effects on the circulation that may limit the benefits you receive from cilostazol. You may wish to discuss how to stop smoking with your prescriber or health care professional.

Ask your prescriber or health care professional before you take certain non-prescription (OTC) pain relievers. These include aspirin, aspirin-containing products, and products that contain NSAIDs: like Motrin®, Aleve® and Orudis-KT®. These OTC medications could interfere with your cilostazol therapy. While taking aspirin with cilostazol may be beneficial for you, check with your prescriber prior to taking this combination on your own.

If you are going to have surgery, tell your prescriber or health care professional that you are taking cilostazol.

What side effects may I notice from taking cilostazol?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• fast, slow, or irregular heartbeat
• fluid (edema) in the legs or ankles
• palpitations, chest pain or tightness
Rare:
• black, tarry stools
• blood in urine or stools
• nosebleed or bleeding from gums
• skin rash or itching (hives)
• unusual bruising
• unusually heavy menstrual bleeding

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• dizziness
• diarrhea, or changes in stool appearance or frequency ("loose stools")
• headache
• nausea, or upset stomach

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature below 30 degrees C (86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Search unanswered questions...
Enter a question here...
Search: All sources Community Q&A Reference topics
Wikipedia: Cilostazol
Top
Cilostazol
Systematic (IUPAC) name
6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-
3,4-dihydro-2(1H)-quinolinone
Identifiers
CAS number 73963-72-1
ATC code none
PubChem 2754
DrugBank APRD00155
ChemSpider 2652
Chemical data
Formula C20H27N5O2 
Mol. mass 369.46 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding 95–98%
Metabolism Hepatic (CYP3A4- and CYP2C19-mediated)
Half life 11–13 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Cilostazol (pronounced /sɨˈlɒstəzɒl/) is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal.

Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease.

Cilostazol is a selective PDE3 phosphodiesterase inhibitor with therapeutic focus on cAMP. It inhibits platelet aggregation and is a direct arterial vasodilator. Its main effects are dilation of the arteries supplying blood to the legs and decreasing platelet coagulation.

Contents

Mechanism

Cilostazol is a selective PDE3 phosphodiesterase inhibitor with therapeutic focus on increasing cAMP. An increase in cAMP results in an increase in PKA, which is directly related with an inhibition in platelet aggregation.

Clinical Use

Cilostazol is approved for the treatment of intermittent claudication. The typical dose is 100 mg twice a day. The effects may take as much as 3 months to be evident.

In people with heart failure

Cilostazol, clearly effective for a debilitating condition whose current treatment is often inadequate, is a member of a pharmacologic class that is dangerous to people with severe heart failure and unstudied in other people. Cilostazol has been studied in people without heart failure, without evidence of harm, but much more data would be needed to determine that there is no risk at all. Although cilostazol would not be approvable for a trivial condition the Cardio-Renal Advisory Committee and FDA concluded that fully informed patients and physicians should be able to choose to use it to treat intermittent claudication. Patient and physician labeling will describe the basis for concern and the incomplete information available.[1]

Adverse effects

Possible side effects of cilostazol use include headache (the most common), diarrhea, abnormal stools, increased heart rate, and palpitations.[2]

Interactions

Cilostazol is metabolized by CYP3A4 and CYP2C19, two isoenzymes of the cytochrome P450 system. Drugs that inhibit CYP3A4, such as itraconazole, erythromycin, ketoconazole, and diltiazem, are known to interact with cilostazol. The proton pump inhibitor omeprazole, a potent inhibitor of CYP2C19, increases exposure to the active metabolite of cilostazol.[2]

There has been a single report of grapefruit juice possibly increasing the effects of cilostazol;[3] some drug information sources list this as a possible interaction.[4][5][6] The FDA-approved labeling of cilostazol notes that grapefruit juice (which is a CYP3A4 inhibitor) increases the drug's maximum concentration by around 50%.[2]

References

  1. ^ Center for Drug Evaluation and Research (August 11, 1999). "Approval of Cilostazol". U.S. Food and Drug Administration. http://www.fda.gov/cder/news/cilostazol/approval.htm. Retrieved 2007-04-30. 
  2. ^ a b c "Cilostazol: Official FDA information, side effects and uses.". Drugs.com. February 2008. http://www.drugs.com/pro/cilostazol.html. Retrieved 2008-09-22. 
  3. ^ Taniguchi K, Ohtani H, Ikemoto T, Miki A, Hori S, Sawada Y (October 2007). "Possible case of potentiation of the antiplatelet effect of cilostazol by grapefruit juice". J Clin Pharm Ther 32 (5): 457–9. doi:10.1111/j.1365-2710.2007.00844.x. PMID 17875111. 
  4. ^ "Cilostazol for peripheral arterial disease". Yahoo! Health. http://health.yahoo.com/other-other/cilostazol-for-peripheral-arterial-disease/healthwise--aa127481.html. Retrieved 2008-09-21. 
  5. ^ "Cilostazol". MedicineNet.com. May 25, 1999. http://www.medicinenet.com/cilostazol/article.htm. Retrieved 2008-09-22. 
  6. ^ Cerner-Multum, Inc. (November 29, 2007). "Consumer Drug Information: Cilostazol". Drugs.com. http://www.drugs.com/mtm/cilostazol.html. Retrieved 2008-09-22. 

External links



 
 

 

Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Cilostazol" Read more