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Cilostazol



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  ?
PubChem 2754
DrugBank APRD00155
Chemical data
Formula C20H27N5O2 
Mol. mass 369.46 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 95–98%
Metabolism Hepatic (CYP2C19- and CYP3A4-mediated)
Half life 11–13 hours
Excretion renal
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status
Routes Oral

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 cAMP phosphodiesterase inhibitor. 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.

Additional recommended knowledge

Contents

Usage

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.

Interactions and side effects

Drugs that interact with cilostazol include itraconazole, erythromycin, ketoconazole, diltiazem, and omeprazole. Grapefruit juice interacts with the drug; other citrus juices do not.

Possible side effects of cilostazol include headache, diarrhea, abnormal stools, increased heart rate, and palpitations.

Important note

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]

References

  1. ^ Center for Drug Evaluation and Research (August 11 1999). Approval of Cilostazol. U.S. Food and Drug Administration. Retrieved on 2007-04-30.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Cilostazol". A list of authors is available in Wikipedia.
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