Cilostazol
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Synonyms / Brand Names: Cilostazol®, Pletal®
Disclaimer
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Black Box Warning
FDA Package Insert for Cilostazol contains no information regarding Black Box Warning.
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CONTRAINDICATION See full prescribing information for complete boxed warning. Condition Name: Cilostazol and several of its metabolites are inhibitors of phosphodiesterase III. Several drugs with this pharmacologic effect have caused decreased survival compared to placebo in patients with class III-IVcongestive heart failure. Cilostazol tablets are contraindicated in patients with congestive heart failure of any severity. |
Overview
Cilostazol is a_Phosphodiesterase 3 Inhibitor drug that is FDA approved for the treatment of intermittent claudication. There is a Black Box Warning for this drug as shown here. Common adverse reactions include headache, dizziness, palpitation, diarrhea, rhinitis and pharyngitis.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
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Off-Label Use and Dosage (Adult)
Guideline-Supported Use
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Non–Guideline-Supported Use
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- There is limited information about Off-Label Non–Guideline-Supported Use of Cilostazol in adult patients.
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Pediatric Indications and Dosage
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Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
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Condition 2
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Non–Guideline-Supported Use
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Contraindications
- congestive heart failure.
- Haemostatic disorders or active pathologic bleeding.
- [[peptic ulcer].
- Intracranial bleeding.
- Hypersensitivity to any of its components.
Warnings
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Adverse Reactions
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Drug Interactions
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Use in Specific Populations
Pregnancy
- Pregnancy Category (AUS): Cilostazol is not included in Australian Drug Evaluation Committee (ADEC) Pregnancy Categories.
In a rat developmental toxicity study, oral administration of 1000 mg cilostazol/kg/day was associated with decreased fetal weights and increased incidences of cardiovascular, renal and skeletal anomalies (ventricular septal, aortic arch and subclavian artery abnormalities, renal pelvic dilation, 14th rib and retarded ossification). At this dose, systemic exposure to unbound cilostazol in nonpregnant rats was about 5 times the exposure in humans given the MRHD. Increased incidences of ventricular septal defect and retarded ossification were also noted at 150 mg/kg/day (5 times the MRHD on a systemic exposure basis). In a rabbit developmental toxicity study, an increased incidence of retardation of ossification of the sternum was seen at doses as low as 150 mg/kg/day. In nonpregnant rabbits given 150 mg/kg/day, exposure to unbound cilostazol was considerably lower than that seen in humans given the MRHD and exposure to 3,4-dehydro-cilostazol was barely detectable. When cilostazol was administered to rats during late pregnancy and lactation, an increased incidence of stillborn and decreased birth weights of offspring was seen at doses of 150 mg/kg/day (5 times the MRHD on a systemic exposure basis). There are no adequate and well-controlled studies in pregnant women.
Labor and Delivery
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Nursing Mothers
Transfer of cilostazol into milk has been reported in experimental animals (rats). Because of the potential risk to nursing infants, a decision should be made to discontinue nursing or to discontinue cilostazol tablets.
Pediatric Use
The safety and effectiveness of cilostazol in pediatric patients have not been established.
Geriatric Use
Of the total number of subjects (n=2,274) in clinical studies of cilostazol, 56 percent were 65-years-old and over, while 16 percent were 75-years-old and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Pharmacokinetic studies have not disclosed any age-related effects on the absorption, distribution, metabolism and elimination of cilostazol and its metabolites.
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Renal Impairment
Patients on dialysis have not been studied, but, it is unlikely that cilostazol can be removed efficiently by dialysis because of its high protein binding (95% to 98%). Special caution is advised when cilostazol is used in patients with severe renal impairment: estimated creatinine clearance <25 mL/min.
Hepatic Impairment
Patients with moderate or severe hepatic impairment have not been studied in clinical trials. Special caution is advised when cilostazol is used in such patients.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Dietary administration of cilostazol to male and female rats and mice for up to 104 weeks, at doses up to 500 mg/kg/day in rats and 1000 mg/kg/day in mice, revealed no evidence of carcinogenic potential. The maximum doses administered in both rat and mouse studies were, on a systemic exposure basis, less than the human exposure at the MRHD of the drug. Cilostazol tested negative in bacterial gene mutation, bacterial DNA repair, mammalian cell gene mutation and mouse in vivo bone marrow chromosomal aberration assays. It was, however, associated with a significant increase in chromosomal aberrations in the in vitro Chinese Hamster Ovary Cell assay.
Cilostazol did not affect fertility or mating performance of male and female rats at doses as high as 1000 mg/kg/day. At this dose, systemic exposures (AUCs) to unbound cilostazol were less than 1.5 times in males and about 5 times in females, the exposure in humans at the MRHD.
Immunocompromised Patients
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Miscellaneous
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Administration and Monitoring
Administration
Oral
Monitoring
Discontinuation of Therapy
The available data suggest that the dosage of cilostazol tablets can be reduced or discontinued without rebound (i.e., platelet hyperaggregability).
IV Compatibility
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Overdosage
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Chronic Overdose
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Pharmacology
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Cilostazol
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How Supplied
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Patient Information
Patient Information from FDA
(sil-OS-tah-zol)
Please read this leaflet before you start taking cilostazol tablets and each time you renew it in case anything has changed. This leaflet does not replace careful discussions with your doctor. You and your doctor should discuss cilostazol when you start taking it and at regular check-ups. You should follow your doctor’s advice about when to have check-ups. What is cilostazol for? Cilostazol may improve the symptoms of patients with a medical condition called intermittent claudication. What is intermittent claudication? Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. It occurs because narrowing or blockage of the arteries decreases blood flow to the legs. The decreased blood flow does not supply enough oxygen to the leg muscles during walking, resulting in these painful leg cramps.
What treatments are available for intermittent claudication?
The three main treatments available for intermittent claudication are:
- Exercise. Your doctor may advise an exercise program.
- Medication. Your doctor may prescribe a medication such as cilostazol. (See Who should not take cilostazol tablets?)
- Surgery. Your doctor may recommend a surgical procedure to bypass the blocked segment of the artery. Another procedure is called a percutaneous transluminal angioplasty. In this procedure, a catheter (a flexible tube) is inserted into the artery to reduce the blockage and improve blood flow.
How does cilostazol work?
- The exact way that many drugs work is not well understood. Although how cilostazol works is not completely clear, its main effects are to dilate (widen) the arteries supplying blood to the legs and to decrease the ability of platelets in the blood to stick together. Platelets are particles that circulate in the blood and play a role in clotting.
- Cilostazol may reduce the leg pain that patients with intermittent claudication experience, allowing them to walk farther before their leg pain occurs.
- Improvement in symptoms may occur as soon as 2 weeks, but could take up to 12 weeks. If you have not noticed any benefit from cilostazol tablets after 12 weeks you and your doctor may wish to discuss other forms of treatment.
- Sometimes blood vessel disease of the legs causes pain at rest or breakdown of skin in the leg. Cilostazol has not been shown to work in patients with these problems.
Who should not take cilostazol tablets?
- Patients who have congestive heart failure (CHF) must not take cilostazol tablets. The most common symptoms of CHF are shortness of breath and swelling of the legs. However, other conditions may also cause these symptoms. It is important that you discuss with your doctor whether you have CHF.
- Over 1,300 patients took cilostazol in studies that lasted for 3 to 6 months. The mortality rate in these patients was similar to placebo (less than 1%). These studies were too small to be sure there is not some increased risk of dying with longer use or in patients sicker than those in the studies.
How should cilostazol tablets be taken?
- Follow your doctor’s advice about how to take cilostazol tablets.
- You should take cilostazol tablets twice a day, at least one half-hour before or two hours after breakfast and dinner. Take cilostazol tablets at about the same times each day.
- Do not share cilostazol tablets with anyone else. It was prescribed only for you.
- Keep cilostazol tablets and all drugs out of the reach of children.
Can cilostazol tablets be taken with other drugs?
Certain drugs and foods can increase the amount of cilostazol in the blood. Because of this, your doctor may adjust your dose of cilostazol or even stop it if you are taking or are going to take one of the following medications. Drugs Interacting with Cilostazol Generic Name (Brand Names)Type of Drug erythromycin (such as E.E.S.®, Erythrocin®) Antibiotic ketoconazole (Nizoral®), itraconazole (Sporanox®) Antifungal diltiazem (Cardizem®) Antihypertensive omeprazole (Prilosec®) Gastric acid reducer This list does not include every drug that may interact with cilostazol tablets. Therefore, you should tell your doctor about all medications that you are taking, including vitamins, herbal supplements and over-the-counter drugs you can buy without a prescription. You should also check with your doctor before taking a new medication after you have begun cilostazol tablets.
What are the possible side effects of cilostazol tablets?
Cilostazol tablets may cause side effects including headache, diarrhea, abnormal stools, increased heart rate and palpitations. You should discuss possible side effects with your doctor before taking cilostazol tablets and any time you think you are having a side effect. This provides only a summary of information about cilostazol tablets. If you have any questions about cilostazol tablets, talk to your doctor. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Patient Information from NLM
For patient information about Cilostazol from NLM, click here.
Precautions with Alcohol
Alcohol-Cilostazol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
Brand Names®
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