pharmacopeia
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/api/v1/drug/cilostazol

Boxed warning

CONTRAINDICATED IN HEART FAILURE PATIENTS Cilostazol tablets are contraindicated in patients with heart failure of any severity. 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-IV heart failure [see Contraindications ( 4 )] . WARNING: CONTRAINDICATED IN HEART FAILURE PATIENTS See full prescribing information for complete boxed warning. Cilostazol tablets is contraindicated in patients with heart failure of any severity. Cilostazol and several of its metabolites are inhibitors of phosphodiesterase III. Several drugs with the pharmacologic effect have caused decreased survival compared to placebo patients with class III-IV heart failure. (4)

2D structure
6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
SMILES C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
InChIKey RRGUKTPIGVIEKM-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Phosphodiesterase 3 Inhibitors.

Phosphodiesterase 3

Indications

Sourced from openFDA
  • Cilostazol tablets are indicated for the reduction of symptoms of intermittent claudication, as demonstrated by an increased walking distance.

Contraindications

Sourced from openFDA
  • Cilostazol is contraindicated in patients with: Heart failure of any severity: 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-IV heart failure.contraindicated

Dosage & administration

Sourced from openFDA

The recommended dosage of cilostazol is 100 mg twice daily taken at least half an hour before or two hours after breakfast and dinner ( 2.1 ) Reduce the dose to 50 mg twice daily when coadministered with CYP3A4 inhibitors such as ketoconazole, itraconazole, erythromycin, and diltiazem, or CYP2C19 inhibitors such as ticlopidine, fluconazole, and omeprazole ( 2.2 ) 2.1 Recommended dosage The recommended dosage of cilostazol is 100 mg twice daily taken at least half an hour before or two hours after breakfast and dinner. Patients may respond as early as 2 to 4 weeks after the initiation of therapy, but treatment for up to 12 weeks may be needed before a beneficial effect is experienced. If symptoms are unimproved after 3 months, discontinue cilostazol. 2.2 Dose Reduction with CYP3A4 and CYP2C19 Inhibitors Reduce dose to 50 mg twice daily when coadministered with strong or moderate inhibitors of CYP3A4 (e.g., ketoconazole, itraconazole, erythromycin, and diltiazem) or inhibitors of CYP2C19 (e.g., ticlopidine, fluconazole, and omeprazole) [see Drug Interactions ( 7.1 )] .

Warnings & precautions

Sourced from openFDA

Risks of tachycardia, palpitation, tachyarrhythmia or hypotension. Risks of exacerbations of angina pectoris or myocardial infarction in patients with a history of ischemic heart disease ( 5.2 ) Left ventricular outflow tract obstruction has been reported in patients with sigmoid shaped interventricular septum ( 5.1 ) Risks of thrombocytopenia or leukopenia progressing to agranulocytosis-monitor platelets and white blood cell counts ( 5.3 ) Avoid use in patients with hemostatic disorders or active pathologic bleeding ( 5.4 ) 5.1 Tachycardia Cilostazol may induce tachycardia, palpitation, tachyarrhythmia or hypotension. The increase in heart rate associated with cilostazol is approximately 5 to 7 bpm. Patients with a history of ischemic heart disease may be at risk for exacerbations of angina pectoris or myocardial infarction. 5.2 Left Ventricular Outflow Tract Obstruction Left ventricular outflow tract obstruction has been reported in patients with sigmoid shaped interventricular septum. Monitor patients for the development of a new systolic murmur or cardiac symptoms after starting cilostazol. 5.3 Hematologic Adverse Reactions Cases of thrombocytopenia or leukopenia progressing to agranulocytosis when cilostazol was not immediately discontinued have been reported. Agranulocytosis is reversible on discontinuation of cilostazol. Monitor platelets and white blood cell counts periodically. 5.4 Hemostatic Disorders or Active Pathologic Bleeding Cilostazol inhibits platelet aggregation in a reversible manner.

Adverse reactions

Sourced from openFDA

The following adverse reactions are discussed in greater detail in other sections of the labeling: Patients with Heart Failure [see Boxed Warning] Tachycardia [see Warnings and Precautions ( 5.1 )] Left Ventricular Outflow Tract Obstruction [see Warnings and Precautions ( 5.2 )] Hematologic Adverse Reactions [see Warnings and Precautions ( 5.3 )] Hemostatic Disorders or Active Pathologic Bleeding [see Warnings and Precautions ( 5.4 )] Most common adverse reactions greater than or equal to 2% and at least twice that for placebo in patients on 100 mg twice daily are headache, diarrhea, abnormal stools, and palpitation ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AvKARE at 1-855-361-3993; email drugsafety@avkare.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse reactions were assessed in eight placebo-controlled clinical trials involving patients exposed to either 50 or 100 mg twice daily cilostazol tablets (n=1301) or placebo (n=973), with a median treatment duration of 127 days for patients on cilostazol tablets and 134 days for patients on placebo.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Teratogenic Effects Pregnancy Category C. Cilostazol has been shown to be teratogenic in rats at doses that are greater than 5-times the human MRHD on a body surface area basis. There are no adequate and well-controlled studies in pregnant women. 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, 14 th 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.

Overdosage

Sourced from openFDA

Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The patient should be carefully observed and given supportive treatment. Since cilostazol is highly protein-bound, it is unlikely that it can be efficiently removed by hemodialysis or peritoneal dialysis. The oral LD 50 of cilostazol is greater than 5 g per kg in mice and rats and greater than 2 g per kg in dogs.

Approval history

Sourced from openFDA
  • Nov 23, 2004ANDAANDA077021Chartwell Rx
  • Nov 24, 2004ANDAANDA077027Teva
  • Dec 10, 2004ANDAANDA077030Apotex
  • Nov 8, 2005ANDAANDA077310Chartwell Rx
  • Mar 29, 2006ANDAANDA077208Slate Run Pharma

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
6,066 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Diarrhoea3105.1%
  2. 2Fall2363.9%
  3. 3Pneumonia2333.8%
  4. 4Drug Ineffective2313.8%
  5. 5Death2193.6%
  6. 6Dyspnoea2143.5%
  7. 7Off Label Use2123.5%
  8. 8Nausea2103.5%
  9. 9Anaemia1913.1%
  10. 10Asthenia1853.0%
  11. 11Fatigue1833.0%
  12. 12Dizziness1823.0%
  13. 13Vomiting1823.0%
  14. 14Pain In Extremity1732.9%
  15. 15Pain1612.7%

Literature

View JSON

Recent PubMed references pinned to Cilostazol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 184 ClinicalTrials.gov registrations naming Cilostazol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Cilostazol work?
Mechanism-of-action class: Phosphodiesterase 3 Inhibitors.
What is Cilostazol used for?
According to FDA labeling, Cilostazol carries indications including: Cilostazol tablets are indicated for the reduction of symptoms of intermittent claudication, as demonstrated by an increased walking distance.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Cilostazol?
Cilostazol is classified as Platelet aggregation inhibitors excl. heparin, Phosphodiesterase 3 Inhibitor, Phosphodiesterase 3 Inhibitors, Decreased Platelet Activating Factor Activity, Decreased Platelet Aggregation, Positive Chronotropy, Positive Inotropy, Vasodilation.
What are the contraindications for Cilostazol?
Cilostazol labeling lists contraindications including: Cilostazol is contraindicated in patients with: Heart failure of any severity: 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-IV heart failure.. Always consult the full prescribing information and a clinician.
Note. Data for cilostazol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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