cilostazol

Therapeutic Classification: antiplatelet agents

Pharmacologic Classification: platelet aggregation inhibitors

Indications ⬆ ⬇

REMS

Reduction of the symptoms of intermittent claudication as measured by increased walking distance.

Action ⬆ ⬇

Inhibits the enzyme cyclic adenosine monophosphate (cAMP) phosphodiesterase III (PDE III), which results in increased cAMP in platelets and blood vessels, producing inhibition of platelet aggregation and vasodilation.

Therapeutic effects:

Reduced symptoms of intermittent claudication with improved walking distance.

Pharmacokinetics ⬆ ⬇

Absorption: Slowly absorbed after oral administration.

Distribution: Unknown.

Protein Binding: 95–98% bound to plasma proteins; one active metabolite is 97.4% bound, the other is 66% bound.

Metabolism/Excretion: Extensively metabolized by the liver, two metabolites have platelet aggregation inhibitory activity; metabolites are mostly excreted by the kidneys.

Half-Life: Cilostazol and its active metabolites: 11–13 hr.

Time/Action Profile ⬆ ⬇

(symptom reduction)

ROUTE	ONSET	PEAK	DURATION
PO	2–4 wk	up to 12 wk	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
HF;
OB: Potential for congenital defects, stillbirth, and low birth weight;
Lactation: Potential risk to nursing infants; discontinue or bottle feed.

Use Cautiously in:

Pedi: Safety not established.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, left ventricular outflow obstruction, palpitations, tachycardia

GI: diarrhea

Neuro: headache, dizziness

Interactions ⬆ ⬇

Drug-drug:

Concurrent administration of ketoconazole, itraconazole, erythromycin, diltiazem, fluconazole, miconazole, fluvoxamine, fluoxetine, nefazodone, sertraline, or omeprazole↓ metabolism and ↑ levels and activity of cilostazol (use lower doses).
Concurrent use with aspirin has additive effects on platelet function.

Drug-Food:

Grapefruit juice inhibits metabolism and ↑ effects; concurrent use should be avoided.

Route/Dosage ⬆ ⬇

PO (Adults ): 100 mg twice daily (50 mg twice daily if receiving inhibitors of cilostazol metabolism).

Availability ⬆ ⬇

(Generic available)

Tablets: 50 mg; 100 mg

Assessment ⬆ ⬇

Assess patient for intermittent claudication before and periodically during therapy.

Lab Test Considerations:

May occasionally cause anemia, hyperlipemia, hyperuricemia, and albuminuria. May prolong bleeding time.

Implementation ⬆ ⬇

PO: Administer on an empty stomach, 1 hr before or 2 hr after meals.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take cilostazol on an empty stomach, exactly as directed.
Advise patient to avoid grapefruit juice during therapy.
May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to avoid smoking; nicotine constricts blood vessels.

Evaluation/Desired Outcomes ⬆ ⬇

Relief from cramping in calf muscles, buttocks, thighs, and feet during exercise.
- Improvement in walking endurance. Therapeutic effects may be seen in 2–4 wk.

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Pronunciation ⬇

Classifications ⬆ ⬇