Contraindicated w/ CHF of any severity due to possible decrease in survival.
Phosphodiesterase 3 (PDE3) inhibitor
Reduction of symptoms of intermittent claudication.
Reduction of Symptoms: 100mg bid
D/C if symptoms have not improved after 3 months
Moderate/Strong CYP3A4 or Strong CYP2C19 Inhibitors: Consider reduction to 50mg bid
Take at least 1/2 hr before or 2 hrs after breakfast and dinner
Tab: 50mg, 100mg
CHF of any severity. Hemostatic disorders or active pathologic bleeding (eg, peptic ulcer, intracranial bleeding).
Thrombocytopenia/leukopenia progressing to agranulocytosis reported (rare) . May induce tachycardia, palpitation, tachyarrhythmia, and/or hypotension. Patients w/ history of ischemic heart disease may be at risk for angina pectoris or MI exacerbation. Special caution w/ moderate/severe hepatic and severe renal impairment (CrCl <25mL/min).
Headache, palpitation, tachycardia, abnormal stools, diarrhea, peripheral edema, dizziness, infection, rhinitis, pharyngitis, nausea, back pain, dyspepsia, abdominal pain, increased cough.
See Dose Modification. May increase levels and overall pharmacological activity w/ strong or moderate CYP3A4 inhibitors (eg, ketoconazole, itraconazole, erythromycin, diltiazem) and strong CYP2C19 inhibitors (eg, ticlopidine, fluconazole, omeprazole).
PREGNANCY AND LACTATION
Category C, not for use in nursing.
MECHANISM OF ACTION
Phosphodiesterase III inhibitor; not established. Suspected to inhibit phosphodiesterase activity and suppress cAMP degradation resulting in an increase of cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
Distribution: Plasma protein binding (95-98%). Metabolism: Liver (extensive) via CYP450 3A4 (primary), 2C19; 3,4-dehydro-cilostazol, 4'-trans-hydroxy-cilostazol (major active metabolites). Elimination: Urine (74%), feces (20%); T1/2=11-13 hrs.
Assess for hypersensitivity to drug, CHF, hemostatic disorders, active pathologic bleeding, history of ischemic heart disease, renal/hepatic impairment, pregnancy/nursing status, and possible drug interactions.
Monitor for tachycardia, palpitation, tachyarrhythmia, hypotension, and other adverse reactions. Monitor platelets and WBC counts periodically.
Advise to take at least 1/2 hr ac or 2 hrs pc. Inform that benefits of medication may not be immediate and treatment may be required for up to 12 weeks before beneficial effect is experienced.
25°C (77°F); excursions permitted to 15-30°C (59-86°F).
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