CILOSTAZOL
| CILOSTAZOL (sil-os'tah-zol) Pletal Classifications: vasodilator; phosphodiesterase inhibitor; antiplatelet agent; Therapeutic: peripheral vasodilator Pregnancy Category: C |
Availability
50 mg, 100 mg tablets
Action
Inhibition of an isoenzyme which results in vasodilatation and inhibition of platelet aggregation induced by collagen or arachidonic acid.
Therapeutic Effect
Increases the skin temperature of the extremities and improves claudication. Effectiveness is indicated by increased ability to walk further without claudication.
Uses
Intermittent claudication.
Contraindications
Congestive heart failure of any severity; hypersensitivity to cilostazol; acute MI; hemostatic disorders or pathologic bleeding; pregnancy (category C), lactation.
Cautious Use
Cardiac arrhythmias, MI within 6 mo; valvular heart disease; peptic ulcer disease; renal failure. Safety and efficacy in children <18 y are not established.
Route & Dosage
| Intermittent Claudication Adult: PO 100 mg b.i.d. 0.5 h before or 2 h after meals, may need to reduce to 50 mg b.i.d. with concomitant ketoconazole, itraconazole, erythromycin, diltiazem or omeprazole |
Administration
Oral- Give at least ? h before or 2 h after a meal. Do not give with grapefruit juice.
- Store at 20°–25° C (68°–77° F).
Adverse Effects (≥1%)
Body as a Whole: Back pain, headache, infection, myalgia. CNS: Dizziness, vertigo. CV: Palpitations, tachycardia. GI: Abdominal pain, abnormal stools, diarrhea, dyspepsia, flatulence, nausea. Respiratory: Cough, pharyngitis, rhinitis.Interactions
Drug: Aspirin, clopidogrel, diltiazem, erythromycin, fluconazole, fluvoxamine, fluoxetine, ketoconazole, itraconazole, macrolide antibiotics, miconazole, nefazodone, omeprazole, sertraline may increase cilostazol levels. Food: High fat meals may increase peak concentrations. Grapefruit juice may increase concentration.Pharmacokinetics
Absorption: Well absorbed from GI tract. Onset: 2–4 wk. Distribution: 95–98% protein bound. Smoking may decrease serum levels. May be excreted in breast milk. Metabolism: Metabolized by CYP3A4 to active metabolites. Elimination: Metabolites primarily excreted in urine. Half-Life: 1–13 hr.Nursing Implications
Assessment & Drug Effects
- Monitor therapeutic effectiveness indicated by ability to walk farther without leg pain.
- Monitor for S&S of CHF. Do not give cilostazol to patients with preexisting CHF.
Patient & Family Education
- Avoid grapefruit or grapefruit juice while taking cilostazol.
- Allow 2–12 wk for therapeutic response.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug