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

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