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Pharmacologic class: Quinolone derivative

Therapeutic class: Antiplatelet agent

Pregnancy risk category C


Unclear. Thought to inhibit phosphodiesterase III by increasing cyclic adenosine monophosphate in platelets and blood vessels, causing vasodilation and enhancing cardiac contractility and coronary blood flow.


Tablets: 50 mg, 100 mg

Indications and dosages

Intermittent claudication

Adults: 100 mg P.O. b.i.d. at least 30 minutes before or 2 hours after breakfast and dinner

Dosage adjustment

• Concurrent use of diltiazem, erythromycin, itraconazole, ketoconazole, or omeprazole


• Hypersensitivity to drug

• Heart failure


Use cautiously in:

• cardiovascular disorders

• patients receiving other antiplatelet agents concurrently

• pregnant or breastfeeding patients

• children (safety and efficacy not established).


• Give with water 30 minutes before or 2 hours after patient consumes food or milk.

• Don't give with grapefruit juice.

• Be aware that although response may occur within 2 to 3 weeks, patient should continue therapy for up to 12 weeks or as prescribed.

Adverse reactions

CNS: dizziness, headache, vertigo

CV: tachycardia

GI: abdominal pain, abnormal stools, dyspepsia, flatulence

EENT: rhinitis, pharyngitis

Musculoskeletal: back pain, myalgia

Respiratory: increased cough

Other: infection


Drug-drug. CYP3A4 and CYP2C19 inhibitors, diltiazem, erythromycin, macrolides, omeprazole: increased cilostazol blood level

Drug-food. Grapefruit juice, high-fat meals: increased cilostazol blood level

Drug-behaviors. Smoking: decreased exposure to cilostazol

Patient monitoring

• Monitor cardiovascular status.

• Closely monitor patient if he's receiving other antiplatelet drugs.

Patient teaching

• Instruct patient to take drug with full glass of water, 30 minutes before or 2 hours after food or milk.

• Advise patient to report nausea, vomiting, or abdominal pain.

• Instruct patient not to smoke, because smoking impedes drug effects.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, and behaviors mentioned above.


(sil-os-tah-zol) ,


(trade name)


Therapeutic: antiplatelet agents
Pharmacologic: platelet aggregation inhibitors
Pregnancy Category: C


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


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.


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 and 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)

PO2–4 wkup to 12 wkunknown


Contraindicated in: Hypersensitivity;HF; Obstetric: Potential for congenital defects, stillbirth, and low birth weight; Lactation: Potential risk to nursing infants; discontinue or bottle feed.
Use Cautiously in: Pediatric: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • headache (most frequent)
  • dizziness


  • palpitations
  • tachycardia


  • diarrhea


Drug-Drug interaction

Concurrent administration of ketoconazole, itraconazole, erythromycin, diltiazem, fluconazole, miconazole, fluvoxamine, fluoxetine, nefazodone, sertraline, or omeprazole decreases metabolism and increases levels and activity of cilostazol (use lower doses).Concurrent use with aspirin has additive effects on platelet function.Grapefruit juice inhibits metabolism and increases effects; concurrent use should be avoided.


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

Availability (generic available)

Tablets: 50 mg, 100 mg

Nursing implications

Nursing 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.

Potential Nursing Diagnoses

Activity intolerance (Indications)


  • Oral: Administer on an empty stomach, 1 hr before or 2 hr after meals.
    • Do not administer with grapefruit juice. May increase cilostazol levels.

Patient/Family Teaching

  • Instruct patient to take cilostazol on an empty stomach, exactly as directed.
  • 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.

Pletal ®

Cilostazol, see there.


A brand name for CILOSTAZOL.
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