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Cilostazol; Uses, Dosage, Side Effects, Drug Interactions

Cilostazol is a quinolinone derivative and cellular phosphodiesterase inhibitor, more specific for phosphodiesterase III (PDE III). Although the exact mechanism of action of is unknown, cilostazol and its metabolites appear to inhibit PDE III activity, thereby suppressing cyclic adenosine monophosphate (cAMP) degradation. This results in an increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.

Cilostazol is a quinolinone derivative that inhibits specific cellular phosphodiesterases, which cause arterial vasodilation and inhibition of platelet function and makes it a value as a therapy of intermittent claudication and as a means of secondary prevention of stroke. Cilostazol has not been associated with serum enzyme elevations during therapy or with published instances of clinically apparent liver injury.

Cilostazol is a quinolinone-derivative medication used in the alleviation of the symptoms of intermittent claudication in individuals with peripheral vascular disease. Cilostazol is a phosphodiesterase inhibitor with a therapeutic focus on cyclic adenosine monophosphate (cAMP). It inhibits platelet aggregation and is a direct arterial vasodilator. Its main effects are dilation of the arteries supplying blood to the legs and decreasing platelet coagulation.

Mechanism of action of Cilostazol

Cilostazol and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.Cilostazol is a quinolinone derivative indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.

Cilostazol, a phosphodiesterase 3, has been widely used in patients with arterial disease and is known to have additional beneficial effects on dyslipidemia. However, the effect of cilostazol on hepatic steatosis has not been fully elucidated. We investigated the effect of cilostazol on hepatic ABCA1 expression and hepatic steatosis in diet-induced obesity mice model. Hepatic ABCA1 expression and lipid accumulation were analyzed in HepG2 cell lines treated with cilostazol. Male C57BL/6 mice were randomly divided into three groups: (1) fed normal chow diet with vehicle; (2) fed high-fat diet (HFD) with vehicle; (3) fed HFD with cilostazol. Cilostazol (30 mg/kg) was orally administered once daily for 9 weeks. Cilostazol significantly enhanced ABCA1 expression and restored ABCA1 expression reduced by palmitate in HepG2 cells. Cilostazol treatment ameliorated lipid accumulation induced by palmitate, and this effect was diminished when ABCA1 or LRP1 was silenced by small interference RNA. After silencing of LRP1, ABCA1 expression was decreased in HepG2 cells. Cilostazol significantly enhanced hepatic ABCA1 expression and decreased hepatic fat in HFD-fed mice. Hepatic expression of cleaved caspase-3 and PARP1 was also decreased in HFD-fed mice treated with cilostazol. Cilostazol ameliorated hepatic steatosis and increased ABCA1 expression in the hepatocytes. Enhancing ABCA1 expression with cilostazol represents a potential therapeutic avenue for treatment of hepatic steatosis.

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Indications of Cilostazol

Intermittent claudication
Treatment of intracranial atherosclerosis
Secondary stroke prevention.
Myocardial infarction,
Established peripheral arterial disease.
Cardiovascular events
Acute coronary syndrome
Ischemic Stroke, prophylaxis
Percutaneous coronary intervention
Peripheral arterial disease
Platelet aggregation inhibition
Transient ischemic attack
For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
Cilostazol is indicated for the improvement of the maximal and pain-free walking distances in patients with intermittent claudication, who do not have rest pain and who do not have evidence of peripheral tissue necrosis (peripheral arterial disease Fontaine stage II).

Contra-Indications of Cilostazol

Decreased blood platelets
Decreased white blood cells
Angina
Very rapid heartbeat – Torsades de Pointes
Prolonged QT interval on EKG
Chronic heart failure
Abnormal EKG with QT changes from Birth
Bleeding
Fast heartbeat
Tobacco smoking
Blockage of blood flow from the left ventricle of the heart

Dosage of Cilostazol

Strengths: 50 mg; 100 mg

Intermittent Claudication

100 mg orally twice a day administered at least 30 minutes before or 2 hours after breakfast and dinner.

Side Effects of Cilostazol

The most common

stomach or abdominal cramps, gas, or pain
Upper respiratory tract infection
Chest pain
A headache
Joint painPain
Dizziness
Nausea and vomiting
Severe stomach ache
epigastric pain,
diarrhea,
anorexia,
flatulence,
a headache,
dizziness,
fainting, fast or pounding heartbeats.

More common

Less common

Bone pain
burning feeling in the throat or chest
difficulty with swallowing
pain or stiffness in the joints
ringing or buzzing in the ears
swelling of the face, fingers, or lower legs
fast or irregular heartbeat
unusual bruising or bleeding
sudden, severe headache or vomiting
vision changes
unusual weight gain
swelling of the hands, arms, feet, ankles, or lower legs
dark, tarry, or bloody stools
vomit that looks like coffee grounds
signs of infection, which may include fever, sore throat, rash, or chills

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Drug Interactions of Cilostazol

Cilostazol may interact with following drugs ,supplyments & may decrease the efficacy of drug

antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide)
Anticoagulants (blood thinners) such as Coumadin (warfarin)
Aspirin
Antiplatelet medications such as (clopidogrel),
“azole” antifungals (e.g., fluconazole, ketoconazole, )
bupropion
calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
cimetidine
glucosamine
heparin
low molecular weight heparins (e.g., dalteparin, enoxaparin, tinzaparin)
macrolide antibiotics (e.g., clarithromycin, erythromycin)
nonsteroidal anti-inflammatories (NSAIDs; e.g., ibuprofen, diclofenac,ketorolac, naproxen)
proton pump inhibitors (PPIs; e.g., esomeprazole, lansoprazole, omeprazole, pantoprazole)
selegiline
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine , fluoxetine, paroxetine, sertraline)
warfarin

Pregnancy & Lactation of Cilostazol

FDA Pregnancy Category C

Pregnancy

It’s not known whether cilostazol is safe to take during pregnancy.Talk to your doctor before taking this medicine if you’re pregnant or plan to become pregnant. It’s also not known whether the medication passes into breast milk or could harm a breastfeeding baby. Don’t breastfeed while taking cilostazol without first talking to your doctor.

Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if cilostazol crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use .