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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 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.
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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.
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
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For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
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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
- Fast or irregular heartbeat
- fever
- Back pain
- dizziness
- headache
- increased cough
- pain or stiffness in the muscles
- pounding heartbeat
- runny or stuffy nose
- sore throat
- swelling of the arms or legs
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
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 .
References
