Clopidogrel

BRAND NAMES:

Duoplavin – It is the combination of acetylsalicylic acid 75mg and clopidogrel hydrogen sulfate 75mg as Duoplavin 75/75mg film-coated tablets available in the market.

Plavix – Plavix is a drug composed of clopidogrel 75mg film-coated tablets which helps prevent blood clots.

Zyllt – Zyllt medicine has the main ingtredient is clopidogrel as lopidogrel hydrogen sulphate 75mg which are avail in the form of film coated tablets.

MECHANISM OF ACTION: 

In vivo biotransformation of clopidogrel into an active thiol metabolite is necessary. The active metabolite permanently blocks the P2Y component of ADP receptors on the platelet surface, preventing activation of the GPⅡb/Ⅲa receptor complex and lowering platelet aggregation. Clopidogrel-blocked platelets are compromised for their existence (about 7 to 10 day

PHARMACOKINETICS: 

Absorption: Clopidogrel is quickly absorbed after a single or repeated oral dose of 75 mg per day. Clopidogrel metabolite excretion in the urine indicates at least 50% absorption.

Distribution: Clopidogrel's apparent volume of distribution is 39,240±33,520L.

Metabolism: 85-90% of an oral dosage is first passed through the liver via carboxylesterase 1 to an inactive carboxylic acid metabolite, with around 2% of clopidogrel being oxidized to 2-oxo clopidogrel. 35.8% of this conversion is attributed to CYP1A2, 19.4% to CYP2B6, and 44.9% to CYP2619; however, additional research indicates that CYP3A4, CYP3A5, and CYP2C9 may also be involved. Oxoclopidogrel undergoes further metabolism to produce the active metabolite. The conversion rate is 32.9% for CYP2B6, 6.79% for CYP2C9, 20.6% for CYP2C19, and 39.8% for CYP3A4.

Excretion: Over 5 days, an oral dose of radiolabeled clopidogrel is eliminated 50% in urine and 46% in feces. Clopidogrel remains permanently connected to platelets for the rest of their lives, around 8-11 days.

PHARMACODYNAMICS: 

Clopidogrel, a platelet inhibitor, lowers the risk of heart attack and stroke. It has an extended period of activity. It is used once a day and has a broad therapeutic window because the dosages range from 75 to 300 mg per day.

DRUG ADMINISTRATION:

Clopidogrel is often consumed orally, with or without food. The dosage and frequency of medicine administration will be determined by the patient's medical condition, age, and response to treatment as advised by the physician. 

Clopidogrel is usually given once a day, preferably at the same time every day, to maintain a stable amount of the medicine in the body. The medicine is frequently prescribed for long-term use to avoid blood clots, heart attacks, and strokes. 

CONTRAINDICATIONS:

Hypersensitivity (Anaphylaxis) to clopidogrel or any component of the formulation active pathological bleeding (Peptic ulcer, Intra cranial hemorrhage).

DRUG INTERACTIONS:

Drug interactions can alter the effectiveness of medications or increase the risk of severe side effects.

Clopidogrel may interact with other 

Anticoagulants :-Warfarin, Aspirin, rivaroxaban, Apixaban

Pain killers :- Ibuprofen

Antidepressants :- Citalopram

Proton pump inhibitor :- Omeprazole

SIDE EFFECTS :

• Heavier periods. 

• Bleeding gum, Nosebleeds

• Easy brushing

• Diarrhoea

• Stomach pain, indigestion, or heartburn 

OVERDOSE : 

• Overdoses of clopidogrel can be treated by platelet transfusions to restore clotting capacity. 
• The signs of an overdose include vomiting, difficulty breathing, gastrointestinal hemorrhage, and prostration.
• Toxicity: 
• Clopidogrel can cause liver damage as an individual hypersensitivity reaction or as a dose-dependent effect. If a patient develops liver failure or jaundice while using clopidogrel, they should discontinue taking it.

STORAGE :

It is recommended to store ciprodrel at room temperature, approximately 77°F (25°C). It can be kept in storage for a brief time between 59°F and 86°F (15°C and 30°C). This drug shouldn't be kept in damp or moist conditions.