Клопидогрела гидросульфат (Форма I) Uses, Dosage, Side Effects and more

(Клопидогрела гидросульфат (Форма I)) is an inhibitor of platelet aggregation. Lopirel (Клопидогрела гидросульфат (Форма I)) selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation.

Клопидогрела гидросульфат (Форма I) is a prodrug of a platelet inhibitor used to reduce the risk of myocardial infarction and stroke. It has a long duration of action as it is taken once daily and a large therapeutic window as it is given in doses of 75-300mg daily.

Attribute	Details
Trade Name	Клопидогрела гидросульфат (Форма I)
Availability	Prescription only
Generic	Clopidogrel
Clopidogrel Other Names	Clopidogrel, Clopidogrelum
Related Drugs	aspirin, lisinopril, metoprolol, propranolol, Xarelto, Plavix, Brilinta, enoxaparin, rivaroxaban, pravastatin
Type
Formula	C16H16ClNO2S
Weight	Average: 321.822 Monoisotopic: 321.059027158
Protein binding	Both the active and inactive metabolites of clopidogrel are 98% protein bound in plasma. Studies in cows show clopidogrel 71-85.5% bound to serum albumin.
Groups	Approved
Therapeutic Class	Anti-platelet drugs
Manufacturer
Available Country	Russia
Last Updated:	January 7, 2025 at 1:49 am

Uses

(Клопидогрела гидросульфат (Форма I)) is used for the reduction of atherosclerotic events (myocardial infarction, ischaemic stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease.

Клопидогрела гидросульфат (Форма I) is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Acute Myocardial Infarction (AMI), Cardiovascular Events, Atherothrombotic events

How Клопидогрела гидросульфат (Форма I) works

Клопидогрела гидросульфат (Форма I) is metabolized to its active form by carboxylesterase-1. The active form is a platelet inhibitor that irreversibly binds to P2Y₁₂ ADP receptors on platelets. This binding prevents ADP binding to P2Y₁₂ receptors, activation of the glycoprotein GPIIb/IIIa complex, and platelet aggregation.

Dosage

The recommended dose of Lopirel (Клопидогрела гидросульфат (Форма I)) is 75 mg once daily with or without food.

Side Effects

Generally Клопидогрела гидросульфат (Форма I) is well tolerated. However, a few common side effects i.e. Influenza-like symptoms, headache, upper respiratory tract infection, dizziness, muscle and back pain, and rash may occur.

Toxicity

A single dose of clopidogrel at 1500-2000mg/kg was lethal to mice and rats while 3000mg/kg was lethal to baboons. Symptoms of overdose include vomiting, breathing difficulty, gastrointestinal hemorrhage, and prostration. Клопидогрела гидросульфат (Форма I) is irreversibly bound to platelets for their lifetime, which is approximately 11 days. Overdoses of clopidogrel can be treated with platelet transfusions to restore clotting ability.

Precaution

As with other anti-platelet agents, Клопидогрела гидросульфат (Форма I) should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery, or other pathological conditions. Клопидогрела гидросульфат (Форма I) should be discontinued 7 days prior to surgery. Клопидогрела гидросульфат (Форма I) should be used with caution in hepatically impaired patients who may have bleeding diatheses.

Interaction

Concomitant use of Heparin, Warfarin and NSAIDs with Клопидогрела гидросульфат (Форма I) should be undertaken with caution. Клопидогрела гидросульфат (Форма I) potentiate the effect of Aspirin on collagen-induced platelet aggregation. The safety of chronic concomitant administration of Aspirin and Клопидогрела гидросульфат (Форма I) has not been established.

Food Interaction

• Take with or without food.

Drug Interaction

Moderate: aspirin, aspirin, aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acidsUnknown: ubiquinone, ubiquinone, rosuvastatin, rosuvastatin, metoprolol, metoprolol, metoprolol, metoprolol, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Disease Interaction

Major: bleedingModerate: liver diseaseMinor: renal dysfunction

Volume of Distribution

The apparent volume of distribution of clopidogrel is 39,240±33,520L.

Elimination Route

A 75mg oral dose of clopidogrel is 50% absorbed from the intestine. Клопидогрела гидросульфат (Форма I) can be taken with or without food. A meal decreases the AUC of the active metabolite by 57%. The active metabolite of clopidogrel reaches a maximum concentration after 30-60 minutes. Клопидогрела гидросульфат (Форма I) reached a C_max of 2.04±2.0ng/mL in 1.40±1.07h.

The AUC for a 300mg oral dose of clopidogrel was 45.1±16.2ng*h/mL for poor metabolizers, 65.6±19.1ng*h/mL for intermediate metabolizers, and 104.3±57.3ng*h/mL for extensive metabolizers. The C_max was 31.3±13ng/mL for poor metabolizers, 43.9±14ng/mL for intermediate metabolizers, and 60.8±34.3ng/mL for extensive metabolizers.

Half Life

That half life of clopidogrel is approximately 6 hours following a 75mg oral dose while the half life of the active metabolite is approximately 30 minutes.

Clearance

The clearance of a 75mg oral dose was 18,960±15,890L/h and for a 300mg oral dose was 16,980±10,410L/h.

Elimination Route

An oral dose of radiolabelled clopidogrel is excreted 50% in the urine and 46% in the feces over 5 days. The remainder of clopidogrel is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies of Клопидогрела гидросульфат (Форма I) in pregnant women. However, Клопидогрела гидросульфат (Форма I) should be used during pregnancy only if clearly needed.

Lactation: Клопидогрела гидросульфат (Форма I) is not recommended for use while breast-feeding. It is not known for sure whether Клопидогрела гидросульфат (Форма I) is excreted in breast milk, although it is suspected that it is.

Contraindication

Клопидогрела гидросульфат (Форма I) is contraindicated in patients with a hypersensitivity to the drug substance or any component of the product, and those with active pathological bleeding such as peptic ulcer or intracranial hemorrhage.

Special Warning

Use in children: Safety and effectiveness of Клопидогрела гидросульфат (Форма I) in pediatric population have not been established.

Acute Overdose

In the event of over dosage no adverse effects were reported and no therapy was substituted.

Symptoms: Prolonged bleeding time and subsequent bleeding complications.

Management: May restore clotting ability with platelet transfusion.

Storage Condition

Store at 25° C.

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