Lirta pills 75mg, 30pcs

Composition

Active ingredient: clopidogrel 75 mg

Pharmacological action

After oral use at a dose of 75 mg, clopidogrel is rapidly absorbed from the gastrointestinal tract. However, the concentration in the blood plasma increases slightly and 2 hours after use does not reach the level that can be determined (0.025 mcg/l).

It is intensively metabolized in the liver. The main metabolite is an inactive derivative of carboxylic acid and makes up about 85% of the initial substance circulating in the plasma. Cmax of this metabolite in blood plasma after repeated doses of clopidogrel is about 3 mg / l and is observed approximately 1 hour after use.

The pharmacokinetics of the main metabolite are characterized by a linear relationship in the dose range of clopidogrel 50-150 mg.

Clopidogrel and the main metabolite are irreversibly bound to plasma proteins in vitro (98% and 94%, respectively). This bond remains unsaturated in vitro over a wide range of concentrations.

After oral use of C-labeled clopidogrel, approximately 50% of the dose is excreted in the urine and approximately 46% in the faeces within 120 hours. T1 / 2 of the main metabolite is 8 hours.

Compared with healthy young volunteers, the plasma concentration of the main metabolite is significantly higher in elderly patients (aged 75 years and older), while there are no changes in platelet aggregation and bleeding time.

In severe kidney diseases (creatinine clearance 5-15 ml/min), plasma concentrations of the main metabolite are lower than in moderate kidney diseases (creatinine clearance 30-60 ml/min) and in healthy volunteers.

Although the inhibitory effect on ADP-induced platelet aggregation was reduced compared to that in healthy volunteers, the bleeding time increased to the same extent as in healthy volunteers.

Pharmacodynamics

Inhibitor of platelet aggregation. Selectively inhibits the binding of adenosine diphosphate (ADP) to platelet receptors and the activation of the GPIIb/IIIa complex, thus inhibiting platelet aggregation. It also inhibits platelet aggregation caused by other agonists by blocking the increase in platelet activity by released ADP.

It does not affect PDE activity.

Clopidogrel irreversibly changes the ADP receptors on platelets, so platelets remain non-functional throughout their “life”, and normal function is restored as they are renewed (after approximately 7 days).

Clinical pharmacology

Antiplatelet agent.

Indications

Thrombotic complications in patients with myocardial infarction, ischemic stroke, and peripheral artery occlusion.

Thrombotic complications in acute coronary syndrome, unstable angina, non-Q-wave myocardial infarction.

Thrombotic and thromboembolic complications, including stroke, in atrial fibrillation (atrial fibrillation).

Contraindications

Acute bleeding (including peptic ulcer or intracranial hemorrhage), severe liver failure, pregnancy, lactation (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to clopidogrel.

Clopidogrel should be used with caution if there is an increased risk of bleeding due to trauma, surgery, or hemostatic disorders. For planned surgical interventions (if the antiplatelet effect is undesirable), clopidogrel should be discontinued 7 days before surgery.

Clopidogrel should be used with caution in patients with severe hepatic impairment, in which hemorrhagic diathesis may occur.

Side effects

From the side of the blood coagulation system: often-bleeding; infrequently-increased bleeding time.

From the digestive system: very often – gastrointestinal bleeding, diarrhea, abdominal pain, dyspepsia; infrequently-gastric and duodenal ulcers, vomiting, nausea, constipation, bloating; rarely – retroperitoneal hemorrhage; very rarely – gastrointestinal bleeding and retroperitoneal hemorrhage with fatal outcome, pancreatitis, colitis (including ulcerative colitis or ulcerative colitis). lymphocytic colitis), stomatitis, acute liver failure, hepatitis, abnormal liver function indicators.

From the hematopoietic system: infrequently-thrombocytopenia, leukopenia, eosinophilia; rarely-neutropenia, including severe neutropenia; very rarely-thrombotic thrombocytopenic purpura, aplastic anemia, pancytopenia, agranulocytosis, severe thrombocytopenia, granulocytopenia, anemia.

Nervous system disorders: infrequently-intracranial hemorrhage (several fatal cases have been reported), headache, paresthesia, dizziness; very rarely-impaired taste perception, hallucinations, confusion.

From the sensory organs: infrequently-eye hemorrhages (conjunctival, in the tissues and retina of the eye); rarely-vertigo.

From the cardiovascular system: very rarely-vasculitis, decreased blood pressure.

From the respiratory system: often-nosebleeds; very rarely-bleeding from the respiratory tract (hemoptysis, pulmonary bleeding), bronchospasm, interstitial pneumonia.

Immune system disorders: very rare – serum sickness, anaphylactoid reactions.

From the skin and subcutaneous tissues: often-subcutaneous bruising; infrequently-rash, pruritus, purpura (subcutaneous hemorrhage); very rarely – bullous dermatitis (toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme) angioedema, erythematous rash, urticaria, eczema, lichen planus.

Musculoskeletal disorders: very rare – muscle and joint hemorrhages, arthritis, arthralgia, myalgia.

From the urinary system: infrequently-hematuria; very rarely-glomerulonephritis, increased creatine concentration in the blood.

Other: often-bleeding from the site of vascular punctuation; very rarely-fever.

Interaction

When used concomitantly with NSAIDs (including naproxen), the risk of gastrointestinal bleeding increases.

When used concomitantly with acetylsalicylic acid, the antiplatelet effect may be enhanced.

Since clopidogrel can inhibit the activity of the CYP2C9 isoenzyme, when used concomitantly with drugs that are metabolized with the participation of this isoenzyme (including phenytoin, tolbutamine), an increase in their plasma concentrations cannot be excluded.

How to take, course of use and dosage

Take orally 1 time/day. The initial and maintenance dose is 75 mg / day. The loading dose is 300 mg / day.

Overdose

Prolongation of the bleeding time and subsequent complications in the form of the development of bleeding.

Special instructions

If there are symptoms of excessive bleeding (bleeding gums, menorrhagia, hematuria), a study of the hemostatic system (bleeding time, platelet count, tests of platelet functional activity) is indicated. Regular monitoring of laboratory parameters of liver functional activity is recommended.

Use with caution concomitantly with warfarin, heparin, NSAIDs, and for a long time – with acetylsalicylic acid, as currently the safety of such use has not been definitively established.

The effect of clopidogrel on the ability to drive vehicles and manage mechanisms has not been established.

Active ingredient

Clopidogrel

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Heart Attack Prevention, Stroke Prevention, Thrombosis Prevention