Clopidogrel, 75 mg 14 pcs

Clopidogrel is a specific and active inhibitor of platelet aggregation; it has coronarodilator effect.

Selectively reduces binding of ADP to receptors on platelets and activation of GPI Ib/IIIa receptors under the action of ADP. attenuates platelet aggregation. Reduces platelet aggregation caused by other agonists, preventing their activation by released ADP, does not affect phosphodiesterase (PDE) activity.

It irreversibly binds to platelet ADP receptors, which remain immune to ADP stimulation throughout the life cycle (about 7 days). Inhibition of platelet aggregation is observed 2 hours after administration (40% inhibition) of the initial dose of 400 mg.

The maximum effect (60% inhibition of aggregation) develops after 4-7 days of continuous use at a dose of 50-100 mg/day. The antiplatelet effect lasts for the whole period of platelet life (7-10 days).

In case of atherosclerotic vascular lesions it prevents the development of atherothrombosis regardless of the localization of the vascular process (cerebrovascular. cardiovascular or peripheral lesions).

Indications

Prevention of thrombotic complications:

Active ingredient

Composition

1 tablet contains clopidogrel hydrosulfate 97.875 mg, with clopidogrel 75 mg;

excipients:

Pregelatinized starch.

anhydrous lactose (anhydrous milk sugar),

macrogol (polyethylene glycol 6000).

Magnesium stearate.

Microcrystalline cellulose (pH 112),

Castor oil hydrogenated;

composition of the film coating:

Selecoat AQ-01673 (hypromellose (hydroxypropyl methylcellulose), macrogol (polyethylene glycol 400), macrogol (polyethylene glycol 6000), titanium dioxide, Ponceau 4 R dye-based aluminum varnish).

How to take, the dosage

Clopidogrel is taken orally, regardless of meals.

For prevention of ischemic disorders in patients after myocardial infarction, ischemic stroke and diagnosed peripheral arterial disease – 75 mg once daily. The treatment should be started within several days to 35 days after myocardial infarction and from 7 days to 6 months after ischemic stroke.

In acute coronary syndrome without ST-segment elevation (unstable angina pectoris or myocardial infarction without Q-wave), the treatment should be started with a single loading dose of 300 mg and then continued with 75 mg once daily (with simultaneous administration of acetylsalicylic acid 75-325 mg/day). Since the use of acetylsalicylic acid in high doses is associated with a high risk of bleeding, the recommended dose should not exceed 100 mg. The course of treatment is up to 1 year.

In acute ST-segment elevation myocardial infarction, the drug is indicated in a dose of 75 mg once daily with an initial loading dose in combination with acetylsalicylic acid with or without thrombolytics.

In patients aged over 75 years, treatment with clopidogrel should be performed without using a loading dose. Combination therapy should be started as soon as possible after the onset of symptoms and continued for at least 4 weeks.

Interaction

Co-administration of clopidogrel with warfarin is not recommended, since this combination may increase the intensity of bleeding.

The administration of glycoprotein IIb/IIIa inhibitors together with clopidogrel increases the risk of bleeding.

The use of nonsteroidal anti-inflammatory drugs together with clopidogrel increases the risk of bleeding.
Concomitant use of clopidogrel with CYP2C19 inhibitors (e.g., omeprazole) is not recommended.

No clinically significant pharmacodynamic interaction has been noted when using clopidogrel with atenololol, nifedipine, phenobarbital, cimetidine, estrogens, digoxin, theophylline, tolbutamide, antacids.

Special Instructions

During treatment it is necessary to monitor the parameters of the hemostasis system (activated partial thromboplastin time (APTT), platelet count, tests of platelet functional activity); regular examination of liver functional activity.

Clopidogrel should be used with caution in patients at risk of significant bleeding in trauma, surgery; patients receiving acetylsalicylic acid, nonsteroidal anti-inflammatory drugs (including COX-2 inhibitors), heparin or glycoprotein IIb/IIIa inhibitors. Patients should be closely monitored for any signs of bleeding, including hidden bleeding, especially during the first weeks of use and/or after invasive cardiac procedures or surgery. If surgical interventions are planned, treatment with clopidogrel should be discontinued 7 days before surgery.

Patients should be warned that it will take longer than usual to stop bleeding, so they should inform the physician about every bleeding event.

Rare cases of thrombotic thrombocytopenic purpura (TTP) have been reported after clopidogrel administration. This condition has been characterized by thrombocytopenia and microangiopathic hemolytic anemia combined with neurological symptoms, renal dysfunction or fever. The development of TTP is life-threatening and requires emergency measures, including plasmapheresis. Due to insufficient data, clopidogrel should not be prescribed in the acute period of ischemic stroke (in the first 7 days). The drug should be administered with caution in patients with impaired renal function.

Clopidogrel should be prescribed with caution in patients with moderate liver function impairment who may have hemorrhagic diathesis.

In patients with congenital galactose intolerance, glucose-galactase malabsorption syndrome and lactase deficiency should not take clopidogrel.

Contraindications

Side effects

Frequency: very frequently more than 1/10, frequently more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely more than 1/10000 and less than 1/1000, very rarely less than 1/10000, including isolated cases.

Hematopoietic organs: infrequent – thrombocytopenia, leukopenia, eosinophilia; rare – neutropenia, including severe; very rare – thrombotic thrombocytopenic purpura, anemia including aplastic, pancytopenia, agranulocytosis, severe thrombocytopenia, granulocytopenia.

Allergic reactions: very rare – anaphylactic reactions, serum sickness.

Nervous system disorders: infrequent – headache, dizziness, paresthesia, intracranial hemorrhage, including fatal; very rare – mental confusion, hallucinations, taste disorders.

Sensory organs: infrequent – bleeding into the conjunctiva, eyes, retina; rarely – vertigo.

Systems: frequently – hematoma; very rarely – severe bleeding, bleeding from the operating wound, vasculitis, decreased blood pressure.

Respiratory system: very common – nasal bleeding; very rare – bronchospasm, interstitial pneumonitis, pulmonary bleeding, hemoptysis.

The digestive system: frequently – diarrhea, abdominal pain, dyspepsia, gastrointestinal bleeding; infrequently – gastric and 12-duodenal ulcer, gastritis, vomiting, nausea, constipation, flatulence; rarely – retroperitoneal bleeding; very rarely – pancreatitis, colitis, including ulcerative or lymphatic edema.including ulcerative or lymphocytic, stomatitis, acute liver failure, hepatitis, abnormal liver function tests, gastrointestinal bleeding with lethal outcome.

Skin disorders: frequently – subcutaneous hemorrhage; infrequently – skin rash, itching, purpura; very rarely – angioedema, urticaria, erythematous rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, eczema, lichen planus red.

Motor system disorders: very rarely – haemarthrosis, arthritis, arthralgia, myalgia.

Urogenital system: infrequent – hematuria; very rare – glomerulonephritis, hypercreatininemia.
Local reactions: frequent – bleeding at the injection site.

Laboratory indices: infrequent – prolongation of bleeding time.

Others: very rare – fever.

Overdose

Symptoms: prolongation of bleeding time and subsequent complications.

Treatment: If bleeding occurs, appropriate therapy must be given. If rapid correction of prolonged bleeding time is necessary, platelet transfusion is recommended. There is no specific antidote.

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