Plogrel, pills 75 mg, 28 pcs.

Composition

Film-coated tablets 1 tablet contains clopidogrel hydrosulfate 100.8 mg, which corresponds to the content of clopidogrel 75 mg.

Pharmacological action

Plogrel is an antiplatelet agent. Selectively reduces the binding of adenosine diphosphate (ADP) to platelet receptors and activation of glycoprotein IIb/IIIa receptors under the action of ADP, weakening platelet aggregation.

Reduces platelet aggregation caused by other agonists, preventing their activation by free ADP, does not affect the activity of PDE. 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% suppression of aggregation) develops after 4-7 days of continuous administration at a dose of 50-100 mg / day. The antiplatelet effect persists for the entire period of platelet life (7-10 days).

Indications

Plogrel is an antiplatelet agent. Selectively reduces the binding of adenosine diphosphate (ADP) to platelet receptors and activation of glycoprotein IIb/IIIa receptors under the action of ADP, weakening platelet aggregation.

Reduces platelet aggregation caused by other agonists, preventing their activation by free ADP, does not affect the activity of PDE. 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% suppression of aggregation) develops after 4-7 days of continuous administration at a dose of 50-100 mg / day. The antiplatelet effect persists for the entire period of platelet life (7-10 days).

Use during pregnancy and lactation

Due to the lack of data, clopidogrel should not be used during pregnancy and lactation (breastfeeding)

Contraindications

severe hepatic insufficiency;

acute bleeding (including peptic ulcer or intracranial hemorrhage);

lactose intolerance, lactase deficiency and glucose / galactose malabsorption syndrome;

children and adolescents under 18 years of age (efficacy and safety of use have not been established);

pregnancy;

lactation period;

hypersensitivity to the components of the drug.

With caution should prescribe the drug for mild to moderate liver failure, chronic renal failure, pathological conditions that increase the risk of bleeding (including trauma, surgery), tendency to bleeding, simultaneously taking acetylsalicylic acid, warfarin, NSAIDs (including COX-2 inhibitors), heparin, inhibitors of glycoprotein IIb/IIIA, and hereditary decrease in the function of the isoenzyme CYP2C19.

Side effects

Bleeding is the most common reaction that occurs during the first month of taking the drug. Cases of severe bleeding have been reported in patients taking clopidogrel concomitantly with acetylsalicylic acid or clopidogrel with acetylsalicylic acid and heparin.

The frequency of side effects is determined according to the following criteria: very common (>1/10), common (>1/100 and 1/1000 and 1/10 000 and>>

Hematopoietic disorders: infrequently-thrombocytopenia, leukopenia, eosinophilia; rarely-neutropenia, including severe; very rarely-thrombotic thrombocytopenic purpura, anemia, including aplastic, pancytopenia, agranulocytosis, severe thrombocytopenia, granulocytopenia.

From the nervous system: infrequently-headache, dizziness, paresthesia, intracranial bleeding, including with a fatal outcome; very rarely-confusion, hallucinations.

From the sensory organs: infrequently – hemorrhage in the conjunctiva, retina; rarely-vertigo; very rarely-taste disorder.

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

From the side of the blood coagulation system: often-hematoma; very rarely-severe bleeding, bleeding from the surgical wound.

From the respiratory system: very often – nosebleeds; very rarely-bronchospasm, interstitial pneumonitis, pulmonary hemorrhage, hemoptysis.

From the digestive system: often – diarrhea, abdominal pain, dyspepsia, bleeding from the gastrointestinal tract; infrequently – stomach and duodenal ulcers, gastritis, vomiting, nausea, constipation, flatulence; rarely – retroperitoneal bleeding; very rarely – pancreatitis, colitis, including ulcerative or lymphocytic, stomatitis, acute liver failure, hepatitis, impaired liver function tests, bleeding from the liver Gastrointestinal tract with a fatal outcome.

Dermatological reactions: often-subcutaneous hemorrhage; infrequently-skin rash, pruritus, purpura; very rarely-erythematous rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, eczema, lichen planus.

Musculoskeletal disorders: very rare – hemarthrosis, arthritis, arthralgia, myalgia.

From the urinary system: infrequently-hematuria; very rarely-glomerulonephritis, hypercreatininemia.

Allergic reactions: very rarely – angioedema, urticaria, anaphylactic reactions, serum sickness.

From the side of laboratory parameters: infrequently-prolongation of bleeding time, violations of liver function tests, increased blood creatinine concentration.

Other: very rarely – increased body temperature.

Interaction

Concomitant administration of warfarin with clopidogrel may increase the intensity of bleeding, so the use of this combination is not recommended.

The use of glycoprotein IIb/IIIa inhibitors, acetylsalicylic acid, and heparin together with clopidogrel increases the risk of bleeding.

When used concomitantly with NSAIDs, the risk of bleeding may increase.

Concomitant administration with inhibitors of the CYP2C19 isoenzyme (for example, omeprazole) is not recommended.

The active metabolite of clopidorgel inhibits the activity of the CYP2C9 isoenzyme, resulting in increased plasma concentrations of phenytoin, tolbutamide, and NSAIDs.

How to take, course of administration and dosage

Taken orally, regardless of food intake.

To prevent thrombotic complications in patients with myocardial infarction, ischemic stroke or peripheral arterial occlusion,75 mg is prescribed 1 time/day. In patients with myocardial infarction, treatment can be started from the first days to the 35th day of myocardial infarction, and in patients with ischemic stroke-in the period from 7 days to 6 months after the ischemic stroke.

To prevent thrombotic complications in acute coronary syndrome without ST segment elevation (unstable angina, non-Q wave myocardial infarction), start with a single loading dose of 300 mg, and then take 75 mg/day (in combination with acetylsalicylic acid in doses of 75-325 mg/day, the recommended dose is 100 mg/day). The maximum beneficial effect occurs after 3 months. The course of treatment is up to 1 year.

For the prevention of thrombotic complications in acute ST-segment elevation coronary syndrome (acute ST-segment elevation myocardial infarction)prescribe 75 mg / day with an initial single loading dose in combination with acetylsalicylic acid and thrombolytics (or without thrombolytics).

Combination therapy should be initiated as early as possible after the onset of symptoms and continued for at least 4 weeks.

In patients over 75 years of age, treatment with clopidogrel should begin without taking its loading dose.

In patients with a genetically determined decrease in the function of the CYP2C19 isoenzyme, the effect of clopidogrel may decrease. The optimal dosage regimen for these patients has not been established.

Experience with use in patients with chronic renal failure or moderate hepatic insufficiency is limited.

Overdose

Symptoms: prolonged bleeding time and subsequent hemorrhagic complications.

Treatment: if bleeding is detected, symptomatic hemostatic therapy is performed. No antidotes to the pharmaceutical activity of clopidogrel were found. If a rapid correction of prolonged bleeding time is required, platelet transfusion is recommended.

Special instructions

During treatment, it is necessary to monitor the parameters of the hemostatic system (APTT, platelet count, tests of platelet functional activity); regularly examine the functional activity of the liver.

Clopidogrel should be used with caution in patients at risk of severe bleeding from trauma, surgery, in patients with injuries prone to bleeding (especially gastrointestinal and intraocular), as well as in patients receiving acetylsalicylic acid, NSAIDs (including COX-2 inhibitors), heparin or glycoprotein IIb/IIIa inhibitors. Patients should be carefully monitored for any signs of bleeding, including latent bleeding, especially during the first weeks of use of the drug and/or after invasive heart procedures or surgical operations. Concomitant use of clopidogrel and warfarin is not recommended, as it may increase bleeding.

In the case of surgical interventions, if the antiplatelet effect is undesirable, the course of treatment should be stopped 7 days before the operation.

Patients should be warned that since it takes longer to stop the bleeding that occurs during the use of clopidogrel (in combination with or without acetylsalicylic acid), they should inform the doctor about each case of bleeding. Patients should also inform the doctor about taking the drug if they are going to undergo surgery.

After taking clopidogrel, thrombotic thrombocytopenic purpura was very rarely detected, sometimes after short-term use. This condition is characterized by thrombocytopenia and microangiopathic hemolytic anemia in combination with neurological signs, impaired renal function, or fever.

Thrombotic thrombocytopenic purpura is a potentially fatal condition that requires immediate treatment, including plasmapheresis.

Due to the lack of data, clopidogrel should not be recommended for acute (less than 7 days) ischemic strokes.

Experience with the use of clopidogrel in patients with impaired renal function is limited, so these patients should be prescribed clopidogrel with caution.

Patients with severe hepatic impairment should be aware of the risk of hemorrhagic diathesis, experience with the drug in patients with moderate hepatic impairment is limited, so these patients should be prescribed clopidogrel with caution.

Influence on the ability to drive motor vehicles and manage mechanisms

Clopidogrel may cause side effects from the nervous system (headache, dizziness, systemic dizziness, confusion, hallucinations), which may affect the ability to drive vehicles and engage in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25°C.

Shelf life

3 years

Active ingredient

Clopidogrel

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Prevention of thrombosis, Prevention of heart attacks and strokes

Weight

Weight: 18 gr.