Universal reference book for medicines
Product name: EGITROMB ® (EGITROMB ® )

Active substance: clopidogrel

Type: Antiaggregant

Manufacturer: EGIS Pharmaceuticals (Hungary)
Composition, form of production and packaging
Tablets coated with a
white or nearly white-colored film shell are round, biconvex, engraved with "E 181" on one side, without or almost no odor.

1 tab.

clopidogrel hydrogen sulfate 97.86 mg,

which corresponds to the content of clopidogrel 75 mg

Auxiliary substances: silicon microcrystalline cellulose - 198.2 mg (microcrystalline cellulose - 194.236 mg, silicon dioxide colloidal anhydrous - 3.964 mg), giprolase (with a low degree of substitution (L-HPC B1)) - 12 mg, hydrogenated castor oil - 12 mg.

The composition of the shell: opadray white YI-7000 - 10 mg (hypromellose - 6.25 mg, titanium dioxide - 3.125 mg, macrogol 400 - 0.625 mg).

7 pcs.
- blisters (2) - packs of cardboard.
7 pcs.
- blisters (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Antiaggregant drug.
Specific and active inhibitor of platelet aggregation. Selectively reduces the binding of adenosine diphosphate (ADP) to platelet receptors and the activation of GPI Ib / IIIa receptors under the action of ADP, thereby weakening platelet aggregation.
Reduces platelet aggregation, caused by other agonists, preventing their activation by released ADP, does not affect the activity of phosphodiesterase (PDE).

Irreversibly binds to ADP-receptor platelets, which remain immune to stimulation of ADP throughout the life cycle (about 7 days).
The inhibition of platelet aggregation is observed after 2 hours after administration (40% inhibition) of the initial dose. The maximum effect (60% suppression of aggregation) develops after 4-7 days of constant admission in a dose of 50-100 mg / day. Antiaggregant effect persists throughout the life span of platelets (7-10 days).
In the presence of an atherosclerotic lesion, the vessel interferes with the development of atherothrombosis regardless of the localization of the vascular process (cerebrovascular, cardiovascular or peripheral lesions).

PHARMACOKINETICS

Suction

Clopidogrel is quickly absorbed from the digestive tract after repeated administration of 75 mg / day.

Bioavailability is high.
However, the concentration of clopidogrel in the plasma is low and after 2 hours does not reach the measurement limit (0.025 μg / l).
Distribution

Binding to plasma proteins - 98-94%.

Metabolism

Metabolised in the liver.
The main metabolite is an inactive derivative of carboxylic acid, T max of which after repeated oral administration at a dose of 75 mg is achieved after 1 hour ( Cmax - about 3 mg / l).
Excretion

It is excreted by the kidneys - 50% and through the intestine with a fecal mass - 46% (within 120 hours after administration).

T 1/2 of the main metabolite after a single and repeated intake - 8 hours. Concentrations of kidney metabolites - 50%.

Pharmacokinetics in special clinical cases

The concentration of the main metabolite in the plasma after taking the drug at a dose of 75 mg / day is lower in patients with severe renal insufficiency (SC 5-15 ml / min) compared with patients with moderate renal insufficiency (KC from 30 to 60 ml / min) and healthy faces.

INDICATIONS

- prevention of atherothrombotic complications in adult patients with myocardial infarction (with a duration of several days to 35 days), ischemic stroke (with a duration of 7 days to 6 months) or occlusive disease of peripheral arteries;

- prophylaxis of atherothrombotic complications in adult patients with acute coronary syndrome with ST segment elevation with the possibility of performing thrombolytic therapy (in combination with acetylsalicylic acid);

- prevention of atherothrombotic complications in adult patients with acute coronary syndrome without ST segment elevation (unstable angina, myocardial infarction without Q wave), incl.
in patients undergoing stenting (in combination with acetylsalicylic acid);
- prevention of atherothrombotic and thromboembolic complications, including stroke, in atrial fibrillation in adult patients with at least one risk factor for vascular complications that can not take indirect anticoagulants and have a low risk of bleeding (in combination with acetylsalicylic acid).

DOSING MODE

The drug is taken orally, regardless of food intake.

Adults and elderly patients Egitromb ® are prescribed 75 mg once a day.

Treatment should be started within a few days to 35 days in patients after myocardial infarction and from 7 days to 6 months in patients after ischemic stroke .

In case of acute coronary syndrome without ST segment elevation (unstable angina, myocardial infarction without Q wave) , the preparation of Egithromb ® should be started with a single loading dose of 300 mg, and then continue taking 75 mg once a day in combination with acetylsalicylic acid (in a dose 75-325 mg / day).
Since the use of acetylsalicylic acid in higher doses is associated with an increased risk of bleeding, it is recommended to prescribe it in doses not exceeding 100 mg. Data from clinical trials indicate the possibility of using Egitromb ® for up to 12 months, and the maximum effect of therapy is noted by 3 months of use.
In acute myocardial infarction with elevation of the ST segment, Egitromb ® should be taken at a dose of 75 mg 1 time / day.
Treatment should be started with a loading dose and combined with taking acetylsalicylic acid and thrombolytic or without thrombolytics. The effectiveness of therapy lasting more than 4 weeks has not been studied.
Atrial fibrillation Egitromb ® should be taken 1 time / day at a dose of 75 mg.
In combination with the preparation Egitromb ® should start and then continue taking acetylsalicylic acid (75-100 mg / day).
Skipping the next dose

If less than 12 hours have passed after missing the next dose, the missed dose of the drug should be taken immediately, the following doses should be taken at the usual time.

If more than 12 hours have elapsed after missing the next dose, the next dose should be taken at the usual time (do not take a double dose).

Special patient groups

Patients with genetically determined reduced activity of the isoenzyme CYP2C19

The low activity of the isoenzyme CYP2C19 is associated with a decrease in the antiplatelet effect of clopidogrel.
The use of the drug at higher doses (600 mg - loading dose, then 150 mg - 1 time / day) in patients with a low activity of the isoenzyme CYP2C19 increases the antiplatelet effect of clopidogrel. However, currently, clinical trials that take into account clinical outcomes have not established an optimal dosage regimen for clopidogrel for such patients.
Older patients do not need a dose adjustment.

There is no experience of using the drug in children .

The experience of using Egitromb in patients with impaired renal function is limited.

The experience of using the drug in patients with liver diseases of moderate severity (in which there may be manifestations of hemorrhagic diathesis) is limited.

SIDE EFFECT

Bleeding is the most frequent reaction, most often it occurs during the first month of taking the drug.
Cases of severe bleeding have been reported in patients taking clopidogrel simultaneously with acetylsalicylic acid or clopidogrel with acetylsalicylic acid and heparin.
Determination of the incidence of adverse reactions: often (> 1/100, <1/10);
infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000).Within each class of frequency, undesirable effects are presented in order of decreasing severity.
From the coagulation system: often - a hematoma.

On the part of the hematopoiesis system: infrequently - an increase in bleeding time and a decrease in the number of platelets, leukopenia, neutropenia, eosinophilia;very rarely thrombotic thrombocytopenic purpura (TTP) (1/200 000 patients taking the drug), severe thrombocytopenia (platelet count? 30? 10 9 / L), agranulocytosis, granulocytopenia, aplastic anemia / pancytopenia, anemia.

From the central nervous system and peripheral nervous system: infrequently - headache, dizziness, paresthesia;
rarely - systemic dizziness; very rarely - confusion, hallucinations, eating disorders.
From the digestive system: often - gastrointestinal bleeding, diarrhea, abdominal pain, indigestion;
infrequently - hemorrhagic stroke, stomach ulcer, duodenal ulcer, gastritis, nausea, vomiting, constipation, bloating; very rarely - pancreatitis, colitis (including ulcerative or lymphocytic colitis), stomatitis, acute liver failure, hepatitis, impaired functional liver tests.
From the cardiovascular system: very rarely - vasculitis, arterial hypotension.

From the skin: rarely - skin itching;
very rarely - bullous dermatitis (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), erythematous rash, eczema, flat lichen.
Allergic reactions: infrequent - skin rash;
very rarely - hives, angioedema, serum sickness, anaphylactoid reactions.
On the part of the respiratory organs: very rarely - bronchospasm, interstitial pneumonitis.

From the musculoskeletal system: very rarely - arthralgia, arthritis, myalgia.

From the side of the urinary system: very rarely - an increase in serum creatinine, glomerulonephritis.

Other: very rarely - fever.

CONTRAINDICATIONS

hepatic failure of severe degree;

- active bleeding (peptic ulcer or intracranial hemorrhage);

- Pregnancy;

- lactation period (breastfeeding);

- age under 18 years (effectiveness and safety not proven);

- Hypersensitivity to the active substance or any auxiliary component of the drug.

With caution should be used in patients with moderate hepatic insufficiency, chronic renal failure, in pathological conditions that increase the risk of bleeding (including trauma, surgery), concurrent administration of acetylsalicylic acid, NSAIDs (including COX-2 inhibitors), warfarin, heparin and inhibitors of glycoprotein IIb / IIIa, low activity of the isoenzyme CYP2C19 (in such patients, when clopidogrel is used in recommended doses, less active metabolite of clopidogrel is formed and its antiagra is less pronounced
and therefore a higher incidence of cardiovascular complications is possible with clopidogrel at recommended doses in acute coronary syndrome or percutaneous coronary intervention than in patients with normal CYP2C19 isoenzyme activity).
PREGNANCY AND LACTATION

Clinical data on the use of Egitromb ® in pregnancy are absent, so do not prescribe clopidogrel during pregnancy.

Information on the isolation of clopidogrel with breast milk is not available, so the use of the drug during lactation is contraindicated.

APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be applied to the drug in chronic kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Caution should be applied to the drug with moderate hepatic insufficiency.

Contraindicated in patients with severe hepatic impairment.

APPLICATION FOR CHILDREN

Contraindication: age under 18 years (efficacy and safety not proven).

APPLICATION IN ELDERLY PATIENTS

Older patients do not need a dose adjustment.

SPECIAL INSTRUCTIONS

Caution should be used in patients with an increased risk of bleeding during trauma, surgery, in patients with injuries prone to bleeding (especially gastrointestinal and intraocular), as well as in patients receiving acetylsalicylic acid, NSAIDs (incl. h. COX-2 inhibitors), heparin or glycoprotein IIb / IIIa inhibitors.
Patients should be monitored carefully to identify any signs of bleeding, incl. especially during the first weeks of application of the drug and / or after invasive procedures on the heart or surgical operations. The simultaneous use of clopidogrel and warfarin is not recommended; possibly increased bleeding.
During the treatment period, it is necessary to monitor the parameters of the hemostasis system (APTT, platelet count, platelet functional activity tests);
regularly investigate the functional activity of the liver.
In the case of surgical interventions, if antiaggregant effect is undesirable, the course of treatment should be discontinued 7 days before the operation.

Patients should be cautioned that as the bleeding occurs after the use of clopidogrel (in combination with or without acetylsalicylic acid) requires more time, they should inform the doctor of every unusual bleeding event.
Patients should also inform the doctor about taking the drug if they are to be treated promptly before taking any new drug.
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 requiring immediate treatment, incl. with the use of plasmapheresis.
Because of lack of data, clopidogrel can not be recommended for acute (less than 7 days) ischemic stroke.

The experience of using clopidogrel in patients with impaired renal function is limited, therefore, this category of patients should be given caution with clopidogrel.

In severe violations of liver function, the risk of developing hemorrhagic diathesis should be considered.
The experience of using the drug in patients with moderate dysfunction of the liver is limited, so this category of patients should be administered with caution.
Impact on the ability to drive vehicles and manage mechanisms

The drug does not or does not significantly affect the ability to drive vehicles and mechanisms.

OVERDOSE

Symptoms: prolongation of the bleeding time is possible, which can lead to complications associated with bleeding.

Treatment: if it is necessary to quickly reduce the prolonged bleeding time, platelet transfusion can eliminate the effects of clopidogrel.
Antidotes of pharmacological activity of clopidogrel have not been found.
DRUG INTERACTION

Strengthens the antiaggregant effect of acetylsalicylic acid, heparin, thrombolytic agents, indirect anticoagulants, NSAIDs (including inhibitors of COX-2), increases the risk of bleeding from the digestive tract, so the simultaneous use of these drugs requires caution.

Care should be taken when using clopidogrel with glycoprotein IIb / IIIa inhibitors concurrently,
the risk of increased bleeding in trauma or surgical intervention increases in patients.
The simultaneous use of clopidogrel and warfarin is not recommended;
with the possibility of increased bleeding.
There was no clinically significant pharmacodynamic interaction in cases of simultaneous use of clopidogrel with atenolol, nifedipine, or a combination of atenolol with nifedipine.
In addition, the pharmacodynamic activity of clopidogrel did not change significantly with the simultaneous use of phenobarbital, cimetidine or estrogens.
The pharmacokinetics of digoxin or theophylline did not change with simultaneous administration of clopidogrel.

Antacid preparations do not affect the absorption of clopidogrel.

The study of human hepatic microsomes showed that the clopidogrel metabolite, related to carboxylic acids, can suppress the activity of the CYP2C9 isoenzyme.
This can increase plasma concentrations of drugs such as phenytoin, tolbutamide and NSAIDs, which are metabolized with the participation of the CYP2C9 isoenzyme.The use of phenytoin and tolbutamide together with clopidogrel is safe.
Because
Clopidogrel is metabolized prior to the formation of its active metabolite in part by the CYP2C19 system, the use of drugs inhibiting this system can lead to a decrease in the concentration of the active metabolite clopidogrel. Simultaneous use of strong or moderate inhibitors of the CYP2C19 isoenzyme (eg, omeprazole) should be avoided with clopidogrel. If proton pump inhibitors are to be used concurrently with clopidogrel, a drug with the least inhibition of the CYP2C19 isoenzyme, such as pantoprazole, should be given.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children at a temperature of no higher than 25 ° C.
Shelf life - 5 years.
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