Universal reference book for medicines
Product name: AGREGAL (AGREGAL)

Active substance: clopidogrel

Type: Antiaggregant

Manufacturer: NIZHFARM (Russia) manufactured by OB Obolenskoe (Russia)
Composition, form of production and packaging
The tablets covered with a film cover of
pink-cream color, round, biconcave;
Two layers are visible on the cross-section.
1 tab.

clopidogrel hydrogen sulfate 98 mg,

which corresponds to the content of clopidogrel 75 mg

Auxiliary substances: potato starch, lactose, microcrystalline cellulose, hypromellose (hydroxypropylmethylcellulose), macrogol 6000 (polyethylene glycol 6000), stearic acid, magnesium stearate.

The composition of the film shell: hypromellose (hydroxypropylmethylcellulose), titanium dioxide, macrogol 6000 (polyethylene glycol 6000), iron oxide red.

14 pcs.
- packings of cellular contour (1) - packs cardboard.
14 pcs.
- packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Antiaggregant.

Clopidogrel inhibits platelet aggregation due to selective blockade of binding of adenosine diphosphate (ADP) to its receptor on platelets and activation of the GPIIb / IIIa complex.
Inhibits platelet aggregation, caused by other agonists, by eliminating the activity of platelets liberated by ADP, does not affect the activity of PDE.
Changes in ADP-receptor platelets caused by clopidogrel are irreversible: platelets remain non-functional throughout the life span, the antiplatelet effect persists throughout this period.
Recovery of normal function occurs as platelets are refreshed (approximately 7 days later).
In the presence of an atherosclerotic lesion of the vessel, clopidogrel inhibits the development of atherothrombosis regardless of the localization of the vascular process (cerebrovascular, cardiovascular or peripheral lesions).

PHARMACOKINETICS

Suction

After ingestion of 75 mg clopidogrel, the drug is rapidly adsorbed from the digestive tract, but the concentration in the blood plasma is low and after 2 hours after intake it does not reach the measurement limit (0.025 μg / l), and the inhibition of platelet aggregation reaches 40%.
The maximum effect (60% inhibition of aggregation) develops after 4-7 days of constant drug intake at a dose of 98 mg / day (in terms of clopidogrel -75 mg / day).
C max metabolite after repeated use of clopidogrel at a dose of 75 mg is about 3 mg / l and is observed approximately 1 hour after taking the drug.

Distribution

Binding to plasma proteins of clopidogrel and its main metabolite: 98-94%, respectively.

Metabolism

The drug is metabolized in the liver.
The main metabolite is an inactive derivative of carboxylic acid.
Excretion

About 50% of the dose is excreted in urine and approximately 46% with feces (within 120 hours after administration).
T 1/2 of the main metabolite after a single and repeated administration of the drug - 8 hours.
Pharmacokinetics in special clinical cases

The concentration of the main metabolite in the blood plasma after taking clopidogrel 75 mg / day is lower in patients with severe kidney disease (KK 5-15 ml / min) compared with patients with moderate kidney disease (KC from 30 to 60 ml / min) and healthy persons.

C max of the drug in the blood plasma is higher in patients with cirrhosis, both after taking a single dose, and in an equilibrium state.
However, the safety and tolerability of the drug in such patients does not change with the use of 75 mg / day clopidogrel for 10 days.
INDICATIONS

Prophylaxis of ischemic disorders (myocardial infarction, stroke, peripheral arterial thrombosis, sudden vascular death) in patients with atherosclerosis, including:

- after a recent myocardial infarction;

- after an ischemic stroke;

- with diagnosed diseases of peripheral arteries;

- with acute coronary syndrome without ST segment elevation (unstable angina, myocardial infarction without Q wave), in combination with acetylsalicylic acid;

- during the operation of percutaneous coronaroplasty.

DOSING MODE

The drug should be taken orally 1 tablet 1 time / day, regardless of food intake.

Treatment should begin 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 acute coronary syndrome without ST segment elevation (unstable angina, myocardial infarction without Q-wave)
treatment should begin with the appointment of a single loading dose - 4 tab. of the drug Agregal (300 mg clopidogrel), then continue 1 tablet / day (75 mg clopidogrel) with simultaneous administration of acetylsalicylic acid at a dose of 75-375 mg / day.
The maximum rate of joint use of the drug Agregal and acetylsalicylic acid is 1 year (with a longer application safety has not been studied).

The choice of the scheme and duration of treatment with Agregal in the course of percutaneous coronaroplasty is determined by the doctor, depending on the type of stent and the timing of the operation.

SIDE EFFECT

From the coagulation system: gastrointestinal bleeding (2%; required hospitalization in 0.7% of cases);
sometimes - hematomas, hematuria, hemorrhages in the conjunctiva.
On the part of the hematopoiesis system: pronounced neutropenia (the number of granulocytes <450 / μl was observed at 0.04%);
severe thrombocytopenia (platelet count <80 000 / μL, observed in 0.2%).
On the part of the digestive system: abdominal pain, indigestion (constipation, diarrhea, nausea), gastritis;
rarely - changes in hepatic samples.
From the central nervous system and peripheral nervous system: headache, dizziness, paresthesia.

Dermatological reactions: skin rash, itching.

Allergic reactions: very rarely - bronchospasm, angioedema, anaphylactic reactions.

Other: thrombocytopenic purpura (1/200 000).

Other clinically significant side effects noted in a number of large international studies, with a frequency of> 0.1%, as well as all serious side effects are presented below, in accordance with the WHO classification.
Their frequency is defined as follows: often (> 1/100, but <1/10); sometimes (> 1/1000, but <1/100); rarely (> 1/10 000, but <1/1000).
From the side of the central nervous system and peripheral nervous system: often - headache, dizziness, paresthesia;
rarely - vertigo.
From the digestive system: often - diarrhea, abdominal pain;
sometimes - nausea, gastritis, flatulence, constipation, vomiting, peptic ulcer of the stomach and duodenum.
From the coagulation system of the blood: sometimes - lengthening the time of bleeding.

On the part of the hematopoiesis system: sometimes - leukopenia, a decrease in the number of neutrophils, eosinophilia, a decrease in the number of platelets.

Dermatological reactions: sometimes - rash and itching.

CONTRAINDICATIONS

severe hepatic impairment;

- Acute bleeding (eg, peptic ulcer or intracranial hemorrhage);

- Pregnancy;

- the period of lactation (breastfeeding);

- childhood;

- Hypersensitivity to the components of the drug.

With caution
should prescribe the drug to patients with an increased risk of bleeding (trauma, before surgery), moderate hepatic and / or renal failure (possibly the development of hemorrhagic diathesis).
PREGNANCY AND LACTATION

The use of the drug during pregnancy and during breastfeeding is contraindicated because of the lack of safety data.

APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be used in cases of kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated use of the drug in severe hepatic insufficiency.

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

APPLICATION FOR CHILDREN

Contraindicated: children's age.

SPECIAL INSTRUCTIONS

In case of combination of Agregal with acetylsalicylic acid, other NSAIDs, heparin, glycoprotein IIb / IIIa inhibitors or fibrinolytics, a blood test should be performed during the first week of treatment (APTT, number and functional activity of platelets).

The course of treatment with Agregal should be discontinued 7 days before the planned surgical intervention.

The patient should be warned that it is necessary to inform the doctor about each case of bleeding.

OVERDOSE

There have been no cases of overdose.

Treatment: transfusion of platelet mass.
There is no specific antidote.
DRUG INTERACTION

Simultaneous application of the drug Agregal with warfarin is not recommended, since it is possible to increase the intensity of bleeding.

The simultaneous use of Agregal with Ilb / IIIa glycoprotein inhibitors requires caution.

Acetylsalicylic acid does not change the inhibitory effect of the drug Agregal on ADP-induced platelet aggregation, but the Agregal drug increases the effect of acetylsalicylic acid on collagen-induced platelet aggregation.
Joint use of these drugs requires caution.
According to a clinical trial conducted on healthy individuals, clopidogrel does not change either the need for heparin or the action of heparin on blood coagulation.
The simultaneous use of heparin did not alter the inhibitory effect of clopidogrel on platelet aggregation. However, the safety of this combination has not yet been established and the simultaneous use of these drugs requires caution.
The safety of simultaneous application of clopidogrel, a recombinant tissue plasminogen activator (rt-PA) and heparin was investigated in patients with recent myocardial infarction.
The frequency of clinically significant bleeding was similar to that observed in the simultaneous use of rt-PA and heparin. The safety of the joint use of clopidogrel with other fibrinolytics has not yet been established and the simultaneous use of these drugs requires caution.
The simultaneous use of the drug Agregal with NSAIDs requires caution in connection with a possible increase in the risk of bleeding.

There was no clinically significant pharmacodynamic interaction with clopidogrel used with atenolol, nifedipine, phenobarbital, cimetidine, estrogen, digoxin, theophylline, phenytoin, tolbutamide and antacid agents, but there is evidence that clopidogrel inhibits the activity of one of the isoenzymes of COR2C9 and can alter concentration of drugs metabolized by CYP2C9 (including phenytoin, tolbutamide).

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 ° C.
Shelf life - 2 years.

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