ალიმენტური ტრაქტი და მეტაბოლიზმი
სისტემური გამოყენების ინფექციის საწინააღმდეგო
სისხლი და სისხლ-წარმომქმნელი ორგანოები
სამომავლოდ დაგეგმილი პროდუქტები
Blood and Blood Forming Organs
Film coated tablet contains active ingredient: clopidogrel (as bisulphate) 75
PHARMACODYNAMICS. Lopigrol - antiaggregatory agent that has a coronary
vasodilating effect. It blocks selectively and nonreversibly the binding of
adenosindiphosphat (ADP) to thrombocyte receptors, inhibits its activation and
reduces a quantity of functioning ADP-receptors, prevents sorption of fibrogen
and inhibits a thrombocyte aggregation. It decreases a thrombocyte aggregation,
caused by other agonists due to the blockade of ADP released thrombocyte
activity increase not effecting on the activity of phosphodiesterase.
Thrombocyte aggregation inhibition can be seen in 2 h after a single dose intake
of the preparation (40% inhibition). At re-application an effect strengthens and
a stable state is attained in 3-7 days of treatment (up to 60% inhibition).
Thrombocyte aggregation and bleeding time returns to the initial level as
thrombocytes renew, that is in 5-7 days after discontinue the application of
Lopigrol. It prevents the development of aterothrombosis in the presence of
atherosclerotic vascular damage not depending on the vascular process
localization (cerebrovascular, cardiovascular or peripheral lesions).
PHARMACOKINETICS. At oral application it has a good absorption and is
characterized by high bioavailability. Time to Cmax is about 1 h. Clopidogrel is
a precursor of an active substance. It is biotransformed in liver with active
metabolite - thiol-derivative formation, that is formed by oxidation of
clopidogrel in 2-oxo- clopidogrel and the next hydrolysis. An active metabolite
is not found in plasma. The half- life period of circulating metabolite is 8
hours after the acute and repeated administration. It removed in urine (about
50%) and faeces (about 46%).
The prophylaxis of ischemic disturbances in patients with franc atherosclerosis,
- after myocardial infarction, ischemic stroke or recently diagnosed disease of
- at acute coronary syndrome without ST segment elevation (un stable angina or
myocardial infarction without pathologic wave Q) in combination with
- at acute coronary syndrome with ST segment elevation (acute myocardial
infarction) in combination with acetylsalicylic acid, receiving drug treatment,
- microcirculation disturbances of any type in content of complex therapy.
- hepatic failure of heavy degree;
- acute bleeding (for example, peptic ulcer or intracranial hemorrhage);
- hypersensitivity to the components of the preparation;
- children and teens under 18 years old.
From blood coagulation system: gastrointestinal bleeding, hemorrhagic stroke.
From hemopoietic system: neutropenia, thrombocytopenia.
From digestive system: abdominal pain, flatulence, gastritis, constipation,
peptic ulcer, diarrhea.
Dermatological reactions: skin rash, itch.
DOSAGE AND ADMINISTRATION:
For prophylaxis of ischemic disturbances in patients after myocardial infarction,
ischemic stroke and diagnosed disease of peripheral arteries in adults (including
elderly patients) it is prescribed orally in dose 75 mg 1 time/day independently
of the meal intake. The treatment should be started independently in term from
several days up to 35 days after myocardial infarction with pathologic wave Q
and from 7 days up to 6 months - after ischemic stroke.
At acute coronary syndrome without ST segment elevation (unstable angina or
myocardial infarction without wave Q) the treatment should be started with
single loading dose 300 mg, then to continue the drug administration in dose of
75 mg 1 time/day (with co-prescription of acetylsalicylic acid in dose of 75-325
mg/day). Because acetylsalicylic acid administration in large dose is
accompanied by high risk of bleeding, the recommended dose must be not higher
than 100 mg. The treatment course is up to 1 year.
At acute coronary syndrome with ST segment elevation (acute myocardial
the preparation is prescribed in dose of 75 mg 1 time/day with use of initial
in combination with acetylsalicylic acid; in combination or without
thrombolitics. For the
patients older than 75 years old the treatment
with clopidogrel must be carried out without use
of loading dose. A combination therapy is started
as soon as possible after the symptoms
appearance and it continues minimum during a 4
weeks-period. Maximum effect is noted in 3
months of the drug administration.
15 tablets in a blister.
1 blister together with enclosed leaflet in a carton box.