Clopidolut 75mg Hasan prevents events due to atherosclerosis (3 blisters x 14 tablets)

Clopidogrel is a non -heparin platelet inhibitor.

Clopidogrel is a precursor. Clopidogrel must be metabolized by the CYP450 enzyme to create metabolites that inhibit platelet aggregation. Clopidogrel's active metabolites selectively inhibit the cohesion of adenosin diphosphate (ADP) on its P2Y12 receptor in platelets and thereby inhibit the activation through the ADP intermediaries of the Glycoprotein Gpilb/1LA complex, thus inhibiting the collection of platelets.

Due to the non-recovery cohesion, platelets are exposed to the active metabolites of Clopidogrel, which is affected until the end of the platelet life (about 7-10 days) and the usual rehabilitation of platelets takes place at the rate of new platelet formation.

Platelet collections, besides ADP, are also inhibited by choosing the amplification of platelet activation by ADP release.

The repeated dose of 75 mg Clopidogrel significantly inhibits the platelet aggregation due to the ADP from the first day, this inhibitor is increasing and reaching the stability level from the 3rd to Saturday. Platelet's collection and bleeding time gradually return to the basic value, within 5 days after stopping treatment.

Caprie research, comparison of clopidogrel blindness with acetylsalicylic acid (ASA), which has been conducted over 19,185 patients with atherosclerosis due to newly occurring myocardial infarction ( pharmacokinetic

absorption

After using a single dose and a repeated dose of 75 mg/day, Clopidogrel is quickly absorbed. The average plasma concentration of clopidogrel has not metabolized (2.2-2.5 ng/ml) reached about 45 minutes after taking the only dose of 75 mg. The minimum level of absorption is 50%, based on the excretion through the urine of the metabolites of clopidogrel.

Distribution

Clopidogrel and administrative metabolites have no active cohesion with human plasma proteins (98% with clopidogrel and 94% with metabolites).

Metabolism

Clopidogrel is metabolized mainly in the liver in two ways: on the one hand clopidogrel is hydrolyzed by enzyme esterase that produces non -derivative carboxylic acidic activity (accounting for 85% of plasma circulation substances in plasma), on the other hand, clopidogrel metabolism is regulated by many cytochrom P450 enzymes. Clopidogrel is converted first into 2-oxo-clopidogrel and then converted into a clopidogrel's derivative. This metabolism is regulated by CYP3A4, CYP2C19, CYP1A2 and CYP2B6. Thiol metabolites have fast and non -recovery activity with platelet receptors, thus prevent platelets.

Elimination

about 50% clopidogrel is excreted in urine and nearly 46% in the feces for about 120 hours after taking the drug. After taking a single dose of 75 mg, Clopidogrel has a half -hour selling time. The half -life of metabolites is about 30 minutes.

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Caution when using

due to the lack of data, Clopidogrel is not recommended in patients with stroke due to acute ischemia (less than 7 days).

Like other anti -platelets, Clopidogrel should be used carefully with patients at risk of bleeding due to trauma, just surgery (including tooth surgery) or other pathological conditions. If a patient is preparing for surgery without wanting to have a platelet resistance, Clopidogrel should stop using Clopidogrel 7 days before surgery.

Clopidogrel prolongs bleeding time and should be used with caution with patients with blood disorders, which can cause internal bleeding (bleeding in tissues, organs or joints, ...).

Patients should know when using Clopidogrel longer than usual, it is necessary to stop using when bleeding appears and should notify abnormal bleeding to the doctor.

Use carefully clopidogrel in patients with renal failure or liver failure.

Do not use Clopidogrel with warfarin (blood clotting drug) because it can increase the level of bleeding.

Because it is likely to increase the risk of bleeding, it is careful when used in combination with clopidogrel with ASA, nonsteroidal anti -inflammatory drugs, heparin or thrombolytic drugs (see drug interaction).

The ability to drive and operate machinery

Clopidogrel does not affect the ability to drive and operate machinery.

Pregnancy

There are no adequate and controlled studies on pregnant women. Therefore, do not use clopidogrel during pregnancy.

Breastfeeding period

There is no data on whether clopidogrel is excreted through breast milk or not. Should stop breastfeeding while being treated with clopidogrel.

Drug interaction

Warfarin

Do not use warfarin with clopidogrel because of increasing bleeding level.

acetylsalicylic acid (ASA)

ASA does not affect the ability to inhibit platelet gathering due to the ADP of Clopidogrel, but Clopidogrel increases the effect of Asa on platelet aggregation due to collagen. Simultaneous use of 500 mg ASA 2 times/day does not significantly increase the bleeding time due to clopidogrel. Pharmacological interaction between clopidogrel and Asa increases the risk of bleeding is possible. Therefore, it is necessary to be cautious when used in combination.

heparin

Used in combination with heparin does not affect platelet collection due to clopidogrel. Pharmacological interaction between clopidogrel and heparin increases the risk of bleeding that may occur. Therefore, caution when used combined.

Blood solubility

Safety when used in combination with clopidogrel, RTPA and heparin has been assessed in new patients with myocardial infarction. The clinical bleeding rate is similar to the observed ratio when using RT-PA and Heparin in combination with ASA.

Non -steroid anti -inflammatory drugs (NSAIDs)

In a clinical study in healthy people, when used in combination with clopidogrel with Naproxen, there is an increase in hidden stomach bleeding. However, because there is no interaction research between clopidogrel and other NSAIDs, it is unclear whether this combination increases the risk of stomach bleeding. Therefore, be careful when used combined, including COX-2 inhibitors.

digoxin or theophyllin

Pharmacokinetics are not changed when combined with clopidogrel.

Stomach antacids

Do not change Clopidogrel's absorption time.

Phenytoin and Tolbutamid

Data from Caprie study shows that Phenytoin and Tolbutamid can be combined safely with Clopidogrel.