Indications Plavix 75 mg:
For the prevention of atherothrombotic events in patients with:
• Ischemic stroke – is assigned to the interval from 7 days to 6 months later ischemic stroke;
Confirmation of the peripheral arteries by sickness;
• Myocardial infarction – the appointment of the product is justified in a few days (maximum – 35 days later myocardial infarction);
• Acute coronary syndrome without elevation segment S-T in combination with acetylsalicylic acid (myocardial infarction in the absence of pathological Q wave on the electrocardiogram, unstable angina).
Pharmacological Effects Plavix 75 mg:
The active substance Plavix – Clopidogrel. Clopidogrel – antiplatelet drugs, which selectively inhibits the binding of ADP (adenosine diphosphate) with platelet surface receptors. Due to this happening ADP-induced activation of the complex GP IIb / IIIa, which leads to inhibition of platelet aggregation. The same product causes other reactions that contribute to the suppression of platelet aggregation. Effect of the product on platelets – the irreversible, so these platelets throughout their lives will be unable to form aggregates. Restoration of aggregation properties of platelets occurs during the formation of new cells.
After local application of clopidogrel 75 mg per day is rapidly absorbed, but the content of the original substance in the blood plasma is small – only 2 hours there is a concentration that is available limit of measurement – 0.00025 mg / liter. Absorption of the product – within 50%, which can be traced to the level of metabolites are eliminated in the urine. The main metabolite – derived carboxy – has no pharmacological action and accounts for 85% of the original substance that circulates in the blood. The metabolism of clopidogrel is carried out in the liver. Cmax (approximately 3 ml / kg), carboxyl derivative in plasma observed after 60 minutes if you observe the condition of re-admission Plavix 75 mg.
Clopidogrel – prodrug. Active metabolite of a substance – thiol derivative – is metabolized by oxidation of clopidogrel in a 2-oksoklopidogrel. Cc posledstviidstvii 2 oksiklopidogrel hydrolyzed. Phase oxidation of clopidogrel is regulated mainly isoenzymes of cytochrome (P450 ZA4 and 2V6) and nekordinalno – enzymes 1A2, 1A1, and 2S19. Thiol derivative, selected in vitro, irreversibly and rapidly binds to receptors of platelets, which leads to irreversible inhibition of platelet aggregation. Kinetic studies of the main metabolite showed linear relationship with dose from 50 to 150 mg of clopidogrel (increase of plasma metabolites, depending on dosage).
In vitro revealed a reversible binding of the main circulating thiol metabolite and clopidogrel in human plasma proteins (respectively, 94 and 98%).
Half Life thiol metabolite – 8 hours as in the case of a lump sum, and in case of repeated use. Elimination: urine – 50%, with the intestines – 46%.
Plavix 75 mg Dosage and administration:
Plavix is taken inside. Adult dose – 75 mg / day, regardless of the meal. In patients younger than 18 years of efficacy and safety of the product is not installed.
Acute coronary syndrome without elevation segment S-T – starting dose – 300 mg one-time, in consequence of which a maintenance treatment in a dose of 75 mg / day in combination with acetylsalicylic acid, from 75 to 325 mg per day. The optimal duration of therapy is not established. The maximum effect is registered through 3 months of Plavix. Sometimes it shows the therapy for up to 1 year.
Prevention of ischemia in cases of later ischemic stroke, myocardial infarction and confirmed occlusive peripheral artery syndrome – 75 mg / day from the first days of the disease up to 35 days (myocardial infarction) and a 7-day to 6 months – later ischemic stroke.
Plavix 75 mg contra :
• Anaphylactoid reaction to the active substance or other components of Plavix;
• Age of 18 years;
• Pregnancy and breastfeeding;
• Lactase deficiency, a rare hereditary galactose intolerance, malabsorption syndrome, glucose-galactose;
• Acute bleeding;
• Severe liver disease.
Pregnancy Plavix 75 mg:
During pregnancy and lactation – a contraindication for taking Plavix.
Overdose Plavix 75 mg:
In case of overdose can be observed an increase in bleeding time. For fast recovery time of bleeding using platelet transfusions. No specific antidote.
Use with other drugs Plavix 75 mg:
Plavix is not recommended in combination with warfarin, since the likely increase in the intensity of bleeding.
Clopidogrel potentiates the effect of aspirin on collagen-induced reduction of platelet aggregation. Aspirin has no effect on the inhibitory effect on platelet aggregation klopidlogrela. The use of aspirin at a dose of 0.5 g 2 p / day does not cause clinically significant increase in bleeding time, which is extended by the action of Plavix. Do not set the security long-term treatment Plavix, in combination with aspirin. Nevertheless, taking a combination of both products did not cause any negative effects if the condition does not receive more than 1 year.
Clinical trials in healthy volunteers showed that the heparin dosage adjustment when taking Plavix is not required. However, the safety of combining Plavix with heparin has not been established, therefore co-administration of these products is carried out with caution. Heparin does not alter the antiaggregatory effect of clopidogrel.
Clinical trials in healthy volunteers showed that the combination of Plavix with naproxen increases the risk of hidden gastrointestinal bleeding. Have not been investigated combining Plavix with other nonsteroidal anti-inflammatory drugs in terms of risk of bleeding from the gastrointestinal tract. Appointment of receiving nonsteroidal anti-inflammatory products on Plavix therapy requires caution.
Revealed no clinically significant interaction between clopidogrel and nifedipine, or atenolol, or a combination of all three products.
Pharmacodynamics of clopidogrel is practically constant in the case of a combination with cimetidine, phenobarbital, or estrogens.
In combination with Plavix is not detected pharmacokinetic changes when taking theophylline and digoxin.
Antacids on the absorption of clopidogrel is not affected.
Studies of clopidogrel with human liver microsomes showed that Plavix can suppress the activity of a cytochrome – CYP 2C9. Because of this concentration of tolbutamide and phenytoin in the blood may be increased (since these products is metabolized by the enzyme cytochrome P450 CYP 2C9).
CAPRIE study has proven safe to use a combination of Plavix with tolbutamide and phenytoin.
In addition to the above products, and other clinical tests on the interaction of clopidogrel with products that are appointed for the treatment of atherothrombosis, have been conducted. Patients participating in clinical research Plavix, often received beta-adrenergic blockers, diuretics, angiotensin converting factor, antiepileptic drugs, lipid-lowering drugs, calcium channel antagonists, koronarolitiki, antidiabetic products (including insulin), hormone products, the antagonists of GP IIb / IIIa and other means. Clinically significant interactions in these combinations are not revealed.
Product Plavix 75 mg:
Tablets 75 mg, coated tablets. Shell film, pink. The tablets are slightly convex, circular, on a break tablet core can be seen in white on one side and engraved “75″, on the other – “1175″. Blister contains 14 tablets.
Plavix 75 mg composition:
Active ingredient: Clopidogrel Sulfate (as base).
Inactive ingredients: microcrystalline cellulose, 90 microns, macrogol 6000, mannitol, nizkozameschennaya hydroxypropylcellulose, Hydrogenated castor oil, carnauba wax.
Sheath: opadri 32K14834 (hypromellose, lactose, titanium dioxide, red iron oxide, triacetin).
Attention!
Before applying the medication Plavix should consult with your doctor.
Instruction is provided solely for information from Plavix.
