PLATEX 75mg Medochemie tablets prevent arterial thrombosis (3 blisters x 10 tablets)

Mechanism of action

Clopidogrel is a precursor that inhibits platelet gathering depending on the metabolism of the liver into clopidogrel metabolic metabolites.

Clopidogrel is oxidized into intermediate metabolites, 2-oxo-clopidogrel by isenzyme cytochrom P450, which is regulated by CYP3A4, CYP2C19, CYP1A2 and CYP2B6; After that, this intermediate conversion is converted into an active thiol metabolite.

Clopidogrel is a selective inhibitor of adenosin diphosphate (ADP), clopidogrel's active metabolic metabolites selectively and not compete to the P2Y12 position of ADP receptor on platelet surfaces, thus inhibiting ADP's attachment to the receptor and leading to the inhibition of Glycoprotein GPIIB/IIIII Attached platelet fibrinogen inhibits platelet gathering.

Pharmaceutical effect

The repeated dose of Clopidogrel 75 mg/day, inhibiting platelet training effects because ADP appears on the first day of treatment and reaches 40-60% inhibition at a stable level of about 3-7 days; After stopping the drug, platelet training and bleeding time return to the original level within 5 days.

Safety and clinical effectiveness

Clopidogrel's safety and clinical effectiveness in preventing ischemic disasters in the blood vessels have been determined in 5 studies to compare the double blindness involved in more than 88,000 patients: Caprie research comparison clopidogrel with acetylsalicyclic acid and other studies such as Cure, Clarity, Commit and Active-A comparison clopidogride.

In these studies, the preparation included in combination with acetylsalicylic acid and other standard therapies.

Dynamic pharmacokinetics

absorption

Clopidogrel is quickly absorbed quickly and not completely through oral. After taking the dose of Clopidogrel 75mg, the average peak concentration in the plasma of clopidogrel at 2 hours after drinking is very low (2.2-2.5 ng/ml).

Based on the excretion through the urine of metabolites of clopidogrel, the absorption reaches at least 50% of oral dose.

transformation

Clopidogrel is metabolized mainly in the liver by enzyme esterase into inactive metabolites and by the cytochrom P450 system into active thiol metabolites.

Clopidogrel converts into carboxylic acid derivatives by enzyme esterase, which is an inactive metabolic substance that accounts for the majority of drugs circulating in plasma (about 85%). The peak concentration of plasma of this metabolic substance is approximately 3 mg/l about 1 hour after taking Clopidogrel 75 mg.

Clopidogrel is oxidized to 2-oxo-clopidogrel by isenzyme cytochrom P450 is regulated by CYP3A4, CYP2C19, CYP1A2 and CYP2B6, then continued metabolism into active metabolites, but this substance is very unstable if separated from blood; The peak concentration of plasma of the thiol metabolites has the activity of clopidogrel to reach about 30-60 minutes after drinking Clopidogrel 75 mg.

distribution

Introin addiction, clopidogrel and non -active metabolites inversely connect with human plasma proteins are 98% respectively with clopidogrel and 94% for main metabolites and cohesion is not saturated in a wide range of concentration.

Elimination

When using Clopidogrel has 14C marking in humans, about 50% of oral doses are eliminated in the urine and nearly 46% excreted in the feces for about 120 hours after taking the drug. After taking a single dose of Clopidogrel 75 mg, Clopidogrel's sale time is about 6 hours after taken. After taking the single dose and the repeated dose of Clopidogrel 75 mg, the sale time of clopidogrel of non -activated metabolites is about 8 hours after taken.

Children and young people under 18 years of age: There is no data on the safety and effectiveness of the drug for patients under 18 years old.

Patients with renal failure: Experience in treatment is limited in patients with renal failure.

Patients with liver failure: Experience in treatment is limited in patients with liver failure may have organs.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose?

overdose

Overdose due to clopidogrel can cause prolonged bleeding time and complications of bleeding. The overdose symptoms of clopidogrel are vomiting, fatigue, shortness of breath, gastrointestinal bleeding.

Management

There is currently no specific antidote to Clopidogrel's pharmacological activity. If there is bleeding, platelet transmission to antagonistic pharmacological effects of clopidogrel.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

immune system disorders:

Common: gastrointestinal bleeding, diarrhea, abdominal pain, indigestion.

Periodically monitor the parameters of signs of anemia, hemoglobin, hematocrit during clopidogrel treatment.

Replacement of emergency plasma in case of thrombocytopenia.

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

Be cautious when using

bleeding and blood disorders

Due to the risk of hemorrhage and side effects on hematology, in the course of treatment, if there are clinical symptoms suggesting bleeding, it is necessary to quickly perform blood cell count or appropriate tests.

Like other anti-platelet drugs, should be careful to use clopidogrel in patients at risk of bleeding such as injury, surgery or other pathological states and in patients who are taking acetylsalicylic acid, heparin, Glycoprotein IIB/IIIA inhibitors or non-steroid anti-inflammatory drugs including COX-2 inhibitors or Serotonin Serotonin inhibitors.

Patients should be closely monitored any signs of hemorrhage including hidden bleeding, especially in the first few weeks of treatment or after performing invasive procedures in the heart or surgery. It is not recommended to use clopidogrel with oral anticoagulant drugs because this combination can enhance bleeding.

Because Clopidogrel extends the bleeding time, it should be used carefully when used for patients at risk of bleeding caused by trauma, surgery or other pathological conditions. If the patient needs surgery without wanting to affect the anti -platelet effect, the patient needs to stop using Clopidogrel 7 days before the surgery. Patients should notify the doctor or dentist about being taking clopidogrel and other drugs before making an appointment.

Because Clopidogrel extends the bleeding time, caution in patients with injury tends to bleed (especially stomach bleeding and intraocular hemorrhage).

Patients should know that the use of Clopidogrel alone or in combination with acetylsalicylic acid for a long time, it is often necessary to stop taking the drug when bleeding appears and should notify abnormal bleeding for the doctor.

Platelets (TTP)

The plateletal hemorrhage has been recorded but it is rare after using clopidogrel, sometimes only after a short time of taking the drug; And this phenomenon is manifested by a decrease in the number of platelets accompanied by small blood cell anemia or nervous manifestations, renal or fever dysfunction.

Plateletal hemorrhage committee is a life -threatening situation that requires immediate treatment including plasma extract methods.

Incidated bleeding disease

There have been reports on bleeding disease after using clopidogrel. Patients are diagnosed with bleeding diseases that should be treated with specialized measures and should stop using clopidogrel.

stroke due to ischemia

Because there is no data, Clopidogrel should not be used for patients with stroke due to acute ischemia (less than 7 days).

Patients with renal failure

Due to not having much experience using clopidogrel in patients with renal failure, it is cautious when using clopidogrel for these patients.

Patients with liver failure

Contraindicated to use clopidogrel for patients with severe liver failure.

excipients contain lactose

Because Platarex 75mg contains lactose, patients have genetic problems in tolerance of galactose, lactase deficiency or absorbent glucose-galactose should not use this drug.

excipients lecithin

Because the drug contains lecithin, the patient is hypersensitively to peanuts or soy should not use this drug.

The impact of drugs on drivers and operating machinery

Clopidogrel does not affect or negligible effect on driving and operating machinery.

used for pregnant and lactating women

pregnancy:

Animal studies do not show harmful effects related to pregnancy, the development of embryos and fetuses, the development of the birth and after birth.

However, there are no adequate and controlled studies on pregnant women when using clopidogrel, so they only use clopidogrel for pregnant women when really necessary.

Breastfeeding period:

Animal studies have recorded clopidogrel and metabolites excreted in milk.

However, it is not known whether Clopidogrel has excreted into the mother's milk or not, so it is necessary to consider stopping breastfeeding during the use of clopidogrel or stop using clopidogrel depending on the degree of need to take the medication in the nursing mother.

Interactive drug

Oral anticoagulant drugs

It is not recommended to use clopidogrel with oral anticoagulic drugs (such as warfarin) because this combination can enhance bleeding.

Glycoprotein IIB/IIIA receptor inhibitors

Be cautious when used in combination with clopidogrel because it can increase the risk of bleeding due to trauma, surgery or other diseases.

Acetylsalicylic acid

Acetylsalicylic acid does not change the ability to inhibit platelet's platelet exercise through the adp of clopidogrel but clopidogrel increases the effectiveness of acetylsalicylic acid on platelet training through collagen.

However, combining with Acetylsalicylic acid 500 mg, twice a day with Clopidogrel 75 mg/day did not increase the meaning of prolonging bleeding time due to clopidogrel. Pharmacological interaction between clopidogrel and acetylsalicylic acid can occur and increase the risk of bleeding. Therefore, be careful when used in combination.

heparin

The use in conjunction with clopidogrel has shown not to affect the inhibition of platelet training due to clopidogrel.

Hematology interaction between clopidogrel and heparin is possible and increases the risk of bleeding. Therefore, be careful when used in combination.

fiber pills

Safety when used in combination with clopidogrel with specific fiber fiber pepper or non -specific fibrin has been evaluated in patients with acute myocardial infarction.

Clinically significant bleeding ratio is similar to only use of fibrinolytic medication and when using heparin in combination with acetylsalicylic acid.

Steroid anti -inflammatory drugs

In a clinical study conducted in healthy adults, when used in combination with clopidogrel with Naproxen, there is an increase in hidden gastric bleeding.

However, there is no interaction research between clopidogrel and all other nonsteroidal anti -inflammatory drugs, it is unclear whether this combination increases the risk of stomach bleeding.

Therefore, it should be cautious when used in combination with clopidogrel with nonsteroidal anti-inflammatory drugs including COX-2 inhibitors.

Serotonin Serial Inhibitors (SSRIs)

Due to the selective re -absorption inhibitors, serotonin acts on platelet aggregation and increases the risk of bleeding, should be cautious when used simultaneously with clopidogrel.

Other combined treatments

Clopidogrel is partially metabolized by cytochrom CYP2C19 into active metabolites, so the use of clopidogrel with CYP2C19 inhibitors such as omeprazole, esomeprazole, fluvoxamine, fluoxetine, moclobemide, voriconazole, fluconazole, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine, ticlopidine ciprofloxacine, cimetidine, carbamazepine, oxcarbazepine and chloramphenicol can reduce the concentration of drugs of metabolites that are active of clopidogrel and reduce platelet resistance; Therefore, it is not advisable to simultaneously use clopidogrel with average or strong CYP2C19 inhibitors.

There have been a number of clinical studies on the use of clopidogrel in combination with other drugs to observe the interaction of pharmacokinetics and pharmacokinetics. There is no clinical interaction with pharmacological significance when used in combination with clopidogrel with Atenolol, Nifedipine, or both Atenolol and Nifedipine.Clopidogrel's

pharmaceutical force is not significantly affected when used in combination with phenobarbital or estrogen.

Digital pharmacokinetics of Digoxin or Theophylline is not changed when combined with clopidogrel.

Stomach antacids do not change the absorption level of clopidogrel.

Data from Caprie research shows that Phenytoin and Tolbutamide can be safely combined with Clopidogrel.

In addition to the specific drug interactive information described above, no studies have been conducted on interactions between clopidogrel and some commonly used drugs in arterial thrombotic patients; However, patients who are included in clinical trials using clopidogrel have also been used in combination with other drugs including diuretics, beta blockers, yeast inhibitors, calcium antagonists, cholesterol lowering drugs, coronary relaxants, diabetes medicine (including insulin), anti -epileptic drugs and GPIIB/IIIA antagonistic drugs without any side effects.