Sagason 75 Celogen Pharma medicine for myocardial infarction, stroke (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Clopidogrel

Ingredient

Composition information	Content
Clopidogrel	75mg

Uses

indications

Sagason 75 celogen drugs are indicated in the following cases:

Preventive prevention of thrombosis disorders such as myocardial infarction, stroke and peripheral artery disease.

Control and contemplation in patients with atherosclerosis have a new stroke, new myocardial infarction or peripheral artery disease. Clopidogrel is a precursor (Prodrug) with the effect of inhibiting platelet gathering depending on the metabolism in the liver into active thiol metabolites.

Biological metabolism occurs through 2 steps: Clopidogrel is initially oxidized into intermediate metabolites, 2-oxo-clopidogrel, then converted into active thiol metabolites. The metabolic path associated with some isenzyme cytochrom P450 (such as CYP3A4, CYP2C19, CYP1A2, CYP2B6).

Clopidogrel is an adenosin diphosphate receptor inhibitor (ADP Receptor), the active metabolitus of clopidogrel selectively and does not compete with low affinity into the P2Y12 position of the ADP receptor on the platelet surface. Therefore will inhibit the attachment of ADP to the receptor and lead to inhibition of Glycoprotein GPIIB/IIIA platelet complex. This complex is necessary to attach fibrinogen - platelets to inhibit platelets.

Clopidogrel also inhibits solid particles (containing ADP, Calcium and Serotonin) platelets) through ADP intermediaries and Alfa beads (containing fibrinogen and thrombospondin), these particles contain substances that enhance platelet aggregation. Platases are in contact with Clopidogrel to maintain the end of the life of platelets (7 - 10 days). Unlike aspirin, clopidogrel and ticlopidin inhibit non -active platelet training cyclooxygenase to prevent the synthesis of prostaglandin and thromboxan a.

When taking daily dose clopidogrel 75mg, the inhibitory effect of platelets 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 aggregation and bleeding time return to the original level within 5 days.

Dynamic pharmacokinetics

Clopidogrel absorbed quickly and incomplete oral, absorbing at least 50% of oral dose. When taking the dose of 75 mg clopidogrel, the clopidogrel concentration in plasma at 2 hours after taken very low, usually under the quantitative limit (0.00025 mg/liter). The highest concentration of the main metabolites in the plasma of clopidogrel (carboxylic acid conductor is not active for platelet aggregation) is 3 mg/liter at 1 hour after drinking.

Clopidogrel is a precursor and is metabolized through the liver, most of which into carboxylic acid derivatives are inactive metabolites. Metabolized by liver by isenzyme cytochrome P450 including CYP3A4, CYP2C19, CYP1A2, CYP2B6. The active metabolite is a thiol derivative, but it is very unstable if separated from the plasma. Clopidogrel and main metabolites associated with high -ratio plasma proteins (98% and 94%).

Clopidogrel and metabolites are eliminated through urine and feces. About 50% of oral doses are eliminated through urine and 46% excreted in feces. The sale time of metabolites is 8 hours after single dose and repeat dose.

The pharmacokinetics research of the main metabolite shows that Clopidogrel's bioavailability is not affected by food.

Genetic pharmacological pharmacological: The polymorphic gene of CYP2C19 can affect the response to the pharmacokinetics and pharmacokinetics of Clopidogrel. CYP2C19 is involved in creating both active metabolites and intermediate metabolites 2 - Oxo - Clopidogrel. Pharmacokinetics and platelet resistance of metabolites are active of clopidogrel when quantified by experiments to stop platelet exercises from the body varies depending on the genotyps of CYP2C19. The genetic variants of other CYP450 enzymes can also affect the active metabolites of clopidogrel.

Alen CYP2C19*1 corresponds to adequate metabolic function, while allules CYP2C19*2 and CYP2C19*3 have no function. The percentage of people carrying CYP2C19 alenes reduces the function in the general population depends on the race. Most people with poor skin metabolism (85%), Asia (99%) have alleles reducing CYP2C19*2 and CYP2C19*3. Other alleles are less functional and less common. Research shows that a group of patients with poor metabolism and intermediaries with a high rate of cardiovascular events (death, myocardial infarction and stroke) or thrombosis due to stent are compared to people with strong metabolism.

Before taking Sagason 75 Celogen Pharma medicine for myocardial infarction, stroke (3 blisters x 10 tablets)

How to use

oral medication.

Dosage

The dose is calculated by clopidogrel, paying attention to genetic pharmacology in poor metabolic people.

daily dose in adults

75 mg/day.

after myocardial infarction, stroke; Peripheral artery disease

75 mg/day, drink 1 time.

acute coronary syndrome

Unstable angina, myocardial infarction has no difference: If the patient is selected to intervene through the skin, the initial dose is 300 mg before intervention for at least 2 hours, then 75 mg/day (in combination with 75 - 325 mg Aspirin/day). If the patient cannot use aspirin, the first dose of Clopidogrel 300 - 600 mg before intervention for at least 24 hours, then 75 mg/day, lasts at least 12 months.

Myocardial infarction has an ST difference: If the patient is conservative, drink Clopidogrel 75 mg/day (in combination with Aspirin 75 mg - 162 mg/day). Treatment period

Put coronary artery stent in patients who are not at high risk of bleeding or clopidogrel tolerance: The ideal treatment time is 12 months after the stent release slow drug, daily dose of treatment. The minimum treatment period of 1 month if the ceiling stent is placed, 3 months with a stent release syrolimus and 6 months if the stent releases Paclitaxel. If the early treatment is stopped, it can lead to thrombosis in the stent and myocardial infarction (causing myocardial infarction and/or death).

Dosage for patients with renal failure, the elderly

Adjusting the dose in patients with renal failure, the elderly is not necessary.

Dosage for children

There is no information about the optimal dose for children. The information about the dose in children is very limited, it is necessary to continue studies. Research shows that children

For children> 2 years old, no optimal dose is recommended. However, not higher doses of adults. The initial dose can be used 1 mg/kg, then adjusted depending on the response.

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? The symptoms of clopidogrel overdose are vomiting, fatigue, shortness of breath, and gastrointestinal bleeding.

Overdose of clopidogrel by platelet transmission to antagonistic pharmacological effects of clopidogrel.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

When using Sagason 75 celogen, you may experience unwanted effects (ADR).

Very common, 3/100

Digestive: digestive disorders, abdominal pain, vomiting, anorexia, gastritis, constipation.

cardiovascular: chest pain, angioedema, hypertension.

Central nervous system: headache, dizziness, fatigue, human pain.

skin: itching, erythema.

Endocrine and metabolism: Hyper cholesterol.

Urinary tract infections.

Hematology: Bleeding, erythema, nosebleeds.

Liver: Liver function abnormalities.

muscle and bone: joint pain, back pain.

Respiratory: Difficulty breathing, rhinitis, bronchitis, upper respiratory infections, influenza syndrome.

Common, 1/100

Cardiovascular: Atrial fibrillation, heart failure, tachycardia, fainting.

Neurology: fever, insomnia, dizziness, anxiety. skin: indigo.

Endocrine and metabolism: hyperuricemia, gout.

digestive: constipation, first -bleeding, vomiting. urinary: Cystic inflammation.

Hematology: Anemia, bleeding.

Neurosurgery: cramps, nerve pain, muscle weakness.

eyes: cataract, conjunctivitis.

Uncommon, 1/1000

These ADRs are rare but serious, can be life-threatening: Acute liver failure, loss of granulocytes, allergies, anaphylaxis, rash, angioedema, anemia, hyperlemin blood bilirubin, bronchospasm, chromatographic roses, pleural bleeding, hepatitis, interstitial pneumonia, intra-intraucological bleeding, local anemia necrosis, intraocular bleeding, pancreatitis, reduction Skin poisoning, vasculitis, severe neutropenia.

Instructions on how to handle ADR

Periodically monitor parameters of signs of anemia, hemoglobin, hematocrit during clopidogrel treatment. Replace rescue plasma in case of thrombocytopenia.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

contraindicated

Sagason 75 celogen drugs in the following cases:

Patients are allergic to clopidogrel or any ingredient of the drug.

Expression of pathological bleeding (e.g. stomach - duodenal ulcer, intracranial bleeding).

Caution when using

by Clopidogrel extends the bleeding time, should be cautious when used for patients at risk of bleeding due to trauma, surgery, or pathological bleeding such as peptic ulcer, intraocular bleeding, intracranial bleeding. If the patient needs surgery, the medication must be stopped in advance.

When suspected hemorrhage or hematological disorders during clopidogrel treatment, the number of red blood cells and other appropriate tests must be tested.

Plateletal hemorrhage (within the first 2 weeks of treatment) occurred in some cases leading to death, in the event of a plateletal hemorrhage that needs to be replaced with emergency plasma.

In patients with a history of transient oral stroke or stroke, there is a risk of recurrence of ischemic anemia, if combined with prophylaxis with Aspirin in combination with clopidogrel, it increases effectively compared to using clopidogrel but also increases the risk of large bleeding.

The risk of gastrointestinal bleeding increases when using clopidogrel, so be cautious when used for patients with damage in the gastrointestinal tract tends to bleed like ulcers. During Clopidogrel treatment also should be cautious if using other drugs at risk of gastrointestinal ulcers.

Patients with liver failure or renal failure also need to be used cautiously. So far, there are very little information related to the safety of clopidogrel for these objects.

Need to notify patients they are susceptible to bruising and bleeding, prolonged bleeding time during use of clopidogrel.

Patients also need to notify the doctor and dentist about whether they are using clopidogrel before they have surgery or other drugs.

In patients taking 2 -drug anti -platelets (clopidogrel and aspirin) after the stent release slowly, there are some evidence that the ratio of late thrombosis in the stent (often leads to myocardial infarction and/or death) after stopping clopidogrel, even in patients who have long -term treatment. The optimal treatment time of 2 anti -platelets is not known, can continue to be indefinite in people at risk of low bleeding.

Although often recommended to stop clopidogrel before surgery, should consider based on the risk of bleeding of each patient to decide.

The ability to drive and operate machinery

No report.

Pregnancy

only use clopidogrel for pregnant women when really necessary.

The period of breastfeeding

It is necessary to consider stopping breastfeeding during the time of using clopidogrel or stopping clopidogrel depending on the level of need to take medication in the breast -feeding mother.

Drug interaction

Medicines that affect or metabolized by cytochrom P450 can cause pharmacokinetic interaction, due to clopidogrel the metabolic inhibiting metabolism of the isoenzyme CYP2C19 increases the concentration of the following drugs: phenytoin, tamoxifen, tolbutamid, warfarin, torsemid, fluvastatin, anti -drug steroid.

CYP2C19 inhibitors (e.g. omeprazol, cimetidin, fluconazole, ketoconazole, ether, felbamat, fluoxetin, fluvoxamin) can reduce the concentration of active metabolites in the plasma of clopidogrel and reduce platelet resistance.

Clopidogrel may increase the effects/toxicity of the following drugs: anticoagulants, anti -platelet drugs, blood clots, Drotrecogin Alfa, Ibritumomab, Salicylat, Tositumomab, Warfarin.

The effect of clopidogrel increases when used with the following drugs: dasatinib, nonsteroidal anti-inflammatory drugs, ethyl ester of omega-3 acid, pentosan sodium polysulfate, prostacyclin, rifamycin conductivity.

Using clopidogrel in combination with cilostazol can add platelet training effects. Therefore, it is necessary to be cautious when using a combination of Cilostazol with clopidogrel, and must monitor the bleeding time if there is a combination.

Reduce effect: Proton pump inhibitors can cause pharmacokinetic interaction with clopidogrel (reduce the concentration of metabolites that are active of clopidogrel) and pharmacological interaction (reducing platelet resistance), due to CYP2C19 inhibitor inhibitors, reducing the effect of clopidogrel.The effect of clopidogrel may be reduced when used with the following drugs: Calcium channel blockers, macrolide antibiotics, nonsteroidal anti -inflammatory drugs, Proton pump inhibitors, CYP2C19 inhibitors.

Avoid coordination: Avoid coordination of clopidogrel with drugs that are known to inhibit CYP2C19 such as omeprazol, cimetidin, fluconazole, ketoconazole, voriconazole, ellavirin, felbamat, fluoxetin, fluvoxamine, ticlopidin.

Interaction with some herbs: Some herbs increase the plateloon resistance of clopidogrel such as: Linh Lang grass, anise tree, blueberry, pineapple tree, basil, herb oil, garlic, turmeric, ginger, ginseng, ginkgo, grape seed, green tea, chestnut, licorice, red clove, frequency, yard, willow clover, willow.

Storage

Leave a cool place, avoid light, temperature below 30⁰C.

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