Clopidogrel apollo

Transcription

1 Clopidogrel apollo Clopidogrel apollo Clopidogrel CAS Number : Molecular Weight : g/mol Molecular Formula : C16H16ClNO2S Systematic (IUPAC) : methyl (2S)-2-(2-chlorophenyl) -2-{4H,5H,6H,7H-thieno[3,2-c]pyridin-5-yl}acetate Type : small molecule

2 Description Clopidogrel, an antiplatelet agent structurally and pharmacologically similar to ticlopidine, is used to reduce atherosclerotic events such as myocardial infarction, stroke, and vascular death in patients who have had a recent stroke, recent MI, or have established peripheral vascular disease. Categories Antiplatelet Agents Platelet Aggregation Inhibitors Fibrinolytic Agents Taxonomy Kingdom : Organic Classes Thienopyridines Phenylacetates Amino Acids Substructures Thienopyridines Carboxylic Acids and Derivatives Acetates Phenylacetates Ethers Benzene and Derivatives Aryl Halides Halobenzenes Aliphatic and Aryl Amines

3 Heterocyclic compounds Aromatic compounds Amino Acids Thiophenes Pharmacology Indication : For the reduction of atherosclerotic events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease Pharmacodynamics : Clopidogrel, an antiplatelet agent structurally and pharmacologically similar to ticlopidine, is used to reduce atherosclerotic events such as myocardial infarction, stroke, and vascular death in patients who have had a recent stroke, recent MI, or have established peripheral vascular disease. Mechanism of action : The active metabolite of clopidogrel prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADPmediated activation of the glycoprotein GPIIb/IIIa complex. It is proposed that the inhibition involves a defect in the mobilization from the storage sites of the platelet granules to the outer membrane. he drug specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor, which is important in aggregation of platelets and cross-linking by the protein fibrin. No direct interference occurs with the GPIIb/IIIa receptor. As the glycoprotein GPIIb/IIIa complex is the major

4 receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation. By blocking the amplification of platelet activation by released ADP, platelet aggregation induced by agonists other than ADP is also inhibited by the active metabolite of clopidogrel. Absorption : Absorption is at least 50% based on urinary excretion of clopidogrel-related metabolites. Bioavailability has not been found to be affected by food. Protein binding : 98% Metabolism : Hepatic, extensive and rapid, by hydrolysis to the main circulating metabolite, a carboxylic acid derivative, which accounts for approximately 85% of the circulating drug-related compounds. A glucuronic acid derivative of the carboxylic acid derivative has also been found in plasma and urine. Neither the parent compound nor the carboxylic acid derivative has a platelet inhibiting effect. Route of elimination : Following an oral dose of 14Clabeled clopidogrel in humans, approximately 50% of total radioactivity was excreted in urine and approximately 46% in feces over the 5 days post-dosing. Half life : Carboxylic acid derivative: 8 hours (after single and multiple doses). Covalent binding to platelets has accounted for 2% of radiolabeled clopidogrel with a half-life of 11 days.

5 Toxicity : Symptoms of acute toxicity include vomiting (in baboons), prostration, difficult breathing, and gastrointestinal hemorrhage. Affected organisms : Humans and other mammals Drug Class And mechanisms Clopidogrel bisulfate is an anti-platelet drug, that is, a drug that inhibits the ability of platelets to clump together as part of a blood clot. Clopidogrel prevents blood clots by irreversibly binding to the P2Y12 receptor on platelets, preventing adenosine diphosphate (ADP) from activating platelets. It belongs to a class of drugs called P2Y12 inhibitors. Other drugs in this class include ticagrelor (Brilinta) and prasugrel (Effient). Clopidogrel is similar to ticlopidine (Ticlid) in chemical structure and in the way it works. Unlike ticlopidine, clopidogrel bisulfate does not cause serious reductions of white cells in the blood and, therefore, routine blood testing to determine if the white blood cell count is low is not necessary during treatment. The risk of heart attacks and strokes (which usually are caused by blood clots) is increased in patients with a recent history of stroke or heart attack, and patients with peripheral vascular disease. (Peripheral vascular disease is the same as atherosclerotic arterial disease or "hardening" of the arteries in which the arteries become narrowed. It frequently occurs in the legs and often causes claudication or pain in the legs upon walking.) Clopidogrel bisulfate is used to reduce the risk of heart attacks and strokes in these patients. Clopidogrel bisulfate was approved by the FDA in 1997.

6 Dosing Clopidogrel bisulfate usually is taken once daily. It can be taken with or without food. Clopidogrel is activated by enzymes in the liver to its active form. Individuals who have reduced activity of liver enzymes that activate clopidogrel due to liver disease may not adequately respond to clopidogrel. Alternative treatments should be used for these patients. The recommended dose for treating unstable angina or heart attack is 300 mg initially followed by 75 mg daily in combination with mg of aspirin. Peripheral arterial disease or recent stroke is treated with 75 mg daily. Drug interactions The combination of clopidogrel with nonsteroidal antiinflammatory drugs (NSAIDs) such as ibuprofen (Motrin, Advil, Nuprin), naproxen (Naprosyn, Aleve), diclofenac (Voltaren), etodolac (Lodine), nabumetone (Relafen), fenoprofen (Nalfon), flurbiprofen (Ansaid), indomethacin (Indocin), ketoprofen (Orudis; Oruvail), oxaprozin (Daypro), piroxicam (Feldene), sulindac (Clinoril), tolmetin (Tolectin), and mefenamic acid (Ponstel) may increase the risk of stomach and intestinal bleeding. Uses Clopidogrel is used to prevent heart attacks and strokes in persons with heart disease (recent heart attack), recent stroke, or blood circulation disease (peripheral vascular disease).it is also used with aspirin to treat new/worsening chest pain (new heart attack, unstable angina) and to keep blood vessels open and prevent blood clots after certain procedures (such as cardiac

7 stent, coronary artery bypass graft-cabg, balloon angioplasty).it works by blocking certain blood cells called platelets and prevents them from forming harmful blood clots. This "anti-platelet" effect helps keep blood flowing smoothly in your body. How To Use? Read the Medication Guide provided by your pharmacist before you start taking clopidogrel and each time you get a refill. If you have any questions, ask your doctor or pharmacist.take this medication by mouth with or without food as directed by your doctor, usually once daily. Use this medication regularly in order to get the most benefit from it. Remember to use it at the same time each day.dosage and duration of treatment are based on your medical condition and response to treatment. If you are taking this medication to prevent clots after a stent implant or other procedure, take this medication with aspirin for many months to years after the procedure (depending on the procedure/type of stent) as directed by your doctor. Consult your doctor for more details and the risks of stopping early. It is important to continue taking this medication even if you feel well. Do not stop taking this medication without consulting your doctor.get medical help right away if you have any signs that this medication is not working, such as symptoms of a new heart attack or stroke (such as chest/jaw/left arm pain, shortness of breath, unusual sweating, weakness on one side of the body, slurred speech, sudden vision changes, confusion). Why is this medication prescribed?

8 Clopidogrel is used to prevent strokes and heart attacks in patients at risk for these problems. Clopidogrel is in a class of medications called antiplatelet drugs. It works by helping to prevent harmful blood clots that may cause heart attacks or strokes. How should this medicine be used? Clopidogrel comes as a tablet to take by mouth. It is usually taken once a day with or without food. Try to take clopidogrel at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take clopidogrel exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. Clopidogrel will help prevent heart attacks and strokes only as long as you take the medication. Continue to take clopidogrel even if you feel well. Do not stop taking clopidogrel without talking to your doctor. Other uses for this medicine Clopidogrel is also sometimes used to prevent blood clots in people with mitral valve disease (a condition that affects the valve that separates the left upper and lower chambers of the heart) prosthetic (artificial) heart valves, and people undergoing certain heart procedures such as coronary artery stent placement. Talk to your doctor about the possible risks of using this medication for your condition. This medication may be prescribed for other uses; ask your doctor or pharmacist for more information. What special precautions should I follow?

9 Before taking clopidogrel, tell your doctor and pharmacist if you are allergic to clopidogrel or any other medications. tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: anticoagulants ('blood thinners') such as warfarin (Coumadin); certain antifungals such as fluconazole (Diflucan), ketoconazole (Nizoral), and voriconazole (Vfend); aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) such as felbamate (Felbatol), ibuprofen (Advil, Motrin), and naproxen (Aleve, Naprosyn); fluvastatin (Lescol); cimetidine (Tagamet); etravirine (Intelence); fluoxetine (Prozac); fluvoxamine (Luvox); phenytoin (Dilantin); proton pump inhibitors (PPIs) such as esomeprazole (Nexium) and omeprazole (Prilosec, Prilosec OTC, Zegerid); tamoxifen (Nolvadex); ticlopidine (Ticlid); tolbutamide; and torsemide (Demadex). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. tell your doctor if you have bleeding ulcers (sores in the lining of the stomach or small intestine that are bleeding), bleeding in the brain, or any other condition that causes severe bleeding. Your doctor may tell you that you should not take clopidogrel. tell your doctor if you have recently been injured and if you have or have ever had liver or kidney disease or any condition that may cause bleeding, including stomach problems such as ulcers and certain eye problems. tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking clopidogrel, call your doctor.

10 if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking clopidogrel. you should know that you may bleed more easily or for a longer time than usual while you are taking clopidogrel. Be careful not to cut or hurt yourself while you are taking clopidogrel. What special dietary instructions should I follow? Unless your doctor tells you otherwise, continue your normal diet. What should I do if I forget a dose? Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one. What side effects can this medication cause? Clopidogrel may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: excessive tiredness headache dizziness nausea stomach pain diarrhea nosebleed Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately: hives rash itching

11 difficulty breathing or swallowing swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs hoarseness black and tarry stools red blood in stools bloody vomit vomit that looks like coffee grounds unusual bleeding or bruising slow or difficult speech weakness or numbness of an arm or a leg vision loss fever shortness of breath fast heartbeat pale skin purple patches or bleeding under the skin confusion yellowing of the skin or eyes Clopidogrel may cause other side effects. Call your doctor if you have any unusual problems while taking this medication. What storage conditions are needed for this medicine? Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

12 Symptoms of overdose may include the following: unusual bruising or bleeding What other information should I know? Keep all appointments with your doctor and the laboratory. Your doctor may order certain lab tests to check your body's response to clopidogrel. Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription. It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies. apollo asia Division APOLLO Pharmaceuticals API Manufacturers INDIA [P] Ltd. asia Division Mr.Vipin Saxena CEO Cellular: Cellular: Direct : FAX : Wireline Purchase HELPDESK:

13 Wireline Sales HELPDESK: Wireless 24x7 HELPDESK: Blackberry Pin : 32E6500D 32E C58 apollo@hotmail.co.in Sales@apollopharma.in Export@apollopharma.in purchase@apollopharma.in Chat: MSN Hotmail:VipinrSaxena Skype NAME:VipinrSaxena Rocketmail:VipinrSaxena Google mail:vipinrsaxena BlackBerry:28415C58 Regd. Office :- 1104, Maker Chamber V, Nariman Point Mumbai, INDIA Pin: Industrial Office D-62, OIC India Oshiwara Industrial Centre, New Link Road,

14 Goregoan West, Mumbai, INDIA Pin: Manufacturing Unit Address: Plot No. 117A, Village: Chamble Near MonaTona Limited.Wada, Maharashtra, PIN : INDIA apollo@hotmail.co.in Sales@apollopharma.in Export@apollopharma.in purchase@apollopharma.in

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