Cilostazol apollo

Transcription

1 Cilostazol apollo Cilostazol apollo Cilostazol CAS Number : Molecular Weight : g/mol Molecular Formula : C20H27N5O2 Systematic (IUPAC) : 6-[4-(1-cyclohexyl-1H-1,2,3,4- tetrazol-5-yl)butoxy]-1,2,3,4-tetrahydroquinolin-2-one Type : small molecule Description Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with

2 peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal. Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease. Categories Vasodilator Agents Platelet Aggregation Inhibitors Fibrinolytic Agents Phosphodiesterase Inhibitors Bronchodilator Agents Neuroprotective Agents Taxonomy Kingdom : Organic Classes Quinolinones Phenylpropylamines (Iso)quinolines and Derivatives Lactams Substructures Phenols and Derivatives Amino Ketones Ethers Benzene and Derivatives Carboxylic Acids and Derivatives Tetrazoles

3 Heterocyclic compounds Aromatic compounds Quinolinones Anisoles Carboxamides and Derivatives Phenylpropylamines (Iso)quinolines and Derivatives Lactams Imines Cyanamides Phenyl Esters Anilines Pharmacology Indication : For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest). Pharmacodynamics : Cilostazol is a quinolinone derivative indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs. Mechanism of action : Cilostazol and several of its metabolites are cyclic AMP (camp) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing camp degradation with a resultant increase in camp in

4 platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation. Absorption : Cilostazol is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known. Protein binding : 95-98% Metabolism : Hepatic. Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Two metabolites are active, with one metabolite appearing to account for at least 50% of the pharmacologic (PDE III inhibition) activity after administration of cilostazol. Route of elimination : Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Cilostazol is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol. About 30% of the dose was excreted in urine as 4'-trans-hydroxycilostazol.

5 Half life : hours. Toxicity Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs. Affected organisms : Humans and other mammals Drug Class And Mechanisms Cilostazol is a medication for the treatment of intermittent claudication, a condition caused by narrowing of the arteries that supply the legs with blood. Patients with intermittent claudication develop pain when they walk because not enough oxygen-containing blood reaches the active leg muscles. Cilostazol reduces the pain of intermittent claudication by dilating the arteries, thereby improving the flow of blood and oxygen to the legs. (It does this by decreasing the action of an enzyme, phosphodiesterase III.) It also reduces the ability of blood to clot. Cilostazol enables patients with intermittent claudication to walk longer and faster before developing pain. Cilostazol has a different mechanism of action than pentoxifylline (Trental), the other drug approved for intermittent claudication. (Pentoxifylline improves blood flow by making it easier for red blood cells to pass through vessels. It also decreases the viscosity of blood.). The FDA approved cilostazol in January 1999.

6 Dosing The dose is 100 mg twice daily. Cilostazol should be taken at least half an hour before or two hours after dinner and breakfast to prevent food from affecting its absorption. Drug Interactions Erythromycin (E.E.S, Erythrocin), omeprazole(prilosec) and diltiazem (Cardizem) increase the concentration of cilostazol by blocking the action of enzymes that destroy cilostazol. Though not specifically studied, a similar interaction could occur with ketoconazole(nizoral), itraconazole (Sporanox), fluconazole (Diflucan), miconazole(monistat), fluvoxamine (Luvox), fluoxetine (Prozac), nefazodone (Serzone) and sertraline (Zoloft). Diltiazem (Cardizem) and omeprazole (Prilosec) also increase concentrations of cilostazol. Higher concentrations of cilostazol could increase the possibility of toxic effects. Therefore, a dose of 50 mg twice daily should be considered when drugs that may increase the concentration of cilostazol also are being used. Uses Cilostazol is used to improve the symptoms of a certain blood flow problem in the legs (intermittent claudication). Cilostazol can decrease themuscle pain/cramps that occur during exercise/walking. Claudication pain is caused by too little oxygen getting to the muscles. Cilostazol can increase blood flow and the amount of oxygen that gets to the muscles.cilostazol is an "anti-platelet" and a vasodilator. It works by preventing certain blood cells (platelets) from sticking together and by widening blood vessels in the legs. This

7 helps the blood to move more easily and increases blood flow. How To Use? Read the Patient Information Leaflet if available from your pharmacist before you start taking cilostazol and each time you get a refill. If you have any questions, ask your doctor or pharmacist.take this medication by mouth as directed by your doctor, usually twice daily without food, at least 30 minutes before or 2 hours after breakfast and dinner. Dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.use this medication regularly in order to get the most benefit from it. Remember to use it at the same times each day.your symptoms may improve in 2-4 weeks, but it may take up to 12 weeks to notice a benefit from this drug.tell your doctor if your condition persists or worsens. Why is this medication prescribed? Cilostazol is used to reduce the symptoms of intermittent claudication (pain in the legs that worsens when walking and improves when resting that is caused by narrowing of the blood vessels that supply blood to the legs). Cilostazol is in a class of medications called

8 platelet-aggregation inhibitors (antiplatelet medications). It works by improving blood flow to the legs. How should this medicine be used? Cilostazol comes as a tablet to take by mouth. It is usually taken twice a day, at least 30 minutes before or 2 hours after breakfast and dinner. Take cilostazol at around the same times every day. Follow the directions on the prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take cilostazol exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. Cilostazol controls the symptoms of intermittent claudication but does not cure it. Although you may notice improvements in 2 to 4 weeks, it may take up to 12 weeks before you notice the full benefit (increased walking distance) of cilostazol. Continue taking cilostazol even if you feel well. Do not stop taking cilostazol without talking to your doctor. Other uses for this medicine This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information. What special precautions should I follow? Before taking cilostazol, tell your doctor and pharmacist if you are allergic to cilostazol, any other medications, or any of the ingredients in cilostazol. Ask your pharmacist for a list of the ingredients.

9 tell your doctor and pharmacist what other 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); aspirin; antifungal medications such as fluconazole (Diflucan), itraconazole (Sporanox), and ketoconazole (Nizoral); antiplatelet medications such as clopidogrel (Plavix), prasugrel (Effient), and ticlopidine (Ticlid); clarithromycin (Biaxin); diltiazem (Cardizem, Dilacor, Tiazac, others); erythromycin (E-mycin, Ery- Tab, others); fluoxetine (Prozac); fluvoxamine (Luvox); nefazadone; omeprazole (Prilosec); and sertraline (Zoloft). 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, bleeding from any other part of your body, a low number of platelets in your blood, or any other condition that causes severe bleeding. Your doctor will probably tell you not to take cilostazol. tell your doctor if you have or have ever had heart, kidney, or liver disease. tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking cilostazol, call your doctor. 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

10 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? Cilostazol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: headache diarrhea dizziness heartburn nausea stomach pain muscle pain Some side effects can be serious. If you experience any of the following symptoms, call your doctor immediately: fast or irregular heartbeat unusual bleeding or bruising swelling of the arms, hands, feet, ankles, or lower legs 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. Symptoms of overdose may include the following: severe headache dizziness fainting

11 diarrhea fast or irregular heartbeat What other information should I know? Keep all appointments with your doctor. 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: Wireline Sales HELPDESK:

12 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, Goregoan West, Mumbai, INDIA

13 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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