Eplerenone apollo

Transcription

1 Eplerenone apollo Eplerenone apollo Eplerenone CAS Number : Molecular Formula : C24H30O6 Molecular Weight : g/mol Systematic (IUPAC) : methyl (1'R,2R,2'S,9'R,10'R,11'S,15'S,17'R)-2',15'- dimethyl5,5'dioxo18'oxaspiro[oxolane2,14'pentacyclo[ ^{1,17}.0^{2,7}.0^{11,15}]octadecan]-6'-ene-9'- carboxylate

2 Type : small molecule Description Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors. Categories Antihypertensive Agents Aldosterone Antagonists Pharmacology Indication : For improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction. Pharmacodynamics : Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin

3 secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors. Mechanism of action : Eplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the reninangiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-raas mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms. Absorption : The absolute bioavailability of eplerenone is unknown. Volume of distribution : 43 to 90 L Protein binding : 50% Metabolism : Eplerenone is metabolized primarily by CYP3A4, however, no active metabolites have been identified in human plasma.

4 Half life : 4-6 hours Clearance : Apparent plasma cl=10 L/hr Toxicity : The most likely symptoms of human overdosage would be anticipated to be hypotension or hyperkalemia. However, no cases of human overdosage with eplerenone have been reported. Affected organisms: Humans and other mammals Uses This medication is used alone or in combination with other medicines to treat high blood pressure. It works by blocking a chemical (aldosterone) in your body which in turn lowers the amount of sodium and water the body retains. Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems. It is also used to treat congestive heart failure following a heart attack. How To Use? Take this medication by mouth, usually once or twice daily, with or without food, or as directed by your doctor. Use this medication regularly in order to get the most benefit from it. Remember to use it at the same time(s) each day.do not take potassium supplements or salt substitutes containing potassium without talking to your doctor or pharmacist first. This medicine can raise your potassium levels, which rarely can cause serious side effects such as muscle weakness or very slow/irregular heartbeats. Tell your doctor immediately

5 if these effects occur.dosage is based on your medical condition (high blood pressure, congestive heart failure), laboratory test results, and response to therapy. It may take up to 4 weeks for this medication to fully affect your blood pressure.it is important to continue taking this medication even if you feel well. Most people with high blood pressure do not feel sick. Drug interactions The effects of some drugs can change if you take other drugs or herbal products at the same time. This can increase your risk for serious side effects or may cause your medications not to work correctly. These drug interactions are possible, but do not always occur. Your doctor or pharmacist can often prevent or manage interactions by changing how you use your medications or by close monitoring.to help your doctor or pharmacist give you the best care, be sure to tell your doctor or pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products) before starting treatment with this product. While using this product, do not start, stop, or change the dosage of any other medicines you are using without your doctor's approval.some of the products that may interact with this drug include: ACE inhibitors (such as captopril, enalapril), angiotensin II blockers (such as losartan, valsartan), lithium, nonsteroidal antiinflammatory drugs (such as NSAIDs like ibuprofen, indomethacin, naproxen), potassium supplements, certain "water pills" (potassium-sparing types such as amiloride, spironolactone, triamterene).other medications can affect the removal of eplerenone from your body, thereby affecting how eplerenone works.

6 These drugs include azole antifungals (such as fluconazole, ketoconazole, itraconazole), macrolide antibiotics (such as clarithromycin, erythromycin), nefazodone, protease inhibitors (such as nelfinavir, ritonavir, saquinavir), St. John's wort, verapamil. This is not a complete list.this document does not contain all possible interactions. Keep a list of all the products you use. Share this list with your doctor and pharmacist to lessen your risk for serious medication problems. Why is this medication prescribed? Eplerenone is used alone or in combination with other medications to treat high blood pressure. Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. It works by blocking the action of aldosterone, a natural substance in the body that raises blood pressure. How should this medicine be used? Eplerenone comes as a tablet to take by mouth. It is usually taken once or twice a day, with or without food. To help you remember to take eplerenone, take it around the same time(s) 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 eplerenone exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. Your doctor may start you on a low dose of eplerenone and increase your dose after 4 weeks. Eplerenone controls high blood pressure but does not cure it. It may take 4 weeks or longer before you feel the full benefit of eplerenone. Continue to take eplerenone

7 even if you feel well. Do not stop taking eplerenone without talking to your doctor. Other uses for this medicine This medication may be prescribed for other uses; ask your doctor or pharmacist for more information. What special precautions should I follow? Before taking eplerenone, tell your doctor and pharmacist if you are allergic to eplerenone or any other medications. do not take eplerenone if you are taking amiloride (Midamor), amiloride and hydrochlorothiazide (Moduretic), itraconazole (Sporanox), ketoconazole (Nizoral), potassium supplements, spironolactone (Aldactone), spironolactone and hydrochlorothiazide (Aldactazide), triamterene (Dyrenium), or triamterene and hydrochlorothiazide (Dyazide, Maxzide). tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking. Be sure to mention any of the following: angiotensin converting enzyme (ACE) inhibitors such as benazepril (Lotensin), captopril (Capoten), enalapril (Vasotec), fosinopril (Monopril), lisinopril (Prinivil, Zestril), and quinapril (Accupril); angiotensin II receptor antagonists such as eprosartan (Teveten), irbesartan (Avapro), losartan (Cozaar), olmesartan (Benicar), and valsartan (Diovan); aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn); cimetidine (Tagamet); clarithromycin (Biaxin); danazol (Danocrine); delavirdine (Rescriptor); diltiazem (Cardizem, Dilacor,

8 Tiazac); erythromycin (E.E.S., E-Mycin, Erythrocin); fluconazole (Diflucan); fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); HIV protease inhibitors such as indinavir (Crixivan), ritonavir (Norvir), and saquinavir (Fortovase, Invirase); isoniazid (INH, Nydrazid); lithium (Eskalith, Lithobid); metronidazole (Flagyl); nefazodone (Serzone); troleandomycin (TAO); verapamil (Calan, Covera, Isoptin, Verelan); and zafirlukast (Accolate). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. tell your doctor what herbal products you are taking, especially St. John's wort. tell your doctor if you have or have ever had high blood levels of potassium, diabetes, gout, or liver or kidney disease. tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking eplerenone, call your doctor. What special dietary instructions should I follow? Talk to your doctor about drinking grapefruit juice while taking this medicine. Do not use salt substitutes containing potassium while you are taking eplerenone. If your doctor prescribes a low-salt or low-sodium diet, follow these directions carefully. 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.

9 What side effects can this medication cause? Eplerenone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: headache dizziness diarrhea stomach pain cough excessive tiredness flu-like symptoms breast enlargement or tenderness abnormal vaginal bleeding Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them, call your doctor immediately: chest pain tingling in arms and legs loss of muscle tone weakness or heaviness in legs confusion lack of energy cold, gray skin irregular heartbeat Eplerenone 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

10 is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication. Symptoms of overdose may include: fainting dizziness blurred vision upset stomach tingling in arms and legs loss of muscle tone weakness or heaviness in legs confusion lack of energy cold, gray skin irregular or slow heartbeat What other information should I know? Keep all appointments with your doctor and the laboratory. Your doctor will check your blood pressure regularly and order certain lab tests to check your body's response to eplerenone. 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.

11 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: 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

12 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 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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