Labetalol apollo

Transcription

1 Labetalol apollo Labetalol apollo Labetalol CAS Number : Molecular Weight : g/mol Molecular Formula : C19H24N2O3 Systematic (IUPAC) : 2-hydroxy-5-{1-hydroxy-2-[(4- phenylbutan-2-yl)amino]ethyl}benzamide Type : small molecule Description : Blocker of both alpha- and betaadrenergic receptors that is used as an antihypertensive.

2 Categories Antihypertensive Agents Adrenergic beta-antagonists Sympatholytics Adrenergic alpha-antagonists Taxonomy Kingdom : Organic Classes Phenethylamines Phenylpropylamines Benzamides Substructures Hydroxy Compounds Benzyl Alcohols and Derivatives Aliphatic and Aryl Amines Phenols and Derivatives Amino Ketones Benzene and Derivatives Carbamates and Derivatives Amino Alcohols Phenethylamines Aromatic compounds Carboxamides and Derivatives Phenylpropylamines Benzoyl Derivatives Carboxylic Acids and Derivatives Alcohols and Polyols Phenyl Esters

3 Benzamides Pharmacology Indication : For the management of hypertension (alone or in combination with other classes of antihypertensive agents), as well as chronic stable angina pectoris and sympathetic overactivity syndrome associated with severe tetanus. Labetalol is used parenterally for immediate reduction in blood pressure in severe hypertension or in hypertensive crises when considered an emergency, for the control of blood pressure in patients with pheochromocytoma and pregnant women with preeclampsia, and to produce controlled hypotension during anesthesia to reduce bleeding resulting from surgical procedures. Pharmacodynamics : Labetalol is an selective alpha-1 and non-selective beta adrenergic blocker used to treat high blood pressure. It works by blocking these adrenergic receptors, which slows sinus heart rate, decreases peripheral vascular resistance, and decreases cardiac output. Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two diastereoisomeric pairs. Dilevalol, the R,R' stereoisomer, makes up 25% of racemic labetalol. Mechanism of action : Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be

4 approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. The principal physiologic action of labetalol is to competitively block adrenergic stimulation of β-receptors within the myocardium (β1-receptors) and within bronchial and vascular smooth muscle (β2-receptors), and α1- receptors within vascular smooth muscle. This causes a decrease in systemic arterial blood pressure and systemic vascular resistance without a substantial reduction in resting heart rate, cardiac output, or stroke volume, apparently because of its combined α- and β- adrenergic blocking activity. Absorption : Completely absorbed (100%) from the gastrointestinal tract with peak plasma levels occurring 1 to 2 hours after oral administration. The absolute bioavailability of labetalol is increased when administered with food. Protein binding : 50% Metabolism : Primarily hepatic, undergoes significant first pass metabolism Route of elimination : These metabolites are present in plasma and are excreted in the urine, and via the bile, into the feces. Half life : 6-8 hours Toxicity : LD50 = 66 mg/kg (Rat, IV). Side effects or adverse reactions include dizziness when standing up,

5 very low blood pressure, severely slow heartbeat, weakness, diminished sexual function, fatigue Affected organisms : Humans and other mammals Drug Cass And Mechanisms Labetalol is a drug that is used for treating high blood pressure. And is related to carvedilol (Coreg). Nerves from the adrenergic nervous system travel from the spinal cord to arteries where they release norepinephrine. Norepinephrine attaches to adrenergic receptors on arteries and causes the arteries to contract, narrowing the arteries, and increasing blood pressure. Labetalol blocks receptors of the adrenergic nervous system. When labetalol attaches to and blocks the receptors, arteries expand, resulting in a fall in blood pressure. The FDA approved labetalol in August Dosing The recommended starting oral dose of labetalol is 100 mg twice daily and the dose can be increased by 100 mg twice daily every 2-3 days based on the response of the blood pressure. Usual maintenance doses are mg twice daily. Patients with severely high blood pressure may require 1.2 to 2.4 g daily. Side effects may be less if labetalol is given in three daily doses rather than two. Stopping or changing the dose of the drug should be directed by a physician because serious side effects may occur. The initial intravenous dose of labetalol is 20 mg injected over 2 minutes. Additional injections of 40 or 80 mg may be administered every 10 minutes as needed up to a total

6 dose of 300 mg. Labetalol also may be administered by intravenous infusion at 1-2 mg/minute. Drug Interactions Labetalol can mask early warning symptoms ofhypoglycemia (low blood sugar) such as tremors and increased heart rate which are the result of activation of the adrenergic nervous system. Therefore, people with diabetes taking medications that lower blood sugar such as insulin or oral antidiabetic medications may need to increase the frequency with which they monitor their blood sugar in order to prevent hypoglycemia. Combining labetalol with tricyclic antidepressants such as amitriptyline(elavil, Endep), imipramine (Tofranil), or nortriptyline (Pamelor) may lead to an increase in tremor which is a side effect of tricyclic antidepressants. If combined with adrenergic stimulating drugs used for treating asthma, for example, albuterol (Proventil, Ventolin) or pirbuterol (Maxair), the adrenergic blocking effects of labetalol may counteract the effects of the stimulating drugs and reduce their effectiveness for treating asthmatic attacks. More of the adrenergic drug may be needed. Glutethimide (Doriden) may decrease the effectiveness of labetalol by increasing its elimination. When both drugs are used together, more labetalol or less glutethimide may be needed. Why is this medication prescribed? Labetalol is used to treat high blood pressure. Labetalol is in a class of medications called beta blockers. It works by relaxing blood vessels and slowing heart rate to improve blood flow and decrease blood pressure.

7 How should this medicine be used? Labetalol comes as a tablet to take by mouth. It usually is taken two or three times a day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take labetalol exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. Labetalol controls high blood pressure but does not cure it. Continue to take labetalol even if you feel well. Do not stop taking labetalol without talking to your doctor. Other uses for this medicine Labetalol is also used sometimes to treat angina (chest pain) and to treat patients with tetanus. Talk to your doctor about the possible risks of using this drug for your condition. This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information. What special precautions should I follow? Before taking labetalol, tell your doctor and pharmacist if you are allergic to labetalol or any other drugs. tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially other medications for high blood pressure or heart disease; cimetidine (Tagamet); nitroglycerin; medications for asthma, headaches, allergies, colds, or pain; and vitamins. tell your doctor if you have or have ever had heart, kidney, or liver disease; asthma or other lung disease; severe allergies; diabetes; or pheochromocytoma.

8 tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking labetalol, call your doctor. if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking labetalol. you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you. remember that alcohol can add to the drowsiness caused by this drug. 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? Labetalol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: dizziness tingling scalp or skin lightheadedness excessive tiredness headache upset stomach stuffy nose

9 If you experience any of the following symptoms, call your doctor immediately: shortness of breath or wheezing swelling of the feet and lower legs sudden weight gain chest pain 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. What other information should I know? Keep all appointments with your doctor and the laboratory. Your blood pressure should be checked regularly to determine your response to labetalol. Your doctor may ask you to check your pulse (heart rate). Ask your pharmacist or doctor to teach you how to take your pulse. If your pulse is faster or slower than it should be, call 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

10 important information to carry with you in case of emergencies. apollo asia Division APOLLO Pharmaceuticals API Manufacturer 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

11 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 Pin:400104

12 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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