Carvedilol | apllo +9191 46 950 950

Carvedilol | apllo +9191 46 950 950

Carvedilol

CAS Number : 72956-09-3

Molecular Weight : 406.47 g/mol

Molecular Formula : C24H26N2O4

Systematic (IUPAC) : [3-(9H-carbazol-4-yloxy)-2-hydroxypropyl][2-(2-methoxyphenoxy)ethyl]amine

Type : small molecule

Description

Carvedilol is a non-selective beta blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). It blocks beta-1 and beta-2 adrenergic receptors as well as the alpha-1 adrenergic receptors.

Categories

Antihypertensive Agents

Adrenergic Agents

Adrenergic beta-Antagonists

Vasodilator Agents

Taxonomy

Kingdom : Organic

Classes

Carbazoles

Substructures

Hydroxy Compounds

Indoles and Indole Derivatives

Aliphatic and Aryl Amines

Phenols and Derivatives

Carbazoles

Pyrroles

Ethers

Benzene and Derivatives

Amino Alcohols

Catechols

Heterocyclic compounds

Aromatic compounds

Anisoles

Alcohols and Polyols

Phenyl Esters

Pharmacology

Indication : For the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or

cardiomyopathic origin.

Pharmacodynamics : Carvedilol is a nonselective beta-adrenergic blocking agent with alpha1-blocking

activity and is indicated for the treatment of

hypertension and mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. Carvedilol is a racemic mixture in which nonselective b-adrenoreceptor blocking activity is present in the S(-)

enantiomer and a-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol has no intrinsic sympathomimetic activity. The effect of carvedilol's b-adrenoreceptor blocking activity has been demonstrated in animal and human studies showing that carvedilol reduces cardiac output

in normal subjects; reduces exercise-and/or isoproterenol-induced tachycardia and reduces reflex

orthostatic tachycardia.

Mechanism of action : Carvedilol is a racemic mixture in which nonselective beta-adrenoreceptor

blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both

R(+) and S(-) enantiomers at equal potency. Carvedilol's beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca2+ in OH- free radical-treated

myocardium. Carvedilol and its metabolites also prevent OH- radical-induced decrease in sarcoplasmic reticulum

Ca2+-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by

preventing free radical damage.

Absorption : Carvedilol is rapidly and extensively absorbed following oral administration, with an absolute

bioavailability of approximately 25% to 35% due to a significant degree of first-pass metabolism.

Volume of distribution : 115 L

Protein binding : 98%

Metabolism : Hepatic. Carvedilol is metabolized primarily by aromatic ring oxidation and

glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. Demethylation and hydroxylation at the phenol ring produce three active metabolites with b-receptor blocking activity. The 4'-hydroxyphenyl

metabolite is approximately 13 times more potent than carvedilol for b-blockade.

Route of elimination : Carvedilol is extensively metabolized. Less than 2% of the dose was excreted unchanged in the urine. Carvedilol is metabolized

primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. The metabolites of carvedilol are excreted

primarily via the bile into the feces.

Half life : 7-10 hours

Clearance : 500-700 mL/min

Toxicity : Not expected to be toxic following ingestion.

Affected organisms : Humans and other mammals

Drug Class And Mechanisms

Carvedilol is used for treating high blood pressure and congestive heart failure. It is related to labetalol

(Normodyne, Trandate). Carvedilol blocks receptors of the adrenergic nervous system, the system of nerves in which epinephrine (adrenalin) is active. Nerves from the

adrenergic system enter the heart and release an adrenergic chemical (norepinephrine) that attaches to receptors on the heart's muscle and stimulates the

muscle to beat more rapidly and forcefully. By blocking the receptors, carvedilol reduces the heart's rate and

force of contraction and thereby reduces the work of the heart. Carvedilol also blocks adrenergic receptors on arteries and causes the arteries to relax and the blood pressure to fall. The drop in blood pressure further

reduces the work of the heart since it is easier to pump blood against a lower pressure. The FDA first approved

carvedilol in 1995.

Dosing

Carvedilol usually is given twice daily. For high blood pressure, the dose may range from 6.25mg twice daily to a maximum of 25mg twice daily. For congestive heart failure, the dose may range from 3.25mg twice daily to a maximum of 25mg twice daily in persons weighing less than 85kg (187 pounds) or 50mg twice daily in persons weighing more than 85kg (187 pounds). Carvedilol should be taken with food since this increases the amount of absorbed drug that reaches the heart and arteries. Stopping and changing doses of carvedilol

should be done under the direction of a physician since sudden changes in dose can result in serious cardiac

complications such as arrhythmias.

Drug Interactions

Carvedilol can mask early warning symptoms of hypoglycemia (low blood sugar) such as tremors and increased heart rate. (These symptoms are caused by activation of the adrenergic nervous system which is blocked by the carvedilol.) Therefore, patients with

diabetes taking medications that lower blood sugar such

as insulin or oral anti-diabetic medications may need to increase the frequency with which they monitor their

blood sugar. Carvedilol taken with calcium channel blockers such as diltiazem (Cardizem) or verapamil (Calan) may trigger

an irregular heart rhythm or an increase in blood pressure.

Reserpine, monoamine oxidase inhibitors (phenelzine or isocarboxazid) and clonidine (Catapres), because they have similar mechanisms of action as carvedilol, may greatly accentuate the effects of carvedilol and cause a steep decline in blood pressure and/or heart rate. Close monitoring of blood pressure and heart rate may be

needed.

Why is this medication prescribed?

Carvedilol is used to treat heart failure (condition in which the heart cannot pump enough blood to all parts of the body) and high blood pressure. It also is used to treat people whose hearts cannot pump blood well as a result of a heart attack. Carvedilol is often used in

combination with other medications. Carvedilol 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

How should this medicine be used?

Carvedilol comes as a tablet and an extended-release (long-acting) capsule to take by mouth. The tablet is usually taken twice a day with food. The extended-release capsule is usually taken once a day in the

morning with food. Try to take carvedilol at 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 carvedilol exactly as directed. Do not take more or less of it or take it more often than prescribed by your

doctor.

Swallow the extended-release capsules whole. Do not chew or crush the capsules, and do not divide the beads inside a capsule into more than one dose. If you are

unable to swallow the capsules, you may carefully open a capsule and sprinkle all of the beads it contains over a spoonful of cool or room temperature applesauce. Swallow the entire mixture immediately without

chewing.

Your doctor will probably start you on a low dose of carvedilol and gradually increase your dose to allow your body to adjust to the medication. Talk to your doctor about how you feel and about any symptoms you

experience during this time.

Carvedilol may help to control your condition but will not cure it. Continue taking carvedilol even if you feel well. Do not stop taking carvedilol without talking to your doctor. If you suddenly stop taking carvedilol, you may experience serious heart problems such as severe

chest pain, a heart attack, or an irregular heartbeat. Your doctor will probably want to decrease your dose

gradually over 1 to 2 weeks. Your doctor will watch you carefully and will probably tell you to avoid physical

activity during this time.

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 carvedilol,

tell your doctor and pharmacist if you have are allergic to carvedilol or any other medications.

tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, herbal products, and nutritional supplements you are taking or plan to

take. Be sure to mention any of the following: cimetidine (Tagamet); clonidine (Catapres), cyclosporine (Neoral, Sandimmune); digoxin (Lanoxicaps, Lanoxin); diltiazem (Cardizem, Tiazac); epinephrine (Epipen); fluoxetine

(Prozac); insulin; oral medications for diabetes; monoamine oxidase inhibitors (MAOIs) such as isocarboxazid (Marplan), phenelzine (Nardil),

tranylcypromine (Parnate), and selegiline (Eldepryl, Emsam, Zelapar); paroxetine (Paxil); propafenone

(Rythmol); quinidine; reserpine (Serpalan,); rifampin (Rifadin, Rimactane); and verapamil (Calan, Covera-HS, Verelan). Your doctor may need to change the doses of your medications or monitor you carefully for side

effects.

tell your doctor if you have or have ever had asthma or other breathing problems, a slow or irregular heartbeat, or liver disease. Your doctor may tell you not to take

carvedilol.

tell your doctor if you have or have ever had problems with blood flow in your feet or legs, diabetes or any other

condition that causes you to have low blood sugar, hyperthyroidism (condition in which there is too much thyroid hormone in the body), low blood pressure,

Prinzmetal's angina (chest pain that comes at rest with no obvious cause), or pheochromocytoma (a tumor that develops on a gland near the kidneys and may cause high blood pressure and fast heartbeat). Also tell your doctor if you have ever had a serious allergic reaction to

a food or any other substance.

tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant

while taking carvedilol, call your doctor.

if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking carvedilol.

you should know that this medication may make you feel tired, dizzy, or lightheaded, especially when you start taking carvedilol and when your dose is increased. Do

not drive a car or operate machinery until you know how this medication affects you. Be especially careful during

the first hour after you take the medication.

do not drink any alcoholic drinks or take any prescription or nonprescription medications that

contain alcohol for 2 hours before and 2 hours after you take carvedilol extended-release capsules. Ask your

doctor or pharmacist if you do not know if a medication that you plan to take contains alcohol.

you should know that carvedilol may cause dizziness, lightheadedness, and fainting, especially when you get up too quickly from a lying position. This is more

common when you first start taking carvedilol. To avoid this problem, get out of bed slowly, resting your feet on

the floor for a few minutes before standing up.

if you wear contact lenses, your eyes may become dry during your treatment with carvedilol. Tell your doctor if

this becomes bothersome.

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?

Carvedilol may cause hyperglycemia (high blood sugar). Call your doctor immediately if you have any of the

following symptoms of hyperglycemia:

extreme thirst

frequent urination

extreme hunger

weakness

blurred vision

Carvedilol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

tiredness

weakness

lightheadedness

dizziness

headache

diarrhea

nausea

vomiting

vision changes

joint pain

difficulty falling asleep or staying asleep

cough

dry eyes

numbness, burning, or tingling in the arms or legs

Some side effects may be serious. If you experience any of the following symptoms, call your doctor

immediately:

fainting

shortness of breath

weight gain

swelling of the arms, hands, feet, ankles, or lower legs

chest pain

slow or irregular heartbeat

rash

hives

itching

difficulty breathing and swallowing

Carvedilol may cause other side effects. Tell your doctor if you experience any unusual problems while you are

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.

Symptoms of overdose may include

slow heartbeat

dizziness

fainting

difficulty breathing

vomiting

loss of consciousness

seizures

What other information should I know?

Keep all appointments with your doctor and the laboratory. Your doctor may order certain laboratory tests to check your body's response to carvedilol.

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:+91-98-21050033

Cellular:+91-98-20150033

Direct :+91-22-65785588

FAX :+91-22-42950001

Wireline Purchase HELPDESK:

+91-22-65050001

+91-22-65650001

Wireline Sales HELPDESK:

+91-22-65500009

+91-22-65050009

Wireless 24x7 HELPDESK:

+9191-46-951951

+9191-46-950950

Blackberry Pin :

32E6500D | 32E65010 | 28415C58

Email:

apollo@Hotmail.Co.in

Sales@apollopharma.in

Export@apollopharma.in

purchase@apollopharma.in

www.apolloworld.in

www.apollopharma.in

www.apollopharmaceuticals.Net

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:400021

Industrial Office

D-62, OIC India

Oshiwara Industrial Centre,

New Link Road,

Goregoan West,

Mumbai, INDIA

Pin:400104

Manufacturing Unit Address:

Plot No. 117A,

Village: Chamble

Near MonaTona Limited.Wada,

Maharashtra,

PIN : 421312 | INDIA

Email:

apollo@Hotmail.Co.in

Sales@apollopharma.in

Export@apollopharma.in

purchase@apollopharma.in

www.apollo.mn | www.apollo.com.co | www.apollopharmaceuticals.Com