Carvedilol | apllo +9191 46 950 950apollopharma.in/pdf/Carvedilol.pdfCarvedilol is used for treating...
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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.
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