Carvedilol
Encyclopedia
Carvedilol is a non-selective beta blocker
/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure
(CHF). It is marketed under various trade name
s including Carvil (Zydus Cadila), Coreg (GSK
), Dilatrend (Roche), Eucardic (Roche), and Carloc (Cipla
) as a generic drug (as of September 5, 2007 in the U.S.)., and as a controlled-release formulation, marketed in the US as Coreg CR (GSK
). Carvedilol was discovered by Robert R. Ruffolo, Jr
. It has had a significant role in the treatment of Congestive heart failure
.
(β1, β2) and alpha blocker
(α1):
Relative to other beta blockers, carvedilol has minimal inverse agonist
activity. This suggests that carvedilol has a reduced negative chronotropic
and inotropic effect compared to other beta blockers, which may decrease its potential to worsen symptoms of heart failure. However, to date this theoretical benefit has not been established in clinical trials, and the current version of the ACC/AHA guidelines on congestive heart failure management does not give preference to carvedilol over other beta-blockers.
, fatigue, hypotension
, diarrhea
, asthenia, bradycardia
, and weight gain
.
A case report of a patient with panic disorder associated sleep disturbances and nightmares with the improper usage of carvedilol.
s with distinct pharmacodynamics.
The term "racemic
carvedilol" is sometimes used to explicitly denote that both enantiomers are applied.
(CHF), as an adjunct to conventional treatments (ACE inhibitor
s and diuretic
s). The use of carvedilol has been shown to provide additional morbidity and mortality
benefits in CHF. Carvedilol (Carvil) is available at the following doses 3.125 mg (smallest), followed by 6.25 mg,12.5 mg, and 25 mg white tablets.
Beta blocker
Beta blockers or beta-adrenergic blocking agents, beta-adrenergic antagonists, beta-adrenoreceptor antagonists or beta antagonists, are a class of drugs used for various indications. They are particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction ,...
/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure
Congestive heart failure
Heart failure often called congestive heart failure is generally defined as the inability of the heart to supply sufficient blood flow to meet the needs of the body. Heart failure can cause a number of symptoms including shortness of breath, leg swelling, and exercise intolerance. The condition...
(CHF). It is marketed under various trade name
Trade name
A trade name, also known as a trading name or a business name, is the name which a business trades under for commercial purposes, although its registered, legal name, used for contracts and other formal situations, may be another....
s including Carvil (Zydus Cadila), Coreg (GSK
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
), Dilatrend (Roche), Eucardic (Roche), and Carloc (Cipla
Cipla
Cipla Limited is a prominent Indian pharmaceutical company, best-known outside its home country for manufacturing low-cost anti-AIDS drugs for HIV-positive patients in developing countries...
) as a generic drug (as of September 5, 2007 in the U.S.)., and as a controlled-release formulation, marketed in the US as Coreg CR (GSK
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
). Carvedilol was discovered by Robert R. Ruffolo, Jr
Robert R. Ruffolo, Jr
Robert R Ruffolo was President of Research and Development for Wyeth Pharmaceuticals, and corporate Senior Vice President of Wyeth from 2001 to 2008...
. It has had a significant role in the treatment of Congestive heart failure
Congestive heart failure
Heart failure often called congestive heart failure is generally defined as the inability of the heart to supply sufficient blood flow to meet the needs of the body. Heart failure can cause a number of symptoms including shortness of breath, leg swelling, and exercise intolerance. The condition...
.
Pharmacology
Carvedilol is both a beta blockerBeta blocker
Beta blockers or beta-adrenergic blocking agents, beta-adrenergic antagonists, beta-adrenoreceptor antagonists or beta antagonists, are a class of drugs used for various indications. They are particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction ,...
(β1, β2) and alpha blocker
Alpha blocker
Alpha-1 blockers constitute a variety of drugs which block α1-adrenergic receptors in arteries and smooth muscles.-Pharmacology:...
(α1):
- Norepinephrine stimulates the nerves that control the muscles of the heart by binding to the β1- and β2-adrenergic receptorAdrenergic receptorThe adrenergic receptors are a class of metabotropic G protein-coupled receptors that are targets of the catecholamines, especially noradrenaline and adrenaline ....
s. Carvedilol blocks the binding to those receptors, which both slows the heart rhythm and reduces the force of the heart's pumping. This lowers blood pressure thus reducing the workload of the heart, which is particularly beneficial in heart failure patients.
- Norepinephrine also binds to the α1-adrenergic receptors on blood vessels, causing them to constrict and raise blood pressure. Carvedilol blocks this binding to the α1-adrenergic receptors too, which also lowers blood pressure.
Relative to other beta blockers, carvedilol has minimal inverse agonist
Inverse agonist
In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....
activity. This suggests that carvedilol has a reduced negative chronotropic
Chronotropic
Chronotropic effects are those that change the heart rate.Chronotropic drugs may change the heart rate by affecting the nerves controlling the heart, or by changing the rhythm produced by the sinoatrial node...
and inotropic effect compared to other beta blockers, which may decrease its potential to worsen symptoms of heart failure. However, to date this theoretical benefit has not been established in clinical trials, and the current version of the ACC/AHA guidelines on congestive heart failure management does not give preference to carvedilol over other beta-blockers.
Side effects
The most common side effects include dizzinessDizziness
Dizziness refers to an impairment in spatial perception and stability. The term is somewhat imprecise. It can be used to mean vertigo, presyncope, disequilibrium, or a non-specific feeling such as giddiness or foolishness....
, fatigue, hypotension
Hypotension
In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...
, diarrhea
Diarrhea
Diarrhea , also spelled diarrhoea, is the condition of having three or more loose or liquid bowel movements per day. It is a common cause of death in developing countries and the second most common cause of infant deaths worldwide. The loss of fluids through diarrhea can cause dehydration and...
, asthenia, bradycardia
Bradycardia
Bradycardia , in the context of adult medicine, is the resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min. It may cause cardiac arrest in some patients, because those with bradycardia may not be pumping enough oxygen to their heart...
, and weight gain
Weight gain
Weight gain is an increase in body weight. This can be either an increase in muscle mass, fat deposits, or excess fluids such as water.-Description:...
.
A case report of a patient with panic disorder associated sleep disturbances and nightmares with the improper usage of carvedilol.
Enantiomers
Carvedilol has enantiomerEnantiomer
In chemistry, an enantiomer is one of two stereoisomers that are mirror images of each other that are non-superposable , much as one's left and right hands are the same except for opposite orientation. It can be clearly understood if you try to place your hands one over the other without...
s with distinct pharmacodynamics.
The term "racemic
Racemic
In chemistry, a racemic mixture, or racemate , is one that has equal amounts of left- and right-handed enantiomers of a chiral molecule. The first known racemic mixture was "racemic acid", which Louis Pasteur found to be a mixture of the two enantiomeric isomers of tartaric acid.- Nomenclature :A...
carvedilol" is sometimes used to explicitly denote that both enantiomers are applied.
Clinical use
Carvedilol is indicated in the management of congestive heart failureCongestive heart failure
Heart failure often called congestive heart failure is generally defined as the inability of the heart to supply sufficient blood flow to meet the needs of the body. Heart failure can cause a number of symptoms including shortness of breath, leg swelling, and exercise intolerance. The condition...
(CHF), as an adjunct to conventional treatments (ACE inhibitor
ACE inhibitor
ACE inhibitors or angiotensin-converting enzyme inhibitors are a group of drugs used primarily for the treatment of hypertension and congestive heart failure...
s and diuretic
Diuretic
A diuretic provides a means of forced diuresis which elevates the rate of urination. There are several categories of diuretics. All diuretics increase the excretion of water from bodies, although each class does so in a distinct way.- Medical uses :...
s). The use of carvedilol has been shown to provide additional morbidity and mortality
Death
Death is the permanent termination of the biological functions that sustain a living organism. Phenomena which commonly bring about death include old age, predation, malnutrition, disease, and accidents or trauma resulting in terminal injury....
benefits in CHF. Carvedilol (Carvil) is available at the following doses 3.125 mg (smallest), followed by 6.25 mg,12.5 mg, and 25 mg white tablets.