What kind of beta-blocker is acebutolol?
Acebutolol belongs to the group of medicines known as beta-blockers. It works on the heart and blood vessels….About acebutolol.
Type of medicine | A beta-adrenoceptor blocking medicine (often referred to as a beta-blocker) |
---|---|
Also called | Sectral® |
Available as | Tablets and capsules |
What is the mechanism of action of acebutolol?
Acebutolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Acebutolol blocks these receptors, lowering the heart rate and blood pressure. This drug then has the reverse effect of epinephrine.
What is the medication acebutolol used for?
Acebutolol is used alone or together with other medicines (such as hydrochlorothiazide) to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly.
Is acebutolol selective or nonselective?
Cardioselective agents (acebutolol, atenolol, betaxolol, bisoprolol, celiprolol, and metoprolol) are as antihypertensive as the nonselective ones (see Fig.
Is acebutolol a non selective beta-blocker?
Acebutolol (a” se bue’ toe lol) is considered a “selective” beta-adrenergic receptor blocker in that it has potent activity against beta-1 adrenergic receptors which are found in cardiac muscle, but has little or no activity against beta-2 adrenergic receptors found on bronchial and vascular smooth muscle.
Is acebutolol a partial agonist?
Acebutolol is a new hydrophilic, cardioselective beta-adrenergic-blocking agent that possesses partial agonist and membrane-stabilizing activities.
What are the functional groups in acebutolol?
Acebutolol is an ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol. It has a role as a beta-adrenergic antagonist, an anti-arrhythmia drug, an antihypertensive agent and a sympathomimetic agent.
Is acebutolol a vasodilator?
As vasodilators, these drugs decrease the workload of the heart and, to some extent, increase coronary blood flow.
Is acebutolol a non-selective beta-blocker?
How are beta-blockers classified?
Beta-blockers that are used clinically can be divided into two classes: 1) non-selective blockers (block both β1and β2 receptors), or 2) relatively selective β1 blockers (“cardioselective” beta-blockers).
Which beta blockers are partial agonists?
Partial agonists are a subclass of beta blockers used for treatment of high blood pressure. Drugs that belong to this class included acebutolol (Sectral), pindolol (Visken) and celiprolol (Cardem).
What drug is a partial agonist?
Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine. Examples of ligands activating peroxisome proliferator-activated receptor gamma as partial agonists are honokiol and falcarindiol.
Is acebutolol an agonist?
Pharmacology. Acebutolol is a cardioselective beta-1 blocker which also considered a partial agonist due to its intrinsic sympathomimetic activity (ISA). This means it provides low-grade beta stimulation at rest but acting as typical beta-blockers when sympathetic activity is high.
Is a beta-blocker an agonist or antagonist?
Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors, of the sympathetic nervous system, which mediates the fight-or-flight response.
Are beta blockers agonists or antagonists?
Are beta blockers negative inotropes?
Negative inotropes include beta-blockers, calcium channel blockers, and antiarrhythmic medicines and they all work in different ways: Beta-blockers “block” the effects of adrenaline on your body’s beta receptors. This slows the nerve impulses that travel through the heart.
What is a pharmacological antagonist?
Listen to pronunciation. (an-TA-guh-nist) In medicine, a substance that stops the action or effect of another substance. For example, a drug that blocks the stimulating effect of estrogen on a tumor cell is called an estrogen receptor antagonist.
Is acebutolol a Cardioselective beta-blocker?
Acebutolol is a cardioselective beta-blocker used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. Acebutolol has been linked to several instances of clinically apparent drug induced liver injury.
Are beta blockers vasodilators or vasoconstrictors?
beta 1-blockers with beta 2 agonist activity are vasodilatory because they activate postsynaptic beta 2 receptors on vascular smooth muscle cell membranes, via the formation of cyclic AMP.
Is a beta blocker a inotropic agent?
What are selective and non selective beta blockers?
Beta-1 selective blockers are preferred for therapy of heart disease, whereas the nonselective beta-blockers are preferred as therapy to prevent recurrent variceal hemorrhage in patients with cirrhosis and portal hypertension.
What is the pharmacokinetics and metabolism of acebutolol?
Pharmacokinetics and Metabolism. Acebutolol crosses the placental barrier and is secreted in breast milk. In geriatric patients, the bioavailability of Acebutolol and its metabolite is increased, approximately two-fold, probably due to decreases in the first-pass metabolism and renal function in the elderly.
What is acebutolol?
Acebutolol is an ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.
What is the structural formula of acebutolol HCl?
Acebutolol HCl, USP has the following structural formula: C 18 H 28 N 2 O 4 •HCl M.W. 372.89 Acebutolol HCl, USP is a white or slightly off-white powder freely soluble in water, and less soluble in alcohol.
Is acebutolol hydrophilic or hydrophobic?
Acebutolol has a low binding affinity for plasma proteins (about 26%). Acebutolol and its metabolite, diacetolol, are relatively hydrophilic and, therefore, only minimal quantities have been detected in the cerebrospinal fluid (CSF).