Study Set Content:
This is due to an action of the drug on endothelial
()
• Nebivolol may increase insulin sensitivity and
does not adversely affect ()
nitric oxide production, lipid profile
is a B1-selective antagonist with a
modest capacity to activate B 2 receptors.
Celiprolol
There is limited evidence suggesting that celiprool
may have less adverse bronchoconstrictor effect in
asthma and may even promote
bronchodilation
is also a B 1-selective antagonist
Acebutolol
is a reversible adrenoceptor antagonist available
as a racemic mixture of two pairs of chiral isomers.
LABETALOL
Labetalol's affinity for a receptors is less than
that of (), but labetalol is a 1-selective.
Its ß-blocking potency is somewhat lower than
that of
phentolamine ,propanolol
Hypertension induced by labetalol is
accompanied by less tachycardia than occurs with
() and similar a blockers.
phentolamine
antagonizes the actions more potently
at 3 receptors than at a 1 receptors.
Carvedilol
Carvedilol antagonizes the actions more potently
at 3 receptors than at a 1 receptors. Has a half-life
of
6-8 hours.
Metabolism of (RJ-carvedilol is
influenced by polymorphisms in ()
and by drugs that inhibit this enzyme's activity
such as quinidine and fluoxetine, drug
interactions may occur.
CYP2D6 activity
Carvedilol inhibit vascular smooth muscle
() independently of adrenoceptor
blockade. These effects may contribute to the
clinical benefits of the drug in chronic heart
failure.
mitogenesis
Is an ultra-short-acting B 1-selective adrenoceptor
antagonist
ESMOLOL
Esmolol has a () half-life (about 10 minutes).
During continuous infusions of esmolol, steady- state concentrations are achieved quickly, and the
therapeutic actions of the drug are terminated
rapidly when its Infusion is discontinued.
short
is useful in controlling supraventricular
arrhythmias, arrhythmias associated with
thyrotoxicosis, perioperative hypertension, and
myocardial ischemia in acutely ill patients
Esmolol
is a research drug selective for ß 2
receptors.
Butoxamine
have not been
actively sought because there is no obvious clinical
application for them;
• none is available for clinical use.
Selective B 2-blocking drugs
have proved to
be effective and well tolerated in hypertension.
The B-adrenoceptor-blocking drugs
Many hypertensive patients respond to B blocker
used alone, is often used with either a () or a
()
diuretic , vasodilator
In spite of the short half-life of many ()
these drugs may be administered once or twice daily
and still have an adequate therapeutic effect.
B antagonists,
a competitive a and B antagonist, is
effective in hypertension.
Labetalol,
