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÷
O
÷. Ĵ1 selective
Prazosin
Terazosin
Doxazosin
Tamsulosin
C. Ĵh selective
yohimbine
(
The shorter the half-life of the drug in the body, the less time
it takes for the effects of the drug to dissipate .
These drugs can prevent the pressor effects of usual doses ofĴ
agonists.
Release of histamine.
Ot stimulates the GOT smooth muscles
Dose: 5 mg i.v.
Ot is a competitive Ĵ1 antagonist.
Tamsulosin has higher affinity for Ĵ1A and Ĵ1D receptors than for
the Ĵ1÷ subtype .
Ot has a high bioavailability & is extensively metabolized in the
liver .
Tamsulosin has greater potency in inhibiting contraction in
prostate smooth muscle.
Tamsulosin has less effect on standing blood pressure .
Alfuzosin : it is Ĵ1 selective quinazoline derivative that is used in
the treatment of ÷HP
Ot has a bioavailability of about 60% & has an elimination half-
life of about 5 hours.
Ondoramin it is another Ĵ1-selective antagonist that also has
Ondoramin:
efficacy as an antihypertensive.
Yohimbine
Yohimbine: Ot is an indole alkaloid, is an Ĵ2-selective antagonist.
Ot is in the treatment of orthostatic hypotension.
Yohimbine can reverse the antihypertensive effects of an 2-
adrenoceptor agonist such as clonidine .
V
Ô
Ô
prazosin & phenoxybenzamine are used in the treatment of
peripheral vascular occlusive disease like Raynaud's disease.
Prazosin, doxazosin, and terazosin are all efficacious in patients
with ÷PH
These drugs are useful in patients who also have hypertension.
The mechanism of action is by partial reversal of smooth muscle
contraction in the enlarged prostate and in the bladder base.
Orthostatic hypotension
Reflex tachycardia
Hypotension
Nasal stuffiness