Adrenoreceptor

antagonist drugs

Report by:

Asmiyah M. Currie
Adrenoreceptor antagonist - also called
adrenergic blockers or sympatholytic agents.

bind to adrenoceptors but do not trigger the usual

receptor-mediated intracellular effect.

The adrenergic antagonists are classified according to

the their relative affinities for α or β receptors.
Alpha blockers (alpha receptor
antagonist)

Alpha-receptor antagonists may be reversible or

irreversible in their interaction with these receptors

subdivided into two groups:

 Non-selective alpha blocker
 Selective alpha blockers
Non-selective alpha blockers
-can lower blood pressure
- treatment for HTN especially cause by
pheochromocytoma

 Phenoxybenzamine-
 Binds covalently to both a 1 & a 2 receptor
 Irreversible non-competitive
 Long duration of action(24 hrs.)

 Phentolamine-
 Reversible competitive for a 1 & a 2 receptor
 Short duration of action (4hrs.)
Selective alpha blockers:

 Alpha 1 blockers
 Alpha 2 blockers
Alpha 1 blockers(selective)
Ex: prasozine
doxazosin effective treatment for hypertension but lesser effect on enlarge prostate
terazosin
tamsulosin
alfuzosin little effect on blood pressure but more effective in enlarge prostate

Peripheral vascular resistance

Blood pressure

Note: the ending with “osin” is an alpha blockers

Side effects
 Orthostatic hypertension is one of the main
concerns when initiating alpha 1 blockers
although its not severe as that observe with non
selective alpha blockers.

Additionally, vasodilation produce by alpha 1 blockers

can lead to headache and nasal congestion
Alpha 2 blockers

Ex:
Yohimbine-
 limited application in human and they used mainly in research.
 Can be found in dietary supplement
 Used sometimes in veterinary medicine to reverse sedative
effects
 Used as sexual stimulant
 Treatment of erectile dysfunction
Beta blockers(Beta receptor
antagonist)
-are also sub dived to selective and non-selective

-block the beta receptor

-Reduce blood pressure
-treatment of HNT,Heart failure, angina & cardiac arrhythmias
-Work by blocking the effects of the hormone
epinephrine

“The names of all β-blockers end in “-olol” except for

labetalol and carvedilol”
Beta 1 blockers
-located in the heart 1
-decrease the heart rate

Activation: Blockade:

- Cause tachycardia -cause Bradycardia

-cardiac output -cardiac output
- HR -Blood pressurre
- HR
Beta 2 blockers
 Located in skeletal muscle blood vessel

Activation: Blockade:

-cause vasodilation -vasoconstriction

peripheral resistance
Also…
Beta 2 blockers
 Located in the Lungs

Activation: Blockade:

-cause Bronchodilation -cause Bronchoconstriction

Should not be used for patient with COPD and Asthma

Non-selective beta blockers
 Acts on beta 1 and beta 2 receptor
 Treatment for hypertension
 Angina pectoris
 Myocardial infraction

(1st generation)
Ex: propranolol- do to its lipophilicity, can also penetrate into
the CNS and was found to be effective for migraine.

nadolol- more potent

- very long duration of action
- long term management for angina
Timolol- ( eye drop )
-traetment for Open angled glaocoma- production of
aqueous humor in the eye
Betaxolol- selective beta 1blocker
sotalol
(2nd generation)

Selective beta 1 blockers

also called (cardio selective)

-can antagonize beta 2 receptor at high doses

fewer effects on pulmonary function peripheral
resistance
-lower BP & HTN
-increase exercise tolerance & angina
Ex:
 Acebutalol
 Atenolol-used for hypertensive patient with
impaired pulmunary function
 Betaxolol
 Bisoprolol
 Metoprolol-indicated for management of chronic
heart failure
 Esmolol-very short half-life, used to control BP or
heart rhythm during surgery or diagnostic
procedures
-administered via (IV)
(3rd generation)
Beta blockers
-include both non-selective and selective

 Acts on Blood vessel to cause vasodilation

(non-selective agents)

Ex. Carvedilol &labetalol

-(produce peripheral vasodilation by blocking not only beta but
also alpha 1receptors)
(Selective agents)

Ex: nebivolol – which produce vasodilation by inducing the

release of nitric oxide from endothelial cells.

betaxolol-(produce vasodilation by blocking

calcium channel
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