Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism.

Article Details

Citation

Nash DT

Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism.

Clin Cardiol. 1990 Nov;13(11):764-72.

PubMed ID
1980236 [ View in PubMed
]
Abstract

The sympathetic nervous system plays a major role in the pathogenesis of essential hypertension and is mediated by the alpha and beta receptors. The alpha receptor is divided into two types, alpha 1 and alpha 2, based on response to epinephrine and norepinephrine. alpha 1-Adrenergic receptors have a high affinity for drugs such as prazosin, doxazosin, and terazosin, which act to reduce blood pressure by selective blockade of the receptor. These agents provide a rational approach to the treatment of hypertension by correcting elevated total peripheral resistance, the fundamental hemodynamic abnormality in essential hypertension. In contrast, early alpha-adrenergic receptor blockers nonselectively blocked both alpha 1 and alpha 2 receptors and were unsuitable as antihypertensive agents because they induced tachycardia and patients developed a tolerance to them rapidly. alpha 1-Adrenergic blockers also have beneficial effects on plasma lipoproteins, tending to decrease levels of triglycerides and cholesterol and increase levels of high-density lipoprotein (HDL) cholesterol and the HDL cholesterol/total cholesterol ratio. beta-Adrenergic blockers, such as propranolol and atenolol, have been shown to have an adverse effect on the lipid profile by tending to increase levels of triglycerides and decrease HDL cholesterol. A number of mechanisms contribute to these effects, in particular, adrenergic modulation of lipoprotein lipase and the triglyceride secretion rate. Doxazosin has been shown to increase the activity of LDL receptors, which may be partly responsible for its beneficial effect on plasma lipids and lipoproteins.(ABSTRACT TRUNCATED AT 250 WORDS)

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
EpinephrineAlpha-2A adrenergic receptorProteinHumans
Yes
Agonist
Details
EpinephrineAlpha-2B adrenergic receptorProteinHumans
Yes
Agonist
Details
NorepinephrineAlpha-2A adrenergic receptorProteinHumans
Yes
Agonist
Details
NorepinephrineAlpha-2B adrenergic receptorProteinHumans
Yes
Agonist
Details
NorepinephrineAlpha-2C adrenergic receptorProteinHumans
Yes
Agonist
Details
Drug Interactions
DrugsInteraction
Arbutamine
Profenamine
The therapeutic efficacy of Arbutamine can be decreased when used in combination with Profenamine.
Arbutamine
ORM-12741
The therapeutic efficacy of Arbutamine can be decreased when used in combination with ORM-12741.
Arformoterol
Profenamine
The therapeutic efficacy of Arformoterol can be decreased when used in combination with Profenamine.
Arformoterol
ORM-12741
The therapeutic efficacy of Arformoterol can be decreased when used in combination with ORM-12741.
Avanafil
Prazosin
Prazosin may increase the hypotensive activities of Avanafil.
Avanafil
Labetalol
Labetalol may increase the hypotensive activities of Avanafil.
Avanafil
Phentolamine
Phentolamine may increase the hypotensive activities of Avanafil.
Avanafil
Tolazoline
Tolazoline may increase the hypotensive activities of Avanafil.
Avanafil
Phenoxybenzamine
Phenoxybenzamine may increase the hypotensive activities of Avanafil.
Avanafil
Terazosin
Terazosin may increase the hypotensive activities of Avanafil.
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