Most of the alpha-1 adrenergic receptors are located on the vascular smooth muscle (in the skin, sphincters of the gastrointestinal system, kidney, and brain) and cause vasoconstriction when activated by catecholamines such as epinephrine and norepinephrine (NE). The vasoconstriction causes an increase in both systemic arterial blood pressure and peripheral resistance. There are two types of alpha-adrenergic receptors: alpha-1 and alpha-2. Īlpha-blockers produce their pharmacological effects through alteration of the sympathetic nervous system. Idazoxan is being used in research, but has no established clinical role has established. Yohimbine has been used to treat male sexual dysfunction, although the effectiveness has not yet been established and is not currently FDA approved for this use or any other uses. Selective alpha-2 blockers include the medications yohimbine and idazoxan. However, they are not typically first-line agents for the management of hypertension. These medications may also be options to treat essential hypertension. These medications are FDA approved to treat benign prostatic hyperplasia (BPH). Selective alpha-1 blocker ends with the suffix "-osin." These medications include alfuzosin, doxazosin, terazosin, tamsulosin, and prazosin. Although it is worth mentioning that it is not a first-line agent for this condition. In this situation, the use of β-blockers is less desirable due to the risk of unopposed α-adrenergic receptor-mediated coronary vasoconstriction and hypertension. Phentolamine sees occasional use in the treatment of cocaine-induced cardiovascular complications. Phenoxybenzamine is irreversible and phentolamine is reversible alpha-blockers. Both are used intraoperatively to manage hypertensive crisis during pheochromocytoma removal. Both of these medications have FDA approval for use in patients with pheochromocytoma. Nonselective alpha-blockers include phenoxybenzamine and phentolamine. Nonselective Alpha-blockers (alpha-1 and alpha-2) Alpha-blockers fall into three different categories.ġ.
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