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Alpha blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). [2] Historically, alpha-blockers were used as a tool for pharmacologic research to develop a greater understanding of the autonomic nervous system.
Alpha 2 blockers. Alpha 2 blockers inhibit the activation of adenylyl cyclase via Gi protein by antagonising alpha 2 receptors, which curbs the synthesis of cyclic AMP (cAMP). [1] This subsequently reduces the concentration of calcium and the release of neurotransmitters, resulting in smooth muscle dilation. [1] Beta 1 blockers
Alpha-1 blocker, blocks alpha receptors and it relaxes the smooth muscles in the bladder. It helps the urine to flow smoothly and it can lessen the pain caused by the bladder pressing on the prostate. [44] [45] Selective alpha-1 blockers are better tolerated than non-selective alpha blockers in the body and therefore works better on BPH. [2]
The second group contains the alpha (α) adrenoreceptors. There are only α 1 and α 2 receptors. Adrenergic receptors are located near the heart, kidneys, lungs, and gastrointestinal tract. [1] There are also α-adreno receptors that are located on vascular smooth muscle. [2] Antagonists reduce or block the signals of agonists.
Tamsulosin is an alpha blocker and works by relaxing muscles in the prostate. [10] Specifically it is an α 1-adrenergic receptor blocker. [6] Tamsulosin was approved for medical use in the United States in 1997. [6] It is available as a generic medication. [9]
Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They are used as antihypertensives because they block alpha-receptor-mediated vasoconstriction. The block on alpha-2 receptors further potentiates beta-effects, increasing cardiac output.
Alfuzosin, sold under the brand name Uroxatral among others, is a medication of the α 1 blocker class. It is used to treat benign prostatic hyperplasia (BPH). [1]As an antagonist of the α 1-adrenergic receptor, it works by relaxing the muscles in the prostate and bladder neck, making urination easier.
The depolarizing blockers already have ACh-like actions, so these agents have prolonged effect under the influence of acetylcholinesterase inhibitors. Administration of depolarizing blockers initially produces fasciculations (a sudden twitch just before paralysis occurs). This is due to depolarization of the muscle.