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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]
Mechanism of Action of Alpha -1 blocker. Alpha 1 blocker exerts its action on alpha-1 receptor, dilating the smooth muscles. [3] Alpha-1 receptor is a Gq type G-protein coupled receptor. [3] When it is activated, it will lead to activation of phospholipase C, raising the intracellular level of IP3 and DAG. [3]
When the term "alpha blocker" is used without further qualification, it can refer to an α 1 blocker, an α 2 blocker, a nonselective blocker (both α 1 and α 2 activity), or an α blocker with some β activity. [2] However, the most common type of alpha blocker is usually an α 1 blocker. Non-selective α-adrenergic receptor antagonists include:
Alpha 1 blockers cause vasodilation by relaxing smooth muscles that control blood vessel diameter, leading to lower blood pressure. [1] FDA-approved uses of these drugs include treating conditions like benign prostatic hyperplasia, hypertension, pheochromocytoma, extravasation management, and reversal of local anesthesia.
alpha-1 (α 1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the G q heterotrimeric G protein. α 1-adrenergic receptors are subdivided into three highly homologous subtypes, i.e., α 1A-, α 1B-, and α 1D-adrenergic receptor subtypes.
Alpha-blockers can block alpha-1 adrenergic receptors and/or alpha-2 adrenergic receptors. [34] Those that block alpha-1-adrenergic receptors on vascular smooth muscle cells prevent vasoconstriction. [34] Blockade of alpha-2-adrenergic receptors prevents the negative feedback mechanism of norepinephrine (NE). [34]
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.
An equianalgesic chart is a conversion chart that lists equivalent doses of analgesics (drugs used to relieve pain). Equianalgesic charts are used for calculation of an equivalent dose (a dose which would offer an equal amount of analgesia) between different analgesics. [1]