Thursday, 26 March 2015

Adrenergic Receptors Blockers

Bind to adrenergic receptors, but inhibit or block the
(nor-epinephrine and epinephrine)Alpha1 and alpha2 receptorsBeta1 and beta2 receptorsCause both arterial and venous dilation, reducing peripheral vascular resistance and BPUsed to treat hypertensionEffect on receptors on prostate gland and bladder decreased resistance toPhentolamineQuickly reverses the potent vasoconstrictive effects of
Restores blood flow and prevents tissue necrosis.Is non-selective linking covalently to both Alpha 1 , postsynaptic and alpha 2, presynaptic receptors the block is irreversible and non-selective .Actions:
On CVS by  blocking Alpha receptors phenoxybenzamine prevents vasoconstriction of peripheral blood vessels by cathecolamines it cause decrease peripheral resistance and provokes a reflux tachycardia.These receptors , when block will result in more norepinephrine release which stimulate Beta receptors on the heart to increase cardiac output.Beta receptors ( Beta 1, Beta 2, Beta 3 ) stimulate adenylyl
Actions:
On CVS:  diminishes cardiac output having both negative inotropic and chronotropic effects, it directly depress SA Node, and AV Node, resulting in bradycardia , cardiac output in Oxygen consumption are decreased by blocking of Beta 1 Receptors. These effects are useful in the treatment of Angina.Alfuzosin ( UROXATRAL )Doxazosin ( CARDURA )Phenoxybenzamine ( REGITINE )Phentolamine ( TEGITINE )Prazosine (MINIPRESS )Tamsulosin ( FLOMAX )Terazosin ( HYTRIN )Yohimbine ( YOCON )Acebutolol (SECTRAL )Atenolol ( TENORMIN )Betaxolol ( BETOPTIC-S, KERLONE )Bisoprolol ( ZEBETA )Carteolol ( CARTROL )Carvedilol ( COREG, COREG CR )Esmolol ( BREVIBLOC )Labetalol ( TRANDATE )Metoprolol ( LOPRESSOR, TOPROL-XL )Nadolol ( CORGARD )Nebevolol ( BYSTOLIC )Penbutolol (LEVATOL )Pindolol ( VISKEN )Propranolol ( INDERAL LA, INNOPRAN XL )Timolol ( BETIMOL, ISTALOL, TIMOPTIC )

    stimulation of the sympathetic nervous system (SNS)
 Sympatholytics inhibit—or LYSE—sympathetic
    neurotransmitters

Classified by the type of adrenergic receptor they block

Alpha-Blockers
    urinary outflow, thus reducing urinary obstruction and relieving effects

    extravasated  vasopressors  such  as  nor -epinephrine or epinephrine.


    cyclase via the coupling protein Gs, which leads to an
    increase in cyclic adenosine monophosphate
    concentration in the cell .

Bronchoconstriction blocking Beta 2, receptor in the lungs of patient cause contraction of bronchial smooth muscle this can precipitate respiratory crisis in patient with COPD



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