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1 ADRENERGIC ADRENERGIC ANTAGONITS ANTAGONITS

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Page 1: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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ADRENERGICADRENERGIC ANTAGONITS ANTAGONITS

Page 2: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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ADRENERGIC BLOCKERSADRENERGIC BLOCKERSALPHA BLOCKERS

Alpha 1 Blockers Nonselective Alpha

BlockersDoxazosin PhenoxybenzaminePrazosin PhentolamineTerazosin

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BETA BLOCKERSNon Selective Beta 1 selective

Blockers Blockers

Propranolol Metoprolol Timolol AtenololNadolol Esmolol Acebutolol Betaxolol Labetalol - Both Alpha and Beta BLocker

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DRUGS AFFECTING NEUROTRANSMITTER UPTAKE OR RELEASE

CocaineGuanethidineReserpine

Page 5: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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PhenoxybenzaminePhenoxybenzamine

Blocks alpha 1 and 2, irreversible blockade MOSTLY

Actions - prevents V.C,

Epinephrine reversal

Therapeutic uses : – Opposing catecholamines --pheochromocytoma– Causes vasodilation

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SE:Postural hypotensionSexual dysfunction TachycardiaContraindicated in ↓ coronary perfusion.

Page 7: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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PhentolaminePhentolamine

Alpha 1 and 2 blockerDuration of action lessUses & SE – mostly same as

Phenoxybenzamine.

Page 8: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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Alpha 1 specific blockersAlpha 1 specific blockers

PrazosinTerazosinDoxazosin – long acting

Page 9: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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Actions ----- Dose ---- Uses ----- Side effects ----

CVS Avoid high doses HTN

Orthostatic hypotension Nasal stuffiness Fatigue Sexual dysfunction

(less)

Page 10: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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Non selective beta antagonistsNon selective beta antagonists

PropranololTimololNadolol

Page 11: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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PropranololPropranolol

CVS – HR ↓ , CO ↓PERIPHERAL VESSELS – NO ALPHA

ACTIONBRONCHI - ↑ CONTRACTIONSODIUM LEVELS - ↑GLYCOGENOLYSIS -↓ GLUCAGON - ↓BLOCKS DRUGS – Isoproterenol , & β actions of epinephrine

Page 12: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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USESUSES

HTN ---- decreases COANGINA---decreases oxygen demandMI---- protects myocardiumGLAUCOMA-- TimololMIGRAINEHYPERTHYROIDISM– blunts

sympathetic stimulation

Page 13: 1 ADRENERGIC ANTAGONITS. 2 ADRENERGIC BLOCKERS ALPHA BLOCKERS Alpha 1 Blockers Nonselective Alpha Blockers Doxazosin Phenoxybenzamine Prazosin Phentolamine

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SIDE EFFECTSSIDE EFFECTS

BRONCHOCONSTRICTIONCONTRAINDICATION –ASTHMA,

COPDARRHYTHMIAS – gradual reduction in

doseSEXUAL IMPAIREMENT

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NON SELECTIVE BETA NON SELECTIVE BETA ANTAGONISTSANTAGONISTS

TIMOLOLNADOLOL → very long duration of action

Considered more potent than propranolol.

Same effects and SE as propranolol.

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SELECTIVE BETA 1 SELECTIVE BETA 1 ANTAGONISTSANTAGONISTS

ATENOLOLMETOPROLOLESMOLOL

USES – HTN,ANGINACAN BE USED IN COPD, DM CASES

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ANTAGONISTS AND ANTAGONISTS AND PARTIAL AGONISTSPARTIAL AGONISTS

PINDOLOLACEBUTOLOL

USES : HTN with moderate bradycardia

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ALPHA AND BETA ALPHA AND BETA BLOCKERBLOCKER

LABETALOL

Peripheral vasodilation -- ↓ B.PNo vasoconstrictive effectUSES : OLD AGE HTN, PIHSE: Orthostatic hypotension and dizziness.

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NT AFFECTING DRUGSNT AFFECTING DRUGSRESERPINE

- CYTOPLASM TO STORAGE VESICLE

USES -- ↓B.P. ↓ H.R

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NT AFFECTING DRUGSNT AFFECTING DRUGS

GUANETHIDINE

–BLOCKS RELEASEOF NE IN VESICLE TO MEMBRANE

USES—gradual lowering of B.P and H.R. in hypertensives

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NT AFFECTING DRUGSNT AFFECTING DRUGS

COCAINE Block Na-K ATPaseREUPTAKE DECREASED (NE)USES ----local anesthetic???