pharmacology of adrenergic neuron blockers
TRANSCRIPT
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PHARMACOLOGY OF ADRENERGIC
NEURON BLOCKERS
Shahan UllahMPhil Pharmacology
Institute of Basic Medical SciencesKhyber Medical University Peshawar
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ADRENERGIC NEURON BLOCKERS
Reserpine Guanethidine Bretylium
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MECHANISM
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MECHANISM OF ACTIONS RESERPINE It blocks the Mg/ATP dependent
VESICULAR MANO AMINE TRANSPORTER(VMAT)
GUANATHEDINE/BRETYLIUM It inhibits nerve impulse coupled N.A
release from vesicles(bretylium). Displaces N.A from storage vesicles Engages and blocks the N.A reuptake at
axonal membrane.(REUPTAKE 1)
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RESERPINEORGAN/SITE ACTIONCENTRAL NERVOUS YSTEM ↓ dopamine
↓ serotonin↓ nor adrenaline
CARDIOVASCULAR SYSTEM ↓ cardiac output↓ vascular resistance
GIT Ultimate increase motilityUltimate increased secretions
Reproductive system Decrease in libidoNasal region Turbinate lateral wall size
increaseEye Dilator pupillae are blockedMetabolism Anti diabetogenic
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THERAPEUTIC ACTION
RESERPINE
Anti-Hypertensi
ve
Anti-Emeti
cAnti-
Psychotic
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ADVERSE EFFECTS
Organ/site EffectCENTRAL NERVOUS SYSTEM DEPRESSION (suicidal
tendency)NIGHTMARESEXTRA PYRAMIDAL (PARKINSON) EFFECTS
CARDIOVASCULAR SYSTEM MILD POSTURAL HYPOTENSION
GIT DIARRHOEAACIDITY
NASAL REGION NASAL CONGESTIONREPRODUCTIVE SYSTEM DELAYED EJACULATION
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CONTRA INDICATIONS
PEPTIC ULCER
DEPRESSION
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GUANETHIDINE.
Lowering of BP
Triphasic response
Biphasic response
Monophasic
response
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GUANETHIDINEORGAN/SITE ACTIONCENTRAL NEROUS SYSTEM DOESN’T CROSS BBBRENAL ↓INITIAL BLOOD FLOW,
(regulatory action)GASTRO INTESTINAL TRACT INCREASE MOTILITY(PSNS)
INCREASE SECRETIONS(PSNS)
EYE DECREASE I.O.TMIOSIS
NASAL REGION INCREASE SIZE OF TURBINATE LATERAL WALLS (INCREASE CORONARY FLOW)
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ADVERSE EFFECTS Postural hypotension Weakness Diarrhoea Delayed or retrograde ejaculation Nasal stuffiness It cause super sensitivity of receptors
leading to regulation of α1 receptors causing intense vasoconstriction (HTN crisis)
Fluid retention (long term use tolerance develops)
Worsening of CCF.
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THERAPEUTIC PURPOSES ANTI HYPERTENSIVE(Last choice
therapy) For management of Pheochromocytoma
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BRETYLIUM ACTIVITY Prolongs duration of ventricular action potential It prolongs the refractory period of ischemic heart
tissue and decreases its excitability(by blocking K+ channels)
Also blocks N.A release. THERAPEUTIC USE Anti- arrhythmic Anti-hypertensive ADVERSE EFFECTS Postural hypotension Bradycardia Nausea/Vomiting
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