Anesthesia

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Droperidol

Sat, 11/03/2007 - 14:05 — oxygen
Your Ad Here DROPERIDOL Listen to Audio mechanism of action structure-activity relationship pharmacokinetics effects on organ systems drug interactions MECHANISM OF ACTION Central effects: -dopamine receptor antagonist -interferes with serotonin, norepinephrine, and GABA transmission -therefore leads to tranquilizing and antiemetic effects Peripheral effects: -alpha adrenergic blockade -therefore may lead to decreased mean arterial pressure STRUCTURE-ACTIVITY RELATIONSHIPS -butyrophenone -structurally related to haloperidol PHARMACOKINETICS Absorption -usually give intravenously although may occasionally be given intramuscularly as a premedication regimine Distribution -rapid redistribution phase of 10 minutes -delayed sedative effects due to relatively large molecular weight and extensive protein binding -large molecular weight and extensive protein binding slows the pentration of the BBB -prolonged duration of action due to strong receptor binding Biotransformation metabolized extensively in the liver -rapid hepatic clearance Excretion -excreted primarily by the kidney into the urine PHARMACODYNAMICS Effects on Organ Systems Central nervous system -CMR02 not reduced unlike the effects of other induction agents (excluding ketamine) -decreases CBF -decreases ICP secondary to vasoconstriction of cerebral vasculature -potent antiemetic activity -delayed awakening therefore intraoperative use may be limited to small doses (ex. 0.05 mg/kg - 2.5 mg) -may rarely precipitate extrapyramidal reactions (ex. oculogyric crises, torticollis) -avoided in parkinsonian patients Cardiovascular system -decreases mean arterial pressure by peripheral vasodilation from mild alpha adrenergic blockade -may have exaggerated hypotensive effects in hypovolemic patients -antidysrhythmic effects possibly from alpha adrenergic blockade -should be avoided inpatients with pheochromocytoma due to associated catecholamine release from the adrena medulla Respiratory system -when given alone at usuall doses: no significant ventilatory depression -possibly may stimulate hypoxic ventilatory drive Drug Interactions -may preciptate parkinson symptoms -may antagonize effects of levodopa

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