Nupovel Mechanism of Action

Pharmacotherapeutic group: Other general anesthetics. ATC code: N01AX10.
Pharmacology: Pharmacodynamics: Mechanism of Action: Propofol is a short-acting lipophilic intravenous general anesthetic. The drug is unrelated to any of the currently used barbiturate, opioid, benzodiazepine, arylcyclohexylamine, or imidazole intravenous anesthetic agents. Propofol causes global CNS depression, presumably through agonism of GABA_A receptors and perhaps reduced glutamatergic activity through N-methyl-D-aspartate (NMDA) receptor blockade.
Pharmacokinetics: Absorption: Onset of action: Anesthetic: Bolus infusion (Dose dependent): 9-51 seconds (average 30 seconds).
Duration: 3-10 minutes depending on the dose, rate and duration of administration; with prolonged use (10 days ICU sedation) propofol accumulates in tissues and redistributes into plasma when the drug is discontinued, so that the time to awakening (duration of action) is increased; however, if dose is titrated on a daily basis so that the minimum effective dose is utilized, time to awakening may be within 10 to 15 minutes even after prolonged use.
Distribution: Large volume of distribution; highly lipophilic.
V_d: Children 4-12 years: 5-10 L/kg.
Adults: 2-10 L/kg; after a 10-day infusion V_d approaches 60 L/kg; decreased in the elderly.
Protein binding: 97%-99%.
Metabolism: Hepatic to water soluble sulphate and glucuronide conjugates (∼50%).
Half-life elimination: Biphasic: Initial 40 minutes; Terminal: 4-7 hour (after 10 days infusion, may be up to 1-3 days).
Excretion: Urine (∼88% as metabolites, 40% as glucuronide metabolite); feces (<2%).