PHRM 211 Lecture Notes - Lecture 9: Postmarketing Surveillance, Zopiclone, Rebound Effect
Document Summary
Agonists acting at/very close to bdz site (not exactly known) on gaba a receptors. Enhance gaba-mediated inhibition by increasing cl- influx hyperpolarization. Frequency of gaba-mediated cl- channel openings. Amplitude of gaba-mediated ipsps & lengthen decay phase proportionately. More selective for gaba a -receptors containing the 1 subunit may explain why. Z-drugs are less effective as muscle relaxants and anticonvulsants than bdzs. Changes in nrem sleep (stages 1-4) are minimal at therapeutic doses. Impair psychomotor functioning (at similar rates to bdzs) Cns side effects: somnolence, confusion, behavioural changes, nightmares, ataxia, Elderly are at higher risk for side effects. Dose may need to be lowered in hepatic and renal dysfunction. Overdose is clinically similar to bdz overdose. Post-marketing surveillance showed association with tolerance and physical dependence, particularly with long-term use and higher dosing. Not recommended for patients with a history of, or current, drug abuse problems. Characterized by rebound insomnia, anxiety, agitation, delirium, seizures.
