SEDATIVE-HYPNOTIC DRUGS

Drug Benzodiazepine (Triazolam/Alprazolam/ Lorazepam/Diazepam) -Mediate GABA Hyperpolarization -Anxiolytic (low dose) -Hypnosis (higher dose) -Muscle relaxation -Anticonvulsant -Treat anxiety -Treat insomnia -Treat muscle disorder -Treat convulsion -Sedative and amnestic effects (premedication anaesthesia) -Alcohol withdrawal treatment -Confusion and drowsiness -Ataxia -Withdrawal syndrome (weight gain) -Less drug interaction -Dose-dependent decrease in REM and nonREM wave -Less tolerance and physical dependence -Limited capacity to result fatal CNS depression -Relieve anxiety -Has antagonist (flumazenil) Flumazenil acts as antagonist through: -Decrease sedative effect of BZ -Detoxification of BZ poisoning -Antidote to zolpidem overdose Disadvantage -Anxiolytic occurs after 2-4 weeks (delay anxiolytic) Buspirone Zolpidem Barbiturates

Mechanism of Action Pharmacological Action

-Suppress 5HT -Anxiolytic

-Mediate GABA Hyperpolarization -Hypnotic

-Mediate GABA hyperpolarization -Low doses sedation -High doses anaesthesia -Overdose respiratory failure -Anaesthesia -Anticonvulsant -Lower serum bilirubin in neonatal jaundice by increasing bilirubin conjugation and inducing the activity of glucuronyl transferase enzyme -CNS effects: drowsiness -Drug interaction: P450 induction -Tolerance and physical dependence -Teratogenicity

Therapeutic Uses

-Chronic anxiolytic

Side Effects

Advantage

-No hypnotic -No anticonvulsant -No muscle relaxation -Less psychology impairment than BZ and does not affect driving skill -Less abused liability -No CNS depressant effects

-Rapid onset -Short half life with less day time sleepiness -Less liability to cause sleep pattern change with little rebound insomnia -Less tolerance and dependant during prolonged use -Safe except at large doses respiratory failure -Antagonized by flumazenil

-Short duration of action -Nightmares and daytime drowsiness

Replaced by BV due to: -High incidence of tolerance and physical dependence -Low therapeutic index -Enzyme inducers (drug interaction)

Created by Qosru Iskandariah