DRUGS FOR CNS DISORDERS

SEDATIVE-HYPNOTIC DRUGS

MOA Pharmacologic Drugs Adverse Antagonist

Properties Reactions

Benzodiazepines Opening of GABA ONSET SHORT ACTING DOSE-RELATED Flumazenil

activated Cl channels Highly lipid soluble > A,T,O,M CNS depression Competitive
Bind to regulatory site Less lipid soluble Anterograde amnesia antagonist
on GABA a-receptor INTERMEDIATE ACTING Given IV
DURATION RAZE, MAZE, NAZE Low dose = Half-life: 0.7-1.3 hrs
Short-acting = Insomnia Drowsiness, impaired
Long-acting = Anxiety LONG ACTING judgment, diminished Adverse effects:
Diazepam + Chlor- motor skills Agitation,
Confusion,
High dose = Lethargy, Dizziness, Nausea
state of exhaustion,
respiratory depression,
coma

Barbiturates GABA A receptors ABSORPTION ULTRA-SHORT (0.5-1) Drowsiness

Prolonging duration of Well-absorbed orally Thiopental Impaired
Sedative Cl channel openings concentration
Anti-convulsant Block excitatory DISTRIBUTION SHORT (4-8) Mental and
Hypnotics glutamate receptors From the brain to Pentobarbital psychomotor
splanchnic areas, impairment
skeletal muscle, adipose INTERMEDIATE (8-12)
tissues Amobarbital CONTRAINDICATION
Acute Intermittent
Readily crosses placenta LONG (12-24) Porphyria
and depress fetus Phenobarbital

METABOLISM
Liver
 EXCRETION
Inactive metabolites in
urine

Buspirone Mediated by Serotonin ONSET Headache

5-HT 1A receptors Slow onset of action Dizziness
Nervousness
Chronic treatment of Nausea
anxiety disorder Lightheadedness

NO anticonvulsant and
muscle relaxant

Zolpidem Binds to GABA A ABSORPTION Headache

receptors Rapid after oral Dizziness
Anterograde amnesia
Short-term treatment ONSET
of insomnia Rapid
Half-life 2-3 hrs
NO anticonvulsant and
muscle relaxant METABOLISM
Hepatic oxidation by
Effect: Lasts for 5 hrs CYP450 system