GABAERGIC

AGENTS Drug

Class

Pharmacokinetics

Mechanism of Action

Clinical Uses and

General Information

Drawbacks and Side Effects

Diazepam

Benzodiazepine

Increases the frequency of

chloride channel openings by
GABA at GABAA receptor

Anxiolytic
Anticonvulsant
Sedative/hypnotic
Skeletal muscle relaxant
Anesthesia

Respiratory and cardiovascular

depression (can be lethal in
overdose)
Physiologic dependence
Tolerance

Phenobarbital

Barbiturate

Prolong the duration of chloride

channel openings by GABA
at GABAA receptor

Anticonvulsant
Sedative/hypnotic

Muscimol

GABA agonist

A: IM, IV, and PO; rapidly

absorbed from GI tract
B: Highly bound to plasma
proteins
D: Widely distributed; crosses
BBB
M: Hepatic metabolism
E: Metabolites excreted in urine
A: IM, IV and PO; rapidly
absorbed from GI
tract
D: Widely distributed; crosses
BBB
M: Hepatic metabolism; most
metabolite are
inactive
E: Metabolites excreted in urine
A: PO

Treatment of TD

Clinical use limited by

behavioral side effects

Baclofen

GABAB agonist

Opens chloride channel at

GABA
receptor
MOA is unknown; seems to
inhibit afferent pathways in
the spinal cord

Skeletal muscle relaxant

(through action in the CNS)
Less sedating than diazepam

Drowsiness
Increases seizures in patients
with epilepsy
Respiratory depression
Coma

A: Intrathecal and PO; rapidly

absorbed from GI tract
M: Slight degree of hepatic
metabolism
E: Majority excreted unchanged
in urine

DRUGS that ACT at the

NMDA RECEPTOR Drug

Pharmacokinetics

Mechanism of Action

Clinical Uses

Drawbacks and Side Effects

Ketamine

A: IV
D: Rapidly distributed; crosses BBB
M: Hepatic metabolism
E: In urine in feces
Not applicable

Antagonist of glutamic acid

Blocks the NMDA receptor cation
channel

Dissociative anesthetic
Side effects limit clinical use

Blocks the NMDA receptor cation

channel

Psychomimetic drug of abuse

Disorientation
Perceptual illusions
Flashbacks
Similar structure to PCP
Hallucinations
Nystagmus
Hypertension
Seizures

Phencyclidine