7/26/2019 Gabaergic Agents Drug

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GABAERGIC

AGENTS Drug

Class Pharmacokinetics Mechanism of Action Clinical Uses an

General Information

Dra!"acks an Si

Dia#e$am Benzodiazepine A% IM& I'& an P() ra$il*

absorbed from GI tractB% Highly bound to plasmaproteinsD% Widely distributed; crossesBBBM% Hepatic metabolismE% Metabolites excreted in urine

Increases the frequency ofchloride channel openings by

GABA at GABAA receptor

AnxiolyticAnticonulsant

!edatie"hypnotic!#eletal muscle relaxant

Anesthesia

$espiratory and carddepression %can be le

oerdose&'hysiologic depende

(olerance

Pheno"ar"ital Barbiturate A% IM) I* and '+; rapidlyabsorbed from GItract

D% +iel* istri"ute) crosses

BBB

M% Hepatic metabolism; mostmetabolite are

inactieE% Metabolites excreted in urine

'rolong the duration of chloridechannel openings by GABAat GABAA receptor

Anticonulsant!edatie"hypnotic

Muscimol GABA,agonist A% P( +pens chloride channel atGABA

receptor

(reatment of (- .linical use limited behaioral side effec

Baclofen GABAB agonist A% Intrathecal and '+; rapidly

absorbed from GI tractM% !light degree of hepatic

metabolismE% Ma/ority excreted unchanged

in urine

M+A is un#no0n; seems to

inhibit afferent path0ays inthe spinal cord

!#eletal muscle relaxant

%through action in the .1!&2ess sedating than diazepam

-ro0siness

Increases seizures in0ith epilepsy

$espiratory depressi.oma

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DRUGS that ACT at the

NMDA RECEPT(R Drug

Pharmacokinetics Mechanism of Action Clinical Uses Dra!"acks an Sie Effects

,etamine A% I'

D% $apidly distributed; crosses BBBM% Hepatic metabolismE% In urine in feces

Antagonist of glutamic acidBloc#s the 1M-A receptor cation

channel

-issociatie anesthetic!ide effects limit clinical use

-isorientation'erceptual illusions

34lashbac#s5!imilar structure to '.'

Phenc*cliine 1ot applicable Bloc#s the 1M-A receptor cationchannel

'sychomimetic drug of abuse Hallucinations1ystagmus

Hypertension!eizures