Antianxiety Drugs

on 19.6.08 with 0 comments



Antianxiety Drugs

Benzodiazepines

  • increased intracellular influx of Cl-

  • amnesia

  • controlled substance schedual IV

  • Sedative, anticonvulsant, muscle relaxant, hypnotic, No antichol effects

  • Binds GABA receptor- leading to Cl- influx and neuron stabalization ( may effect 5-HT)

  • Rebound insomnia

  • Prod. Paranoid behavior

  • Daytime Hangover (greatest with shortest acting drugs)

  • Low toxicity, effects of alchohol and other drugs may be reinforced

Benzodiazepines

Diazepam (valium)

  • I.V sedation and amnesia dose is 2-20 mg

  • Indicated for antianxiety and muscle relaxation

  • Approved for tx for nocturnal bruxism

  • Long acting 20-50 hr T1/2


Triazolam

  • Shotest T1/2 (theraputic effect 3-4 hrs)

  • Increased dose causes increased memory lose and amnesia

  • Strongest rebound insomnia

Midazolam

  • I.V dose for pre-op 1-1.5 milligrams

  • Indications: amnesia, sedation, anti-anxiety

  • More potent than diazepam

  • Must lower narcotic doses to prevent respiratory depression


Lorazepam

  • Low water solubility

  • Short acting T1/2 = 10-18 hrs

  • Drug of choice for status epilepticus (diazepam also a standard)


  • contraindicated in narrow angle glaucoma

Buspirone (benzodiazepine deriv.)

(structurally similar to Halperidol)

  • Anxiolytic without sedation!

  • Partian 5HT1a agonist

  • Preferred for long term anxiety tx

  • Short T1/2

  • No anticholinergic effect


Flumazenil

  • Competitively aBlocks benzodiazepine-GABA receptor site

    • Used as an antidote


Category: Pharmacology Notes

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