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18 Cards in this Set

  • Front
  • Back

Benzodiazepines

Potentiate GABA


increase frequency of Cl channel opening


Have no GABA mimetic effect


Act through BZ receptors



BZ-1 receptor

Mediate sedation

BZ-2 receptor

mediate antianxiety and impairment of cognitive functions

Alprazolam

Anxiety, panic, phobias

Diazepam

Anxiety, preop sedation, muscle relaxation, withdrawal states

Lorazepam

Anxiety, preop sedation, status epilepticus (IV)

Midazolam

preop sedation, anesthesia IV

Temazepam

Sleep disorders

Oxazepam

Sleep disorders, anxiety

Pharmacokinetics

Liver metabolites

Outside The Liver

Oxazepam, Temazepam, and Lorazepam

Withdrawal signs of BZs

Rebound insomnia


Anxiety


Seizures when BZs were used as antiepileptic or in high doses

Barbiturates

Prolong GABA activity


Increase duration of Cl channel opening


Have GABA mimetic activity at high doses


Have their own binding site at GABA-A complex

Phenobarbital

Seizures

Withdrawal signs of Barbiturates and ethanol

Anxiety


Agitation


Life-threatening seizures

Drugs interactions GABA-A

Additive with other CNS depressants


anesthetics


antihistamines


opiates


B-blockers

Zolpidem and zaleplon

BZ-1 receptor agonists


Less effect on cognitive function (BZ-2)


Overdose reversed by flumazenil


Used in sleep disorders

Buspirone

No effect on GABA


5-HT1A partial agonist


Generalized anxiety disorders


Takes 1 to 2 weeks for effects