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Benzodiazepines
chemical category of drugs most frequently prescribed as sedative-hypnotic and anxiolytic drugs. anxiolytic used to reduce anxiety
mode of action
-depresses CNS activity at GABA receptors without inhibiting REM sleep or activating CYP450
indications
many: commonly used for sedation, relief of agitation, tx of depression, sleep induction, skeletal muscle relaxation, anxiety relief, & tx of seizure disorders, also alcohol withdrawal
contraindications
known allergies, narrow-angle glaucoma, and pregnancy
adverse effects
headache, drowsiness, paradoxical excitement/nervousness, dizziness/vertigo, cognitive impairment and lethargy, "hangover" sometimes reported, sometime palpitations, dry mouth, nausea, vomiting, kypokinesia, nightmares
toxicity/overdose
may result in: drowsiness, confusion, coma, diminished reflexes. OD of benzos alone rarely result in hyptotension or resp depression. lethal with other substances like alcohol and barbs
tx of OD supportive & symptomatic, like gastric lavage, activated charcoal. Flumazenil is benzo antidote & can acutely reduce sedative effect-only in excessive OD
antidote
Flumazenil(Romazicon) can be used to acutely reverse sedative effect. this normally done in extreme OD case. competes with benzos at the binding site. short half-life
interactions
lethal interactions when paired with other CNS depressants such as alcohol and opioids. herbal: kava and valerian, and grapefruit.
popular benzos
Diazepam(valium), Midazolam(versed), Temazepam(restoril),
nonbenzodiazepams
zaleplon(Sonata): hypnotic, zolpidem(Ambien) hypnotic, eszopiclone(Lunesta) hypnotic, ramelteon(Rozerem) hypnotic.