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14 Cards in this Set
- Front
- Back
Therapeutic effects of benzodiazepines
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1) anxiolytic effect
2) sedative/hypnotic effect 3) anticonvulsant effect 4) muscle relaxant |
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MOA of benzodiazepines
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-enhances the effects of the inhibitory neurotransmitter
GABA -causes Cl- channels to open and influx of cl- which hyperpolarizes the cell and decreases neuornal firing |
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side effects of benzodiazepines
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1) sedation, drowsiness and lightheadedness
2) mental clouding, confusion, psychomotor impairment, slurred speech, ataxia 3) memory impairment-anterograde amnesia 4) dishinhibition of supressed behavior 5)euphoria 6) hangover effect 7) rebound anxiety 8) re spiratory depression 9) tolerance 10) dependence 11) teratogenicity |
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what types of drugs cause rebound anxiety
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short acting benzos such as triazolam (halcion)
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what types of benzos might have a problem os respiratory depression?
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drugs used for surgical anesthesia such as midazolam ( versed)
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effects of benzos on sleep
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1) decreased sleep latency
2) decreased duration of stages 3 and 4 3) decreased number of awakenings 4) decrease in duration of REM sleep 5) INCREASED duration of stage 2 non-REM sleep 6) possible rebound increased in REM sleep following abrupt d/c of drug |
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uses of benzos
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1) txt of anxiety
2) sedative-hypnotic effects 3) txt of alcohol withdrawal 4) txt of convulsive seizures and status epileptics 5) relief of skeletal muscle spasm and spasticity 6) preanesthetic medication of supplement 7) induction of anesthesia |
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drug interactions with benzos
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1) additive to alcohol and other cns depressants
2) cimetidine, disulfuiram, isoniazide, inhibit oxidative metabolism and prolong life ( except lorazepam and oxazepam) 3) cross tolerance and cross dependence with alcohol 4) others |
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metabolism of benzos
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most drugs oxidized by the liver ( except lorazepam and oxazepam)
some form active metabolites that have longer durations generally do not induce other drug metabolizing enzymes |
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buspirone
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mild- moderate anxiety
partial agonist at 5ht-1a receptors no cross tolerance no immeadiate therapeutic effects drug of choice for txt of ANXIETY sedative or alcohol abuse who have been through withdrawal phase minimal sedative-hypnotic,musce relaxant, or respiratory depression |
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barbiturate poisoning
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may involve severe severe cns depression
txt is symptomatic, No ANTEDOTE |
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z-hypnotics
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non-benzo sedative- hypnotic
enhance effects of GABA less anxiolytic, relaxant, anticonvulsant activities metabolized in the liver zaleplon is short-acting zolpidem and eszopiclone are longer acting effects of cns depression less suppression of REM sleep and produce less rebound insomnia as benzos increase total sleep time and sleep latency |
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propofol
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iv
approved for continuous sedation in ICU when intubated and mechanically ventilated many adverse effects: hypotension, tremors, seizures. n/v |
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gammahydroxybutyrate (GHB)
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analog of GABA
ergogenic effect (improve athletic performance) and abused by athletes and now for cns effects ( sedation, euphoria, amnesia) "date rape" drug high dose associated with seizures, coma or death |