Neuro - sedatives Flashcards
Barbiturates
Phenobarbital; Pentobarbital; Thiopental; Secobarbital
MOA of barbiturates
Facilitate GABA-A action by increasing duration of chloride channel opening; thus decreasing neuron firing; Contraindicated in porphyria; Used as a sedative for anxiety; seizures; insomnia; and induction of anesthesia (thiopental)
Side effects of barbiturates
Respiratory and cardiovascular depression (can be fatal); CNS depression (can be exacerbated by EtOH use); Dependence; Drug interactions (induces cytochrome P-450); Overdose treatment is supportive (assist respiration and maintain BP)
Benzodiazepines
Diazepam; Lorazepam; Triazolam Temazepam Oxazepam Midazolam Chlordiazepoxide Alprazolam
MOA of benzodiazepines
Facilitate GABA-A action by increasing frequency of chloride channel opening; Decrease REM sleep; Most have long half lives and active metabolites; Exceptions - triazolam; oxazepam; and midazolam are short acting - higher addictive potential; Used in anxiety; spasticity; status elipticus (lorazepam and diazepam); detoxification (especially alcohol withdrawal-DTs); night terrors; sleepwalking; general anesthetic (amnesia; muscle relaxation); hypnotic (insomnia)
Side effects of benzodiazepines
Dependence; Additive CNS depression effects with alcohol; Less risk of respiratory depression and coma than with barbiturates; Treat overdose with flumazenil (competitive antagonist at GABA benzodiazepine receptor)
ZolpidemZaleplonEszopiclone
Nonbenzodiazepine hypnoticsAct via the BZ1 subtype of the GABA receptorEffects reversed by flumazenilUsed to treat insomnia
Side effects of zolpidem; zaleplon; and eszopiclone
Ataxia; headaches; confusionShort duration because of rapid metabolism by liver enzymesUnlike older sedative-hypnotics; cause only modest day-after psychomotor depression and few amnestic effectsDecreased dependence risk than benzodiazepines
Inhaled anesthetics
HalothaneEnfluraneIsofluraneSevofluraneMethoxyflurane**Nitrous Oxide
Effects of inhaled anesthetics
Myocardial depressionRespiratory depressionNausea/emesisIncreased cerebral blood flow**Decreased cerebral metabolic demand
Side effects of halothane
Hepatotoxicity
Side effects of methoxyflurane
Nephrotoxicity
Side effects of enflurane
Proconvulsant
Side effects of nitrous oxide
Expansion of trapped gas in a body cavity
Malignant Hyperthermia
Rare; life-threatening hereditary condition in which inhaled anesthetics (except nitrous oxide) and succinylcholine induce fever and severe muscle contractions Treatment is dantrolene.