Neuro: Pharm - Anesthetics Flashcards
Barbiturates:
Phenobarbital, pentobarbital, thiopental, secobarbital
Barbiturates: MOA
Facilitate GABA A action by increasing duration of Cl- channel opening, thus decreasing neuron firing (barbidurates increases duration). Contraindicated in porphyria.
Barbiturates: Uses
Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)
Induction of anesthesia
thiopental
Barbiturates: Toxicity
Respiratory and cardiovascular depression (can be fatal); CNS depression (can be exacerbated by EtOH use); dependence; drug interactions (induces cytochrome P-450)
Overdose Tx of barbiturates:
supportive –> assist respiration and maintain BP
Benzodiazepines:
Diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam
Benzos: MOA
Facilitate GABA A action by increasing FREQUENCY of Cl- channel opening.
Most have long half lives and active metabolites
“Frenzodiazepines” increase frequency
Benzos, barbs, and EtOH all bind GABA A, which is a ligand-gated Cl- channel
Short acting Benzos:
alprazolam, triazolam, oxazepam, midazolam
ATOM
Benzos: uses
anxiety, spasticity, status epilepticus (lorazepam and diazepam), detoxification (especially alcohol withdrawal-DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)
Benzos: toxicity
dependence, additive CNS depression effects with alcohol. Less risk of respiratory depression and coma than with barbiturates
Tx benzo overdose with:
Flumazenil (competitive antagonist at GABA benzodiazepine receptor)
Nonbenzodiazepine Hypnotics:
Zolpidem (Ambien), Zaleplon, esZopiclone.
“All ZZZs put you to sleep”
Nonbenzo hypnotics: MOA
Act via BZ1 subtype of GABA receptor. Effects reversed by flumazenil
Nonbenzo hypnotics: uses
Insomnia
Nonbenzo hypnotics: toxicity
Ataxia, HA, confusion.
Short duration bc of rapid metabolism by liver enzymes. Unlike older sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects. Decrease dependence risk than benzodiazepines.
Inhaled anesthetics:
Halothane, enflurane, isoflurane, sevolfurane, methoxyflurane, nitrous oxide, desflurane
Inhaled anesthetics: MOA
unknown
Inhaled anesthetics: Effects
myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)
Inhaled anesthetics: toxicity
Hepatotoxicity (halothane), nephrotoxicity (methoxyflurane), proconvulsant (enflurane), expansion of trapped gas in a body cavity (nitrous oxide.
Can cause MALIGNANT HYPERTHERMIA
Malignant hyperthermia
rare, life-threatening hereditary condition in which inhaled anesthetics (except nitrous oxide) and succinylcholine induce fever and severe muscle contractions.
Tx: dantrolene
Dantrolene: MOA and use
Tx for malignant hyperthermia
Blocks ryanodine Receptor
IV Anesthetics: mnemonic
BBKing on Opioids PROPoses FOOLishly
Barbiturates, Benzos, Ketamine, Opioids, Propofol
Barbiturate for IV anesthetic:
Thiopental
Thiopental: MOA
high potency, high lipid solubility, rapid entry into brain
effect terminated by rapid redistribution into tissue (skeletal muscle) and fat
Decreases cerebral blood flow
“hangover effect” if injected multiple times