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Properties of benzodiazepines ✔Correct Answer-Bind to gamma subunit of GABA(A) complex to
increase frequecy of Cl- channel opening; no GABAmimetic activity; BZ1 mediates sedation; BZ2
mediates antianxiety and impairment of cognitive functions
Benzodiazepine drugs ✔Correct Answer-Alprazolam, diazepam, lorazepam, midazolam,
temazepam, oxazepam
Uses of alprazolam ✔Correct Answer-Anxiety, phobias, panic attacks
Uses of diazepam ✔Correct Answer-Anxiety, preop sedation, muscle relaxation, withdrawal states
Uses of lorazepam ✔Correct Answer-Anxiety, preop sedation, status epilepticus
Uses of midazolam ✔Correct Answer-Preop sedation and anesthesia, anterograde amnesia
Uses of temazepam ✔Correct Answer-Sleep disorders
Uses of oxazepam ✔Correct Answer-Sleep disorder and anxiety
Pharmacokinetics of benzodiazepines ✔Correct Answer-Liver metabolized to active compounds
except oxazepam, temazepam, lorazepam; t1/2: diazepam > lorazepam > alprazolam > temazepam >
oxazepam > midazolam
Uses of barbiturates ✔Correct Answer-Phenobarbital for seizures; thiopental for induction of
anesthesia
Properties of barbiturates ✔Correct Answer-Prolong GABA activity; increase duration of Cl-
channel opening; GABAmimetic activity at high doses; bind to beta subunit of GABA(a) complex;
inhibit complex I of ETC
Pharmacokinetics of barbiturates ✔Correct Answer-General inducers of P450; contraindicated in
porphyrias
Withdrawal signs of benzodiazepines ✔Correct Answer-Rebound insomnia, anxiety, seizures
Withdrawal signs of barbiturates and ethanol ✔Correct Answer-Anxiety, agitation, life threatening
seizures
Drug interactions of GABAa drugs ✔Correct Answer-Life threatening respiratory depression if used
with other CNS depressants (antihistaminics, opiates, beta blockers); Barbiturates induce metabolism
of lipid-soluble drugs (oral contraceptives, carbamazepine, phenytoin, warfarin)
Flumazenil ✔Correct Answer-Benzodiazepine receptor antagonist. Used as antidote for
benzodiazepine overdose.
, Zolpidem ✔Correct Answer-BZ1 receptor agonist used in sleep disorders. No cognitive impairment
(no BZ2 actions), overdose reversed by flumazenil, less tolerance and abuse liability
Buspirone ✔Correct Answer-No effect on GABA, 5-HT1a partial agonist, used for generalized
anxiety, nonsedative, 1-2 weeks for effects
Effects of alcohols ✔Correct Answer-GABA mimetic activity causes CNS depression; metabolic
acidosis; fetal alcohol syndrome
Metabolism of ethylene glycol ✔Correct Answer-Ethylene glycol + alcohol DH --> glycoaldehyde +
aldehyde DH --> glycolic acid --> oxalic acid
Effects of ethylene glycol ✔Correct Answer-CNS depression, severe metabolic acidosis,
nephrotoxicity
Metabolism of methanol ✔Correct Answer-Methanol + alcohol DH --> formaldehyde + aldehyde
DH --> formic acid
Effects of methanol ✔Correct Answer-Respiratory failure, severe anion gap metabolic acidosis,
ocular damage
Treatment of alcohol overdose ✔Correct Answer-Fomepizole (alcohol DH inhibitor) and
hemodialisis
Metabolism of ethanol ✔Correct Answer-Ethanol + alcohol DH --> acetaldehyde + NADH +
acetaldehyde DH --> acetic acid + NADH
Effects of ethanol ✔Correct Answer-CNS depression, metabolic acidosis, acetaldehyde toxicity
Acetyldehyde toxicity ✔Correct Answer-Nausea, vomit, headache, hypotension, inactivates folate,
decreases availability of thiamine
Drugs that cause disulfram-like effects ✔Correct Answer-Disulfram-like effects = acetaldehyde
toxicity. Disulfram inhibits acetaldehyde DH. Metronidazole, cefamandole, cefoperazone, cefotetan,
chlorpropamide
Anticonvulsant drugs ✔Correct Answer-Phenytoin, carbamazepine, benzodiazepines, barbiturates,
lamotrigine, topiramate, felbamate, ethosuximide, valproic acid
Drugs used for partial seizures ✔Correct Answer-Valproic acid, phenytoin, carbamazepine
Drugs used for general tonic-clonic seizures ✔Correct Answer-Valproic acid, phenytoin,
carbamazepine
Drugs used for general absence seizures ✔Correct Answer-Ethosuximide
Drugs used for status epilepticus ✔Correct Answer-Lorazepam, diazepam, phenytoin
Phenytoin MOA ✔Correct Answer-Inhibits fast Na channels in axons which decreases conduction
and prevents seizure propagation