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38 Cards in this Set
- Front
- Back
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hypnosis?
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sleep
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coma?
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still have deep pain reflexes
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surgical anesthesia?
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no pain perception
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general CNS depressants?
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dose-dependent response;
barbiturates are the principal drugs |
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major advantage of benzodiazepines and related hypnotics?
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do not depress respiration (unless other CNS depressants are taken concomitantly)
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mechanism of action of barbiturates?
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bind GABA-A receptor in allosteric location to potentiate the action of GABA (influx of Cl- enhanced);
directly stimulate the receptor at high doses |
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thiopental?
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ultra-short acting barbiturate;
highly fat soluble; IV for surgery |
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pentobarbital?
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short-intermediate acting barbiturate;
metabolized by liver; used as hypnotic |
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secobarbital?
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short-intermediate acting barbiturate;
metabolized by liver; used as hypnotic |
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amobarbital?
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short-intermediate acting barbiturate;
metabolized by liver; used as hypnotic |
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phenobarbital?
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long-acting barbiturate;
renal excretion; antiseizure |
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barbiturate CNS effects?
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induce all levels of depression;
low therapeutic index; can increase the reaction to pain; induced tolerance and addiction |
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barbiturate PNS effects?
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depress autonomic ganglia (induce hypotension);
depress cholinergic transmission at NMJ |
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barbiturate respiration effects?
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neurogenic drive: reduced at hypnotic dose and abolished at 3x dose;
chemoreceptor/hypoxic drive: fail at 10x dose |
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barbiturate cardiovascular system effects?
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anesthesia: may cause hypotension in patients with CHF;
toxic doses: depression of cardiac conduction |
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barbiturate liver effects?
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induced P450 enzymes;
contraindicated in porphyria |
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barbiturate kidney effects?
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no direct effect;
renal failure secondary to CV collapse |
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toxicity of barbiturates?
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paradoxical excitement; pain (increases subjective perception); hypersensitivity (rare fatal exfoliative dermatitis after phenobarbital)
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drug interactions of barbiturates?
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other sedatives and drugs: compete for metabolism increasing depressant effects;
vit D, K anticoagulants and steroids: enhanced metabolism |
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chloral hydrate?
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non-barbiturate sedative-hypnotic;sedation in children for diagnostic and dental procedures
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paraldehyde?
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non-barbiturate sedative-hypnotic;
formerly used in alcohol withdrawl; characteristic disagreeable odor |
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ethchlorvinol?
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non-barbiturate sedative-hypnotic;
occasionally used as an anticonvulsant |
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meprobamate?
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non-barbiturate sedative-hypnotic;
high abuse potential; gastric bezoars due to indigestible filler in tablets; active metabolite of carisoprodol (soma) [OTC] |
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mechanism of benzodiazepines?
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enhance GABA-mediated chloride flux, thereby hyperpolarizing the postsynaptic membrane; DO NOT directly activate the receptor
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triazolam?
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short acting (<6h) benzodiazepine
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midazolam?
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short acting (<6h) benzodiazepine
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temazepam?
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intermediate acting (6h>T1/2>24h) benzodiazepine
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diazepam?
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long acting (>24h) benzodiazepine
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flurazepam?
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long acting (>24h) benzodiazepine
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chlordiazepoxide?
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long acting (>24h) benzodiazepine
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date rape drug?
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flunitrazepam (rohypnol)
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benzodiazepine CNS effects?
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depression up to coma but do not induce respiratory depression;
preanesthetic |
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toxicity of benzodiazepines?
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ataxia;
confusion, amnesia, imparied cognition; more common in geriatric; dependence, abuse issues; overdose taken alone is rarely fatal |
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zaleplon (sonata)?
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novel benzodiazepine-receptor agonist;hypnotic agent;
low tolerance, dependence; assumed to bind to subtype of GABA-A |
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zolpidem (ambien)?
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novel benzodiazepine-receptor agonist;
hypnotic agent; low tolerance, dependence; assumed to bind to subtype of GABA-A |
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eszopiclone (lunesta)?
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novel benzodiazepine-receptor agonist;
hypnotic agent; low tolerance, dependence; assumed to bind to subtype of GABA-A |
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flumazenil?
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benzodiazepine-receptor antagonist;
competitive antagonist; reverse sedative effects; rapid onset, short duration |
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drugs that alleviate anxiety symptoms?
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antihistamines, propranolol (stage fright), hydroxyzine, buspirone
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