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31 Cards in this Set
- Front
- Back
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Muscimol
- selective agonist of GABA-A receptor - major psychoactive alkaloid present in many mushrooms of Amanita genus |
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Gaboxadol
- experimental sleep aid drug developed by Lundbeck and Merk |
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Bicuculline
- light-sensitive - competitive antagonist of GABA-A receptors - mimics epilepsy (since it blocks the inhibitory action of GABAreceptors) |
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Picrotoxin
- non-competitive antagonist for GABA-A receptors → channel blocker - stimulant and convulsant effects |
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Barbital
- 5,5-diethylbarbituric acid - discontinued as a sedative-hypnotic - interesting because of thebiological consequence of its low lipid/water partition coefficient - slowly eliminated, mostly intact, by the kidney |
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Phenobarbital
- 5-ethyl-5-phenylbarbituricacid - long-acting sedative and hypnotic - valuable anticonvulsant (especially in generalizedtonic-clonic and partial seizures) - metabolism to the p-hydroxy compoundfollowed by glucuronidation accounts for about 90% of adose |
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Mephobarbital
- 3-methyl-5-ethyl-5-phenylbarbituric acid - metabolically N-dealkylatedto phenobarbital (accounts for almost all activity) - mainly anticonvulsant |
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Amobarbital
- sedative-hypnotic and analgesicproperties. |
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Butabarbital
- useful for certain applications such as treatingsevere insomnia and relieving anxiety before surgical procedures |
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Secobarbital
- anaesthetic - anticonvulsant - sedative - hypnotic |
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Pentobarbital
- treatment of seizures andpreoperative (and other) sedation - short-termhypnotic |
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Glutethimide
- one of the most active non-barbituratehypnotics - low aqueous solubility → dissolution and absorption from the GI track is somewhaterratic - undergoes extensiveoxidative metabolism - half life = 10 hours - racemic mixture |
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Ethchlorvynol
- mild sedative-hypnotic with a quickonset and short duration of action - t1/2 = 5.6 hours - extensively metabolized to itssecondary alcohol - inducesmicrosomal hepatic enzymes |
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Meprobamate
- officially indicated as an antianxiety agent - sedative-hypnotic agentcentrally acting - skeletal muscle relaxant |
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Carisoprodol
- mono-N-isopropyl-substituted relative ofmeprobamate - indicated in acute skeletomuscular conditionscharacterized by pain, stiffness, and spasm - major side effect of the drug = drowsiness |
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Chlorphenesin Carbamate
- the p-chloro substituted and 1-carbamate derivative of the lead compound in the development of thisgroup of agents, mephenesin |
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Chloral Hydrate
- aldehyde hydrate stableenough to be isolated - quickly converted to trichloroethanol (generally assumed to account for almost all of the hypnoticeffect) - GI upsetcommonly occurs for the drug ifundiluted or taken on an emptystomach |
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Paraldehyde
- liquidwith a strong characteristic odor detectable inthe expired air and an unpleasant taste → use almost exclusively to aninstitutional setting |
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Chlordiazepoxide
- indicated for the short term (2–4 weeks) treatment of anxiety - treatment for the management of acute alcohol withdrawal syndrome - well absorbed after oral administration - peak plasma levels are reached in 2 to 4 hours - half-life = 6-30 hours |
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Diazepam
- very lipophilic → rapidly and completely absorbed after oraladministration - anticonvulsant - premedication in anesthesiology - various spastic disorders |
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Oxazepam
- activemetabolite of both chlordiazepoxideand diazepam - prototype for the 3-hydroxybenzodiazepines - short-acting anxiolytic |
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Lorazepam
- 2′-chloro derivative ofoxazepam - the 2′-chloro substituent increases activity - metabolism is relatively rapid anduncomplicated because of the 3-hydroxyl group inthe compound - half life = 2-6 hours |
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Prazepam
- long overall half-life - extensive N-dealkylation occurs to yield activenordazepam - 3-Hydroxylation of both prazepamand nordazepam occurs - short term treatment of anxiety |
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Flurazepam
- insomnia - metabolism of the dialkylaminoalkyl side chain is extensive - major metabolite is N-dealkyl flurazepam, which has a very long half-life and persists for several days after administration → excessive sedation - half-life = 7 hours |
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Quazepam
- relatively selective for the benzodiazepine modulatory site on GABA-A receptors with α1 subunit and are hypnotic agents - metabolized by oxidation to the 2-oxo compound and then N-dealkylation - half-life = 39 hours |
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Clorazepate Dipotassium
- becomes Nordazepam - quick onset - overall long half-life - polar - similar to chlordiazepoxide and diazepam
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Nordazepam
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Alprazolam
- rapidly absorbed from the GItract - protein binding is lower (∽70%) than with mostbenzodiazepines because of its lower lipophilicity - duration ofaction is short - highly potent anxiolytic on amilligram basis |
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Triazolam
- ultrashort-actinghypnotic because it is rapidly α-hydroxylatedto the 1-methyl alcohol - sleep inducer (especially in elderly patients because itcauses less daytime sedation) - metabolicallyinactivated primarily by hepatic and intestinal CYP3A4 - coadministration with grapefruit juice increasesits peak plasma concentration by 30% leading toincreased drowsiness |
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Zolpidem
- high selectivity for the α1 subunit of benzodiazepinebinding site on GABAA receptor complex - rapid onset of action of 1.6 hours and good bioavailability (72%) - lipophilic - short elimination half-life - aryl methyl groups is extensivelyα-hydroxylated to inactive metabolites by CYP3A4 - metabolites are inactive, short-lived, and eliminated in the urine - half-lifein the elderly or the patients with liver disease is increased (modified in patients with hepatic insufficiency) -preferred for sleep maintenance |
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Eszopiclone
- aka Zopiclone - "superagonist" - racemix mixture - less selective for the α1 subunit of GABAAreceptor - relativelylonger elimination half-life (∽6 hours) than zolpidem - maybe used for patients who tend to awaken during the night |
