CNS depressants and sedatives Flashcards
what are the benzodiazepine sedative-hypnotic drugs?
- flurazepam
- temazepam
- triazolam
- midazolam
what are the benzodiazepine anxiolytic drugs?
- alprazolam
- clorazepate
- diazepam
- lorazepam
- oxazepam
what are the benzodiazepine-like (Z) drugs?
- zolpidem
2. eszopiclone
what is the serotonin agonist anxiolytic drug?
buspirone
what are the therapeutic uses for sedative-hypnotic drugs?
relief of anxiety and insomnia
which chemical moiety is responsible for the sedative-hypnotic effects of benzodiazepines?
electronegative substituent in the 7 position
where are benzodiazepines metabolized?
liver
what are the three metabolites of benzodiazepine metabolism? what are their half lives?
- inactive soluble glucuronides (3-hydroxy benzos) - short half life
- weakly active (triazolo benzos) - short half life
- long lived active (2-keto benzos) - long half life
which benzodiazepine metabolites are not influenced by age? which ARE influenced by age?
- not influenced by age - 3-hydroxy
2. influenced by age - 2-keto
what is the mechanism of action for benzodiazepines?
- potentiate effects of GABA at GABAa receptors
2. increase frequency of opening and conductance
what are the major adverse effects of benzodiazepines?
- respiratory depression
- tolerance
- anterograde amnesia
- dependence
- withdrawal
what is the function of flumazenil?
benzodiazepine antagonist
what is the mechanism of action of benzodiazepine antagonists?
compeititive inhibitor that binds to the BZ receptor - reverses effects of benzodiazepine
what is the clinical use for the benzodiazepine-like (Z) drugs?
insomnia
what are the barbiturate drugs?
- pentobarbital
- phenobarbital
- thiopental
what are the clinical uses for the barbiturates?
- anesthesia
- sedative hypnotic
- anticonvulsant
- medically induced coma
what is the mechanism of action for barbiturates?
increase duration of GABA-gated chloride channel opening
what type of drug is ramelteon? what is the clinical use?
- sedative
2. insomnia
what is the MOA of ramelteon?
melatonin receptor agonist
what type of drug is buspirone? what is the MOA?
- NON-sedating anxiolytic
2. partial agonist at 5HT1a (auto)receptors
what is the beta blocker sedative hypnotic?
propanolol
what are the antihistamine sedative hypnotics?
- hydroxyzine
2. diphenhydramine
flurazepam, temazepam, triazolam, midazolam are what type of drug? what is the MOA?
- benzodiazepine sedative-hypnotic drugs
2. potentiate effects of GABA at GABAa receptors and increase frequency of opening and conductance
alprazolam, clorazepate, diazepam, lorazepam, and oxazepam are what type of drug? what is the MOA?
- benzodiazepine anxiolytic drugs
2. potentiate effects of GABA at GABAa receptors and increase frequency of opening and conductance
