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Pharm 22 - Sedative-Hypnotics
Pharmacology of sedating and hypnotic drugs
54
Pharmacology
Professional
02/07/2012

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Term
Benzos bind to which receptor?
Definition
GABA-A
Term
Benzos facilitate...
Definition
GABA-mediated chloride ion channel opening
Term
What do Benzos do to the cell membrane?
Definition
enhance hyperpolarization
Term
What are the EFFECTS of benzos?
Definition
Dose-dependent depressant effects on CNS - sedation, relief of anxiety, amnesia, hypnosis, anesthesia, coma, respiratory depression
Term
What are the clinical applications for benzos?
Definition
acute anxiety states, panic attacks, GAD, insomnia and other sleep disorders, relaxation of skel muscle, anesthesia, seizures
Term
Metabolism of benzos? Tox? Interactions?
Definition
hepatic metab with some active metabolites, CNS depressant effects, dependence, additive CNS depression with ethanol and other drugs
Term
MOA of flumazenil?
Definition
Antagonist at benzo binding sites on GABA-A
Term
Name a benzodiazepine antagonist
Definition
flumazenil
Term
What are the EFFECTS of flumazenil?
Definition
blocks actions of benzos and zolpidem but not other sedative-hypnotics
Term
Which drug blocks the actions of benzos and zolpidem but not other sedative-hypnotics?
Definition
flumazenil
Term
Clinical applications for flumazenil?
Definition
benzo overdose
Term
Which drug is used in benzo overdose?
Definition
flumazenil
Term
How is flumazenil given? Half-life? Tox?
Definition
IV, short, agitation, confusion, possible withdrawal symptoms
Term
Which receptor do barbituates bind to? What do they do to the cell membrane?
Definition
GABA-A, hyperpolarize
Term
Is the dose-response relationship of barbituates steeper or shallower than the dose-response relationship of benzos?
Definition
steeper
Term
What are the clinical applications for barbs?
Definition
anesthesia (thiopental), insomnia (secobarbital), seizure disorders (phenobarbital)
Term
The half lives for benzos range from __ to __ hrs
Definition
2- 40 hrs
Term
The half lives for barbs range from __ to __ hrs
Definition
4 to 60 hrs
Term
Can barbituates be given orally? How are they metabolized? Which drug has 20% renal elimination?
Definition
yes, hepatically, phenobarbital
Term
What effect do barbs have on hepatic drug metabolizing enzymes?
Definition
induce them
Term
Name some newer hypnotics
Definition
eszopiclone, zaleplon, zolpidem
Term
eszopiclone, zaleplon, zolpidem - what category are these?
Definition
newer hypnotics
Term
What is the MOA of eszopiclone, zaleplon, zolpidem?
Definition
bind to subgroup of GABA-A recepts, acting like benzos to enhance membrane depolarization
Term
Which drugs bind to subgroup of GABA-A recepts, acting like benzos to enhance membrane depolarization
Definition
eszopiclone, zaleplon, zolpidem
Term
what are the EFFECTS of eszopiclone, zaleplon, zolpidem?
Definition
rapid onset of hypnosis, few amnestic effects or day-after psychomotor depression or somnolence
Term
Which drugs cause rapid onset of hypnosis, few amnestic effects or day-after psychomotor depression or somnolence?
Definition
eszopiclone, zaleplon, zolpidem
Term
Clinical applications for eszopiclone, zaleplon, zolpidem?
Definition
sleep disorders, especially those characterized by difficulty in falling asleep
Term
eszopiclone, zaleplon, zolpidem - half lives? Metabolized by what?
Definition
short half lives, CYP substrates
Term
What type of drug is ramelteon?
Definition
a melatonin receptor agonist
Term
name a melatonin receptor agonist
Definition
ramelteon
Term
what is the MOA of ramelteon?
Definition
activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS
Term
which drug activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS?
Definition
ramelteon
Term
EFFECTS of ramelteon?
Definition
rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms
Term
which drug produces rapid onset of sleep with minimal rebound insomnia or withdrawal symptoms?
Definition
ramelteon
Term
what are the clinical applications for ramelteon?
Definition
sleep disorders, especially those characterized by difficulty in falling asleep, not a controlled substance
Term
Which drug is used for sleep disorders, especially those characterized by difficulty in falling asleep, and is not a controlled substance?
Definition
ramelteon
Term
Ramelteon forms an active metabolite via ____
Definition
CYP1A2
Term
which drug forms an active metabolite via CYP1A2?
Definition
ramelteon
Term
Toxicity of ramelteon?
Definition
dizziness, fatigue, endocrine changes
Term
Which drug has toxicity that includes dizziness, fatigue, endocrine changes?
Definition
ramelteon
Term
Which drug inhibits the metabolism of ramelteon?
Definition
fluvoxamine
Term
fluvoxamine inhibits the metabolism of which drug?
Definition
ramelteon
Term
What is the MOA of buspirone?
Definition
uncertain, partial agonist at 5-HT receptors but affinity for D2 also possible
Term
which drug has an MOA that is uncertain, might be a partial agonist at 5-HT receptors but affinity for D2 also possible?
Definition
buspirone
Term
What are the EFFECTS of buspirone?
Definition
slow onset (1-2 wks) of anxiolytic effects, minimal psychomotor impairment, no additive CNS depression with other drugs
Term
Name the drug with the following effects: slow onset (1-2 wks) of anxiolytic effects, minimal psychomotor impairment, no additive CNS depression with other drugs
Definition
buspirone
Term
Clinical applications for buspirone?
Definition
generalized anxiety states
Term
Does buspirone form an active metabolite? Is the half life short or long?
Definition
yes, short
Term
Toxicity and interactions for buspirone?
Definition
tachy, paresthesias, GI distress. Interactions - CYP3A4 inducers/inhibitors
Term
Toxicity: tachy, paresthesias, GI distress. Interactions: CYP3A4 inducers/inhibitors. NAME THE DRUG.
Definition
buspirone
Term
What is the common mechanism by which sedative-hypnotics can cause death?
Definition
Depression of medullary and cardiovascular centers
Term
"Date rape drug"
Definition
Flunitrazepam (rohypnol)
Term
What is the most important sign of withdrawal from sedative-hypnotic drugs?
Definition
excessive CNS stimulation - seizures
Term
Treatment of withdrawal syndrome includes...
Definition
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
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