Sedative/Hypnotics & Barbituates Flashcards
Class of Flurazepam
Benzodiazepine Receptor Agonist
Class of Triazolam
Benzodiazepine Receptor Agonist
Class of Secobarbital
Barbiturate
Class of Zolpidem
Non-Benzodiazepine Benzodiazepine Receptor Agonist (Allosteric GABA-A agonist). GABAa receptor containing a1 subunit.
Class of Ramelteon
Melatonin Receptor Agonist
Halflife of Triazolam and what does this mean?
Ultrashort: 1.5 to 5 hours = Incidence of daytime drowsiness is low.
T/F: Triazolam has a residual anti-anxiety effect?
False
What can occur in a single night with Triazolam?
Rebound insomnia and REM rebound
Is incidence of of anterograde amnesia higher or lower with triazolam than with other hypnotics?
HIGHER
What are two major SE of triazolam?
Somnolence (14%) and Headache (10%)
Duration of action for flurazepam?
6-8 hr : Long acting
T/F: Flurazepam has a residual anti-anxiety effect
True
T/F: The tolerance to flurazepam is SLOW to develop?
True: (2 weeks)- but not recommended for daily long term usage
Because of the long duration of flurazepam, what side effect may it have?
Interfere with daytime wakefullness
Most common side effects of Zolpidem?
Drowsiness, drugged feeling, dizziness. Increasing reports of somnambulism, sleep eating, sleep driving, etc.
Why might you use ramelteon?
Quick acting, No rebound insomnia, with withdrawal, may work for circadian rhythm problems.
SE of Ramelteon:
Dizziness, somnolence, fatigue. Metabolized by CYP 1A2 (not with fluvoxamine).
MOA for Phenobarbital, secobarbital, and thiopental?
1) Bind to barbiturate binding site on GABA-A receptor.
2) Potentiate action of GABA (positive allosteric modulator) at normal doses.
3) At high concentrations barbiturates are direct GABA-A receptor agonists.
T/F: It is difficult to separate the sedative and hypnotic properties of barbiturates?
True- so they usually occur together.
Barbiturates strongly induce which enzymes?
Cytochrome P450: Leads to multiple drug reactions.
The therapeutic window for barbiturates is narrow/wide?
NARROW: 10x the normal therapeutic dose- overdose can be fatal.
What is a serious problem with barbiturates?
Physical dependence
