Sedative and Hypnotic Drugs (Wolff) Flashcards
The following drugs make up what class?
1) alprazolam
2) clonazepam
3) diazepam
4) lorazepam
5) midazolam
6) temazepam
Benzodiazepines
eszopiclone and zolpidem are from what class of drugs?
Non-Benzodiazepine BZ1 agonists
flumazenil is from what class of drugs?
Benzodiazepine antagonist
The following drugs make up what class?
1) pentobarbital
2) phenobarbital
3) thiopental
Barbiturates
ramelteon is from what class of drugs?
Melatonin agonist
suvorexant is from what class of drugs?
Dual orexin receptor antagonist
doxepin is from what class of drugs?
Antihistamine
Why are Benzodiazepine widely distributed throughout the body (CNS, placenta, breast-milk)?
They are highly lipid soluble
What is MOA of benzodiazepines?
What effect does this have?
1) Facilitate GABA interactions with GABA(A) receptor which increases frequency of Cl- channel opening
2) Causes local hyperpolarization, meaning cell is less likely to fire
What is the most common side effect of benzodiazepines?
Drowsiness
What population are particular susceptible to side effects of Benzodiazepine?
What populations are resistant?
1) Elderly
2) Alcoholics and barbiturate drug abusers
While patients adapt quickly to the change in normal sleep patterns from benzodiazepines, what happens with abrupt discontinuation?
Rebound insomnia
What black box warning do benzodiazepines have?
Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death
Because benzodiazepines create a calming effect on the brain, how can the user appear?
Drunk
diazepam (Valium) is a major substrate of which CYP?
CYP3A4
What is the MOA of zolpidem (Ambien)
What does it act like?
1) Binds selectively to BZ1 receptors, a subgroup of GABA(A) receptors
2) Benzodiazepines
What is the clinical application for zolpidem?
Insomnia
What black box warning does zolpidem have?
Complex sleep behaviors including sleep-walking and sleep-driving
What is the MOA of flumazenil?
Antagonist at benzodiazepine-binding sites on the GABA(A) receptor
Flumazenil blocks the actions of?
1) Benzodiazepines
2) Zolpidem
What black box warning does flumazenil have?
Can cause seizures
Which barbiturate is used to control tonic-clonic seizures?
Phenobarbital
Which barbiturate was among those used as a sedative-hypnotic but was largely replaced by benzodiazepines in clinic?
Pentobarbital
Which barbiturate was used as intravenous sedatives/anesthetics but was largely replaced by propofol?
thiopental
