Anxiolytic Agents

Question 1

Serotonin agents stimulate anxiolysis via the 5HT receptors in the nucleus of __________.

Answer 1

Raphe

Question 2

Buspirone has what mechanism?

Answer 2

Agonist of the 5HT1A receptor; it is a weaker anxiolytic than GABA, but it has a fewer side effects; takes 2-4 weeks to become effective

Question 3

True or false: benzodiazepines cannot produce anesthesia.

Answer 3

True… just conscious sedation

Question 4

Why do benzodiazepines produce anterograde amnesia?

Answer 4

Because they decrease the release of glutamate, and glutamate is the neurotransmitter used by memory-forming neurons

Question 5

True or false: GABA is needed for benzodiazepines to work.

Answer 5

True

Question 6

True or false: flumazenil can be used for barbiturate overdose.

Answer 6

False. Although flumazenil antagonizes the GABA-A channel, it does so at a different site than barbiturates and alcohol. It can treat overdose with Z drugs.

Question 7

Benzodiazepines cause the GABA channel to open _____________, while barbiturates and alcohol cause GABA channels to open _____________.

Answer 7

more frequently; for longer

Question 8

True or false: the “z” drugs (eszopiclone, zolpidem, zaleplon) cannot treat seizures.

Answer 8

True. While they can in theory, they put people to sleep first and are thus not an effective anticonvulsant.

Question 9

Benzodiazepines are typically dangerous only when ____________________.

Answer 9

combined with ethanol or barbiturates

Question 10

True or false: benzodiazepines are potent inducers of CYP450.

Answer 10

False. But they are metabolized by CYP450, so use caution in patients who might have upregulated or inhibited CYP450.

Question 11

Inhalational anesthetics also work by _______________.

Answer 11

potentiating GABA receptors

Question 12

True or false: the benzodiazepines and “Z” drugs bind the same subunit of GABA.

Answer 12

True –the alpha-1 subunit; but the benzodiazepines also bind the other subunits, while the Z drugs do not.

Question 13

The -zepams are conjugated where?

Answer 13

Extrahepatically! The -olams, however, are not: think -OLam = Old Liver.

Question 14

True or false: benzodiazepines cause retrograde amnesia.

Answer 14

False. They cause anterograde amnesia.

Question 15

What side effects should you monitor in a patient taking buspirone?

Answer 15

Extrapyramidal side effects –it has some D2 blocking ability.