Pharmacology of Anxiety

Question 1

what are the most commonly used agents (Drug category) for most anxiety disorders

Answer 1

Antidepressants [SSRIs - SNRIs]

Question 2

______ drugs produce drowsiness and facilitate the onset and maintenance of sleep that resembles natural sleep and from which the recipient can be easily aroused

Answer 2

Hypnotic

Question 3

Dosages in the therapeutic range for both benzodiazepines and barbiturates produce what effects?

Answer 3

antianxiety,
anticonvulsant,
muscle relaxant,
sedative, and hypnotic effects

Question 4

Benzodiazepines ______ the effect of GABA, while barbiturates ______the effect of GABA (both actions requiring presence of GABA for this effect).

Answer 4

intensify,

prolong

Question 5

Barbiturate action is less selective and also depresses
___________ . With barbiturates, greater CNS depression and full surgical anesthesia can be obtained, thus they have a lower ________

Answer 5

excitatory neurotransmitters (glutamate),
safety margin.

Question 6

Benzodiazepines do not affect _________ as do other CNS depressants such as barbiturates and general anesthetics and thus are incapable of inducing and maintaining ________

Answer 6

excitatory neurotransmitters,

surgical anesthesia

Question 7

what are Zolpidem - eszopiclone - zaleplon? (Commonly referred to as “Z”-drugs.)

Answer 7

non-benzodiazepines that interact with the benzodiazepine binding site as agonists

Question 8

what is Flumazenil?

Answer 8

an antagonist at the benzodiazepine binding site, reverses the CNS effects of benzodiazepines

Question 9

GABA receptors with _______ subunits are highly expressed in the ______ and these receptors appear to mediate sedative (sleep), amnestic, and anticonvulsant actions of benzodiazepines

Answer 9

α1 ,

cortex

Question 10

GABA receptors with ______ subunits are highly expressed in the ________ and these receptors appear to mediate myorelaxant, motor impairing, anxiolytic, and ethanol-potentiating effects of benzodiazepines

Answer 10

α2/α5,

limbic system / and brain stem

Question 11

Z-drugs” (zolpidem, zaleplon, eszopiclone) are not benzodiazepines structurally and bind only to GABA-chloride channels with α1 subunits resulting in _______ without ________(reduced potential for dependence)

Answer 11

sleep ,

anxiolysis

Question 12

_______ is drug of choice for status epilepticus

Answer 12

Diazepam (or lorazepam)

Question 13

Symptoms are more severe in withdrawal from barbiturates, ethanol, and benzodiazepines with ________ half-lives

Answer 13

shorter

Question 14

Diazepam, alprazolam, and triazolam have ______ oral absorption

Answer 14

rapid

Question 15

Lorazepam has consistent and reliable ________-absorption

Answer 15

intramuscular

Question 16

As lipid-soluble drugs, benzodiazepines require biotransformation to more water-soluble metabolites, so t1/2 depends mainly on activity of ________.

Answer 16

drug metabolizing enzymes [CYP2C19, CYP3A4]

Question 17

Most benzodiazepines undergo CYP450 oxidations (phase I [N-dealkylation and aliphatic hydroxylation]) with subsequent inactivation via ________, then elimination in the urine

Answer 17

conjugation by glucuronidation (phase II)

Question 18

Lorazepam and oxazepam (and temazepam) are metabolized directly to the inactive glucuronides (NO P450 step) and as a result have shorter half-lives and fewer problems with cumulative and residual effects. Thus, they are good choices for use in the elderly with impaired ______ and in patients with _________

Answer 18

phase I metabolic pathways,

hepatic dysfunction

Question 19

Barbiturates are classic inducers of __________and represent a major source of clinically significant drug interactions that has contributed to their declining use

Answer 19

CYP450 enzymes

Question 20

Chronic use of ________ is strongly discouraged in the elderly

Answer 20

benzodiazepines

Question 21

__________ is major concern that limits use of benzodiazepines in chronic management of anxiety disorders

Answer 21

Potential for abuse

Question 22

Usual oral doses of benzodiazepines alone do not affect respiration or CVS function BUT they can exacerbate breathing problems in patients with _______ & __________

Answer 22

chronic pulmonary disease,

symptomatic sleep apnea

Question 23

: Flumazenil Reverses sedative effects of _______
and available for use in overdosage situations or to hasten recovery following surgical use.
•

Answer 23

benzodiazepines

Question 24

Flumazenil is not effective in _______ or _____toxicity - supportive treatment only for overdose of these agents

Answer 24

barbiturate,

ethanol

Question 25

Buspirone is an alternative as an anxiolytic it is not a benzodiazepine, but a _____partial agonist located presynaptically on nerve terminals

Answer 25

5HT1A