Antixiolytics, Sedatives, and Hypnotics

Question 1

Pentobarbital

Answer 1

Barbiturate, used for medically induced comas

Question 2

Sedative Anxiolytics

Answer 2

Calming or sedating with relief of anxiety, depress psychomotor and cognitive function.

Question 3

Weakly active, short lived metabolites

Answer 3

Alprazolam, triazolam, short duration

Question 4

Hypnotics

Answer 4

Promote drowsiness, onset, and maintenance of sleep. Increase stage 2 non REM, decrease REM and stage 4 non REM.

Question 5

Melatonin Receptor Agonist

Answer 5

Ramelteon, treats insomina with little effect on sleep architecture. No dependence or tolerance.

Question 6

Serotonin Receptor Agonist

Answer 6

Busiprone, Non sedating antixiolytic with delayed onset. No amnesia or muscle relaxation. 5HT1A (Autoreceptor) partial agonist. Decreases 5HT release.

Question 7

Benzodiazepine MoA

Answer 7

Binds to GABA Receptors and increases the frequency of opening of the Cl- channels.

Question 8

Non Linear CNS Depressants

Answer 8

Benzodiazepines, newer hypnotics

Question 9

Benzodiazepine Related Hypnotics

Answer 9

Ezopiclone, Zolpidem, Zaleplon. Selectively bind A1 subunits, rapid acting, short duration.

Question 10

Benzodiazepine Absorption

Answer 10

Oral, poor parenteral

Question 11

Inactive water soluble glucuronides

Answer 11

Rapidly metabolized, short duration. Lorazepam and Oxazepam. Age independent.

Question 12

Phenobarbital

Answer 12

Barbiturate, anticolvulsant

Question 13

A2 and A3 GABA Receptor subunit

Answer 13

Anxiolytic effects

Question 14

Miscellaneous Sedative Hypnotics

Answer 14

Propranolol (stage fright), Hydroxyzine, Diaphenhydramine, Ethanol, and Propofol.

Question 15

Thiopental

Answer 15

Barbiturate, anesthetic

Question 16

Long-lived and active metabolites

Answer 16

All other benzos

Question 17

Benzodiazepine Structure

Answer 17

Electronegative group at position 7

Question 18

Benzodiazepine Side Effects and Toxicity

Answer 18

Drowsiness and sedation, ataxia, respiratory suppression, Anterograde amnesia, tolerance, and dependence.

Question 19

A1 GABA Receptor subunit

Answer 19

Sedative effects

Question 20

Linear CNS Depressants

Answer 20

Barbiturates and Alcohol

Question 21

Barbiturates

Answer 21

Act on GABA Receptors, prolong Cl- channel opening, slow metabolism.

Question 22

Benzodiazepine Metabolism

Answer 22

Liver, CYP34 + glucuronidation

Question 23

Benzodiazepine Antagonist

Answer 23

Flumazenil, competitive inhibitor of GABA Receptor, short acting, IV