CNS Sedative Hypnotics

Question 1

What type of drug should produce drowsiness and should encourage and maintain a state of sleep?

Answer 1

Hypnotic Drug

Question 2

What are some clinical uses for Sedative Hypnotics?

Answer 2

relief of anxiety and insomnia
treatment of epilepsy
muscle relaxation

Question 3

What does the rate of absorption of sedative hypnotics depend on?

Answer 3

Lipophilicity

Question 4

T/F: Many phase I metabolites are pharmacologically active with relatively long half lives

Answer 4

True

Question 5

What is biodisposition of sedative hypnotics influenced by?

Answer 5

Hepatic function

Question 6

Is the elimination of half lives increased or decreased with older patients with altered hepatic function?

Answer 6

Increased

Question 7

What do BZD, Barbituates, and newer sedative hypnotics bind to?

Answer 7

GABA-A

Question 8

What is the benzodiazepine antagonist that triggers withdrawal and seizures in Pxs who are dependent on BZDs?

Answer 8

Flumazenil

Question 9

What is a major inhibitory neurotransmitter in the central nervous system?

Answer 9

GABA

Question 10

What increases the efficiency of GABAergic synaptic inhibition, enhances GABA’s effects, and only work in the presence of GABA?

Answer 10

Benzodiazepines

Question 11

What reduces anxiety, has sedative and hypnotic actions, anterograde amnesia, anticonvulsants, and acts as a muscle relaxant?

Answer 11

Benzodiazepines

Question 12

Are BZD lipophilic or lipophobic?

Answer 12

Lipophilic

Question 13

What increases the duration of the GABA-gated chloride channel openings and is a more pronounced central depressant? Bind to GABA-A receptor and stimulates Cl- influx by prolonging the duration of the opening of the ion channel

Answer 13

Barbiturates

Question 14

Why are Barbituates less selective in their actions than benzodiazepines?

Answer 14

they depress the actions of glutamic acid via binding to the AMPA receptor

Question 15

What makes Barbituates lethal?

Answer 15

endless amount of sedation

Question 16

What are the actions of Barbituates?

Answer 16

Depression of CNS and Respiratory system
Enzyme induction
Anesthesia
Anticonvulsant
Anxiety

Question 17

Which has a very narrow therapeutic index?

Answer 17

Barbituates

Question 18

Which has a very wide therapeutic index?

Answer 18

Benzodiazepines

Question 19

What is an adverse effect of Flumazenil?

Answer 19

Triggers withdrawal and seizures

Question 20

What drug is used for insomnia, binds to the BZ1 subtype of the GABA receptor, and strong sedative effects, and has rapid onset of action (lasts about 5 hours), but can cause Nightmares?

Answer 20

Zolpidem

Question 21

What drug is an oral nonbenzodiazepine hypnotic, treats insomnia for up to 6 months, has rapid absorption?

Answer 21

Eszopiclone

Question 22

What stimulates MT1 and MT2 receptors, promote and induce sleep, and maintain the circadian rhythm?

Answer 22

Melatonin

Question 23

What is used to treat insomnia in which falling asleep is the main complaint and is selective agonist at MT1 and MT2 melatonin receptors?

Answer 23

Ramelteon