CHAPTER 22 (WEEK 8) SEDATIVE HYPNOTIC DRUGS

Question 1

belong to a chemically
heterogeneous class of drugs, almost all causes
a dose-dependent CNS depressant effects

Answer 1

Sedative hypnotics

Question 2

produces drowsiness & encourage sleep & maintenance of state of sleep

Answer 2

Hypnosis

Question 3

relief of anxiety; calming effect

Answer 3

Sedative

Question 4

Widely used sedative-hypnotic

Answer 4

Benzodiazepines

Question 5

Substituent @ 7 positions (Halogen or Nitro group) is
required for a sedative-hypnotic effect

Answer 5

Benzodiazepines

Question 6

WHAT ARE THE SHORT-ACTING (T 1/2 < 5HRS) BENZODIAZEPINES?

Answer 6

Midazolam and Triazolam

Question 7

WHAT ARE THE INTERMEDIATE-ACTING (T 1/2 5-24 HRS) BENZODIAZEPINES?

Answer 7

Alprazolam, Clonazepam, Estazolam, Lorazepam, Oxazepam, Temazepam

Question 8

WHAT ARE THE LONG-ACTING (T 1/2 >24 HRS) BENZODIAZEPINES?

Answer 8

Chlordiazepoxide, Clorazepate, Diazepam, Flurazepam, Prazepam, Quazepam

Question 9

WHAT ARE THE NON-BZD?

Answer 9

Zolpidem, Zaleplon, Eszopiclone, Ramelteon & Tasimelteon, Suvorexant, Buspirone

Question 10

ULTRA-SHORT ACTING DOA: <3 hrs (BARBITURATES)

Answer 10

Thiopental

Question 11

INTERMEDIATE ACTING DOA: 3 -6 hrs (BARBITURATES)

Answer 11

Pentobarbital, Amobarbital, Secobarbital

Question 12

LONG-ACTING DOA: 10 -12 hrs (BARBITURATES)

Answer 12

Phenobarbital

Question 13

Most sedative-hypnotics are lipid-soluble & are absorbed well from the?

Answer 13

GIT

Question 14

What Barbiturates undergo hydroxylation?

Answer 14

Alprazolam & Triazolam

Question 15

What barbiturates undergo Extrahepatic conjugation

Answer 15

Lorazepam & Oxazepam

Question 16

Barbiturates are extensively metabolized Except for what drug?

Answer 16

Phenobarbital

Question 17

is oxidized to Trichloroethanol

Answer 17

Chloral hydrate

Question 18

Water-soluble metabolites are excreted mainly via?

Answer 18

Urine

Question 19

GABAA receptor-Cl- ion channel is composed of HOW many subunits?

Answer 19

5

Question 20

What subunit is used for SLEEP?

Answer 20

Alpha 1

Question 21

What subunit is used for anxiety?

Answer 21

Alpha 2/3

Question 22

binds between α1 & β2 subunits

Answer 22

GABA

Question 23

binds between α1 & γ2 subunits

Answer 23

Benzodiazepines

Question 24

Increases frequency of GABA-mediated chloride ion channel opening → Hyperpolarization → ↓ neuron firing

Answer 24

Benzodiazepines

Question 25

Antagonist at BZD receptor

Answer 25

Flumazenil

Question 26

Increases duration of GABA-mediated chloride ion channel opening → Hyperpolarization → ↓ neuron firing

Answer 26

Barbiturates

Question 27

Maternal use of this drug shortly before delivery is associated with floppy infant syndrome and also slightly increases oral cleft risk

Answer 27

Benzodiazepines