Module 13: Sedative Hypnotics, Barbs, Benzos

Question 1

main inhibitory NT in the CNS
-Allows Cl- ions to pass thru post synaptic neuron making neuron less responsive to excitation –> causing sedation

Answer 1

GABA

Question 2

1st prescribed benzo
thermally unstable
metabolized to Nordiazepam

Answer 2

Chlordiazepoxide

Question 3

Used in Benzo ODs

Answer 3

Flumazenil

Question 4

2 Analytical Challenges of Benzos

Answer 4

Polar, Thermally labile

Question 5

Major site of absorption for Barbs:

Answer 5

Small intestine

Question 6

Class of drugs with narrow therapeutic index (small diff btwn therapeutic and toxic)

Answer 6

Barbs

Question 7

_____ + urea –> barbituric acid + H2O

Answer 7

Malonic Acid

Question 8

Barb taken for migraines

Answer 8

Butalbital;

short-intermediate acting

Question 9

Barb used in animal euthanasia

Answer 9

Pentobarbital;

short acting

Question 10

Barb used to control seizures

Answer 10

Phenobarbital;

long acting;

therapeutic concentration: 15-40 mcg/mL

Question 11

Prodrug that is a structural analog of phenobarbital

Answer 11

Primidone

Question 12

Barb that is the target of most immunoassays

Answer 12

Secobarbital

Question 13

Increasing lipid solubility _______ the potency and _______ duration of activity.

Answer 13

Increase; decreases

Question 14

class of drugs that are weak acids, extensively metabolized in the liver, extract at pH of 5-7

Answer 14

Barbiturates

Question 15

Barbs are classified based on their:

Answer 15

duration of action

Question 16

One of the most important pharmacokinetic characteristics of barbiturates is their ability to:

Answer 16

Induce microsomal liver enzymes

(diminish drug action of other drugs that are metabolized by CYP450 enzymes)

Question 17

Barbs: Hydroxylation at the _____ constituent is a common metabolic route.

Answer 17

C5b

Question 18

Butalbital, amobarbital and pentobarbital have major ions at:

Answer 18

141 and 156

Question 19

True/false: Common oxybarbiturates have mass spectral similarities based on their constituents at the C5 position.

Answer 19

True

Question 20

Barbs: the major structural modification occurs at this position.

Answer 20

C5

Question 21

Death following barbiturate intoxication is often due to:

Answer 21

Respiratory failure

Question 21

The _______ barbiturates are used to induce surgical anesthesia:

Answer 21

Ultra-short acting

Question 22

Barbs: This is the major inhibitory neurotransmitter in the brain.

Answer 22

GABA

Question 23

True/False: Generally, benzodiazepines are highly protein bound.

Answer 23

True

Question 23

Diazepam –> Nordiazepam

Answer 23

Dealkylation

Question 24

True/False: Generally, benzodiazepines do not display a significant first-pass effect prior to distribution.

Answer 24

False - primarily metabolized in the liver

Question 25

Adjusting the pH to _______ allows extraction of benzodiazepines into an immiscible organic solvent.

Answer 25

9-10 (think slightly basic)

Question 26

For Benzos: Enzymatic hydrolysis is preferred over acidic hydrolysis because:

Answer 26

Some benzodiazepines are unstable in acid and rearrange to form benzophenones.

Question 27

Benzodiazepine especially effective in managing panic disorder.

Answer 27

Alprazolam

Question 28

Benzodiazepine used for the short term treatment of insomnia.

Answer 28

Temazepam

Question 29

True/False: Lorazepam glucuronide accumulates in plasma and attains concentrations greater than lorazepam.

Answer 29

True

Question 30

This benzodiazepine is relatively unstable in postmortem specimens due to bacterial and thermal degradation.

Answer 30

Clonazepam (think of how shitty it looks sometimes)

Question 31

Tolerance to the sedative effects of benzodiazepines develops usually within a _______ of the initiation of therapy.

Answer 31

Week

Question 32

This condition can significantly affect elimination of Benzos:

Answer 32

Renal Disease

Question 33

What is the shortest acting benzodiazepine including their active metabolites.

Answer 33

Triazolam

Question 34

Benzo effective in managing acute ethanol withdrawal.

Answer 34

Diazepam

Question 35

Enzyme involved in the metabolism of many benzodiazepines.

Answer 35

CYP3A4

Question 36

Benzodiazepines display _______ rather than generalized CNS depressant actions.

Answer 36

Selective

Question 37

Benzo that can be missed by several commercially available immunoassay screening tests.

Answer 37

Lorazepam

Question 38

The major binding protein for Benzos:

Answer 38

albumin

Question 39

Clonazepam undergoes ______ to form 7-Aminoclonazepam.

Answer 39

Reduction

Question 40

This drug is a derivative of imidazopyridine.

Answer 40

Zolpidem

Question 41

Zolpidem differs from benzodiazepine drugs because:

Answer 41

Zolpidem binds specifically to the GABAA receptor subtypes

Question 42

Glutethimide is structurally similar to this barbiturate.

Answer 42

Phenobarbital