Hypnotics

Question 1

The major classes of neurotransmitters are

Answer 1

Small molecules gag gaa and histamine, serotonin and noradrenaline

Gaseous molecules
CO and NO

Neuropeptides
Endocannabinoids

Question 2

The major classes of neurotransmitters are

Answer 2

Small molecules gag gaa and histamine, serotonin and noradrenaline

Gaseous molecules
CO and NO

Neuropeptides
Endocannabinoids

Question 3

The actions of glutamate and aspartate include

Answer 3

Increased proteinase activity
Increased intracellular NO build up
Increased calcium build up and free radical

Question 4

The receptors which glutamate binds to include

Answer 4

NMDA
Kainate
AMPA ( a amino 3 hydroxy 5methyl 4isoxazolepropionic acid)

Question 5

Aspartate and glutamate are found majorly in …..

Answer 5

Cerebrum
Spinal cord
Cerebellum

Question 6

The major inhibitory neurotransmitters in the brain and spinal cords are ……. and ……. respectively

Answer 6

GABA
Glycine

Question 7

GABA is formed from ……….

Answer 7

Decarboxylation of glycine

Question 8

Barbiturates works on ………… receptors

Answer 8

Benzodiapine receptors BDZ

Question 9

The nomenclature of the benzodiazepine ring is……

Answer 9

A benzene ring fused to a 1,4 diazepine ring

Question 10

All clinically important benzodiazepine contains……… group

Answer 10

5 aryl substituent ring

Question 11

Benzodiazepines can be administered through ……….. routes

Answer 11

Enteral and paraenteral

Question 12

All orally administered benzodiazepine are …………… absorbed except

Answer 12

Completely absorbed except clorazepate

Question 13

Clorazepate is rapidly carboxylated to ………….. in the gastric juice

Answer 13

Nordazepam

Question 14

BZD are highly protein bound T/F

Answer 14

True

Question 15

Alprazolam is has ………. % of protein binding

Answer 15

70%

Question 16

Diazepam has ……… % of protein binding

Answer 16

99%

Question 17

BDZ are metabolised in the ………..

Answer 17

Liver

Question 18

The BDZ are metabolised first to their ……….. forms

Answer 18

Active

Question 19

The active forms of BDZ are cleared rapidly than their parent drugs T/F

Answer 19

False

Question 20

The back bone of barbiturates are

Answer 20

Barbiturates acid
Trioxohexahydropyrimidine

Question 21

The back bone of barbiturates are

Answer 21

Barbiturates acid
Trioxohexahydropyrimidine

Question 22

The two forms of barbiturates are and what makes them different

Answer 22

Oxabarbiturates O2 at position II
Thiobarbiturates O2 is replaced by sulfur

Question 23

Clinically active barbiturates contains ……….. functional group

Answer 23

5 alkyl or aryl group

Question 24

Contrast Thiobarbiturates and oxabarbiturates

Answer 24

Thiobarbiturates are more lipophillic due to the substitution

Easily absorbed
Early onset of action
Increase hypnotic potency
But quick degradation which leads to a lesser duration of action.

Question 25

Barbiturates are usually administered through ………. route

Answer 25

Orally

Question 26

Barbiturates can be administered through ……….. and ……… routes

Answer 26

Oral and parenteral route

Question 27

Barbiturates readily cross the placenta and are secreted in breast milk with the exceptions of ….

Answer 27

Aprobarbital
Phenobarbital

Question 28

All barbiturates are completely metabolised in …………… and excreted in …………..

Answer 28

Liver and excreted in the kidney

Question 29

What is the peculiarity in the excretion of barbiturates

Answer 29

~Quater of phenobarbital and almost all the aprobarbital are excreted unchanged

Question 30

Rxn of metabolism of barbiturates in the liver include

Answer 30

C oxidation at C5
N hydroxylation
N dealkylation
N glycosylation
Desulfuration

Question 31

The three stages of metabolism of benzodiazepene are

Answer 31

Modification or removal of substituent
Alpha hydroxylation
Glucuronidation

Question 32

The first two stages of bzd metabolism results in active metabolites T/F

Answer 32

True