Hypnotics

Question 1

How many GABA receptors are there that hypnotics act on?

Answer 1

BZ1 BZ2 and BZ3

Question 2

Which GABA receptor is responsible for their sedative effects?

Answer 2

BZ1

Question 3

Which GABA receptor is responsible for myorelaxant and anticonvulsant effects?

Answer 3

BZ2

Question 4

Which GABA receptor is responsible for anxiolytic effects?

Answer 4

BZ3

Question 5

Which GABA receptor do Z-drugs primarily bind to?

Answer 5

BZ1

Question 6

How do benzos work?

Answer 6

enhance the effect of GABA
Positive allosteric modulators of the GABA-A receptor

activation of benzodiazepine receptors causes a conformational change to a central pore, allowing chloride ions to enter the neuron. The influx of the chloride anion results in hyperpolarization of the neuron, resulting in CNS depression
benzodiazepines increase the frequency of the GABA-A receptor Cl– channel opening in the presence of GABA. In the absence of GABA, benzodiazepines have no effects on GABA-A receptor function

Question 7

What are benzos divided into?

Answer 7

Hypnotics - short half life
Anxiolytics - long half life

Question 8

What makes up the structure of the benzodiazepine receptor?

Answer 8

Protein comprised of 5 transmembrane subunits (2 alpha, 2 beta and 1 gamma)

Question 9

What subunits form the binding site for GABA?

Answer 9

alpha and beta

Question 10

Which subunits form a binding site for benzos?

Answer 10

alpha and gamma

Question 11

How are most benzos metabolised?

Answer 11

Hepatic CYP3A4 and CYP2C19

Question 12

How is lorazepam metabolised?

Answer 12

direct glucuronidation without CYP450 metabolism

Question 13

What are side effects of benzos?

Answer 13

numbed emotions, confusion state, depression
drowsiness, reduced alertness, headache, dizziness
diplopia
muscle weakness
fatigue, ataxia

Question 14

What is the half life of diazepam?

Answer 14

20-100 hours

Question 15

What is the half life of clonazepam

Answer 15

18-50 hours

Question 16

What is the half life of chlordiazepoxide?

Answer 16

5-30 hours

Question 17

What is the half life of nitrazepam

Answer 17

15-38 hours

Question 18

What is the half life of temazepam

Answer 18

8-22 hours

Question 19

What is the half life of lorazepam

Answer 19

10-20 hours

Question 20

What is the half life of alprazolam

Answer 20

10-15 hours

Question 21

What is the half life of oxazepam

Answer 21

6-10 hours

Question 22

What is the half life of zopiclone

Answer 22

5-6 hours

Question 23

What is the half life of zolpidem

Answer 23

2 hours

Question 24

What is the half life of zaleplon

Answer 24

2 hours

Question 25

How should benzos be withdrawn?

Answer 25

reduce 5-10% every 2 weeks

Question 26

Which benzo produces a less severe withdrawl?

Answer 26

diazepam

Question 27

Give the equivalent doses to 1mg lorazepam: 1. Lormetazepam 2. Diazepam 3. Nitrazepam 4. Temazepam 5. Chlordiazepoxide 6. Oxazepam 7. Clonazepam

Answer 27

1. Lormetazepam 1mg 2. Diazepam 10mg 3. Nitrazepam 10mg 4. Temazepam 20mg 5. Chlordiazepoxide 25mg 6. Oxazepam 30mg 7. Clonazepam 0.5mg

Question 28

What are the physical features of benzo withdrawal?

Answer 28

Stiffness Weakness GI disturbance Paraesthesia Flu-like symptoms Visual disturbance

Question 29

What are the psychological features of benzo withdrawal?

Answer 29

Anxiety Insomnia Nightmares Depersonalisation Decreased memory and concentration Delusions and hallucinations Depression

Question 30

How do benzos affect chloride channels compared to barbiturates?

Answer 30

Benzos increase the frequency of chloride channels Barbiturates increase the duration of chloride channel opening

Question 31

What type of drug class if zopiclone?

Answer 31

cyclopyrrolone

Question 32

What are contraindications of zopiclone?

Answer 32

Unstable myasthenia gravis Respiratory failure Severe OSA

Question 33

iS ZOPICLONE safe in breastfeeding?

Answer 33

No as passes through the milk in high quantities

Question 34

What are side effects of zopiclone?

Answer 34

metallic taste heartburn lightening of sleep on withdrawal

Question 35

What are side effects of zolpidem?

Answer 35

drowsiness fatigue depression falls amnesia

Question 36

What receptors does melatonin work?

Answer 36

MT1 MT2 and MT3

Question 37

How does daridorexant work?

Answer 37

dual orexin receptor antagonist, acting on both orexin 1 and orexin 2 receptors and equipotent on both. The orexin neuropeptides act on orexin receptors to promote wakefulness

Question 38

Do orexin receptor antagonists alter the proportion of sleep stages?

Answer 38

no

Question 39

When are orexin receptor antagonists controindicated?

Answer 39

narcolepsy

Question 40

What are the side effects of orexin receptor antagonists?:

Answer 40

headache somnolence