Sedatives and Anxiolytics

Question 1

What are the pharmacological features of Benzodiazepines?

Answer 1

Highly lipophilic --> well absorbed orally
Highly protein bound 
Hepatic metabolism 
Active metabolites - long acting 
Act of GABA receptors

Question 2

Name 2 short acting benzos

Answer 2

Lorazepam

Temazepam

Question 3

Name a long acting benzo

Answer 3

Diazepam

Question 4

What is the antidote for benzos?

Answer 4

Flumazenil

Question 5

Why must flumazenil be given more regularly than benzos?

Answer 5

Shorter half life

Question 6

What are the features of GABA receptors?

Answer 6

Pentameric arrangement with central ion channel pore
30 forms
Anaesthetics and benzos allosterically activate the receptor

Question 7

Which GABA subunit mediates sedation?

Answer 7

alpha-1

Question 8

Which GABA subunit mediates anxiolysis?

Answer 8

alpha-2

alpha-3

Question 9

What are Z drugs?

Answer 9

Drugs that act via benzodiazepine receptors, but are structurally different to benzos but have similar pharmacodynamic profile

Question 10

Name 3 Z-drugs

Answer 10

Zopiclone
Zaleplon
Zolpidem

Question 11

What is the mechanism of tolerance to benzos?

Answer 11

Desensitisation of GABA receptors

Sensitisation of excitatory NMDA receptors

Question 12

Describe the features of withdrawal from benzodiazepines

Answer 12

Anxiety
Depression 
Disturbed sleep
Pain, stiffness, muscular aches 
Convulsions

Question 13

What are the clinical uses of sedatives and anxiolytics?

Answer 13

Enable uncomfortable diagnostic and therapeutic procedures 
Acute alcohol withdrawal
Insomnia 
Generalised anxiety states 
Anticonvulsant

Question 14

What does the CAGE questionaire ask about?

Answer 14

Cut - have you ever though you should cut down your drinking?
Annoyed - have you ever been annoyed with other people criticising your drinking?
Guilty - have you ever felt guilty about drinking?
Eye-opener - have you ever taken alcohol in the morning to steady your nerves or ease a hangover?

Question 15

What are the symptoms of alcohol withdrawal?

Answer 15

Insomnia/ anxiety/ agitation
Tremor 
N/V
Sweating
Palpitations 
Hallucinations 
Seizures

Question 16

What investigations may suggest chronic alcohol consumption?

Answer 16

Raised MCV
Pancytopenia
Folate deficiency
Prolonged prothrombin time

Question 17

What is recommended therapy for acute anxiety?

Answer 17

Guided self help
Reduce caffeine, reduce alcohol
Mantras, mindfullness, worrytime app
CBT

Question 18

Where is melatonin produced?

Answer 18

Pineal gland

Question 19

When is melatonin produced?

Answer 19

High at night, low during day

Question 20

What triggers secretion of melatonin?

Answer 20

Input from retina

Question 21

What is sleep hygiene?

Answer 21

Practice that aims to make people more aware of behavioural, environmental and temporal factors that may be detrimental or beneficial to sleep

Question 22

What is prescribed as a last resort in insomnia?

Answer 22

Short acting benzo or z-drug

Question 23

Name a drug that can be used for anxiety

Answer 23

Pregabalin

Question 24

Describe the use of benzos in management of prolonged seizures

Answer 24

IV lorazepam

No access then rectal diazepam or intranasal midazolam

Question 25

Name a drug used for alcohol withdrawl

Answer 25

Librium (chlordiazepoxide)

Question 26

Why must you prescribe with caution in elderly people with insomnia?

Answer 26

Confusion
Falls
Slow metabolism

Question 27

What is melatonin prescribed for?

Answer 27

Sleep disturbance in children