Hypnotic Sedatives

Question 1

Sedative binding at allosteric site of the GABA-A receptor POTENTIATING GABA

Answer 1

Benzodiazepine

Question 2

Ion channel of GABA A receptor causing less excitation and hyperpolarization

Answer 2

Chloride

Question 3

Benzodiazepines effect promote hyperpolarization of chloride channels by

Answer 3

Increasing frequency of opening

Question 4

Causes sedation, decrease in anxiety, calming effect, hypnosis and drowsiness

Answer 4

Benzodiazepine

Question 5

Benzodiazepines are metabolized in the

Answer 5

liver

Question 6

Short acting benzodiazepines (4)

Answer 6

Oxazepam
Trazolam
Alprazolam
Midazolam

Question 7

Forms active metabolites increasing risk of toxicity for elderly and those with liver disease
t 1/2 100

2 drugs

Answer 7

Long acting benzodiazepams

Diazepam
Chlordiazepoxide

Question 8

Has self tapering effect for alcohol withdrawal hence first line

Answer 8

Long acting Benzodiazepine

Question 9

3 stages of withdrawal (alcohol)

Answer 9

8-12h after last dose: insomnia, tremulousness, anxiety, autonomic instability

12-48h : Seizure give BZD IV (status epilepticus, > 30 mins tonic/clonic) Diazepam or Lorazepam

48-96h : delirium tremens fever, agitation, disorientation

Question 10

For patients with alcohol withdrawal and concomittant liver failure

Answer 10

Oxazepam

Lorazepam

Question 11

Benzodiazepine treats (6)

Answer 11

1 Alcohol withdrawal
2 Anesthetic conscious sedation in minor operation
3 Insomnia (short term)
4 Parasomnia 
5 Central muscle relaxant - spasticity
6 Acute Anxiety

Question 12

BZD Adverse effects (2)

Answer 12

dose dependent effect on CNS impaired judgement drowsiness and central ataxia
Aterograde amnesia - conscious sedation

Question 13

bzd Contraindication (2)

Answer 13

1 do not give with other hypnotics (alcohol, barbiturates, narcoleptic, 1st gen antihistamine)
2 elderly

Question 14

Binds to GABA A receptor at an allosteric site but with shorter duration of action greater specificity, less anxiolysis and anti convulsant property

Answer 14

Zolpidem zaleplone eszopidone

Question 15

Short duration of action non-bzd used for difficulty falling asleep or sleep onset insomnia

Answer 15

Zolpidem

Zaleplone

Question 16

Used for sleep onset and maintenance insomnia longer half life 5-7 h

Answer 16

Eszopidone

Question 17

Antidote for non BZD hypnotics

Answer 17

Flumazenil

Question 18

Endogenous molecule by the brain regulating sleep cycle

Answer 18

Melatonin

Question 19

Melatonin receptor agonist maintaining circadian rhythm

Answer 19

Ramelteon

Tazamelteon

Question 20

Ramelteon and Tazamelteon MOA

Answer 20

agonist of MT1 and MT2 receptors at suprachiasmatic nucleus

Question 21

Advantage of using melatonin receptors (4)

Answer 21

No rebound insomnia
No effect on sleep architecture
No withdrawal sx
No dose adjustment in elderly

Question 22

Oldest antiseizure and sedative drug in critically ill

Answer 22

Barbiturates

Question 23

Barbiturates MOA

Answer 23

Prolongs duration of opening of Chloride channels leading to potentiation of GABA A

Question 24

ultra shortacting barbiturate for induction in intubation (<30 sec)
Lipid soluble
Crosses BBB

Answer 24

Thiopental

Question 25

Thiopental MOA

Answer 25

Rapidly acting due to redistribution to skeletal muscles and adipose

Question 26

Previous first line for seizure but benchmarked due to SE

1st line in neonates

Answer 26

Phenobarbital

Question 27

Phenobarbital SE (2)

Answer 27

1 hypotension

2 respiratory depression

Question 28

For seizure and essential tremors given together with propanlol

Answer 28

Primidone

Question 29

Barbiturates are inducers of

increase metabolism of (2)

Answer 29

CYP450

warfarin
statin