A.24

Question 1

Non-benzodiazepine anxiolytics and non-benzodiazepine hypnotics

Answer 1

1. GABAA- R agonist (specific for α1 subunit of the receptor)/”z” drugs: Zolpidem, Zaleplon
2. Non GABAergic hypnotic: Ramelteon, Melatonin
3. Non GABAergic anxiolytic: Busiprone
4. SSRI

Question 2

paresthesia

Answer 2

burning sensation in hands and feet

Question 3

Zaleplon, Zolpidem

Answer 3

MOA: GABAA agonist→ ↑affinity to BDZ-Rs with α1 subunit;
IND: sleep disorders (especially sleep onset insomnia); Effect: Induces sleep (physiological pattern), but little effect on sleep maintenance, minimal anxiolytic, muscle relaxant and antiepileptic effect (non-BDZ!); Extra: zaleplon has 1h T1/2, overdose reversed by flumazenil;
SEs: CNS depression;
ROA: p.o

Question 4

Busiprone

Answer 4

MOA: non-GABAergic anxiolytic, 5HT1A partial agonist (agonist on its own, antagonist together with full agonist);
IND: Generalized anxiety disorders;
Effect: selective anxiolytic effect;
Extra: slow onset of anxiolytic effect (1-3 weeks)→ used in generalized anxiety, but not very effective in panic disorders;
SEs: GI distress, tachycardia, paresthesia;
ROA: p.o

Question 5

SSRI

Answer 5

Drugs: Fluoxetine, es(citalopram), Sertraline;
Effect: antidepressants;
IND: Depression, generalized anxiety disorder, chronic panic attacks, OCD, PTSD, Bulimia;
Extra: prescribed alone or in combination with low dose BDZs

Question 6

Melatonin, Ramelteon

Answer 6

MOA: non-GABAergic hypnotic, Ramelteon= MT1 + MT2 agonists;
Effect: melatonin Rs have important roles in the regulation of the sleep-wake cycle (suprachiasmatic nucleus), decrease time of sleep onset during chronic insomnia→ no rebound insomnia;
IND: disorders of the circadian rhythm (e.g. jetlag, insomnia etc.), difficulties falling asleep;
SEs: unusual dreams, fatigue, dizziness;
ROA: p.o