Others sedative hypnotics

Question 0

Zaleplon (Sonata)

Answer 0

Not benzos, bind BZ1 subtype. Dosage halved in women. Very high margin of safety. Recommended short term insomnia/often used chronically.

Question 1

Zolpidem (Ambien)

Answer 1

Not benzos, bind BZ1 subtype,(facilitates GABA mediated inhibition)
very short half life (XR available)
FDA dosage halved in women. Very high margin of safety. Caution w/history of drug/EtOh abuse. Recommended short term insomnia/often used chronically.

Question 2

Eszopiclone (Lunesta)

Answer 2

Less selective than Zolipidem/Zaleplon. Longer half life. W/d symptoms of CNS stimulation, axiety, seizures (abrupt cessation). Long term insomnia.

Question 3

Ramelteon (Rozerem)

Answer 3

Agonist at melatonin MT1/MT2. Regulates sleepiness/maintain circadian rhythms, shortens delay to sleep onset. Oral, extensive 1st pass in liver. Possible drug interactions due to metabolism (metabolized by CYP1A2 and/or CYP2C9). Caution in liver disease. Additive sedation w/EtOH and hypnotics. Rifampin increases metabolism. Metabolism inhibited by: ketoconazole, fluconazole, HIV protease, fluvoxamine.
Side effects: increase in serum prolactin concentrations and dec. in testosterone, may cause adrenocorticol insufficiency, little or no rebound insomina or wd, no effect REM sleep

Question 4

Buspirone (BuSpar)

Answer 4

Relieves anxiety w/o sedation, full effect takes 2 weeks to develop.
5-HT1a receptor partial agonist act esp on the hippocampus- decrease the release of Seratonin from the dorsal raphe neurons, increases activity of noradrengeric and dopaminergic pathways.
Oral, first pass by liver (drug interactions) and excreted by kidney.
Low abuse potential.
Does not potentiate CNS depression w/EtOH or benzos but will not prevent symptoms of w/d. Inc levels: ketoconazole, erythromycin. Red levels: rifampin. MAO inhibitor.
Used for generalized anxiety or with depression combined w/antidepressents.
Good for use in recovering addicts
Not good for severe anxiety and/or panic disorder

Question 5

Chloral Hydrate (Noctec)

Answer 5

Antihistimine
Used in kids for conscious sedation pre dental procedures for anxiety. Converted in body to trichlorethanol acts similar to barbs on GABAa. Low margin of safety, causes allergic response, gastric irritation, and may produce cardiac arrhythmia. High doses lead to respiratory and vasomotor depression.
Tolerance and dependence may offure- and long term use may cause liver damage and fatal intoxication. do not use with hepatic or renal impairment

Question 6

Diphenhydramine (Benadryl)

Answer 6

Occasional insomnia

Question 7

Kava

Answer 7

Herbal prep, OTC, unknown mechanism, FDA warning-severe liver toxicity, Do not use in pregnancy, used for mild anxiety.

Question 8

Valerian

Answer 8

Herbal, mild anxiolytic, combined in chamomile (sleepytime tea), may be hepatotoxic, do not use in pregnancy or w/liver disease, used for mild anxiety.

Question 9

B-antagonists (propanolol, etc.)

Answer 9

Used for performance anxiety (tremor, tachycardia, palpitations) and acute stress disorder. No effect on anxiety itself. Decrease autonomic responses to anxiety but have no effect on the anxiety itself