Takeda; patent expires 2017.
Indicated for both transient and chronic insomnia. Approved for sleep initiation but not for sleep maintenance.
A melatonin receptor agonist, with high affinity for the melatonin receptor subtypes MT1 and MT2. It has no affinity for the GABA receptors.
Supplied as 8 mg orange-yellow tablets (breakable).
Start at 8 mg QHS for most patients. Elderly may require only half that dose. While higher doses than 8 mg are safe, the major company-sponsored study indicated that 16 mg is paradoxically less effective than 8 mg for patient with transient insomnia.
Appears to cause little in the way of next day fatigue or other impairment.
Abuse potential: One company-sponsored study showed that 14 patients with a history of drug abuse rated Rozerem as no more abusable than placebo.
Increases serum prolactin in women by an average of 34%.
Pregnancy Category C
Additive effect when combined with alcohol and other drugs or medications that have sedative effects.
Fluvoxamine, ketoconazole, and fluconazole increase Rozerem levels.
Rozerem does not affect levels of other drugs
Half life is somewhat confusing. While it is listed as “1-2.6 hours,” this refers only to the half-life of the parent drug. One if its metabolites, “M-II” is highly bioactive and has a half life of 2 to 5 hours. Thus, the overall half life may well be greater than 5 to 6 hours, depending on the individual. Since there is significant inter-individual variation in speed of metabolism, the duration of action will be very difficult to predict in a given patient.
No active metabolites. Metabolized in the liver by aldehyde oxidase.
Absorbed more slowly if taken after a meal.
Cut dose in half in hepatic insufficiency. No adjustments needed in renal impairment.
Major advantage is a lower abuse liability; Rozerem is the only hypnotic that is not classified as a controlled substance. Major disadvantages are its effects on increasing prolactin in women and possibly decreasing testosterone in men.