Pharmacologic:melatonin receptor agonist
Treatment of insomnia characterized by difficult sleep onset.
Activates melatonin receptors, which promotes maintenance of circadian rhythm, a part of the sleep-wake cycle. Therapeutic Effects: Easier onset of sleep.
Adverse Reactions/Side Effects
CNS: abnormal thinking, behavior changes, dizziness, fatigue, hallucinations, headache, insomnia (worsened), sleep driving. GI: nausea. Endo: ↑ prolactin levels, ↓ testosterone levels. Misc: ANGIOEDEMA.
PHYSICAL THERAPY IMPLICATIONS
Examination and Evaluation
Be alert for signs of angioedema, including rashes, raised patches of red or white skin (welts), burning/itching skin, swelling in the face, and difficulty breathing. Notify physician immediately of these signs.
Monitor daytime drowsiness, hallucinations, behavior changes, and “drugged” feelings. Repeated or excessive symptoms may require change in dose or medication.
Guard against falls and trauma (hip fractures, head injury, and so forth). Implement fall-prevention strategies, especially in older adults or if drowsiness and fatigue carry over into the daytime (See Appendix E).
Help patient explore non pharmacologic methods to improve sleep, such as relaxation techniques, regular exercise, avoid caffeine, and so forth.
Advise patient about the risk of daytime drowsiness and decreased attention and mental focus. Use care if driving or in other activities that require strong concentration.
Caution patient and family/caregivers that “sleepwalking” and other complex activities, including driving a car (sleep driving), may occur while completely asleep. Care should be taken to monitor such activities and prevent access to motor vehicles while under the influence of this drug.
Advise patient to avoid alcohol and other CNS depressants because of the increased risk of sedation and adverse effects.
Instruct patient and family/caregivers to report other troublesome side effects such as severe or prolonged headache, nausea, abnormal thoughts, worsening insomnia, or decreased libido (due to changes in prolactin or testosterone).
Absorption: Well absorbed (84%), but bioavailability is low (1.8%) due to extensive 1st-pass liver metabolism. Absorption in increased by a high-fat meal.
Distribution: Widely distributed to body tissues.
Metabolism and Excretion: Extensively metabolized by the liver; mainly by CYP1A2 enzyme system. Metabolites are excreted mostly in urine (88%); 4% excreted in feces.
TIME/ACTION PROFILE (blood levels)
|ROUTE ||ONSET ||PEAK ||DURATION |
|PO ||rapid ||30–90 min ||unknown |
Contraindicated in: Hypersensitivity; History of angioedema with previous use; Severe hepatic impairment; Concurrent use of fluvoxamine; OB: Lactation; Pedi: Safety not established.
Use Cautiously in: Depression or ...