Ramelteon

INTRODUCTION

Indications

Treatment of insomnia characterized by difficult sleep onset.

Action

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.

Interventions

• 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.

Patient/Client-Related Instruction

• 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).

Pharmacokinetics

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.

Half-life: 1–2.6 hr.

Contraindications/Precautions

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 ...