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INTRODUCTION

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ramelteon (ra-mel-tee-on)

Rozerem

Classification

Therapeutic: sedative/hypnotics

Pharmacologic:melatonin receptor agonist

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Indications
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Treatment of insomnia characterized by difficult sleep onset.

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Action
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Activates melatonin receptors, which promotes maintenance of circadian rhythm, a part of the sleep-wake cycle. Therapeutic Effects: Easier onset of sleep.

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Adverse Reactions/Side Effects
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CNS: abnormal thinking, behavior changes, dizziness, fatigue, hallucinations, headache, insomnia (worsened), sleep driving. GI: nausea. Endo: ↑ prolactin levels, ↓ testosterone levels. Misc: ANGIOEDEMA.

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PHYSICAL THERAPY IMPLICATIONS

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Examination and Evaluation
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  • 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.

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Interventions
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  • 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.

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Patient/Client-Related Instruction
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  • 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).

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Pharmacokinetics
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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.

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Distribution: Widely distributed to body tissues.

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Metabolism and Excretion: Extensively metabolized by the liver; mainly by CYP1A2 enzyme system. Metabolites are excreted mostly in urine (88%); 4% excreted in feces.

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Half-life: 1–2.6 hr.

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Table Graphic Jump Location
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TIME/ACTION PROFILE (blood levels)

ROUTE ONSET PEAK DURATION
PO rapid 30–90 min unknown

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Contraindications/Precautions
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Contraindicated in: Hypersensitivity; History of angioedema with previous use; Severe hepatic impairment; Concurrent use of fluvoxamine; OB: Lactation; Pedi: Safety not established.

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Use Cautiously in: Depression or history of suicidal ideation; Moderate hepatic impairment; Concurrent ...

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