Names and pronunciation
(rah-mel′tee-on) Rozerem
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Drug reference
(rah-mel′tee-on) Rozerem
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Func. class.: Sedative/hypnotic, antianxiety
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Chem. class.: Melatonin receptor agonist
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Do not confuse: Rozerem/Razadine
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ACTION: Binds selectively to melatonin receptors (MT1, MT2); thought to be involved in circadian rhythms and in the normal sleep/wake cycle
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USES: Insomnia (difficulty with sleep onset)
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CONTRAINDICATIONS: Breast feeding, children, infants, hypersensitivity Precautions: Pregnancy, hepatic dis- ease, alcoholism, COPD, seizure disor- der, sleep apnea, suicidal ideation, angioedema, depression, sleep-related behaviors (sleepwalking), schizophre- nia, bipolar disorder; alcohol intoxica- tion, hepatic encephalopathy
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SIDE EFFECTS CNS: Dizziness, somnolence, fatigue, R headache, worsening insomnia, depres- sion, complex sleep-related reactions (sleep driving, sleep eating), suicidal thoughts/behaviors GI: Nausea, diarrhea, dysgeusia, vomiting SYST: Severe allergic reactions, angio edema
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INTERACTIONS • Possible toxicity: antiretroviral prote- ase inhibitors Increase: ramelteon effect, toxicity— alcohol; CYP1A2 inhibitors, azole antifungals (ketoconazole, fluconazole), fluvoxaMINE, anxiolytics, sedatives, hyp- notics, barbiturates, ciprofloxacin, strong CYP2C9 inhibitors, strong CYP3A4 inhibi- tors, opioids Decrease: effect of ramelteon—strong CYP inducer (rifAMPin) Drug/Food • Prolonged absorption, sleep onset re- duced: high-fat/heavy meal Drug/Lab Increase: protein level Decrease: testosterone level
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DOSAGE AND ROUTES • Adult: PO 8 mg within 30 min of bed- time Hepatic dose • Do not use with severe hepatic dis- ease; use with caution for mild to moder- ate hepatic disease
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Available forms: Tabs 8 mg
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Administer: • Within 30 min of bedtime for sleep- lessness; on empty stomach for fast onset, do not give within 1 hr of high-fat foods • Do not break, crush, chew tabs; swal- low whole • Store in tight container in cool envi- ronment
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Assess: • Severe hypersensitive reactions: as- sess for angioedema (facial swelling); product should be discontinued • Sleep characteristics: type of sleep problem: falling asleep, staying asleep; complex sleep disorders (sleep walking/ driving/eating) after taking product • Mental status: mood, sensorium, af- fect, memory (long, short term), suicidal ideation • LFTs: before treatment, periodically • Beers: avoid use in older adults with a high risk of delirium; delirium might be induced or worsened • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, may be fetal toxic; cautious use in breastfeeding, ex- cretion is unknown
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Evaluate: • Therapeutic response: ability to sleep at night, decreased amount of early morning awakening
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To avoid driving, other activities re- quiring alertness until product stabilized; drowsiness may continue the next day • To avoid alcohol ingestion, CNS de- pressants • About alternative measures to improve sleep: reading, exercise several hr before bedtime, warm bath, warm milk, TV, self- hypnosis, deep breathing • To report if pregnancy is planned or suspected; to avoid breastfeeding • To take product within 30 min before going to bed • Not to ingest a high-fat/heavy meal be- fore taking product • To report cessation of menses, galactor- rhea (women), decreased libido, infertility, worsening of insomnia, behavioral changes, severe allergic reactions, suicidal thoughts/ behaviors, if insomnia gets worse, swelling of face, tongue, trouble breathing • Med guide should be given to patient and reviewed
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PHARMACOKINETICS Absorbed rapidly; peak ½-1½ hr; protein binding 82%; rapid first-pass metabolism via liver by CYP1A2; 84% excreted in urine, 4% in feces; half-life 2-5 hr metabolite
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• Adult: PO 8 mg within 30 min of bed- time Hepatic dose
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