Names and pronunciation
(loe-FEX-i-deen) Lucemyra
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Drug reference
(loe-FEX-i-deen) Lucemyra
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Func. class.: Opioid withdrawal agent
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Chem. class.: Central alpha-2 agonist
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ACTION: A central alpha-2 agonist that binds to adrenergic receptors, resulting in a reduction in the release of norepinephrine and a decrease in sym- pathetic tone
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USES: For the mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults
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CONTRAINDICATIONS: Hyper- sensitivity Precautions: Abrupt discontinuation, acute MI, alcoholism, bradycardia, breastfeeding, cardiac dysrhythmias, CV disease, children, coadministration with other CNS depressants, coronary artery disease, dehydration, diabetes mellitus, dialysis, driving or operating machinery, electrolyte imbalance, ethanol ingestion, females, geriatric patients, heart failure, hepatic disease, hypertension, hypocal- cemia, hypomagnesemia, hypotension, infertility, long QT syndrome, malnutri- tion, poor metabolizers, pregnancy, renal disease, syncope, thyroid disease
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INTERACTIONS • Increase: QT prolongation—type IA, IC, III antidysrhythmics, antihistamines, anti depressants; monitor ECG if used concur rently • Increase: CNS effects and sedation— other CNS depressants; if used concur- rently, monitor for increased sedation • Increase: hypotension—antihyperten- sives; avoid concurrent use if possible • Increase: hypotension, bradycardia— CYP2D6 inhibitors
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DOSAGE AND ROUTES • Adult: PO Initially, 0.54 mg (3 × 0.18- mg tablets) 4× daily during peak with- drawal symptoms (first 5-7 days after last use of opioid), with dosing based on opiate withdrawal symptoms and tolera- bility; may use up to 14 days. Space dos- ing 5-6 hr apart; max 0.72 mg (4 tabs) as a single dose; max 2.88 mg (16 tabs) per day. To discontinue, gradually taper dose over 2-4 days to reduce drug withdrawal symptoms (reduce by 1 tab per dose ev- L ery 1-2 days)
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Available forms: Tabs 0.18 mg
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Administer: • May administer orally without regard to meals
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Assess: • QT prolongation: Monitor ECG in heart failure, bradyarrhythmias, liver or kidney impairment, or during concurrent use of other medications that lead to QT prolon gation • Electrolyte imbalances (hypokalemia, hypomagnesemia) should be corrected before use; monitor electrolytes for changes • Somnolence and sedation may cause impairment of cognitive and motor skills; may be increased when coadministered with other CNS depressants (benzodiaz- epines, ethanol, and barbiturates) • Abrupt discontinuation: monitor B/P during tapering; a significant increase in B/P may occur with abrupt discontinua- tion. May also cause diarrhea, insomnia, anxiety, chills, hyperhidrosis, and ex- tremity pain • Hepatic disease: may reduce drug clearance. Dosage reductions are recom mended based on degree of hepatic im pairment • Renal impairment: may reduce drug clearance. Dosage reductions may be needed based on degree of renal impair ment, including renal failure (end-stage renal disease, patients on dialysis); may be used without regard to timing of dialysis • Geriatric patients: caution is recom- mended when administering to patients over age 65. Dose adjustments may be needed • Fertility: infertility has been noted in some animal studies • Pregnancy/breastfeeding: safety not established. Consider the benefits of breastfeeding, the risk of potential in- fant drug exposure, and the risk of an untreated or inadequately treated condition Teach patient/family • About self-monitoring for hypotension, bradycardia, and related symptoms; that moving from a supine to upright position may increase the risk for hypotension or orthostatic effects • To stay hydrated; to recognize symp- toms of hypotension; if hypotension oc- curs, to sit or lie down; to carefully rise from a sitting or lying position • To withhold doses when experiencing hypotension or bradycardia and to con- tact health care provider for guidance on dose adjustments • To use caution or avoid performing activities that require mental alertness, such as driving or operating machinery, until effect of product is known • Not to discontinue without consulting health care provider, taper • To inform health care provider of other medications being taken, including ethanol ingestion • That patients who complete opioid dis- continuation are at an increased risk of fatal overdose should they resume opioid use
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CLINICAL CONSIDERATIONS
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PHARMACOKINETICS Protein binding 55%, 30% of dose is converted to inactive metabolites during first-pass metabolism by CYP2D6, CYP1A2, and CYP2C19, excretion kidney 15%-20%, half-life 17-22 hr after repeated dosing, peak 3-5 hr
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• Adult: PO Initially, 0.54 mg (3 × 0.18- mg tablets) 4× daily during peak with- drawal symptoms (first 5-7 days after last use of opioid), with dosing based on opiate withdrawal symptoms and tolera- bility; may use up to 14 days. Space dos- ing 5-6 hr apart; max 0.72 mg (4 tabs) as a single dose; max 2.88 mg (16 tabs) per day. To discontinue, gradually taper dose over 2-4 days to reduce drug withdrawal symptoms (reduce by 1 tab per dose ev- L ery 1-2 days)
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