lofexidine (Rx)

Brand and Other Names:Lucemyra
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.18mg

Opioid Withdrawal

Indicated for mitigation of withdrawal symptoms to facilitate abrupt opioid discontinuation in adults; for short-term use (see Dosing Considerations)

Starting dose: Three 0.18-mg tablets (0.54 mg) PO QID (5-6 hr between doses) during the period of peak withdrawal symptoms (generally the first 5-7 days after last opioid use)

Not to exceed a total daily dose of 2.88 mg (16 tablets)

No single dose should exceed 0.72 mg (4 tablets)

Treatment may be continued for up to 14 days with dosing guided by symptoms

Dose should be reduced, held, or discontinued for individuals who demonstrate a greater sensitivity

Lower doses may be appropriate as opioid withdrawal symptoms wane

Discontinue by gradually reducing dose over a 2- to 4-day period to mitigate lofexidine withdrawal symptoms (eg, reducing by 1 tablet per dose every 1-2 days) (see Cautions)

Dosage Modifications

Hepatic impairment

  • Mild (Child-Pugh score 5-6): 3 tablets QID (2.16 mg/day)
  • Moderate (Child-Pugh score 7-9): 2 tablets QID (1.44 mg/day)
  • Severe (Child-Pugh score >9): 1 tablet QID (0.72 mg/day)

Renal impairment

  • Mild or moderate (eGFR 30-89.9 mL/min/1.73 m²): 2 tablets QID (1.44 mg/day)
  • Severe (eGFR <30 mL/min/1.73 m²), ESRD, or dialysis: 1 tablet QID (0.72 mg/day)
  • May be administered without regard to timing of dialysis

Dosing Considerations

While lofexidine may lessen the severity of withdrawal symptoms, it may not completely prevent them and is only approved for treatment for up to 14 days

Not a treatment for opioid use disorder (OUD), but can be used as part of a broader, long-term treatment plan for managing OUD

Safety and efficacy not established

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Interactions

Interaction Checker

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              Serious - Use Alternative (108)

              • acebutolol

                lofexidine, acebutolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • alfuzosin

                alfuzosin and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • alprostadil IV

                lofexidine, alprostadil IV. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • amiloride

                lofexidine, amiloride. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • amlodipine

                lofexidine, amlodipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • amyl nitrite

                lofexidine, amyl nitrite. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • apomorphine

                apomorphine and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • atenolol

                lofexidine, atenolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • azilsartan

                lofexidine, azilsartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • bedaquiline

                bedaquiline and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • benazepril

                lofexidine, benazepril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • bendroflumethiazide

                lofexidine, bendroflumethiazide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • betaxolol

                lofexidine, betaxolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • bisoprolol

                lofexidine, bisoprolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • bosentan

                lofexidine, bosentan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • bumetanide

                lofexidine, bumetanide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • calcium/magnesium/potassium/sodium oxybates

                lofexidine, calcium/magnesium/potassium/sodium oxybates. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • candesartan

                lofexidine, candesartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • captopril

                lofexidine, captopril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • carvedilol

                lofexidine, carvedilol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • ceritinib

                ceritinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • chlorothiazide

                lofexidine, chlorothiazide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • chlorthalidone

                lofexidine, chlorthalidone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • clarithromycin

                clarithromycin and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • clevidipine

                lofexidine, clevidipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • clonidine

                lofexidine, clonidine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • clozapine

                clozapine and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • crizotinib

                crizotinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • dasatinib

                dasatinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • degarelix

                degarelix and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • diltiazem

                lofexidine, diltiazem. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • enalapril

                lofexidine, enalapril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • entrectinib

                lofexidine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

              • eplerenone

                lofexidine, eplerenone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • epoprostenol

                lofexidine, epoprostenol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • eprosartan

                lofexidine, eprosartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • esmolol

                lofexidine, esmolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • ethacrynic acid

                lofexidine, ethacrynic acid. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • felodipine

                lofexidine, felodipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • fenoldopam

                lofexidine, fenoldopam. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • fexinidazole

                fexinidazole and lofexidine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.

              • fosinopril

                lofexidine, fosinopril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • furosemide

                lofexidine, furosemide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • glasdegib

                lofexidine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.

              • guanfacine

                lofexidine, guanfacine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • hydralazine

                lofexidine, hydralazine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • hydrochlorothiazide

                lofexidine, hydrochlorothiazide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • hydroxychloroquine sulfate

                hydroxychloroquine sulfate and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • iloprost

                lofexidine, iloprost. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • indapamide

                lofexidine, indapamide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • irbesartan

                lofexidine, irbesartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • isosorbide dinitrate

                lofexidine, isosorbide dinitrate. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • isosorbide mononitrate

                lofexidine, isosorbide mononitrate. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • isradipine

                lofexidine, isradipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • ivosidenib

                ivosidenib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of QTc prolonging drugs with ivosidenib or replace with alternate therapies. If coadministration of a QTc prolonging drug is unavoidable, monitor for increased risk of QTc interval prolongation.

              • labetalol

                lofexidine, labetalol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • lefamulin

                lefamulin and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.

              • lisinopril

                lofexidine, lisinopril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • losartan

                lofexidine, losartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • mecamylamine

                lofexidine, mecamylamine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • methyclothiazide

                lofexidine, methyclothiazide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • methyldopa

                lofexidine, methyldopa. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • metolazone

                lofexidine, metolazone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • metoprolol

                lofexidine, metoprolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • metyrosine

                lofexidine, metyrosine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • minoxidil

                lofexidine, minoxidil. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • mobocertinib

                mobocertinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

              • moexipril

                lofexidine, moexipril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nadolol

                lofexidine, nadolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nebivolol

                lofexidine, nebivolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nicardipine

                lofexidine, nicardipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nifedipine

                lofexidine, nifedipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nimodipine

                lofexidine, nimodipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nisoldipine

                lofexidine, nisoldipine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroglycerin IV

                lofexidine, nitroglycerin IV. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroglycerin PO

                lofexidine, nitroglycerin PO. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroglycerin sublingual

                lofexidine, nitroglycerin sublingual. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroglycerin topical

                lofexidine, nitroglycerin topical. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroglycerin transdermal

                lofexidine, nitroglycerin transdermal. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroglycerin translingual

                lofexidine, nitroglycerin translingual. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nitroprusside sodium

                lofexidine, nitroprusside sodium. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • nylidrin

                lofexidine, nylidrin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • olmesartan

                lofexidine, olmesartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • papaverine

                lofexidine, papaverine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • penbutolol

                lofexidine, penbutolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • perindopril

                lofexidine, perindopril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • phenoxybenzamine

                lofexidine, phenoxybenzamine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • phentolamine

                lofexidine, phentolamine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • pindolol

                lofexidine, pindolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • pitolisant

                lofexidine and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.

              • ponesimod

                ponesimod, lofexidine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Consult cardiologist if considering treatment. Coadministration of ponesimod with drugs that decrease HR may have additive effects on decreasing HR and should generally not be initiated in these patients.

              • prazosin

                lofexidine, prazosin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • propranolol

                lofexidine, propranolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • quinapril

                lofexidine, quinapril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • ramipril

                lofexidine, ramipril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • sacubitril/valsartan

                lofexidine, sacubitril/valsartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • sodium oxybate

                lofexidine, sodium oxybate. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.

              • sotalol

                lofexidine, sotalol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • spironolactone

                lofexidine, spironolactone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • telmisartan

                lofexidine, telmisartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • terazosin

                lofexidine, terazosin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • timolol

                lofexidine, timolol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • torsemide

                lofexidine, torsemide. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • trandolapril

                lofexidine, trandolapril. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • treprostinil

                lofexidine, treprostinil. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • triamterene

                lofexidine, triamterene. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • valsartan

                lofexidine, valsartan. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              • verapamil

                lofexidine, verapamil. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.

              Monitor Closely (218)

              • abiraterone

                abiraterone will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • albuterol

                lofexidine increases and albuterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

                albuterol and lofexidine both increase QTc interval. Use Caution/Monitor.

              • alfentanil

                alfentanil and lofexidine both increase sedation. Use Caution/Monitor.

              • alfuzosin

                lofexidine and alfuzosin both increase QTc interval. Use Caution/Monitor.

              • alprazolam

                alprazolam and lofexidine both increase sedation. Use Caution/Monitor.

              • amiodarone

                amiodarone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • amitriptyline

                amitriptyline and lofexidine both increase sedation. Use Caution/Monitor.

                amitriptyline decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • amobarbital

                amobarbital and lofexidine both increase sedation. Use Caution/Monitor.

              • amoxapine

                amoxapine and lofexidine both increase sedation. Use Caution/Monitor.

                amoxapine decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • anagrelide

                anagrelide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • arformoterol

                lofexidine increases and arformoterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

                arformoterol and lofexidine both increase QTc interval. Use Caution/Monitor.

              • aripiprazole

                aripiprazole and lofexidine both increase sedation. Use Caution/Monitor.

                aripiprazole and lofexidine both increase QTc interval. Use Caution/Monitor.

              • armodafinil

                lofexidine increases and armodafinil decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • arsenic trioxide

                arsenic trioxide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • artemether

                artemether and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • asenapine

                asenapine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • atomoxetine

                atomoxetine and lofexidine both increase QTc interval. Use Caution/Monitor.

              • azelastine

                azelastine and lofexidine both increase sedation. Use Caution/Monitor.

              • azithromycin

                azithromycin increases toxicity of lofexidine by QTc interval. Use Caution/Monitor.

              • baclofen

                baclofen and lofexidine both increase sedation. Use Caution/Monitor.

              • belladonna and opium

                belladonna and opium and lofexidine both increase sedation. Use Caution/Monitor.

              • benperidol

                benperidol and lofexidine both increase sedation. Use Caution/Monitor.

              • benzphetamine

                lofexidine increases and benzphetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • brompheniramine

                brompheniramine and lofexidine both increase sedation. Use Caution/Monitor.

              • buprenorphine

                buprenorphine and lofexidine both increase sedation. Use Caution/Monitor.

              • buprenorphine buccal

                buprenorphine buccal and lofexidine both increase sedation. Use Caution/Monitor.

              • bupropion

                bupropion will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • butabarbital

                butabarbital and lofexidine both increase sedation. Use Caution/Monitor.

              • butalbital

                butalbital and lofexidine both increase sedation. Use Caution/Monitor.

              • butorphanol

                butorphanol and lofexidine both increase sedation. Use Caution/Monitor.

              • caffeine

                lofexidine increases and caffeine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • carbinoxamine

                carbinoxamine and lofexidine both increase sedation. Use Caution/Monitor.

              • carisoprodol

                carisoprodol and lofexidine both increase sedation. Use Caution/Monitor.

              • chloral hydrate

                chloral hydrate and lofexidine both increase sedation. Use Caution/Monitor.

              • chlordiazepoxide

                chlordiazepoxide and lofexidine both increase sedation. Use Caution/Monitor.

              • chloroquine

                chloroquine increases toxicity of lofexidine by QTc interval. Use Caution/Monitor.

              • chlorpheniramine

                chlorpheniramine and lofexidine both increase sedation. Use Caution/Monitor.

              • chlorpromazine

                chlorpromazine and lofexidine both increase sedation. Use Caution/Monitor.

              • chlorpropamide

                chlorpropamide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • chlorzoxazone

                chlorzoxazone and lofexidine both increase sedation. Use Caution/Monitor.

              • cinacalcet

                cinacalcet will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • cinnarizine

                cinnarizine and lofexidine both increase sedation. Use Caution/Monitor.

              • citalopram

                citalopram and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • clemastine

                clemastine and lofexidine both increase sedation. Use Caution/Monitor.

              • clofazimine

                clofazimine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • clomipramine

                clomipramine and lofexidine both increase sedation. Use Caution/Monitor.

                clomipramine decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • clonazepam

                clonazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • clorazepate

                clorazepate and lofexidine both increase sedation. Use Caution/Monitor.

              • clozapine

                clozapine and lofexidine both increase sedation. Use Caution/Monitor.

              • cocaine

                cocaine will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • codeine

                codeine and lofexidine both increase sedation. Use Caution/Monitor.

              • cyclizine

                cyclizine and lofexidine both increase sedation. Use Caution/Monitor.

              • cyclobenzaprine

                cyclobenzaprine and lofexidine both increase sedation. Use Caution/Monitor.

              • cyproheptadine

                cyproheptadine and lofexidine both increase sedation. Use Caution/Monitor.

              • dantrolene

                dantrolene and lofexidine both increase sedation. Use Caution/Monitor.

              • darunavir

                darunavir will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • desflurane

                desflurane and lofexidine both increase sedation. Use Caution/Monitor.

              • desipramine

                desipramine and lofexidine both increase sedation. Use Caution/Monitor.

                desipramine decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • deutetrabenazine

                deutetrabenazine and lofexidine both increase QTc interval. Modify Therapy/Monitor Closely. For patients requiring deutetrabenazine doses >24 mg/day and are taking other drugs known to prolong QTc, assess the QTc interval before and after increasing the dose of deutetrabenazine or other medications known to prolong QTc.

              • dexchlorpheniramine

                dexchlorpheniramine and lofexidine both increase sedation. Use Caution/Monitor.

              • dexfenfluramine

                lofexidine increases and dexfenfluramine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • dexmedetomidine

                dexmedetomidine and lofexidine both increase sedation. Use Caution/Monitor.

              • dexmethylphenidate

                lofexidine increases and dexmethylphenidate decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • dextroamphetamine

                lofexidine increases and dextroamphetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • dextromoramide

                dextromoramide and lofexidine both increase sedation. Use Caution/Monitor.

              • diamorphine

                diamorphine and lofexidine both increase sedation. Use Caution/Monitor.

              • diazepam

                diazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • diethylpropion

                lofexidine increases and diethylpropion decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • difenoxin hcl

                difenoxin hcl and lofexidine both increase sedation. Use Caution/Monitor.

              • dimenhydrinate

                dimenhydrinate and lofexidine both increase sedation. Use Caution/Monitor.

              • diphenhydramine

                diphenhydramine and lofexidine both increase sedation. Use Caution/Monitor.

              • diphenoxylate hcl

                diphenoxylate hcl and lofexidine both increase sedation. Use Caution/Monitor.

              • dipipanone

                dipipanone and lofexidine both increase sedation. Use Caution/Monitor.

              • disopyramide

                disopyramide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • dobutamine

                lofexidine increases and dobutamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • dofetilide

                dofetilide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • dopamine

                lofexidine increases and dopamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • dopexamine

                lofexidine increases and dopexamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • doxepin

                doxepin and lofexidine both increase sedation. Use Caution/Monitor.

                doxepin decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • doxylamine

                doxylamine and lofexidine both increase sedation. Use Caution/Monitor.

              • dronedarone

                dronedarone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • droperidol

                droperidol and lofexidine both increase sedation. Use Caution/Monitor.

              • eliglustat

                eliglustat and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • ephedrine

                lofexidine increases and ephedrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • epinephrine

                lofexidine increases and epinephrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • epinephrine racemic

                lofexidine increases and epinephrine racemic decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • escitalopram

                escitalopram increases toxicity of lofexidine by QTc interval. Use Caution/Monitor.

              • estazolam

                estazolam and lofexidine both increase sedation. Use Caution/Monitor.

              • ethanol

                ethanol and lofexidine both increase sedation. Use Caution/Monitor.

              • etomidate

                etomidate and lofexidine both increase sedation. Use Caution/Monitor.

              • fenfluramine

                lofexidine increases and fenfluramine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • fluoxetine

                fluoxetine will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

                fluoxetine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • fluphenazine

                fluphenazine and lofexidine both increase sedation. Use Caution/Monitor.

              • flurazepam

                flurazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • formoterol

                lofexidine increases and formoterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • fostemsavir

                lofexidine and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

              • haloperidol

                haloperidol and lofexidine both increase sedation. Use Caution/Monitor.

              • hydromorphone

                hydromorphone and lofexidine both increase sedation. Use Caution/Monitor.

              • hydroxyzine

                hydroxyzine and lofexidine both increase sedation. Use Caution/Monitor.

              • ibutilide

                ibutilide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • iloperidone

                iloperidone and lofexidine both increase sedation. Use Caution/Monitor.

                iloperidone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • imipramine

                imipramine and lofexidine both increase sedation. Use Caution/Monitor.

                imipramine decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • isoproterenol

                lofexidine increases and isoproterenol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • ketamine

                ketamine and lofexidine both increase sedation. Use Caution/Monitor.

              • ketotifen, ophthalmic

                ketotifen, ophthalmic and lofexidine both increase sedation. Use Caution/Monitor.

              • levalbuterol

                lofexidine increases and levalbuterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • levorphanol

                levorphanol and lofexidine both increase sedation. Use Caution/Monitor.

              • lisdexamfetamine

                lofexidine increases and lisdexamfetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • lofepramine

                lofepramine and lofexidine both increase sedation. Use Caution/Monitor.

                lofepramine decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • lopinavir

                lopinavir and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • loprazolam

                loprazolam and lofexidine both increase sedation. Use Caution/Monitor.

              • lorazepam

                lorazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • lorcaserin

                lorcaserin will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • lormetazepam

                lormetazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • loxapine

                loxapine and lofexidine both increase sedation. Use Caution/Monitor.

              • loxapine inhaled

                loxapine inhaled and lofexidine both increase sedation. Use Caution/Monitor.

              • lumefantrine

                lumefantrine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • maprotiline

                maprotiline and lofexidine both increase sedation. Use Caution/Monitor.

                maprotiline decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • marijuana

                lofexidine and marijuana both increase sedation. Use Caution/Monitor.

              • melatonin

                lofexidine and melatonin both increase sedation. Use Caution/Monitor.

              • meperidine

                meperidine and lofexidine both increase sedation. Use Caution/Monitor.

              • meprobamate

                lofexidine and meprobamate both increase sedation. Use Caution/Monitor.

              • metaproterenol

                lofexidine increases and metaproterenol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • metaxalone

                metaxalone and lofexidine both increase sedation. Use Caution/Monitor.

              • methadone

                methadone and lofexidine both increase sedation. Use Caution/Monitor.

                methadone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • methamphetamine

                lofexidine increases and methamphetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • methocarbamol

                methocarbamol and lofexidine both increase sedation. Use Caution/Monitor.

              • methylenedioxymethamphetamine

                lofexidine increases and methylenedioxymethamphetamine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • midazolam

                midazolam and lofexidine both increase sedation. Use Caution/Monitor.

              • midodrine

                lofexidine increases and midodrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • mifepristone

                mifepristone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • mirabegron

                mirabegron will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • mirtazapine

                lofexidine and mirtazapine both increase sedation. Use Caution/Monitor.

              • modafinil

                lofexidine increases and modafinil decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • morphine

                morphine and lofexidine both increase sedation. Use Caution/Monitor.

              • motherwort

                lofexidine and motherwort both increase sedation. Use Caution/Monitor.

              • moxifloxacin

                moxifloxacin and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • moxonidine

                lofexidine and moxonidine both increase sedation. Use Caution/Monitor.

              • nabilone

                lofexidine and nabilone both increase sedation. Use Caution/Monitor.

              • nalbuphine

                nalbuphine and lofexidine both increase sedation. Use Caution/Monitor.

              • naltrexone

                lofexidine will decrease the level or effect of naltrexone by unknown mechanism. Modify Therapy/Monitor Closely. Coadministration of lofexidine with oral naltrexone resulted in statistically significant differences in the steady-state pharmacokinetics of naltrexone. The efficacy of oral naltrexone may be reduced if administered within 2 hours of taking lofexidine. Interaction not expected with other naltrexone routes of administration.

              • nilotinib

                nilotinib and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • norepinephrine

                lofexidine increases and norepinephrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • nortriptyline

                nortriptyline and lofexidine both increase sedation. Use Caution/Monitor.

                nortriptyline decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • olanzapine

                olanzapine and lofexidine both increase sedation. Use Caution/Monitor.

              • opium tincture

                opium tincture and lofexidine both increase sedation. Use Caution/Monitor.

              • orphenadrine

                orphenadrine and lofexidine both increase sedation. Use Caution/Monitor.

              • osilodrostat

                osilodrostat and lofexidine both increase QTc interval. Use Caution/Monitor.

              • oxaliplatin

                oxaliplatin will increase the level or effect of lofexidine by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.

              • oxazepam

                oxazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • oxycodone

                oxycodone and lofexidine both increase sedation. Use Caution/Monitor.

              • oxymorphone

                oxymorphone and lofexidine both increase sedation. Use Caution/Monitor.

              • ozanimod

                ozanimod and lofexidine both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.

              • paliperidone

                paliperidone and lofexidine both increase sedation. Use Caution/Monitor.

                paliperidone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • papaveretum

                papaveretum and lofexidine both increase sedation. Use Caution/Monitor.

              • papaverine

                lofexidine and papaverine both increase sedation. Use Caution/Monitor.

              • paroxetine

                paroxetine will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • pentazocine

                pentazocine and lofexidine both increase sedation. Use Caution/Monitor.

              • pentobarbital

                pentobarbital and lofexidine both increase sedation. Use Caution/Monitor.

              • perphenazine

                perphenazine and lofexidine both increase sedation. Use Caution/Monitor.

              • phendimetrazine

                lofexidine increases and phendimetrazine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • phenobarbital

                phenobarbital and lofexidine both increase sedation. Use Caution/Monitor.

              • phentermine

                lofexidine increases and phentermine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • phenylephrine

                lofexidine increases and phenylephrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • phenylephrine PO

                lofexidine increases and phenylephrine PO decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor. .

              • pholcodine

                lofexidine and pholcodine both increase sedation. Use Caution/Monitor.

              • pimavanserin

                pimavanserin and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • pimozide

                pimozide and lofexidine both increase sedation. Use Caution/Monitor.

                pimozide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • pirbuterol

                lofexidine increases and pirbuterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • primidone

                primidone and lofexidine both increase sedation. Use Caution/Monitor.

              • procainamide

                procainamide and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • prochlorperazine

                prochlorperazine and lofexidine both increase sedation. Use Caution/Monitor.

              • promethazine

                promethazine and lofexidine both increase sedation. Use Caution/Monitor.

              • propofol

                propofol and lofexidine both increase sedation. Use Caution/Monitor.

              • propylhexedrine

                lofexidine increases and propylhexedrine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • protriptyline

                protriptyline and lofexidine both increase sedation. Use Caution/Monitor.

                protriptyline decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • quazepam

                quazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • quetiapine

                quetiapine and lofexidine both increase sedation. Use Caution/Monitor.

                quetiapine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • quinidine

                quinidine will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

                quinidine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • ramelteon

                lofexidine and ramelteon both increase sedation. Use Caution/Monitor.

              • ribociclib

                ribociclib and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • risperidone

                risperidone and lofexidine both increase sedation. Use Caution/Monitor.

              • ritonavir

                ritonavir will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • rolapitant

                rolapitant will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • salmeterol

                lofexidine increases and salmeterol decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • scullcap

                lofexidine and scullcap both increase sedation. Use Caution/Monitor.

              • secobarbital

                secobarbital and lofexidine both increase sedation. Use Caution/Monitor.

              • selpercatinib

                selpercatinib increases toxicity of lofexidine by QTc interval. Use Caution/Monitor.

              • sevoflurane

                sevoflurane and lofexidine both increase sedation. Use Caution/Monitor.

              • shepherd's purse

                lofexidine and shepherd's purse both increase sedation. Use Caution/Monitor.

              • sotalol

                sotalol and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • stiripentol

                stiripentol, lofexidine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.

              • sufentanil

                sufentanil and lofexidine both increase sedation. Use Caution/Monitor.

              • tapentadol

                tapentadol and lofexidine both increase sedation. Use Caution/Monitor.

              • temazepam

                temazepam and lofexidine both increase sedation. Use Caution/Monitor.

              • terbutaline

                lofexidine increases and terbutaline decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • tetrabenazine

                tetrabenazine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • thioridazine

                thioridazine and lofexidine both increase sedation. Use Caution/Monitor.

                thioridazine will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

                thioridazine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • thiothixene

                thiothixene and lofexidine both increase sedation. Use Caution/Monitor.

              • tipranavir

                tipranavir will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

              • topiramate

                lofexidine and topiramate both increase sedation. Modify Therapy/Monitor Closely.

              • toremifene

                toremifene and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • tramadol

                tramadol and lofexidine both increase sedation. Use Caution/Monitor.

              • trazodone

                trazodone and lofexidine both increase sedation. Use Caution/Monitor.

                trazodone decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • triazolam

                triazolam and lofexidine both increase sedation. Use Caution/Monitor.

              • triclabendazole

                triclabendazole and lofexidine both increase QTc interval. Use Caution/Monitor.

              • triclofos

                triclofos and lofexidine both increase sedation. Use Caution/Monitor.

              • trifluoperazine

                trifluoperazine and lofexidine both increase sedation. Use Caution/Monitor.

              • trimipramine

                trimipramine and lofexidine both increase sedation. Use Caution/Monitor.

                trimipramine decreases effects of lofexidine by unspecified interaction mechanism. Use Caution/Monitor.

              • triprolidine

                triprolidine and lofexidine both increase sedation. Use Caution/Monitor.

              • valbenazine

                valbenazine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • vandetanib

                vandetanib and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • vemurafenib

                vemurafenib and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              • voclosporin

                voclosporin, lofexidine. Either increases effects of the other by QTc interval. Use Caution/Monitor.

              • xylometazoline

                lofexidine increases and xylometazoline decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • yohimbine

                lofexidine increases and yohimbine decreases sedation. Effect of interaction is not clear, use caution. Use Caution/Monitor.

              • ziconotide

                lofexidine and ziconotide both increase sedation. Use Caution/Monitor.

              • ziprasidone

                ziprasidone and lofexidine both increase sedation. Use Caution/Monitor.

                ziprasidone and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

              Minor (2)

              • eucalyptus

                eucalyptus and lofexidine both increase sedation. Minor/Significance Unknown.

              • sage

                lofexidine and sage both increase sedation. Minor/Significance Unknown.

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              Adverse Effects

              >10%

              Insomnia (51-55%)

              Orthostatic hypotension (29-42%)

              Bradycardia (24-32%)

              Hypotension (30%)

              Dizziness (19-23%)

              Somnolence (11-13%)

              Sedation (12-13%)

              Dry mouth (10-11%)

              1-10%

              Syncope: (0.9-1.4%)

              Tinnitus: (0.9-3.2%)

              Postmarketing Reports

              There has been one report of QT prolongation, bradycardia, torsades de pointes, and cardiac arrest with successful resuscitation in a patient who received lofexidine and three reports of clinically significant QT prolongation in subjects concurrently receiving methadone with lofexidine

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              Warnings

              Contraindications

              None

              Cautions

              May cause hypotension, bradycardia, and syncope; monitor vital signs before dosing and symptoms related to bradycardia and orthostasis; avoid use in patients with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, chronic renal failure, and in patients with marked bradycardia

              Increased risk of QT prolongation; monitor ECG in congestive heart failure, bradyarrhythmias, hepatic impairment, renal impairment, or patients taking medications that lead to QT prolongation (eg, methadone); correct any electrolyte abnormalities (eg, hypokalemia, hypomagnesemia) prior to initiating treatment

              Patients administering therapy in outpatient setting should be capable of and instructed on self-monitoring for hypotension, orthostasis, bradycardia, and associated symptoms; instruct outpatients to withhold doses when experiencing symptoms of hypotension or bradycardia and to contact health care provider for guidance on how to adjust dosing; if clinically significant or symptomatic hypotension and/or bradycardia occur, next dose should be reduced in amount, delayed, or skipped

              Inform patients that therapy may cause hypotension and that patients moving from a supine to an upright position may be at increased risk for hypotension and orthostatic effects

              Instruct patients to stay hydrated, on how to recognize symptoms of low blood pressure, and how to reduce risk of serious consequences should hypotension occur (eg, sit or lie down, carefully rise from a sitting or lying position)

              Advise patients in an outpatient setting that, until they learn how they respond to therapy, they should be careful or avoid doing activities such as driving or operating heavy machinery

              Increased risk of opioid overdose after opioid discontinuation

              • Not a treatment for opioid use disorder
              • Patients who complete opioid discontinuation are likely to have a reduced tolerance to opioids and are at increased risk of fatal overdose should they resume opioid use
              • Use lofexidine in patients with opioid use disorder only in conjunction with a comprehensive management program for the treatment of opioid use disorder and inform patients and caregivers of this increased risk of overdose

              Sudden discontinuation of treatment

              • Stopping abruptly can cause a marked rise in blood pressure; symptoms including diarrhea, insomnia, anxiety, chills, hyperhidrosis, and extremity pain have been observed with discontinuation
              • Instruct patients not to discontinue therapy without consulting their healthcare provider
              • When discontinuing therapy with tablets, gradually reduce the dose (see Dosing)
              • Manage symptoms related to discontinuation by administering the previous dose and subsequent taper

              Drug interaction overview

              • Avoid use in combination with medications that decrease pulse or blood pressure to avoid the risk of excessive bradycardia and hypotension
              • Methadone and lofexidine both prolong the QT interval; monitor ECG when used concomitantly
              • Coadministration with naltrexone may reduce efficacy of oral naltrexone
              • Coadministration with CYP2D6 inhibitors
                • Concomitant use of paroxetine resulted in increased plasma levels of lofexidine; monitor for symptoms of orthostasis and bradycardia with concomitant use of a CYP2D6 inhibitor
              • Coadministration with CNS depressants
                • Lofexidine potentiates CNS depressive effects of benzodiazepines and is expected to potentiate CNS depressive effects of alcohol, barbiturates, and other sedating drugs
                • Advise patients to inform healthcare provider of other medications they are taking, including alcohol
                • In an outpatient setting, advise patients to be careful or to avoid doing activities such as driving or operating heavy machinery
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              Pregnancy

              Pregnancy

              There are no available data regarding use in pregnant women

              Animal data

              • In animal studies, lofexidine decreased breeding rate and increased resorptions at exposures below human exposure
              • Impact of lofexidine on male fertility has not be adequately characterized in animal studies

              Lactation

              No information is available regarding the presence of lofexidine or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production

              Caution if administered to breastfeeding women

              The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child or from the underlying maternal condition

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Centrally acting alpha2-agonist that binds to receptors on adrenergic neurons; this reduces the release of norepinephrine and decreases sympathetic tone

              Absorption

              Absolute bioavailability: 72%

              Peak plasma time: 3-5 hr (single dose)

              Peak plasma concentration: 0.82 mg/mL (3 hr); 0.64 ng/mL (4 hr)

              AUC: 14.9 ng·hr/mL (3 hr); 12 ng·hr/mL (4 hr)

              Shows approximately dose-proportional pharmacokinetics

              Food does not alter pharmacokinetics

              Distribution

              Protein bound: 55%

              Vd: 480 L (PO); 297.9 L (IV); extensive distribution into body tissue

              Not preferentially taken up by blood cells

              Metabolism

              ~30% of administered dose is converted to inactive metabolites during first-pass effect associated with drug absorption from the gut

              Hepatic metabolized by CYP2D6 (major), CYP1A2 (minor), and CYP2C19 (minor)

              Elimination

              Half-life: ~12 hr

              Half-life, terminal: 11-13 hr (first dose); 17-22 hr (steady-state)

              Clearance: 17.6 L/hr

              Pharmacogenomics

              CYP2D6 poor metabolizers

              • Likely that lofexidine exposure would be increased similarly to taking strong CYP2D6 inhibitors (~28%) by CYP2D6 poor metabolizers
              • Monitor adverse events (eg, orthostatic hypotension, bradycardia) in known CYP2D6 poor metabolizers
              • ~8% of whites and 3-8% of blacks cannot metabolize CYP2D6 substrates and are classified as poor metabolizers
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              Administration

              Oral Administration

              May take with or without food

              Storage

              Store in original container at controlled room temperature 25°C (77°F); excursions permitted between 15-30°C (59-86°F)

              Keep away from excess heat and moisture both in the pharmacy and after dispensing

              Do not remove desiccant packs from bottles until all tablets are used

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Lucemyra oral
              -
              0.18 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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              Formulary

              FormularyPatient Discounts

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              • View the formulary and any restrictions for each plan.
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              • Compare formulary status to other drugs in the same class.
              • Access your plan list on any device – mobile or desktop.

              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.