Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (136)
- 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.
- adagrasib
adagrasib, lofexidine. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.
- 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.
- amisulpride
amisulpride and lofexidine both increase QTc interval. Avoid or Use Alternate Drug. ECG monitoring is recommended if coadministered.
- 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.
- buprenorphine
buprenorphine and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine buccal
buprenorphine buccal and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine subdermal implant
buprenorphine subdermal implant and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine transdermal
buprenorphine transdermal and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine, long-acting injection
buprenorphine, long-acting injection and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- desflurane
desflurane 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.
- dolasetron
dolasetron and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- donepezil
donepezil and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- efavirenz
efavirenz and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- encorafenib
encorafenib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- eribulin
eribulin and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- fingolimod
fingolimod and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- gemifloxacin
gemifloxacin and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- gilteritinib
gilteritinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- glasdegib
lofexidine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- granisetron
granisetron and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- hydroxyzine
hydroxyzine 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.
- isoflurane
isoflurane and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- itraconazole
itraconazole and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- oxaliplatin
oxaliplatin and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- primaquine
primaquine and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- sertraline
sertraline and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- sevoflurane
sevoflurane and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- siponimod
siponimod and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- sunitinib
sunitinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- tacrolimus
tacrolimus and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- 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.
- vorinostat
vorinostat and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
Monitor Closely (222)
- 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.
- asenapine transdermal
asenapine transdermal and lofexidine both increase QTc interval. Use Caution/Monitor.
- 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 topical
cocaine topical 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. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).
- 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.
doxepin and lofexidine both increase QTc interval. 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.
- gadobenate
gadobenate and lofexidine both increase QTc interval. Use Caution/Monitor.
- 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.
- lithium
lithium and lofexidine both increase QTc interval. 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.
mirtazapine and lofexidine both increase QTc interval. 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.
olanzapine and lofexidine both increase QTc interval. 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.
- solifenacin
solifenacin and lofexidine both increase QTc interval. 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.
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
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
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.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
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
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Lucemyra oral - | 0.18 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Formulary
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