Lofexidine
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From MedlinePlus, U.S. National Library of Medicine
Dosing in kidney impairment
Dosage Recommendations for Patients with Renal Impairment Recommended dosage adjustments based on the degree of renal impairment are shown in Table 2. Lofexidine tablets may be administered without regard to the timing of dialysis [see Use in Specific Populations , Clinical Pharmacology ] . [See table below.]
| Moderate Impairment | Severe Impairment, End-Stage Renal Disease, or on Dialysis | |
|---|---|---|
| Estimated GFR, mL/min/1.73 m2 | 30-89.9 | < 30 |
| Recommended dose | 2 tablets 4 times daily (1.44 mg per day) | 1 tablet 4 times daily (0.72 mg per day) |
Dosing in liver impairment
Dosage Recommendations for Patients with Hepatic Impairment Recommended dosage adjustments based on the degree of hepatic impairment are shown in Table 1. [see Use in Specific Populations , Clinical Pharmacology ] . [See table below.]
| Mild Impairment | Moderate Impairment | Severe Impairment | |
|---|---|---|---|
| Child-Pugh score | 5-6 | 7-9 | > 9 |
| Recommended dose | 3 tablets 4 times daily (2.16 mg per day) | 2 tablets 4 times daily (1.44 mg per day) | 1 tablet 4 times daily (0.72 mg per day) |
Drug interactions
Check lofexidine against a medication listLabel text (5 paragraphs)
Methadone : Methadone and Lofexidine tablets both prolong the QT interval. ECG monitoring is recommended when used concomitantly. ( 7.1 ) Oral Naltrexone : Concomitant use may reduce efficacy of oral naltrexone. ( 7.2 ) 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. ( 7.4 )
7.1 Methadone Lofexidine tablets and methadone both prolong the QT interval. ECG monitoring is recommended in patients receiving methadone and Lofexidine tablets concomitantly [see Warnings and Precautions (5.2) , Clinical Pharmacology (12.3) ] .
7.2 Oral Naltrexone Coadministration of Lofexidine tablets and oral naltrexone resulted in statistically significant differences in the steady-state pharmacokinetics of naltrexone. It is possible that oral naltrexone efficacy may be reduced if used concomitantly within 2 hours of Lofexidine tablets. This interaction is not expected if naltrexone is administered by non-oral routes [see Clinical Pharmacology (12.3) ] .
7.3 CNS Depressant Drugs Lofexidine tablets potentiate the CNS depressant effects of benzodiazepines and may potentiate the CNS depressant effects of alcohol, barbiturates, and other sedating drugs. Advise patients to inform their healthcare provider of other medications they are taking, including alcohol [see Warnings and Precautions (5.3) ] .
7.4 CYP2D6 Inhibitor - Paroxetine Coadministration of Lofexidine tablets and paroxetine resulted in a 28% increase in the extent of absorption of Lofexidine. Monitor for orthostatic hypotension and bradycardia when an inhibitor of CYP2D6 is used concomitantly with Lofexidine tablets [see Clinical Pharmacology (12.3) ] .
Contraindications
None. None. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
LiverTox has no chapter for lofexidine. Check the label's hepatic warnings.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary The safety of Lofexidine tablets in pregnant women has not been established. In animal reproduction studies, oral administration of lofexidine during organogenesis to pregnant rats and rabbits caused a reduction in fetal weights, increases in fetal resorptions, and litter loss at exposures below that in humans. When oral lofexidine was administered from the beginning of organogenesis through lactation, increased stillbirths and litter loss were noted along with decreased viability and lactation indices. The offspring exhibited delays in sexual maturation, auditory startle, and surface righting.
These effects occurred at exposures below that in humans [see Animal Data ] . The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies carry some risk of birth defect, loss, or other adverse outcomes. The background risk of major birth defects in the U.S. general population is 2% to 4% and of miscarriage is 15% to 20% of clinically recognized pregnancies.
Data Animal Data Increased incidence of resorptions, decreased number of implantations, and a concomitant reduction in the number of fetuses were observed when pregnant rabbits were orally administered lofexidine hydrochloride during organogenesis (from gestation day [GD] 7 to 19) at a daily dose of 5.0 mg/kg/day (approximately 0.08 times the maximum recommended human dose [MRHD] of 2.88 mg lofexidine base on an AUC basis). Maternal toxicity evidenced by increased mortality was noted at the highest tested dose of 15 mg/kg/day (approximately 0.4 times the MRHD on an AUC basis).
Decreased implantations per dam and decreased mean fetal weights were noted in a study in which pregnant rats were treated with oral lofexidine hydrochloride during organogenesis (from GD 7 to 16) at a daily dose of 3.0 mg/kg/day (approximately 0.9 times the MRHD on an AUC basis). This dose was associated with maternal toxicity (decreased body weight gain and mortality). No malformations or evidence of developmental toxicity were evident at 1.0 mg/kg/day (approximately 0.2 times the MRHD on an AUC basis).
A dose-dependent increase in pup mortality was noted in all doses of lofexidine hydrochloride administered orally to pregnant rats from GD 6 through lactation at an exposure less than the human exposure based on AUC comparisons. Doses higher than 1.0 mg/kg/day (approximately 0.2 times the MRHD on an AUC basis) resulted in incidences of total litter loss and maternal toxicity (piloerection and decreased body weight gain). At the highest dose tested of 2.0…
Breastfeeding (LactMed)
No data are available in nursing mothers on the excretion into milk or safety of lofexidine in nursing mothers. A computer model predicted a maximum relative infant dose of about 3%, which should be acceptable. Although it is not contraindicated during breastfeeding, lofexidine should be used with caution until more data are available. An alternate drug may be preferred, especially while nursing a newborn or preterm infant.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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