LOFEXIDINE

LOFEXIDINE is an FDA-registered drug product whose active ingredient is LOFEXIDINE HYDROCHLORIDE. It is labelled by BioCorRx Pharmaceuticals Inc taken by oral and marketed as a human prescription drug product. Identifiers on file: NDC 85789-901, application NDA209229, label effective 20260722. It is one of 4 FDA drug label records sharing the active ingredient LOFEXIDINE HYDROCHLORIDE. This page reproduces the FDA-approved label text so you can check what a product is, who makes it and how it is supplied before discussing it with a pharmacist or prescriber.

Across FDA labelling, products containing LOFEXIDINE HYDROCHLORIDE are most often described in connection with: lofexidine tablets, mitigation opioid, withdrawal symptoms, facilitate abrupt, discontinuation adults, central alpha-, adrenergic agonist. Wording differs between labels, and the full indications section on this page takes precedence when it is present.

1 INDICATIONS AND USAGE Lofexidine tablets are indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults. Lofexidine tablets are a central alpha-2 adrenergic agonist indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults. ( 1 )

2 DOSAGE AND ADMINISTRATION The usual Lofexidine tablets dosage is three 0.18 mg tablets taken orally 4 times daily at 5- to 6-hour intervals. Lofexidine tablets treatment may be continued for up to 14 days with dosing guided by symptoms. ( 2.1 ) Discontinue Lofexidine tablets with a gradual dose reduction over 2 to 4 days. ( 2.1 ) Hepatic or Renal Impairment : Dosage adjustments are recommended based on degree of impairment. ( 2.2 , 2.3 ) 2.1 Dosing Information The usual Lofexidine tablets starting dosage is three 0.18 mg tablets taken orally 4 times daily during the period of peak withdrawal symptoms (generally the first 5 to 7 days following last use of opioid) with dosing guided by symptoms and side effects. There should be 5 to 6 hours between each dose. The total daily dosage of Lofexidine tablets should not exceed 2.88 mg (16 tablets) and no single dose should exceed 0.72 mg (4 tablets). Lofexidine tablets treatment may be continued for up to 14 days with dosing guided by symptoms. Discontinue Lofexidine tablets with a gradual dose reduction over a 2- to 4-day period to mitigate Lofexidine tablets withdrawal symptoms (e.g., reducing by 1 tablet per dose every 1 to 2 days) [see Warnings & Precautions (5.5) ] . The Lofexidine tablets dose should be reduced, held, or discontinued for individuals who demonstrate a greater sensitivity to Lofexidine tablets side effects [see Warnings and Precautions (5.1) , Adverse Reactions (6.1) ] . Lower doses may be appropriate as opioid withdrawal symptoms wane. Lofexidine tablets can be administered in the presence or absence of food. 2.2 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 (8.6) , Clinical Pharmacology (12.3) ] . Table 1: Dosage Recommendations in Patients with Hepatic Impairment 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) 2.3 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 (8.7) , Clinical Pharmacology (12.3) ] . Table 2: Dosage Recommendations in Patients with Renal Impairment Moderate Impairment Severe Impairment, End-Stage Renal Disease, or on Dialysis Estimated GFR, mL/min/1.73 m 2 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)

4 CONTRAINDICATIONS None. None. ( 4 )

6 ADVERSE REACTIONS The following serious adverse reactions are described elsewhere in labeling: Hypotension, Bradycardia, and Syncope [see Warnings and Precautions (5.1) ] QT Prolongation [see Warnings and Precautions (5.2) ] Central Nervous System Depression [see Warnings and Precautions (5.3) ] Opioid Overdose [see Warnings and Precautions (5.4) ] Discontinuation Symptoms [see Warnings and Precautions (5.5) ] Most common adverse reactions (incidence ≥ 10% and notably more frequent than placebo) are orthostatic hypotension, bradycardia, hypotension, dizziness, somnolence, sedation, and dry mouth. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact BioCorRx Pharmaceuticals Inc at 1-833-LUCEMYRA or FDA at 1-800-FDA-1088 or www.fda.gov/ medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to adverse reaction rates observed for another drug and may not reflect the rates observed in practice. The safety of Lofexidine tablets was supported by three randomized, double-blind, placebo-controlled clinical trials, an open-label study, and clinical pharmacology studies with concomitant administration of either methadone, buprenorphine, or naltrexone. The three randomized, double-blind, placebo-controlled clinical trials enrolled 935 subjects dependent on short-acting opioids undergoing abrupt opioid withdrawal. Patients were monitored before each dose in an inpatient setting. Table 3 presents the incidence, rounded to the nearest percent, of adverse events that occurred in at least 10% of subjects treated with Lofexidine tablets and for which the incidence in patients treated with Lofexidine tablets was greater than the incidence in subjects treated with placebo in a study that tested two doses of Lofexidine tablets, 2.16 mg per day and 2.88 mg per day, and placebo. The overall safety profile in the combined dataset was similar. Orthostatic hypotension, bradycardia, hypotension, dizziness, somnolence, sedation, and dry mouth were notably more common in subjects treated with Lofexidine tablets than subjects treated with placebo. Table 3: Adverse Reactions Reported by ≥10% of Lofexidine tablets-Treated Patients and More Frequently than Placebo Adverse Reaction Lofexidine tablets 2.16 mg 1 (%) N=229 Lofexidine tablets 2.88 mg 1 (%) N=222 Placebo (%) N=151 Insomnia 51 55 48 Orthostatic Hypotension 29 42 5 Bradycardia 24 32 5 Hypotension 30 30 1 Dizziness 19 23 3 Somnolence 11 13 5 Sedation 13 12 5 Dry Mouth 10 11 0 1 Assigned dose; mean average daily dose received was 79% of assigned dose due to dose-holds for out-of-range vital signs. Other notable adverse reactions associated with the use of Lofexidine tablets but reported in <10% of patients in the Lofexidine tablets group included: Syncope: 0.9%, 1.4% and 0% for Lofexidine tablets 2.16 mg/day and 2.88 mg/day and placebo, respectively Tinnitus: 0.9%, 3.2% and 0% for Lofexidine tablets 2.16 mg/day and 2.88 mg/day and placebo, respectively Blood pressure changes and adverse reactions after Lofexidine tablets cessation Elevations in blood pressure above normal values (≥140 mmHg systolic) and above a subject’s pre-treatment baseline are associated with discontinuing Lofexidine tablets, and peaked on the second day after discontinuation, as shown in Table 4 . Blood pressure values were evaluated for 3 days following the last dose of a 5-day course of Lofexidine tablets 2.88 mg/day. Table 4: Blood Pressure Elevations after Stopping Treatment Abrupt Lofexidine tablets Discontinuation 2.88 mg (N = 134) Placebo (N = 129) N at risk n (%) N at risk n (%) Systolic Blood Pressure on Day 2 after Discontinuation ≥ 140 mmHg and ≥ 20 mmHg increase from baseline 58 23 (39.7) 37 6 (16.2) ≥ 170 mmHg and ≥ 20 mmHg increase from baseline 58 5 (8.6) 37 0 Blood pressure elevations of a similar magnitude and incidence were observed in a small number of patients (N=10) that had a one-day, 50% dose reduction prior to discontinuation. After stopping treatment, subjects who were taking Lofexidine tablets also had a higher incidence of diarrhea, insomnia, anxiety, chills, hyperhidrosis, and extremity pain compared to subjects who were taking placebo. Sex-specific adverse event findings Four out of 101 females (4%) had serious cardiovascular adverse events compared to 3 out of 289 (1%) males assigned to receive Lofexidine tablets 2.88 mg/day. Discontinuations and dose-holds due to bradycardia and orthostatic hypotension, which are the most common adverse reactions associated with Lofexidine tablets, occurred with a greater incidence in females assigned to receive the highest studied dose of Lofexidine tablets, 2.88 mg/day as shown in Table 5 . Table 5: Discontinuations and Dose-Holds for Bradycardia and Orthostatic Hypotension by Lofexidine tablets Dose and Sex Lofexidine tablets 2.16 mg Lofexidine tablets 2.88 mg Male 22/162 (14%) 29/158 (18%) Female 9/67 (13%) 20/64 (31%) 6.2 Postmarketing Experience Lofexidine tablets are marketed in other countries for relief of opioid withdrawal symptoms. The following events have been identified during postmarketing use of lofexidine tablets. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Since lofexidine tablets’ initial market introduction in 1992, the most frequently reported postmarketing adverse event with lofexidine tablets has been hypotension [see Warnings and Precautions (5.1) ] . There has been one report of QT prolongation, bradycardia, torsades de pointes, and cardiac arrest with successful resuscitation in a patient who received lofexidine tablets, and three reports of clinically significant QT prolongation in subjects concurrently receiving methadone with lofexidine tablets.

FDA lists 4 drug label records with LOFEXIDINE HYDROCHLORIDE as the active ingredient. The most common dosage forms and the manufacturers with the most records are summarised below; strengths, pack sizes and inactive ingredients can still differ between apparently similar products.

What is LOFEXIDINE used for?
1 INDICATIONS AND USAGE Lofexidine tablets are indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults. Lofexidine tablets are a central alpha-2 adrenergic agonist indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults. ( 1 )

Who makes LOFEXIDINE?
BioCorRx Pharmaceuticals Inc is the labeler of record for LOFEXIDINE. 4 FDA label records share the active ingredient LOFEXIDINE HYDROCHLORIDE, so generic and branded versions may come from different companies; the manufacturer named on your pack is the one that matters for any enquiry.

What form does LOFEXIDINE come in?
administered by oral. Strengths and pack sizes vary by label, so compare the NDC on your pack with the identifier listed on this page.

Is LOFEXIDINE prescription or over-the-counter?
The FDA label for this product is recorded as human prescription drug. Marketing status can differ between strengths and countries, so check the dispensing rules where you live.

Are there other products containing LOFEXIDINE HYDROCHLORIDE?
Yes. 4 FDA drug label records list LOFEXIDINE HYDROCHLORIDE as the active ingredient. Products with the same active ingredient can usually be substituted only when a prescriber or pharmacist confirms it is appropriate.

Has LOFEXIDINE been recalled?
No FDA recall record in our database matches this product name or manufacturer. Recall data is updated periodically, so a very recent notice may not appear here yet.

Where does this information come from?
All content is reproduced from FDA Structured Product Labelling data via openFDA. It is provided for identification and reference only and is not medical advice.