Lofexidine
Generic Name: lofexidine
Brand Names:
Lofexidine
11 DESCRIPTION Lofexidine tablets contain lofexidine, a central alpha-2 adrenergic agonist, as the hydrochloride salt. Lofexidine hydrochloride is chemically designated as 2-[1-(2,6-dichlorophenoxy)ethyl]-4,5 dihydro-1 H - imidazole monohydrochloride with a molecular formula of C 11 H 12 Cl 2 N 2 O•HCl. Its molecular weight is 295.6 g/mole and its structural formula is: Lofexidine hydrochloride is a white to off-white crystalline powder freely soluble in water, methanol, and ethanol.
Overview
11 DESCRIPTION Lofexidine tablets contain lofexidine, a central alpha-2 adrenergic agonist, as the hydrochloride salt. Lofexidine hydrochloride is chemically designated as 2-[1-(2,6-dichlorophenoxy)ethyl]-4,5 dihydro-1 H - imidazole monohydrochloride with a molecular formula of C 11 H 12 Cl 2 N 2 O•HCl. Its molecular weight is 295.6 g/mole and its structural formula is: Lofexidine hydrochloride is a white to off-white crystalline powder freely soluble in water, methanol, and ethanol.
Uses
1 INDICATIONS & 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)
Dosage
2 DOSAGE & ADMINISTRATION The usual lofexidine tablet dosage is three 0.18 mg tablets taken orally 4 times daily at 5- to 6-hour intervals. Lofexidine tablet 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 tablet 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.
Side Effects
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 ANI Pharmaceuticals, Inc.
Interactions
7 DRUG INTERACTIONS 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)] .
Warnings
5 WARNINGS AND PRECAUTIONS Risk of Hypotension, Bradycardia, and Syncope : May cause a decrease in blood pressure, a decrease in pulse, and syncope. Monitor vital signs before dosing and advise patients on how to minimize the risk of these cardiovascular effects and manage symptoms, should they occur. Monitor symptoms related to bradycardia and orthostasis. When using in outpatients, ensure that patients are capable of self-monitoring for signs and symptoms. Avoid use in patients with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, or chronic renal failure, as well as in patients with marked bradycardia. (5.1) Risk of QT Prolongation : Lofexidine tablets prolong the QT interval. Avoid use in patients with congenital long QT syndrome. 4 CONTRAINDICATIONS None. None (4)
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.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied Available as 0.18 mg round, convex-shaped, peach colored, film-coated tablets, debossed with “909” on one side and “N” on other side, free from physical defects.
Frequently Asked Questions
What is Lofexidine used for?▼
1 INDICATIONS & 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)
What are the side effects of Lofexidine?▼
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 ANI Pharmaceuticals, Inc.
Can I take Lofexidine during 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.
What are the important warnings for Lofexidine?▼
5 WARNINGS AND PRECAUTIONS Risk of Hypotension, Bradycardia, and Syncope : May cause a decrease in blood pressure, a decrease in pulse, and syncope. Monitor vital signs before dosing and advise patients on how to minimize the risk of these cardiovascular effects and manage symptoms, should they occur. Monitor symptoms related to bradycardia and orthostasis. When using in outpatients, ensure that patients are capable of self-monitoring for signs and symptoms. Avoid use in patients with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, or chronic renal failure, as well as in patients with marked bradycardia. (5.1) Risk of QT Prolongation : Lofexidine tablets prolong the QT interval. Avoid use in patients with congenital long QT syndrome. 4 CONTRAINDICATIONS None. None (4)
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.