Version July 2025
Opioid withdrawal: Oral: Initial: 0.54 mg 4 times daily (every 5 to 6 hours) during peak withdrawal symptoms (generally the first 5 to 7 days after last opioid use); adjust dosing based on tolerability and withdrawal symptoms and may continue for up to 14 days if needed; maximum dose: 0.72 mg/dose or 2.88 mg/day. Note: Lower doses may be appropriate as opioid withdrawal symptoms wane.
Discontinuation of therapy: Decrease dose gradually over 2 to 4 days (eg, reduce by 0.18 mg per dose every 1 to 2 days).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
eGFR ≥90 mL/minute/1.73 m2: No dosage adjustment necessary.
eGFR 30 to 89.9 mL/minute/1.73 m2: 0.36 mg 4 times daily
eGFR <30 mL/minute/1.73 m2: 0.18 mg 4 times daily
ESRD or on hemodialysis: 0.18 mg 4 times daily; minimally dialyzable; administer without regard to the timing of dialysis
Mild impairment (Child-Pugh class A): No dosage adjustment necessary.
Moderate impairment (Child-Pugh class B): 0.36 mg 4 times daily
Severe impairment (Child-Pugh class C): 0.18 mg 4 times daily
Refer to adult dosing; use with caution; consider lower doses
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions may include concomitant administration of methadone, buprenorphine, or naltrexone.
>10%:
Cardiovascular: Bradycardia (24% to 32%), hypotension (30%), orthostatic hypotension (29% to 42%)
Gastrointestinal: Xerostomia (10% to 11%)
Nervous system: Dizziness (19% to 23%), drowsiness (11% to 13%), insomnia (51% to 55%), sedated state (12% to 13%)
1% to 10%:
Cardiovascular: Syncope (≤1%)
Otic: Tinnitus (≤3%)
Postmarketing: Cardiovascular: Prolonged QT interval on ECG (Schmittner 2004), torsades de pointes
There are no contraindications listed in the manufacturer's labeling.
Concerns related to adverse effects:
• Accidental opioid overdose: Lofexidine is not a treatment for opioid use disorder, and it should be used only in conjunction with a comprehensive management program for the treatment of opioid use disorder. Patients who had been treated with lofexidine may respond to lower opioid doses than previously used. This could result in potentially life-threatening opioid overdose. Patients should be aware that they may be more sensitive to lower doses of opioids after lofexidine treatment is discontinued, after a missed dose, or near the end of the dosing interval.
• Cardiovascular effects: May cause syncope or a decrease in blood pressure or heart rate; monitor vital signs before dosing and observe for symptoms of bradycardia and syncope. Reduce dose or interrupt therapy if clinically significant bradycardia and/or hypotension occur. Avoid use in patients with severe coronary insufficiency, recent myocardial infarction, significant bradycardia, cerebrovascular disease, and chronic renal failure.
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).
• QT prolongation: May cause QT prolongation; avoid use in patients with congenital long QT syndrome. Monitor ECG in at-risk patients (heart failure, bradyarrhythmias, hepatic impairment, renal impairment, concomitant QT-prolonging medications). In patients with electrolyte abnormalities, correct abnormality first, then monitor ECG before initiating lofexidine.
Disease-related concerns:
• Hepatic impairment: Prolongation of the QTc interval is more pronounced in patients with severe hepatic impairment. Use caution in patients with hepatic impairment.
• Renal impairment: Prolongation of the QTc interval is more pronounced in patients with severe renal impairment. Use caution in patients with renal impairment; avoid use in patients with chronic renal failure.
Special populations:
• CYP2D6 poor metabolizers: Exposure to lofexidine may be increased; monitor for orthostasis and bradycardia.
Other warnings/precautions:
• Discontinuation of therapy: Discontinuing lofexidine abruptly may result in a marked rise in blood pressure, anxiety, chills, diarrhea, extremity pain, hyperhidrosis and insomnia. When discontinuing therapy, treatment should be gradually reduced to avoid these symptoms. Do not abruptly discontinue.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Lucemyra: 0.18 mg [contains fd&c yellow #6 (sunset yellow)]
Generic: 0.18 mg
Yes
Tablets (Lofexidine HCl Oral)
0.18 mg (per each): $17.51 - $27.72
Tablets (Lucemyra Oral)
0.18 mg (per each): $29.18
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Oral: Administer with or without food.
Opioid withdrawal: Mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults.
Substrate of CYP2D6 (Major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Ajmaline: Lofexidine may increase QTc-prolonging effects of Ajmaline. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification
Alfuzosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Amifostine: Blood Pressure Lowering Agents may increase hypotensive effects of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider Therapy Modification
Amiodarone: Lofexidine may increase QTc-prolonging effects of Amiodarone. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification
Amisulpride (Oral): May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor
Amisulpride (Oral): May increase QTc-prolonging effects of QT-prolonging Agents (Moderate Risk). Risk C: Monitor
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may increase hypotensive effects of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor
Arginine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Artemether and Lumefantrine: May increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor
Barbiturates: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Benperidol: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Beta-Blockers: May increase rebound hypertensive effects of Alpha2-Agonists. This effect can occur when the Alpha2-Agonist is abruptly withdrawn. Alpha2-Agonists may increase AV-blocking effects of Beta-Blockers. Sinus node dysfunction may also be enhanced. Management: Closely monitor heart rate during treatment with a beta blocker and clonidine. Withdraw beta blockers several days before clonidine withdrawal when possible, and monitor blood pressure closely. Recommendations for other alpha2-agonists are unavailable. Risk D: Consider Therapy Modification
Blood Pressure Lowering Agents: May increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor
Bradycardia-Causing Agents: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor
Brimonidine (Topical): May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Bromperidol: May decrease hypotensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase hypotensive effects of Bromperidol. Risk X: Avoid
Chloroquine: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Chloroquine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Citalopram: Lofexidine may increase QTc-prolonging effects of Citalopram. Citalopram may increase QTc-prolonging effects of Lofexidine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Clofazimine: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Clofazimine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
CNS Depressants: Lofexidine may increase CNS depressant effects of CNS Depressants. Risk C: Monitor
CYP2D6 Inhibitors (Strong): May increase serum concentration of Lofexidine. Risk C: Monitor
Dabrafenib: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Dabrafenib. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Diazoxide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Domperidone: QT-prolonging Agents (Moderate Risk) may increase QTc-prolonging effects of Domperidone. Risk X: Avoid
Dronedarone: Lofexidine may increase QTc-prolonging effects of Dronedarone. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification
DULoxetine: Blood Pressure Lowering Agents may increase hypotensive effects of DULoxetine. Risk C: Monitor
Encorafenib: May increase QTc-prolonging effects of QT-prolonging Miscellaneous Agents (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Escitalopram: Lofexidine may increase QTc-prolonging effects of Escitalopram. Escitalopram may increase QTc-prolonging effects of Lofexidine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Etrasimod: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor
Fingolimod: Bradycardia-Causing Agents may increase bradycardic effects of Fingolimod. Management: Consult with the prescriber of any bradycardia-causing agent to see if the agent could be switched to an agent that does not cause bradycardia prior to initiating fingolimod. If combined, perform continuous ECG monitoring after the first fingolimod dose. Risk D: Consider Therapy Modification
Fluorouracil Products: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Fluorouracil Products. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Gadobenate Dimeglumine: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Gadobenate Dimeglumine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Halofantrine: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Halofantrine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Haloperidol: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Haloperidol. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Herbal Products with Blood Pressure Lowering Effects: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Hypotension-Associated Agents: Blood Pressure Lowering Agents may increase hypotensive effects of Hypotension-Associated Agents. Risk C: Monitor
Iloperidone: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Ivabradine: Bradycardia-Causing Agents may increase bradycardic effects of Ivabradine. Risk C: Monitor
Lacosamide: Bradycardia-Causing Agents may increase AV-blocking effects of Lacosamide. Risk C: Monitor
Landiolol: Bradycardia-Causing Agents may increase bradycardic effects of Landiolol. Risk X: Avoid
Levodopa-Foslevodopa: Blood Pressure Lowering Agents may increase hypotensive effects of Levodopa-Foslevodopa. Risk C: Monitor
Levoketoconazole: QT-prolonging Agents (Moderate Risk) may increase QTc-prolonging effects of Levoketoconazole. Risk X: Avoid
Lormetazepam: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Mavorixafor: May increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk X: Avoid
Metergoline: May decrease antihypertensive effects of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may increase orthostatic hypotensive effects of Metergoline. Risk C: Monitor
Methadone: Lofexidine may increase QTc-prolonging effects of Methadone. Management: Consider alternatives to this drug combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification
Midodrine: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor
Mirtazapine: May decrease antihypertensive effects of Alpha2-Agonists. Management: Consider avoiding concurrent use. If the combination cannot be avoided, monitor for decreased effects of alpha2-agonists if mirtazapine is initiated/dose increased, or increased effects if mirtazapine is discontinued/dose decreased. Risk D: Consider Therapy Modification
Molsidomine: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Naftopidil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Naltrexone: Lofexidine may decrease serum concentration of Naltrexone. Risk C: Monitor
Nicergoline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Nicorandil: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Nitroprusside: Blood Pressure Lowering Agents may increase hypotensive effects of Nitroprusside. Risk C: Monitor
Obinutuzumab: May increase hypotensive effects of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider Therapy Modification
Ondansetron: QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Ondansetron. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Ozanimod: May increase bradycardic effects of Bradycardia-Causing Agents. Risk C: Monitor
Peginterferon Alfa-2b: May decrease serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Peginterferon Alfa-2b may increase serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor
Pentamidine (Systemic): QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of Pentamidine (Systemic). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Pentoxifylline: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Pholcodine: Blood Pressure Lowering Agents may increase hypotensive effects of Pholcodine. Risk C: Monitor
Phosphodiesterase 5 Inhibitors: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Pimozide: May increase QTc-prolonging effects of QT-prolonging Agents (Moderate Risk). Risk X: Avoid
Piperaquine: QT-prolonging Agents (Moderate Risk) may increase QTc-prolonging effects of Piperaquine. Risk X: Avoid
Ponesimod: Bradycardia-Causing Agents may increase bradycardic effects of Ponesimod. Management: Avoid coadministration of ponesimod with drugs that may cause bradycardia when possible. If combined, monitor heart rate closely and consider obtaining a cardiology consult. Do not initiate ponesimod in patients on beta-blockers if HR is less than 55 bpm. Risk D: Consider Therapy Modification
Prostacyclin Analogues: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
QT-prolonging Agents (Highest Risk): May increase QTc-prolonging effects of Lofexidine. Management: Consider alternatives to this combination. If combined, monitor for QTc interval prolongation and ventricular arrhythmias. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification
QT-prolonging Antidepressants (Moderate Risk): Lofexidine may increase QTc-prolonging effects of QT-prolonging Antidepressants (Moderate Risk). QT-prolonging Antidepressants (Moderate Risk) may increase QTc-prolonging effects of Lofexidine. QT-prolonging Antidepressants (Moderate Risk) may decrease therapeutic effects of Lofexidine. Management: Consider avoiding this combination when possible. Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk D: Consider Therapy Modification
QT-prolonging Antipsychotics (Moderate Risk): QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of QT-prolonging Antipsychotics (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-prolonging Class IC Antiarrhythmics (Moderate Risk): QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of QT-prolonging Class IC Antiarrhythmics (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-Prolonging Inhalational Anesthetics (Moderate Risk): QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of QT-Prolonging Inhalational Anesthetics (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-prolonging Kinase Inhibitors (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Miscellaneous Agents (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-prolonging Miscellaneous Agents (Moderate Risk): May increase QTc-prolonging effects of Lofexidine. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Miscellaneous Agents (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase serum concentration of QT-prolonging Miscellaneous Agents (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-prolonging Quinolone Antibiotics (Moderate Risk): QT-prolonging Miscellaneous Agents (Moderate Risk) may increase QTc-prolonging effects of QT-prolonging Quinolone Antibiotics (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk): May increase QTc-prolonging effects of QT-prolonging Miscellaneous Agents (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Quinagolide: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Serotonin/Norepinephrine Reuptake Inhibitor: May decrease therapeutic effects of Alpha2-Agonists. Risk C: Monitor
Sertindole: May increase QTc-prolonging effects of QT-prolonging Agents (Moderate Risk). Risk X: Avoid
Silodosin: May increase hypotensive effects of Blood Pressure Lowering Agents. Risk C: Monitor
Siponimod: Bradycardia-Causing Agents may increase bradycardic effects of Siponimod. Management: Avoid coadministration of siponimod with drugs that may cause bradycardia. If combined, consider obtaining a cardiology consult regarding patient monitoring. Risk D: Consider Therapy Modification
Sotalol: Lofexidine may increase QTc-prolonging effects of Sotalol. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. Risk D: Consider Therapy Modification
Thioridazine: QT-prolonging Agents (Moderate Risk) may increase QTc-prolonging effects of Thioridazine. Risk X: Avoid
TiZANidine: Alpha2-Agonists may increase hypotensive effects of TiZANidine. Risk X: Avoid
Tricyclic Antidepressants: May decrease therapeutic effects of Lofexidine. Management: Consider avoiding this drug combination when possible. If concurrent administration is required, monitor blood pressure carefully at the beginning of the combined therapy and when either drug is stopped. Adjust the dosage accordingly. Risk D: Consider Therapy Modification
Information related to the use of lofexidine in pregnancy is limited (Akhurst 2000). Abrupt discontinuation of opioid therapy in dependent patients is generally not recommended during pregnancy (ASAM 2020).
It is not known if lofexidine is present in breast milk.
According to the manufacturer, lofexidine should be used with caution in breastfeeding patients; the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Blood pressure; heart rate; electrolytes and ECG at baseline in at-risk populations; opioid withdrawal symptoms
Lofexidine is a central alpha-2 adrenergic agonist that reduces the release of norepinephrine and decreases sympathetic tone. It binds to alpha-2A (ki=7.2 nM) and alpha-2C (ki=12 nM) adrenoreceptors. Due to its high selectivity for the alpha-2A receptor, lofexidine is thought to be associated with less anti-hypertensive activity than clonidine (Gish 2010).
Absorption: Well-absorbed
Distribution: Oral: Vd apparent = 480 L; IV: Vd = 297.9 L
Protein binding: ~55%
Metabolism: First pass effect associated with gut absorption (~30% of the dose is converted to inactive metabolites); hepatic via CYP2D6 (primary), CYP1A2 and CYP2C19
Bioavailability: 72%
Half-life elimination: 11 to 13 hours (first dose); 17 to 22 hours (steady state)
Time to peak: 3 to 5 hours
Excretion: Urine (93.5%; 15% to 20% unchanged); feces (0.92%)
Altered kidney function: Cmax, AUC and half-life increased slightly with the severity of renal impairment.
Hepatic function impairment: Half-life was prolonged in patients with hepatic impairment.
