Lofexidine tablets for oral use were approved by FDA in May 2018, for reducing the intensity of opioid withdrawal symptoms. It was earlier approved in the UK in 1992.
Lofexidine is a centrally acting α-2 adrenergic receptor agonist, prescribed for reducing the severity of opioid withdrawal symptoms in adults, with the focus to facilitate the abrupt discontinuation of opioids or following the completion of opioid therapy.
Lofexidine is the first non-opioid drug approved for the symptomatic management of opioid withdrawal.
Lofexidine is also used for treating women suffering from postmenopausal hot flashes.
Lofexidine should not be used in patients with
• Allergy to lofexidine
• Heart disease
• History of opioid use disorder (opioid addiction)
• Severe kidney failure
• Decreased heart rhythm
• Electrolyte abnormalities (low levels of magnesium and potassium)
• Children below 12 years of age
Caution is required in treating pregnant and breastfeeding women due to lack of sufficient data; lofexidine should only be considered if the benefit outweighs the risk.
• Lofexidine tablets are available at a strength of 0.18 mg per tablet.
• The recommended initial adult dose is three 0.18 mg tablets at a time and should not exceed four tablets (0.72 mg).
• Tablets are generally taken for the first 5 to 7 days after the last dose of opioids and can be continued over a period of 2 weeks based on the severity of withdrawal symptoms.
• The total daily dose of lofexidine should not exceed 16 tablets (2.88 mg).
• Dose adjustments are required in patients with severe kidney or liver dysfunction with one 0.18 mg tablet taken four times a day that adds to a maximum of 0.72mg per day.
• Lofexidine tablets should be taken by mouth four times daily, either with or without food.
• Swallow the tablet as a whole with sufficient quantity of water.
• Patients are advised to take a part of lofexidine dose after evening meal to reduce the effect of insomnia or sleeping difficulty induced by opioid withdrawal.
• Lofexidine affects mental alertness, and hence driving vehicles, operating heavy machinery or handling hazardous chemicals should be strictly avoided.
• Patients with electrolyte abnormalities such as hypokalemia and hypomagnesemia should be treated first before starting treatment with lofexidine.
• Alcohol consumption should be avoided as lofexidine increases the depressive effects on the brain.
• Do not discontinue taking lofexidine tablets abruptly as it could result in a sudden rise in blood pressure. It usually requires a gradual dose reduction supervised by the prescriber.
• Blood pressure, pulse rate, and ECG should be monitored regularly before, during and after the treatment. Observe patients for at least 72 hours after dose initiation, or until a stable dose is achieved.
• Patients should be advised not to stand immediately from a sitting or a lying position to avoid accidental falls or injuries.
• Decreased heart rate
• Low blood pressure
• Dizziness or lightheadedness
• Abnormalities in heart rhythm
• Dryness of mucous membranes (mouth, throat, and nose)
• Patients taking lofexidine tablets should drink sufficient quantity of water to keep hydrated, so as to avoid dehydration or getting overheated, as it may result in a sudden drop in heart rate or in low blood pressure.
• Scheduling counseling with a health counselor will help to overcome the craving of taking opioids after withdrawal of opioid therapy.
Avoid taking lofexidine tablets along with the following drugs that increase the QT interval or heart rhythm abnormalities
Drugs that result in a severe loss of potassium should also be avoided with lofexidine as it may also result in prolongation of QT interval.
• Diuretics (e.g., Furosemide, Hydrochlorothiazide)
Lofexidine can increase the effects of antihypertensive drugs (e.g., metoprolol, losartan) leading to low blood pressure or decreased cardiac rhythm and hence should be avoided taken together.
The effects of depression caused on the central nervous system are increased if lofexidine is taken with the following drugs and hence they should not be taken together.
• Benzodiazepines (e.g., Diazepam, Alprazolam)
• Barbiturates (e.g. Phenobarbitone, Secobarbital)
• Other sedative drugs
The effect of oral naltrexone can be reduced if it is taken within 2 hours of lofexidine; this can be overcome by taking naltrexone by non-oral routes.
• Store lofexidine tablets at room temperature, between 15 °C and 25 °C.
• Protect lofexidine tablets from excess heat and moisture.
• Do not remove the desiccant from the bottle which helps to keep the tablets dry.
• Keep lofexidine tablets out of reach of children.
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