What is the recommended dosage and administration schedule for Bupropion (Bupropion) Hydrochloride XL?

Bupropion Hydrochloride XL Dosage and Administration

The recommended dosage for Bupropion Hydrochloride XL is 150 mg once daily in the morning for the first 4 days, then increasing to the target dose of 300 mg once daily in the morning. 1

Initial Dosing and Titration

• Start with 150 mg once daily in the morning
• After 4 days, increase to the target dose of 300 mg once daily
• Bupropion XL should be swallowed whole (not crushed, divided, or chewed)
• May be taken with or without food
• Always administer in the morning 1

Important Administration Guidelines

• Gradual dose increases minimize the risk of seizures
• The extended-release (XL) formulation allows for once-daily dosing, improving adherence compared to immediate-release (IR) formulations that require three times daily dosing 2, 3
• The XL formulation has a prolonged absorption profile (Tmax 5 hours) compared to IR (1.5 hours) and SR (~3 hours) formulations 2

Dose Adjustments for Special Populations

Hepatic Impairment

• Moderate to severe impairment (Child-Pugh score 7-15): Maximum dose 150 mg every other day
• Mild impairment (Child-Pugh score 5-6): Consider reducing dose and/or frequency 1

Renal Impairment

• For GFR <90 mL/min: Consider reducing dose and/or frequency 1

Discontinuation Protocol

• When discontinuing treatment with 300 mg once daily, decrease to 150 mg once daily prior to complete discontinuation
• Gradual tapering helps minimize withdrawal symptoms 1

Drug Interactions and Contraindications

Contraindications

• Seizure disorder
• Current or prior diagnosis of bulimia or anorexia nervosa
• Concurrent use of MAO inhibitors (allow 14 days between stopping MAOIs and starting bupropion)
• Abrupt discontinuation of alcohol, benzodiazepines, or antiepileptic drugs 4, 1

Precautions

• Monitor blood pressure and heart rate, especially in the first 12 weeks
• Use caution in patients with history of seizures or conditions that lower seizure threshold
• Avoid use with other medications that lower seizure threshold 4, 1

Common Adverse Effects

• Insomnia (4%)
• Dry mouth (20%)
• Headache
• Nausea
• Anxiety/jitteriness
• Decreased appetite 5, 4

Clinical Pearls

• Bupropion XL has a lower risk of sexual dysfunction compared to SSRIs, making it a good option for patients concerned about this side effect 4, 3
• The medication has minimal weight gain potential compared to other antidepressants 3
• Bupropion inhibits CYP2D6 and may reduce clearance of medications metabolized by this enzyme 2
• Bupropion is extensively metabolized by the liver, with hydroxybupropion being the primary active metabolite 2

Remember that bupropion should not be used with MAOIs or within 14 days of discontinuing an MAOI due to risk of hypertensive reactions 1. The once-daily XL formulation offers convenience and bioequivalence to the other formulations while potentially improving adherence.