bupropion hydrochloride

bu·pro·pi·on hydrochloride (by-prp-n)

n.

A drug used to treat depression and nicotine dependence.

---

bupropion hydrochloride

Budeprion SR, Budeprion XL, Wellbutrin, Wellbutrin SR, Wellbutrin XL, Zyban

Pharmacologic class: Aminoketone

Therapeutic class: Second-generation antidepressant, smoking-cessation aid

Pregnancy risk category C

FDA Boxed Warning

• Although drug isn't indicated for depression, it contains same active ingredient as antidepressants Wellbutrin, Wellbutrin SR, and Wellbutrin XL. Antidepressants increase risk of suicidal thinking and behavior in children and adolescents with major depressive disorder and other psychiatric disorders. Risk is greater during first few months of treatment, and must be balanced with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, and unusual behavior changes when therapy begins. Advise family to observe patient closely and communicate with prescriber as needed.
• Drug isn't approved for use in pediatric patients.

Action

Unclear. Thought to decrease neuronal reuptake of dopamine, serotonin, and norepinephrine in CNS. Action as smoking-cessation aid may result from noradrenergic or dopaminergic activity.

Availability

Tablets: 75 mg, 100 mg

Tablets (sustained-release): 100 mg, 150 mg, 200 mg

⊘Indications and dosages

➣ Depression

Adults: Initially, 100 mg P.O. b.i.d. (morning and evening). After 3 days, may increase to 100 mg t.i.d. After 4 weeks, may increase to a maximum dosage of 450 mg/day in divided doses. No single dose should exceed 150 mg. With total daily dosage of 300 mg, wait at least 6 hours between doses; with total daily dosage of 450 mg, wait at least 4 hours between doses. Alternatively, give one 150-mg sustained-release tablet daily; increase to 150-mg sustained-release tablet b.i.d. based on clinical response.

➣ Smoking cessation

Adults: 150-mg sustained-release tablet once daily for 3 days, then 150-mg sustained-release tablet b.i.d. for 7 to 12 weeks. Space doses at least 8 hours apart.

Contraindications

• Hypersensitivity to drug
• Seizures
• Anorexia nervosa or bulimia
• MAO inhibitor use within past 14 days
• Acute alcohol or sedative withdrawal

Precautions

Use cautiously in:
• renal or hepatic impairment, unstable cardiovascular status
• elderly patients
• pregnant or breastfeeding patients
• children.

Administration

• Be aware that sustained-release tablets should be swallowed whole and not crushed or chewed.
• Single dose shouldn't exceed 150 mg for immediate-release tablets or 200 mg for sustained-release tablets.
• Avoid bedtime doses because they may worsen insomnia.
☞ Know that drug shouldn't be withdrawn abruptly.

Route	Onset	Peak	Duration
P.O.	Unknown	2 hr	Unknown
P.O. (sustained)	Unknown	3 hr	Unknown

Adverse reactions

CNS: agitation, headache, insomnia, mania, psychoses, depression, dizziness, drowsiness, tremor, anxiety, nervousness, seizures

CV: hypertension, hypotension, tachycardia, palpitations, complete atrioventricular block

EENT: blurred vision, amblyopia, auditory disturbances, epistaxis, rhinitis, pharyngitis

GI: nausea, vomiting, dyspepsia, abdominal pain, flatulence, mouth ulcers, dry mouth

GU: urinary frequency, nocturia, vaginal irritation, testicular swelling

Metabolic: hyperglycemia, changes in libido, hypoglycemia, syndrome of inappropriate antidiuretic hormone secretion

Musculoskeletal: arthralgia, myalgia, leg cramps, twitching, neck pain

Respiratory: bronchitis, increased cough, dyspnea

Skin: photosensitivity, dry skin, pruritus, rash, urticaria, diaphoresis, skin temperature changes

Other: altered taste, increased or decreased appetite, weight gain or loss, hot flashes, fever, allergic reaction, flulike symptoms

Interactions

Drug-drug. Benzodiazepine withdrawal, corticosteroids, other antidepressants, over-the-counter stimulants, phenothiazines, theophylline: increased risk of seizures

Cimetidine: inhibited bupropion metabolism

Levodopa, MAO inhibitors: increased risk of adverse reactions

Ritonavir: increased bupropion blood level

Drug-diagnostic tests. Glucose: increased level

Drug-behaviors. Alcohol use or cessation: increased risk of seizures

Sun exposure: increased risk of photosensitivity

Patient monitoring

• Monitor blood pressure, ECG, CBC, and renal and hepatic function. Monitor tricyclic antidepressant (TCA) blood level if patient's taking TCAs concurrently.
• Be aware that if patient is also on nicotine patch for smoking cessation, the combination may cause or increase risk of hypertension.
• Check for oral and dental problems.

Patient teaching

• Instruct patient to swallow sustained-release tablets without crushing or chewing.
☞ Caution patient not to discontinue drug abruptly.
• Emphasize importance of frequent oral hygiene. (Dry mouth increases risk of caries and dental problems.)
• Caution patient to avoid alcohol, because it may increase risk of seizures.
• Advise patient to keep regular appointments for periodic blood tests and hepatic and renal studies.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.