Nefazodone hydrochloride
Nefazodone hydrochloride (Serzone)
Nefazodone hydrochloride
(nih- FAY-zoh-dohn)
Pregnancy Category: C Serzone (Rx)

Classification: Antidepressant

Action/Kinetics: Exact antidepressant mechanism not known. Inhibits neuronal uptake of serotonin and norepinephrine and antagonizes central 5-HT ₂ receptors and alpha-1-adrenergic receptors (which may cause postural hypotension). Produces none to slight anticholinergic effects, moderate sedation, and slight orthostatic hypotension. Peak plasma levels: 1 hr. t 1/2: 2-4 hr. Time to reach steady state: 4-5 days. Extensively metabolized by the liver with less than 1% excreted unchanged in the urine. Food delays the absorption of nefazodone and decreases the bioavailability by approximately 20%.

Uses: Treatment of depression.

Contraindications: Use with cisapride or pimozide; in combination with an MAO inhibitor or within 14 days of discontinuing MAO inhibitor therapy. Clients hypersensitive to nefazodone or other phenylpiperazine antidepressants.

Special Concerns: Use with caution in clients with a recent history of MI, unstable heart disease and taking digoxin, or a history of mania. Use with caution during lactation. Safety and efficacy have not been determined in individuals below 18 years of age. There is a possibility of a suicide attempt in depression that may persist until significant remission occurs.

Side Effects: CNS: Dizziness, insomnia, agitation, somnolence, lightheadedness, activation of mania or hypomania, confusion, memory impairment, paresthesia, abnormal dreams, decreased concentration, ataxia, incoordination, psychomotor retardation, tremor, hypertonia, decreased libido, vertigo, twitching, depersonalization, hallucinations, suicide thoughts/attempt apathy, euphoria, hostility, abnormal gait, abnormal thinking, derealization, paranoid reaction, dysarthria, myoclonus, neuroleptic malignant syndrome (rare). CV: Postural hypotension, hypotension, sinus bradycardia, tachycardia, hypertension, syncope, ventricular extrasystoles, angina pectoris, CVA (rare). GI: Nausea, dry mouth, constipation, dyspepsia, diarrhea, increased appetite, vomiting, eructation, periodontal abscess, gingivitis, colitis, gastritis, mouth ulceration, stomatitis, esophagitis, peptic ulcer, rectal hemorrhage. Dermatologic: Pruritus, dry skin, acne, alopecia, urticaria, maculopapular rash, vesiculobullous rash, eczema. Musculoskeletal: Asthenia, arthralgia, arthritis, tenosynovitis, muscle stiffness, bursitis. Respiratory: Pharyngitis, increased cough, dyspnea, bronchitis, asthma, pneumonia, laryngitis, voice alteration, epistaxis, hiccups. Hematologic: Ecchymosis, anemia, leukopenia, lymphadenopathy. Ophthalmologic: Blurred vision, abnormal vision, visual field defect, dry eye, eye pain, abnormal accommodation, diplopia, conjunctivitis, mydriasis, keratoconjunctivitis, photophobia, night blindness. Body as a whole: Headache, infection, flu syndrome, chills, fever, neck rigidity, allergic reaction, malaise, photosensitivity, facial edema, hangover effect, enlarged abdomen, hernia, pelvic pain, halitosis, cellulitis, weight loss, gout, dehydration. GU: Urinary frequency, UTI, urinary retention, vaginitis, breast pain, cystitis, urinary urgency, metrorrhagia, amenorrhea, polyuria, vaginal hemorrhage, breast enlargement, menorrhagia, urinary incontinence, abnormal ejaculation, hematuria, nocturia, kidney calculus. Miscellaneous: Peripheral edema, thirst, abnormal LFTs, ear pain, hyperacusis, deafness, taste loss.

Laboratory Test Alterations: AST, ALT, LDH. Hematocrit. Hypercholesterolemia, hypoglycemia.

Overdose Management: Symptoms: N&V;, somnolence, increased incidence of severity of any of the reported side effects. Treatment: Symptomatic and supportive in the cases of hypotension or excessive sedation. Gastric lavage may be used.

Drug Interactions: Alprazolam / Alprazolam plasma levels Buspirone / Levels of both drugs lightheadedness, somnolence, dizziness, asthenia Carbamazepine / Carbamazepine plasma levels Cisapride / Risk of serious cardiac arrhythmias Digoxin / Digoxin plasma levels HMG-CoA reductase inhibitors / Risk of rhabdomyolysis and myositis MAO inhibitors / Serious and possibly fatal reactions including symptoms of hyperthermia, rigidity, myoclonus, autonomic instability with possible rigid fluctuations of VS, and mental status changes that may include extreme agitation progressing to delirium and coma Pimozide / Plasma levels of pimozide resulting in QT prolongation and possible serious CV events, including death due to ventricular tachycardia of the torsades de pointes type Propranolol / Propranolol plasma levels Sibutramine / Serotonin syndrome, including CNS irritability, motor weakness, shivering, myoclonus, and altered consciousness Trazodone / Serotonin syndrome, including CNS irritability, motor weakness, shivering, myoclonus, and altered consciousness Triazolam / Triazolam plasma levels

How Supplied: Tablet: 50 mg, 100 mg, 150 mg, 200 mg, 250 mg

Dosage
?Tablets Antidepressant.
Adults, initial: 200 mg/day given in two divided doses. Increase dose in increments of 100-200 mg/day at intervals of no less than 1 week. The effective dose range is 300-600 mg/day. The initial dose for elderly or debilitated clients is 100 mg/day given in two divided doses.