nefazodone


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Related to nefazodone: trazodone

nefazodone

 [nĕ-fa´zo-dōn]
an antidepressant, used as the hydrochloride salt.

nefazodone

(neff-a-zoe-done) ,

Serzone

(trade name)

Classification

Therapeutic: antidepressants
Pregnancy Category: C

Indications

Major depression.Panic disorder, post-traumatic stress disorder (PTSD).

Action

Inhibits the reuptake of serotonin and norepinephrine by neurons.
Antagonizes alpha1-adrenergic receptors.

Therapeutic effects

Antidepressant action, which may develop only after several weeks.

Pharmacokinetics

Absorption: Well absorbed but undergoes extensive and variable first-pass hepatic metabolism (bioavailability about 20%).
Distribution: Widely distributed; enters the CNS.
Protein Binding: ≥99%.
Metabolism and Excretion: Extensively metabolized. One metabolite (hydroxynefazodone) has antidepressant activity.
Half-life: Nefazodone—2–4 hr; hydroxynefazodone—1.5–4 hr.

Time/action profile (antidepressant action)

ROUTEONSETPEAKDURATION
POdays–wkseveral wkunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Concurrent MAO inhibitor therapy;Active liver disease or baseline ↑ serum transaminases.
Use Cautiously in: May ↑ risk of suicide attempt/ideation especially during dose early treatment or dose adjustment;History of suicide attempt or drug abuse;Underlying cardiovascular or cerebrovascular disease;History of mania; Obstetric: Safety no established; Lactation: Discontinue drug or bottle-feed; Pediatric: Safety not established in children; suicide risk may be greater in children and adolescents ; Geriatric: Initiate therapy at lower doses.

Adverse Reactions/Side Effects

Central nervous system

  • suicidal thoughts (life-threatening)
  • dizziness (most frequent)
  • insomnia (most frequent)
  • somnolence (most frequent)
  • agitation
  • confusion
  • weakness

Ear, Eye, Nose, Throat

  • abnormal vision
  • blurred vision
  • eye pain
  • tinnitus

Respiratory

  • dyspnea

Cardiovascular

  • bradycardia
  • hypotension

Gastrointestinal

  • hepatotoxicity (life-threatening)
  • constipation (most frequent)
  • dry mouth (most frequent)
  • nausea (most frequent)
  • gastroenteritis

Genitourinary

  • erectile dysfunction

Dermatologic

  • rash

Hematologic

  • decreased hematocrit

Interactions

Drug-Drug interaction

Serious, potentially fatal reactions may occur during concurrent use withMAO inhibitors(do not use concurrently or within 2 wk of MAO inhibitors; discontinue nefazodone at least 14 days before starting MAO inhibitor therapy).↑ CNS depression with other CNS depressants including alcohol, antihistamines, opioid analgesics, and sedative/hypnotics.May ↑ blood levels and effects of alprazolam or triazolam.May ↑ serum digoxin levels.Additive hypotension may occur with antihypertensives, nitrates, or acute ingestion of alcohol.May ↑ risk of myopathy with HMG-CoA reductase inhibitors.↓ antidepressant action with concomitant use of carbamazepine.May ↓ clearance of haloperidol, so haloperidol dose may need to be ↓.↑ risk of serotonin syndrome with St. John’s wort and SAMe.Kava-kava, valerian, or chamomile can ↑ CNS depression.

Route/Dosage

Oral (Adults) 100 mg twice daily initially; may be ↑ weekly up to 600 mg/day in 2 divided doses.
Oral (Geriatric Patients) 50 mg twice daily initially; may be ↑ weekly as tolerated.

Availability (generic available)

Tablets: 50 mg, 100 mg, 150 mg, 200 mg, 250 mg

Nursing implications

Nursing assessment

  • Assess mental status (orientation, mood, behavior) frequently. Inform health care professional if patient demonstrates significant increase in anxiety, nervousness, or insomnia.
  • Assess suicidal tendencies, especially in early therapy. Restrict amount of drug available to patient.
  • Monitor BP and pulse before and periodically during therapy.
  • Monitor liver function tests prior to and routinely during therapy. Obtain LFTs at first sign of hepatic dysfunction (nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine).
  • Assess for sexual dysfunction throughout treatment.
  • Lab Test Considerations: May cause decrease in hematocrit and leukopenia.
    • Monitor liver function periodically. If serum AST or ALT levels are >3 times the upper limit of normal discontinue nefazodone.
    • May also cause hypercholesterolemia and hypoglycemia.

Potential Nursing Diagnoses

Ineffective coping (Indications)
Risk for injury (Side Effects)

Implementation

  • Do not confuse Serzone (nefazodone) with Seroquel (quetiapine).
  • Discontinue nefazodone prior to elective surgery to prevent potential interactions with general anesthesia.
  • Oral: Administer doses twice daily.

Patient/Family Teaching

  • Instruct patient to take medication as directed. Several weeks may be required to obtain a full antidepressant response. Once response is obtained, therapy should be continued for at least 6 mo. If a dose is missed, take as soon as possible unless almost time for next dose. Do not double doses.
  • May cause drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to the drug is known.
  • Advise patient to make position changes slowly to minimize orthostatic hypotension.
  • Encourage patient and family to be alert for emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, impulsivity, akathisia, hypomania, mania, worsening of depression and suicidal ideation, especially during early antidepressant therapy. Assess symptoms on a day-to-day basis as changes may be abrupt. If these symptoms occur, notify health care professional.
  • Caution patient to avoid taking alcohol or other CNS depressant drugs during therapy and not to take other prescription, OTC medications, or herbal products without consulting health care professional.
  • Advise patient to notify health care professional immediately if signs of liver dysfunction (jaundice, anorexia, GI complaints, malaise, dark urine) occur.
  • Inform patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may minimize dry mouth. If dry mouth persists for more than 2 wk, consult health care professional regarding use of saliva substitute.
  • Instruct patient to notify health care professional of signs of allergy (rash, hives) or if agitation, blurred or other changes in vision, confusion, dizziness, unsteadiness, difficult or frequent urination, difficulty concentrating, or memory problems occur.
  • Instruct female patient to inform health care professional if pregnancy is planned or suspected or if breast feeding.
  • Emphasize the importance of follow-up examinations to monitor progress.

Evaluation/Desired Outcomes

  • Increased sense of well-being.
    • Renewed interest in surroundings. May require several weeks of therapy to obtain full response. Need for therapy should be periodically reassessed. Therapy is usually continued for 6 mo or more.

nefazodone

/ne·fa·zo·done/ (nĕ-fa´zo-dōn) an antidepressant, used as the hydrochloride salt.

nefazodone

Serzone® Psychiatry An anxiolytic serotonin antagonist reuptake inhibitor Adverse effects Sedation, vertigo, weakness
References in periodicals archive ?
Nefazodone is effective for PTSD but is associated with rare but serious hepatotoxicity.
The combination of the prokinetic medication cisapride and the antidepressants fluvoxamine and nefazodone is of particular concern.
A double-blind placebo-controlled trial of nefazodone in the treatment of major depression in alcohol dependent patients.
They are venlafaxine (Effexor) and nefazodone (Serzone).
5 mg when coadministered with a strong CYP3A4/5 inhibitor (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin).
Nefazodone prescribed at doses of 500-600 mg per day to 10 Vietnam combat veterans with PTSD had a strong effect on nightmares (d = 1.
For example, although sexual dysfunction is a commonly reported adverse event associated with second-generation antidepressants, "bupropion is associated with a lower rate of sexual adverse events than fluoxetine or sertraline, whereas paroxetine has higher rates of sexual dysfunction than fluoxetine, fluvoxamine, nefazodone, or sertraline," they stated.
of Patients Mean Dose [mg] in 24 hr Fluoxetine 2 40 Nefazodone 1 300 Sertraline 2 175 Clonazepam 1 2 Lithium 2 1050 Valproate 2 1125 TOTAL NUMBER OF 10 MEDICATIONS AVERAGE NUMBER OF MEDICATIONS 1.
The drugs include bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), and trazodone (Desyrel).
At press time, those changes had been made in the labels for venlafaxine (Effexor and Effexor XR), nefazodone (Serzone), bupropion (Wellbutrin, Zyban), citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), and paroxetine (Paxil).
We describe the case of a patient with rhabdomyolysis that occurred after the patient's simvastatin was titrated to 80 mg at approximately the same time that his antidepressant medication was switched to nefazodone.