NEFAZODONE

NEFAZODONE
(nef-a-zo'done)
Classifications: psychotherapeutic agent; antidepressant; selective serotonin reuptake inhibitor (ssri);
Therapeutic: antidepressant
; ssri
Prototype: Fluoxetine HCl
Pregnancy Category: C

Availability

50 mg, 100 mg, 150 mg, 200 mg, 250 mg tablets

Action

Antidepressant with a dual mechanism of action. Inhibits neuronal serotonin (5-HT1) reuptake and also possesses 5-HT2 antagonist properties.

Therapeutic Effect

Antidepressant effects with minimal cardiovascular effects, fewer anticholinergic effects, less sedation, and less sexual dysfunction than other antidepressants.

Uses

Treatment of depression.

Contraindications

Hypersensitivity to nefazodone or alcohol; hepatic disease, hepatitis, jaundice; MAOI therapy; mania; severe restlessness, suicidal ideation; surgery, neonates; pregnancy (category C), lactation.

Cautious Use

Older adults, women of childbearing age; history of seizure disorders, seizures; renal or hepatic impairment; recent MI, unstable cardiac disease; hypotension; angina, stroke, hypovolemia, dehydration, bipolar disorder; history of mania; ECT therapy. Safety and efficacy in children <18 y are not established.

Route & Dosage

Depression
Adult: PO 50–100 mg b.i.d., may need to increase up to 300–600 mg/d in 2–3 divided doses
Geriatric: PO Start with 50 mg b.i.d.

Administration

Oral
  • Do not give within 14 d of discontinuation of an MAO inhibitor.
  • Store at 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

Body as a Whole: Anaphylactic reactions, angioedema. CNS: Headache, dizziness, drowsiness, asthenia, tremor, insomnia, agitation, anxiety. GI: Dry mouth, constipation, nausea, liver toxicity. Special Senses: Visual disturbances, blurred vision, scotomata. Endocrine: Galactorrheas, gynecomastia, serotonin syndrome. Skin: Stevens-Johnson syndrome, liver failure.

Interactions

Drug: May cause serotonin syndrome (see Appendix F) with maois or ssris; may increase plasma levels of some benzodiazepines, including alprazolam and triazolam. May decrease plasma levels and effects of propranolol. May increase levels and toxicity of buspirone, carbamazepine, cilostazol, digoxin; reports of QTc prolongation and ventricular arrhythmias with pimozide; increased risk of rhabdomyolysis with lovastatin, simvastatin; increased risk of ergotamine toxicity with dihydroergotamine, ergotamine. Herbal: St. John's wort may cause serotonin syndrome.

Pharmacokinetics

Onset: 1 wk. Peak: 3–5 wk. Metabolism: In liver to at least two active metabolites. Half-Life: Nefazodone 3.5 h, metabolites 2–33 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for worsening of depression or emergence of suicidal ideation.
  • Evaluate concurrent drugs for possible interactions.
  • Monitor patients with a history of seizures for increased activity.
  • Assess safety, as dizziness and drowsiness are common adverse effects.
  • Lab tests: Monitor periodically liver function and CBC during long-term therapy.

Patient & Family Education

  • Be aware that significant improvement in mood may not occur for several weeks following initiation of therapy.
  • Do not drive or engage in potentially hazardous activities until response to the drug is known.
  • Report changes in visual acuity.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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