Nefazodone

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Poland: Serzone.

North America

USA: Nefazodone.

Latin America

Brazil: Serzone.

Drug combinations

Chemistry

Nefazodone Hydrochloride: C~25~H~32~ClN~5~O~2~ HCl. Mw: 506.47. (1) 3H-1,2,4-Triazol-3-one, 2-[3-[4-(3-chlorophenyl)-1-piperazinyl)]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-, monohydrochloride; (2) 1-[3-[4-(m-Chlorophenyl)-1-piperazinyl]propyl]-3-ethyl-4-(2-phenoxyethyl)-Δ^2^-1,2,4-triazolin-5-one monohydrochloride. CAS-82752-99-6; CAS-83366-66-9 (nefazodone)(1984).

Pharmacologic Category

Antidepressants; Serotonin Modulators; Serotonin Reuptake Inhibitor/Antagonist. (ATC-Code: N06AX06).

Mechanism of action

Inhibits neuronal reuptake of serotonin and norepinephrine. Also blocks 5-HT~2~ and α~1~ receptors.

Therapeutic use

Treatment of depression.

Pregnancy and lactiation implications

Use with caution in pregnant and nursing women.

Unlabeled use

Post-traumatic stress disorder.

Contraindications

Hypersensitivity to nefazodone, related compounds, or any component of the formulation. Liver injury due to previous nefazodone treatment, active liver disease, or elevated serum transaminases. Concurrent use or use within previous 14 days of MAOIs. Use during acute recovery phase of MI. Concurrent use with carbamazepine, cisapride, or pimozide. Concurrent therapy with triazolam or alprazolam generally contraindicated.

Warnings and precautions

Antidepressants increase risk of suicidal thinking and behavior in children, adolescents, and young adults (18-24 years of age) with major depressive disorder and other psychiatric disorders. Nefazodone not FDA approved for use in children. May worsen psychosis in some patients or precipitate shift to mania or hypomania in bipolar disorder. Monotherapy in bipolar disorder should be avoided. Nefazodone not FDA approved for treatment of bipolar depression. May cause anticholinergic effects (blurred vision, constipation, urinary retention, xerostomia); use with caution in decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, or visual problems. Degree of anticholinergic blockade produced by this agent is very low relative to other antidepressants. Cases of life-threatening hepatic failure reported. May cause orthostatic hypotension (risk low relative to other antidepressants). May cause sedation (degree of sedation low relative to other antidepressants). Rare reports of priapism occurred. Incidence of sexual dysfunction with nefazodone generally lower than with SSRIs. Use with caution in history of cardiovascular disease (including previous MI, stroke, tachycardia, or conduction abnormalities); risk of conduction abnormalities with this agent is very low relative to other antidepressants. Use with caution in renal impairment, or in risk of seizures, including patients with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Effects may be potentiated when used with other sedative drugs. Use with caution in the elderly. Therapy should not be abruptly discontinued in patients receiving high doses for prolonged periods. May increase risks associated with electroconvulsive therapy.

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