Desvenlafaxine

— THERAPEUTIC CATEGORIES —
  • Mood disorders

Desvenlafaxine Generic Name & Formulations

General Description

Desvenlafaxine 50mg, 100mg; ext-rel tabs.

Pharmacological Class

SNRI.

How Supplied

Contact supplier

Mechanism of Action

The exact mechanism of the antidepressant action of desvenlafaxine is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system, through inhibition of their reuptake.

Desvenlafaxine Indications

Indications

Major depressive disorder.

Desvenlafaxine Dosage and Administration

Adult

Swallow whole. 50mg once daily. Moderate renal impairment (CrCl 30–50mL/min): max 50mg/day. Severe renal impairment (CrCl <30mL/min), ESRD: max 50mg every other day. Do not give supplemental dose after dialysis. Moderate to severe hepatic impairment: max 100mg/day. Withdraw gradually.

Children

Not established.

Desvenlafaxine Contraindications

Contraindications

During or within 14 days of MAOIs (see Interactions). Concomitant linezolid or IV methylene blue.

Desvenlafaxine Boxed Warnings

Not Applicable

Desvenlafaxine Warnings/Precautions

Warnings/Precautions

Increased risk of suicidal thinking and behavior in children, adolescents, and young adults; monitor for clinical worsening or unusual changes. Screen for bipolar disorder. Monitor for serotonin syndrome; discontinue immediately if occurs. Pre-existing hypertension, cardio- or cerebrovascular disease. Monitor BP; consider dose reduction or discontinuation if elevated BP persists. Increased risk of bleeding. Avoid in untreated anatomically narrow angles. History of mania/hypomania. Seizure disorder. Volume-depleted. Hyponatremia (esp. in elderly). Sexual dysfunction. Renal or hepatic impairment. Avoid abrupt cessation. Reevaluate periodically. Write ℞ for smallest practical amount. Elderly. Pregnancy; see full labeling for effects on mother and neonates. Nursing mothers.

Desvenlafaxine Pharmacokinetics

Absorption

Absolute oral bioavailability: ~80%.

Distribution

Volume of distribution at steady state: 3.4 L/kg. Plasma protein bound: 30%.

Metabolism

Hepatic (CYP3A4).

Elimination

Renal.

Desvenlafaxine Interactions

Interactions

See Contraindications. Allow ≥14 days after MAOI discontinuance before starting desvenlafaxine; allow ≥7 days after desvenlafaxine discontinuance before starting an MAOI. Increased risk of serotonin syndrome with other serotonergic drugs (eg, SSRIs, SNRIs, triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, meperidine, methadone, tryptophan, buspirone, amphetamines, St. John's Wort) or with drugs that impair serotonin metabolism (eg, MAOIs, linezolid, IV methylene blue). Avoid alcohol. Increased risk of bleeding with aspirin, NSAIDs, warfarin, or other drugs that affect coagulation; monitor closely. May be affected by CYP2D6 substrates. False (+) urine immunoassay screening tests for PCP and amphetamine.

Desvenlafaxine Adverse Reactions

Adverse Reactions

Nausea, dizziness, insomnia, hyperhidrosis, constipation, somnolence, decreased appetite, anxiety, specific male sexual dysfunction; rare: interstitial lung disease or eosinophilic pneumonia (consider discontinuing if occurs).

Desvenlafaxine Clinical Trials

See Literature

Desvenlafaxine Note

Notes

Formerly known under the brand name Khedezla.

Desvenlafaxine Patient Counseling

See Literature