Manufacturer:

Labopharm Inc.

Pharmacological Class:

Triazolopyridine

Active Ingredient(s):

Trazodone HCl 150mg, 300mg; scored ext-rel tabs.

Indication(s):

Major depressive disorder.

Pharmacology:

Trazodone is believed to exert its antidepressant effects by potentiating serotonergic activity through selective inhibition of neuronal reuptake of serotonin. Trazodone also acts as an antagonist at the serotonin 5-HT_2A/2C receptors. Activation of serotonin 5-HT_2A/2C receptors, which studies have shown to be upregulated in patients with depression, inhibits dopamine and norepinephrine release which may contribute to depression. Trazodone does not stimulate the CNS.

Clinical Trials:

A randomized, double-blind, multicenter, two-arm trial was conducted to assess the efficacy of Oleptro in patients with unipolar major depressive disorder. The study, which randomized 412 adult patients, demonstrated a statistically significant difference in the Hamilton Rating Scale for Depression (HAMD-17) total score change from baseline at eight weeks between the Oleptro and placebo groups.

Legal Classification:

Rx

Adults:

May be swallowed whole or broken in half along the scored line; do not crush or chew. Take on empty stomach at bedtime. ≥18yrs: Initially 150mg once daily. May increase by 75mg/day at 3-day intervals; max 375mg/day.

Children:

<18yrs: not recommended.

Warnings/Precautions:

Monitor for clinical worsening, suicidality and unusual changes in behavior, esp. during initiation and dose changes. Acute post MI: not recommended. Monitor for serotonin syndrome or neuroleptic malignant syndrome-like symptoms; discontinue if occurs. Bipolar disorder. Mania/hypomania. Psychosis. Cardiovascular disease. Predisposition to QT prolongation. Hypokalemia. Hypomagnesemia. Renal or hepatic impairment. Volume depletion. Predisposition to priapism (eg, sickle cell anemia, multiple myeloma, leukemia, or anatomically deformed penis). Write Rx for smallest practical amount. Reevaluate periodically. Avoid abrupt cessation. Elderly. Pregnancy (Cat.C). Nursing mothers.

Interaction(s):

Do not use during or within 14 days of MAOIs. Concomitant trytophan: not recommended. Potentiates alcohol, barbiturates, other CNS depressants, digoxin, phenytoin, antihypertensives. Potentiated by CYP3A4 inhibitors (eg, ritonavir, indinavir, ketoconazole, itraconazole). Increased risk of arrhythmias with concomitant potent CYP3A4 inhibitors or drugs that prolong the QT interval; consider lower trazodone dose. Antagonized by CYP3A4 inducers (eg, carbamazepine). Increased risk of bleeding with concomitant NSAIDs, aspirin, anticoagulants. Monitor for serotonin syndrome with SSRIs, SNRIs, triptans (esp. during initiation and dose increases), MAOIs, antipsychotics, antidopaminergic agents. Monitor PT with warfarin. Increased risk of hyponatremia with diuretics.

Adverse Reaction(s):

Somnolence/sedation, dizziness, constipation, blurred vision, headache, anticholinergic effects, GI upset, fatigue, myalgia, hypotension, syncope, hyponatremia, sexual dysfunction, CNS disturbances, dyspnea, night sweats, QT prolongation, torsades de pointes (possible); rare: priapism (discontinue if occurs).

How Supplied:

Tabs—30