Desyrel (Trazodone Hydrochloride) Drug Information: Clinical Pharmacology

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May 27, 2012

Desyrel

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Please Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

CLINICAL PHARMACOLOGY

The mechanism of DESYREL (trazodone hydrochloride) 's antidepressant action in man is not fully understood. In animals, DESYREL (trazodone hydrochloride) selectively inhibits serotonin uptake by brain synaptosomes and potentiates the behavioral changes induced by the serotonin precursor, 5-hydroxytryptophan. Cardiac conduction effects of DESYREL (trazodone hydrochloride) in the anesthetized dog are qualitatively dissimilar and quantitatively less pronounced than those seen with tricyclic antidepressants. DESYREL (trazodone hydrochloride) is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system.

Pharmacokinetics

Absorption

In humans, DESYREL (trazodone hydrochloride) is well absorbed after oral administration without selective localization in any tissue. When DESYREL (trazodone hydrochloride) is taken shortly after ingestion of food, there may be an increase in the amount of drug absorbed, a decrease in maximum concentration and a lengthening in the time to maximum concentration. Peak plasma levels occur approximately one hour after dosing when DESYREL (trazodone hydrochloride) is taken on an empty stomach or two hours after dosing when taken with food.

Metabolism

In vitro studies in human liver microsomes show that trazodone is metabolized to an active metabolite, m-chlorophenylpiperazine (mCPP) by cytochrome P450 3A4 (CYP3A4). Other metabolic pathways that may be involved in metabolism of trazodone have not been well characterized.

Elimination

In some patients, DESYREL (trazodone hydrochloride) may accumulate in the plasma.

Drug-Drug Interactions

See also PRECAUTIONS: DRUG INTERACTIONS. In vitro drug metabolism studies reveal that trazodone is a substrate of the cytochrome P450 3A4 (CYP3A4) enzyme and trazodone metabolism can be inhibited by the CYP3A4 inhibitors ketoconazole, ritonavir, and indinavir. The effect of short-term administration of ritonavir (200 mg twice daily, 4 doses) on the pharmacokinetics of a single dose of trazodone (50 mg) has been studied in 10 healthy subjects. The Cmax of trazodone increased by 34%, the AUC increased 2.4-fold, the half-life increased by 2.2-fold, and the clearance decreased by 52%. Adverse effects including nausea, hypotension, and syncope were observed when ritonavir and trazodone were coadministered.

Carbamazepine induces CYP3A4. Following co-administration of carbamazepine 400 mg/day with trazodone 100 mg to 300 mg daily, carbamazepine reduced plasma concentrations of trazodone (as well as mCPP) by 76% and 60%, respectively, compared to pre-carbamazepine values.

For those patients who responded to DESYREL (trazodone hydrochloride) , one-third of the inpatients and one-half of the outpatients had a significant therapeutic response by the end of the first week of treatment. Three-fourths of all responders demonstrated a significant therapeutic effect by the end of the second week. One-fourth of responders required 2 to 4 weeks for a significant therapeutic response.

Last reviewed on RxList: 4/13/2011
This monograph has been modified to include the generic and brand name in many instances.