Monograph
N06AX05 - Trazodone |
Propably not porphyrinogenic |
PNP |
Rationale
Trazodone is a substrate of CYP 3A4, but has no inhibitory or inductive effects on CYP enzymes.
Chemical description
Trazodone is a serotonin uptake inhibitor.
Therapeutic characteristics
Trazodone is used in the management of depression and anxiety. It is administered orally. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in carbohydrate intake.
Metabolism and pharmacokinetics
Trazodone is metabolised in the liver where it undergoes N-oxidation and hydroxylation. It is metabolised to its active metabolite m-chlorophenylpiperazine via the cytochrome P450 isoenzyme CYP3A4. It is also a substrate of CYP 2D6 and CYP 1A2. Trazodone is mainly excreted in the urine in the form of its metabolites, either in free or in conjugated form. Some of the drug is excreted in the faeces via biliary elimination. There is no evidence to suggest that trazodone has potential for induction or inhibition of cyp-enzymes.
Published experience
Uneventful use reported by Holroyd (1999).
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Psychotropic drugs in acute intermittent porphyria.
Holroyd S, Seward RL, et al. Clin Pharmacol Ther. 1999 Sep;66(3):323-5. |
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| 2. | Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources.
Rotzinger S, Fang J, et al. Drug Metab Dispos. 1998 Jun;26(6):572-5. |
9616194 |
| * | Drug reference publications | |
| 3. | DrugBank. Trazodone.
|
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| 4. | Sweetman SC, editor. Martindale: The complete drug reference. Trazodone
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| * | Summary of Product Characteristics | |
| 5. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Molipaxin.
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