CYP2D6 inhibition in patients treated with sertraline.
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Sproule BA, Otton SV, Cheung SW, Zhong XH, Romach MK, Sellers EM
CYP2D6 inhibition in patients treated with sertraline.
J Clin Psychopharmacol. 1997 Apr;17(2):102-6. doi: 10.1097/00004714-199704000-00007.
- PubMed ID
- 10950472 [ View in PubMed]
- Abstract
Sertraline, a selective serotonin reuptake inhibitor used to treat depression, inhibits CYP2D6 in vitro (Ki = 1.2 microM) less potently than fluoxetine (Ki = 0.15 microM). To determine the extent and time course of CYP2D6 inhibition in patients, six males (mean age: 40 years, range: 29-64 years), who were starting treatment for depression with sertraline, were phenotyped on five occasions (once before treatment and approximately 3, 7, 14, and 21 days later). Phenotype status was determined using oral dextromethorphan (30 mg) by calculating the urinary ratio of O-demethylated metabolites to parent drug (i.e., log ODMR). CYP2D6 genotype was determined by leukocyte DNA analysis using polymerase chain reaction amplification. Compliance was confirmed by sertraline plasma levels. Daily sertraline dosages ranged from 50 to 150 mg. Genotype results indicated all subjects were extensive metabolizers (four homozygous wild type [wt], two heterozygous wt/B mutation). Phenotype results showed that CYP2D6 inhibition in patients treated with sertraline appeared to be related to baseline CYP2D6 activity and sertraline dosage. Some patients with high CYP2D6 activity can demonstrate inhibition with sertraline dosages as low as 50 mg.
DrugBank Data that Cites this Article
- Drug Reactions
Reaction Details - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareAripiprazoleSertraline The serum concentration of Aripiprazole can be increased when it is combined with Sertraline. Aripiprazole lauroxilSertraline The serum concentration of Aripiprazole lauroxil can be increased when it is combined with Sertraline.
