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100 MCQs from Dr. Guy Molyneaux and Colleagues
Published in David Browne, Selena Morgan Pillay, Guy Molyneaux, Brenda Wright, Bangaru Raju, Ijaz Hussein, Mohamed Ali Ahmed, Michael Reilly, MCQs for the New MRCPsych Paper A, 2017
Dr Pauline Devitt, Dr Angela Noonan, Dr Klaus Oliver Schubert, Prof Finian O’Brien
Sertraline has no known active metabolites. Citalopram and amitriptyline have several active metabolites, including desmethylcitalopram and nortriptyline respectively; fluoxetine metabolises to norfluoxetine and mirtazapine metabolises to desmethylmirtazapine. (7)
Antidepressants in pregnant and breastfeeding women
Published in Kathleen A. Kendall-Tackett, Depression in New Mothers, 2016
Escitalopram, as a newer antidepressant, was not included in the Weissman et al. review, but it too has a favorable profile for breastfeeding mothers. A recent study examined the transfer of escitalopram and its metabolite into breast milk from eight women who were taking escitalopram for postpartum depression (Rampono et al., 2006). Mothers had been taking the medication for an average of 55 days. The total relative infant dose for escitalopram and its metabolite was 5.3 percent of the maternal weight-adjusted dose (3.9 percent for escitalopram; 1.7 percent for desmethylescitalopram). The levels were undetectable in four infants, and at very low levels in two others. Based on the infant dose calculations, the authors concluded that escitalopram is preferred to citalopram for the treatment of depression during breastfeeding, and is safe for breastfeeding women.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Citalopram, an SSRI used to treat major depression associated with mood disorders, is converted to N-desmethylcitalopram (N-norcitalopram) and then to N,N- didesmethylcitalopram and citalopram N-oxide (Rao 2007). Citalopram is sold as a racemic mixture, while escitalopram is the S-enantiomer of the racemic citalopram, which has been marketed as a drug as only the S-enantiomer has the desired antidepressant effect (Hyttel et al. 1992). Clinical studies have demonstrated that steady-state concentrations of R-citalopram exceed those of S-citalopram during chronic administration of racemic citalopram to humans and that the elimination half-life of R-citalopram exceeds that of S-citalopram (Bondolfi et al. 1996; Foglia et al. 1997; Rochat et al. 1995). CYP3A4, 2C19, and 2D6 are involved in the first demethylation step of citalopram, all favoring conversion of the biologically active S-enantiomer (escitalopram) (Figure 3.10) (Olesen and Linnet 1999; von Moltke et al. 2001). The approximate relative contribution at low substrate concentrations is estimated to be 34% by CYP3A4, 36% by 2C19, and 30% by 2D6 (von Moltke et al. 2001). Inhibitor studies indicated that CYP3A4 is responsible for 40%-50% of N-desmethylcitalopram formation at therapeutic citalopram concentrations, while the contribution of CYP2C19 increases and that of 2D6 tends to decrease with increasing drug concentration. CYP2D6 exclusively catalyzes the second demethylation step, and citalopram N-oxide is also exclusively formed by CYP2D6 (Olesen and Linnet 1999). However, none of the studied CYP enzymes mediates deami-nation to the propionic acid derivative.
Clinical insights gained through metabolomic analysis of human breast milk
Published in Expert Review of Proteomics, 2019
Flaminia Bardanzellu, Chiara Peila, Vassilios Fanos, Alessandra Coscia
Another group validated HPLC coupled to electrospray mass spectrometry (HPLC-ESI-MS) to detect BM levels of selective serotonin reuptake inhibitors-SSRI (citalopram, fluoxetine, fluvoxamine, paroxetine and sertraline and their major metabolites desmethylcitalopram and norfluoxetine) [92]. In mothers affected by postpartum depressive symptoms, or previously treated and continuing drug administration during lactation, these drugs may pass through breastfeeding and negatively affect neonatal outcome.