Clinical Pharmacokinetics of Imipramine and Desipramine

@article{Sallee1990ClinicalPO,
  title={Clinical Pharmacokinetics of Imipramine and Desipramine},
  author={Floyd R. Sallee and B. G. Pollock},
  journal={Clinical Pharmacokinetics},
  year={1990},
  volume={18},
  pages={346-364}
}
  • F. Sallee, B. Pollock
  • Published 1 May 1990
  • Medicine, Biology, Psychology
  • Clinical Pharmacokinetics
SummaryThe pharmacokinetics of Imipramine and desipramine have been extensively investigated with recent studies designed to understand sources of intersubject variability and to study discrete clinical populations rather than healthy volunteers. Sources of intersubject variability in pharmacokinetics are both genetic (oxidative phenotype) and environmental. Oxidative phenotype has an important impact on first-pass metabolism. In individuals with poor metabolism, systemic availability for… 
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Highly Influential Citations
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Background Citations
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104 Citations

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Clomipramine, like the other tricyclics, is an antidepressant with a fairly narrow therapeutic range, combined with a high interindividual variability, makes this class of drugs ideal candidates for blood concentration monitoring.
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The semi-mechanistic population model developed is suitable to describe the pharmacokinetic behaviour of desipramine for the dose routinely used in drug-drug interaction (DDI) studies and a sample size of 21 subjects in cross-over design is appropriate for assessing CYP2D6 interaction with novel compounds.
Steady-state plasma concentrations of imipramine and desipramine in relation to S-mephenytoin 4'-hydroxylation status in Japanese depressive patients.
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The individually predetermined assessment of the CYP2C19-mediated metabolic capacity of imipramine would be more valuable than that of the CyP2D6-mediated capacity for forecasting the steady-state concentrations of im ipramine and desipramines in Japanese depressive patients, thereby attaining an individualized optimization of imIPramine therapy.
The Use of In Vitro Data and Physiologically-Based Pharmacokinetic Modeling to Predict Drug Metabolite Exposure: Desipramine Exposure in Cytochrome P4502D6 Extensive and Poor Metabolizers Following Administration of Imipramine
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This example suggested that mechanistic PBPK modeling combined with information obtained from in vitro studies can provide quantitative solutions to predict in vivo pharmacokinetics of drugs and major metabolites in a target human population.
Imipramine and 2-hydroxyimipramine: comparative cardiotoxicity and pharmacokinetics in swine
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It is concluded that 2-OH-IMI has increased penetrance into the CNS despite a smaller Vd and that it is significantly more cardiotoxic than its parent.
Effect of Terbinafine on the Pharmacokinetics and Pharmacodynamics of Desipramine in Healthy Volunteers Identified as Cytochrome P450 2D6 (CYP2D6) Extensive Metabolizers
Terbinafine‐CYP2D6 inhibition was evaluated by assessing 48‐hour concentration‐time profiles of the tricyclic antidepressant desipramine in 12 healthy volunteers identified as extensive cytochrome…
Development and Qualification of Physiologically Based Pharmacokinetic Models for Drugs With Atypical Distribution Behavior: A Desipramine Case Study
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A physiologically based pharmacokinetic (PBPK) model is developed and qualified for desipramine, which accounts for the high Vss of the drug following intravenous and oral administration of doses up to 100 mg and the extended time to reach maximum concentration after oral dosing due to enterocyte trapping.
The Effects of Desvenlafaxine and Paroxetine on the Pharmacokinetics of the Cytochrome P450 2D6 Substrate Desipramine in Healthy Adults
TLDR
Desvenlafaxine, especially at the recommended therapeutic dose of 50 mg/d for major depressive disorder in the United States, has little potential to interact with CYP2D6 substrates.
Pilot study of plasma concentrations of mosapramine, a new iminodibenzyl antipsychotic agent, after multiple oral administration in schizophrenic patients
Pharmacokinetics of the newer antidepressants: clinical relevance.
  • C. DeVane
  • Medicine, Biology
    The American journal of medicine
  • 1994
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