Prediction of interindividual variation in drug plasma levels in vivo from individual enzyme kinetic data and physiologically based pharmacokinetic modeling

Bogaards, J.J.P.; Hissink, Erna M.; Briggs, Mike; Weaver, Richard J.; Jochemsen, R.; Jackson, Peter F.; Bertrand, Marc; Bladeren, P.J. van

doi:10.1016/s0928-0987(00)00146-9

Cited by 43 publications

(24 citation statements)

References 15 publications

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“…This is a consideration mainly for risk policy and depends on the precaution and safety desired with respect to evidence. Bogaards et al (2000) have likewise shown that the inter-individual variation in liver EROD and Cyp1a2 activity is 20-fold (see below). Also found much interindividual variation in AHH and EROD induction by DLCs in a highly exposed Taiwanese population.…”

Section: Inter-individual and Inter-population Variationmentioning

confidence: 78%

Risks and Management of Dioxins and Dioxin-like Compounds in Baltic Sea Fish: An Integrated Assessment

2006

TemaNord

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Section: Inter-individual and Inter-population Variationmentioning

confidence: 78%

Risks and Management of Dioxins and Dioxin-like Compounds in Baltic Sea Fish: An Integrated Assessment

2006

TemaNord

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“…It is absorbed rapidly by the oral route and is metabolized in the liver by three CYP isoenzymes, namely CYPA1, CYPA2 and CYP2C9. Three agomelatine metabolites (3-hydroxy S20098, 3-hydroxy-7-methoxy S20098 and 7-desmethyl S20098) have been identified [77].…”

Section: Agomelatine: a Novel Melatonergic Antidepressantmentioning

confidence: 99%

Therapeutic potential of melatonin agonists

Cardinali¹,

Pandi-Perumal

Srinivasan

et al. 2008

Expert Review of Endocrinology & Metabolism

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Melatonin, a hormone secreted by the pineal gland, has been successfully employed to improve sleep in both normal patients and insomniacs, and for the treatment of circadian rhythm sleep disorders. Melatonergic MT 1 and MT 2 receptors exist in high concentrations in the suprachiasmatic nucleus of the hypothalamus and have been shown to be instrumental for the sleep-promoting and circadian rhythm-regulating effects of melatonin. A lack of consistency among reports on the therapeutic efficacy of melatonin has been attributed to differences in melatonin's bioavailability and the short half-life of the hormone. In view of the need for longer acting melatonergic agonists that improve sleep efficiency without causing drug abuse or dependency, ramelteon (Rozerem™, Takeda) was developed. Ramelteon, which acts via MT 1 /MT 2 melatonergic agonism, has been found clinically effective for improving total sleep time and sleep efficiency in insomniacs. Agomelatine (Valdoxan™, Servier) is another MT 1 /MT 2 melatonergic agonist that also displays antagonist activity at 5-HT 2C serotonin receptors. Agomelatine has been found effective in treating depression and sleep disorders in patients with major depressive disorder. A slow-release preparation of melatonin (Circadin™, Neurim) has been shown to be effective in treating sleep disorders in the elderly population.

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“…Plasma concentrations after ingestion of 30 Á 120 mg agomelatine reach their maximum after about 30 min (Bogaards et al 2000). The plasma protein binding ranges from 75 to 95% (Le Quellec et al, 1994).…”

Section: Melatonin and Agonistic And Selective Serotonin Antagonisticmentioning

confidence: 99%

“…The plasma protein binding ranges from 75 to 95% (Le Quellec et al, 1994). Its metabolism is mediated predominantly by cytochrome P450 CYP1A2, CYP2C9 and, to a far lesser extent, by CYP1A1 (Bogaards et al 2000).…”

Section: Melatonin and Agonistic And Selective Serotonin Antagonisticmentioning

confidence: 99%

Drug treatment of depression in the 2000s: an overview of achievements in the last 10 years and future possibilities

Baghai

Volz²,

Möller³

2006

The World Journal of Biological Psychiatry

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During the past 10 years our knowledge about the pharmacotherapy of depression has been consolidated, and a variety of very interesting new compounds launched onto the market. The pipeline of the pharmaceutical industry is still filled with an assortment of new developments and very promising new approaches towards the pharmacotherapy of depressive disorders. Future pharmacological treatments of depression will not only enhance serotonergic and noradrenergic neurotransmission: other systems, such as the melatonergic receptor system and the hypothalamus-pituitary-adrenal axis, are also the targets of newly developed and upcoming substances with putative antidepressant effects. The main advantages of the currently available newer pharmacotherapeutic options are the broadening of the spectrum of possible antidepressant treatments, which is of particular importance for the growing number of patients suffering from difficult-to-treat depression, and a far better tolerability profile in comparison to older compounds such as tricyclic antidepressants. Unresolved issues are the unacceptably high rate of non-responsiveness during antidepressant treatment, a latency of sometimes several weeks until clinical improvement and remission can be achieved, and a variety of possible side effects also present during treatment with modern compounds. This review mainly presents the development of antidepressant pharmacotherapies during the past 10 years, together with pharmacokinetic and pharmacodynamic information and a comparison of different pharmacological treatment principles evaluated in randomized controlled clinical trials. In addition, new pharmacological strategies that are not yet available on the market and strategies currently under development are reviewed in detail. The study of new treatment options is of major importance to provide better strategies for the clinical management of depression in the future, and is thus also of great socio-economic importance.

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Prediction of interindividual variation in drug plasma levels in vivo from individual enzyme kinetic data and physiologically based pharmacokinetic modeling

Cited by 43 publications

References 15 publications

Risks and Management of Dioxins and Dioxin-like Compounds in Baltic Sea Fish: An Integrated Assessment

Risks and Management of Dioxins and Dioxin-like Compounds in Baltic Sea Fish: An Integrated Assessment

Therapeutic potential of melatonin agonists

Drug treatment of depression in the 2000s: an overview of achievements in the last 10 years and future possibilities

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