Pharmacokinetics, cardiovascular and metabolic actions of cyclohexylamine in man

Eichelbaum, Michel; Hengstmann, Jürgen H.; Rost, H. D.; Brecht, Th.; Dengler, H. J.

doi:10.1007/bf00311057

Cited by 20 publications

(2 citation statements)

References 24 publications

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“…These is exactly what would be predicted if you have a specific assay for the parent drug and have an active metabolite that is not detected or accounted for. More recent literature has demonstrated that levosimendan has two active metabolites OR-1896 and OR-1855 that have mean elimination half-lives of 72.6 and 81.3 hours, respectively, compared to the elimination half-life of parent drug that ranges between 1.1 to 1.4 hours [324]. …”

Section: Input Rate: Pharmaceutical Formulation Effects and The Direcmentioning

confidence: 99%

Understanding the Hysteresis Loop Conundrum in Pharmacokinetic / Pharmacodynamic Relationships

et al. 2014

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Hysteresis loops are phenomena that sometimes are encountered in the analysis of pharmacokinetic and pharmacodynamic relationships spanning from pre-clinical to clinical studies. When hysteresis occurs it provides insight into the complexity of drug action and disposition that can be encountered. Hysteresis loops suggest that the relationship between drug concentration and the effect being measured is not a simple direct relationship, but may have an inherent time delay and disequilibrium, which may be the result of metabolites, the consequence of changes in pharmacodynamics or the use of a non-specific assay or may involve an indirect relationship. Counter-clockwise hysteresis has been generally defined as the process in which effect can increase with time for a given drug concentration, while in the case of clockwise hysteresis the measured effect decreases with time for a given drug concentration. Hysteresis loops can occur as a consequence of a number of different pharmacokinetic and pharmacodynamic mechanisms including tolerance, distributional delay, feedback regulation, input and output rate changes, agonistic or antagonistic active metabolites, uptake into active site, slow receptor kinetics, delayed or modified activity, time-dependent protein binding and the use of racemic drugs among other factors. In this review, each of these various causes of hysteresis loops are discussed, with incorporation of relevant examples of drugs demonstrating these relationships for illustrative purposes. Furthermore, the effect that pharmaceutical formulation has on the occurrence and potential change in direction of the hysteresis loop, and the major pharmacokinetic / pharmacodynamic modeling approaches utilized to collapse and model hysteresis are detailed.

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Section: Input Rate: Pharmaceutical Formulation Effects and The Direcmentioning

confidence: 99%

Understanding the Hysteresis Loop Conundrum in Pharmacokinetic / Pharmacodynamic Relationships

et al. 2014

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“…[16] An early study has reported that ingestion of cyclohexylamine increased blood pressure and plasma free fatty acids, and that cyclohexylamine have a sympathomimetic capability. [17] Animal studies demonstrated that cyclohexylamine was deaminated to the corresponding ketones by microsomes in the rabbit liver. [18] Interestingly, metabolomics analysis in the present study could not detect cyclohexylamine at the baseline; however, cyclohexylamine increase was detected in several subjects after exercise.…”

Section: Discussionmentioning

confidence: 99%

The impact of exhaustive exercise on metabolic profiles in young men: a metabolomics approach

Akazawa¹,

Nakamura²,

Otomo³

2020

Preprint

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Background: Exercise-induced fatigue leads to reduction in the ability exert physical performance. Prolonged and intensive exercise stimulates several metabolic pathways to produce energy. The purpose of the present study was to investigate the impact of exhaustive exercise on metabolomic pathways. Methods: Nine young recreationally active men were recruited to this study. Participants performed step incremental maximal exercise until maximum exhaustion. Saliva samples were collected pre- and post-exercise (immediately after exercise cessation) using a salimetric oral swab, and salivary metabolites were analyzed using capillary electrophoresis and time-of-flight mass spectrometry. Results: Two hundred ten metabolites were detected, representing different clustering principle component structures between pre- and post-exercise. Orthogonal partial least squares discriminant analysis identified 29 metabolites with highly related variable importance for projection score and 16 metabolites significantly increased after exercise. Furthermore, increase in cyclohexylamine was positively correlated with an increase in fatigue on a visual analog scale. Conclusion: The present study demonstrated that exhaustive exercise changed the saliva metabolomic pathways related to energy production including glycolysis, lipolysis, amino acid metabolism, amines, and ketone bodies.

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Cyclohexylamin [MAK Value Documentation in German language, 2003]

2012

The MAK‐Collection for Occupational Health and Safety

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Veröffentlicht in der Reihe Gesundheitsschädliche Arbeitsstoffe , 36. Lieferung, Ausgabe 2003 Der Artikel enthält folgende Kapitel: Allgemeiner Wirkungscharakter Wirkungsmechanismus Toxikokinetik und Metabolismus Aufnahme, Verteilung, Ausscheidung Metabolismus Erfahrungen beim Menschen Einmalige Exposition Wiederholte Exposition Wirkung auf Haut und Schleimhäute Allergene Wirkung Reproduktionstoxizität Genotoxizität Kanzerogenität Tierexperimentelle Befunde und In‐vitro‐Untersuchungen Akute Toxizität Subakute, subchronische und chronische Toxizität Wirkung auf Haut und Schleimhäute Allergene Wirkung Reproduktionstoxizität Genotoxizität Kanzerogenität Bewertung

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Pharmacokinetics, cardiovascular and metabolic actions of cyclohexylamine in man

Cited by 20 publications

References 24 publications

Understanding the Hysteresis Loop Conundrum in Pharmacokinetic / Pharmacodynamic Relationships

Understanding the Hysteresis Loop Conundrum in Pharmacokinetic / Pharmacodynamic Relationships

The impact of exhaustive exercise on metabolic profiles in young men: a metabolomics approach

Cyclohexylamin [MAK Value Documentation in German language, 2003]

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