Cholestase nach antiarrhythmischer Therapie mit Propafenon

Konz, Karl‐Heinz; Berg, Paul; Seipel, L

doi:10.1055/s-2008-1069406

Cited by 11 publications

(4 citation statements)

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“…It is a beta-adrenergic blocker that causes bradycardia and bronchospasm (Siddoway et al, 1984) . The major metabolic process for propafenone occurs in the liver (Konz et al, 2008;Schlepper, 1987). The bioavailability and plasma concentration for propafenone In the APRBT sample, the ethyl acetate fraction showed 12 peaks, indicating certain compounds in the fraction.…”

Section: Figure 4 Lcms/ms Chromatogram Of Aprbt Honey Extractsmentioning

confidence: 99%

Identification of Active Chemical Compounds of Honey from Some Regions in Indonesia

Sumarlin

Enita

Afandi

et al. 2021

sci. technol. indones.

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Bees produce honey from plant nectar, plant secretions, and excretions of plant-sucking insects. Indonesian local honey contains active compounds that have the potential effect as antioxidant and anticancer. The composition and biological effects of honey vary depending on the flower sources; seasonal and environmental factors can also influence the composition and the physical products. This research was conducted to identify the chemical compounds found in several honey samples produced by beekeepers in Indonesia with LCMS/MS method and to determine the profiles of the honey from Indonesia with the Chemspider and MassBank Database. Honey samples were collected from several regions in Indonesia. The results of the analysis showed that the honey’s diastase number vary from region to region and showed that the HMF contents are relatively low. The compounds that were allegedly found through LCMS/MS analysis include and have been traced based on literature studies had bioactive activity and beneficial to health, include: millefin (potential for treating heart disease and cancer), mangiferin (anti-inflammatory, anti-diabetes, immunomodulators, anti-tumor, antioxidants), rhamnetin (anti-inflammatory), tricin (antioxidant-like), acacetin (inhibit tumor angiogenesis agents), aurantiamide acetate (antiviral or anti-inflammatory, therapeutic agent for the treatment of influenza), salvigenin (controlling inflammation, acute and chronic pain), brucine (modulates anti-inflammatory and analgesic properties), dehydrocostus lactone (anti-inflammatory), santonin (anthelmintic activity), dimethylesculetin (bilirubin clearance), imidazole 4- acetic acid (neuropharmacological properties), propafenone (antiarrhythmic), yohimbine (affected sexual performance), Velutin (anti-inflammatory), narigenin (linked to cardiovascular disease protection). Eventually, honey is is such a natural product with a number of salient therapeutic properties. However, there are still components that were found but their roles cannot be described in detail. Therefore, it is recommended that further meticulous studies should bring to light the other hidden properties of the honey compounds.

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Section: Figure 4 Lcms/ms Chromatogram Of Aprbt Honey Extractsmentioning

confidence: 99%

Identification of Active Chemical Compounds of Honey from Some Regions in Indonesia

Sumarlin

Enita

Afandi

et al. 2021

sci. technol. indones.

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“…One case of acute PPF poisoning was reported in a patient who had received only a low dose of PPF. , Hepatotoxicity due to this drug is 0.1–0.2%, and advanced age and a history of myocardial infarction can increase the risk of PPF side effects. Clinical manifestations include acute cholestasis or hepatocyte necrosis. , The underlying mechanism involved in the development of its hepatotoxicity remains unclear. The hypersensitivity or specific toxicity induced by PPF metabolites is possible.…”

Section: Introductionmentioning

confidence: 99%

“…Clinical manifestations include acute cholestasis or hepatocyte necrosis. 8,9 The underlying mechanism involved in the development of its hepatotoxicity remains unclear. The hypersensitivity or specific toxicity induced by PPF metabolites is possible.…”

Section: ■ Introductionmentioning

confidence: 99%

Metabolic Activation and Cytotoxicity of Propafenone Mediated by CYP2D6

Shi

Chen

et al. 2022

Chem. Res. Toxicol.

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Propafenone (PPF) is a class IC antidysrhythmic drug, which is commonly used for the treatment of atrial fibrillation and other supraventricular arrhythmias. It is also a β-adrenoceptor antagonist that can cause bradycardia and bronchospasm. Hepatotoxicity is one of the adverse reactions reported, with clinical manifestations including acute cholestasis and hepatocyte necrosis. However, the mechanism of PPF-induced hepatotoxicity remains unclear. The present study was conducted to identify reactive metabolite(s) to determine related metabolic pathways and define the possible association of the bioactivation with PPF cytotoxicity. An O-demethylation phase I metabolite (M1), a further position C5 hydroxylation (para-position of the benzene ring) metabolite (M2), glutathione (GSH) conjugates (M3 and M4), and N-acetylcysteine (NAC) conjugates (M5 and M6) were detected in rat liver microsomal incubations containing PPF and GSH or NAC as trapping agents. The corresponding GSH conjugates and NAC conjugates were found in the bile and urine of rats after PPF administration, respectively. The observed GSH and NAC conjugates indicate that a quinone metabolite was generated in vitro and in vivo. Recombinant P450 enzyme incubations showed that CYP2D6 was the principal enzyme catalyzing this metabolic activation. Quinidine, a selective inhibitor of CYP2D6, attenuated the susceptibility of hepatocytes to the cytotoxicity of PPF. The results suggest that PPF was metabolized to a p-quinone intermediate which may be involved in PPF-induced hepatotoxicity.

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“…[2] It is metabolized primarily in the liver. [34] Its bioavailability and plasma concentration differ among patients under long-term therapy. They are genetically determined by the hepatic cytochrome P-450 2D6.…”

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confidence: 99%

Propafenone hepatotoxicity: Report of a new case and review of the literature

Younan

Barada

Faraj

et al. 2013

Saudi J Gastroenterol

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Propafenone is a class Ic antiarrhythmic drug. It is a beta-adrenergic blocker that causes bradycardia and bronchospasm. It is metabolized primarily in the liver. Its bioavailability and plasma concentration differ among patients under long-term therapy. They are genetically determined by the hepatic cytochrome P-450 2D6. Hepatic toxicity is highly uncommon. To date, only eight patients were reported in the reviewed world literature. In this article, one new case will be reported emphasizing the importance of medication history taking in patients presenting with new-onset liver enzymes abnormalities.

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Cholestase nach antiarrhythmischer Therapie mit Propafenon

Cited by 11 publications

References 0 publications

Identification of Active Chemical Compounds of Honey from Some Regions in Indonesia

Identification of Active Chemical Compounds of Honey from Some Regions in Indonesia

Metabolic Activation and Cytotoxicity of Propafenone Mediated by CYP2D6

Propafenone hepatotoxicity: Report of a new case and review of the literature

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