ChemInform Abstract: NITRENDIPINE: IDENTIFICATION AND SYNTHESIS OF MAIN METABOLITES

Meyer, H.; Scherling, D.; Karl, Wolfgang

doi:10.1002/chin.198414226

Cited by 8 publications

(13 citation statements)

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“…On the other hand, the primary oxidation product M4 and the 1,4-dihydropyridines M2 and M3 with hydrolytically cleaved ester side chains were observed as minor metabolites (table IV). The prevalence of metabolites with oxidised dihydropyridine nucleus is agreement with findings published for other dihydropyridines (Kobayashi and Kobayashi 1998, Meyer et al 1983, Scherling et al1988and 1991, Takayama et al 1989, Terashita et al 1987). …”

Section: Discussionsupporting

confidence: 81%

Urinary excretion of the 1,4-dihydropyridine calcium antagonist VULM 993 and its metabolites in the rat

Štefek

Faberova

Musil

et al. 2001

Eur. J. Drug Metab. Pharmacokinet.

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After oral dose of the 1,4-dihydropyridine calcium antagonist 14C-VULM 993 (50 mg/kg) a mean of 44.5% of the administered radioactivity was excreted via urine during the first 72 hours. Using an extractive fractionation procedure, the urinary metabolites were classified on the basis of their polarity and acidic/basic properties. Approx. 40% of total urine metabolites were found to be polar, non-extractable compounds--mostly glucuronide/sulphate conjucates. About one half of all urine metabolites were shown to possess overall acidic nature. G.l.c.-m.s. and t.l.c.-m.s. analyses of urine extracts revealed the presence of only minor amounts of the parent drug toghether with six metabolites identified as products of 1,4-dioxaspiro[4,4]nonane moiety cleavage, hydrolysis of one or both ester side functions also combined with 1,4-dihydropiridine nucleus dehydrogenation. Technique of thin-layer radio-chromatography was used to quantify urinary excretion rates of the parent drug and the established metabolites.

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Section: Discussionsupporting

confidence: 81%

Urinary excretion of the 1,4-dihydropyridine calcium antagonist VULM 993 and its metabolites in the rat

Štefek

Faberova

Musil

et al. 2001

Eur. J. Drug Metab. Pharmacokinet.

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“…10) which can be removed from the parent drug (M II) and from its pyridine analog (M III) [13]. Further hydrolysis and hydroxylation yields M V. In human urine, low concentrations of other metabo lites may be present, some of them have already been identified in rats treated with l4C-labeled NT [14] and NM [15]. Urinary excretion of NF.…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics and Metabolism of Calcium-Blocking Agents Nifedipine, Nitrendipine, and Nimodipine

et al. 1986

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“…NIT and nifedipine (NIF) were purchased from the National Institute for the Control of Pharmaceutical and Biological Products (Beijing, China). The reference substance of DNIT was prepared according to the reported method (Meyer et al, 1983). Its purity (99.5%) was determined by HPLC/UV and LC/MS methods.…”

Section: Methodsmentioning

confidence: 99%

“…It undergoes extensive first-pass metabolism, resulting in low bioavailability and wide interindividual variability in pharmacokinetics (Krol et al, 1987;Mikus et al, 1987). NIT is predominantly metabolized by an oxidative mechanism to the pharmacologically inactive pyridine metabolite dehydronitrendipine (DNIT; Meyer et al, 1983).…”

Section: Introductionmentioning

confidence: 99%

Quantitative determination of nitrendipine and its metabolite dehydronitrendipine in human plasma using liquid chromatography–tandem mass spectrometry

Chen

Zhong

Huang

et al. 2001

Biomedical Chromatography

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A sensitive and high-throughput LC-MS-MS method was developed for simultaneous determination of nitrendipine (NIT) and its major metabolite, dehydronitrendipine (DNIT) in human plasma using nifedipine as the internal standard. Plasma samples were prepared based on a simple liquid-liquid extraction. The extracted samples were analyzed on a Zorbax SB C(18) column interfaced with a triple quadrupole tandem mass spectrometer. Positive atmospheric pressure chemical ionization was employed as the ionization source. The analytes were detected by use of selected reaction monitoring mode. Standard curves were linear (r > or = 0.995) over the concentration range of 0.4-40 ng/mL for NIT and 0.2-20 ng/mL for DNIT. The intra- and inter-run precision was measured to be below 8.5% for NIT and DNIT. The inter-run accuracy was less than 4% for the analytes. The overall extraction recoveries of NIT and DNIT were determined to be about 75% and 78% on average, respectively. The chromatographic run time was approximately 3 min. More than 120 samples could be assayed daily with this method, including sample preparation, data acquisition and processing. The method developed was successfully used to investigate plasma concentrations of NIT and DNIT in a pharmacokinetic study of volunteers who received NIT orally.

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ChemInform Abstract: NITRENDIPINE: IDENTIFICATION AND SYNTHESIS OF MAIN METABOLITES

Abstract: Von dem Nitren‐ dipin (Ia) werden die Strukturen der Hauptmetaboliten (IIa)‐(IIc) sowie (IIIa) bis (IIIc) durch geeignete Synthesen oder durch spektroskopischen Vergleich mit den Referenzsubstanzen (VII), (VIII) und (Xa) und (Xb) aufgeklärt.

Cited by 8 publications

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Urinary excretion of the 1,4-dihydropyridine calcium antagonist VULM 993 and its metabolites in the rat

Urinary excretion of the 1,4-dihydropyridine calcium antagonist VULM 993 and its metabolites in the rat

Pharmacokinetics and Metabolism of Calcium-Blocking Agents Nifedipine, Nitrendipine, and Nimodipine

Quantitative determination of nitrendipine and its metabolite dehydronitrendipine in human plasma using liquid chromatography–tandem mass spectrometry

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