219 surgical patients of either Caucasian, Chinese or Nepalese origin were given pethidine 1 mg/kg by intramuscular injection as pre-operative medication. Urine was collected for 24 h and analysed for pethidine, pethidinic acid, pethidinic acid conjugates, norpethidine, norpethidinic acid, and norpethidinic acid conjugates. The mean proportion of the percentage of metabolites attributable to oxidative demethylation, hydrolysis and conjugation was almost identical in each ethic group (P > 0.2). It was concluded that there were no differences in the metabolic variability of the biotransformation of pethidine in Asians and Caucasians in whom the urine pH had not been acidified.
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http://dx.doi.org/10.1007/BF03188810 | DOI Listing |
Exp Neurol
October 2024
Center for Transformative Research in Metabolism, Institute of Arctic Biology, University of Alaska Fairbanks, Fairbanks, AK, USA. Electronic address:
N-clyclohexyladenosine (CHA) is an adenosine A receptor agonist that inhibits thermogenesis. Cardiovascular side effects however, limit use of CHA as a therapeutic. We and others have shown that this can be reversed by administering 8-p-(sulfophenyl)theophylline (8-SPT), a nonspecific antagonist that does not cross the BBB.
View Article and Find Full Text PDFBiomed Pharmacother
September 2024
Department of Pharmacology, Faculty of Medicine, Erzincan Binali Yildirim University, Erzincan 24100, Turkey. Electronic address:
Pharmaceutics
February 2024
Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
Hepatic carboxylesterase 1 (CES1) metabolizes numerous prodrugs into active ingredients or direct-acting drugs into inactive metabolites. We aimed to develop a semi-physiologically based pharmacokinetic (semi-PBPK) model to simultaneously predict the pharmacokinetics of CES1 substrates and their active metabolites in liver cirrhosis (LC) patients. Six prodrugs (enalapril, benazepril, cilazapril, temocapril, perindopril and oseltamivir) and three direct-acting drugs (flumazenil, pethidine and remimazolam) were selected.
View Article and Find Full Text PDFCurr Drug Deliv
May 2024
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Until the drugs enter humans life, they may face problems in transportation, drug delivery, and metabolism. These problems can cause reducing drug's therapeutic effect and even increase its side effects. Together, these cases can reduce the patient's compliance with the treatment and complicate the treatment process.
View Article and Find Full Text PDFHeliyon
March 2022
Department of Burn, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, 200025, China.
Background: Browning of white adipose tissue is associated with elevated resting metabolic rates and is considered to be one of the indispensable causes of hypermetabolism in burn patients. Hypermetabolism means increased resting energy expenditure, raised body temperature and acute-phase proteins. Persistently elevated levels of circulating stress hormones have been reported to induce browning of subcutaneous white adipose tissue.
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