This study was designed to assess the plasma disposition kinetics of single oral 4-, 6-, and 8-mg doses of lacidipine, a new once-daily calcium-entry blocker. Seventeen healthy volunteers attended the study. In almost all cases, detectable levels were found up to 24 h after the drug administration, using a new HPLC-RIA assay. The usual pharmacokinetic parameters were calculated: Cmax, tmax, AUCinf, lambda z and t1/2. The half-life was similar after all doses, around 7 h, whereas Cmax and AUCinf did not show a linear correlation with the doses.
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http://dx.doi.org/10.1097/00005344-199423005-00020 | DOI Listing |
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Organ Transplantation, The Second Affiliated Hospital of Nanchang University, Minde Road No. 1, Nanchang, 330006, Jiangxi, China.
Multimorbidity, therapeutic complexity, and polypharmacy, which greatly increases the risk of drug-drug interactions (DDIs) and adverse medical outcomes, have become important and growing challenges in clinical practice. Statins are frequently prescribed to manage post-transplant dyslipidemia and reduce overall cardiovascular risk in solid organ transplant recipients. This study aimed to determine whether rosuvastatin has significant DDIs with tacrolimus (the first-line immunosuppressant) and to evaluate the risk of hepatotoxicity associated with concomitant therapy.
View Article and Find Full Text PDFPharmaceutics
January 2025
Department of Pharmaceutical Bioscience, Translational Drug Discovery and Development, Uppsala University, SE-75124 Uppsala, Sweden.
: N-acetyl-galactosamine small interfering RNAs (GalNAc-siRNA) are an emerging class of drugs due to their durable knockdown of disease-related proteins. Direct conjugation of GalNAc onto the siRNA enables targeted uptake into hepatocytes via GalNAc recognition of the Asialoglycoprotein Receptor (ASGPR). With a transient plasma exposure combined with a prolonged liver half-life, GalNAc-siRNA exhibits distinct disposition characteristics.
View Article and Find Full Text PDFClin Pharmacol Ther
January 2025
Novartis Pharmaceuticals Corporation, East Hanover, New Jersey, USA.
Iptacopan, a first-in-class complement factor B inhibitor acting proximally in the alternative complement pathway, has been shown to be safe and effective for patients with complement-mediated diseases. Iptacopan selectively binds with high affinity to factor B, a soluble, plasma-based, hepatically produced protein. Factor B is abundant in the circulation but can be saturated at the iptacopan clinical dose of 200 mg twice daily.
View Article and Find Full Text PDFEur J Pharm Sci
January 2025
Laboratory of Pharmacology, Faculty of Pharmacy, University of Coimbra, Portugal; CIBIT/ICNAS - Coimbra Institute for Biomedical Imaging and Translational Research, University of Coimbra, Portugal. Electronic address:
Zonisamide exhibits significant pharmacokinetic variability, demanding for the development of population pharmacokinetic (PopPK) models to identify key factors influencing drug disposition. This study aimed to develop and validate a PopPK to optimize zonisamide posology in patients with refractory epilepsy. A total of 114 plasma concentrations of zonisamide, obtained from 64 patients, were used for PopPK model development, employing the nonlinear mixed-effects modelling approach.
View Article and Find Full Text PDFAm J Vet Res
January 2025
Department of Large Animal Medicine and Surgery, College of Veterinary Medicine, University of Georgia, Athens, GA.
Objective: To investigate the disposition of enrofloxacin and its active metabolite, ciprofloxacin, in plasma, pulmonary epithelial lining fluid (PELF), peritoneal fluid, and CSF in horses following IV administration of enrofloxacin at doses of 5 mg/kg and 7.5 mg/kg of body weight.
Methods: 6 healthy, mature mares were randomly assigned to receive a single dose of enrofloxacin at either 5 mg/kg or 7.
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