Modeled Hepatic/Plasma Exposures of Fluvastatin Prescribed Alone in Subjects with Impaired Cytochrome P450 2C9*3 as One of Possible Determinant Factors Likely Associated with Hepatic Toxicity Reported in a Japanese Adverse Event Database
Biol Pharm Bull. 2024;47(3):635-640. doi: 10.1248/bpb.b24-00012.ABSTRACTFluvastatin is a 3-hydroxy-3-methylglutaryl CoA reductase inhibitor that competitively inhibits human cytochrome P450 (P450) 2C9 in vitro. Drug interactions between a variety of P450 2C9 substrates/inhibitors and fluvastatin can increase the incidence of fluvastatin-related hepatic or skeletal muscle toxicity in vivo. In this survey, the prescribed dosage of fluvastatin was reduced or discontinued in 133 of 164 patients receiving fluvastatin alone, as recorded in the Japanese Adverse Drug Event Report database of spontaneously reported events. The medi...
Source: Biological and Pharmaceutical Bulletin - March 18, 2024 Category: Drugs & Pharmacology Authors: Koichiro Adachi Katsuhiro Ohyama Yoichi Tanaka Yoshiro Saito Makiko Shimizu Hiroshi Yamazaki Source Type: research
Modeled Hepatic/Plasma Exposures of Fluvastatin Prescribed Alone in Subjects with Impaired Cytochrome P450 2C9*3 as One of Possible Determinant Factors Likely Associated with Hepatic Toxicity Reported in a Japanese Adverse Event Database
Biol Pharm Bull. 2024;47(3):635-640. doi: 10.1248/bpb.b24-00012.ABSTRACTFluvastatin is a 3-hydroxy-3-methylglutaryl CoA reductase inhibitor that competitively inhibits human cytochrome P450 (P450) 2C9 in vitro. Drug interactions between a variety of P450 2C9 substrates/inhibitors and fluvastatin can increase the incidence of fluvastatin-related hepatic or skeletal muscle toxicity in vivo. In this survey, the prescribed dosage of fluvastatin was reduced or discontinued in 133 of 164 patients receiving fluvastatin alone, as recorded in the Japanese Adverse Drug Event Report database of spontaneously reported events. The medi...
Source: Biological and Pharmaceutical Bulletin - March 18, 2024 Category: Drugs & Pharmacology Authors: Koichiro Adachi Katsuhiro Ohyama Yoichi Tanaka Yoshiro Saito Makiko Shimizu Hiroshi Yamazaki Source Type: research
Modeled Hepatic/Plasma Exposures of Fluvastatin Prescribed Alone in Subjects with Impaired Cytochrome P450 2C9*3 as One of Possible Determinant Factors Likely Associated with Hepatic Toxicity Reported in a Japanese Adverse Event Database
Biol Pharm Bull. 2024;47(3):635-640. doi: 10.1248/bpb.b24-00012.ABSTRACTFluvastatin is a 3-hydroxy-3-methylglutaryl CoA reductase inhibitor that competitively inhibits human cytochrome P450 (P450) 2C9 in vitro. Drug interactions between a variety of P450 2C9 substrates/inhibitors and fluvastatin can increase the incidence of fluvastatin-related hepatic or skeletal muscle toxicity in vivo. In this survey, the prescribed dosage of fluvastatin was reduced or discontinued in 133 of 164 patients receiving fluvastatin alone, as recorded in the Japanese Adverse Drug Event Report database of spontaneously reported events. The medi...
Source: Biological and Pharmaceutical Bulletin - March 18, 2024 Category: Drugs & Pharmacology Authors: Koichiro Adachi Katsuhiro Ohyama Yoichi Tanaka Yoshiro Saito Makiko Shimizu Hiroshi Yamazaki Source Type: research
Conversion of Olmesartan to Olmesartan Medoxomil, A Prodrug that Improves Intestinal Absorption, Confers Substrate Recognition by OATP2B1
CONCLUSION: Olmesartan-MX is a substrate for OATP2B1, and the naringin-sensitive transport system contributes to the improved intestinal absorption of olmesartan-MX compared with its parent drug, olmesartan.PMID:38485855 | DOI:10.1007/s11095-024-03687-1 (Source: Cell Research)
Source: Cell Research - March 15, 2024 Category: Cytology Authors: Naomi Fukazawa Tomohiro Nishimura Keisuke Orii Saki Noguchi Masatoshi Tomi Source Type: research
Conversion of Olmesartan to Olmesartan Medoxomil, A Prodrug that Improves Intestinal Absorption, Confers Substrate Recognition by OATP2B1
ConclusionOlmesartan-MX is a substrate for OATP2B1, and the naringin-sensitive transport system contributes to the improved intestinal absorption of olmesartan-MX compared with its parent drug, olmesartan. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - March 14, 2024 Category: Drugs & Pharmacology Source Type: research
Utilizing Pharmacogenomic Data for a Safer Use of Statins among the Emirati Population
CONCLUSION: Among the sparse studies available, the present one demonstrates all SLCO1B1 and CYP2C9 function-impairing alleles among Emiratis. We highlighted how population-specific pharmacogenomic data can predict safer choices of statins, especially in understudied populations.PMID:38284696 | DOI:10.2174/0115701611283841231227064343 (Source: Current Vascular Pharmacology)
Source: Current Vascular Pharmacology - January 29, 2024 Category: Drugs & Pharmacology Authors: Mais N Alqasrawi Zeina N Al-Mahayri Hiba Alblooshi Habiba Alsafar Bassam R Ali Source Type: research
Statin-related neurocognitive disorder: a real-world pharmacovigilance study based on the FDA adverse event reporting system
CONCLUSIONS: This study suggests a significant association between the NCDE and statins, including atorvastatin, simvastatin, and pravastatin. The intensity of the association increased with age.PMID:38275183 | DOI:10.1080/17512433.2024.2311875 (Source: Expert Review of Clinical Pharmacology)
Source: Expert Review of Clinical Pharmacology - January 26, 2024 Category: Drugs & Pharmacology Authors: Min Xiao Li Li Weiwei Zhu Fengbo Wu Bin Wu Source Type: research
Genetic Determinants of Response to Statins in Cardiovascular Diseases
Curr Cardiol Rev. 2024 Jan 9. doi: 10.2174/011573403X267793231220114042. Online ahead of print.ABSTRACTDespite extensive efforts to identify patients with cardiovascular disease (CVD) who could most benefit from the treatment approach, patients vary in their benefit from therapy and propensity for adverse drug events. Genetic variability in individual responses to drugs (pharmacogenetics) is considered an essential determinant in responding to a drug. Thus, understanding these pharmacogenomic relationships has led to a substantial focus on mechanisms of disease and drug response. In turn, understanding the genomic and mole...
Source: Current Cardiology Reviews - January 11, 2024 Category: Cardiology Authors: Ghazaleh Ghorbannezhad Shima Mehrabadi Negar Golampour-Shamkani Amirhossein Barjasteh Poorya Etesamizadeh Mohammad Tayyebi Majid Khazaei Seyed Mahdi Hassanian Gordon A Ferns Amir Avan Source Type: research
Uptake of Fluorescein via a pH-Dependent Monocarboxylate Transporter by Human Kidney 2 (HK-2) Cells
Biol Pharm Bull. 2024;47(1):79-87. doi: 10.1248/bpb.b23-00570.ABSTRACTHerein, we investigated whether a fluorescent probe for an organic anion transporter (OAT), fluorescein (FLS), could be accumulated by human kidney 2 (HK-2) cells derived from human kidney proximal tubular epithelia. HK-2 cells took up FLS in a pH-dependent and concentration-dependent manner. FLS accumulation by HK-2 cells was inhibited by monocarboxylic acids, ibuprofen, rosuvastatin, and indoleacetic acid but not by typical substrates for OATs. A typical protonophore, carbonyl cyanide p-trichloromethoxyphenylhydrazone completely abolished FLS accumulat...
Source: Biological and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takaharu Takiguchi Kazuaki Sugio Masayuki Masuda Shotaro Sasaki Seiji Miyauchi Source Type: research
Uptake of Fluorescein via a pH-Dependent Monocarboxylate Transporter by Human Kidney 2 (HK-2) Cells
Biol Pharm Bull. 2024;47(1):79-87. doi: 10.1248/bpb.b23-00570.ABSTRACTHerein, we investigated whether a fluorescent probe for an organic anion transporter (OAT), fluorescein (FLS), could be accumulated by human kidney 2 (HK-2) cells derived from human kidney proximal tubular epithelia. HK-2 cells took up FLS in a pH-dependent and concentration-dependent manner. FLS accumulation by HK-2 cells was inhibited by monocarboxylic acids, ibuprofen, rosuvastatin, and indoleacetic acid but not by typical substrates for OATs. A typical protonophore, carbonyl cyanide p-trichloromethoxyphenylhydrazone completely abolished FLS accumulat...
Source: Biological and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takaharu Takiguchi Kazuaki Sugio Masayuki Masuda Shotaro Sasaki Seiji Miyauchi Source Type: research
Uptake of Fluorescein via a pH-Dependent Monocarboxylate Transporter by Human Kidney 2 (HK-2) Cells
Biol Pharm Bull. 2024;47(1):79-87. doi: 10.1248/bpb.b23-00570.ABSTRACTHerein, we investigated whether a fluorescent probe for an organic anion transporter (OAT), fluorescein (FLS), could be accumulated by human kidney 2 (HK-2) cells derived from human kidney proximal tubular epithelia. HK-2 cells took up FLS in a pH-dependent and concentration-dependent manner. FLS accumulation by HK-2 cells was inhibited by monocarboxylic acids, ibuprofen, rosuvastatin, and indoleacetic acid but not by typical substrates for OATs. A typical protonophore, carbonyl cyanide p-trichloromethoxyphenylhydrazone completely abolished FLS accumulat...
Source: Biological and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takaharu Takiguchi Kazuaki Sugio Masayuki Masuda Shotaro Sasaki Seiji Miyauchi Source Type: research
Uptake of Fluorescein via a pH-Dependent Monocarboxylate Transporter by Human Kidney 2 (HK-2) Cells
Biol Pharm Bull. 2024;47(1):79-87. doi: 10.1248/bpb.b23-00570.ABSTRACTHerein, we investigated whether a fluorescent probe for an organic anion transporter (OAT), fluorescein (FLS), could be accumulated by human kidney 2 (HK-2) cells derived from human kidney proximal tubular epithelia. HK-2 cells took up FLS in a pH-dependent and concentration-dependent manner. FLS accumulation by HK-2 cells was inhibited by monocarboxylic acids, ibuprofen, rosuvastatin, and indoleacetic acid but not by typical substrates for OATs. A typical protonophore, carbonyl cyanide p-trichloromethoxyphenylhydrazone completely abolished FLS accumulat...
Source: Biological and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takaharu Takiguchi Kazuaki Sugio Masayuki Masuda Shotaro Sasaki Seiji Miyauchi Source Type: research
Uptake of Fluorescein via a pH-Dependent Monocarboxylate Transporter by Human Kidney 2 (HK-2) Cells
Biol Pharm Bull. 2024;47(1):79-87. doi: 10.1248/bpb.b23-00570.ABSTRACTHerein, we investigated whether a fluorescent probe for an organic anion transporter (OAT), fluorescein (FLS), could be accumulated by human kidney 2 (HK-2) cells derived from human kidney proximal tubular epithelia. HK-2 cells took up FLS in a pH-dependent and concentration-dependent manner. FLS accumulation by HK-2 cells was inhibited by monocarboxylic acids, ibuprofen, rosuvastatin, and indoleacetic acid but not by typical substrates for OATs. A typical protonophore, carbonyl cyanide p-trichloromethoxyphenylhydrazone completely abolished FLS accumulat...
Source: Biological and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takaharu Takiguchi Kazuaki Sugio Masayuki Masuda Shotaro Sasaki Seiji Miyauchi Source Type: research
Incidence Of Adverse Events Is Higher When Heart Transplant Recipients Are On High Versus Standard Dose Statin In Combination With Cyclosporine
Heart transplant recipients receive a calcineurin inhibitor (CNI) for immunosuppression. While tacrolimus is the CNI of choice, switching to cyclosporine (CSA) may be necessary due to side effects. Treatment with a statin decreases incidence of cardiac allograft vasculopathy and mortality post-transplant. CSA interacts with statins by increasing their levels, with high intensity statins often contraindicated. Per the AHA, maximum recommended statin doses for heart transplants on CSA include atorvastatin 10 mg, pravastatin 20 mg, rosuvastatin 5 mg, and fluvastatin 40 mg. (Source: Journal of Cardiac Failure)
Source: Journal of Cardiac Failure - January 1, 2024 Category: Cardiology Authors: Gabriel E. Diaz, Besher Kashlan, Cole Block, Jenna Negrelli, Michelle Fine, Joshua Newman, Mingxi D. Yu, Max Liebo Tags: 153 Source Type: research
