Article
Infectious Diseases
Huixiang Liu, Hongchang Zhou, Jie Xing
Summary: The metabolite PQM of the antimalarial drug piperaquine showed no significant in vitro antimalarial activity and had no significant toxicity in vivo. In healthy subjects, the concentration of PQM remained low after recommended doses of piperaquine and did not accumulate with repeated dosing.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2023)
Article
Physiology
Katarzyna Buszko, Krystian Kubica, Eva-Luise Hobl, Piotr Adamski, Kacper Wnuk, Bernd Jilma, Jacek Kubica
Summary: This study aimed to build a mathematical model describing the pharmacokinetics of ticagrelor and its active metabolite in a stable setting with concomitant administration of morphine. The model accurately reproduced experimental results and led to conclusions consistent with clinical observations that morphine delays the time of maximum drug concentration. The model also allowed for predicting the effect of drug dose on receptor blocking efficacy.
FRONTIERS IN PHYSIOLOGY
(2021)
Article
Pharmacology & Pharmacy
M. E. Otto, K. R. Bergmann, G. Jacobs, Michiel J. van Esdonk
Summary: Recent repurposing of ketamine as treatment for pain and depression has increased the demand for accurate population pharmacokinetic (PK) models for informing new clinical trial designs. This study aimed to externally validate available PK models on (S)-(nor)ketamine concentrations, improve the best performing model, and provide a solid foundation for future simulation studies of (S)-(nor)ketamine PK in healthy volunteers after (S)-ketamine infusion.
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Jiayu Li, Pei Hu, Li Zhou, Fumiko Nagahama, Rui Chen
Summary: This study found ethnic differences in the pharmacokinetics of granisetron patches between Chinese and Caucasian populations, but analysis of a population pharmacokinetic model showed no significant differences in pharmacokinetic parameters between the two groups. Therefore, this study provides valuable insights for optimizing dosage across Chinese and Caucasian populations.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Anne Michelli Reis Silveira, Gustavo Henrique Bueno Duarte, Anna Maria Alves de Piloto Fernandes, Pedro Henrique Dias Garcia, Nelson Rogerio Vieira, Marcia Aparecida Antonio, Patricia de Oliveira Carvalho
Summary: Rosuvastatin, a lipid-lowering agent used for hypercholesterolemia treatment, exhibits significant inter-individual variability in absorption due to genetic polymorphisms. Investigating metabolic markers associated with this variability is crucial for optimizing drug therapy efficacy and minimizing side effects. The application of pharmacometabolomic strategies to predict pharmacokinetic parameters using plasma metabolites shows promising potential for personalized drug therapy.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Multidisciplinary Sciences
Y. A. de Reus, P. Hagedoorn, M. G. G. Sturkenboom, F. Grasmeijer, M. S. Bolhuis, I Sibum, H. A. M. Kerstjens, H. W. Frijlink, O. W. Akkerman
Summary: This study assessed the local tolerability, safety, and pharmacokinetic parameters of inhaled HCQ using a dry powder inhaler. The results showed that single doses of inhaled dry powder HCQ up to 20 mg are safe and well tolerated, without significant adverse effects.
Article
Chemistry, Medicinal
Jae Hoon Kim, Jung Sunwoo, Ji Hye Song, Yu-Bin Seo, Won Tae Jung, Kyu-Yeol Nam, YeSeul Kim, Hye Jung Lee, JungHa Moon, Jin-Gyu Jung, Jang Hee Hong
Summary: The interaction between atorvastatin and omega-3 fatty acids was evaluated in a phase 1 trial, and it was found that co-administration of the two drugs affected their concentrations, indicating a drug-drug interaction.
Article
Pharmacology & Pharmacy
Myeong-Bae Shin, Sung-Ah Kim, Sooyoung Lee, Wang-Seob Shim, Kyung-Tae Lee, Seung-Kwon Lee, Sung-Vin Yim, Bo-Hyung Kim
Summary: Fermentation of red ginseng produces fermented red ginseng with increased downstream ginsenosides which have beneficial pharmacological effects and are easily absorbed by the human body. A clinical trial showed higher systemic exposure of ginsenosides, particularly CK and Rh2, after administration of fermented red ginseng compared to regular red ginseng.
Article
Pharmacology & Pharmacy
Roberta Bartolucci, Anne-Gaelle Dosne, Denes Csonka, Juan Jose Perez-Ruixo, Paolo Magni, Italo Poggesi
Summary: This study developed a comprehensive population pharmacokinetic model to describe the pharmacokinetics of macitentan and aprocitentan in healthy adults and adult subjects with pulmonary arterial hypertension. Covariates such as body weight, sex, race, renal impairment, and health status significantly influenced the pharmacokinetics of these drugs.
CLINICAL PHARMACOKINETICS
(2021)
Article
Pharmacology & Pharmacy
Muhammad Ali Syed, Ghiyyas Aziz, Muhammad Bilal Jehangir, Tanveer A. Tabish, Ameer Fawad Zahoor, Syed Haroon Khalid, Ikram Ullah Khan, Khaled Mohamed Hosny, Waleed Yousof Rizg, Sana Hanif, Rabia Arshad, Muhammad Abdul Qayyum, Muhammad Irfan
Summary: This study developed a mucoadhesive gel scaffold based on agarose and carbopol for simultaneous release of benzocaine and tibezonium iodide. The results showed that the AG-CP scaffold provided better mucoadhesive properties compared to pure AG or CP, with excellent performance in terms of mucoadhesive time, drug release, and stability. The mucoadhesive study on healthy volunteers did not provoke any adverse reactions.
Article
Pharmacology & Pharmacy
Simona Rizea-Savu, Simona Nicoleta Duna, Roxana Colette Sandulovici
Summary: Alverine citrate is commonly prescribed for conditions such as irritable bowel syndrome, and painful diverticular disease of the colon. Despite the availability of clinical efficacy data, there is limited information on the pharmacokinetics and metabolism of alverine in literature. A study revealed high pharmacokinetic variability in the parent alverine, and identified hydroxylation to the active metabolite 4-hydroxy alverine as a susceptible metabolic process in Caucasian individuals.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Cui Tang, Chen-xi Ou-yang, Wen-jing Chen, Chan Zou, Jie Huang, Chang Cui, Shuang Yang, Can Guo, Xiao-yan Yang, Yu Lin, Qi Pei, Guo-ping Yang
Summary: By using a PBPK model, researchers successfully established the pharmacokinetic profile of indacaterol and confirmed its feasibility in the development of inhaled drugs. The study findings suggest that particle size is the most crucial factor affecting the in vivo pharmacokinetics of indacaterol.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Review
Oncology
Igor Radanovic, Naomi Klarenbeek, Robert Rissmann, Geert Jan Groeneveld, Emilie M. J. van Brummelen, Matthijs Moerland, Jacobus J. Bosch
Summary: This study investigated the utilization of immuno-oncology compounds in clinical trials with healthy volunteers and the evaluation of pharmacodynamic endpoints. The study found that while these trials are not widely conducted, they offer advantages such as early dose selection and prevention of non-therapeutic dosing regimens for cancer patients. The focus is on safety and pharmacodynamic endpoints.
FRONTIERS IN ONCOLOGY
(2022)
Article
Chemistry, Medicinal
Moon Hee Lee, Seok-Kyu Yoon, Hyungsub Kim, Yong-Soon Cho, Sungpil Han, Shi Hyang Lee, Kyun-Seop Bae, Jina Jung, Sung Hee Hong, Hyeong-Seok Lim
Summary: This study aimed to examine the pharmacokinetic interactions between bazedoxifene and cholecalciferol and the tolerability of their combined administration in healthy male subjects. The results showed that this combined therapy was well tolerated at the dose levels used in the study, and there was a mild degree of pharmacokinetic interaction.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2023)
Article
Multidisciplinary Sciences
Shaheen Perveen, Shahnaz Gauhar, Rabia Ismail Yousuf, Huma Ali, Farya Zafar, Anab Fatima Sheikh
Summary: This study evaluated the effect of ranitidine on the pharmacokinetics of amoxicillin. The results showed that ranitidine significantly reduced the peak plasma concentration of amoxicillin. Therefore, it is recommended to administer both drugs with a time interval to enhance the therapeutic effect of amoxicillin.