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Pharmacokinetics pharmacodynamics

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https://www.readbyqxmd.com/read/28445495/pharmacokinetic-and-pharmacodynamic-modelling-after-subcutaneous-intravenous-and-buccal-administration-of-a-high-concentration-formulation-of-buprenorphine-in-conscious-cats
#1
Graeme M Doodnaught, Beatriz P Monteiro, Javier Benito, Daniel Edge, Francis Beaudry, Ludovic Pelligand, Paulo Steagall
BACKGROUND: The aim of this study was to describe the joint pharmacokinetic-pharmacodynamic model and evaluate thermal antinociception of a high-concentration formulation of buprenorphine (Simbadol™) in cats. METHODS: Six healthy cats (4.9 ± 0.7 kg) were included in a prospective, randomized, blinded, crossover study. Simbadol™ (1.8 mg mL-1) was administered by the subcutaneous (SC; 0.24 mg kg-1), intravenous (IV; 0.12 mg kg-1) or buccal (OTM; 0.12 mg kg-1) route of administration and thermal thresholds (TT) were compared with a saline group (SAL)...
2017: PloS One
https://www.readbyqxmd.com/read/28444224/pharmacodynamics-of-colistin-and-fosfomycin-a-treasure-trove-combination-combats-kpc-producing-klebsiella-pneumoniae
#2
Miao Zhao, Zackery P Bulman, Justin R Lenhard, Michael J Satlin, Barry N Kreiswirth, Thomas J Walsh, Amanda Marrocco, Phillip J Bergen, Roger L Nation, Jian Li, Jing Zhang, Brian T Tsuji
Objectives: KPC-producing Klebsiella pneumoniae are an emerging public health problem around the globe. We defined the combinatorial pharmacodynamics and ability to suppress resistance of two 'old' antibiotics, fosfomycin and colistin, in time-kill experiments and hollow-fibre infection models (HFIM). Methods: Two KPC-2-producing K. pneumoniae isolates were used: one susceptible to both colistin and fosfomycin (KPC 9A: MIC colistin 0.25 mg/L and MIC fosfomycin ≤8 mg/L) and the other resistant to colistin and susceptible to fosfomycin (KPC 5A: MIC colistin 64 mg/L and MIC fosfomycin 32 mg/L)...
April 21, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28442937/simultaneous-administration-of-fluoxetine-and-simvastatin-ameliorates-lipid-profile-improves-brain-level-of-neurotransmitters-and-increases-bioavailability-of-simvastatin
#3
Abdulrahman K Al-Asmari, Zabih Ullah, Aqeel Salman Al Masoudi, Ishtiaque Ahmad
Simvastatin (STT), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, is widely prescribed for dyslipidemia, whereas fluoxetine (FLX) is the first-choice drug for the treatment of depression and anxiety. A recent report suggests that selective serotonin reuptake inhibitors can interact with the cytochrome P450 3A4 substrate, and another one suggests that STT enhances the antidepressant activity of FLX. However, the data are inconclusive. The present study was designed to explore the pharmacokinetic and pharmacodynamic consequences of coadministration of STT and FLX in experimental animals...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28441481/best-practices-of-computer-aided-drug-discovery-cadd-lessons-learned-from-the-development-of-a-preclinical-candidate-for-prostate-cancer-with-a-new-mechanism-of-action
#4
Fuqiang Ban, Kush Dalal, Huifang Li, Eric LeBlanc, Paul S Rennie, Artem Cherkasov
Small-molecule drug design is a complex and iterative decision-making process relying on pre-existing knowledge and driven by experimental data. Low molecular weight chemicals represent an attractive therapeutic option as they are readily accessible to organic synthesis and can easily be characterized.1 Their potency, as well as pharmacokinetic and pharmacodynamic properties can be systematically and rationally investigated, and ultimately optimized via expert science behind medicinal chemistry and methods of computer-aided drug design (CADD)...
April 25, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28441162/managing-herpes-zoster-in-older-adults-prescribing-considerations
#5
Linda Beuscher, Geri Reeves, Debbie Harrell
NPs must be aware of special prescribing considerations for medication safety when managing the care of older adults with herpes zoster. Age-related physiologic changes of the body impact the pharmacokinetics and pharmacodynamics of antiviral and pain medications and can lead to potential adverse events.
April 24, 2017: Nurse Practitioner
https://www.readbyqxmd.com/read/28441044/pharmacokinetics-and-pharmacodynamics-of-midazolam-following-intravenous-and-intramuscular-administration-to-sheep
#6
Bradley T Simon, Elizabeth M Scallan, Odette O, Lisa Sams Ebner, Michelle N Cerullo, Christelle Follette, Sherry K Cox, Thomas J Doherty, Ignacio Lizarraga
OBJECTIVE To determine the pharmacokinetic and pharmacodynamic effects of midazolam following IV and IM administration in sheep. ANIMALS 8 healthy adult rams. PROCEDURES Sheep were administered midazolam (0.5 mg/kg) by the IV route and then by the IM route 7 days later in a crossover study. Physiologic and behavioral variables were assessed and blood samples collected for determination of plasma midazolam and 1-hydroxymidazolam (primary midazolam metabolite) concentrations immediately before (baseline) and at predetermined times for 1,440 minutes after midazolam administration...
May 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28440659/alleviation-of-multiple-asthmatic-pathologic-features-with-orally-available-and-subtype-selective-gabaa-receptor-modulators
#7
Gloria S Forkuo, Amanda N Nieman, Nina Y Yuan, Revathi Kodali, Olivia B Yu, Nicolas M Zahn, Rajwana Jahan, Guanguan Li, Michael Rajesh Stephen, Margaret L Guthrie, Michael M Poe, Benjamin D Hartzler, Ted William Harris, Gene T Yocum, Charles W Emala, Douglas A Steeber, Douglas C Stafford, James M Cook, Leggy A Arnold
We describe pharmacokinetic and pharmacodynamic properties of two novel oral drug candidates for asthma. Phenolic α4β3γ2 GABAAR selective compound 1 and acidic α5β3γ2 selective GABAAR positive allosteric modulator compound 2 relaxed airway smooth muscle ex vivo and attenuated airway hyperresponsiveness (AHR) in a murine model of asthma. Importantly, compound 2 relaxed acetylcholine contracted human tracheal airway smooth muscle strips. Oral treatment of compound 1 and 2 decreased eosinophils in bronchoalveolar lavage fluid in ovalbumin sensitized and challenged mice, thus exhibiting anti-inflammatory properties...
April 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28440204/apixaban-metabolism-pharmacologic-properties-and-drug-interaction
#8
Peter Kubisz, Lucia Stanciakova, Miroslava Dobrotova, Matej Samos, Marian Mokan, Jan Stasko
BACKGROUND: Apixaban is an oral, potent, highly selective, reversible and direct inhibitor of activated coagulation factor X, that is the end point of the intrinsic and extrinsic coagulation pathway. Additionally, apixaban has the capacity to indirectly inhibit thrombin-induced platelet aggregation. This new oral anticoagulant represents an immediate-release form of peroral drug with quick dissolution, linear pharmacokinetics, good bioavailability and rapid onset and offset of action...
April 24, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28440008/major-bleeding-risks-of-different-low-molecular-meight-heparin-agents-a-cohort-study-in-12-934-patients-treated-for-acute-venous-thrombosis
#9
N van Rein, J S Biedermann, F J M van der Meer, S C Cannegieter, N Wiersma, H W Vermaas, P H Reitsma, M J H A Kruip, W M Lijfering
BACKGROUND: Low-molecular-weight-heparins (LMWHs) are considered members of a class of drugs with similar anticoagulant properties. However, pharmacodynamics and pharmacokinetics between LMWHs differ, which may result in different bleeding risks. As these agents are used by many patients, small differences may lead to a large effect on numbers of major bleeding events. OBJECTIVES: To determine major bleeding risks for different LMWH agents and dosing schedules. METHODS: Cohort with acute venous thrombosis patients from four anticoagulation clinics who used a LMWH and a vitamin K antagonist...
April 25, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28439817/developing-the-totality-of-evidence-for-biosimilars-regulatory-considerations-and-building-confidence-for-the-healthcare-community
#10
REVIEW
Richard Markus, Jennifer Liu, Monica Ramchandani, Diana Landa, Teresa Born, Primal Kaur
Biosimilars are highly similar versions of approved branded biologics. Unlike generics, they are not exact replicas of reference products. Minor differences between biosimilars and reference products in some aspects are expected; likewise, biosimilar products will differ from each other. The objective of this review is to discuss the challenges associated with the development and approval of biosimilar products that are unique because of their complex structure and specialized manufacturing processes, which can impact not only efficacy but also immunogenicity and safety...
April 24, 2017: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
https://www.readbyqxmd.com/read/28438821/effects-of-i-v-push-administration-on-%C3%AE-lactam-pharmacodynamics
#11
Jill M Butterfield-Cowper, Kimberli Burgner
PURPOSE: The effects of i.v. push administration on the pharmacodynamic exposures of meropenem, cefepime, and aztreonam were evaluated. METHODS: Pharmacokinetic and pharmacodynamic analyses were conducted using previously published pharmacokinetic data for meropenem, cefepime, and aztreonam. The probability of target attainment (PTA) was assessed using Monte Carlo simulations for 30-minute and 5-minute infusions of approved dosing regimens and alternative dosing schemes often used in clinical practice, including 500 mg every 6 hours and 1 g every 8 hours for meropenem, 1 g every 6 hours and 2 g every 8 hours for cefepime, and 2 g every 8 hours for aztreonam...
May 1, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28438781/transporter-mediated-disposition-clinical-pharmacokinetics-and-cholestatic-potential-of-glyburide-and-its-primary-active-metabolites
#12
Rui Li, Yi-An Bi, Anna Vildhede, Renato J Scialis, Sumathy Mathialagan, Xin Yang, Lisa D Marroquin, Jian Lin, Manthena V S Varma
Glyburide is widely used for the treatment of type 2 diabetes mellitus. We studied the mechanisms involved in the disposition of glyburide and its pharmacologically active hydroxy metabolites, M1 and M2b; and evaluated their clinical pharmacokinetics and the potential role in glyburide-induced cholestasis employing physiologically based pharmacokinetic (PBPK) modeling. Transport studies of parent and metabolites in human hepatocytes and transfected cell systems imply hepatic uptake mediated by organic anion transporting polypeptides...
April 24, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28437852/a-diagnostic-microdosing-approach-to-investigate-platinum-sensitivity-in-non-small-cell-lung-cancer
#13
Si-Si Wang, Maike Zimmermann, Hongyong Zhang, Tzu-Yin Lin, Michael Malfatti, Kurt Haack, Kenneth W Turteltaub, George D Cimino, Ralph de Vere White, Chong-Xian Pan, Paul T Henderson
The platinum-based drugs cisplatin, carboplatin and oxaliplatin are often used for chemotherapy, but drug resistance is common. The prediction of resistance to these drugs via genomics is a challenging problem since hundreds of genes are involved. A possible alternative is to use mass spectrometry to determine the propensity for cells to form drug-DNA adducts-the pharmacodynamic drug-target complex for this class of drugs. The feasibility of predictive diagnostic microdosing was assessed in non-small cell lung cancer (NSCLC) cell culture and a pilot clinical trial...
April 24, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28437278/pharmacodynamic-and-kinetic-behavior-of-low-intermediate-and-high-dose-landiolol-during-long-term-infusion-in-caucasians
#14
Günther Krumpl, Ivan Ulč, Michaela Trebs, Pavla Kadlecová, Juri Hodisch, Gabriele Maurer, Bernhard Husch
PK, PD, safety, and tolerability of long-term administration of landiolol, a fast-acting cardioselective β-blocker, were investigated for the first time in Caucasian subjects in a prospective clinical trial.Blood concentrations of landiolol and its metabolites, HR, BP and ECG parameters were studied in twelve healthy volunteers receiving continuous infusions of a new 12 mg/mL formulation of landiolol using a dose-escalation regimen (10 µg/kg BW/min for 2 hr, 20 µg/kg BW/min for 2 hr, 40 µg/kg BW/min for 20 hr, 6 hr follow-up)...
April 18, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28436937/efficacy-of-anti-sclerostin-monoclonal-antibody-bps804-in-adult-patients-with-hypophosphatasia
#15
Lothar Seefried, Jasmin Baumann, Sarah Hemsley, Christine Hofmann, Erdmute Kunstmann, Beate Kiese, Yue Huang, Simon Chivers, Marie-Anne Valentin, Babul Borah, Ronenn Roubenoff, Uwe Junker, Franz Jakob
BACKGROUND: Hypophosphatasia (HPP) is a rare genetic disorder resulting in variable alterations of bone formation and mineralization that are caused by mutations in the ALPL gene, encoding the tissue-nonspecific alkaline phosphatase (ALP) enzyme. METHODS: In this phase IIA open-label, single-center, intra-patient, dose-escalating study, adult patients with HPP received 3 ascending intravenous doses of 5, 10, and 20 mg/kg BPS804, a fully human anti-sclerostin monoclonal antibody, on days 1, 15, and 29, respectively...
April 24, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28435985/elucidating-the-a%C3%AE-42-anti-aggregation-mechanism-of-action-of-tramiprosate-in-alzheimer-s-disease-integrating-molecular-analytical-methods-pharmacokinetic-and-clinical-data
#16
Petr Kocis, Martin Tolar, Jeremy Yu, William Sinko, Soumya Ray, Kaj Blennow, Howard Fillit, John A Hey
BACKGROUND: Amyloid beta (Aβ) oligomers play a critical role in the pathogenesis of Alzheimer's disease (AD) and represent a promising target for drug development. Tramiprosate is a small-molecule Aβ anti-aggregation agent that was evaluated in phase III clinical trials for AD but did not meet the primary efficacy endpoints; however, a pre-specified subgroup analysis revealed robust, sustained, and clinically meaningful cognitive and functional effects in patients with AD homozygous for the ε4 allele of apolipoprotein E4 (APOE4/4 homozygotes), who carry an increased risk for the disease...
April 24, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28434401/ivermectin-to-reduce-malaria-transmission-i-pharmacokinetic-and-pharmacodynamic-considerations-regarding-efficacy-and-safety
#17
REVIEW
Carlos Chaccour, Felix Hammann, N Regina Rabinovich
Ivermectin is an endectocide that has been used broadly in single dose community campaigns for the control of onchocerciasis and lymphatic filariasis for more than 30 years. There is now interest in the potential use of ivermectin regimens to reduce malaria transmission, envisaged as community-wide campaigns tailored to transmission patterns and as complement of the local vector control programme. The development of new ivermectin regimens or other novel endectocides will require integrated development of the drug in the context of traditional entomological tools and endpoints...
April 24, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28432800/effect-of-n-methyl-deuteration-on-pharmacokinetics-and-pharmacodynamics-of-enzalutamide
#18
Xuehai Pang, Lingling Peng, Yuanwei Chen
Enzalutamide, a 2nd generation antiandrogen, has been developed for the treatment of CRPC. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger anti-tumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.
April 22, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28432741/pharmacokinetic-and-pharmacodynamic-effects-of-two-omeprazole-formulations-on-stomach-ph-and-gastric-ulcer-scores
#19
S Raidal, F M Andrews, S G Nielsen, G Trope
REASONS FOR PERFORMING THE STUDY: Limited data are available on the relative pharmacokinetics and pharmacodynamics of different omeprazole formulations. OBJECTIVES: To compare pharmacokinetic and pharmacodynamic effects of a novel omeprazole formulation against a currently registered product. STUDY DESIGN: Masked two period, two treatment crossover. METHODS: Twelve clinically healthy horses were studied over two 6-day treatment periods...
April 22, 2017: Equine Veterinary Journal
https://www.readbyqxmd.com/read/28432691/tenapanor-administration-and-the-activity-of-the-h-coupled-transporter-pept1-in-healthy-volunteers
#20
Susanne Johansson, David P Rosenbaum, Johan Palm, Bergur Stefansson, Mikael Knutsson, Eleanor A Lisbon, Constanze Hilgendorf
AIM: Tenapanor (RDX5791/AZD1722), an inhibitor of gastrointestinal Na(+) /H(+) exchanger NHE3, is being evaluated for the treatment of patients with constipation-predominant irritable bowel syndrome and the treatment of hyperphosphataemia in patients with chronic kidney disease on dialysis. By reducing intestinal H(+) secretion, inhibition of NHE3 by tenapanor could indirectly affect H(+) -coupled transporter activity, leading to drug-drug interactions. We investigated the effect of tenapanor on the activity of the H(+) -coupled peptide transporter PepT1 via assessment of the pharmacokinetics of cefadroxil - a compound transported by PepT1 - in healthy volunteers...
April 22, 2017: British Journal of Clinical Pharmacology
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