The development of new therapeutic agents for the mitigation of pediatric disorders is largely hindered by the inability for investigators to assess pediatric pharmacokinetics (PK) in healthy patients due to substantial safety concerns. Pediatric patients are a clinical moving target for drug delivery due to changes in absorption, distribution, metabolism and excretion (ADME) and the potential ...

Linezolid is a new antimicrobial agent effective against drug-resistant gram-positive pathogens which are common causes of infections in hospitalized patients. Many such patients rely on the intravenous or enteral route for nutrition and drug administration. Therefore, the bioavailability of linezolid administered enterally in the presence of enteral feedings in hospitalized patients was examin...

Genetic variants in the pharmacokinetic (PK) mechanism are the main underlying factors affecting the antiplatelet response to clopidogrel. Using a genomewide association study (GWAS) to identify new genetic loci that modify antiplatelet effects in Chinese patients with coronary heart disease, we identified novel variants in two transporter genes (SLC14A2 rs12456693, ATP-binding cassette [ABC]A1...

objective(s): the purpose of the current study was to assess the feasibility of microspheres from biocompatible polymer for oral bioavailability (ba) enhancement of potent sulfonamide- type loop diuretic- furosemide - which used in the treatment of congestive heart failure, caused edema, cirrhosis, renal disease and as an adjunct in acute pulmonary edema. the comparatively poor and inconstant b...

a rapid and sensitive liquid chromatography–tandem mass spectrometry (lc-ms) method for the estimation of enalapril and enalaprilat in human plasma. detection of analytes was achieved by tandem mass spectrometry with electrospray ionization (esi) interface in positive ion mode was operated under the multiple-reaction monitoring mode. sample pretreatment involved in a one-step protein precipitat...

As part of our ongoing small-molecule metabotropic glutamate (mGlu) receptor positive allosteric modulator (PAM) research, we performed structure-activity relationship (SAR) studies around a series of group II mGlu PAMs. Initial analogues exhibited weak activity as mGlu2 receptor PAMs and no activity at mGlu3. Compound optimization led to the identification of potent mGlu2/3 selective PAMs with...

Total intravenous anesthesia (TIVA) can be defined as a technique, in which general anesthesia is induced and maintained using purely i.v. agents. TIVA has become more popular and possible in recent times because of the pharmacokinetic (PK) and pharmacodynamic properties of propofol and the availability of short-acting synthetic opioids. Also, new concepts in PK modeling and advances in compute...

BACKGROUND The conduct of multicenter pharmacokinetic (PK) analyses for long-established drugs entails specific problems, because samples have to be obtained within daily clinical practice. Practices for intravenous (IV) drug administration vary between hospitals, including the use of different infusion devices, the use of infusion line systems with different line volumes, and different priming...

Pharmacokinetic (PK)/pharmacodynamic (PD) modeling has made an enormous contribution to intravenous anesthesia. PK/PD models have provided us with insight into the factors affecting the onset and offset of drug effect. For example, we are now able to describe the influence of cardiac output on the disposition of intravenous drugs within the first few minutes after administration of the drug. We...

Current pharmacokinetic (PK) bioequivalence guidelines do not account for batch-to-batch variability in study design or analysis. Here we evaluate the magnitude of batch-to-batch PK variability for Advair Diskus 100/50. Single doses of fluticasone propionate and salmeterol combinations were administered by oral inhalation to healthy subjects in a randomized clinical crossover study comparing th...