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  1. Tang BH, Guan Z, Allegaert K, Wu YE, Manolis E, Leroux S, et al.
    Clin Pharmacokinet, 2021 11;60(11):1435-1448.
    PMID: 34041714 DOI: 10.1007/s40262-021-01033-x
    BACKGROUND: Population pharmacokinetic evaluations have been widely used in neonatal pharmacokinetic studies, while machine learning has become a popular approach to solving complex problems in the current era of big data.

    OBJECTIVE: The aim of this proof-of-concept study was to evaluate whether combining population pharmacokinetic and machine learning approaches could provide a more accurate prediction of the clearance of renally eliminated drugs in individual neonates.

    METHODS: Six drugs that are primarily eliminated by the kidneys were selected (vancomycin, latamoxef, cefepime, azlocillin, ceftazidime, and amoxicillin) as 'proof of concept' compounds. Individual estimates of clearance obtained from population pharmacokinetic models were used as reference clearances, and diverse machine learning methods and nested cross-validation were adopted and evaluated against these reference clearances. The predictive performance of these combined methods was compared with the performance of two other predictive methods: a covariate-based maturation model and a postmenstrual age and body weight scaling model. Relative error was used to evaluate the different methods.

    RESULTS: The extra tree regressor was selected as the best-fit machine learning method. Using the combined method, more than 95% of predictions for all six drugs had a relative error of < 50% and the mean relative error was reduced by an average of 44.3% and 71.3% compared with the other two predictive methods.

    CONCLUSION: A combined population pharmacokinetic and machine learning approach provided improved predictions of individual clearances of renally cleared drugs in neonates. For a new patient treated in clinical practice, individual clearance can be predicted a priori using our model code combined with demographic data.

    Matched MeSH terms: Metabolic Clearance Rate
  2. Pan Y, Ong CE, Pung YF, Chieng JY
    Xenobiotica, 2019 Jul;49(7):863-876.
    PMID: 30028220 DOI: 10.1080/00498254.2018.1503360
    Nanoparticles (NPs) have wide spectrum applications in the areas of industry and biomedicine. However, concerns about their toxic and negative impacts on the environments as well as human health have been raised. Cytochrome P450s (CYPs) are involved in endogenous and exogenous metabolism. Modulations of CYP can adversely damage drug metabolism, detoxification of xenobiotics and animal physiology functions. This article focused on NPs-CYP interactions for humans and animals available in the literature. It was found that different NPs process specific inhibitory potencies against CYPs involved in drug metabolism. Moreover, NPs were able to modify the expression of CYPs genes or protein in humans and other animals, which highlighted their detoxification functions. Nonetheless, changes of CYPs responsible for hormone synthesis and metabolism resulted in endocrine disturbances. Hence, there is a need to screen newly developed NPs to evaluate their interactions with CYPs. The future studies should further strategize the in vitro approaches to reveal the molecular mechanisms behind interactions by taking full considerations of the interference of co-factors, buffers, substrates and metabolites with NPs. Moreover, in vivo studies should compare the influences of NPs via different administration routes and different duration of treatments to reveal the physiological significance.
    Matched MeSH terms: Metabolic Clearance Rate
  3. Lye HS, Alias KA, Rusul G, Liong MT
    Ultrason Sonochem, 2012 May;19(3):632-41.
    PMID: 21907608 DOI: 10.1016/j.ultsonch.2011.08.004
    This study aimed to evaluate the effect of ultrasound treatment on the cholesterol removing ability of lactobacilli. Viability of lactobacilli cells was significantly increased (P < 0.05) immediately after treatment, but higher intensity of 100 W and longer duration of 3 min was detrimental on cellular viability (P < 0.05). This was attributed to the disruption of membrane lipid bilayer, cell lysis and membrane lipid peroxidation upon ultrasound treatment at higher intensity and duration. Nevertheless, the effect of ultrasound on membrane properties was reversible, as the viability of ultrasound-treated lactobacilli was increased (P < 0.05) after fermentation at 37 °C for 20 h. The removal of cholesterol by ultrasound-treated lactobacilli via assimilation and incorporation of cholesterol into the cellular membrane also increased significantly (P < 0.05) upon treatment, as observed from the increased ratio of membrane C:P. Results from fluorescence anisotropies showed that most of the incorporated cholesterol was saturated in the regions of phospholipids tails, upper phospholipids, and polar heads of the membrane bilayer.
    Matched MeSH terms: Metabolic Clearance Rate/radiation effects
  4. Abdullah AS, Baggot JD
    Vet Res Commun, 1988;12(6):441-6.
    PMID: 3222919
    The disposition kinetics and cumulative urinary excretion of sulfamethazine were compared in goats fed normally (control) and following a 72-hour period of starvation (fasting). The only pharmacokinetic parameter which showed a statistically significant difference between the two groups was the body (systemic) clearance. This decreased from 2.26 +/- 0.28 ml/min.kg (means +/- SD, n = 6) in the control group to 1.16 +/- 0.54 ml/min.kg in the fasting group (p less than 0.01). Since the apparent volume of distribution was not affected by starvation, the decreased clearance was attributed to slower metabolism of the drug. Because of the analytical method used to measure sulfamethazine concentrations in plasma and urine, no conclusion could be drawn as to whether the rates of hydroxylation or of acetylation, or both metabolic pathways were decreased in the starved condition.
    Matched MeSH terms: Metabolic Clearance Rate
  5. Holford N, O'Hanlon CJ, Allegaert K, Anderson B, Falcão A, Simon N, et al.
    Br J Clin Pharmacol, 2024 Apr;90(4):1066-1080.
    PMID: 38031322 DOI: 10.1111/bcp.15978
    AIMS: We propose using glomerular filtration rate (GFR) as the physiological basis for distinguishing components of renal clearance.

    METHODS: Gentamicin, amikacin and vancomycin are thought to be predominantly excreted by the kidneys. A mixed-effects joint model of the pharmacokinetics of these drugs was developed, with a wide dispersion of weight, age and serum creatinine. A dataset created from 18 sources resulted in 27,338 drug concentrations from 9,901 patients. Body size and composition, maturation and renal function were used to describe differences in drug clearance and volume of distribution.

    RESULTS: This study demonstrates that GFR is a predictor of two distinct components of renal elimination clearance: (1) GFR clearance associated with normal GFR and (2) non-GFR clearance not associated with normal GFR. All three drugs had GFR clearance estimated as a drug-specific percentage of normal GFR (gentamicin 39%, amikacin 90% and vancomycin 57%). The total clearance (sum of GFR and non-GFR clearance), standardized to 70 kg total body mass, 176 cm, male, renal function 1, was 5.58 L/h (95% confidence interval [CI] 5.50-5.69) (gentamicin), 7.77 L/h (95% CI 7.26-8.19) (amikacin) and 4.70 L/h (95% CI 4.61-4.80) (vancomycin).

    CONCLUSIONS: GFR provides a physiological basis for renal drug elimination. It has been used to distinguish two elimination components. This physiological approach has been applied to describe clearance and volume of distribution from premature neonates to elderly adults with a wide dispersion of size, body composition and renal function. Dose individualization has been implemented using target concentration intervention.

    Matched MeSH terms: Metabolic Clearance Rate
  6. Ruzilawati AB, Mohd Suhaimi AW, Gan SH
    J Clin Pharm Ther, 2010 Feb;35(1):105-12.
    PMID: 20175819 DOI: 10.1111/j.1365-2710.2009.01042.x
    To estimate population pharmacokinetic parameters of repaglinide in 121 healthy Malaysian volunteers.
    Matched MeSH terms: Metabolic Clearance Rate
  7. Ismail R, Rahman AF
    J Clin Pharm Ther, 1993 Feb;18(1):55-8.
    PMID: 8473361
    We used OPT to estimate individual and population pharmacokinetics for carbamazepine (CBZ) in Malaysian epileptic patients attending our Neurology Clinic. We noted that plasma CBZ concentrations and clearances correlated poorly with daily doses and body weights respectively but we found the values for clearance, volumes of distribution, elimination rate constants and half lives to be in good agreement with earlier reports. We conclude that OPT is a simple yet useful program to derive individual and population pharmacokinetic parameters for CBZ for use in dosage adjustments. We also conclude that although the Malaysian population do not differ substantially in handling CBZ, available data for the pharmacokinetic parameters must be used cautiously in applying it to the therapeutic drug monitoring for CBZ in our patients.
    Matched MeSH terms: Metabolic Clearance Rate
  8. Najat Dzaki, Ghows Azzam
    Trop Life Sci Res, 2019;30(2):191-200.
    MyJurnal
    In Drosophila, the Glycerol-3-phosphate dehydrogenase (Gpdh) enzyme plays an active role in many pathways, including the glycerol metabolic pathway and the alphaglycerophosphate cycle. It is also important for ethanol metabolism, as well as flight muscle development. Recent years have exposed small RNAs as a major posttranscriptional regulator of multiple metabolic-pathway genes. Of the many kinds of these RNAs at work, micro RNAs (miRNAs) are the most widely implicated and well understood. However, the roles they may play in regulating Gpdh has never been shown in any model organism. In this study, a pasha-mutant D. melanogaster strain was found to express only 25% of the Gpdh levels typical of their wild type counterparts. Such mutants lack the ability to produce pasha, a protein integral during miRNA-processing, and as a consequence do not produce mature miRNAs. As miRNA-centric regulation often culminates in the depletion of their targets, the concurrent downregulation of Gpdh observed in their absence here therefore alludes to two possibilities: one, that rather than being explicitly bound and repressed by miRNAs, Gpdh expression relies on their action upon an upstream Gpdh-antagonist; or two, that Gpdh may come under the regulation of another class of miRNA-like elements called mirtrons, which do not require pasha to be processed into their functional form. The preliminary findings in this study further highlights the imperative nature of miRNAs in regulating metabolic processes and subsequently, ensuring proper organismal development and its continued survival.
    Matched MeSH terms: Metabolic Clearance Rate
  9. Wong JW, Yuen KH
    Int J Pharm, 2001 Oct 04;227(1-2):177-85.
    PMID: 11564552
    The bioavailability of beta- and gamma-cyclodextrin artemisinin complexes was evaluated in comparison with a normal commercially available preparation, Artemisinin 250. Twelve healthy male volunteers participated in the study conducted according to a three-way crossover design. The bioavailability was compared using the parameters, total area under the plasma level-time curve (AUC(0-infinity)), peak plasma concentration (C(max)), and time to reach peak plasma concentration (T(max)). A statistically significant difference was observed between the values of the complexes and Artemisinin 250 for the three parameters. However, no statistically significant difference was observed between the values of the beta- and gamma-cyclodextrin complexes. Moreover, the 90% confidence interval for the ratio of the AUC(0-infinity) values of the beta-cyclodextrin complex over those of Artemisinin 250 was estimated to be between 1.51-2.04, while that of C(max) was between 1.73-2.93. For the gamma-cyclodextrin complex, the respective intervals were 1.30-1.76 and 1.43-2.43. These findings indicated that the beta- and gamma-cyclodextrin complexes had a much higher rate and extent of bioavailability compared to Artemisinin 250. In addition, the absorption of artemisinin was observed to be poor and negligible when the preparations started to arrive in the colon. This could be attributed to poor dissolution of artemisinin in the semi-solid faecal matter in the lower part of the gastrointestinal tract.
    Matched MeSH terms: Metabolic Clearance Rate
  10. Malik AS, Zabidi MH, Noor AR
    Singapore Med J, 1994 Apr;35(2):215-6.
    PMID: 7939826
    Traditional medicine is practised to some degree in all cultures. Many different types of herbal preparations and "oils" are widely used in Malaysia, too. We report a case of acute salicylism due to accidental ingestion of one brand of such oils. Compulsory labelling of traditional drugs with their chemical ingredients is suggested for proper and timely management of such cases.
    Matched MeSH terms: Metabolic Clearance Rate
  11. Gendeh BS, Gibb AG, Aziz NS, Kong N, Zahir ZM
    Otolaryngol Head Neck Surg, 1998 Apr;118(4):551-8.
    PMID: 9560111
    A prospective study was undertaken in 16 patients with chronic renal failure on continuous ambulatory peritoneal dialysis, with 22 episodes of peritonitis treated with vancomycin, a known ototoxic agent. Twelve patients had one episode each, and four had recurrent peritonitis. Each treatment course consisted of two infusions of vancomycin (30 mg/kg body weight) in 2 L of peritoneal dialysate administered at 6-day intervals. Serum vancomycin analyzed by enzyme immunoassay showed a mean trough level of 11.00 microg/ml on day 6 and mean serum levels of 33.8 and 38.6 microg/ml about 12 hours after administration on days 1 and 7, respectively. Similar levels, well within the therapeutic range, were encountered with repeated vancomycin therapy for recurrent episodes of peritonitis, suggesting that no changes occurred in the pharmacokinetic profile of the drug. Pure-tone audiometry, electronystagmography, and clinical assessment performed during each course of treatment showed no evidence of ototoxicity even on repeated courses of vancomycin therapy. The results suggest that vancomycin therapy when given in appropriate concentrations as a single therapeutic agent is both effective and safe. We believe, however, that vancomycin administered in combination with an aminoglycoside may produce ototoxic effects that may be greatly aggravated, possibly because of synergism.
    Matched MeSH terms: Metabolic Clearance Rate/physiology
  12. Yeong CH, Ng KH, Abdullah BJJ, Chung LY, Goh KL, Perkins AC
    Appl Radiat Isot, 2014 Dec;94:216-220.
    PMID: 25222875 DOI: 10.1016/j.apradiso.2014.08.009
    Radionuclide imaging using (111)In, (99m)Tc and (153)Sm is commonly undertaken for the clinical investigation of gastric emptying, intestinal motility and whole gut transit. However the documented evidence concerning internal radiation dosimetry for such studies is not readily available. This communication documents the internal radiation dosimetry for whole gastrointestinal transit studies using (111)In, (99m)Tc and (153)Sm labeled formulations. The findings were compared to the diagnostic reference levels recommended by the United Kingdom Administration of Radioactive Substances Advisory Committee, for gastrointestinal transit studies.
    Matched MeSH terms: Metabolic Clearance Rate
  13. Jamal JA, Roberts DM, Udy AA, Mat-Nor MB, Mohamad-Nor FS, Wallis SC, et al.
    Int J Antimicrob Agents, 2015 Jul;46(1):39-44.
    PMID: 25881872 DOI: 10.1016/j.ijantimicag.2015.02.014
    Here we describe the pharmacokinetics of piperacillin administered by continuous infusion (CI) versus intermittent bolus (IB) dosing in critically ill patients receiving continuous venovenous haemofiltration (CVVH) and compare the frequency of pharmacodynamic/pharmacokinetic (PK/PD) target attainment with each dosing strategy. This was a prospective pharmacokinetic trial in 16 critically ill patients with severe sepsis or septic shock undergoing CVVH and randomised to receive either CI or IB administration of a standard daily dose of piperacillin/tazobactam (11.25g/day on Day 1 followed by 9g/day). Serial blood samples were measured on two occasions. Piperacillin pharmacokinetics were calculated using a non-compartmental approach. Blood concentrations were compared with established PK/PD targets. On occasion 1 (Days 1-3 of therapy), IB administration resulted in significantly higher piperacillin peak concentrations (169 vs. 89mg/L; P=0.002), whereas significantly higher steady-state concentrations were observed in CI patients (83 vs. 57mg/L; P=0.04). Total clearance and clearance not mediated by CVVH were significantly higher with CI administration [median (interquartile range), 1.0 (0.7-1.1) and 0.8 (0.6-1.0)mL/kg/min; P=0.001 and 0.001, respectively]. The estimated unbound piperacillin concentrations were four times above the target susceptibility breakpoint (16mg/L) for the entire dosing interval (100%fT>4xMIC) in 87.5% of patients receiving CI administration (sampling occasion 1), compared with 62.5% of IB patients achieving the desired target (50%fT>4xMIC). Compared with IB dosing, and despite similar CVVH settings, CI administration of piperacillin results in a pharmacokinetic profile that may optimise outcomes for less susceptible pathogens.
    Matched MeSH terms: Metabolic Clearance Rate
  14. Moo KS, Radhakrishnan S, Teoh M, Narayanan P, Bukhari NI, Segarra I
    Yao Xue Xue Bao, 2010 Jul;45(7):901-8.
    PMID: 20931790
    Imatinib is an efficacious anticancer drug with a spectrum of potential antitumour applications limited by poor biodistribution at therapeutic concentrations to the tissues of interest. We assess the pharmacokinetic and tissue distribution profile of imatinib in a liposome formulation. Its single dose (6.25 mg x kg(-1)) in a liposome formulation was administered iv to male mice. Imatinib concentration was measured in plasma, spleen, liver, kidney and brain using a HPLC assay. Non-compartmental pharmacokinetic approach was used to assess the disposition parameters. The plasma disposition profile was biphasic with a plateau-like second phase. The AUC(0-->infinity) was 11.24 microg x h x mL(-1), the elimination rate constant (k(el)) was 0.348 h(-1) and the elimination half life (t(1/2)) was 2.0 h. The mean residence time (MRT) was 2.59 h, V(SS) was 1.44 L x kg(-1) and clearance was 0.56 L x h x kg(-1). Liver achieved the highest tissue exposure: CMAX = 18.72 microg x mL(-1); AUC(0-->infinity)= 58.18 microg x h x mL(-1) and longest t(1/2) (4.29 h) and MRT (5.31 h). Kidney and spleen AUC(0-->infinity) were 47.98 microg x h x mL(-1) and 23.46 microg x h x mL(-1), respectively. Half-life was 1.83 h for the kidney and 3.37 h for the spleen. Imatinib penetrated into the brain reaching approximately 1 microg x g(-1). Upon correction by organ blood flow the spleen showed the largest uptake efficiency. Liposomal imatinib presented extensive biodistribution. The drug uptake kinetics showed mechanism differences amongst the tissues. These findings encourage the development of novel imatinib formulations to treat other cancers.
    Matched MeSH terms: Metabolic Clearance Rate
  15. Sulaiman H, Abdul-Aziz MH, Roberts JA
    Semin Respir Crit Care Med, 2017 06;38(3):271-286.
    PMID: 28578552 DOI: 10.1055/s-0037-1602716
    Hospital-acquired pneumonia and ventilator-associated pneumonia continue to cause significant morbidity and mortality. With increasing rates of antimicrobial resistance, the importance of optimizing antibiotic treatment is key to maximize treatment outcomes. This is especially important in critically ill patients in intensive care units, in whom the infection is usually caused by less susceptible organisms. In addition, the marked physiological changes that can occur in these patients can cause serious changes in antibiotic pharmacokinetics which in turn alter the attainment of therapeutic drug exposures. This article reviews the various aspects of the pharmacokinetic changes that can occur in the critically ill patients, the barriers to achieving therapeutic drug exposures in pneumonia for systemically delivered antibiotics, the optimization for commonly used antibiotics in hospital- and ventilator-associated pneumonia, the agents that should be avoided in the treatment regimen, as well as the use of adjunctive therapy in the form of nebulized antibiotics.
    Matched MeSH terms: Metabolic Clearance Rate
  16. Tan SY, Kan E, Lim WY, Chay G, Law JH, Soo GW, et al.
    J Pharm Pharmacol, 2011 Jul;63(7):918-25.
    PMID: 21635257 DOI: 10.1111/j.2042-7158.2011.01296.x
    The pharmacokinetic interaction between metronidazole, an antibiotic-antiparasitic drug used to treat anaerobic bacterial and protozoal infections, and imatinib, a CYP3A4, P-glycoprotein substrate kinase inhibitor anticancer drug, was evaluated.
    Matched MeSH terms: Metabolic Clearance Rate
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