Tag: M.W=200-350

Andrews, L. M. published the artcileA population pharmacokinetic model to predict the individual starting dose of tacrolimus in adult renal transplant recipients, Related Products of pyridine-derivatives, the main research area is tacrolimus renoprotectant CYP3A4 albumin kidney transplantation adult; cytochrome P450 enzymes; genetics and pharmacogenetics; immunosuppression Immunology; pharmacokinetics; population analysis; renal transplantation.

To describe the pharmacokinetics of tacrolimus immediately after kidney transplantation, and to develop a clin. tool for selecting the best starting dose for each patient. Data on tacrolimus exposure were collected for the first 3 mo following renal transplantation. A population pharmacokinetic anal. was conducted using nonlinear mixed-effects modeling. Demog., clin. and genetic parameters were evaluated as covariates. A total of 4527 tacrolimus blood samples collected from 337 kidney transplant recipients were available. Data were best described using a two-compartment model. The mean absorption rate was 3.6 h-1, clearance was 23.0 l h-1 (39% interindividual variability, IIV), central volume of distribution was 692 l (49% IIV) and the peripheral volume of distribution 5340 l (53% IIV). Interoccasion variability was added to clearance (14%). Higher body surface area (BSA), lower serum creatinine, younger age, higher albumin and lower haematocrit levels were identified as covariates enhancing tacrolimus clearance. Cytochrome P 450 (CYP) 3A5 expressers had a significantly higher tacrolimus clearance (160%), whereas CYP3A4*22 carriers had a significantly lower clearance (80%). From these significant covariates, age, BSA, CYP3A4 and CYP3A5 genotype were incorporated in a second model to individualize the tacrolimus starting dose: Dosemg=222nghml-1*22.5lh-1*1.0ifCYP3A5*3/*3or1.62ifCYP3A5*1/*3orCYP3A5*1/*1*1.0ifCYP3A4*1or unknownor0.814ifCYP3A4*22*Age56-0.50*BSA1.930.72/1000 Both models were successfully internally and externally validated. A clin. trial was simulated to demonstrate the added value of the starting dose model. For a good prediction of tacrolimus pharmacokinetics, age, BSA, CYP3A4 and CYP3A5 genotype are important covariates. These covariates explained 30% of the variability in CL/F. The model proved effective in calculating the optimal tacrolimus dose based on these parameters and can be used to individualize the tacrolimus dose in the early period after transplantation.

British Journal of Clinical Pharmacology published new progress about Adult, mammalian. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mao, Junjun published the artcileIncorporating nonlinear kinetics to improve predictive performance of population pharmacokinetic models for ciclosporin in adult renal transplant recipients: A comparison of modelling strategies, Related Products of pyridine-derivatives, the main research area is ciclosporin renoprotectant pharmacokinetic renal transplantation; Ciclosporin; Modelling strategies; Nonlinear kinetics; Population pharmacokinetics.

Ciclosporin has been shown to follow nonlinear pharmacokinetics (PK) in renal transplant recipients who received ciclosporin (Neoral, Novartis)-based triple immunosuppressive therapy. Some of these nonlinear properties have not been fully considered in population PK (popPK) anal. Therefore, the aim of this study was to determine the potential influence of nonlinearity and the functional forms of covariates on model predictability as well as to analyze multiple nonlinear factors in the in vivo process. A total of 2969 ciclosporin whole-blood measurements, including 1328 pre-dose and 1641 2-h post-dose concentrations, were collected from 173 patients who underwent their first renal transplantation. Four popPK models based on different modeling strategies were developed to investigate the discrepancy between empirical and theory-based, linear and nonlinear compartmental kinetic models and empirical formulas on model predictability. Prediction and simulation-based diagnostics (prediction-corrected visual predictive checks) were performed to determine the stability and predictive performance of these four models. Model predictability improved when nonlinearity was considered. The theory-based nonlinear model which incorporated nonlinear property based on known theor. relationships performed better than the other two compartmental models. The nonlinear Michaelis-Menten model showed a remarkable improvement in predictive performance compared to the other three compartmental models. The saturated binding of ciclosporin to erythrocytes, auto-inhibition induced by the inhibitory effects of ciclosporin on cytochrome P 450 3A4/P-glycoprotein may have contributed to the nonlinearity. Ciclosporin-prednisolone drug interaction should be given serious consideration in clin. settings. Incorporation of nonlinear properties is likely to be a promising approach for improving ciclosporin model predictability. Theory-based modeling is helpful to improve model predictability. However, ciclosporin nonlinear kinetics resources need further investigation.

European Journal of Pharmaceutical Sciences published new progress about Adult, mammalian. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Giantin, Mery published the artcileFunctional impact of cytochrome P450 3A (CYP3A) missense variants in cattle, Formula: C17H18N2O6, the main research area is CYPA missense mutation testosterone nifedipine mol docking.

Cytochrome P 450 3A is the most important CYP subfamily in humans, and CYP3A4/CYP3A5 genetic variants contribute to inter-individual variability in drug metabolism However, no information is available for bovine CYP3A (bCYP3A). Here we described bCYP3A missense single nucleotide variants (SNVs) and evaluated their functional effects. CYP3A28, CYP3A38 and CYP3A48 missense SNVs were identified in 300 bulls of Piedmontese breed through targeted sequencing. Wild-type and mutant bCYP3A cDNAs were cloned and expressed in V79 cells. CYP3A-dependent oxidative metabolism of testosterone (TST) and nifedipine (NIF) was assessed by LC-MS/MS. Finally, SNVs functional impact on TST hydroxylation was measured ex vivo in liver microsomes from individually genotyped animals. Thirteen missense SNVs were identified and validated. Five variants showed differences in CYP3A catalytic activity: three CYP3A28 SNVs reduced TST 6β-hydroxylation; one CYP3A38 variant increased TST 16β-hydroxylation, while a CYP3A48 SNV showed enhanced NIF oxidation Individuals homozygous for rs384467435 SNV showed a reduced TST 6β-hydroxylation. Mol. modeling showed that most of SNVs were distal to CYP3A active site, suggesting indirect effects on the catalytic activity. Collectively, these findings demonstrate the importance of pharmacogenetics studies in veterinary species and suggest bCYP3A genotype variation might affect the fate of xenobiotics in food-producing species such as cattle.

Scientific Reports published new progress about Allele frequency. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Yilei published the artcileCYP3A5 genotype-dependent drug-drug interaction between tacrolimus and nifedipine in Chinese renal transplant patients, Category: pyridine-derivatives, the main research area is tacrolimus nifedipine human renal transplant CYP3A5 genotype drug interaction; CYP3A5; drug-drug interaction; nifedipine; renal transplantation; tacrolimus.

The drug-drug interactions (DDIs) of tacrolimus greatly contributed to pharmacokinetic variability. Nifedipine, frequently prescribed for hypertension, is a competitive CYP3A5 inhibitor which can inhibit tacrolimus metabolism The objective of this study was to investigate whether CYP3A5 genotype could influence tacrolimusnifedipine DDI in Chinese renal transplant patients. All renal transplant patients were divided into CYP3A5*3/*3 homozygotes (group I) and CYP3A5*1 allele carriers (CYP3A5*1/*1 + CYP3A5*1/*3) (group II). Each group was subdivided into patients taking tacrolimus co-administered with nifedipine (CONF) and that administrated with tacrolimus alone (Controls). Tacrolimus trough concentrations (C0) were measured using high performance liquid chromatog. A retrospective anal. compared tacrolimus dose (D)-corrected trough concentrations (C0) (C0/D) between CONF and Controls in group I and II, resp. At the same time, a multivariate line regression anal. was made to evaluate the effect of variates on C0/D. In this study, a significant DDI between tacrolimus and nifedipine with respect to the CYP3A5*3 polymorphism was confirmed. In group I (n = 43), the C0/D of CONF was significantly higher than in Controls [225.2 ± 66.3 vs. 155.1 ± 34.6 ng/mL/(mg/kg); p = 0.002]. However, this difference was not detected in group II (n = 27) (p = 0.216). The coadministrated nifedipine and CYP3A5*3/*3 homozygotes significantly increased tacrolimus concentrations in multivariate line regression anal. A CYP3A5 genotype-dependent DDI was found between tacrolimus and nifedipine. Therefore, personalized therapy accounting for CYP3A5 genotype detection as well as therapeutic drug monitoring are necessary for renal transplant patients when treating with tacrolimus and nifedipine.

Frontiers in Pharmacology published new progress about Allele frequency. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Teimouri, Arezou published the artcileStability of Compounded Topical Nifedipine in Cream, Gel, and Ointment Bases., HPLC of Formula: 21829-25-4, the main research area is .

The objective of this study was to investigate the stability of compounded nifedipine cream in gel and ointment formulations dispensed in white plastic and glass amber jars. Extemporaneously compounded nifedipine cream (Glaxal Base), gel (K-Y Jelly), and ointment (Aquaphor) in white plastic and glass amber jars were stored at 4°C, 23°C, and 40°C. We determined potency on days 0, 7, 14, 30, 60, and 90, and subsequently assigned beyond-use-dates based on United States Pharmacopeia recommendations, organoleptic properties, and pH changes. Nifedipine potency in cream and ointment stored in white plastic jars was within ±10% of initial for 90 days (excluding day 14 for cream). In glass amber jars, potency was outside the acceptable range by day 14 at 23°C but within range for 90 days at 4°C (excluding day 30). Nifedipine potency was maintained for 90 days in both jars at 23°C and 4°C (excluding day 30) and in white plastic jars at 40°C, but 60 days stored in glass amber jars. The pH of formulations was stable with changes of less than 1-unit pH. At 40°C, a significant decrease in apparent viscosity of cream was evident on day 90. There was a decrease in apparent viscosity and phase separation of the ointment at 40°C and an increase in apparent viscosity (difficult to mix) at 4°C on day 14 onwards. Significant organoleptic changes were observed by day 7 at 40°C (decrease in apparent viscosity and abnormal odor by day 90), day 30 at 4°C (thicker consistency), and day 90 at 23°C (abnormal odor). Storage in white plastic jars at 23°C is recommended for compounded topical nifedipine cream and ointment (for 90 days), and for gel (60 days).

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Teimouri, Arezou published the artcileDrug-release Assessment of Compounded Topical Nifedipine and Diltiazem in Commonly Used Bases for Wound Healing., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is .

The objective of this study was to determine release profiles of extemporaneously compounded nifedipine and diltiazem in commonly used bases in pharmacy practice. Release of nifedipine 0.2%, 2%, and 10% (w/w) from Glaxal Base, K-Y Jelly, and Aquaphor Healing Ointment, and of diltiazem 2% (w/w) from GlaxalBase, hydroxyethyl cellulose-based gel, and white petrolatum was quantified using the Franz-cell diffusion system. The cumulative release was determined at 0.5 hour, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, and 6 hours. Two-way ANOVA with Tukey’s posthoc test was used for statistical analyses, with a P-value of <0.05 considered significant. At a 0.2% concentration, cumulative nifedipine release was highest from Glaxal Base. At 2% and 10% concentrations, nifedipine release was highest from K-Y Jelly, although this was only significantly different from Glaxal Base at 6 hours and 1.5 hours, 4 hours, 6 hours (P<0.05), respectively. Diltiazem release from Glaxal Base and white petrolatum was significantly lower than the gel (P<0.05). No significant difference in diltiazem release from Glaxal Base at 0.5 hour was observed versus white petrolatum (P>0.05). Nifedipine and diltiazem release both followed Higuchi’s mathematical model with the highest coefficient of determination (R2) for all formulations. Of the bases studies, Glaxal Base is the recommended base for compounding topical nifedipine (0.2%). For higher concentrations of nifedipine (2% and10%), both Glaxal Base and K-Y Jelly are suitable options for base selection. A hydroxyethylcellulose-based gel is recommended for topical diltiazem (2%).

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Riepl, Mike published the artcileA Compendium of Compounding Agents and Formulations, Part 4: Nifedipine and Pentoxifylline., Category: pyridine-derivatives, the main research area is .

The medical, economic, and social effects of painful chronic wounds such as anal fissures, which frequently prove refractory to treatment with commercially available medications, are often underestimated by clinicians. Those types of injuries, which afflicted individuals are often reluctant to discuss with healthcare providers, can lead to a greatly restricted lifestyle; result in depression, anxiety, social isolation, and embarrassment; require extended or repeated hospital stays; and create a financial burden for the patient and for society. Because interpatient variables can preclude the effectiveness of standardized mass-produced wound-healing products, a compounded formulation that can be formulated to include drugs proven effective in safe but off-label uses and that can be modified as patients’ medical needs require may achieve the therapeutic goal. In this report, 2 such agents shown to promote wound healing are profiled: the vasodilator nifedipine, a first-generation calcium channel blocker that is used to treat hypertension and angina pectoris; and pentoxifylline, a synthetic dimethylxanthine derivative that facilitates vasodilation, improves erythrocyte flexibility, enhances blood flow, and reduces blood viscosity. Formulations that incorporate those drugs, which are underrecognized as effective healing agents when compounded as directed, are included for easy reference.

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Y published the artcileRegulation of magnesium sulfate combined with nifedipine and labetalol on disease-related molecules in serum and placenta in the treatment of preeclampsia., HPLC of Formula: 21829-25-4, the main research area is .

OBJECTIVE: To explore the regulatory effect of magnesium sulfate combined with nifedipine and labetalol on disease-related molecules in serum and placenta in the treatment of preeclampsia. PATIENTS AND METHODS: Altogether 100 patients with preeclampsia admitted to the Children & Women’s Healthcare of Laiwu City were selected. They were divided into control group and experimental group according to different treatment methods. Among them, 51 patients in the control group were treated with magnesium sulfate combined with nifedipine, and 49 patients in the experimental group were treated with labetalol on the basis of the treatment in the control group. The therapeutic effects of the two methods were compared. The levels of the following factors in the two groups were compared: kallikrein expression, pregnancy-associated plasma protein A (PAPP-A), pregnancy-specific β1 glycoprotein (SPI), placental growth factor (PLGF), human placental prolactin (HPL), transforming growth factor β1(TGF-β1), vascular cell adhesion molecule 1 (VCAM-1) and E-selectin in serum and placenta tissues. RESULTS: After treatment, the blood pressure in the experimental group was lower than that in the control group (p<0.05). The expression of kallikrein in serum and placental tissue of the patients in the experimental group was higher than that of the patients in the control group (p<0.05); PAPP-A level was lower than that in the control group (p<0.05); TGF-β1 level was higher than that in the control group (p<0.05); VCAM-1 and E-selectin were lower than those in the control group (p<0.05), and kallikrein and TGF-β1 in serum and placenta in the non-occurrence group were higher than those in the occurrence group (p<0.05). The serum and placenta PAPP-A, VCAM-1, and E-selectin in the non-occurrence group were lower than those in the occurrence group (p<0.05). CONCLUSIONS: Magnesium sulfate combined with nifedipine and labetalol has good efficacy in the treatment of preeclampsia. They can promote the expression of endogenous kallikrein, reduce the level of pregnancy-related hypertension predictors, and weaken the infiltration ability of cytotrophoblasts. European review for medical and pharmacological sciences published new progress in MEDLINE about 21829-25-4, 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Zhenzhen published the artcileCase Report: Optical Coherence Tomography Can Find Typical Features in Pregnancy-induced Hypertension with Retinopathy., Quality Control of 21829-25-4, the main research area is .

SIGNIFICANCE: Pregnancy-induced hypertension is a unique yet common complication in pregnant women and may cause retinopathy. Optical coherence tomography (OCT) may help find the features of retinopathy that are difficult to observe through fundus examination. Not all patients can fully recover from retinopathy. PURPOSE: This report describes a case of pregnancy-induced hypertension with retinopathy and represents the features of retinopathy in OCT and fundus fluorescein angiography. CASE REPORT: A 29-year-old pregnant woman presented with bilateral blurred vision and xanthopsia 2 days before her induced labor; she was also diagnosed as pre-eclamptic in the obstetrics department. The vision in her right eye was 20/33, and that in her left eye was 20/20. Fundus fluorescein angiography showed scattered-dot hypofluorescence around the disc at an early stage, and needle-like hyperfluorescence gradually appeared near the disc with late-stage fluorescein leakage in both eyes. Optical coherence tomography revealed multiple shallow retinal detachments with hyperreflective bright spots in the outer retina and clumped hyperreflective materials on the retinal pigment epithelium (RPE). CONCLUSIONS: Typical findings and some tiny changes in the outer retina and RPE can be observed through spectral-domain OCT. The clumped hyperreflective deposits in the outer retina may be by-products of RPE swelling and necrosis that lead to barrier dysfunctions and fluid leakage. These described features may help diagnose retinopathy from pregnancy-induced hypertension. Although it is a self-limited disease, the disruptions in the ellipsoid and interdigitation zones may not fully recover and result in reduced visual dysfunction. Therefore, control of hypertension is indicated.

Optometry and vision science : official publication of the American Academy of Optometry published new progress in MEDLINE about 21829-25-4, 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Quality Control of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Ruonan published the artcileBibliometric analysis of research trends and characteristics of drug-induced gingival overgrowth., Category: pyridine-derivatives, the main research area is Scopus; bibliometric; citation analysis; drug-induced gingival overgrowth; research trends.

Objectives: Drug-induced gingival overgrowth (DIGO) is a frequent adverse medication reaction that is generally caused by cyclosporine, phenytoin, and nifedipine, which belong to the category of immunosuppressants, anticonvulsants, and calcium channel blockers, respectively. This bibliometric analysis aims to depict the main citation characteristics and analyze the research trends in DIGO investigations. Methods: An exhaustive search was performed in the Scopus database to create the bibliometric list of DIGO in the syntax. Furthermore, the information related to the number of citations, drugs related to DIGO, study topic and design, authorship, publication year, journal, contributing institution, country of origin, and the department was extracted. Results: In total, 399 papers on DIGO were retrieved in this study. The total number of citations and that after the removal of self-citations were 7,814 and 7,314, respectively. The mean number of citations was 19.6 in a range of 0-608. The main paper types were articles (76.94%) and reviews (19.55%). A remarkable increasing trend in the number of citations has been observed since 1994. Cyclosporine (44.89%) is the most commonly used drug that shares a close relationship with DIGO, followed by phenytoin (18.22%), nifedipine (17.93%), and amlodipine (6.81%). The review (27.82%) type constituted the most widely used design in the DIGO studies. According to the top 20 keywords, the risk factors and pathogenesis of DIGO have been prominent topics of research works for several years. Conclusions: This bibliometric analysis will facilitate the understanding of researchers and clinicians, especially those at the beginning of their careers in periodontology on DIGO, by identifying landmark research and providing an overview of this field.

Frontiers in public health published new progress about Scopus; bibliometric; citation analysis; drug-induced gingival overgrowth; research trends. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem