Category: pyridine-derivatives

Zhu, Yun-Ting published the artcileEffects of apatinib on the pharmacokinetics ofnifedipine and warfarin in patients with advancedsolid tumors, Formula: C17H18N2O6, the main research area is CYP2C9; CYP3A4; apatinib; drug-drug interaction; nifedipine; warfarin.

Background and Purpose: Apatinib is a small-mol. tyrosine kinase inhibitor for the treatment of recurrent or progressive advanced-stage gastric adenocarcinoma or gastroesophageal junction cancer. The in vitro inhibition studies suggested that apatinib exerted potent inhibition on CYP3A4 and CYP2C9. To evaluate the potential of apatinib as a perpetrator in CYP450-based drug-drug interactions in vivo, nifedipine and warfarin were, resp., selected in the present study as the probe substrates of CYP3A4 and CYP2C9 for clin. drug-drug interaction studies. Since hypertension and thrombus are common adverse effects of vascular targeting anticancer agents, nifedipine and warfarin are usually coadministered with apatinib in clin. practice. Methods: A single-center, open-label, single-arm, and self-controlled trial was conducted in patients with advanced solid tumors. The patients received a single dose of 30 mg nifedipine on Day 1/14 and a single dose of 3 mg warfarin on Day 3/16. On Day 9-21, the subjects received a daily dose of 750 mg apatinib, resp. The pharmacokinetics of nifedipine and warfarin in the absence or presence of apatinib was, resp., investigated. Results: Compared with the single oral administration, coadministration with apatinib contributed to the significant increases of AUC0-48h and Cmax of nifedipine by 83% (90% confidence interval [CI] 1.46-2.31) and 64% (90% CI 1.34-2.01), resp. Similarly, coadministration with apatinib contributed to the significant increases of AUC0-t and Cmax of S-warfarin by 92% (90% CI 1.68-2.18) and 24% (90% CI 1.10-1.39), resp. Conclusion: Concomitant apatinib administration resulted in significant increases in systemic exposure to nifedipine and S-warfarin. Owing to the risk of pharmacokinetic drug-drug interactions based on CYP3A4/CYP2C9 inhibition by apatinib, caution is advised in the concurrent use of apatinib with either CYP2C9 or CYP3A4 substrates.

Drug Design, Development and Therapy published new progress about CYP2C9; CYP3A4; apatinib; drug-drug interaction; nifedipine; warfarin. 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

Fu, Chengxiao published the artcilePopulation Pharmacokinetic Modelling for Nifedipine to Evaluate the Effect of Parathyroid Hormone on CYP3A in Patients with Chronic Kidney Disease., Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is CYP3A; chronic kidney disease; nifedipine; parathyroid hormone; population pharmacokinetic.

Purpose: Parathyroid hormone (PTH) can induce the downregulation of CYP3A in chronic kidney disease (CKD). Nevertheless, the effect of PTH on CYP3A-mediated clearance pathways from a clinical perspective remains unclear. Methods: This study employed population pharmacokinetic (PopPK) modeling to delineate potential changes in CYP3A activity in patients with CKD. Pharmacokinetic data for nifedipine, a typical CYP3A substrate, as well as covariate information, were prospectively collected from 157 patients with a total of 612 concentrations. PopPK data analysis was performed using a nonlinear mixed-effects model. Results: The pharmacokinetics of nifedipine were optimally described according to a one-compartment model with zero-order absorption and first-order elimination. The estimated population parameters (and interindividual variability) were apparent clearance (CL/F) 49.61 L/h (58.33%) and apparent volume of distribution (V/F) 2300.26 L (45.62%), and the PTH level negatively correlated with CL/F. In comparison with the reference level, it was observed that the dosage of nifedipine should be reduced with the maximum boundary value of PTH, after a Monte Carlo simulation. Conclusion: This study provides insight into the effects of PTH on CYP3A-mediated clearance pathways. Moreover, PTH could be used as a guide for the appropriate administration of CYP3A eliminated drugs in patients with CKD.

Drug design, development and therapy published new progress about CYP3A; chronic kidney disease; nifedipine; parathyroid hormone; population pharmacokinetic. 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, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, C. S. published the artcileReaction of dehydroacetic acid with ammonia, Quality Control of 33259-24-4, the main research area is dehydroacetic acid ammonia reaction; nicotinic acid aminodimethyl; pyridone aminodimethyl; lutidine amino.

Dehydroacetic acid reacts with aqueous NH3 at 200° to give the major product 2,6-dimethyl-4-pyridinol and 6 minor by-products, i.e., 4-amino- and 4-hydroxy-2,6-dimethylnicotinic acids, 4-amino-, 4-hydroxy-, and 3-acetyl-4-hydroxy-6-methyl-2-pyridones, and 4-amino-2,6-lutidine. Isolation and synthesis of the by-products, proof of the structures and the mechanistic interpretation of their formation are discussed.

Tetrahedron published new progress about dehydroacetic acid ammonia reaction; nicotinic acid aminodimethyl; pyridone aminodimethyl; lutidine amino. 33259-24-4 belongs to class pyridine-derivatives, name is 3-Bromo-2,6-dimethylpyridin-4-amine, and the molecular formula is C7H9BrN2, Quality Control of 33259-24-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Morikawa, Satoru published the artcileTreatment of calcium channel blocker-induced gingival overgrowth without modifying medication., Product Details of C17H18N2O6, the main research area is dentistry and oral medicine; hypertension.

Gingival overgrowth is a common side effect of calcium channel blockers used in the treatment of cardiovascular diseases. While controversial, management includes discontinuing the calcium channel blocker. We report the case of a 66-year-old Japanese man with hypertension and type 2 diabetes mellitus who was diagnosed with severe periodontitis covering almost all the teeth. The patient had been on nifedipine (40 mg/day) and amlodipine (10 mg/day) medication for 5 years. With his physician’s consent, nifedipine was discontinued during his treatment for periodontitis, which consisted of oral hygiene instructions and scaling and root planing on all areas. Gingivectomy was performed on the areas of hard fibrous swelling. Nifedipine was resumed during periodontal treatment when the patient’s hypertension worsened. His periodontal scores improved when he resumed treatment. We report that significant improvement in gingival overgrowth can occur with basic periodontal treatment, surgery and sustained intensive follow-up without adjusting calcium channel blockers.

BMJ case reports published new progress about dentistry and oral medicine; hypertension. 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, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gainder, Shalini published the artcileTo study the changes in fetal hemodynamics with intravenous labetalol or nifedipine in acute severe hypertension., Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Doppler; Hypertension; Labetalol; Nifedipine; Pregnancy.

OBJECTIVE: To compare the efficacy of intravenous labetalol or oral nifedipine in treatment of acute maternal hypertension and study the fetal hemodynamic changes using color Doppler ultrasound that follows treatment. STUDY DESIGN: Thirty women with severe preeclampsia having acute hypertension (more than or equal to 160/105 mmHg) were randomized in 2 groups to receive intravenous labetalol or oral nifedipine until blood pressure was lowered to less than or equal to 140/90 mmHg. Doppler vascular indices namely pulsatility index, resistance index, S/D ratio of umbilical (UA) and middle cerebral artery (MCA) were measured baseline at the time of acute severe hypertension and repeated after control of blood pressure, to assess the changes in fetal hemodynamics if any with labetalol or nifedipine. RESULTS: Both nifedipine and labetalol were found to be effective when used for rapid control of blood pressure. Mean age of women in both groups and mean gestational age was statistically comparable. No change in fetal heart rate before and after treatment was observed in both groups. Doppler vascular indices of UA and MCA showed no significant changes as compared to baseline values in both groups. CONCLUSION: The use of labetalol and nifedipine were not related to any significant changes in fetal Doppler, which is reassuring about the safety of these drugs when treating acute severe hypertension in pregnancy. Choice between these two drugs should be based on cost, availability respective contraindications, and clinician’s experience.

Pregnancy hypertension published new progress about Doppler; Hypertension; Labetalol; Nifedipine; Pregnancy. 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, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Doherty, Anne published the artcileHemodynamic Complications in Pregnancy: Preeclampsia and Beyond., Formula: C17H18N2O6, the main research area is Endothelial inflammation; Fetal growth restriction; Hemodynamic adaptation; Preeclampsia; Vascular remodeling.

Normal pregnancy is a complex and dynamic process that requires significant adaptation from the maternal system. Failure of this adaptive process in pregnancy contributes to many pregnancy related disorders, including the hypertensive disorders of pregnancy. This article discusses placental development and how abnormalities in the process of vascular remodeling contribute to the multisystem maternal and fetal disease that is preeclampsia and fetal growth restriction. We review some of the consequences of this condition on the mother and fetus, aspects of the clinical management of preeclampsia and how it can influence both mother and infant in the postnatal period and beyond.

Clinics in perinatology published new progress about Endothelial inflammation; Fetal growth restriction; Hemodynamic adaptation; Preeclampsia; Vascular remodeling. 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

Javed, Arslan published the artcileDevelopment of Simple Dissolution Methods for Felodipine and Combined Amlodipine Besylate-Indapamide Extended Release Tablets without Stationary (Felodipine) Basket., Synthetic Route of 72509-76-3, the main research area is Felodipine basket; amlodipine besylate; dissolution; felodipine; indapamide; similarity factor; stationary hanging basket.

BACKGROUND: The dissolution method for certain drugs needs specialized conditions. Dissolution testing for felodipine extended release (ER) tablets (Plendil® 5 mg) and amlodipine-indapamide fixed dose (Natrilam®, 5/1.5 mg) ER tablets requires the use of a stationary (felodipine) basket in USP Apparatus II. OBJECTIVE: The study aimed to develop simple methods for Plendil® and Natrilam® without the use of a felodipine basket. METHODS: The dissolution profiles obtained from different media and paddle speeds were used to compute miscellaneous dissolution parameters and were compared to those obtained from standard (existing) methods using a felodipine basket. RESULTS: The f1, f2, and bootstrap f2 (5th % percentile) values for Plendil® 2.47, 88.17, and 54.62, respectively, and all other dissolution factors revealed similarity between standard and the selected test method with 1% Tween 20 at 50 rpm. For Natrilam®, f1 and f2 and bootstrap f2 5.13, 72.92, and 62.67, respectively, and all other dissolution parameters showed similarity of the standard and selected test method using 0.1N HCl media having 0.38 gm/L EDTA with a sinker at 100 rpm. Release of products assumed zero-order and Weibull model, respectively. CONCLUSION: Test dissolution methods for Plendil® and Natrilam® tablets produced equivalent dissolution profiles compared to their respective standard methods with stationary basket USP Apparatus II.

Current pharmaceutical design published new progress about Felodipine basket; amlodipine besylate; dissolution; felodipine; indapamide; similarity factor; stationary hanging basket. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Alavifard, Sepand published the artcileFirst-line antihypertensive treatment for severe hypertension in pregnancy: A systematic review and network meta-analysis., Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Antihypertensive agents; Hydralazine; Labetalol; Network meta-analysis; Nifedipine; Pregnancy-induced hypertension.

BACKGROUND: Hydralazine, labetalol, and nifedipine are the recommended first-line treatments for severe hypertension in pregnancy. While all three are effective, there is a lack of sufficient evidence regarding their comparative safety and efficacy. OBJECTIVE: To determine the comparative safety and efficacy of the first-line treatment options for severe hypertension in pregnancy. METHODS: A systematic search of Medline, Embase, and Cochrane Central Register of Controlled Trials up to May 31, 2018 was conducted. RCTs in pregnancy comparing a first-line antihypertensive agent to another first-line agent for the treatment of severe hypertension in pregnancy. Screening, data abstraction, and quality assessment were done by two independent reviewers. To estimate relative effects from all available evidence, a Bayesian network meta-analysis with vague priors was conducted. MAIN RESULTS: Of the 1330 publications identified, 17 RCTs comprised of a total of 1591 women met our selection criteria. For successful treatment of severe hypertension, nifedipine was found to be superior to hydralazine (OR 4.13 [95% CrI 1.01-20.75]) but not labetalol (OR 3.43 [95% CrI 0.94-19.95]). This was not associated with an increased risk for caesarean delivery or maternal side effects. There was no significant difference between labetalol and hydralazine. CONCLUSIONS: Given the results of this systematic review and network meta-analysis, maternity care providers should feel comfortable initiating management of severe hypertension in pregnancy using oral nifedipine.

Pregnancy hypertension published new progress about Antihypertensive agents; Hydralazine; Labetalol; Network meta-analysis; Nifedipine; Pregnancy-induced hypertension. 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, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wautlet, Cynthie K published the artcileHypertensive Crisis in Pregnancy., Related Products of pyridine-derivatives, the main research area is Antihypertensive treatment; Hypertension; Hypertensive crisis; Preeclampsia; Pregnancy.

Severe hypertension in pregnancy is a medical emergency, defined as systolic blood pressure (BP) â‰?160 mm Hg and/or diastolic BP â‰?110 mm Hg taken 15 minutes to 4 or more hours apart. Outside pregnancy, acute severe hypertension (HTN) is defined as a BP greater than 180/110 to 120 reproducible on 2 occasions. The lower threshold for severe HTN in pregnancy reflects the increased risk for adverse outcomes, particularly maternal stroke and death, and may be a source of under-recognition and treatment delay, particularly in nonobstetrical health care settings. Once a severe hypertension episode is recognized, antihypertensive therapy should be initiated as soon as feasibly possible, at least within 30 to 60 minutes. Intravenous (IV) labetalol, hydralazine, and oral immediate-release nifedipine are all recommended first-line agents and should be administered according to available institutional protocols and based on provider knowledge and familiarity.

Obstetrics and gynecology clinics of North America published new progress about Antihypertensive treatment; Hypertension; Hypertensive crisis; Preeclampsia; Pregnancy. 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

Maurya, Priyanka published the artcileAppraisal of Felodipine Nanocrystals for Solubility Enhancement and Pharmacodynamic Parameters on Cadmium Chloride Induced Hypertension in Rats., Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Antisolvent precipitation; cadmium chloride; crystallinity; felodipine; heart rate variability; heat of fusion.

AIM: Felodipine (FDP), an antihypertensive drug possesses low water solubility and extensive first-pass metabolism leading to poor bioavailability. This impelled us to improve its solubility, bioavailability, and pharmacodynamic properties through the Nanocrystal (NC) approach. METHODS: FDP-NC were prepared with Poloxamer F125 (PXM) by the antisolvent precipitation method. The experimental setup aimed at fine-tuning polymer concentration, the proportion of antisolvent to solvent, and the duration of ultrasonication for NC formulation. RESULTS: Optimized formulation was characterized for particle size, solubility, and PDI. Particle reduction of 74.96 times was achieved with a 9X solubility enhancement as equated to pure FDP. The morphology of NC was found to be crystalline through scanning electron microscopy observation. The formation of the crystal lattice in FDP-NC was further substantiated by the XRD and DSC results. Lowering of the heat of fusion of FDP-NC is a clear indication of size reduction. The stability studies showed no substantial change in physical parameters of the FDP-NC as assessed by particle size, zeta potential, and drug content. CONCLUSION: The crystalline nature and improved solubility of FDP-NC improve the dissolution profile and pharmacodynamic data. The stability study data ensure that FDP-NC can be safely stored at 25°C. It is revealed that FDP-NC had a better release profile and improved pharmacodynamic effects as evident from better control over heart rate than FDP.

Current drug delivery published new progress about Antisolvent precipitation; cadmium chloride; crystallinity; felodipine; heart rate variability; heat of fusion. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem