Month: December 2022

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

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

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

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

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

Gao, Zongming published the artcileAn In Vitro Dissolution Method for Testing Extended-Release Tablets Under Mechanical Compression and Sample Friction, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Critical quality attributes (CQAs); Extended-release (ER); Gastrointestinal (GI) condition; In vitro dissolution testing; Mechanical apparatus under GI condition (MAGIC) system; Medium flow-through configuration; Simulated GI compression and friction.

The release and dissolution of an active pharmaceutical ingredient (API) from the solid oral formulation into the gastrointestinal (GI) tract is critical for the drug′s absorption into systemic circulation. Extended-release (ER) solid oral dosage forms are normally subjected to phys. shear and grinding forces as well as pressure exerted by peristaltic movements when passing through the GI tract. The complex phys. contraction and sample friction exerted by the GI tract are not simulated well by compendial dissolution methods. These limitations render traditional in vitro dissolution testing unable to discriminate and predict a product′s in vivo performance. The objective of this study was to develop a dissolution method that better simulates the GI environment that products are subject to when taken by patients. A newly designed Mech. Apparatus under GI Conditions (MAGIC) was assembled with a dissolution platform and mech. capabilities to allow in vitro dissolution testing under sample contractions and friction. The dissolution platform, with medium flow-through configuration, was manufactured by 3D printing. A 60 mg polymer matrix-based ER nifedipine product was tested. To simulate GI physiol. conditions during the dissolution testing, the flow rate of the medium, and a combination of mech. compression with rotation induced sample friction at various rotation frequencies were explored. The polymer matrix-based nifedipine ER formulation used here failed its controlled release functionality in the simulated GI environment under mech. compression and sample friction. The results showed that the MAGIC system, with flow-through configuration under compression and sample friction, has advantages over compendial methods in testing ER solid oral formulations.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Critical quality attributes (CQAs); Extended-release (ER); Gastrointestinal (GI) condition; In vitro dissolution testing; Mechanical apparatus under GI condition (MAGIC) system; Medium flow-through configuration; Simulated GI compression and friction. 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

Teragawa, Hiroki published the artcileThe Significance of Recognizing Myocardial Bridge in the Coronary Spasm Diagnosis in Myocardial Infarction with Nonobstructive Coronary Arteries., Product Details of C17H18N2O6, the main research area is coronary spasm; myocardial bridge; myocardial infarction with nonobstructive coronary arteries; vasospastic angina.

A 61-year-old man experienced chest oppression for 1 hour. He was positive for troponin T and underwent emergent coronary angiography (CAG), which did not reveal significant coronary stenosis. He was diagnosed with myocardial infarction with nonobstructive coronary arteries (MINOCA). We performed a spasm-provocation test, which revealed a focal spasm at the segment of the myocardial bridge. After receiving a calcium-channel blocker, he exhibited a good clinical course. Coronary spasm is considered an underlying cause of MINOCA; therefore, the presence of a myocardial bridge may help with the diagnosis.

Internal medicine (Tokyo, Japan) published new progress about coronary spasm; myocardial bridge; myocardial infarction with nonobstructive coronary arteries; vasospastic angina. 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

Ibrahim, Mohammed H. published the artcileThe effectiveness of nifedipine/indomethacin combination therapy and nifedipine monotherapy for postponing preterm birth (25-34 weeks of gestation) in Sudanese women: a randomized clinical trial study protocol, SDS of cas: 21829-25-4, the main research area is Control trial; Indomethacin; Nifedipine; Preterm labor; Tocolytics.

Abstract: Background: Preterm birth is the most common cause of neonatal morbidity and mortality. Tocolytics are considered a standard treatment for women with threatened preterm delivery to allow time for maternal steroid administration and transfer to referral centers with neonatal intensive care units. However, there is controversy about the best tocolytic therapy to be considered as the first choice. The aim of this study is to compare the tocolytic effectiveness and tolerability of combination therapy with nifedipine and indomethacin vs. nifedipine monotherapy among Sudanese women with preterm labor (PTL) as well as to compare the possible neonatal outcomes associated with each drug. Methods/design: This is a randomized controlled clin. trial to be conducted in the Medani Maternity Hospital, Sudan. Women aged 18-40 years that are diagnosed with preterm labor and have a gestational age between 25 and 34 wk will be eligible to participate in this trial. The diagnosis of threatened PTL is defined as persistent uterine contractions “”(four contractions every 20 min or eight contractions every 60 min)”” with cervical changes “”(cervical effacement â‰?0% or cervical dilatation >two cm)””. Patients will be eligible regardless of the presentation of the fetus. It will be randomly decided whether participants receive nifedipine/indomethacin combination therapy or nifedipine monotherapy. The primary outcome is the number of women who do not deliver and do not need alternative tocolytic drug (terbutaline). The secondary outcome is an estimated association with neonatal morbidity and mortality. The sample size will be 117 subjects in each arm of the study, according to a type I error of 0.05 and a study power of 80%. Discussion: We expect higher effectiveness of the combination indomethacin/nifedipine tocolytic therapy compared with nifedipine monotherapy. We plan to suggest this combination therapy as the best option for postponing PTL. Trial registration: Clin. trial registration: PACTR202004681537890, date of registration: March 8, 2020.

BMC Pregnancy and Childbirth published new progress about Control trial; Indomethacin; Nifedipine; Preterm labor; Tocolytics. 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, SDS of cas: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Campochiaro, Corrado published the artcileAutoimmunity and immunodeficiency at the crossroad: autoimmune disorders as the presenting feature of selective IgM deficiency., HPLC of Formula: 21829-25-4, the main research area is connective tissue disease; immunology.

Selective immunoglobulin M deficiency (sIgMD) is an immunodeficiency with undefined pathogenesis and commonly presenting with recurrent infections. 1 The European Society for Immunodeficiencies Registry defines sIgMD as a serum IgM level repeatedly below 2 SD of normal with normal levels of serum IgA, IgG and IgG subclasses, normal vaccination responses, absence of T-cell defects and absence of causative external factors. Rarely it can also be associated with autoimmune diseases. 2-7 Here we describe a patient with primary sIgMD; who presented with multiple autoimmune diseases without a history of recurrent infections and we provide a short literature review on sIgMD and autoimmune diseases.

BMJ case reports published new progress about connective tissue disease; immunology. 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

Wang, Pengfei published the artcileThe fingerprints of nifedipine/isonicotinamide cocrystal polymorph studied by terahertz time-domain spectroscopy, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Cocrystal polymorph; Nifedipine; Quantum chemical calculations; Spectral fingerprints; Terahertz time-domain spectroscopy; Vibrational modes.

Cocrystal is constructed to improve physicochem. properties of active pharmaceutical ingredient and prevent polymorphism via intermol. interactions. However, recent examples on cocrystal polymorphs display significantly different properties. Even though some anal. techniques have been used to characterize the cocrystal polymorphic system, it remains unclear how intermol. interactions drive and stabilize the structure. In this work, we study the cocrystal polymorphs of nifedipine (NFD) and isonicotinamide (INA) using terahertz (THz) spectroscopy. Form I and form II of NFD-INA cocrystals show spectral fingerprints in THz region. Temperature-dependent THz spectra display distinguished frequency shifts of each fingerprint. Combined with solid-state d. functional theory (DFT) calculations, the exptl. fingerprints and their distinct responses to temperature are elucidated by specific collective vibrational modes. The vibrations of hydrogen bonding between dihydropyridine ring of NFD and INA are generally distributed below 1.5 THz, which play important roles in stabilizing cocrystal and preventing the oxidation of NFD. The rotations of Me group in NFD are widely distributed in the range of 1.5-4.0 THz, which helps the steric recognition. The results demonstrate that THz spectroscopy is a sensitive tool to discriminate cocrystal polymorphs. It has the potential to be used as a non-invasive technique for pharmaceutical screening.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Cocrystal polymorph; Nifedipine; Quantum chemical calculations; Spectral fingerprints; Terahertz time-domain spectroscopy; Vibrational modes. 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem