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Preterm labor, defined as contractions occurring every 5–10 minutes with cervical changes before the 37th week of estimated gestation, is a significant cause of perinatal mortality. This meta-analysis aims to evaluate the effectiveness and safety of magnesium sulfate compared to nifedipine in managing preterm labor. The systematic review protocol was registered with PROSPERO (CRD42023422419). Manuscripts published up to September 2024 were systematically searched in databases. Dichotomous data were pooled as odds ratios using a random-effects model with the Mantel-Haenszel method, while continuous data were analyzed as mean ± standard deviation values, mean differences, and standardized mean differences using inverse-variance fixed-effects analysis. Fifteen randomized clinical trials (RCTs) were included, enrolling a total of 2,186 pregnant women. Nifedipine showed a greater effect compared to a 4-gram IV dose of magnesium sulfate. However, the efficacy of these tocolytics in prolonging pregnancy by 48 hours did not significantly differ between nifedipine and a 6-gram IV dose of magnesium sulfate. Additionally, magnesium sulfate was associated with more adverse drug reactions. The moderate certainty of evidence found here requires confirmation in large, adequately powered RCTs. [ABSTRACT FROM AUTHOR]

Cytochrome P450 3A (CYP3A) enzymes catalyze the metabolism of a wide range of endogenous and exogenous compounds. Genetic variations in the 3 CYP3A isoforms (CYP3A28, CYP3A74, and CYP3A76) may influence their expression and activity, leading to inter-individual differences in xenobiotic metabolism. In domestic cattle, understanding how genetic variations modulate CYP3A activity is crucial for both its therapeutic implications (clinical efficacy and adverse drug effects) and food safety (residues in foodstuff). Here, we updated the variant calling of CYP3As in 300 previously sequenced Piedmontese beef cattle, using the most recent reference genome, which contains an updated, longer sequence for CYP3A28. All but one previously identified missense variants were confirmed and a new variant, R105W in CYP3A28, was discovered. Through computational mutagenesis and molecular docking, we computationally predicted the impact of all identified CYP3A variant enzymes on protein stability and their affinity for aflatoxin B1 (AFB1), a potent carcinogen and food contaminant. For CYP3A28, we also computationally predicted its affinity for the probe substrate nifedipine (NIF). We found that CYP3A28 with R105W variant cannot accommodate NIF nor AFB1 in the binding pocket, thus affecting their metabolism. Our work provides computational foundation and prioritized ranking of CYP3A variants for future experimental validations. [ABSTRACT FROM AUTHOR]

ABO group incompatibility at the time of transfusion of blood products carries risks ranging from mild adverse reactions to death of the patient. In modern obstetrics, the leading cause of death is obstetric hemorrhage, for which uterotonics, compression sutures, arterial ligatures, solutions, and blood products are used. For this reason, it is necessary to know the blood group . and Rh of each patient admitted for obstetric surgery and have her sign a consent form for transfusion of blood or blood derivatives, explaining all the adverse effects that may occur in the event of complications. We describe a case of postpartum transfusion with a hemolytic reaction due to ABO incompatibility and its clinical management. [ABSTRACT FROM AUTHOR]

Yiqi Fumai lyophilized injection (YQFM), a compound traditional Chinese medicine prescription derived from "Sheng Mai Powder," is approved for the treatment of cardiovascular diseases. YQFM is usually prescribed in combination with some Western medicines to treat patients, such as aspirin, nifedipine, and clopidogrel. However, the herb–drug interactions (HDIs) of YQFM are still unclear. We determined the effect of YQFM on drug metabolism‐related CYP450 enzymes by in vitro assays. And the effects of YQFM on the pharmacokinetics of aspirin, nifedipine, or clopidogrel were analyzed in rats, as well as the effect of YQFM on the prothrombin time of aspirin or clopidogrel, to evaluate the safety and efficacy of co‐administration. Our study indicated that the clinical dose of YQFM did not significantly influence the relevant CYP450 isoenzymes. Besides, YQFM had no effect on the pharmacokinetics of aspirin, nifedipine, or clopidogrel single and multiple administrations in rats. In pharmacodynamics study, YQFM also had no impact on prothrombin time of aspirin or clopidogrel. Based on the results of pharmacogenomics, pharmacokinetics, and pharmacodynamics, the HDIs of YQFM have a good safety profile, and the combination with the above three drugs might have synergistic effects due to the different efficacy of YQFM‐quality markers. [ABSTRACT FROM AUTHOR]

Background: Cheilanthes tenuifolia (Burm.f.), commonly known as the Sword Fern or Narrow‐leaved Cloak Fern, is a little evergreen fern that belongs to the Pteridaceae family and is abundant in various bioactive compounds exerting promising medicinal properties. The current study is designed to evaluate in vivo analgesic and antidiarrheal activity of the methanol leaf extract of C. tenuifolia (MCT). Methods: For this purpose, Swiss albino mice were used to investigate the analgesic and antidiarrheal properties using acetic acid‐induced writhing and castor oil‐induced diarrhea methods, respectively. The mice were administered orally with different doses of MCT (125, 250, and 500 mg/kg). The vehicle performed as a negative control (NC), while diclofenac sodium (DCN) (25 mg/kg), loperamide (LOP) (3 mg/kg), bismuth subsalicylate (BSS) (10 mg/kg), and nifedipine (NDP) (2.5 mg/kg) were supplied as positive controls (PC) (p.o.). In both models, combination treatment of MCT (higher dose) and PC was also administered to different groups of animals for assessing potential antagonistic or synergistic activity. Results: Findings of the in vivo study demonstrated that MCT dose‐dependently significantly (p < 0.05) exhibited analgesic and antidiarrheal properties by reduction in the number of writhing and reductions in the total fecal output in contrast to the NC group. Moreover, in combination treatment, MCT significantly (p < 0.05) synergized the activity of PC in both models, exerting potential analgesic and antidiarrheal activity. Conclusion: In conclusion, MCT has analgesic and antidiarrheal activity; it might be beneficial for the management of pain and diarrhea. [ABSTRACT FROM AUTHOR]

Piperine has been reported to inhibit the enzyme activity of cytochrome P450 (CYP) 3A4. The aim of this study was to develop and validate a physiologically based pharmacokinetic (PBPK) model for piperine and to predict potential food–drug interactions (FDIs) between piperine and CYP3A4 substrate drugs using these models. The PBPK model for piperine was successfully developed and validated. Using this model, FDIs with ten CYP3A4 substrate drugs were simulated. The predicted area under the curve (AUC) ratios (with and without piperine, following a 7-day intake of 20 mg/day) for six drugs were found to exceed 1.25, with significant increases in AUC observed for ritonavir (31%), nifedipine (34%), cyclosporine (35%), triazolam (36%), alfentanil (39%), and simvastatin (59%) in humans. These findings suggest that caution should be exercised when consuming amounts of black pepper equivalent to a daily intake of 20 mg piperine during treatment with CYP3A4 substrate drugs, as it may significantly alter their pharmacokinetics. [ABSTRACT FROM AUTHOR]

Objective • Heart failure is a common cardiovascular disease, and its prevalence is increasing year by year. For patients with heart failure combined with non-valvular reduced ejection fraction, drug therapy has always been a key treatment. This study aimed to explore the clinical efficacy of sacubitril valsartan sodium and enalapril in such patients. Methods • Study design: This study used a prospective observational design. From February 2020 to February 2022, we included 123 patients with non-valvular heart failure and reduced ejection fraction who were treated in Xingtai Third Hospital. Patients were divided into two groups according to the treatment plan: Group A (n=61) received enalapril, and Group B (n=62) received nifedipine. All patients received conventional treatment. We compared the efficacy of the two groups of patients 8 weeks after treatment. During the study, the laboratory indicators, echocardiographic indicators, cardiovascular markers, and possible adverse reactions of the two groups of patients before and after treatment were recorded. Results • After 8 weeks of treatment, the effective rate of group B was higher than group A (P < .05). There were no differences in the levels of total protein, total bilirubin, total cholesterol and serum creatinine between the two groups before and after treatment (P > .05). The serum creatinine level in the two groups after treatment was higher than that before treatment, and the level in group B was lower than that in group A (P < .05). There were no statistically significant differences in the levels of total protein, total bilirubin and total cholesterol between the two groups before and after treatment (P > .05), and there was no statistically significant difference in the level of serum creatinine between the two groups before treatment (P > .05), and the level of serum creatinine after treatment was higher than that before treatment, and the level of group B was lower than that of group A (P < .05). Before treatment, there was no significant difference in the levels of high-sensitive troponin T and n-terminal brain natriuretic peptide and cyclic guanosine phosphate between the two groups (P > .05). After treatment, the levels of high- sensitive troponin T and N-terminal brain natriuretic peptide in the two groups were lower than those before treatment, and those in group B were lower than those in group A. The level of cyclic guanosine phosphate in group A was lower than that before treatment, the level of cyclic guanosine phosphate in group B was higher than that before treatment, and the level of group B was higher than that of group A (P < .05). The incidence of adverse cardiovascular events in group B was lower than that in group A (P < .05). In this study, the effective rate of treatment group B was significantly higher than that of treatment group A, indicating that treatment group B had a better therapeutic effect. In addition, there were no significant differences between the two groups in a series of biochemical parameters, but it is worth noting that after treatment, the serum creatinine level of group B was significantly lower than that of group A, which may indicate that the treatment of group B is not only more effective but also Reduces the risk of certain adverse cardiovascular events. Conclusion • The main findings of the study showed that Sacubitril valsartan sodium showed better clinical efficacy than enalapril in patients with heart failure and non-valvular reduced ejection fraction. Specifically, the drug significantly improved patients’ kidney function, reduced cardiovascular marker levels, and reduced the incidence of adverse cardiovascular events. These findings have important clinical implications for guiding treatment selection in patients with heart failure. [ABSTRACT FROM AUTHOR]

Nifedipine, a calcium channel blocker, is effective in managing cardiovascular conditions. However, its variable solubility in different solvent systems poses formulation challenges. Understanding its solubility behavior is crucial for optimizing drug delivery strategies and enhancing therapeutic outcomes. This study employs various techniques rooted in established solubility theories to explore nifedipine solubility across different solvents. Experimental techniques, complemented by computational modelling, including extended Hildebrand solubility approach, Hansen's approach, and polynomial regression analysis are used. Experimental data on nifedipine solubility in various solvent blends are collected and analyzed to elucidate the underlying molecular interactions driving solubility. The study reveals that nifedipine exhibits complex solubility behavior influenced by factors such as solvent polarity (), dispersion forces (), and hydrogen bonding interactions ( as found from four parameter approach. These results align with the chemical structure of nifedipine, offering insight into the drug ability to interact. Hydrogen bonding partial parameters provided a rational explanation for the solubility behavior of nifedipine, highlighting its role as a proton donor and Lewis acid. The technique of ideal solubility intersecting observed mole fraction solubility (10.62 H) proved valuable in predicting nifedipine solubility, particularly when closely aligned with peak solubility (10.13 H). By examining the total solubility parameter values obtained from different methods, it can be concluded that the best solvents for nifedipine fall within values ranging from 10 to 13 H. These findings contribute to the understanding of nifedipine solubility and provide insights into the design of effective drug delivery systems. [ABSTRACT FROM AUTHOR]

Calcium channel blockers (CCB) are the best-known, most widely used drugs in the treatment of hypertension in the world. Gingival hyperplasia is one of the uncommon side effects of CCB usage. Among CCBs, it's most commonly seen due to nifedipine. Gingival hyperplasia is rarely seen with the use of amlodipine. The mechanism of drug-induced gingival enlargement is not entirely understood, but it's clear that it is due to multifactorial influences. Although the pharmacologic effect of each drug is different, all of them are estimated to act similarly to the secondary target tissue, i.e., the gingival connective tissue, thus resulting in common histopathological findings. Both inflammatory and non-inflammatory mechanisms are involved. This case has been presented to emphasize that the development of gingival hyperplasia in patients with hypertension could be a side effect of amlodipine usage. [ABSTRACT FROM AUTHOR]

The unstable balance in the immature hemostatic system of the premature fetus and newborn can be easily disturbed under the influence of stressful factors associated with childbirth, including tocolytic therapy. The objective: to study in vivo the blood coagulation and fibrinolysis in newborns after tocolytic therapy. Materials and methods. The study was performed in two clinical groups of newborns (gestational term up to 34 weeks) from mothers who received tocolytic treatment with hexoprenaline (I group, 26 babies) or nifedipine (II group, 22 newborns) for a long time before birth. A group of preterm infants born without tocolysis (III group, 18 children) and a group of full-term infants (IV group, 18 children) were the comparison ones. The hemostatic profile of the newborn in vivo was determined using the ROTEM® delta device (Instrumentation Laboratory, Germany) in a portion of blood with a volume of 300–340 µl, which was obtained after the birth of the fetus from a fragment of the umbilical cord between two clamps. Clot formation and lysis were assessed by kinetic parameters of coagulation. The analysis of elastograms is performed by a program from the device interface. For coagulation analysis, the r ex-tem® and fib-tem® test systems (Tem Innovations GmbH, Germany) were used. Results. In the case of hexoprenaline tocolysis, the α angle was insignificantly different from the values of the III and IV groups (70.8±9.47° vs. 76.7±4.84 and 79.9±4.62°; p>0.05), and after of tocolysis with nifedipine the angle α (54.8±10.16°; p<0.05) is probably smaller than the indicators of the III and IV groups, which indicates the slowing down of blood clot formation in the newborn. The characteristics of the process of clot formation – the amplitude at the 5th and 10th minutes (A5, A10) and the maximal clot firmness/maximal amplitude (MCF/MA) after hexoprenaline tocolysis (I group) exceeded those of newborns of the III group without tocolysis – 14.6±8.73; 19.3±6.20; 23.4±6.97 mm versus 13.2±3.34; 15.5±4.34; 15.2±11.37 mm with a significant difference according to A10 and MCF/MA (p<0.05) and term newborns of the IV group according to A10 and MCF/MA (16.0±7.39 and 17.4±7.04 ; p<0.05). The growth of clot amplitudes after tocolysis with hexoprenaline resembled the sequence of growth of the parameters of full-term newborns, differing quantitatively. In the case of nifedipine tocolysis, all parameters of the clot amplitude are significantly reduced – 8.2±3.34; 10.0±2.27; 11.4±3.03 mm compared to the III group – 13.2±3.34; 15.5±4.34; 15.2±11.37 mm (р<0.05), all the more, to the already the indicators of the IV group, as close as possible to the indicators of extremely premature newborns – 4.6±1.39, 8.0±3.01, 7.9±5.56 mm. Lysis index at 30 min (LI 30) lagged behind the indicators of the control groups (95.6±5.50 and 98.2±1.33% compared to 91.7±15.28 (p>0.05) and 85.4±22.81%; p<0.05). Maximum lysis (ML) had the lowest mean values among all premature infants (3.2±1.56; 4.4±4.25; 8.1±2.50%; p>0.05), lagging behind the index of full-term newborns (17.1±2.34%; p<0.05). Conclusions. 1. Tocolysis with the use of hexoprenaline sulfate is reflected in a premature newborn by the acceleration of the process of clot formation and the slowing down of fibrinolysis in umbilical cord blood. The reflection of this effect on the thromboelastogram is close to the kinetic processes of blood coagulation in full-term infants. 2. After the use of nifedipine for tocolytic therapy, there are the signs of delayed clot formation and disordered fibrinolysis on the thromboelastogram, as indicated by a large variance in the maximal lysis index (4.4±4.25 mm). [ABSTRACT FROM AUTHOR]

Background: Hypertension is a prevalent health condition with severe implications for cardiovascular health. Combination therapy involving Candesartan and Nifedipine has emerged as a promising approach for managing hypertension due to the synergistic effects of these medications. Methods: This study aimed to develop a Design of Experiment (DoE) based Green High-Performance Liquid Chromatography (HPLC) method for the simultaneous estimation of Candesartan and Nifedipine in a combined dosage form. Reversed-phase HPLC was utilized with UV-Vis spectrophotometry for detection. DoE principles were applied to optimize chromatographic conditions, including pH, ethanol percentage in the mobile phase, and flow rate. Results: Optimal chromatographic separation was achieved using a composite mobile phase comprising ethanol and potassium dihydrogen phosphate buffer (45:55, v/v) at pH 3.7, with a flow rate of 1 mL/min. Statistical analysis confirmed the significance of these parameters in achieving efficient separation. The developed method exhibited high precision, accuracy, and reliability across various validation parameters, including specificity, linearity, repeatability, and robustness. Conclusion: The proposed DoE-based Green HPLC method offers a sustainable and efficient approach for the simultaneous estimation of Candesartan and Nifedipine in hypertension management. By integrating green chemistry principles with systematic method development, this method provides a reliable analytical tool for routine quality control purposes in pharmaceutical formulations containing these medications. [ABSTRACT FROM AUTHOR]

Many diseases exhibit circadian fluctuation, including diabetes, asthma, rheumatoid arthritis, and hypertension. These disorders cannot be effectively treated with conventional dosage forms and instead require time-scheduled drug release for pharmacological effectiveness. The objective of this work was to use simple process to overcome the solubility problem by employing a novel solubilizer and to generate peristaltic release based on the physical and chemical interactions between acrylic copolymer and organic acid. To address the solubility issue of nifedipine, sepitrap 4000 is being used as a solubilizer inside the core tablet. The resulting physical mixture underwent various analyzes including saturated solubility, in-vitro dissolution, FTIR, DSC, and PXRD. A saturation solubility analysis confirmed 368% improvement as significant impact of sepitrap 4000 on nifedipine solubility and bioavailability. The 32 complete factorial design was used to optimize press-coated pulsatile formulation, with lag time and time required to release 50% of drug, as responses and concentrations of eudragit RSPO and tartaric acid as independent variables. According to stability study, developed pulsatile product was found to be suitably stable under rapid and regulated settings. As a result, produced pulsatile tablet is suitable formulation for alleviation of early morning blood pressure spikes and other cardiac problems that follow a circadian rhythm. [ABSTRACT FROM AUTHOR]

Insulin resistance, induced by high fructose consumption, affects cognitive function negatively. Nifedipine may be suggested for neurological disorders. This study aimed to assess the effect of nifedipine with either a normal diet (ND) or a ketogenic diet (KD) in cognitive dysfunction. Male Wistar rats received 10% fructose in drinking water for 8 weeks to induce insulin resistance. Rats received nifedipine (5.2 mg/kg/day; p.o.) later with ND or KD for an additional five weeks. One and two-way ANOVAs were used in analyzing the data. Reversion to the ND improved insulin resistance and lipid profile, besides brain-derived neurotrophic factor (BDNF), glycogen synthase kinase-3 beta (GSK3β), and insulin-degrading enzyme (IDE) levels. Rats fed KD alone and those that received nifedipine with KD did not show similar improvement in the previously mentioned parameters as the ND group. However, nifedipine-ND rats showed improvement in cognitive behavior and insulin resistance. Treatment with nifedipine-KD ameliorated GSK3β, amyloid β (Aβ), and tau protein levels. As the nifedipine-KD combination succeeded in diminishing the accumulated Aβ and tau protein, KD may be used for a while due to its side effects, then nifedipine treatment could be continued with an ND. This conclusion is based on the finding that this combination mitigated insulin resistance with the associated improved behavior. [ABSTRACT FROM AUTHOR]

This study assessed the pharmacokinetics (PKs) and pharmacodynamics (PDs) of two antihypertensive drugs, nifedipine and captopril, by exploring their main (blood pressure [BP]) and secondary effects (heart rate [HR] and QT interval [QT]) in spontaneously hypertensive rats. This study aimed to assess the relationship between PKs and PDs. Using these PD parameters, BP, HR, and QT during coadministration were estimated. The coadministration of nifedipine and captopril resulted in an increase in nifedipine's total body clearance (CLtot) and a reduction in its mean residence time (MRT) with an increase in the terminal elimination half‐life (t1/2) and volume of distribution at steady state (Vdss) of captopril. However, no significant PK interactions were observed. During monotherapy, BP reduced rapidly following nifedipine infusion. Subsequently, despite the increase in nifedipine plasma concentration, BP recovered, likely because of homeostasis. Similar results were observed with coadministration. Subsequently, BP demonstrated a sustained reduction that was greater than or equal to the additive effect estimated from each PK. Captopril exhibited a minimal effect on HR, except for a transient increase observed immediately after starting infusion, consistent with observations during coadministration. Subsequently, the HR reduction was nearly equal to that calculated from the nifedipine PK. QT prolongation was more rapid with captopril than with nifedipine. Although QT prolongation during the initial 60 min of coadministration was approximately the sum of both effects, the recovery period to baseline QT was faster than that in the simulation. [ABSTRACT FROM AUTHOR]

BACKGROUND: Treatment of chronic hypertension during pregnancy has been shown to reduce the risk of adverse perinatal outcomes. In this study, we examined the prevalence and treatment of chronic hypertension during pregnancy and assessed changes in these outcomes following the release of the updated 2017 hypertension guidelines of the American College of Cardiology and American Heart Association. METHODS: We analyzed the MerativeTM Marketscan® Research Database of United States commercial insurance claims from 2007 to 2021. We assessed the prevalence of chronic hypertension during pregnancy and oral antihypertensive medication use over time. We then performed interrupted time series analyses to evaluate changes in these outcomes. RESULTS: The prevalence of chronic hypertension steadily increased from 1.8% to 3.7% among 1 900 196 pregnancies between 2008 and 2021. Antihypertensive medication use among pregnant individuals with chronic hypertension was relatively stable (57%-60%) over the study period. The proportion of pregnant individuals with chronic hypertension treated with methyldopa or hydrochlorothiazide decreased (from 29% to 2% and from 11% to 5%, respectively), while the proportion treated with labetalol or nifedipine increased (from 19% to 42% and from 9% to 17%, respectively). The prevalence or treatment of chronic hypertension during pregnancy did not change following the 2017 American College of Cardiology and American Heart Association hypertension guidelines. CONCLUSIONS: The prevalence of chronic hypertension during pregnancy doubled between 2008 and 2021 in a nationwide cohort of individuals with commercial insurance. Labetalol replaced methyldopa as the most commonly used antihypertensive during pregnancy. However, only about 60% of individuals with chronic hypertension in pregnancy were treated with antihypertensive medications. [ABSTRACT FROM AUTHOR]

Purpose: The primary aim of this study was to optimize, characterize, and test a controlled-release organogel of nifedipine for oral delivery. The formulation employed 12-hydroxy stearic acid as a gelator with soybean oil as a base. This research sought to investigate the potential of this organogel system to provide a controlled release alternative for nifedipine administration. Methods: Preformulation studies and drug-excipient compatibility tests were conducted for nifedipine and the selected excipients. A controlled release organogel was created using the heating method. A quadratic model was applied to design formulations (F1-F14) with varying concentrations of 12-hydroxy stearic acid and distinct cooling rates (gradual and quick cooling) at five levels, utilizing a one-factor response surface approach. The prepared formulations were evaluated using various assessment parameters. Design Expert 7.0 was employed to statistically derive the optimized batch. Differential scanning calorimetry and Fourier-transform infrared spectroscopy were used to compare the preformulation test results between nifedipine and the excipients. Results: The optimized controlled-release organogel exhibited a drug release profile of 86.02% at 10 h, which increased to 96.04% after 12 h. The data for the optimized formulation revealed a significant correlation between expected and actual responses, indicating the efficacy of the quadratic model and the response surface approach in predicting formulation behavior. Conclusions: The study concluded that an organogel formulation using 12-hydroxy stearic acid as an organogelator and soybean oil as a base could be beneficial for controlled-release formulations of nifedipine. The results suggest that this organogel system is a viable alternative for the controlled release of nifedipine, offering a promising method for its oral administration. [ABSTRACT FROM AUTHOR]

Livedoid vasculopathy (LV) is a chronic, recurrent thrombotic vasculopathy characterized by painful ulcerations on the lower extremities, which heal slowly and leave atrophic white scars known as "atrophie blanche." This report presents the case of a 31-year-old woman with a 4-year history of recurrent painful ulcerations on her legs and feet. A skin biopsy revealed findings consistent with LV, and an exhaustive laboratory workup ruled out secondary causes such as thrombophilia, malignancies, autoimmune diseases, and peripheral arterial disease. The patient showed remarkable improvement with a treatment regimen of pentoxifylline, nifedipine, and warfarin, resulting in complete ulcer resolution and sustained remission over 5 months. Our case highlights the importance of a comprehensive diagnostic approach and a multidisciplinary treatment strategy in managing primary LV to achieve remission and prevent recurrence of skin ulcerations. [ABSTRACT FROM AUTHOR]

Preterm delivery is associated with perinatal outcomes such as neonatal complications and deaths. Uterine contraction suppressants are administered to treat. In Japan, ritodrine hydrochloride (ritodrine) and magnesium sulfate (magnesium) are covered by insurance. However, ritodrine was withdrawn from the United States market in 2011, and in Europe, its administration was only limited for short-term use in 2013. In this study, we analyzed in the use of ritodrine and magnesium using the NDB Open Data Japan and annual trends in the number of births issued by the Ministry of Health, Labor, and Welfare for 2019-2021. Ritodrine prescribed per birth decreased from 2019 to 2020, while the level 2021 was the same as 2020. Magnesium decreased between 2019 and 2021. The ages were administered ranged from 15-49 years. The results of this study suggest that ritodrine and magnesium are still frequently used in Japan for the treatment of preterm labor. Recently, the American College of Obstetricians and Gynecologists advocated the use of calcium antagonists such as nifedipine as the first choice. We extracted trends in the use of nifedipine, in the target age group for the treatment of imminent preterm labor. The number of nifedipine prescriptions increased every year. However, nifedipine has no indication for the treatment of imminent preterm labor in Japan, it should be noted that this is not accounting for the treatment of impending preterm labor because the prescriptions were classified as vasodilators in the NDB Open Data. [ABSTRACT FROM AUTHOR]

Objectives: To investigate the effects of intravenous nicardipine as initial therapy and oral labetalol combined with nifedipine controlled-release tablet as subsequent treatment of severe peripartum hypertension. Material and methods: Intravenous nicardipine was delivered as the initial treatment, after the target blood pressure (BP) had been achieved, oral labetalol was used to maintain the target BP. If oral labetalol failed to maintain the target BP, oral labetalol combined with nifedipine controlled-release tablet was used. Results: A total number of 131 patients were enrolled. The target BP (BP < 140/90 mmHg) was achieved in all patients within 60 minutes by intravenous nicardipine. After receiving labetalol orally, the target BP was maintained in nine patients. However, in 104 patients, we had to combine oral labetalol and nifedipine controlled-release tablet due to re-elevation of their systolic BP to 140-159 mmHg. In 18 patients, we restarted intravenous nicardipine because their systolic BP re-elevated above 160 mm Hg. Among the 104 patients who received oral labetalol and nifedipine controlled-release tablet, the target BP was achieved and maintained in 96 patients, and eight patients had to restart nicardipine. Of the total number of 26 patients in whom intravenous nicardipine was resumed, the target BP was successfully maintained in 22 patients with oral labetalol combined with nifedipine controlled-release tablet. Conclusions: Intravenous nicardipine rapidly and safely lowered severe peripartum hypertension. As subsequent therapy, oral labetalol combined with nifedipine controlled-release tablet protocol may be applied to effectively maintain a target BP. [ABSTRACT FROM AUTHOR]

The isobaric condensed-phase heat capacities of selected pharmaceutical active ingredients (APIs), namely nifedipine (CAS RN: 21829-25-4), griseofulvin (CAS RN: 126-07-8), probucol (CAS RN: 23288-49-5) and 5,5-diphenylhydantoin (CAS RN: 57-41-0), were determined over a wide temperature range starting from 2 K by combination of relaxation (heat pulse) calorimetry, Tian-Calvet calorimetry and power-compensated differential scanning calorimetry. Heat capacity measurements were taken for clearly specified polymorphs, a liquid phase (including subcooled liquid) and a glassy amorphous phase, if feasible. For 5,5-diphenylhydantoin, a heat capacity anomaly was detected in the temperature range 160 to 190 K and interpreted based on additional calorimetric and temperature-variable crystallographic measurements as a sequence of two phase transitions, which are reported for the first time in this work. Based on the determined phase behavior and heat capacity data from near 0 K, standard thermodynamic functions for crystalline and liquid phases were calculated for all APIs studied. This work significantly extends the availability of reliable heat capacity data and related thermodynamic properties for APIs required for modeling their solubility and other applications involving thermodynamic modeling. [ABSTRACT FROM AUTHOR]

The aim of this study was to develop and evaluate the transdermal patch formulations of nifedipine. The patch formulations containing nifedipine were prepared and optimized with different ratios of vinyl and cellulose-derived polymers, drug contents, and permeation enhancers. Among the various formulations, the patch formulation containing a 1:5 ratio of ethyl cellulose and polyvinyl pyrrolidone was selected for ex vivo pharmacokinetic study based on in vitro permeation studies using stratum corneum of the pig's skin. The cumulative percentage release after the transdermal administration of the optimized patch formulation was 71.43%, and the plasma concentration of nifedipine was maintained for 16 hrs. The physicochemical evaluation study including flatness, thickness, moisture content and uptake, drug content in vitro release, and ex vivo permeation indicated satisfactory results. The formulation batch with clove oil as a penetration enhancer has shown better ex vivo permeation as compared to the formulations without enhancers and another synthetic enhancer. These results suggest that the optimized patch formulation Q3 could be further developed for clinical applications, providing the therapeutic plasma level of nifedipine over an extended period. Hence analyzing the results of the evaluation tests, in vitro and ex vivo data on the preparation and optimization of nifedipine-loaded transdermal patch, it can be concluded that the formulation shows its feasibility as an effective transdermal delivery system for nifedipine. [ABSTRACT FROM AUTHOR]

What Is Known and Objective. Tocolytic agents are used to prolong gestational age and prevent immediate preterm birth (PTB). This study aims to provide an overview of the use of tocolytics among patients with PTB in China through retrospectively analyzing trends in application, influencing factors, and inappropriate prescriptions. Methods. The prescription data of five tocolytic agents from 2016 to 2021 were extracted from the database of the Hospital Prescription Analysis Cooperation Project. Drug consumption was expressed as number of prescriptions, cost of prescriptions, and DDDs (defined daily doses). Pearson correlation analysis was used to examine the association between DDDs and DDC (defined daily cost). The appropriateness of prescriptions was analyzed in terms of drug dosage form, administration, clinical diagnosis, and combined medication. Results. The total number of tocolytic prescriptions and the total cost of tocolytic agents increased by 6.12% and 387.58%, respectively, over the six‐year duration of the study. From 2016 to 2021, the ranking of the number of prescriptions and DDDs of tocolytic agents was magnesium sulfate > ritodrine > nifedipine > indomethacin > atosiban. During the study period, the cost of tocolytic agents increased significantly, which was mainly related to the increased costs of magnesium sulfate in 2017 and atosiban in 2018 and 2019. The ranking of DDCs was atosiban > ritodrine > magnesium sulfate > nifedipine = indomethacin from 2016 to 2021. For atosiban, the DDC was negatively correlated with the DDDs. Inappropriate prescription, which accounted for 14.84% of all prescriptions, was mainly manifested in the inappropriate selection of nifedipine dosage form, low frequency of nifedipine and indomethacin, and overdosing of ritodrine. Furthermore, 22.87% of tocolytic prescriptions remained active after 34 weeks of gestation, and 7.24% of the prescriptions authorized the use of combination drugs, with magnesium sulfate and nifedipine being the most commonly prescribed combination. What Is New and Conclusion. Magnesium sulfate, ritodrine, and nifedipine were the top three tocolytic agents. As the inappropriate use of tocolytic agents continues to persist, it is important to intensify efforts to ensure the safety and the appropriateness of maternal medication. [ABSTRACT FROM AUTHOR]

We describe the evolution of treatment recommendations for chronic hypertension (CHTN) in pregnancy, the CHTN and pregnancy (CHAP) trial, and its impact on obstetric practice. The US multicenter CHAP trial showed that antihypertensive treatment for mild CHTN in pregnancy [blood pressures (BP)<160/105 mm Hg] to goal<140/90 mm Hg, primarily with labetalol or nifedipine compared with no treatment unless BP were severe reduced the composite risk of superimposed severe preeclampsia, indicated preterm birth <35 weeks, placental abruption, and fetal/neonatal death. As a result of this trial, professional societies in the United States recommended treatment of patients with CHTN in pregnancy to BP goal<140/90 mm Hg. [ABSTRACT FROM AUTHOR]