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nifedipine (Darbelan 10)

✓ Approved

Teva Pharmaceutical Industries Ltd. · CACNA1C · 小分子

什么是 nifedipine？

nifedipine 是一种小分子，由Teva Pharmaceutical Industries Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Darbelan 10
公司Teva Pharmaceutical Industries Ltd.
药物类别小分子
分子靶点CACNA1C
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Teva Pharmaceutical Industries Ltd.

作用机制

分子靶点

nifedipine 作用于 1 个分子靶点：

CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

nifedipine 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Cardiac disordersAngina pectoris✓ Approved
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedRevista brasileira de ginecologia e obstetricia : revista da Federacao Brasileira das Sociedades de Ginecologia e Obstetricia2026-10-25

Atosiban versus nifedipine for the management of preterm labor: a systematic review and meta-analysis of randomized controlled trials.

Pascon Alessandro A, Fumes Ana Júlia AJ, Rüdinger Nícolas Hammad NH, da Costa Ricardo Filipe Alves RFA et al.

To compare the efficacy, maternal safety, and neonatal outcomes of atosiban versus nifedipine in the management of preterm labor, with particular attention to neonatal intensive care unit (NICU) admission rates. PubMed, EBSCOHost, ClinicalTrials.gov and the World Health Organization International Clinical Trials Registry Platform (ICTRP), and the Cochrane Central Register of Controlled Trials were systematically searched up to May 25, 2025. No language restrictions were applied. Randomized controlled trials (RCTs) comparing atosiban and nifedipine in women with clinically diagnosed preterm labor were included, provided they reported at least one outcome related to pregnancy prolongation. Six RCTs comprising 1,070 patients met inclusion criteria. Two reviewers independently extracted data on efficacy, maternal adverse effects, and neonatal outcomes using a standardized form. Risk of bias was assessed with the Cochrane Risk of Bias 2 (RoB 2) tool. Pooled analyses showed no significant difference between atosiban and nifedipine in delaying delivery for 48 hours (risk ratio [RR] 1.09; 95% confidence interval [CI] 0.97-1.23) or 7 days (RR 1.04; 95% CI 0.89-1.22). Atosiban was associated with a significantly lower risk of maternal headache, hypotension, and tachycardia. Atosiban was associated with a non-statistically significant trend toward higher NICU admission (RR 1.36; 95% CI 0.97-1.94; p=0.079), an estimate derived from only two RCTs with substantial heterogeneity (I2=69.8%) and warranting cautious interpretation. No significant differences were observed for neonatal death, sepsis, or hemorrhagic disease. Atosiban and nifedipine offer comparable tocolytic efficacy. Atosiban carries a more favorable maternal safety profile but shows a non-significant trend toward higher NICU admission warranting confirmation in larger trials. Tocolytic selection should therefore be individualized, weighing maternal tolerability against this uncertain neonatal signal.Systematic Review Registration: PROSPERO CRD420251065426.

PMID 42923929
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PubMedPharmaceutical research2026-10-24

Time-Lapse Macro Imaging and LLM-Assisted Phenotypic Analysis of Release Dynamics in Nifedipine Controlled-Release Tablets.

Xu Ke K, Yang Yixiang Y, Chen Yuling Y, Zhang Xinzi X et al.

To develop an exploratory flow-through time-lapse macro-imaging framework combining rule-based image analysis and multimodal large language models (LLMs) for comparing release phenotypes of nifedipine osmotic pump tablets. Sixteen marketed products, comprising Adalat OROS and 15 generics, were imaged in triplicate for 36 h under sequential pH 1.0 (2 h) and pH 6.8 (34 h) conditions at 37 ± 0.5°C. Images acquired every 30 s were analyzed using a pixel color-based drug similarity method (PCDS), the Dis-GPT agent, and a pharmaceutical knowledge-base-assisted DIS Chatflow. The framework captured drug-layer extrusion, local aggregation, release continuity, and push-layer morphology. Eight generics (02, 03, 04, 10, 12, 13, 15, and 16) were classified as similar to the reference by all three methods. Product 08 was consistently classified as different, exhibiting granular extrusion, bead-like aggregation, and reduced continuity; products 06 and 07 showed method-dependent deviations in release timing and push-layer extrusion. Flow-through time-lapse imaging revealed process-level release features not represented by cumulative dissolution profiles. Combining transparent pixel-based measurements with structured LLM analysis provides an exploratory framework for comparing visible release phenotypes and generating hypotheses about release mechanisms in controlled-release tablets.

PMID 42920046
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PubMedAnalytical chemistry2026-10-20

DES-Based Green Synthesis of 2D Fluorescent Molybdenum Disulfide for Highly Sensitive and Selective Detection of Nifedipine.

Ullah Rafee R, Rehman Shams Ur SU, Khan Adnan A, Wu Hui-Fen HF

Highly fluorescent 2D MoS2-x nanosheets exhibiting intense blue emission were synthesized using a green chemistry approach, utilizing DES as both the reaction medium and a surface passivating agent. The material was synthesized via a hydrothermal method, followed by ultrasonication-assisted exfoliation to yield ultrathin nanosheets with enhanced photoluminescence properties. The 2D MoS2-x nanosheets demonstrated strong fluorescence at λem = 420 nm when excited at λex = 330 nm. These nanosheets were employed as a fluorescence probe for the detection of the calcium channel blocker drug nifedipine (NIF) via a fluorescence quenching mechanism. Upon addition of NIF, the fluorescence of the 2D MoS2-x nanosheets was quenched due to electron transfer from the nanosheets to the electron-deficient NIF molecules, combined with the inner filter effect (IFE). The nanosheets enabled highly sensitive and selective detection of NIF, with photoluminescence spectroscopy revealing a broad linear detection range of 0.6-360 nM (R2 = 0.993) and an exceptionally low limit of detection (LOD) of 0.40 nM. The system showed high selectivity toward NIF over structurally similar compounds, drugs, and common metal ions. The sensor was effectively applied for the detection of NIF in urine and Lotus Pond water samples, highlighting its potential for practical pharmacological monitoring. This study presents a sustainable and effective approach for fabricating DES-assisted 2D nanosheets for trace-level analyte detection.

PMID 42899538
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PubMedAmerican journal of hypertension2026-10-19

Amlodipine and Nifedipine Associations with B-Type Natriuretic Peptide in Women with Hypertension and Heart Failure with Preserved Ejection Fraction.

Harada Eisaku E, Yamada Toshihiro T, Mizuno Yuji Y, Arima Yuichiro Y et al.

Calcium channel blockers (CCBs) are frequently prescribed to manage hypertension in patients with heart failure with preserved ejection fraction (HFpEF). However, whether individual dihydropyridine agents exert uniform class effects on myocardial wall stress remains unclear. This retrospective, single-center observational study analyzed 465 consecutive patients with hypertension and HFpEF (354 women and 111 men) evaluated at Kumamoto Kinoh Hospital between May 2012 and July 2018. Multivariable linear regression models assessed associations between individual dihydropyridine CCBs (amlodipine vs. nifedipine) and plasma log-transformed B-type natriuretic peptide (lnBNP) levels. In multiple imputation models among women, adjusted differences in lnBNP relative to no-CCB were 0.236 (95% CI, 0.031 to 0.441) for nifedipine and -0.118 (95% CI, -0.273 to 0.037) for amlodipine. Direct linear contrasts in women confirmed lower lnBNP levels with amlodipine than with nifedipine (adjusted difference, -0.355; 95% CI, -0.562 to - 0.147). In men, the corresponding amlodipine-versus-nifedipine difference was -0.051 (95% CI, -0.697 to 0.595; P=0.876). The formal sex-by-drug interaction contrast in complete-case analysis yielded an adjusted difference of - 0.424 (95% CI, -1.055 to 0.208; P = 0.188), with male precision constrained by sample size (7 male nifedipine users). In women with hypertension and heart failure with preserved ejection fraction, amlodipine use was associated with lower adjusted ln(BNP) levels than nifedipine use. These observational findings challenge the assumption of an interchangeable dihydropyridine class effect on myocardial wall stress, suggesting that individual pharmacological profiles-rather than uniform class-level equivalence-warrant attention in clinical evaluations.

PMID 42895302
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PubMedPharmacological research2026-10-18

Nifedipine-modulated gut microbiota attenuates hypertensive vascular injury through Bifidobacterium-associated inosine-Adora2b signaling.

Ren Xiaoyu X, Yan Xuefang X, Tang Ping P, Jin Jiajia J et al.

Although antihypertensive drugs mitigate hypertensive vascular injury, their vascular benefits are not fully explained by blood pressure reduction alone. Many cardiovascular drugs reshape the gut microbiota, which in turn influences their vascular pharmacology. We therefore investigated whether gut microbiota remodeling contributes to nifedipine-mediated vascular protection in high-salt hypertensive rats and a pilot patient cohort. Combining 16S rRNA sequencing, untargeted metabolomics, fecal microbiota transplantation, microbiota depletion, supplementation, and selective receptor antagonism, we found that nifedipine ameliorated gut dysbiosis. Transplantation of nifedipine-modulated microbiota improved intestinal barrier integrity and reduced vascular inflammation, oxidative stress, collagen deposition, and vascular smooth muscle cell (VSMC) phenotypic switching, while only marginally lowering blood pressure. Conversely, microbiota depletion markedly attenuated these vascular benefits despite preserving nifedipine-induced blood pressure lowering. These vascular benefits were associated with nifedipine-restored Bifidobacterium animalis subsp. lactis 420 (B420) and increased inosine availability. Supplementation with either recapitulated major vascular protective effects of nifedipine without statistically significant changes in blood pressure. In hypertensive patients, nifedipine treatment was associated with higher intestinal B420 abundance and inosine levels. In vitro, inosine modulated macrophages in an Adora2b- and Rap1-dependent manner, with accompanying changes in cAMP and KLF4, ameliorating VSMC dysfunction via paracrine signaling. In vivo, systemic Adora2b antagonism attenuated the vascular protective effects of both inosine and B420. Together, our findings support a gut microbiota-dependent component of nifedipine-mediated vascular protection that extends beyond blood pressure lowering, involving B420, increased inosine availability, and Adora2b signaling. We also nominate B420 and inosine as candidate adjuncts to calcium channel blocker therapy.

PMID 42892458
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PubMedWilderness & environmental medicine2026-10-15

Silent Hypoxemia in High-Altitude Pulmonary Edema: A Case Report.

Karki Iswor I, Thapa Sabitra S, Chapagain Subodh S

We report a case of a trekker who ascended to Tilicho Lake (4919 m) from Kathmandu (1400 m) in 3 days. On day 3, he descended to Shree Kharka (4045 m). The following day, he trekked to Yak Kharka (4025 m) where, although he had no symptoms, he measured his own oxygen saturation (SpO2) at 72% in ambient air. Overnight, his SpO2 ranged from 75-80% on oxygen 2L/min via nasal cannula. The next day his SpO2 dropped to 47% while still on oxygen. He descended on horseback to Manang (3500 m), where his SpO2 was 70% on room air. He was diagnosed with high-altitude pulmonary edema (HAPE). He was treated with oxygen, 4L by nasal cannula, and nifedipine. The following day, he flew to Kathmandu, where he made a full recovery. Trekkers may develop life-threatening HAPE without obvious symptoms or signs. Slow ascent can decrease the likelihood of developing HAPE, but trekkers do not always follow the recommended ascent rate. Early detection, by history and physical examination and with point-of-care ultrasound (POCUS), if available, is critical in resource-limited regions such as ours. The keys to managing HAPE are early recognition and management, including descending to a lower altitude as soon as possible.

PMID 42878551
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