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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

PubMedJournal of mass spectrometry : JMS2026-06-11

A Combined MS/MS and IMS Study Into the Fragmentation Pathway of Nifedipine.

Han Peiliang P, Thomassen Newton N, Honing Maarten M

Collision-induced dissociation (CID) of small molecules, typically with a molecular mass below 1500 Da, is widely applied for the structural identification of drug metabolites, synthetic by-products and unknown compounds. Nonetheless, the interpretation of MS/MS spectra derived from protonated or sodiated molecules mainly relies on the comparison with literature data and proposed structures usually lack rigorous mechanistic justification and conclusive evidence. The commonly applied even-electron rule, as implemented in most literature and prediction software, does not support radical loss from protonated molecules. Similarly, fragmentation pathways of sodium adduct ions remain insufficiently explored and lack mechanistic rationalization. To improve the understanding of radical loss from even-electron nitro-containing compounds, a mechanistic study of fragmentation patterns of nifedipine, m-nifedipine, and related analogues was performed. Fragment ions generated from [M+H]+ and [M+Na]+ of nifedipine revealed distinct mechanisms compared with its positional isomers, while showing similarities with analogues like nisoldipine and aranidipine. The nitro group at the ortho position significantly influences fragment stability, leading to a unique fragmentation mechanism described as ortho effect. The mechanism was further investigated using isotope labelled analogs, ion mobility spectrometry (IMS), precursor ion scan (PIS), and density functional theory (DFT) calculations. Different approaches in combining IMS with MS/MS demonstrated strong capability for elucidation of fragmentation pathways.

PMID 42273714
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PubMedEuropean journal of internal medicine2026-06-11

Cardiological hypertensive emergencies: Real word data compared to guidelines indications.

Brucato Filippo F, Tognola Chiara C, De Censi Lorenzo L, Andrian Elisa E et al.

Cardiological Hypertensive Emergencies (CHE) are characterized by markedly elevated blood pressure (BP) values associated with acute cardiac hypertension-mediated organ damage (acute coronary syndrome, acute heart failure, acute pulmonary edema, or aortic dissection). This study aimed to evaluate the prevalence, clinical features and real-world BP management of CHE and to assess adherence to guideline recommendations by comparing ED practice before and after recent guideline release (2017 vs 2019). This single-center retrospective analysis included all adult patients admitted to the ED of Niguarda Hospital, Milan, during 2017 and 2019 with severely elevated BP (SBP ≥180 mmHg and/or DBP ≥120 mmHg) and acute cardiological organ damage. Target achievement was defined as ≥25% SBP reduction for 2017 and SBP <140 mmHg (<120 mmHg for aortic dissection) for 2019. 282 CHE were analysed representing nearly half of all hypertensive emergencies in both years. Nitroglycerin was the predominant intravenous therapy used. Short-acting nifedipine use strongly decrease from 2017 to 2019. Baseline BP values were 193.2/95.2 ± 14.2/17.4 mmHg and decreased significantly during the ED stay (∆ 37.4/17.1 vs 26.0/20.4 mmHg). The proportion of patients achieving guideline-defined targets was lower in 2019, reflecting the introduction of more stringent BP goals. This real-world analysis demonstrates a persistent gap between guideline recommendations and clinical practice in the management of CHE. The reduced target achievement in 2019 suggests that the adoption of aggressive BP targets remains incomplete, potentially due to concerns regarding hypoperfusion, limited dissemination of guideline updates or differences in documentation.

PMID 42270489
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PubMedFrontiers in pharmacology2026-06-08

Comparative maternal-fetal outcomes associated with different antihypertensive treatment strategies in preeclampsia: a retrospective cohort study.

Zhao Lin L, Chen Rui R, Xu Yahui Y, Wu Haiying H

Preeclampsia seriously threatens maternal and infant health. Antihypertensive therapy is key to improving perinatal outcomes, yet comparative maternal-fetal evidence for oral agents remains limited. To compare maternal-fetal outcomes of oral labetalol versus oral nifedipine in preeclampsia, informing individualized clinical treatment. This retrospective cohort study included consecutive preeclampsia patients admitted from January 2023 to December 2025, divided into Labetalol (n = 154) and nifedipine (n = 136) groups. Both received magnesium sulfate as needed, plus aspirin or low-molecular-weight heparin based on platelet count and coagulation function. After 1:1 propensity score matching (PSM), maternal and fetal outcomes were compared. Primary outcomes were maternal complications and neonatal outcomes. Secondary outcomes included uterine artery blood flow, hemodynamics, fetal growth restriction, and adverse drug reactions. Following PSM, baseline characteristics were comparable between the two groups (P > 0.05). Both achieved similar improvements in blood pressure, uterine artery blood flow (S/D, PI, RI), and hemodynamic indicators (plasma and whole blood viscosity, hematocrit) (P > 0.05). The Labetalol Group, compared to the nifedipine Group, had significantly lower rates of postpartum hemorrhage (8.8% vs. 17.0%, P = 0.043) and preterm birth (24.6% vs. 37.3%, P = 0.041), and higher neonatal birth weight (2933.95 ± 803.23 g vs. 2541.35 ± 631.41 g, P < 0.001). Conversely, the nifedipine Group experienced higher incidences of headache (16.4% vs. 7.3%, P = 0.037) and facial flushing (13.6% vs. 4.6%, P = 0.019). Multivariate Logistic regression identified maternal age ≥35 years, pre-pregnancy overweight/obesity, preeclampsia onset at <34 weeks, primiparity, multiple pregnancy, severe preeclampsia, and pre-gestational diabetes as independent risk factors for adverse maternal-fetal outcomes (all P < 0.05). Both labetalol and nifedipine effectively control blood pressure and improve uteroplacental blood flow and most maternal-fetal outcomes in patients with preeclampsia. Adverse effects (headache and facial flushing) were more commonly observed with nifedipine, whereas labetalol was associated with a lower incidence of preterm birth and postpartum hemorrhage. These findings suggest potential advantages of labetalol in specific outcomes, but causal inferences are limited by the observational study design.

PMID 42256404
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PubMedAnnals of medicine and surgery (2012)2026-06-08

High-altitude cerebral edema and high-altitude pulmonary edema in a trekker with a decent ascent profile: a case report.

Bhatta Suraj S, Joshi Surya Prakash SP, Shrestha Suraj S, Ghimire Ranjeet R et al.

High-altitude illness (HAI) comprises a spectrum of disorders, including acute mountain sickness (AMS), high-altitude pulmonary edema (HAPE), and high-altitude cerebral edema (HACE). Although gradual ascent is the most effective preventive strategy, severe complications such as HAPE and HACE can still occur in susceptible individuals despite recommended ascent profiles. A 31-year-old male trekker in the Manang Valley (3350 m) developed HAPE and HACE despite gradual ascent and 6 days of acclimatization. He presented with severe headache, nausea, and shortness of breath. Examination showed cyanosis, SpO2 39%, respiratory rate 35, bilateral lung crackles, and positive cerebellar signs. Prompt treatment with oxygen, dexamethasone, acetazolamide, and nifedipine led to improvement. He was airlifted to a lower altitude and fully recovered. Despite a gradual ascent and absence of comorbidities, the patient developed concurrent HAPE and HACE, illustrating that severe illness can occur even in low-risk profiles. This underscores the role of individual susceptibility and highlights the importance of maintaining a high index of suspicion in all high-altitude trekkers. This case illustrates that even with proper acclimatization and ascent, severe forms of HAI, such as HAPE and HACE, can occur. It underscores the role of individual vulnerability, possibly influenced by genetic and environmental factors, in the pathogenesis of altitude illness. Prompt recognition and early intervention are essential to prevent fatal outcomes.

PMID 42254131
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PubMedAnnals of medicine and surgery (2012)2026-06-08

High-altitude pulmonary edema: a case series of four patients from Nepal.

Paudyal Anish A, Bhatta Sachin S, Dhungana Sanjay S, Karki Sphurna S et al.

High-altitude pulmonary edema (HAPE) is a potentially fatal, non-cardiogenic pulmonary edema that develops after rapid ascent above 2500 m. Its incidence is influenced by ascent rate, altitude, and individual susceptibility, with risk factors including overexertion, cold exposure, respiratory infection, and genetic predisposition. Despite Nepal's extensive high-altitude trekking activity, published HAPE reports remain limited. This case series describes the clinical presentation, diagnostic features, and management outcomes of HAPE in Nepalese trekkers to promote early recognition and guide timely interventions. This retrospective case series included patients with HAPE managed at a tertiary care center in Nepal. Cases were identified from hospital records, and relevant literature was narratively reviewed to contextualize findings. Four previously healthy adults developed acute HAPE after rapid ascent above 4000 m in Nepal. They presented with dyspnea, cough, hypoxemia (SpO2 55-60%), and bilateral crackles. Imaging confirmed non-cardiogenic pulmonary edema. All patients received supplemental oxygen, nifedipine, and supportive care, resulting in gradual clinical improvement and discharge within 3-5 days. This series highlights the clinical variability of HAPE and emphasizes early diagnosis, descent, and oxygen therapy as mainstays of treatment. Rapid ascent, excessive exertion, cold exposure, and preceding respiratory infection were identified as common triggers. Diagnosis relied on clinical assessment supported by imaging, including bedside ultrasound. All patients recovered with conservative management. HAPE is life-threatening but reversible with prompt recognition and management. Strengthening clinician awareness, training, and early diagnostic capacity in high-altitude regions is essential to reduce associated morbidity and mortality.

PMID 42254115
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PubMedAmerican journal of obstetrics and gynecology2026-06-06

Combinational Tocolysis: Evaluating Lower-Dose Combinations of Nifedipine, Indomethacin and Aminophylline for Tocolytic Synergism in Pregnant Human Myometrium.

Reduanul Hossain Md M, Paul Marina M, Smith Roger R, Paul Jonathan W JW

Tocolytics, such as nifedipine, indomethacin, and aminophylline, often cause side effects that limit their clinical usefulness. It is possible that effective tocolysis could be achieved by combining tocolytics with synergistic actions so that doses of individual agents can be reduced, concurrently reducing the likelihood of off-target side effects. Since these drugs act through markedly different signaling pathways to inhibit myometrial contractions, it was hypothesized that nifedipine, indomethacin, and aminophylline in combinations would produce tocolytic synergism, which might have clinical value. To evaluate whether nifedipine, indomethacin, and aminophylline produce tocolytic synergisms when applied in dual and triple combinations on pregnant human myometrial tissue strips undergoing spontaneous rhythmic contractions ex vivo. Myometrial strips generating spontaneous contractions were treated with IC25 (25% inhibitory concentration) or IC50 (50% inhibitory concentration) concentrations of three different dual tocolytic combinations: nifedipine + indomethacin, nifedipine + aminophylline, and indomethacin + aminophylline, or one triple combination: nifedipine + indomethacin + aminophylline. The area under the curve (AUC) for the baseline contractility (100%) (pre-treatment) and following combination treatment (post-treatment) was measured for 1 h. For each tocolytic combination, the expected percent inhibition was calculated based on the individual tocolytic effects using the Bliss Independence Model and then compared with the experimentally observed inhibition. The combinational effect was considered synergistic if the experimentally observed inhibition (IC25(OBS) and IC50(OBS)) scores were significantly greater than the theoretically expected (IC25(EXP) and IC50(EXP)) inhibition scores. Contraction inhibition was significantly greater than expected for the dual combinations of nifedipine + indomethacin (n=6) [e.g., IC50(EXP) score (0.72) vs IC50(OBS) score (0.86); p=0.0003] and nifedipine + aminophylline (n=6) [e.g., IC50(EXP) score (0.72) vs IC50(OBS) score (0.92); p=0.0002], confirming synergism, whereas the dual combination of indomethacin + aminophylline produced only an additive effect (n=6) [e.g., IC50(EXP) score (0.68) vs IC50(OBS) score (0.74); p=0.25]. The triple combination of nifedipine + indomethacin + aminophylline (n=6) also yielded tocolytic synergism [IC25(EXP) score (0.51) vs IC25(OBS) score (0.73); p=0.0004] and achieved near complete inhibition of ex vivo contractility when constituent drugs were applied to myometrial strips at just IC25 concentrations. Of the four combinations examined, nifedipine + indomethacin, nifedipine + aminophylline, and nifedipine + indomethacin + aminophylline demonstrated synergism. The combination of indomethacin + aminophylline exhibited only an additive effect. Given the narrow therapeutic indications for tocolysis-primarily limited to short-term (≤48 hours) use to facilitate antenatal corticosteroid administration and maternal transfer-the synergistic lower-dose combinations identified here may enable more effective and safer tocolysis. These findings support further clinical investigation of combinational tocolysis to improve preterm birth outcomes while minimizing maternal and fetal adverse effects.

PMID 42248442
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