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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 drug targeting2026-09-06

Ufasomal Nanocarriers for Enhanced Cardiac Delivery of Nifedipine: A Novel Strategy to Mitigate Doxorubicin-Induced Cardiotoxicity in Breast Cancer Therapy.

Farouk Hanan O HO, Abo El-Ela Fatma I FI, Baali Fahad H FH, Belal Amany A et al.

The cardiotoxicity of doxorubicin significantly restricts its effectiveness, even though it remains a crucial element of breast cancer chemotherapy. Nifedipine (NFP) offers multi-mechanistic therapeutic benefits, including vasodilation, anti-proliferative activities, suppression of cellular apoptosis, and potent anti-inflammatory and antioxidant properties. However, the translation of oral NFP into an effective cardioprotective adjuvant is hindered by its poor solubility, first-pass hepatic metabolism, and poor bioavailability. Hence, this study aimed to develop a nasal NFP-loaded ufasomes (NLU) spray formulation to enhance the permeation, bioavailability, sustained release, and cardiac accumulation of NFP when co-administered with doxorubicin. Various NLU formulations were developed and optimized employing Design-Expert® software. The in vivo cardioprotective efficacy of the nasal NLU was comprehensively evaluated in a doxorubicin-induced cardiotoxicity rat model. The optimal NLU substantially prolonged drug sustainability and amplified mucosal permeability by 69.07% and 6.47-fold, respectively, compared to the free NFP suspension. Furthermore, nasal NLU formulation achieved a remarkable 7.33-fold enhancement in bioavailability and a 5.40-fold increase in cardiac tissue accumulation when contrasted with conventional oral NFP administration. Furthermore, the nasal NLU spray exhibited superior cardioprotective and antioxidant performance over the oral NFP. In conclusion, these findings establish the nasal NLU formulation as a promising therapeutic platform to mitigate doxorubicin-induced cardiotoxicity.

PMID 42700144
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PubMedInternational journal of surgery case reports2026-09-06

The role of integrated radiology in diagnosis and treatment of renal artery stenosis: a case report.

Wahyono Djuwita Adi DA, Darmawan Marsha Ruthy MR, Drajat Endang E, Praptini Mirna Nurasri MN et al.

Renal artery stenosis (RAS) is a significant cause of ischemic nephropathy and secondary hypertension and is often underdiagnosed. While atherosclerosis predominates in older adults, younger patients are affected by various etiologies, such as fibromuscular dysplasia (FMD). Early diagnosis and intervention using integrated radiologic modalities are crucial to prevent irreversible end-organ damage in such patients. A 16-year-old male presented with a 6-month history of dizziness and refractory hypertension, with peak readings above 190/100 mm Hg despite aggressive antihypertensive therapy (amlodipine, nifedipine, and spironolactone). His physical examination was unremarkable except for elevated blood pressure (140/100 mmHg). Computed tomography angiography (CTA) of the renal arteries revealed a tight focal stenosis in the right renal artery, with post-stenotic dilation and collateral circulation to both poles of the right kidney. Selective digital subtraction angiography (DSA) confirmed these findings. Percutaneous transluminal renal angioplasty (PTRA) was performed using sequentially larger balloons (2.5 mm to 5.0 mm), and a vascular stent was deployed, achieving complete recanalization and robust distal flow. The patient was discharged on dual antiplatelet therapy with no complaints. This case highlights the utility of CTA for detailed anatomical assessment and DSA for confirmation and intervention. The need for stenting post-angioplasty due to residual stenosis underscores the importance of having a comprehensive endovascular strategy. Early and effective management of RAS is crucial to prevent long-term complications in young patients. Integrated imaging is essential for diagnosis, lesion characterization, and procedural planning in RAS patients. Endovascular revascularization is an effective treatment with early technical and clinical success.

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PubMedJournal of drugs in dermatology : JDD2026-09-04

Topical Sirolimus for Refractory Cutis Marmorata Telangiectatica Congenita in Adulthood: A Case Report.

Bhatt Ram D RD, Karpoff Kateryna K, Heitman Nicholas N, Aslam Rabail R et al.

Cutis marmorata telangiectatica congenita (CMTC) is a rare congenital vascular disorder characterized by persistent, violaceous, reticulated skin changes that may be complicated by painful ulcerations. Although localized disease often improves with age, generalized CMTC can persist into adulthood and may be associated with limb asymmetry, ocular abnormalities, and neurologic sequelae. Diagnosis can be challenging in atypical adult presentations despite established major and minor criteria. We report a case of a 50-year-old woman with congenital livedo reticularis and Raynaud syndrome who presented with lifelong unilateral left lower-extremity hypoplasia and fixed lacy violaceous patches. Over the preceding decade, she developed recurrent, spontaneous, painful ulcerations exacerbated by cold exposure. Examination revealed a hypoplastic left leg with reticulated violaceous patches and tender, crusted erosions without venectasia; biopsy findings ruled out vasculitis, and the overall clinicopathologic picture met all three major and multiple minor Kienast-Hoeger criteria for CMTC. Multiple therapies targeting vasospasm and microvascular flow (including sildenafil, pentoxifylline, diosmiplex, nifedipine, and aspirin) failed to improve symptoms. Initiation of once-daily topical sirolimus (1 mg/mL) resulted in marked pain reduction within four weeks and cessation of new ulcerations, with visible improvement and healed erosions by two months. This case supports topical sirolimus as a promising off-label option for adult CMTC with chronic ulcerative disease.

PMID 42696321
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PubMedNihon yakurigaku zasshi. Folia pharmacologica Japonica2026-09-03

[Revolutionizing physiology: advances in organ-on-a-chip technology].

Li Qiang Q, Takahashi Ken K

To address the low predictability (92% clinical failure rate) and high costs associated with species differences in traditional animal testing, this research advocates for New Approach Methodologies (NAMs) in alignment with the US FDA Modernization Act 2.0. The central achievement presented is the development of a "human Heart-on-a-chip." This microfluidic device co-cultures human iPS-derived cardiomyocytes, fibroblasts, and vascular endothelial cells to mimic living 3D tissue structures and fluid environments. The system demonstrated superior physiological reproducibility compared to conventional methods in evaluating drug responses (e.g., nifedipine) and detecting fatal side effects like QT prolongation. In addition to the heart, applications are advancing across diverse organ and disease models, including the construction of ischemia-reperfusion injury models using kidney chips and pulmonary fibrosis models using lung chips, the evaluation of barrier functions via blood-brain barrier (BBB) chips, and the analysis of interactions between cancer cells and immune cells using cancer chips. It is concluded that these technologies enable high-precision in vitro reproduction of human physiology and pathology, thereby improving the efficiency of drug screening, reducing economic losses, and accelerating the paradigm shift toward the 3Rs (Replacement, Reduction, and Refinement) in animal experimentation.

PMID 42686555
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PubMedNigerian journal of clinical practice2026-08-31

Comparison of Oral and Intravenous Nitroglycerin in the Treatment of Acute Postpartum Hypertension After Cesarean Delivery for Preeclampsia.

Incebiyik M M, Fedai H H, Tammo O O, Kizildemir Y Z YZ et al.

Acute postpartum hypertension is common among women with preeclampsia, particularly after cesarean delivery, and is traditionally managed with intravenous (IV) antihypertensive agents. However, evidence directly comparing IV nitroglycerin-based regimens with oral-only strategies is limited. To compare the efficacy of oral-only antihypertensive therapy versus IV nitroglycerin-based regimens in achieving 24-hour blood pressure control among women with preeclampsia after cesarean delivery. In this two-center retrospective cohort study, we included women with preeclampsia who developed acute hypertension within 24 hours after cesarean delivery. Patients were categorized into three groups: oral-only therapy, IV nitroglycerin plus oral therapy, and IV nitroglycerin-only regimens. The primary outcome was 24-hour blood pressure control (systolic <160 mmHg and diastolic <110 mmHg). Secondary outcomes included 30-day healthcare utilization and in-hospital complications. Multivariable regression models adjusted for baseline characteristics. All strategies achieved substantial blood pressure reduction. Rates of 24-hour control were high and comparable across groups ( P = 0.941), with no significant advantage of IV nitroglycerin over oral-only therapy after adjustment. Short-term clinical outcomes, including 30-day emergency visits ( P = 0.930) and in-hospital complications ( P = 0.810), were similar across groups. In subgroup analyses, IV nitroglycerin and oral nifedipine yielded similar hemodynamic responses. Oral-only therapy provides 24-hour blood pressure control and short-term outcomes comparable with resource-intensive IV nitroglycerin regimens. In stable postpartum patients, oral therapy can be used as first-line management.

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PubMedNeurology2026-08-31

Systematic Review of Pharmacologic Treatment for Migraine Prevention in Adults: Report of the AAN Guidelines Subcommittee and the American Headache Society.

Pringsheim Tamara T, Smith Don B DB, Tanveer Sarah S, Becker Werner J WJ et al.

This systematic review (SR) provides updated evidence-based conclusions regarding the use of pharmacologic migraine prevention in adults to inform a new joint American Academy of Neurology (AAN) and American Headache Society practice guideline. A multidisciplinary panel conducted an SR following the 2017 AAN Clinical Practice Guideline Process Manual. Randomized controlled trials evaluating pharmacologic preventive treatments for adults with episodic or chronic migraine were included. Searches encompassed MEDLINE, Embase, and ClinicalTrials.gov from database inception through June 6, 2024. Studies were screened in duplicate, with dual independent risk-of-bias assessment. Outcomes included change in monthly headache days, ≥50% responder rate, and validated patient-reported quality of life (QOL) measures. Raw mean differences, standardized mean differences, and risk ratios were calculated. A modified Grading of Recommendations Assessment, Development, and Evaluation process was used to classify certainty of evidence. A total of 217 studies met inclusion criteria. For episodic migraine, high-confidence evidence showed that galcanezumab and erenumab are more effective than placebo in reducing headache frequency. Moderate-confidence evidence supported benefit from atogepant, eptinezumab, fremanezumab, propranolol, topiramate, and valproate. Several additional oral agents including amitriptyline, bisoprolol, flunarizine, fluoxetine, levetiracetam, metoprolol, nifedipine, pizotifen, and telmisartan had low-confidence evidence suggesting possible benefit. For chronic migraine, high-confidence evidence supported reductions in headache frequency with fremanezumab, galcanezumab, and onabotulinumtoxinA. Moderate-confidence evidence supported benefit from atogepant, eptinezumab, erenumab, topiramate and valproate. Across both episodic and chronic migraine populations, erenumab, fremanezumab, galcanezumab, eptinezumab, rimegepant, atogepant, topiramate and onabotulinumtoxinA demonstrated improvements in patient-reported QOL outcomes on validated instruments. Evidence comparing active treatments was limited and generally of low or very low confidence, restricting conclusions about comparative effectiveness. This SR provides a comprehensive synthesis of evidence on pharmacologic migraine prevention in adults. High- and moderate-confidence findings confirm the efficacy of several established and newer preventive therapies and demonstrate improvements in patient-reported outcomes across multiple validated measures. These conclusions informed the development of evidence-based recommendations, presented in a companion publication, to guide clinicians in selecting preventive medications for adults with episodic and chronic migraine.

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