Drug Database
NI

nifedipine (Darbelan 10)

✓ Approved

Teva Pharmaceutical Industries Ltd. · CACNA1C · Small Molecule

What is nifedipine?

nifedipine is a small molecule developed by Teva Pharmaceutical Industries Ltd.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesDarbelan 10
CompanyTeva Pharmaceutical Industries Ltd.
Drug ClassSmall Molecule
Molecular TargetCACNA1C
RouteOral (PO)
StatusApproved

Mechanism of Action

Molecular Targets

nifedipine acts on 1 molecular target:

CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

nifedipine is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Cardiac disordersAngina pectoris✓ Approved
Vascular disordersHypertension✓ Approved

Related Research Articles

PubMedBMC cardiovascular disorders2026-05-24

Drug-induced psoriasis following sacubitril/valsartan: a case report and literature review.

Tang Tang T, Guo Mu M, Yu Huimin H, Zhang Yun Y et al.

Drug exposure is one of the potential mechanisms implicated in the onset or exacerbation of psoriasis. To date, several cardiovascular agents have been implicated. Sacubitril/valsartan (SV) has been widely used in the treatment of hypertension and heart failure (HF). Its common adverse reactions include angioedema, hypotension, renal impairment, and hyperkalemia. However, SV may cause psoriasis, which needs clinical attention. This report describes a case of a middle-aged male patient who developed psoriasis following SV therapy. The rashes presented as well-demarcated red or violaceous plaques with noticeable scaling. After being diagnosed with psoriasis, he was started on topical clobetasol propionate ointment, and SV was discontinued and replaced with ramipril for blood pressure control. During follow-up, the skin lesions showed marked improvement. However, the patient developed similar cutaneous manifestations again when SV was re-administered. He had previously developed psoriasis while using nifedipine, but transitioned to olmesartan and subsequently improved significantly with topical medication. Sacubitril enhances the effect of natriuretic peptides, which may be accompanied by a compensatory increase in angiotensin Ⅱ (Ang Ⅱ) levels, possibly contributing to the psoriasis. To the best of our knowledge, this is the first reported case worldwide of psoriasis potentially associated with SV, and the underlying mechanism appears likely to be related to sacubitril. It serves as a caution for clinicians prescribing SV, particularly in patients with a history of psoriasis or positivity for the HLA-Cw*0602 allele. Further studies are warranted to confirm the mechanism by which sacubitril induces psoriasis.

PubMedBMC pregnancy and childbirth2026-05-19

Antihypertensive drug use for hypertensive disorders of pregnancy in hospitals across nine Chinese cities: a real-world data study.

Zhu Zhenling Z, Tang Yong Y, Lv Jianfeng J, Wang Xianli X

To investigate the prescribing patterns of antihypertensive drugs for hypertensive disorders of pregnancy (HDP) in hospitals across nine chinese cities from 2019 to 2024. Medication use data for HDP patients were extracted from the database of the Hospital Pharmacy Committee of the Chinese Pharmaceutical Association, covering hospitals in nine major cities across China. The analysis included indicators such as total number of prescriptions, patient age, regional, average prescription cost, defined daily doses (DDDs), defined daily cost (DDC), and B/A ratio (ranking ratio). Furthermore, patterns of combination therapy and prescription rationality were assessed. Between 2019 and 2024, HDP patients were concentrated in the age of 30-34 years and in the North China region. Among outpatients, the top three antihypertensive drugs were oral labetalol (75.90%), oral nifedipine (17.42%), and oral methyldopa (3.36%). Among inpatients, the top three antihypertensive drugs were oral nifedipine (42.69%), oral labetalol (38.86%), and nicardipine for injection (5.84%). In outpatient, monotherapy accounted for 90.77%, followed by dual therapy (8.99%). Among inpatients, monotherapy constituted 60.01%, dual therapy accounted for 37.33%. Among drugs ranked high in terms of DDDs, oral labetalol had a B/A ratio of 1, with a daily cost of 12.31 CNY; oral nifedipine had a B/A ratio > 1, with a daily cost of 1.03 CNY; and nicardipine for injection had a B/A ratio < 1, with a daily cost of 474.41 CNY. The use of antihypertensive drugs in patients with HDP is gradually aligning with guideline-recommended treatment strategies.

PubMedBiochemical and biophysical research communications2026-05-19

A novel small-molecule secretagogue, MDC134, amplifies glucose-dependent insulin secretion in pancreatic β-cells.

Murao Naoya N, Takahashi Harumi H, Yokoi Norihide N, Okano Kentaro K et al.

Insulin secretion from pancreatic β-cells is controlled by multiple mechanisms, including metabolic, electrophysiological, and second-messenger pathways. To identify insulinotropic small molecules, we performed in silico similarity screening using zatebradine, an HCN-channel ligand, as a structural query and functionally evaluated 26 hit compounds. Compound 2 showed the strongest insulinotropic activity and was used to synthesize the novel compound MDC134. MDC134 enhanced insulin secretion in MIN6-K8 cells and isolated mouse islets under stimulatory glucose conditions. MDC134 enhanced insulin secretion in isolated mouse islets and showed a tendency to increase insulin secretion in isolated non-diabetic human islets. Under high-glucose conditions, MDC134 increased intracellular Ca2+ levels, and nifedipine abolished its insulinotropic effect, indicating the involvement of voltage-dependent L-type Ca2+ channel-mediated Ca2+ influx. MDC134 also increased cellular cAMP content, although less potently than GLP-1. MDC134 treatment did not clearly affect glucose tolerance in C57BL/6J or ob/ob mice but significantly suppressed glucose elevation in β-cell-specific Kcnj11 knockout mice. These findings identify MDC134 as a novel glucose-dependent insulinotropic small molecule that enhances β-cell insulin secretion through Ca2+ influx and cAMP-associated amplification, and suggest that it may be useful for therapeutic strategies for diabetes characterized by impaired insulin secretion.

PubMedJACC. Case reports2026-05-14

Intracoronary Electrocardiography During Dobutamine Stress for Functional Assessment of Myocardial Bridging.

Miyazaki Yoshichika Y, Kimpara Ami A, Soh Mitsuhito M, Sekine Otoya O et al.

Myocardial bridging (MB) can cause exertional ischemia, but functional assessment is challenging when ischemia is localized and undetected by surface electrocardiography (ECG). An 83-year-old man with vasospastic angina presented with recurrent exertional chest discomfort. Coronary angiography revealed MB in the mid-left anterior descending artery without significant epicardial stenosis. Intracoronary acetylcholine induced complete occlusion of a diagonal branch with symptom reproduction. Dobutamine stress testing using a pressure-sensor guidewire showed a resting full-cycle ratio ≤0.76 at 20 μg/kg/min, indicating functionally significant ischemia. Surface ECG remained unchanged; however, intracoronary ECG demonstrated marked ST-segment depression distal to the bridged segment, confirming localized ischemia. Switching medical therapy from nifedipine to diltiazem led to symptomatic improvement. Intracoronary ECG performed during dobutamine stress testing may enable direct visualization of localized myocardial ischemia associated with MB, even in the absence of ischemic changes on surface ECG.

PubMedAAPS PharmSciTech2026-05-13

Identifying Optimal Drug Loading in Stable Amorphous Solid Dispersion Formulations: A Rheological Approach.

Narala Sagar S, Yang Fengyuan F, Karan Kapish K, Kogan Michael M et al.

Synthetic polymers play a crucial role in enhancing the performance of drug formulations by enabling controlled release, improving bioavailability, and ensuring stability. Copovidone is frequently employed as an excipient in hot-melt extrusion (HME) to augment the solubility of active pharmaceutical ingredients (APIs). However, this method faces two significant challenges: identifying the optimal copovidone/API composition (the solubility of the crystalline API in the copovidone matrix) and the inadequate time-dependent stability of some amorphous APIs in the copovidone matrix. To overcome these issues, it's crucial to accurately assess the solubility and miscibility of the crystalline drug within the polymer, which is essential for developing a stable polymer/API amorphous system. This study utilized Plasdone™ S630 Ultra copovidone, a widely used solubility enhancer, to solubilize the poorly water-soluble active pharmaceutical ingredient (API) nifedipine. Several amorphous copovidone/nifedipine extrudates with drug loadings ranging from 10 to 60% w/w were produced via HME at temperatures above nifedipine's melting point to optimize the copovidone/API ratio for stability and homogeneity. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) measurements confirmed that all extrudates were amorphous regardless of drug loading (even at 60% w/w), as indicated by the presence of a single glass transition temperature and broad diffraction patterns. The extrudate stability and homogeneity were evaluated through a heat-cool temperature cycle using a rheometer. At lower drug loads, the extrudates exhibited homogeneity with consistent rheological behavior during the rheological temperature cycles. Medium drug loads led to slight rheological deviations, indicating a heterogeneous structure with API-rich areas. In contrast, high drug loads exhibited larger changes in rheological properties, likely indicating the dynamic formation of API nuclei. Although all extrudates exhibited enhanced solubility compared to their crystalline forms, those with higher drug loading showed poor physical stability, as evidenced by API recrystallization during accelerated-condition storage. In conclusion, this designed rheological study helps formulation scientists determine the optimal polymer/API composition (semi-phase diagram). This diagram and subsequent stability tests reveal that thermodynamic stability depends on the formulation composition, underscoring the importance of determining the API's solubility in the polymer.

PubMedEuropean journal of pharmacology2026-05-12

The effect of dehydroepiandrosterone on the vascular system: role of H2S/NO pathways.

Turnaturi Carlotta C, Indolfi Chiara C, Correale Melania M, Esposito Erika E et al.

Dehydroepiandrosterone (DHEA) is an adrenal steroid hormone that serves as a precursor to androgens and estrogens and participates in several physiological processes. Its levels naturally decline with age, and reduced DHEA concentrations have been associated with an increased risk of cardiovascular disease. However, this relationship is complex, and further research is required to clarify whether DHEA supplementation may help to prevent age-related vascular dysfunction. Here, we investigated the vascular effects of DHEA using mouse aorta and bovine aortic endothelial cells (BAEC), focusing on the potential involvement of hydrogen sulfide (H2S). DHEA exhibited a more pronounced vasorelaxant effect in endothelium intact aortas, mediated not only by nitric oxide (NO) but also by H2S. A significant increase in H2S production was observed following incubation of the aorta with DHEA compared to the vehicle. In addition to H2S, the involvement of L-type calcium channels in DHEA-induced vasorelaxation was found. Nifedipine, an inhibitor of L-type calcium channels, significantly reduced DHEA-induced vasorelaxation, and vice versa, suggesting a shared target. Consistent with the aortic findings, an increase in NO formation was observed in BAEC exposed to DHEA. Using two complementary approaches, we further demonstrate that DHEA enhanced H2S production in BAEC, with effects persisting for up to 2 h. Collectively, these findings suggest that DHEA promotes vasodilation through dual NO- and H2S-dependent pathways, along with modulation of L-type calcium channels. Our data provide new insights into the mechanisms of action of DHEA, supporting its protective role in the vasculature.

+9996 more articles available with a free account

Sign up free to view all articles →

Ask about nifedipine