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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 molecular histology2026-07-25

Dual modulation of intracellular Ca2+ signaling by hispidulin through endoplasmic reticulum mobilization and extracellular Ca2+ entry in human breast cancer cells.

Wang Nai-Yu NY, Chang Cheng-Chung CC, Chou Chiang-Ting CT, Chang Po-Min PM et al.

Hispidulin, a naturally occurring flavonoid found in various medicinal plants, exhibits anti-proliferative effects in multiple cancer models; however, its role in regulating intracellular calcium (Ca2+) signaling in human breast cancer cells remains unclear. Here, we investigated its effects on intracellular Ca2+ dynamics, cytotoxicity, and Ca2+-associated signaling in T-47D human breast cancer cells. Hispidulin (40-120 μM) induced a concentration-dependent increase in intracellular Ca2+ levels ([Ca2+]i) accompanied by reduced cell viability, and pretreatment with the intracellular Ca2+ chelator BAPTA-AM further enhanced cytotoxicity, indicating that disruption of Ca2+ homeostasis potentiates cell death. Removal of extracellular Ca2+ partially attenuated the response, with additional inhibition by nifedipine, a dihydropyridine-sensitive Ca2+ channel blocker, suggesting involvement of voltage-dependent Ca2+ influx. The Ca2+ response was also reduced by 2-aminoethoxydiphenyl borate (2-APB), an inhibitor of store-operated Ca2+ entry (SOCE), and by the protein kinase C (PKC) inhibitor GF109203X, implicating SOCE and PKC signaling. Thapsigargin-induced depletion of endoplasmic reticulum (ER) Ca2+ stores indicated that hispidulin mobilizes ER Ca2+, while phospholipase C (PLC) inhibition by U73122 completely abolished the [Ca2+]i increase. Collectively, these findings demonstrate that hispidulin regulates intracellular Ca2+ homeostasis via PLC-dependent ER Ca2+ release and extracellular Ca2+ influx through SOCE and nifedipine-sensitive Ca2+ entry components, leading to PKC activation. Enhanced cytotoxicity following Ca2+ chelation further underscores the importance of Ca2+ homeostasis in determining cellular responses to hispidulin.

PMID 42501117
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PubMedJournal of clinical hypertension (Greenwich, Conn.)2026-07-25

Serum Uric Acid Changes in Relation to Nighttime Blood Pressure Dipping Status in Patients on Antihypertensive Therapy.

Zhang Di D, Huang Qi-Fang QF, Li Yan Y, Wang Ji-Guang JG

We performed a post hoc exploratory secondary analysis to investigate whether baseline circadian blood pressure (BP) pattern was associated with changes in serum uric acid (SUA) during 8-week antihypertensive therapy. Of the 494 hypertensive patients who received amlodipine (5-10 mg) or nifedipine GITS (30-60 mg) for 8 weeks, 369 patients with available laboratory data and valid follow-up ambulatory BP monitoring data were included in the present analysis, including 221 dippers (nocturnal systolic BP decline ≥ 10%) and 148 non-dippers (nocturnal systolic BP decline < 10%). Analysis of covariance was used to estimate least square mean changes in SUA according to baseline dipping pattern. After 8-week antihypertensive treatment, SUA decreased significantly in dippers (-12.4 ± 3.4 µmol/L, p = 0.0004) but not in non-dippers (-3.3 ± 4.2 µmol/L, p = 0.44). In the repeated-measures analysis, SUA levels decreased significantly over time (p = 0.002), whereas no significant time-by-dipping interaction was observed (p = 0.23). Baseline BP dipping pattern may be modestly associated with short-term SUA changes during antihypertensive therapy. However, the absence of a significant time-by-dipping interaction suggests that these findings should be interpreted cautiously and require further confirmation.

PMID 42501048
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PubMedFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association2026-07-24

Lead-induced apoptosis in Sertoli cells is associated with Ca2+ dysregulation.

Zhang Chi C, Li Yunting Y, Zhang Yangle Y, Qiao Hanming H et al.

Lead (Pb) is a common environmental toxicant associated with male reproductive injury. Sertoli cells (SCs) are essential for spermatogenesis, but the mechanism of Pb-induced SC injury remains unclear. This study investigated whether Pb exposure induces SC apoptosis and explored the possible mechanisms involved. An early pubertal mouse model of Pb exposure and TM4 cells were used. Cell viability, morphology, apoptosis, apoptosis-related protein expression, intracellular Ca2+ levels, membrane potential-related fluorescence, and ERK phosphorylation were assessed. Nifedipine, Bay K8644, and U0126 were used for intervention. Pb exposure induced a pro-apoptotic molecular expression pattern in mouse testes. In TM4 cells, Pb reduced cell viability, induced morphological deterioration, and increased apoptosis in a concentration- and time-dependent manner. Pb also altered intracellular Ca2+ levels and membrane potential-related fluorescence. Nifedipine partially reversed Pb-induced changes in Bax and Bcl-2, whereas Bay K8644 produced no additional significant effect. Pb reduced the p-ERK1/2-to-total ERK1/2 ratio, and U0126 further suppressed ERK phosphorylation and aggravated apoptosis-related molecular alterations. Pb exposure induced apoptosis-related molecular alterations in mouse testes and apoptosis in TM4 SCs. These effects were associated with disrupted Ca2+ homeostasis, and inhibition of ERK signaling further aggravated Pb-induced apoptosis-related molecular alterations.

PMID 42492755
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PubMedBMC pregnancy and childbirth2026-07-21

Fetal cephalohematoma following external cephalic version: a case report.

Xie Jiangyan J

External cephalic version (ECV) is an obstetric procedure that involves manually turning the fetus inside the pregnant woman's abdomen to change a breech or transverse presentation to a cephalic presentation. It can significantly increase the proportion of cephalic presentations during delivery and reduce the cesarean section rate for term singleton breech presentations, making it a relatively safe operation. In this case, we report a case of fetal cephalohematoma following ECV, which has not been previously documented in the literature. A 33-year-old multiparous woman with a breech presentation underwent an ECV at 39 weeks and 1 day of gestation. Nifedipine was taken orally before the procedure to inhibit uterine contractions, and combined spinal-epidural anesthesia was performed. ECV was successful on the third attempt. On the 10th postoperative day, an ultrasound examination revealed a fetal cephalohematoma, and a cesarean section was eventually performed. The fetal cephalohematoma gradually resolved after birth, without causing severe adverse effects on the newborn. ECV has few complications and can significantly reduce the cesarean section rate in breech presentations. However, during the procedure, it is important to strengthen perioperative management and improve the operator's professional skills to reduce the risk of complications. The procedure should be performed gently, without unnecessary force.

PMID 42477611
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PubMedEuropean journal of obstetrics, gynecology, and reproductive biology2026-07-17

The association between oral antihypertensive agents and perinatal outcomes in early-onset fetal growth restriction: A post-hoc analysis of the Dutch OPTICORE study.

Hup Rosalie J RJ, van de Meent Mette M, Ganzevoort Wessel W, Gordijn Sanne J SJ et al.

Early-onset fetal growth restriction (FGR) and hypertensive disorders of pregnancy frequently co-occur, reflecting shared underlying placental pathology. We evaluated whether the type of oral antihypertensive agent (OAA) (i.e. methyldopa, labetalol, nifedipine, or a combination) is associated with birthweight or adverse perinatal outcomes in pregnancies complicated by early-onset FGR. A post-hoc analysis of the OPtimal TIming of antenatal COrticosteroid administration in early-onset fetal growth REstriction (OPTICORE) study was performed, including women treated with methyldopa, labetalol, nifedipine, or a combination. The primary outcome was birthweight. Secondary outcomes included gestational age (GA) and adverse perinatal outcome measures as defined by the Core Outcome Set for FGR (COSGROVE). Outcomes were compared separately in monotherapy and combination therapy groups. Adjusted multilevel linear or logistic regression analyses were performed. Of the 1,453 women included in the OPTICORE study, 849 (58.4%) received OAAs during pregnancy, with exposure groups ranging from 14 to 230 patients. No significant differences were found in absolute birthweight, GA, or adverse perinatal outcomes between monotherapy groups nor between combination therapy groups. Among early-onset FGR pregnancies, we found no differences in birthweight, GA, or adverse perinatal outcomes between the commonly used OAAs methyldopa, labetalol, and nifedipine when compared head-to-head, nor between different combination therapies. These findings suggest that OAA treatment in this context should not be guided by concerns regarding fetal growth or adverse perinatal outcomes. However, since some exposure groups included a limited number of patients and possible bias by indication, results should be interpreted with caution.

PMID 42462570
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PubMedEuropean journal of hospital pharmacy : science and practice2026-07-11

The optimisation of extemporaneous compounding of low-dose nifedipine capsules.

Pajula Katja K, Sunnarborg Rasmus R, Ramon Carla Riera CR, Lehtonen Marko M et al.

Extemporaneous compounding is often necessary when a suitable drug product is not on the market (eg, when the patient is a child). The medication of children often differs from adults as there are several excipients which are generally recognised as safe but which nevertheless are unsuitable ingredients for paediatric medication. Extemporaneous compounding is the only manufacturing method to tailor the final drug product with specific needs. However, the disadvantage is the lack of standardised instructions. The situation is even more difficult if the active pharmaceutical ingredient is light sensitive. The aim of the study was to optimise the extemporaneous compounding of low-dose nifedipine (NIF) capsules size 3 (0.3 mL) and 4 (0.21 mL) by comparing the volumetric and gravimetric methods. The suitability of several fillers-lactose (LAC), mannitol (MAN) and microcrystalline cellulose (MCC)-for capsule compounding was evaluated. The powder properties of NIF, LAC, MAN and MCC were characterised. The volumetric and gravimetric methods (12 batches) were evaluated by the European Pharmacopoeia (Ph. Eur.). The light degradation of NIF was studied with a UV-Vis spectrophotometer. All manufactured capsules met the Ph. Eur. requirements on uniformity of mass (2.9.5.). With regard to uniformity of content (2.9.6.), nine of the 12 batches met the Ph. Eur. However, deviation from the average content was greater with LAC than with MAN and MCC. According to the uniformity of dosage units (Ph. Eur. 2.9.40.), eight of the 12 batches met the requirements, with LAC being slightly poorer than MAN and MCC. Both volumetric and gravimetric methods were suitable for low-dose NIF capsule compounding. The powder loss during preparation was greater with the gravimetric method, even though it produced better quality capsules. MAN and MCC were slightly better than LAC as capsule fillers. Solid NIF degraded slowly when exposed to artificial light whereas dissolved NIF degraded in less than an hour.

PMID 42431730
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