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diltiazem (diltiazam, Aptalis / diltiazem, SURECAPS)

✓ Approved

Adare Pharma Solutions · CACNA1C · 小分子

什么是 diltiazem？

diltiazem 是一种小分子，由Adare Pharma Solutions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diltiazam, Aptalis, diltiazem, SURECAPS
公司Adare Pharma Solutions
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, Adare Pharma Solutions

作用机制

分子靶点

diltiazem 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

diltiazem 针对 1 个适应症，涉及 1 个治疗领域。

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

相关研究文献

PubMedCatheterization and cardiovascular interventions : official journal of the Society for Cardiac Angiography & Interventions2026-09-09

Acute Inferior Myocardial Infarction with Anomalous Origin of the Right Coronary Artery, Myocardial Bridging and Fibro-Lipid Plaque.

Shen Jun J, Wu Yanming Y, Wang Biao B

We describe a 35-year-old male patient who had acute inferior myocardial infarction based on clinical signs and electrocardiographic abnormalities after experiencing sudden chest pain for 2 h. An abnormal origin of the right coronary artery (RCA) from the left coronary sinus was discovered by emergency coronary angiography, along with mild stenosis in the mid-RCA segment that persisted even after intracoronary nitroglycerin was administered. The mid-RCA lesion was identified by intravascular ultrasonography (IVUS) as a 48% stenotic fibro-lipid plaque with a lipid core and thin fibrous top. A minimum luminal diameter of 2.14 mm was found at the deformed RCA ostium with concomitant myocardial bridging. The patient experienced total symptom alleviation and an uneventful recovery after receiving dual antiplatelet therapy, intense lipid-lowering treatment, diltiazem for myocardial bridging, and stringent risk factor control. For long-term risk reduction, a multidisciplinary evaluation is planned for surgical of the coronary abnormality. In addition to highlighting the significance of tailored management approaches for congenital coronary anomalies combined with acquired vulnerable plaques, this case underscores the crucial role of multimodality imaging, particularly IVUS, in accurate etiological diagnosis and treatment decision-making for young patients with acute myocardial infarction (AMI) caused by complex coronary lesions.

PMID 42712015
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PubMedNutricion hospitalaria2026-09-07

[Oral urea as a safety strategy in complex syndrome of inappropriate antidiuretic hormone secretion - Challenges posed by polypharmacy and institutionalization].

Figueredo Carme C, Azketa Ane A, Orois Añón Aida A, Solé Sancho Judith J et al.

syndrome of inappropriate antidiuretic hormone secretion (SIADH) is a common cause of euvolemic hyponatremia in older adults. we report the case of a 72-year-old woman with chronic SIADH, probably secondary to sertraline, in the setting of polyp harmacy and chronic liver disease. Initially, serum sodium normalized with fluid restriction guided by the Furst formula under caregiver supervision. Following the death of her primary caregiver and admission to a long-term care facility, an increase in sertraline dosage and the inability to maintain fluid restriction led to recurrent hyponatremia (serum sodium 126 mEq/l). Tolvaptan was avoided because of the risk of interaction with diltiazem (CYP3A4 inhibitor) and underlying liver disease. Oral urea was initiated and titrated to 30 g/day, achieving gradual and sustained normalization of serum sodium (134-135 mEq/l) without adverse effects or changes to her psychotropic treatment. Six months later, the patient remains clinically stable on 15 g/day of oral urea with progressive sertraline dose reduction. this case highlights oral urea as a safe, effective, and cost-effective therapeutic option for SIADH when fluid restriction is not feasible and vaptans are unsuitable, particularly in frail older adults with polypharmacy and complex social circumstances.

PMID 42704000
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PubMedImmunobiology2026-08-28

Luhong formula attenuates cardiomyocyte hypoxia/reoxygenation injury in vitro through SLC7A11-mediated ferroptosis.

Zhang Saiwen S, Zhou Dan D, Zhou Yaozhong Y, Cai Wan W

This study investigates whether Luhong Formula (LHF) inhibits hypoxia/reoxygenation (H/R)-induced ferroptosis in cardiomyocytes and the underlying mechanism. H9c2 cells were subjected to H/R injury and treated with LHF extract, diltiazem (positive control), or Fer-1 (ferroptosis inhibitor). CCK-8, colorimetric assays, and transmission electron microscopy showed that LHF significantly increased cell viability, reduced LDH release, restored SOD activity and GSH content, and alleviated mitochondrial damage. FerOrange staining and C11-BODIPY flow cytometry revealed that LHF decreased intracellular Fe2+ levels and lipid ROS accumulation. Immunofluorescence and Western blot demonstrated that LHF up-regulated GPX4 expression, showing effects comparable to those of Fer-1 and diltiazem in this in vitro system. Using SLC7A11-overexpressing and -silencing stable cell lines, we found that SLC7A11 overexpression mimicked LHF's protective effects, while SLC7A11 silencing partially reversed them. Co-immunoprecipitation confirmed that H/R increased SLC7A11 ubiquitination, whereas LHF reduced this modification, thereby stabilizing SLC7A11 protein. Collectively, LHF is associated with reduced SLC7A11 ubiquitination, which correlates with up-regulated GPX4 and blocked ferroptosis, alleviating H/R injury in cardiomyocytes. These findings provide preliminary evidence for a potential regulatory effect of LHF on SLC7A11 protein stability, although direct measurements of protein half-life and detailed ubiquitin topology require further investigation. These findings suggest that LHF inhibits H/R-induced ferroptosis in H9c2 cells, at least in part, through the SLC7A11/GPX4 pathway, which may contribute to its cardioprotective effect.

PMID 42664531
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PubMedJournal of veterinary internal medicine2026-08-27

Effect of amiodarone, diltiazem, or both to achieve strict heart rate control in dogs with atrial fibrillation.

Tjostheim Sonja S SS, Kellihan Heidi B HB, Stepien Rebecca L RL

Dogs with atrial fibrillation (AF) live longer if heart rate is strictly controlled (SHRC, 24-h mean heart rate ≤ 125 beats per minute [bpm]). Amiodarone and diltiazem are used to lower ventricular response rate (VRR) in dogs with AF, but information about their relative efficacy for achieving SHRC is lacking. Describe heart rate response with sequential escalation of amiodarone or diltiazem monotherapy to combination therapy. Thirteen client-owned dogs with AF. Prospective cohort study with an adaptive treatment protocol. Dogs with AF with mean daily heart rate (MDHR) > 125 bpm (baseline, 24-h Holter) were randomized to receive amiodarone or diltiazem at standard doses. Dogs were reassessed 21 days later, and the other drug (amiodarone or diltiazem) was added if SHRC was not achieved. Dogs were then reassessed at 42 and 63-147 days after starting treatment. If MDHR >125 bpm at any repeat assessment, the second drug was added. Timing of final assessment was dependent on whether treatment was escalated. Monotherapy with amiodarone and diltiazem was initially used in 7 and 6 dogs, respectively. SHRC was achieved in 3 dogs (amiodarone, n = 2; diltiazem, n = 1) at first follow-up. At last follow-up, 11 of 13 dogs were receiving both drugs (median [range] 50 [20-153] days). Combination therapy of amiodarone and diltiazem did not result in SHRC (139 [94-160] bpm) in most dogs (7/11, 64%). Monotherapy with amiodarone or diltiazem or combination therapy of amiodarone/diltiazem did not achieve SHRC in most dogs in this study.

PMID 42658783
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PubMedNeurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology2026-08-25

A novel CACNA1S variant associated with diltiazem-related worsening of hypokalemic periodic paralysis: a case report.

Sugiura Hidenori H, Watanabe Kazuki K, Furuhashi Kai K, Kawano Tatsuhiro T et al.

Hypokalemic periodic paralysis (HypoPP) is a skeletal muscle channelopathy characterized by recurrent episodes of transient paralysis associated with hypokalemia. Most cases are caused by heterozygous missense variants in CACNA1S, which encodes the α1 subunit of the skeletal muscle L-type calcium channel (CaV1.1). Known triggers include excessive carbohydrate intake, rest after strenuous exercise, and emotional stress; however, worsening potentially associated with the use of L-type calcium channel blockers (LTCCBs) has not been well documented. A 68-year-old man with HypoPP and a five-generation family history of the disease developed increased frequency of paralytic attacks and progressive muscle weakness after initiation of LTCCBs (nifedipine and diltiazem) for vasospastic angina. Exome sequencing and segregation analysis identified a novel heterozygous CACNA1S variant (NM_000069.3:c.4097T > G, p.(Met1366Arg)), which co-segregated with disease among genotyped affected family members and was classified as likely pathogenic. Despite continued nifedipine therapy, paralytic episodes ceased following discontinuation of diltiazem, and muscle strength improved. The p.(Met1366Arg) variant is located in the S6 segment of CaV1.1, outside the canonical S4 arginine residues implicated in most cases of CACNA1S-related HypoPP; nevertheless, strong intrafamilial segregation evidence supports its pathogenicity. Furthermore, its proximity to the diltiazem-binding site raises the possibility of altered drug-channel interactions. The observed diltiazem-associated worsening of HypoPP may be variant-specific rather than a class effect of LTCCBs. Nevertheless, careful monitoring may be warranted when prescribing these agents to patients with HypoPP.

PMID 42637926
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PubMedBMJ open2026-08-20

Potentially inappropriate prescribing in Iranian elderly population: a nationwide claims-based analysis.

Kharaghani Mohammad Amin MA, Kianipour Reza R, Ataei Seyed Mohammad-Navid SM, Ebrahimpour Sholeh S et al.

Potentially inappropriate prescribing (PIP) in the elderly is associated with adverse outcomes and increased healthcare use. We aimed to estimate its prevalence and pattern among the elderly population of Iran using the Screening Tool of Older Persons' Prescriptions (STOPP) criteria. Retrospective, population-based observational study. Nationwide data of Iran Health Insurance Organization (IHIO) prescription claims from 24 provinces (21 March 2014 to 19 March 2017). Adults aged ≥60 years with at least one prescription in the dataset were included. The study comprised 2 696 300 older adults who received 28 575 400 prescriptions. Not applicable. Using a two-stage curation process, we selected STOPP version 3 criteria that could be operationalised from dispensing data alone (age, Anatomical Therapeutic Chemical code, dose, duration and concurrent use). For each criterion, we calculated prescription and patient level PIP prevalence overall and among at-risk prescriptions. Across the curated STOPP criteria, 313 315 prescriptions issued to 131 012 patients met at least one PIP criterion. The most frequent PIPs were concurrent beta blocker and diltiazem use (99 027 prescriptions; 1.26% of patients), benzodiazepine therapy ≥4 weeks (89 240 prescriptions; 1.60% of patients), ≥2 anticholinergic drugs (47 079 prescriptions; 0.78% of patients) and concomitant non-steroidal anti-inflammatory drug plus anticoagulant (25 685 prescriptions; 0.38% of patients). PIPs involving acetylcholinesterase inhibitors, ticlopidine, clonidine and methyldopa were rare. In this nationwide claims-based study, about 5% of elderly Iranians were exposed to PIPs, particularly chronic benzodiazepine use, excessive anticholinergic burden and high-risk cardiovascular and antithrombotic combinations. Our findings provide concrete targets for claims-based surveillance and interventions to improve prescribing safety in Iran's ageing population.

PMID 42624577
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