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diltiazem (Cardizem SR / Corolater)

✓ Approved

Bausch Health Companies Inc. · CACNA1C · 小分子

什么是 diltiazem？

diltiazem 是一种小分子，由Bausch Health Companies Inc.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Cardizem SR, Corolater
公司Bausch Health Companies Inc.
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, Bausch Health Companies Inc.

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 2 个适应症，涉及 2 个治疗领域。

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

相关研究文献

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Clinical efficacy, safety evaluation, and mechanism of acetylcysteine in improving first-line anti-tuberculosis treatment of newly diagnosed pulmonary TB: an open-label, randomized, single-center trial.

Zhang Huan H, Liu Ming M, Shi Lu L, Wang Xianlei X et al.

To investigate the clinical efficacy, safety and mechanism of N-acetylcysteine combined with conventional antituberculosis drugs in the treatment of newly diagnosed pulmonary tuberculosis. A total of 90 newly diagnosed pulmonary tuberculosis patients were randomly assigned to a Control group (n = 30), Aerosol NAC group (n = 30), or Oral NAC group (n = 30). The Control group received standard HRZE therapy, whereas the Aerosol NAC and Oral NAC groups received additional nebulized N-acetylcysteine (300 mg twice daily) or oral N-acetylcysteine (600 mg once daily), respectively. Clinical efficacy, sputum conversion, St. George's Respiratory Questionnaire (SGRQ) scores, liver function indices, oxidative stress biomarkers, inflammatory markers, and adverse events were assessed over 3 months. Data were analyzed using one-way ANOVA, repeated-measures ANOVA, Chi-square tests, and Bonferroni-adjusted post hoc analyses. Treatment successful response rates were significantly higher in the Aerosol NAC group (96.67%) and Oral NAC group (93.33%) than in the Control group (70.00%) (p < 0.05). At 3 months, sputum conversion rates reached 93.33 and 96.67% in the Aerosol NAC and Oral NAC groups, respectively, compared with 73.33% in the Control group (p < 0.05). Both NAC groups demonstrated significantly lower SGRQ scores, improved liver function parameters (AST, ALT, TBIL, and GGT), higher antioxidant enzyme levels (SOD and GSH-Px), lower MDA concentrations, and reduced inflammatory markers (IFN-γ, PCT, and IL-4) compared with the Control group (all p < 0.05). The incidence of adverse reactions was lower in both NAC groups (10.0%) than in the Control group (40.0%) (p < 0.05). Adjunctive N-acetylcysteine, administered either by aerosol inhalation or orally, significantly improved treatment outcomes, accelerated sputum conversion, reduced oxidative stress and inflammation, protected liver function, and decreased adverse events in patients with newly diagnosed pulmonary tuberculosis.

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PubMedFrontiers in dental medicine2026-09-10

Innovative herbal oil formulation as a pre-prosthetic mucosal conditioner: a prospective controlled cytological study on the degree of keratinization in edentulous ridge mucosa before and after Its topical application.

Dandekery Savitha S, Shetty Rajesh R, Shetty Sanath S, B Suman S et al.

Adequate keratinization of the edentulous ridge is fundamental for denture support, retention, stability, and mucosal resilience. This study evaluated the effect of topical Moringa oleifera stem bark oil on oral mucosal keratinization in edentulous ridges using a prospective controlled clinical trial design with a water-massage control group. One hundred and eight completely edentulous participants were enrolled between April 2025 and September 2025: a treatment group (n = 54) received twice-daily topical Moringa oleifera stem bark oil for four weeks, and a control group (n = 54) received twice-daily water massage of the same ridge area. Exfoliative cytology was performed at baseline (T0), Week 2 (T2), and Week 4 (T4). The in vitro cytocompatibility of the oil was additionally evaluated in human keratinocyte (HaCaT) cells using the MTT assay, performed in three independent experiments (biological triplicate), each with three technical replicates per concentration. Statistical analyses included the Friedman test (within-group temporal changes), the Wilcoxon signed-rank test with Bonferroni correction (post-hoc pairwise comparisons), and the Mann-Whitney U test (between-group comparisons) for the clinical cytology data. Effect sizes are reported as Kendall's W and rank-biserial correlation (r). The treatment group demonstrated a significant progressive increase in superficial keratinized cells, from a median of 57.5 at T0 to 114.0 at T4 [Friedman χ 2(2) = 59.40, p < 0.001, Kendall's W = 0.632]. Post-hoc Wilcoxon analysis confirmed significant improvements at each interval (all Bonferroni-corrected p < 0.001, r = 0.615-0.796). The control group showed no significant temporal change in superficial cells (Friedman p = 0.162, Kendall's W = 0.037). Between-group differences became more pronounced over time: superficial cell counts were not significantly different at baseline (p = 0.433), diverged at Week 2 (p = 0.002, r = 0.319), and were highly significantly different at Week 4 (p < 0.001, r = 0.777). The MTT assay (three independent experiments, each with technical triplicates; n = 3 per concentration) showed that the oil was non-toxic to HaCaT keratinocytes at concentrations up to 50 μg/mL. Mean cell viability trended higher than the untreated control in a concentration-dependent manner; however, this comparison was descriptive only, as no inferential statistical test was applied to the in vitro dataset, and the apparent trend should not be interpreted as a statistically confirmed effect. No adverse reactions were observed clinically. Topical Moringa oleifera stem bark oil was associated with a significant increase in cytological markers of keratinization, with no change in the water-massage control group, and descriptively demonstrated favourable in vitro cytocompatibility, with viability trending higher than control across tested concentrations (mean ± SD, three independent experiments); this in vitro trend was not evaluated by inferential statistics and warrants confirmation with formal statistical comparison in future work. These findings suggest promising potential as a pre-prosthetic mucosal conditioning approach, pending confirmation in larger, randomized, placebo (vehicle)-controlled trials with longer follow-up, histological verification, and patient-centred outcomes. Clinical Trial Registration: CTRI/2025/04/084650; Patent Publication No. 202241052361. (https://ctri.nic.in) CTRI/2025/04/084650; Patent Publication No. 202241052361.

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Short-Term Efficacy and Safety of Topical Sirolimus Gel in Pediatric Superficial Microcystic Lymphatic Malformations: A Single-Center Interventional Study of 30 Patients.

Xu Weiyang W, Ding Yu Y, Zhao Lei L, Pi Mengqi M et al.

To evaluate the efficacy and safety of 0.2% topical sirolimus gel for pediatric superficial microcystic lymphatic malformations (LMs). This single-center interventional study included 30 pediatric patients (14 males and 16 females; aged 2-15 years) with superficial microcystic lymphatic malformations. All patients received 0.2% topical sirolimus gel twice daily for 12 weeks according to a predefined treatment and follow-up protocol. Clinical efficacy was assessed at baseline and week 12 using clinical examination, standardized photography, symptom scores, and available imaging findings, together with a four-grade physician-assessed response scale. Adverse events were monitored throughout treatment, and blood sirolimus concentrations were measured at weeks 4 and 12. All patients showed lesion reduction, with an overall response rate of 96% (29/30). At week 12, efficacy was graded as IV in 10 patients, III in 11, II in 8, and I in 1. Among patients with pain symptoms, pain scores decreased significantly after treatment (2.88 ± 0.78 vs 1.18 ± 0.88; P < 0.05). In 10 patients with measurable lesions, maximum lesion diameter decreased significantly from 3.22 ± 1.36 cm to 1.89 ± 1.33 cm (P < 0.05). Only mild local adverse effects were observed, and blood sirolimus concentrations remained below 2.0 ng/mL in all patients. Topical sirolimus gel demonstrated favorable efficacy and safety for pediatric superficial microcystic LMs.

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A Dose-Escalation Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of HP501 in Male Chinese Gout Patients with Hyperuricemia.

Chen Longxia L, Ding Ruilin R, Chen Yuanwei Y, Li Xinghai X et al.

HP501, a novel highly selective renal urate transporter 1 (URAT1) inhibitor, represents a promising therapeutic option for hyperuricemia. This Phase I study evaluated the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of HP501 in Chinese gout patients. 37 patients with gout and hyperuricemia were enrolled in this single-center, open-label, dose-escalation study. Participants were sequentially assigned to receive HP501 at 60, 80, and 100 mg twice daily (BID) following single- and multiple-dose regimens. Safety assessments, PK parameters, and PD reductions were systematically evaluated. HP501 demonstrated an acceptable safety and tolerability profile across all dose cohorts. The most common adverse events (≥10% of patients) included gout flare (36.1%), prostatic hypertrophy (36.1%), elevated ALT (16.7%), and kidney stones (11.1%), all of which were mild to moderate in severity. PK analysis revealed dose-proportional increases in Cmax and AUC (60 to 100 mg BID), with corresponding dose-dependent reductions in serum UA levels. All patients achieved therapeutic UA targets (<360 µmol/L). These findings support the clinical advancement of HP501, with 60 to 100 mg BID identified as the recommended dose range for further investigation in subsequent trials. However, these findings are preliminary and limited by the single-center design, small sample size, and exclusion of female patients, warranting confirmation in larger, more diverse populations.

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Comparison of two self-reported tools for assessment of sleep quality.

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An easy to administer tool is needed for clinical assessment of sleep quality by healthcare providers. This study compared two brief, validated sleep questionnaires in order to identify an appropriate tool for clinical assessment. Women (N = 121) between the ages of 25-89 years (60.3 ± 15.9 years) completed the Richards-Campbell Sleep Questionnaire, the Restorative Sleep Questionnaire, and associated measures of quality of life, well-being, stress, and physical activity. There were no differences in sleep quality assessments between the two questionnaires for sleep last night (daily), during the past 7 days (weekly), or during the past 4 weeks (monthly). Overall, participants reported good daily, weekly, and monthly sleep quality (mean scores 71.1-75.3 out of 100), although both questionnaires assessed significantly better (p ≤ 0.002) daily sleep quality compared to weekly and monthly. There were no floor effects for either questionnaire, but ceiling effects were noted for the Richards-Campbell Sleep Questionnaire daily and weekly versions. When participants were grouped by sleep quality, very good sleepers reported better quality of life (p˂ 0.05) and well-being (p˂ 0.001), and less stress (p˂ 0.05) compared to poor sleepers for all versions of the Restorative Sleep Questionnaire and for the Richards-Campbell Sleep Questionnaire daily and weekly versions. For overall identification and assessment of good versus poor sleep quality, clinicians can choose either the Richards-Campbell Sleep Questionnaire or the Restorative Sleep Questionnaire. However, caution may be needed for short-term (daily, weekly) assessment for which the Restorative Sleep Questionnaire may be more appropriate due to fewer ceiling effects.

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Morphine tolerance limits its long-term clinical utility, and neuroinflammation is a key underlying mechanism. This study investigated whether zonisamide, an antiepileptic drug with anti-inflammatory properties, attenuates morphine-induced neuroinflammation and morphine tolerance. In vitro, BV-2 microglial cells were treated with morphine (200 μM) with or without zonisamide (10 μM). Quantitative real-time PCR, enzyme-linked immunosorbent assay (ELISA), and Western blot analysis were used to assess inflammatory mediators and signaling pathways. In vivo, male C57BL/6 mice received repeated morphine injections (10 mg/kg, s.c., twice daily) for 9 days to induce tolerance, with or without zonisamide (30 mg/kg, i.p.). Behavioral tests (hot plate and tail flick) were performed to evaluate analgesic tolerance. Immunofluorescence was performed to assess microglial activation (Iba1), and Western blot analyses were conducted to evaluate TLR4 expression, p38 phosphorylation, and pro-inflammatory cytokine protein levels. Pharmacological inhibition of TLR4 with TAK-242 was used to verify the involvement of TLR4 signaling. In vitro, zonisamide suppressed morphine-induced upregulation of interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF)-α, and Toll-like receptor 4 (TLR4) mRNA, reduced morphine-induced secretion of IL-1β, IL-6, and TNF-α at the protein level, and inhibited morphine-induced p38 mitogen-activated protein kinase (MAPK) phosphorylation. In vivo, zonisamide did not affect acute morphine analgesia but significantly attenuated the development of chronic morphine tolerance. Spinal cord analyses revealed that zonisamide reduced microglial activation (Iba1), TLR4 expression, p38 phosphorylation, and pro-inflammatory cytokine (IL-1β, TNF-α) protein levels. Pharmacological inhibition of TLR4 with TAK-242 produced a behavioral effect similar to that of zonisamide, and combined treatment did not provide additional benefit, suggesting overlapping signaling effects. These findings indicate that zonisamide attenuates morphine tolerance in association with reduced spinal TLR4/p38 MAPK signaling and neuroinflammation. This study provides a mechanistic rationale for repurposing zonisamide as an adjunct therapy to improve long-term pain management and mitigate opioid-related adverse effects.

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