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nitroglycerin (Millisrol Tape)

✓ Approved

Nippon Kayaku Co.,Ltd. · 小分子 · 小分子

什么是 nitroglycerin？

nitroglycerin 是一种小分子，由Nippon Kayaku Co.,Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Transdermal。

药物档案

商品名Millisrol Tape
公司Nippon Kayaku Co.,Ltd.
药物类别小分子
给药途径Transdermal
状态Approved
来源： ClinicalTrials.gov, Nippon Kayaku Co.,Ltd.

治疗适应症

nitroglycerin 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

PubMedChemical record (New York, N.Y.)2026-09-10

From Barrier Disruption to Precision Skin Interface Engineering: Next-Generation Transdermal Drug Delivery.

Zhou Cong-Zheng CZ, Lin Xin-Yu XY, Yu Shou-Shan SS, Qiao Sheng-Lin SL

Transdermal drug delivery (TDD) is reemerging as a clinically attractive route for noninvasive therapy, driven by the growing demand for alternatives to repeated injection and by the rapid development of materials capable of regulating transport across the skin. By avoiding gastrointestinal degradation and hepatic first-pass metabolism, TDD can provide prolonged drug exposure, reduce peak-to-trough fluctuations in plasma concentration, and improve adherence in long-term treatment. Its broader implementation, however, is still constrained by the exceptional barrier function of the stratum corneum, which severely limits the passive transport of hydrophilic molecules, charged species, and macromolecular therapeutics. In this review, we critically discuss the structural basis of the skin barrier and summarize the evolution of TDD strategies from conventional chemical permeation enhancement and device-assisted physical disruption to nanocarrier-mediated, biomimetic, and intelligent bio-delivery systems. Particular emphasis is placed on the mechanistic logic that connects carrier composition, interfacial interactions, skin microenvironment remodeling, and therapeutic performance. Representative examples are analyzed to highlight both opportunities and translational bottlenecks. Finally, we outline future directions in multimodal delivery, pathology-adapted design, standardized evaluation, and scalable manufacturing, which will be essential for transforming TDD from a permeability enhancement technology into a precision-regulated therapeutic platform.

PMID 42717625
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PubMedJournal of medicinal chemistry2026-09-10

Structure-Function Analysis of the Benzyloxy Moiety of the Delta-Opioid Receptor Positive Modulator BMS-986187: Identification of a Derivative with High Selectivity for the Delta-Opioid Receptor over the Mu-Opioid Receptor In Vitro and In Vivo.

Li Mengchu M, Zhang Sherrice S, Powell Alexander J AJ, Stewart Hannah C HC et al.

Positive allosteric modulators (PAMs) of the delta-opioid receptor (DOR) enhance endogenous opioid signaling while avoiding the convulsant liability of orthosteric agonists. However, the prototypical DOR-PAM, BMS-986187, also potentiates mu-opioid receptor (MOR) signaling, raising concerns regarding respiratory depression and abuse liability. Here, we report a structure-activity study of the benzyloxy moiety of BMS-986187 to improve selectivity for DOR over MOR, while retaining DOR-PAM potency. Fifty-two new analogues and 12 previously reported ones featuring mono- and disubstitution of the benzyl ring and phenyl-heterocycle replacements were synthesized and evaluated in β-arrestin2 recruitment assays. Ortho-substituted derivatives consistently enhanced DOR-PAM potency, although often increased MOR-PAM activity. One pyridyl derivative (compound 35) retained high DOR-PAM potency and efficacy (EC50 = 0.1 μM, Emax = 91%) with no detectable MOR activity. In mice, compound 35 enhanced DOR-mediated reversal of nitroglycerin-induced hyperalgesia, an effect absent in DOR-knockout mice, without enhancing MOR-mediated antinociception, demonstrating in vivo selectivity.

PMID 42720491
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PubMedJournal of acute medicine2026-09-10

Profile and Outcomes of Patients Presenting With Sympathetic Crashing Acute Pulmonary Edema (SCAPE) to a Tertiary Care Emergency Department in North India: A Prospective Observational Study.

Sharma Ankit A, Bhardwaj Bharat Bhushan BB, Arora Poonam P, Mathew Roshan R et al.

Sympathetic crashing acute pulmonary edema (SCAPE) is a severe manifestation of acute heart failure, characterized by sudden pulmonary edema due to elevated sympathetic activity. This study aimed to describe the clinical profile, management, and short-term outcomes of patients with SCAPE presenting to a tertiary care hospital in North India. This prospective observational study described the clinical profile of patients with SCAPE who were managed with high-dose nitroglycerin (NTG). Sixty-two patients with a mean age of 49.4 years were enrolled, and 90.3% had one or more comorbidities. All patients exhibited signs of sympathetic excess and pulmonary edema on point-of-care ultrasound (POCUS). The treatment protocol included high-dose NTG and non-invasive ventilation (NIV). Male sex, chronic kidney disease, longer symptom duration, plethoric inferior vena cava on POCUS, higher initial lactate, and the need for hemodialysis were identified as predictors of poor outcomes in the univariate analysis. This study highlights that a protocol-based approach using high-dose NTG and NIV in managing SCAPE patients shows a favorable outcome, resulting in low rates of mechanical ventilation and mortality despite high comorbidity burden and ICU admission rates.

PMID 42719725
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PubMedCureus2026-09-10

Treating Intractable Nausea and Vomiting in Cerebellar and Medullary Stroke.

Bhatti Adil A, Schultz Peter P, Amin Shantanu S, Khalid Taimur T et al.

Cerebellar and medullary stroke can cause persistent nausea and vomiting that may be resistant to initial antiemetic monotherapy and interfere with oral intake and recovery. Evidence guiding management remains limited. We report a 48-year-old man with diabetes mellitus and acute-to-subacute infarcts involving the inferomedial right cerebellum and posterior right medulla who presented with 10 days of persistent nausea and vomiting accompanied by focal neurologic symptoms. Diabetic gastroparesis was considered, but abdominal imaging and gastric emptying scintigraphy did not support a contributory gastrointestinal cause. Ondansetron and metoclopramide provided only limited or temporary relief. Symptoms improved after sequential escalation to ondansetron, chlorpromazine, prochlorperazine, and amitriptyline; transdermal scopolamine was included in the discharge regimen. Nausea and vomiting were nearly resolved before discharge and fully resolved by three-month follow-up. Because multiple medications were introduced over a short interval and natural neurologic recovery may have contributed, the effect of any individual agent or combination cannot be determined. This case suggests that receptor-diverse pharmacotherapy may be considered when initial treatment fails while underscoring the need for further study of efficacy, safety, and medication sequencing.

PMID 42719464
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PubMedDrugs in R&D2026-09-09

Study on the Pharmacokinetics and Pharmacodynamics of Transdermal Estradiol Gel Administered Repeatedly in Postmenopausal Women.

Sirviö Jouni J, Ahtola-Sätilä Tuula T, Kirjavainen Merja M, Rytilä Paula P

Transdermal administration of estrogen has established its positioning among hormone replacement therapies in menopause. In Divigel® (estradiol hemihydrate gel 0.1%), 17β-estradiol, a body-identical estrogen, is formulated to be absorbed through the skin. This study aimed to provide systematic data on the pharmacokinetics and pharmacodynamics of Divigel to further enable its use in individualized therapies. The study was conducted over a 14-day treatment period using three escalating doses (0.5 mg, 1.0 mg, and 1.5 mg) in ten postmenopausal women. A 3-day or 4-day follow-up period was conducted after each treatment period. Wash-out between the periods was at least 2 weeks. The serum levels of estradiol (E2) and its metabolite estrone (E1) were analyzed, and the therapeutically informative ratio of E2/E1 was calculated. In addition, the temporal course of the excretion of E1, E2, and estriol (E3) in urine was studied. Serum levels of gonadotropins, follicle-stimulating hormone and luteinizing hormone, were measured as pharmacodynamic biomarkers. Serum concentrations of E2 were proportional to dose, and profiles were dose dependent. A steady-state E2 concentration was achieved within 3-5 days of daily administration of 1.0-mg and 1.5-mg doses. After the first and last application, the serum E2/E1 ratio increased clearly above 1.0 within 2-12 hours post-dose, i.e., approximating premenopausal levels, whereas it returned and remained close to parity at steady state, which still is clearly above the measured baseline (menopausal) levels. The urine levels of E1 and E3 were comparable and much higher than E2 urine levels. After the last application on day 14, the average serum concentration values of E2 (calculated as area under the concentration-time curve from time 0 to 24 hours divided by the 24-hour application interval) were 12.4 ± 7.0, 29.7 ± 7.3, and 55.0 ± 33.1 pg/mL at 0.5-mg, 1.0-mg and 1.5-mg doses, respectively. Those fit into the clinically effective concentration range at the doses of 1.0 mg or 1.5 mg in all the subjects. Follicle-stimulating hormone levels were lower after application of Divigel at every dose compared with their pre-dosing baseline. Luteinizing hormone levels also decreased following E2 administration. Treatment was well tolerated, and no safety concerns or skin reactions were observed. Transdermal estradiol treatment with Divigel produced dose-proportional, clinically meaningful serum E2 levels and E2/E1 ratios in postmenopausal women. All administered doses also showed expected hormonal pharmacodynamic effects and were well tolerated. Not applicable in the USA and European Union for a pharmacokinetic study commenced in 1999.

PMID 42714801
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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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