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enalapril maleate + HCTZ (Vasoretic / Vaseretic / Renidur)

✓ Approved

Merck & Co. · ACE · 小分子

什么是 enalapril maleate + HCTZ？

enalapril maleate + HCTZ 是一种小分子，由Merck & Co.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Vasoretic, Vaseretic, Renidur
公司Merck & Co.
药物类别小分子
分子靶点ACE, SLC12A3
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Merck & Co.

作用机制

分子靶点

enalapril maleate + HCTZ 作用于 2 个分子靶点：

ACEangiotensin I converting enzyme (DCP1, ACE1)
SLC12A3solute carrier family 12 member 3 (NCCT, NCC)
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

enalapril maleate + HCTZ 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
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedJournal of applied toxicology : JAT2026-10-26

Large-Scale Monitoring, Biochemical Mechanism, and Fitness Cost of Resistance to Chlorfenapyr in a Near-Isogenic Strain of Spodoptera litura (Lepidoptera: Noctuidae) From China.

Liu Chenghong C, Tang Juan J, Qu Cheng C, Ma Xiaoli X et al.

Spodoptera litura is a globally important polyphagous herbivore that has developed resistance to many widely used insecticides. Chlorfenapyr is a pyrrole insecticide with demonstrated efficacy against lepidopteran pests, but the susceptibility baseline and field-evolved resistance in S. litura remain poorly characterized. In this study, we built a near-isogenic strain (JZ-NIL) based on one field-collected chlorfenapyr-resistant population of S. litura and characterized patterns of cross-resistance, fitness costs, and mechanism of metabolic resistance. In comparison with the susceptible Lab-S strain, the field-sampled JZ population displayed approximately 225.0-fold resistance to chlorfenapyr. The JZ-NIL strain was built and showed 124.2-fold chlorfenapyr resistance, with no apparent cross-resistance to broflanilide, chlorpyrifos, chlorantraniliprole, emamectin benzoate, indoxacarb, and spinetoram. Assays of enzyme activity and tests of synergism showed that diethyl maleate (DEM) made a synergistic ratio of 1.9 against chlorfenapyr, and glutathione S-transferase (GST) activity in JZ-NIL was 1.8-fold significantly higher than in the strain of Lab-S, indicating that GST-mediated metabolism contributes to chlorfenapyr resistance. In addition, pupation rate, fecundity, and hatchability were significantly lower in JZ-NIL than in Lab-S. The relative fitness of JZ-NIL was 0.54 compared with Lab-S. Overall, these results indicate that GST-mediated detoxification contributes to chlorfenapyr resistance in S. litura and that this resistance is associated with significant fitness costs. Further studies are needed to clarify the metabolic and target-site mechanisms underlying chlorfenapyr resistance.

PMID 42928584
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PubMedJFMS open reports2026-10-25

Echocardiographic description of pulmonary vein stenosis in a cat with atrioventricular septal defect.

Seyednejad Farzin F, Locquet Laurent L, Ardehali Pantea P, Astaraki Niusha N

A 2.5-year-old, intact female British Shorthair cat was referred for cardiology evaluation owing to intermittent panting and a heart murmur identified on cardiac auscultation before elective surgery. Physical examination revealed a left parasternal grade II/VI systolic murmur without arrhythmia. Thoracic radiographs showed cardiomegaly without pulmonary infiltration. The echocardiography was prompted by auscultation, history and radiological findings. Transthoracic echocardiography demonstrated marked right atrial enlargement and eccentric hypertrophy of the right ventricle. Echocardiography revealed a partial atrioventricular septal defect characterised by a large ostium primum defect (0.79 cm) and an anterior mitral valve cleft, resulting in a left-to-right shunt (estimated Qp:Qs ≈ 2.2). Doppler interrogation of the left pulmonary vein entering the lateral wall of the left atrium demonstrated focal turbulence and increased peak velocity (1.08 m/s), corresponding to a pressure gradient of approximately 4.7 mmHg, findings consistent with suspected unilateral pulmonary vein stenosis. Tricuspid regurgitation velocity (2.2 m/s) did not reflect increased afterload. Elective surgery was postponed owing to uncertainty regarding peri-anaesthetic haemodynamic risk. Medical treatment with enalapril and clopidogrel was initiated. At the 9-month follow-up, the cat remained clinically stable and echocardiographic findings were unchanged. Pulmonary vein stenosis is rarely reported in cats. This report describes the concurrent presence of partial atrioventricular septal defect and suspected unilateral pulmonary vein stenosis. These findings highlight the detection of a congenital heart defect in a young cat, despite the low-grade murmur.

PMID 42920847
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PubMedActa ophthalmologica2026-10-24

Therapeutic efficacy and systemic pharmacokinetics of a dual-drug hydrogel contact lens for sustained glaucoma therapy.

Varshitha Vangol V, Sankararajan Umadevi U

Conventional topical therapy for glaucoma is limited by poor ocular bioavailability, rapid precorneal drug loss, frequent dosing and systemic absorption through the nasolacrimal pathway, which may reduce therapeutic efficacy and increase the risk of adverse effects. Drug-eluting hydrogel contact lenses have emerged as a promising strategy to overcome these limitations by enabling sustained ocular drug delivery. This study aimed to evaluate the therapeutic efficacy, ocular biocompatibility and systemic pharmacokinetic profile of an optimized dual-drug-loaded HEMA-based hydrogel contact lens delivering timolol maleate (TM) and brimonidine tartrate (BT) for sustained glaucoma management. Optimized hydrogel contact lenses composed of 2-hydroxyethyl methacrylate (HEMA), N, N-dimethylacrylamide (DMA), N-vinylpyrrolidone (NVP) and ethylene glycol dimethacrylate (EGDMA) were fabricated by UV photopolymerization and loaded with TM and BT (4 mg/mL each). Ocular biocompatibility was assessed using the modified Draize irritation test. Therapeutic efficacy was evaluated in a steroid-induced ocular hypertension New Zealand White rabbit model by monitoring intraocular pressure (IOP) for 24 h. Systemic drug exposure was determined by validated high-performance liquid chromatography (HPLC) analysis of plasma samples, while ocular safety was further confirmed through histopathological examination. The optimized hydrogel lens exhibited excellent ocular biocompatibility, with a maximum Draize score of 0.33 ± 0.12 that resolved completely within 48 h and no histopathological evidence of ocular tissue damage. In hypertensive rabbits, the dual-drug hydrogel lens maintained normotensive IOP (16.1 ± 0.8 mmHg) for 24 h, representing a 43.5% reduction from baseline and significantly outperforming conventional eye drops beyond 4 h (p < 0.01). Plasma concentrations of both TM and BT remained below the limit of quantification (<2.0 ng/mL) throughout the study, whereas conventional eye drops produced measurable systemic exposure (TM: 18.4 ± 2.1 ng/mL; BT: 8.2 ± 1.2 ng/mL), demonstrating effective minimization of systemic drug absorption. The optimized dual-drug-loaded hydrogel contact lens provided sustained intraocular pressure reduction, excellent ocular biocompatibility and negligible systemic drug exposure compared with conventional topical therapy. These findings highlight its potential as a sustained ocular drug-delivery platform capable of improving therapeutic efficacy, reducing systemic adverse effects and enhancing long-term treatment adherence in glaucoma management. Further long-term preclinical investigations and clinical studies are warranted to support clinical translation.

PMID 42920388
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PubMedPesticide biochemistry and physiology2026-10-23

Inheritance and biochemical mechanism of abamectin resistance in a near-isogenic strain of Panonychus citri (Acari: Tetranychidae).

Liu Xun-Yan XY, Zhang Chun-Yu CY, Pan Deng D, Dou Wei W et al.

The citrus red mite, Panonychus citri, has developed severe resistance to the widely used pesticide like abamectin. Understanding the inheritance, cross-resistance profile, and biochemical mechanism of pesticide resistance in P. citri is critical for developing effective resistance management strategies. Here, we established an abamectin-resistant near-isogenic strain (NIL-Aba) by backcrossing the susceptible strain (SS strain) with a field collected abamectin-resistant strain (NN-Aba strain) for eight generations, coupled with continuous abamectin selection. The NIL-Aba strain exhibited 2278.44-fold resistance to abamectin relative to the SS strain, and showed cross-resistance with high level to emamectin benzoate (2841.04-fold) and pyridaben (115.21-fold), moderate level to fenpropathrin (15.37-fold) and cyflumetofen (10.73-fold). Genetic analysis indicated that abamectin resistance in NIL-Aba was autosomal, polygenic, and incompletely recessive. Synergist and enzyme activity assays demonstrated that piperonyl butoxide and triphenyl phosphate significantly inhibited abamectin resistance, with synergism ratios of 2.42- and 2.57- fold, respectively. Diethyl maleate produced a smaller synergistic effect (SR = 1.60). Furthermore, the NIL-Aba strain exhibited significantly higher activities of cytochrome P450 monooxygenases, carboxylesterases and glutathione S-transferases than the SS strain, indicating the involvement of three enzyme families in abamectin detoxification. The establishment of NIL-Aba provides a genetically controlled resource for dissecting the molecular basis of abamectin resistance in P. citri. These findings also provide a theoretical foundation for rotating abamectin with other pesticides, which is crucial for prolonging its efficacy in the field against P. citri and for optimizing resistance management strategies.

PMID 42919523
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PubMedEcotoxicology (London, England)2026-10-23

Unraveling acetamiprid resistance in Aphis craccivora (Hemiptera: Aphididae): resistance risk assessment, fitness costs, cross-resistance, biochemical and molecular characterization, and in silico docking study.

Aioub Ahmed A A AAA, Hashem Ahmed S AS, Ahmed Heba H R HHR, Alkeridis Lamya A LA et al.

Aphis craccivora Koch (Hemiptera: Aphididae) is a major sucking pest of legumes. Neonicotinoid insecticides are extensively utilized for A. craccivora control. The extended use of neonicotinoids, including acetamiprid (ACP) to manage A. craccivora, has led to the development of resistance. However, the potential to delay the development of ACP resistance in A. craccivora has not yet been investigated. Our study aimed to examine the development of ACP resistance in A. craccivora over 20 generations, and the associated heritability (h2), fitness costs, biochemical mechanisms, and potential cross-resistance were evaluated. Gene expression of GST and Cyp-450 was measured under ACP exposure, and molecular docking of ACP with these proteins in the presence of diethyl maleate (DEM) and piperonyl butoxide (PBO) was analyzed. Our data showed that the ACP-resistant (ACP-R) strain of A. craccivora showed a 25.57-fold enhancement in LC₅₀ compared to the Sus-strain, with realized heritability (h²) of 0.21 and reduced fitness (0.69). The net reproduction rate (R0), mean relative growth rate (MRGR), intrinsic rate of increase (r), and finite rate of increase (λ) were markedly lower in the ACP-R strain than in the Sus-strain of A. craccivora. Upregulation of Cyp-450 (CYP18A1, CYP4CJ14) and GST (GSTS3, GSTO1) genes enhanced enzyme activity, while Car-E showed no significant correlation with ACP susceptibility. Enzyme inhibitors PBO and DEM increased ACP toxicity, and molecular docking suggested their interaction with Cyp-450 and GST proteins contributes to resistance. Our findings offer key insights into ACP resistance in A. craccivora, supporting the development of management strategies and decision-making tools.

PMID 42911287
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PubMedBrain injury2026-10-20

Intranasal administration of enalapril confers acute neuroprotection by mitigating mitochondrial dysfunction and apoptosis in a rat model of ischemic stroke.

Sadeghian Nooshin N, Salimpour Azar Saied S, Shadman Javad J, Abedi Ali A et al.

Stroke remains a leading cause of mortality and long-term disability worldwide, with effective treatments hindered by its complex pathophysiology. This study is the first to explore the neuroprotective potential of intranasal enalapril, in mitigating ischemic stroke outcomes through its influence on mitochondrial function. Male Sprague-Dawley rats were subjected to middle cerebral artery occlusion (MCAO), followed by the intranasal administration of enalapril (0.03 mg/kg) post-ischemia. Neurological function was evaluated after 24 hours of reperfusion through the modified neurological severity score (mNSS), grip strength, and hot plate tests. Brain infarct volume was quantified via Triphenyltetrazolium chloride staining. Blood- brain barrier (BBB) integrity was evaluated via the Evans Blue extravasation assay. Additionally, we employed immunofluorescence techniques to assess apoptosis through TUNEL staining and evaluated mitochondrial function by examining mitochondrial swelling, succinate dehydrogenase activity, mitochondrial membrane potential and reactive oxygen species production. Intranasal administration of enalapril significantly reduced the infarct volume, preserved BBB integrity, and attenuated sensorimotor deficits in MCAO rats. These protective effects were closely associated with enhanced regional cerebral blood flow, a significant reduction in neuronal apoptosis, and improved mitochondrial function. Intranasal enalapril may provide a novel approach to neuroprotection in ischemic stroke, potentially through mechanisms that enhance mitochondrial function and reduce neuronal apoptosis.

PMID 42897973
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