北京若生智能科技有限公司
Drug Database
EN

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

PubMed[Zhonghua yan ke za zhi] Chinese journal of ophthalmology2026-09-07

[Tafluprost/timolol fixed-dose combination versus tafluprost monotherapy for open-angle glaucoma and ocular hypertension: a multicenter, randomized, double-blind, parallel-group trial].

Wang K D KD, Zhao P P, Wu L L LL, Zhang T H TH et al.

Objective: To evaluate the efficacy and safety of a preservative-free tafluprost/timolol maleate fixed-dose combination compared with preservative-free tafluprost monotherapy in Chinese patients with open-angle glaucoma (OAG) or ocular hypertension (OHT). Methods: This was a multicenter, randomized, double-blind, parallel-controlled clinical trial conducted across 25 centers, including the Eye & ENT Hospital of Fudan University, from January 2019 to November 2022. Patients diagnosed with OAG or OHT who required enhanced intraocular pressure (IOP) reduction after a 4-week washout period were enrolled. Participants were randomized 1∶1 to receive either tafluprost/timolol or tafluprost once daily for 3 months. The primary endpoint was the change from baseline in mean diurnal IOP (the average of measurements at 8:00, 10:00, and 16:00) at Month 3. Secondary endpoints included IOP changes at individual time points and the proportion of responders achieving predefined IOP reduction thresholds. Safety was assessed via the incidence of adverse events (AEs). Analysis of covariance (ANCOVA) using the Markov Chain Monte Carlo (MCMC) method was employed for the primary endpoint; superiority was established if the upper limit of the 95% confidence interval (CI) was<0 mmHg (1 mmHg=0.133 kPa). Continuous variables in secondary endpoints were compared using ANCOVA, and responder rates were analyzed using Fisher's exact test. Results: A total of 219 patients were enrolled (tafluprost/timolol group: n=110; tafluprost group: n=109). The primary efficacy analysis set included 215 patients (tafluprost/timolol: n=107; tafluprost: n=108). Baseline characteristics were well-balanced between the two groups. The majority of patients were male [127 (59.1%)] with a mean age of (44.80±15.71) years at screening. At Month 3, the mean diurnal IOP reduction from baseline was (6.56±3.44) mmHg in the tafluprost/timolol group and (5.36±2.94) mmHg in the tafluprost group. After adjusting for baseline IOP, the between-group difference was -1.312 mmHg (95%CI: -2.010 to -0.696); as the upper limit was<0 mmHg, tafluprost/timolol demonstrated superior IOP-lowering efficacy to tafluprost. Responder rates for IOP reductions of≥15%,≥25%, and≥30% were significantly higher in the tafluprost/timolol group (P=0.016, 0.028, and 0.032, respectively). The incidence of ocular AEs was 20.0% (22/110) in the tafluprost/timolol group and 26.6% (29/109) in the tafluprost group. The most common AE was conjunctival hyperemia, occurring in 2.7% (3/110) and 8.3% (9/109) of the groups, respectively. Conclusion: Compared with preservative-free tafluprost monotherapy, the tafluprost/timolol combination provides significantly greater IOP reduction in patients with OAG and OHT, while maintaining a favorable safety profile.

PMID 42706141
阅读全文 →
PubMedCureus2026-09-06

Recurrent Episodes of New-Onset Supraventricular Tachycardia in Severe Early-Onset Pre-eclampsia and Fetal Growth Restriction: A Report of a Complex Cardio-Obstetric Case.

Kaladharan Nair Aiswarya A, Sarkar Rupak Kumar RK, Sankar Ajesh A

Supraventricular tachycardia (SVT) is one of the commonly reported sustained arrhythmias in pregnancy. The rapid progression from early-onset fetal growth restriction (FGR) to severe pre-eclampsia is a well-recognised manifestation of placental dysfunction. The coexistence of both leads to significant maternal and fetal morbidity, adding substantial complexity to management. We present the case of a 27-year-old primigravida of Caucasian origin with an otherwise uncomplicated pregnancy who attended at 28 weeks' gestation solely because of a maternal concern that her baby appeared small. This seemingly routine presentation initiated a rapid sequence of events, culminating in the diagnosis of severe early-onset FGR, fulminant pre-eclampsia and recurrent new-onset SVT. Her clinical course was characterised by simultaneous maternal and fetal deterioration, creating significant management challenges in the context of severe hypertension, placental dysfunction and fetal compromise. Following delivery by caesarean section for worsening maternal and fetal status, she required intensive care admission, repeated administration of adenosine and ongoing multidisciplinary management to achieve cardiovascular stabilisation. Recurrent episodes of SVT persisted into the postpartum period, necessitating further specialist input and escalation to the regional Maternal Medicine Network. She was subsequently stabilised on bisoprolol and enalapril, with no further documented SVT episodes before discharge. This case highlights the rare coexistence of severe placental disease and recurrent episodes of new-onset SVT in pregnancy, and the complexities associated with balancing maternal cardiovascular stability against fetal well-being. It underscores the importance of early multidisciplinary involvement, including obstetric, cardiology, anaesthetic, critical care and maternal medicine teams. Furthermore, it demonstrates that delivery is not always the definitive solution to complex obstetric pathology, as significant maternal cardiovascular morbidity may persist beyond the immediate postpartum period. Finally, the case emphasises the importance of listening to maternal concerns regarding fetal well-being, even when initial assessments are reassuring, and recognising the need for ongoing psychological support and counselling following traumatic pregnancy complications.

PMID 42698818
阅读全文 →
PubMedPharmacology research & perspectives2026-09-03

A Cohort Study on Incidence and Factors Associated With Adverse Drug Reactions of Enalapril in Lusaka, Zambia.

Yikon'a Ntemena N, Mumba Ngosa N, Pedretti Sarah S, Hoenck Helen H et al.

Angiotensin-converting enzyme inhibitors (ACEIs) are widely prescribed but are associated with adverse drug reactions (ADR), including angioedema, which is typically reported in 0.1%-0.7%. Data from sub-Saharan Africa are limited. This study aimed to estimate the incidence and risk factors of enalapril-associated ADRs in a Zambian cohort, with particular focus on angioedema. We conducted an ambispective cohort study of 400 adults initiating enalapril at two tertiary hospitals in Lusaka, Zambia. Enalapril was the only ACEI available to the participants, and the primary outcome was the occurrence of enalapril-associated ADRs requiring treatment discontinuation or modification. Kaplan-Meier methods were used to estimate event-free survival, and Cox proportional hazards regression was used to identify factors associated with ADR occurrence. Angioedema occurred in 19/400 participants (4.8%). Overall, 22% (88/400) of participants experienced at least one ADR impacting treatment. The most frequent ADRs were cough (10.3%) and dizziness (5.0%). In multivariable analysis, male sex was independently associated with a lower risk of ADR (adjusted hazard ratio [aHR] 0.59, 95% CI 0.37-0.93). No significant associations were identified for the high rate of angioedema. The incidence of enalapril-associated angioedema in this cohort was substantially higher than that reported in global as well as African American populations. These findings have clinical relevance for prescribing and monitoring ACEIs in sub-Saharan African populations. Further studies are needed to confirm this signal and explore underlying mechanisms.

PMID 42687339
阅读全文 →
PubMedBiochemistry2026-09-03

Fluorine-Induced Elimination Drives Mechanism-Based Inactivation of Isocitrate Lyase.

Fernando Kolambapatabandige Gayantha Shamin KGS, Renault Yohann J G YJG, Molino Rachel R, O'Hagan David D et al.

Fluorinated succinate analogues were evaluated as mechanistic probes of Mycobacterium tuberculosis isocitrate lyase (MtICL). However, 2,2-difluorosuccinate (1; Ki = 6.1 mM) and 2,2,3-trifluorosuccinate (2; Ki = 23.5 μM) act as reversible noncompetitive inhibitors and meso-2,3-difluorosuccinate (3) displayed slow-onset reversible inhibition (Ki = 30 μM), the 2-fluorosuccinate enantiomers ((R)-4 and (S)-4) produced time-dependent irreversible inactivation. Inactivation by 4 was observable under turnover conditions in the presence of glyoxylate and succinate, consistent with a two-step kinetic mechanism. The S enantiomer inactivated more efficiently than (R)-4, consistent with stereoelectronic alignment required for elimination of HF following abstraction of the pro-S proton. 1H NMR analysis detected maleate formation from (S)-4, and mass spectrometry revealed a +132 Da adduct consistent with covalent modification of Cys191. Notably, kinact/KI values for 4 exceeded that measured for maleate, indicating that covalent capture occurs from an enzyme-bound intermediate prior to product release. These results support a mechanism in which fluorine substitution redirects the enolate-generating half-reaction of MtICL toward elimination and covalent modification. (S)-2-Fluorosuccinate therefore represents a succinate-analogue mechanism-based inactivator that exploits a catalytic step distinct from previously described isocitrate-analogue inhibitors.

PMID 42689529
阅读全文 →
PubMedJournal of labelled compounds & radiopharmaceuticals2026-09-01

Synthesis and Characterization of 2-(1-Hydroxyethyl)Promazine Sulfoxide-d4 HCl as an Internal Standard for the Accurate Quantitation of 2-(1-Hydroxyethyl)Promazine Sulfoxide in Equine Urine.

Holmes Justin C JC, Smith Ballard C BC, Awuah Samuel G SG, Eisenberg Rodney R et al.

Acetylpromazine, 1-{10-[3-(dimethylamino)propyl]-10H-phenothiazin-2-yl}ethenone, C19H22N2OS, 326.46 g·mol-1 is a phenothiazine derivative at one time used in human medicine as an antipsychotic medication but now predominantly used in veterinary medicine as a sedative/tranquilizer and referred to as acepromazine. In performance horses its use is regulated by using a 10 ng/mL threshold for the major urinary metabolite 2-(1-hydroxyethyl) promazine-sulfoxide (HEPS) in equine urine. To enable accurate quantitation of HEPS in equine urine we have synthesized and purified hydroxyethylpromazine sulfoxide-d4 (HEPS-d4) to be used as a stable isotopically labeled internal standard. Although labeled HEPS is commercially available (CAS 1346605-30-8), to the best of our knowledge there is no published synthetic procedure in the scientific literature. Here we demonstrate a viable synthetic procedure consisting of four major steps: (i) freebasing the Acepromazine maleate salt, (ii) H-D exchange of Acepromazine at room temperature, (iii) reduction of the ketone with NaBD4, and (iv) oxidation of the thioether via hydrogen peroxide and acetic acid. This deuterated internal standard will allow for precise LC/MS quantitation of HEPS at regulatory threshold concentrations, enabling accurate detection and quantitation of picogram/mL concentrations in equine urine samples, thereby supporting regulatory compliance for equine medication control programs.

PMID 42676282
阅读全文 →
PubMedPest management science2026-08-28

The I4746K mutation in the ryanodine receptor is associated with high-level resistance to diamide insecticides in Phthorimaea absoluta.

Atış Abdullah Emre AE, Gündüz Kübra Kahveci KK, Yılmazlar Alize A, İnak Emre E et al.

The South American tomato pinworm, Phthorimaea absoluta, has developed resistance to diamide insecticides mainly through target-site mutations in the ryanodine receptor (RyR), including I4746M, G4903E, and G4903V. Recently, a novel mutation, I4746K, has been identified in field populations of P. absoluta, but its contribution to resistance remains unclear. In this study, a field population (TR-Krş-21) harboring the I4746K mutation exhibited 116.65-fold resistance to chlorantraniliprole (CHL). After six rounds of laboratory selection with CHL, resistance increased to 1109.94-fold (CHL-Sel), with a realized heritability of 0.58. Resistance remained stable for 1 year without insecticide exposure, and genetic analyses indicated that it is autosomal, incompletely dominant, and polygenic. Cross-resistance was observed among diamide insecticides, but not to abamectin or broflanilide. Synergist bioassays with piperonyl butoxide and diethyl maleate showed that inhibition of detoxification enzymes did not fully restore susceptibility. CHL selection resulted in a positive correlation between I4746K allele frequency and resistance, and genetic linkage analysis confirmed a significant association between the mutation and the resistant phenotype. Modeling and molecular dynamics simulations revealed that the I4746K substitution reshapes ligand-receptor interactions without markedly reducing overall binding affinity. Finally, a quantitative sequencing protocol and a tetra-primer amplification-refractory mutation system polymerase chain reaction assay were developed for rapid detection of the I4746K mutation. This study emphasizes the significance of the I4746K mutation in diamide resistance and offers valuable insights into how this mutation variably influences the binding of diamide insecticides, thereby informing strategies for resistance management in P. absoluta. © 2026 Society of Chemical Industry.

PMID 42663378
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多enalapril maleate + HCTZ