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losartan + HCTZ (Gizaar / Hyzaar / Cozaar plus)

✓ Approved

Merck & Co. · AGTR1 · 小分子

什么是 losartan + HCTZ?

losartan + 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Gizaar, Hyzaar, Cozaar plus
公司Merck & Co.
药物类别小分子
分子靶点AGTR1, SLC12A3
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

losartan + HCTZ 作用于 2 个分子靶点:

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
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

losartan + 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

PubMedFoot (Edinburgh, Scotland)2026-06-13

A national survey of BOFAS members on the treatment of primary osteochondral lesions of the talus.

Samy David A DA, Ankers Thomas T, Mangwani Jitendra J, Calder James J et al.

Osteochondral defects (OCDs) of the talus are a "TOP 10" research priority in foot and ankle surgery, identified by the James Lind Alliance in partnership with BOFAS, BOA and NIHR. To inform a research strategy, the treatment preferences of BOFAS members were surveyed. A questionnaire on the presentation, investigation and management of primary OCDs of the talus that had failed non-surgical treatment was formulated by the BOFAS National Clinical Study Group, ratified by the Scientific Committee, and distributed via Microsoft Forms. Surgical treatment was categorised by defect size (small: ≤15 mm; large: >15 mm) and depth (shallow: ≤5 mm; deep: >5 mm), with depth defined as the cranio-caudal dimension into subchondral bone on MRI. There were 90 responses (90/224; 40.2% response rate). Bone marrow stimulation (BMS; microfracture or nanofracture) was the dominant first-line choice across all categories. For small, shallow lesions, 85/90 respondents (94%) chose BMS. For large, shallow lesions, BMS was chosen by 59 (68%), BMS plus a scaffold (AMIC/ACIC) by 18 (21%), and BMS plus a biological agent (cBMA/PRP) by 6 (7%). For small, deep lesions, BMS remained most popular (69 respondents; 77%). For large, deep lesions, BMS was chosen by 43 (49%), BMS plus scaffold by 23 (26%), and osteochondral autograft transfer (OATS) by 7 (8%). Post-operative weight-bearing preferences varied considerably, with 49% allowing immediate unrestricted weight-bearing. This is the largest national BOFAS survey on OLT management to date in the United Kingdom. BMS was the most popular treatment across all lesion types, consistent with Guelfi et al. (2021). However, significant practice variation exists, particularly for larger and deeper lesions. High-quality randomised controlled trials are needed to establish optimal evidence-based treatment for OLTs.

PMID 42284707
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PubMedNeuro-oncology advances2026-06-12

Focused ultrasound for brain metastases.

Ozair Ahmad A, Moiz Bilal B, Anastasiadis Pavlos P, Gandhi Dheeraj D et al.

Brain metastases (BMs) increasingly represent a significant cause of morbidity and mortality in cancer patients. The efficacy of systemic therapies for BMs, in contrast to extracranial metastases (EMs), remains limited secondary to a host of challenges. These include insufficient drug delivery due to the blood-brain barrier and blood-tumor barrier, the unique immunological milieu in the tumor microenvironment and cerebrospinal fluid, the diversity of immunogenomic landscapes in BMs across genetically distinct malignancies, the branching evolution of BM from EMs, and the challenges in longitudinally obtaining information regarding clinically actionable genetic alterations in BMs for precision oncology. These complex, long-standing challenges require treatment strategies that address multiple problems concurrently, as represented by the potential of focused ultrasound (FUS) for enhancing effectiveness of several existing BM-specific management strategies. Beyond historically investigated applications of FUS for BMs, including thermoablation and histotripsy, new frontiers include enhanced drug delivery of systemic therapies, plasma sono-liquid biopsy of BM-derived factors, radiosensitization, and immunomodulation. These applications, as discussed here, enable multiple combinatorial opportunities of FUS with targeted- and/or immunotherapies for BMs. With multiple ultrasound delivery platforms (including MR-guided, neuro-navigation-guided, and implantable devices) being investigated in neuro-oncology trials worldwide, this review provides strategies for designing and optimizing future research efforts.

PMID 42281803
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PubMedNanomedicine : nanotechnology, biology, and medicine2026-06-12

CHP/MMP2 dual-targeting soft mesoporous organosilica nanoparticles loaded with losartan for modulating cardiac fibrosis.

Yang Qing Q, Zhang Shilin S, Dang Meng M, Taub Cynthia C et al.

Myocardial fibrosis (MF) drives heart failure and arrhythmias, yet drug delivery to injured myocardium is hindered by the dynamic cardiac microenvironment and lack of lesion-specific targeting. Here, we developed a dual-targeted, soft mesoporous organosilica nanoparticles (SMONs) system, which were co-functionalized with a cardiac homing peptide (CHP) and an anti-matrix metalloproteinase 2 antibody (Ab-MMP 2) for the delivery of losartan (LOS). LOS@SMONs-CHP/MMP2 exhibited excellent deformability and outstanding cellular uptake capability. In a murine model of isoproterenol (ISO)-induced myocardial fibrosis, LOS@SMONs-CHP/MMP2 exhibited significantly increased accumulation of fibrosis. In vitro treatment with these nanoparticles potently suppressed cardiac fibroblast activation, proliferation and migration, and markedly reduced collagen deposition and expression of fibrotic markers in vivo. Consequently, cardiac systolic function was substantially improved, outperforming free losartan. Comprehensive biosafety evaluations confirmed minimal cytotoxicity and no acute organ toxicity. This study offering a promising and translatable nano platform for the treatment of cardiac fibrosis.

PMID 42276182
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PubMedJournal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG2026-06-12

Amitriptyline oral drops for the treatment of burning mouth syndrome: a case series of 13 patients.

Licata Gaetano G, Caccavale Stefano S, Arisi Mariachiara M, Ariasi Cesare C et al.

Burning mouth syndrome (BMS) is a chronic oral neuropathic pain disorder. We conducted a retrospective case series of 13 postmenopausal women with primary BMS treated with low-dose oral amitriptyline administered as liquid drops, allowing flexible titration to the individual minimum effective dose. Pain intensity was assessed using a visual analog scale (VAS), and quality of life was measured with the Dermatology Life Quality Index (DLQI) at baseline and during follow-up (6-12 months). Mean baseline VAS was 7.4 and mean DLQI was 13.8. Clinically meaningful improvement was observed in 92.3% of patients, with complete remission in 6 cases and ≥50% pain reduction in 6 cases. Mean final VAS decreased to 1.7 and mean DLQI to 3.2. Symptomatic relief typically occurred within 2-4 weeks after reaching the effective dose and was maintained during follow-up. Low-dose amitriptyline administered with individualized titration appears to be a safe and effective option for refractory primary BMS.

PMID 42281237
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PubMedMolecules (Basel, Switzerland)2026-06-12

Imidazole-Based AT1 Receptor Ligands: Design, Synthesis and Pharmacological Evaluation.

Descamps Florian F, Rami Marouane M, Goossens Jean-François JF, Melnyk Patricia P et al.

The angiotensin II type 1 (AT1) receptor is a key component of the renin-angiotensin system (RAS) and a validated target for cardiovascular and renal disorders. Developing small molecules with defined AT1 versus AT2 binding profiles remains important for both therapeutic and mechanistic studies. Here, a series of novel imidazole-based compounds was synthesized and evaluated for their binding affinities toward angiotensin II type 1 (AT1) and type 2 (AT2) receptors. Binding studies were conducted by measuring the displacement of radiolabeled [3H]-angiotensin II ([3H]-AII) in PLC-PRF-5 human hepatoma cells for AT1 receptors and calf cerebellum membranes for AT2 receptors. Structure-activity relationship (SAR) analysis revealed that sulfonamide substitution significantly enhanced AT1 receptor affinity, whereas sterically hindered derivatives and ester-containing compounds were less active. Molecular docking studies using the AT1 receptor crystal structure (PDB: 8TH4) rationalized the observed activity trends. The most active compound showed high AT1 affinity (Ki = 5 nM), comparable to losartan, and all compounds displayed preferential binding for AT1 over AT2 receptors.

PMID 42280273
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PubMedOrthopedic reviews2026-06-12

Algorithm-Based Surgical Decision-Making for Focal Knee Cartilage Defects: A Pragmatic Clinical Framework with Illustrative Cases.

Suiindik Birzhan B, Raimagambetov Yerik Y, Baktybergen Kazybek K, Saginova Dina D et al.

To evaluate the early clinical and radiological outcomes of an algorithm-based surgical decision-making framework for focal knee cartilage defects using reproducible, cost-effective techniques in routine clinical practice. This retrospective case series included five consecutive patients with ICRS Grade 3-4 chondral or osteochondral lesions. Treatment followed a structured decision-making algorithm based on fragment viability, lesion size, and patient-specific factors. Surgical procedures included bone marrow stimulation (BMS, n=2), osteochondral autograft transplantation (OAT, n=1), and osteochondral fragment refixation for osteochondritis dissecans (OCD, n=2). Clinical outcomes were assessed using the Visual Analogue Scale (VAS) and the Knee Injury and Osteoarthritis Outcome Score (KOOS) at 1, 3, and 6 months. Structural repair was evaluated at 6 months using MRI-based MOCART 2.0 scoring. All patients demonstrated progressive clinical improvement. Mean VAS scores decreased from 6.6 preoperatively to 1.2 at 6 months. KOOS scores improved across all subscales, with the greatest gains observed in activities of daily living. MRI evaluation demonstrated variable structural maturation (mean MOCART 2.0 score: 60, range 45-75), with superior outcomes observed in patients undergoing fragment refixation. Even in an older patient with extensive pathology, bone marrow stimulation resulted in satisfactory short-term outcomes. The proposed algorithm-based approach provides a practical and reproducible framework for selecting surgical treatment in focal knee cartilage defects. Despite the limited sample size, the consistent clinical improvement supports the feasibility and applicability of this decision-making model, particularly in real-world and resource-constrained settings.

PMID 42282140
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