Merck & Co. · AGTR1 · Small Molecule
olmesartan + amlodipine is a small molecule developed by Merck & Co.. It is approved for therapeutic indications via oral (po).
| Brand Names | Sevikar, Normetec, Konverge |
| Company | Merck & Co. |
| Drug Class | Small Molecule |
| Molecular Target | AGTR1, CACNA1C |
| Route | Oral (PO) |
| Status | Approved |
olmesartan + amlodipine acts on 2 molecular targets:
| AGTR1 | angiotensin II receptor type 1 (HAT1R, AT1) |
| CACNA1C | calcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2) |
olmesartan + amlodipine is developed for 1 unique indication across 1 therapeutic area.
| Therapeutic Area | Condition | Phase |
|---|---|---|
| Vascular disorders | Hypertension | ✓ Approved |
Kario Kazuomi K, Rakugi Hiromi H, Ito Chiyo C, Sayyed Sarfaraz S et al.
Liang Shuang S, Zhang Shuang S, Li Ling L, Luo Jing J et al.
The impact of China's national centralized volume-based procurement (NVBP) policy on antihypertensive drug procurement in underdeveloped, multi-ethnic regions remains understudied. This study evaluated changes in procurement prices, volumes, and costs for four antihypertensive drugs following the second NVBP batch in Guangxi, an economically disadvantaged region in southwestern China. Monthly procurement data for four NVBP antihypertensive drugs (Olmesartan Medoxomil, Candesartan Cilexetil, Terazosin Hydrochloride, and Indapamide) were collected from January 2019 to April 2021, covering 16 months before and 12 months after policy implementation (May 1, 2020). Interrupted time series (ITS) analysis with Newey-West standard errors was used to assess immediate and sustained changes in log-transformed defined daily doses (DDDs) and defined daily dose costs (DDDc). Sensitivity analyses examined robustness to a January 2021 procurement spike. Following policy implementation, the average unit price of the four drugs decreased by 81.52%, and median DDDc dropped by 96.88% to 99.78%. ITS models showed significant immediate increases in DDDs for all four drugs (all p < 0.001), but no significant sustained long-term trend (all β 3 not significant, p > 0.05). A sharp DDDs spike occurred in January 2021, followed by a decline. Sensitivity analyses confirmed that the spike did not affect the direction or significance of the main estimates. The second NVBP batch was associated with substantial and sustained reductions in procurement prices and costs for these four antihypertensive drugs in Guangxi. However, procurement volumes showed marked volatility without stable long-term growth. These findings, based on procurement records rather than patient-level data, suggest that price reductions alone may not ensure consistent procurement patterns. Strengthening supply chain resilience and aligning procurement schedules with clinical demand may support more stable drug supply in disadvantaged regions.
Mariowska Agnieszka A, Nowicki Filip F, Horwat Paulina P, Rzepczyk Szymon S
Amlodipine is one of the basic drugs used in the treatment of hypertension. It belongs to the dihydropyridine calcium channel blocker and is one of the most frequently used drugs, which translates into its widespread use in the clinic and popularity. Amlodipine overdose may be associated with life-threatening complications, but fatal overdoses have not been well described and pose significant challenges in post-mortem diagnosis. The aim of the study was to analyze cases of fatal amlodipine overdose with particular attention to the circumstances of the events and the diagnostics performed. As a result of the literature review using relevant keywords and boolean operators, 13 articles were identified that met the study inclusion criteria. The articles included in the study were published between 1997 and 2024 and were mostly from Europe. There were 17 cases described, 9 of which were men. The average age in the group included in the study was 43.8 years. Most cases were suicidal overdoses, and the events usually occurred at home. The most common finding at autopsy was passive congestion and edema in the lungs. No specific histopathological findings were revealed except for the confirmation of autopsy gross findings. The most frequently analyzed material for toxicological tests to assess amlodipine content was blood. An important role in the assessment of cases of fatal overdose is the assessment of the place where the body was found. Due to the widespread availability of the drug, further research is needed on fatal overdose, especially regarding post-mortem diagnosis.
Berhe Teshome T, Negash Zenebe Z, Tegegne Gobezie T GT, Berha Alemseged Beyene AB
Chronic kidney disease (CKD) remains a major treatment challenge in low- and middle-income countries due to limited resources, delayed diagnosis, poor access to essential medicines, and inadequate renal replacement services. Given the limited evidence on CKD management and outcomes in these settings, this study aimed to evaluate the clinical outcomes and associated factors among patients with CKD at Zewditu Memorial Hospital and Tikur Anbessa Specialized Hospital, Ethiopia. A retrospective cross-sectional study design was employed. All adult patients with CKD attending the renal clinics at both hospitals between March and July 2019 were enrolled. Sociodemographic and clinical characteristics were collected through structured patient interviews and review of medical records. Data were analyzed using Statistical Package for Social Science (SPSS) version 23. Of 300 CKD patients included in the study, nearly half of them had CKD-related complications, and 11% were in end-stage renal disease (ESRD). Among those with complications, 29% had hospitalization prior to data extraction. Most participants (83.7%) adhered to clinician-recommended non-pharmacological interventions. Enalapril and amlodipine were prescribed for 39.0% and 37.3% of patients, respectively, and polypharmacy was observed in 53.3% of patients with stage five CKD. A substantial proportion of patients with CKD had complications, including hospitalization and ESRD. Polypharmacy was prevalent among patients with advanced CKD, underscoring the need for comprehensive management and close monitoring to improve treatment outcomes.
Deshpande Milind M, Kavlekar Duwarkesh B DB, Kumar V S Vishwa VSV, Patil Dhairyasheel D et al.
The navicular bone is a tarsal bone of the foot. It is an important bone that supports the medial arch of the foot. Navicular bone fractures are a rare injury. Fractures may occur as a result of stress or trauma. In both scenarios, it may be considered high risk due to poor blood supply to the bone. It is more common in athletes while kicking, sprinting, twisting, or falling. We report a case of a comminuted navicular fracture in an individual fixed with the Joshi external stabilization system (JESS). A 40-year-old male presented with injury to the right foot. The patient met with an accident; he was brought to the casualty department. He was conscious, cooperative, and alert. No other bony injury was noted. There was no history of blunt abdominal trauma; however, blunt chest trauma was noted. No history of diabetes mellitus. The patient was newly detected hypertensive and was treated with tablet amlodipine 5 mg bd and tablet telmisartan 40 mg at night. Navicular bone fracture is a rare injury. It results from either stress fractures or trauma. Early diagnosis of suspicion and prompt treatment are key to success. JESS was the choice of treatment in this case. Other cases may need open reduction and internal fixation.
Chakith M R Sai MRS, Pradeep Sushma S, Raj Ranjith R, Reddy Pruthvish P et al.
Psoriasis is a chronic, immune-mediated skin disorder characterized by excessive inflammation and the overexpression of pro-inflammatory cytokines, including IL-6, IL-1β, IL-17 A, and IFN-γ. Despite the availability of targeted therapies, current treatments often entail high costs, limited accessibility, and adverse side effects. Drug repurposing-utilizing approved medications for novel indications-offers a cost-effective strategy to accelerate the development of alternative therapies with established safety profiles. Twelve FDA-approved antihypertensive drugs-including ACE inhibitors, angiotensin receptor blockers, beta-blockers, and calcium channel blockers-were computationally evaluated for anti-inflammatory potential in psoriasis. Target cytokines were identified using network analysis via STRING and Cytoscape. Molecular docking was performed against IL-6, IL-1β, IL-17 A, and IFN-γ. The top-performing ligands underwent further analysis using ADMET prediction, BOILED-Egg visualization, Density Functional Theory (DFT) calculations, and molecular dynamics (MD) simulations to assess pharmacokinetics, electronic properties, and protein-ligand complex stability. Apremilast, a clinically approved anti-psoriatic agent, served as the reference drug. Lisinopril, Ramipril, Amlodipine, and Atenolol emerged as top candidates based on docking scores and pharmacokinetic profiles. Among them, Lisinopril exhibited the strongest binding affinity across all four cytokines, comparable to or exceeding that of Apremilast. Amlodipine demonstrated the highest electronic reactivity, and all selected drugs showed favorable ADMET properties. MD simulations over 200 ns confirmed the dynamic stability of the Lisinopril-IL-6 complex. Lisinopril has shown potential as a molecular candidate through detailed computational analysis of cytokine interactions. However, these results are purely predictions and should be viewed with caution, especially considering reports of potential ACE inhibitor-related psoriasis worsening. Further thorough laboratory, animal, and clinical studies are necessary to assess its practical application and safety in treating psoriasis.
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