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amlodipine besilate + irbesartan (DSP8153)

✓ Approved

Sumitomo Pharma Co., Ltd. · AGTR1 · 小分子

什么是 amlodipine besilate + irbesartan？

amlodipine besilate + irbesartan 是一种小分子，由Sumitomo Pharma Co., Ltd.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DSP8153
公司Sumitomo Pharma Co., Ltd.
药物类别小分子
分子靶点AGTR1, CACNA1C
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Sumitomo Pharma Co., Ltd.

作用机制

分子靶点

amlodipine besilate + irbesartan 作用于 2 个分子靶点：

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
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

amlodipine besilate + irbesartan 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

PubMedAnalytical methods : advancing methods and applications2026-09-07

One Health prescribing - development of enantioselective liquid chromatography - tandem mass spectrometry methods to inform chiral switch of prescription pharmaceuticals.

Wagstaff Tony A TA, Barron Gemma A GA, Pfleger Sharon S, Petrie Bruce B

The One Health philosophy highlights the need to sustainably balance and optimise the health of humans, animals, and ecosystems. Pharmaceuticals are essential for human health, but their usage poses downstream risks to aquatic life. Thus, pharmaceuticals need to be environmentally friendlier whilst delivering the same intended health outcomes. Chiral switch, whereby racemic formulations are replaced with enantiopure versions, is proposed to reduce the environmental burden of pharmaceuticals under the One Health philosophy. This research aimed to develop enantioselective methodologies applicable to complex environmental matrices to inform the chiral switch of commonly prescribed pharmaceuticals. This was achieved using cation exchange solid-phase extraction (SPE) and two separate chiral-high performance liquid chromatography (HPLC) methods for selective detection and quantification of 16 pharmaceuticals (anti-depressants, beta-blockers, calcium-channel blocker, central nervous system stimulant, skeletal muscle relaxant) and primary metabolites in wastewaters. An InfinityLab Poroshell 120 Chiral-V was used to separate cationic enantiomers and CHIRALPAK® ZWIX(+) for zwitterions with enantioresolutions ranging from 0.6 to 4.2. Quantitation limits and trueness values of the SPE-chiral HPLC methods ranged from 6.5 × 10-2 ng L-1 to 42 ng L-1 and from 60% to 119%, respectively. Application of the methodology to wastewater samples revealed several analytes were in non-racemic composition including citalopram, fluoxetine, mirtazapine, desmethylmirtazapine, and ritalinic acid. Greatest enantiomer enrichment was observed for desmethylmirtazapine with a maximum enantiomeric fraction of 0.80. Furthermore, to the best of our knowledge this is the first study to report the enantiomeric composition of baclofen, amlodipine, hydroxyatenolol and ritalinic acid in wastewater. Further application of these newly developed methods can help develop more accurate environmental risk assessments of pharmaceutical enantiomers to inform the proposed chiral switch decision making process in healthcare.

PMID 42703855
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PubMedBioinformation2026-09-06

Effect of amlodipine and telmisartan on bone metabolism markers in newly diagnosed hypertensive patients.

Garg Kamlesh K, Raveendranath Perumal P, Gulati Sameer S, Zaheer Sufian S et al.

Hypertension may adversely affect bone health, but the skeletal effects of commonly prescribed antihypertensive drugs remain inadequately u nderstood. In this 24-week prospective study, 96 newly diagnosed Stage I hypertensive patients received either Amlodipine (5-10 mg) or Telmisartan (40-80 mg), with serial assessment of bone metabolism markers. Both drugs achieved comparable blood pressure control throughout the study period. Telmisartan significantly reduced PTH and IL-6 levels while enhancing BS-ALP and transiently increasing osteocalcin, whereas Amlodipine demonstrated only a temporary rise in BS-ALP. Thus, data shows the telmisartan may provide additional benefits on bone remodeling and skeletal health in hypertensive patients at risk of fragility.

PMID 42701587
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PubMedBMJ case reports2026-09-06

Loss of blood pressure control after rifampin initiation: a clinically significant antihypertensive drug-drug interaction.

Park Joomong J

A man in his early 60s with previously well-controlled hypertension developed sudden deterioration in blood pressure control 2 weeks after starting isoniazid-rifampin therapy for latent tuberculosis infection. His blood pressure had previously been stable on an angiotensin receptor blocker and a calcium channel blocker. He presented with a headache and newly uncontrolled hypertension. Rather than representing progression of essential hypertension, the deterioration was temporally associated with rifampicin-induced cytochrome P450 enzyme induction. Rifampin is a potent inducer of CYP3A4 and can reduce plasma concentrations of calcium channel blockers such as amlodipine by up to approximately 80%, substantially diminishing their antihypertensive effect. Blood pressure improved after escalation of antihypertensive therapy while antituberculosis treatment continued without interruption. This case highlights the importance of structured medication review when evaluating sudden loss of blood pressure control in primary care.

PMID 42700982
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PubMedInternational journal of surgery case reports2026-09-06

The role of integrated radiology in diagnosis and treatment of renal artery stenosis: a case report.

Wahyono Djuwita Adi DA, Darmawan Marsha Ruthy MR, Drajat Endang E, Praptini Mirna Nurasri MN et al.

Renal artery stenosis (RAS) is a significant cause of ischemic nephropathy and secondary hypertension and is often underdiagnosed. While atherosclerosis predominates in older adults, younger patients are affected by various etiologies, such as fibromuscular dysplasia (FMD). Early diagnosis and intervention using integrated radiologic modalities are crucial to prevent irreversible end-organ damage in such patients. A 16-year-old male presented with a 6-month history of dizziness and refractory hypertension, with peak readings above 190/100 mm Hg despite aggressive antihypertensive therapy (amlodipine, nifedipine, and spironolactone). His physical examination was unremarkable except for elevated blood pressure (140/100 mmHg). Computed tomography angiography (CTA) of the renal arteries revealed a tight focal stenosis in the right renal artery, with post-stenotic dilation and collateral circulation to both poles of the right kidney. Selective digital subtraction angiography (DSA) confirmed these findings. Percutaneous transluminal renal angioplasty (PTRA) was performed using sequentially larger balloons (2.5 mm to 5.0 mm), and a vascular stent was deployed, achieving complete recanalization and robust distal flow. The patient was discharged on dual antiplatelet therapy with no complaints. This case highlights the utility of CTA for detailed anatomical assessment and DSA for confirmation and intervention. The need for stenting post-angioplasty due to residual stenosis underscores the importance of having a comprehensive endovascular strategy. Early and effective management of RAS is crucial to prevent long-term complications in young patients. Integrated imaging is essential for diagnosis, lesion characterization, and procedural planning in RAS patients. Endovascular revascularization is an effective treatment with early technical and clinical success.

PMID 42699528
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PubMedEJIFCC2026-09-06

Drug-Induced Liver Injury During First-Line Anti-Tubercular Therapy (Isoniazid, Rifampicin, Pyrazinamide, and Ethambutol): A Case Report with De-challenge and Rechallenge.

Chokkakula Sridevi S, Balasani Ashwitha A, Ammana Sathwika Reddy SR

The primary treatment for tuberculosis, which includes isoniazid, rifampicin, pyrazinamide, and ethambutol, is vital for managing the disease but often leads to drug-induced liver injury (DILI), especially in older adults. It is important to accurately identify and manage hepatotoxicity caused by this treatment to safely continue therapy. This report discusses a case of liver injury induced by first-line anti-tubercular drugs in an elderly patient, emphasiz-ing the importance of de-challenge, alternative non-hepatotoxic treatments, and a carefully monitored stepwise rechallenge. An 84-year-old woman with pulmonary tuberculosis and hypertension (treated with amlodipine) experienced abnormal liver function tests after starting first-line anti-tubercular therapy. A thorough clinical evaluation, laboratory tests, causality assessment, de-challenge, alternative treatment, and stepwise rechallenge were conducted with close biochemical monitoring. Initial tests showed significant hyperbilirubinemia (total bilirubin 5.2 mg/dL), elevated aspartate aminotransferase (AST 176-247 U/L), slightly increased Alanine Aminotransferase (ALT 40-55 U/L), and an R-ratio of about 2.6, indicating a predominantly cholestatic pattern with mixed features of liver injury. After discontinuing the hepatotoxic treatment and starting alternative medications (Moxifloxacin, Streptomycin, and Ethambutol), liver function tests improved significantly within 3-5 days. Once liver parameters normalized, Rifampicin was gradually reintroduced, and liver function tests remained stable four days after rechallenge, with no return of hepatotoxicity. This case illustrates that early detection of liver injury from anti-tubercular therapy, prompt de-challenge, use of alternative non-hepatotoxic drugs, and a carefully monitored stepwise rechallenge can enable the safe continuation of tuberculosis treatment in elderly patients. Close biochemical monitoring, along with consideration of therapeutic drug monitoring, may further improve patient safety.

PMID 42698981
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PubMedThe American journal of emergency medicine2026-09-04

Absence of hyperdynamic contractility in the setting of amlodipine-induced shock.

Bleifuss William J WJ, Olives Travis D TD, Carlson Greta Kreider GK, Cole Jon B JB

Amlodipine is a commonly prescribed antihypertensive, and among the calcium channel blockers is associated with the most fatalities in the United States. Vasoplegic shock secondary to dihydropyridine overdose is typically managed with intravenous fluids, calcium replacement and vasopressors. While high dose insulin (HDI) has established efficacy in non-dihydropyridine calcium channel blocker induced cardiogenic shock, utility in amlodipine toxicity remains controversial.

PMID 42697099
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