amiloride hydrochloride / Generic mfg. - LARVOL DELTA

What a MES!: A Case of Abiraterone-induced Mineralocorticoid Excess Syndrome (ENDO 2025) - "However, its dual inhibition of 17α-hydroxylase and 17,20-lyase can lead to adverse effects from cortisol suppression.A 79-year-old male with prostate carcinoma and bone metastases on Triptorelin pamoate every six months and abiraterone 250 mg twice daily with prednisone 5 mg once daily for over a year has hypertension with more than three anti-hypertensive medications, including a diuretic, and also has diabetes with chronic kidney disease...Abiraterone was discontinued, and prednisone was switched to dexamethasone due to its lack of mineralocorticoid activity. As amiloride was unavailable, finerenone, a selective mineralocorticoid receptor antagonist, was initiated.Abiraterone inhibits CYP17A1, reducing cortisol production by blocking 17α-hydroxylase and suppressing androgen synthesis, key for prostate cancer progression...Finerenone, a novel, selective MRA, is as effective as spironolactone with fewer side effects and better cardiovascular outcomes, particularly in..."

Clinical • Cardiovascular • Chronic Kidney Disease • Diabetes • Endocrine Disorders • Genito-urinary Cancer • Hormone Sensitive Prostate Cancer • Hypertension • Metabolic Disorders • Nephrology • Oncology • Prostate Cancer • Renal Disease • Solid Tumor • AR

A Case of Severe Polyuria: Diagnostic Challenges and Management of Nephrogenic Diabetes Insipidus (ENDO 2025) - "Background:Arginine vasopressin V2 resistance (AVP-R), commonly known as nephrogenic diabetes insipidus (NDI), is an uncommon disorder in which the kidneys fail to respond to AVP, causing significant polyuria. Hereditary AVP-R, as seen in this patient, is a rare condition characterized by varying degrees of resistance to AVP. Approximately 90% of hereditary cases are linked to X-linked AVPR2 mutations (2,3), underscoring the importance of genetic testing. This case shows the difficulties in distinguishing AVP-R (NDI) from other causes of polyuria and demonstrates the pivotal role of desmopressin testing in confirming the diagnosis."

Clinical • Cardiovascular • Endocrine Disorders • Hypertension • Infectious Disease • Metabolic Disorders • Pneumonia • Respiratory Diseases

Inhibition of senescence-associated β-Galactosidase by Amiloride in senescent airway epithelial cells (ERS 2025) - No abstract available

Pulmonary Disease • Respiratory Diseases

The potentiating activity of benzodiazepine site of the GABA(A) receptor is inhibited by competitive antagonists of orthosteric site. (PubMed, Neurochem Int) - "In this work, we studied the influence of competitive antagonists of the GABAA receptor gabazine (GBZ), bicuculline (Bic), and amiloride (Ami) on the potentiating effect of the agonist of BDZ site zolpidem (Zolp)...The results show that the potentiating effect of Zolp is reduced by half in the presence of competitive GABAA receptor antagonists (p < 0. 001)."

Journal

From mechanism to therapy: How EIPA modulates dendritic cell-mediated allergic responses via IL-12b and TIM4. (PubMed, Biomed Pharmacother) - "Ethylisopropylamiloride (EIPA) has been shown to attenuate immune inflammation...Consequently, the Th2 response and airway allergy were mitigated. In conclusion, EIPA attenuates the allergic response by upregulating IL-12b production, reducing TIM4 expression in DCs, and suppressing the Th2 response."

Journal • Allergy • Immunology • Inflammation • Targeted Protein Degradation • IL12B • KDM4D

Loss of cadherin 17 downregulates LGR5 expression, stem cell properties and drug resistance in metastatic colorectal cancer cells. (PubMed, Cell Death Dis) - "Consequently, the loss of CDH17 increased sensitivity to 5-FU, irinotecan, oxidative stress and anoikis in CRC cells...In conclusion, CDH17 plays a crucial role in maintaining colorectal cancer cell stemness and chemoresistance via LGR5/Wnt/MYC signaling and SLC38A5 expression. These findings underscore the therapeutic potential of CDH17 targeting in metastatic CRC, and support the use of amiloride for inhibiting liver metastasis."

Journal • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • CDH17 • DSC1 • LGR5 • SLC38A5

Dual Diagnostic Dilemma: Gitelman Syndrome and Incidental Neuroendocrine Tumor in a Young Adult With Refractory Hypokalemia. (PubMed, Cureus) - "Management comprised high-dose potassium and magnesium supplementation, amiloride, octreotide, and everolimus. Moreover, it emphasizes the limitations in managing double disease entities in a young individual and the insurmountable hurdles for advanced treatments like peptide receptor radionuclide therapy in underdeveloped nations. This report highlights the importance of further studying the association between the interplay of genetic syndromes (such as Gitelman syndrome) and associated neoplasms, as well as the vital coordination of complex and multidisciplinary management in rare clinical situations."

Journal • Cardiovascular • Diabetes • Embryonal Tumor • Endocrine Cancer • Hepatocellular Cancer • Hypertension • Metabolic Disorders • Nephrology • Neuroendocrine Tumor • Oncology • Pancreatic Cancer • Solid Tumor • Type 1 Diabetes Mellitus • SSTR

Severe Late-Onset Abiraterone-Induced Hypokalemia in a Diabetic Patient With Concomitant Adrenal Gland Incidentaloma: A Diagnostic Challenge. (PubMed, Case Rep Endocrinol) - "Physicians should consider dexamethasone over prednisone in persistent MES cases, always monitoring also for the risk of developing Cushing syndrome. Given the rising prostate cancer incidence, clinicians must remain vigilant for MES-related complications with abiraterone, including delayed-onset severe hypokalemia."

Journal • Cardiovascular • Castration-Resistant Prostate Cancer • Cushing’s Disease • Diabetes • Endocrine Disorders • Genito-urinary Cancer • Hypertension • Metabolic Disorders • Oncology • Prostate Cancer • Solid Tumor

Embryo-derived trypsin-induced calcium entry is inhibited by endometrial infertility factor, LEFTY2. (PubMed, Front Cell Dev Biol) - "Treatment of endometrial cells with trypsin was followed by an increase of [Ca2+]i, an effect that was significantly blunted by amiloride and LEFTY2. Taken together, we demonstrate that high trypsin levels are associated with a positive pregnancy outcome and that infertility factor LEFTY2 downregulates trypsin induced Ca2+ increase due in part by interference with nifedipine sensitive Ca2+ entry. These findings contribute further to our knowledge of unexplained infertility and failed assisted reproductive technologies."

Journal • Infertility • Sexual Disorders

CARD: Safety and Efficacy of Chlorthalidone + Amiloride to Elderly Patients Treatment With Arterial Hypertension (clinicaltrials.gov) - P3 | N=246 | Completed | Sponsor: Eurofarma Laboratorios S.A. | Unknown status ➔ Completed

Trial completion • Cardiovascular • Hypertension • Pulmonary Arterial Hypertension

Ifosfamide-Induced Partial Arginine Vasopressin Resistance Responsive to Vasopressin/Desmopressin and Amiloride. (PubMed, Cureus) - "This is a case of partial arginine vasopressin resistance following the sixth cycle of doxorubicin-ifosfamide-mesna therapy for recurrent spindle cell sarcoma of the thigh. The diagnosis was confirmed with serum and urine chemistry testing showing urine hypo-osmolality (161 mOsm/kg) with polyuria (4.8 L urine output) in 24 hours, serum hyperosmolality (355 mOsm/kg), and an elevated baseline plasma copeptin of 82 pmol/L. Treatment with intravenous vasopressin followed by amiloride and supraphysiologic doses of oral desmopressin improved symptomatic hypernatremia."

Journal • Metabolic Disorders • Oncology • Sarcoma • Solid Tumor • Spindle Cell Sarcoma

Pregnancy, primary aldosteronism and renal tubular disorders: A systematic review of the utility of amiloride in pregnancy (ERA 2025) - "Pregnancy often presents the first opportunity to diagnose serious disease in women. Hypertension is frequently attributed as being pathognomonic of preeclampsia when associated with intrauterine growth retardation, leading to a failure to consider secondary testing. While there may be a negative reporting bias for side effects of amiloride during pregnancy, it has been used successfully and appears to be low risk base on the reported cases."

Review • Cardiovascular • Endocrine Disorders • Glomerulonephritis • Gynecology • Hypertension • Nephrology • Renal Disease

Blood pressure modulation through altered Epithelial Sodium Channel (ENaC) expression induced by microbiome exchange between Milan normotensive and hypertensive rat strains (ERA 2025) - "Putative role of ENaC on enhanced SBP in MN-HOM was further suggested by amiloride challenging on these rats, in which MN-HOM showed a reduction in SBP comparable to MN-BSL after amiloride treatment. We have demonstrated that the hypertensive phenotype in NA rats was transferred to MN rats through homogenization, indicating that the intestinal microbiota or metabolites derived therefrom could modulate ENaC in the cortex and eventually modulate SBP. Further studies are underway to identify metabolites from gut microbiota which may modulate ENaC and eventually blood pressure."

Preclinical • Cardiovascular • Hypertension

Amiloride synergizes with EGFR PROTACs and inhibitors to overcome therapeutic resistance in NSCLC. (PubMed, Bioorg Chem) - "Among NSCLC patients, approximately 15-30 % harbor activating mutations in the Epidermal Growth Factor Receptor (EGFR), making them eligible for treatment with tyrosine kinase inhibitors (TKIs) like osimertinib, which has shown significant therapeutic benefits. Collectively, MK-870 synergizes with EGFR-targeting agents through coordinated modulation of sodium channel proteins and NHE-mediated pH homeostasis. These novel insights highlight MK-870 as a promising adjuvant for overcoming EGFR-targeted therapeutic resistance in NSCLC, offering a new avenue for improving patient outcomes in this challenging disease."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • EGFR

Optimizing Anesthesia for High-Risk Patients: Scalp Block for Frontal Lobe Epithelioma Excision (Euroanaesthesia 2025) - "His medications included furosemide, pantoprazole, prednisone, hydroxychloroquine, apixaban, and amiloride...A landmark – guided scalp block targeting the supraorbital, supratrochlear, zygomaticotemporal, auriculotemporal, lesser and greater occipital nerves bilaterally was performed using 1 mL of 0.5% ropivacaine and 1 mL of 1% lidocaine at each injection point...Scalp block is an effective anesthesia and analgesia strategy for head surgery. RA enhances quality of recovery."

Clinical • Anesthesia • Atrial Fibrillation • Benign Prostatic Hyperplasia • Cardiovascular • Cognitive Disorders • Hepatology • Musculoskeletal Pain • Pain • Pulmonary Arterial Hypertension

Effect of vanzacaftor/tezacaftor/ivacaftor on cystic fibrosis airway epithelial cells (ECFS 2025) - "Objectives: The latest triple-component CFTR modulator drug, consisting of vanzacaftor (V), tezacaftor (T) and deutivacaftor (D), is becoming a new treatment alternative to the established combination of elexacaftor (E), tezacaftor (T) and ivacaftor (I) in people with cystic fibrosis (pwCF)...ISC was measured after sequential addition of 100 M amiloride, 10 M forskolin (Fsk) and 100 M 3-isobutyl-1-methylxanthine (IBMX), 10 M I, 10 M CFTRinhibitor-172 (CFTRinh172) and 100 M ATP... Our results show significantly greater restoration of CFTR function in F508del/F508del HNEC treated with VTI compared to ETI. These results are in line with the improved sweat chloride values seen in the clinical trial.Supported by Ministry of Health of the Czech Republic, grant no NU23-07-00079."

Cystic Fibrosis • Genetic Disorders • Immunology • Respiratory Diseases

ENaC contributes to macrophage dysfunction in cystic fibrosis. (PubMed, Am J Physiol Lung Cell Mol Physiol) - "Sodium channel expression in CF MDMs normalized after Amiloride treatment with minimal effect on other ion channels. In summary, ENaC modulation in immune cells is a novel potential therapeutic target for CF infection control, either in combination with CFTR modulators, or as a sole agent for people not eligible for CFTR modulators."

Journal • Cystic Fibrosis • Genetic Disorders • Immunology • Infectious Disease • Inflammation • Pulmonary Disease • Respiratory Diseases • CFTR

ENaC inhibitors for the management of lithium related polyuria: a systematic review. (PubMed, J Affect Disord) - "Although it appears very likely that ENaC inhibitors help ameliorate polyuria in lithium-treated patients, the quantity and quality of evidence is low. Heterogeneity in patient characteristics, intervention characteristics and study designs limit conclusions regarding the contribution of factors likely to influence ENaC-I effectiveness for lithium-induced polyuria. Besides, adverse effects require further exploration."

Journal • Review • Metabolic Disorders • Nephrology • Renal Disease

EIPA, A Macropinocytosis Blocking Agent, Inhibits Siniperca Chuatsi Rhabdovirus Infection In Vitro and In Vivo. (PubMed, Microb Pathog) - "Only ethyl-isopropyl amiloride (EIPA), a macropinocytosis inhibitor, effectively inhibited SCRV replication in CPB cells without cytotoxicity...To evaluate the effect in vivo, largemouth bass (Micropterus salmoides) were infected with SCRV and fed with EIPA. The results showed that EIPA effectively inhibited SCRV infection in vitro and in vivo, suggesting its potential applicability as a therapeutic agent for SCRV treatment."

Journal • Preclinical • Infectious Disease

Pharmacological inhibition of ENaC or NCX can attenuate hepatic ischemia-reperfusion injury exacerbated by hypernatremia. (PubMed, J Zhejiang Univ Sci B) - "The application of amiloride (Amil), a specific inhibitor of ENaC, reduced ischemia-reperfusion injury (IRI) aggravated by HS both in vivo and in vitro, as evidenced by decreased serum transaminases, inflammatory cytokines, apoptosis, and oxidative stress. SN-6, a specific inhibitor of NCX, had a similar effect to Amil. In summary, hypernatremia aggravates hepatic IRI, which can be attenuated by pharmacological inhibition of ENaC or NCX."

Journal • Cardiovascular • Hepatology • Liver Failure • Reperfusion Injury • Transplantation • MPO

Don't Get Salty, Baby! A Rare Case of Geller Syndrome (ATS 2025) - "She received magnesium for maternal seizure prophylaxis and labetalol for blood pressure control...Geller syndrome was suspected and amiloride was initiated, with rapid improvement in K levels...An activating mutation in the gene that encodes MR S810L allows progesterone to bind in a similar way that aldosterone does, which leads to increased salt reabsorption in the renal sodium channels...Increased awareness of this disease in obstetrics and critical care is essential, as its risks pose a major threat to the lives of expectant mothers and their children. Consideration of screening for this genetic mutation in routine obstetric practice may be beneficial, as treatment is readily available."

Clinical • Cardiovascular • CNS Disorders • Epilepsy • Gynecology • Hypertension • Obstetrics

Impact of Common Co-morbidities on Cardiopulmonary Function and Alveolar Fluid Clearance in Mice (ATS 2025) - "AFC was quantified in live mechanically-ventilated mice by the BSA concentration method, with or without 100 μM amiloride in the instillate... Aging and obesity impair cardiopulmonary function and AFC even in the absence of any lung insult. Underlying defects in AFC may predispose elderly and obese patients to worse ARDS outcomes. and the presence of these co-morbidities should be considered when conducting clinical trials of therapeutics designed to improve AFC."

Preclinical • Acute Respiratory Distress Syndrome • Genetic Disorders • Infectious Disease • Obesity • Pneumonia • Respiratory Diseases • Septic Shock

Reimagining Lithium – How Practical Insights From the Dawn of Psychopharmacology Inform New Molecules for Mood and Behavioral Disorders (APA 2025) - "One important goal of this session is to demystify lithium's journey through the kidney, to provide clinicians with a practical polyuria monitoring scheme, and to explain why the ENaC inhibitor amiloride (a potassium sparing diuretic) is the most evidence-based strategy to manage polyuria...Instructional Level Intermediate; Learning Objectives Objective One: Understand lithium's unique clinical benefits and neuroprotective properties, and the hypothesis that potent GSK3ß inhibition underlies these effects. Objective Two: Understand how lithium's affinity for the epithelial sodium channel in principal cells causes polyuria, why polyuria is an early signal of lithium related renal dysfunction, and how to monitor for and Objective Three: Understand how GSK3ß inhibition activates collapsin response mediator protein 2 (CRMP2) to support synaptic plasticity, and how this paradigm supports the development of investiga Objective Four: Objective Five:;..."

Alzheimer's Disease • Behavior Disorders • Bipolar Disorder • CNS Disorders • Dementia • Mental Retardation • Mood Disorders • Nephrology • Psychiatry • Renal Disease • CRMP

Lower Airway Potential Difference Testing Using a Novel Integrated Image Guided System (ATS 2025) - "We then tested a freshly euthanized swine to bronchoscopically introduce the probe into the lower airways to obtain PD values after perfusion of solutions to inhibit the epithelial sodium channel, ENaC (ΔAmiloride) and activate CFTR (ΔCl-free + isoproterenol)... Use of the novel image guided LAPD probe was feasible, safe, well tolerated, provided physiologically relevant PD values, and has the potential to substantially improve the quality of measurements in a pre-manufactured system. As treatment options for CF advance to include lower airway specific genetic therapies, functional readouts of CFTR activity resident within the lung are necessary to assess therapeutic and biological efficacy. Further enrollment of subjects to establish LAPD discrimination and normative values in CF disease state are underway."

Anesthesia • Cystic Fibrosis • Gene Therapies • Genetic Disorders • Immunology • Respiratory Diseases • CFTR

CFTR-Mediated Ion and Fluid Transport by Primary Ferret AT2 Epithelia (ATS 2025) - "In the presence of amiloride and DIDS to inhibit ENaC and non-CFTR anion channels, respectively, IBMX/forskolin induced chloride currents by WT AT2 ALI cultures (ΔIsc 33.57 ± 9.65 µA/cm2), but not G551D cultures (ΔIsc 0.13 ± 0.69 µA/cm2)... We demonstrate the ability to propagate ferret AT2 cells and maintain them as undifferentiated epithelia in ALI and organoid cultures. chloride movement by AT2 cells facilitates salt-mediated fluid movement, which counterbalances CFTR-independent fluid absorption. The mechanisms by which these processes interact in native mixed epithelial populations containing both AT2 and AT1 cells remain to be determined."

Cystic Fibrosis • Genetic Disorders • Immunology • Respiratory Diseases