Details of the Drug

General Information of Drug (ID: DMRTSGP)

Drug Name
Amiloride
Synonyms
Amiclaran; Amilorida; Amiloridum; Amipramidin; Amipramizid; Amipramizide; Amiprazidine; Amyloride; Guanamprazin; Guanamprazine; Midamor; Amiloride HCL; Amiloride hydrochloride hydrate; Amiclaran (TN); Amikal (Hydrochloride dihydrate); Amilorida [INN-Spanish]; Amiloride (INN); Amiloride [INN:BAN]; Amiloridum [INN-Latin]; Biduret (TN); Midamor (Hydrochloride dihydrate); MK-870 (Hydrochloride dihydrate); AMILORIDE (SEE ALSO: AMILORIDE HCL (2016-88-8)); N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide; N-Amidino-3,5-diamino-6-chlorpyrazincarboxamid; Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, monohydrochloride; 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide; 3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide; 3,5-diamino-N-[amino(imino)methyl]-6-chloropyrazine-2-carboxamide; 3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide; Amiloride (Na-Ca chanel blocker)
Indication
Disease Entry ICD 11 Status REF
Congestive heart failure BD10 Approved [1]
Edema MG29 Approved [2]
Therapeutic Class
Diuretics
Affected Organisms
Humans and other mammals
ATC Code
C03DB01: Amiloride
C03DB: Other potassium-sparing agents
C03D: ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS
C03: DIURETICS
C: CARDIOVASCULAR SYSTEM
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 229.63
Logarithm of the Partition Coefficient (xlogp) -0.7
Rotatable Bond Count (rotbonds) 1
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption
The drug is rapidly absorbed following oral administration []
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [3]
Elimination
49% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 6 - 9 hours [4]
Metabolism
The drug is not metabolised []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.47285 micromolar/kg/day [5]
Water Solubility
The ability of drug to dissolve in water is measured as 50 mg/mL [3]
Chemical Identifiers
Formula
C6H8ClN7O
IUPAC Name
3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide
Canonical SMILES
C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N
InChI
InChI=1S/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15)
InChIKey
XSDQTOBWRPYKKA-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
16231
ChEBI ID
CHEMBL945
CAS Number
2609-46-3
UNII
7DZO8EB0Z3
DrugBank ID
DB00594
TTD ID
D0I0RJ
VARIDT ID
DR00207
ACDINA ID
D00029
Drug-Molecule Activity Atlas (DMA)NEW Click to Jump to the Detailed DMA Information of This Drug
Drug Pharmacogenomic Perturbation (DPP)NEW Click to Jump to the Detailed DPP Information of This Drug
Drug ADMET Endpoint Profile (DAE)NEW Click to Jump to the Detailed DAE Information of This Drug
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Acid-sensing ion channel 1 (ASIC1) TTRJYB6 ASIC1_HUMAN Modulator [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [7]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Substrate [8]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Glutamate receptor-interacting protein 1 (GRIP1) OT958HK1 GRIP1_HUMAN Drug Response [9]
Multidrug and toxin extrusion protein 1 (SLC47A1) OTZX0U5Q S47A1_HUMAN Gene/Protein Processing [10]
Myogenic factor 5 (MYF5) OTTVO2S5 MYF5_HUMAN Gene/Protein Processing [11]
Pancreas/duodenum homeobox protein 1 (PDX1) OTX1DKRA PDX1_HUMAN Protein Interaction/Cellular Processes [12]
Protein c-Fos (FOS) OTJBUVWS FOS_HUMAN Gene/Protein Processing [13]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Post-Translational Modifications [14]
Serine/threonine-protein phosphatase PP1-alpha catalytic subunit (PPP1CA) OT7Y43A1 PP1A_HUMAN Post-Translational Modifications [14]
Vascular endothelial growth factor A, long form OTIM9MZ3 VEGFA_HUMAN Gene/Protein Processing [15]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Amiloride
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Eplerenone DMF0NQR Major Increased risk of hyperkalemia by the combination of Amiloride and Eplerenone. Heart failure [BD10-BD1Z] [16]
Digitoxin DMWVIGP Moderate Increased risk of hypomagnesemia by the combination of Amiloride and Digitoxin. Heart failure [BD10-BD1Z] [17]
Coadministration of a Drug Treating the Disease Different from Amiloride (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Linezolid DMGFPU2 Moderate Additive hypotensive effects by the combination of Amiloride and Linezolid. Bacterial infection [1A00-1C4Z] [18]
Amoxicillin DMUYNEI Minor Altered absorption of Amiloride caused by Amoxicillin. Bacterial infection [1A00-1C4Z] [19]
Pentosan polysulfate DM2HRKE Moderate Increased risk of hyperkalemia by the combination of Amiloride and Pentosan polysulfate. Chronic pain [MG30] [20]
Phenylbutazone DMAYL0T Moderate Antagonize the effect of Amiloride when combined with Phenylbutazone. Chronic pain [MG30] [21]
Ketoprofen DMRKXPT Moderate Antagonize the effect of Amiloride when combined with Ketoprofen. Chronic pain [MG30] [21]
Levomilnacipran DMV26S8 Moderate Increased risk of hyponatremia by the combination of Amiloride and Levomilnacipran. Chronic pain [MG30] [22]
Olopatadine DMKMWQG Moderate Additive CNS depression effects by the combination of Amiloride and Olopatadine. Conjunctiva disorder [9A60] [23]
Drospirenone DM1A9W3 Moderate Increased risk of hyperkalemia by the combination of Amiloride and Drospirenone. Contraceptive management [QA21] [24]
Ardeparin DMYRX8B Moderate Increased risk of hyperkalemia by the combination of Amiloride and Ardeparin. Coronary thrombosis [BA43] [25]
Danaparoid DM6CLBN Moderate Increased risk of hyperkalemia by the combination of Amiloride and Danaparoid. Deep vein thrombosis [BD71] [25]
Sertraline DM0FB1J Moderate Increased risk of hyponatremia by the combination of Amiloride and Sertraline. Depression [6A70-6A7Z] [22]
Vilazodone DM4LECQ Moderate Increased risk of hyponatremia by the combination of Amiloride and Vilazodone. Depression [6A70-6A7Z] [22]
Paroxetine DM5PVQE Moderate Increased risk of hyponatremia by the combination of Amiloride and Paroxetine. Depression [6A70-6A7Z] [22]
Selegiline DM6034S Moderate Additive hypotensive effects by the combination of Amiloride and Selegiline. Depression [6A70-6A7Z] [18]
Vortioxetine DM6F1PU Moderate Increased risk of hyponatremia by the combination of Amiloride and Vortioxetine. Depression [6A70-6A7Z] [22]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Amiloride and Isocarboxazid. Depression [6A70-6A7Z] [18]
Milnacipran DMBFE74 Moderate Increased risk of hyponatremia by the combination of Amiloride and Milnacipran. Depression [6A70-6A7Z] [22]
Escitalopram DMFK9HG Moderate Increased risk of hyponatremia by the combination of Amiloride and Escitalopram. Depression [6A70-6A7Z] [22]
Tranylcypromine DMGB5RE Moderate Additive hypotensive effects by the combination of Amiloride and Tranylcypromine. Depression [6A70-6A7Z] [18]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Amiloride and OPC-34712. Depression [6A70-6A7Z] [26]
Phenelzine DMHIDUE Moderate Additive hypotensive effects by the combination of Amiloride and Phenelzine. Depression [6A70-6A7Z] [18]
Eslicarbazepine DMZREFQ Moderate Increased risk of hyponatremia by the combination of Amiloride and Eslicarbazepine. Epilepsy/seizure [8A61-8A6Z] [27]
Mefenamic acid DMK7HFI Moderate Antagonize the effect of Amiloride when combined with Mefenamic acid. Female pelvic pain [GA34] [21]
Procarbazine DMIK367 Moderate Additive hypotensive effects by the combination of Amiloride and Procarbazine. Hodgkin lymphoma [2B30] [18]
Eprosartan DM07K2I Major Increased risk of hyperkalemia by the combination of Amiloride and Eprosartan. Hypertension [BA00-BA04] [28]
Aliskiren DM1BV7W Moderate Increased risk of hyperkalemia by the combination of Amiloride and Aliskiren. Hypertension [BA00-BA04] [29]
Moexipril DM26E4B Major Increased risk of hyperkalemia by the combination of Amiloride and Moexipril. Hypertension [BA00-BA04] [30]
Captopril DM458UM Major Increased risk of hyperkalemia by the combination of Amiloride and Captopril. Hypertension [BA00-BA04] [30]
Losartan DM72JXH Major Increased risk of hyperkalemia by the combination of Amiloride and Losartan. Hypertension [BA00-BA04] [28]
TAK-491 DMCF6SX Major Increased risk of hyperkalemia by the combination of Amiloride and TAK-491. Hypertension [BA00-BA04] [28]
Perindopril DMOPZDT Major Increased risk of hyperkalemia by the combination of Amiloride and Perindopril. Hypertension [BA00-BA04] [30]
Quinapril DMR8H31 Major Increased risk of hyperkalemia by the combination of Amiloride and Quinapril. Hypertension [BA00-BA04] [30]
Telmisartan DMS3GX2 Major Increased risk of hyperkalemia by the combination of Amiloride and Telmisartan. Hypertension [BA00-BA04] [28]
Irbesartan DMTP1DC Major Increased risk of hyperkalemia by the combination of Amiloride and Irbesartan. Hypertension [BA00-BA04] [28]
Lisinopril DMUOK4C Major Increased risk of hyperkalemia by the combination of Amiloride and Lisinopril. Hypertension [BA00-BA04] [30]
Potassium chloride DMMTAJC Major Increased risk of hyperkalemia by the combination of Amiloride and Potassium chloride. Hypo-kalaemia [5C77] [31]
Tolvaptan DMIWFRL Moderate Increased risk of hyperkalemia by the combination of Amiloride and Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [32]
Meclofenamic acid DM05FXR Moderate Antagonize the effect of Amiloride when combined with Meclofenamic acid. Inflammatory spondyloarthritis [FA92] [21]
Propiomazine DMKY8V1 Moderate Additive hypotensive effects by the combination of Amiloride and Propiomazine. Insomnia [7A00-7A0Z] [26]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Amiloride and ITI-007. Insomnia [7A00-7A0Z] [26]
Ozanimod DMT6AM2 Moderate Additive hypotensive effects by the combination of Amiloride and Ozanimod. Multiple sclerosis [8A40] [18]
Promethazine DM6I5GR Moderate Additive hypotensive effects by the combination of Amiloride and Promethazine. Nausea/vomiting [MD90] [26]
Sibutramine DMFJTDI Moderate Increased risk of hyponatremia by the combination of Amiloride and Sibutramine. Obesity [5B80-5B81] [22]
Naproxen DMZ5RGV Moderate Antagonize the effect of Amiloride when combined with Naproxen. Osteoarthritis [FA00-FA05] [21]
Etodolac DM6WJO9 Moderate Antagonize the effect of Amiloride when combined with Etodolac. Pain [MG30-MG3Z] [21]
Diflunisal DM7EN8I Moderate Antagonize the effect of Amiloride when combined with Diflunisal. Pain [MG30-MG3Z] [21]
Ibuprofen DM8VCBE Moderate Antagonize the effect of Amiloride when combined with Ibuprofen. Pain [MG30-MG3Z] [21]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Amiloride and Safinamide. Parkinsonism [8A00] [18]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Amiloride and Rasagiline. Parkinsonism [8A00] [18]
Bromfenac DMKB79O Moderate Antagonize the effect of Amiloride when combined with Bromfenac. Postoperative inflammation [1A00-CA43] [21]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Amiloride and Levomepromazine. Psychotic disorder [6A20-6A25] [26]
Meloxicam DM2AR7L Moderate Antagonize the effect of Amiloride when combined with Meloxicam. Rheumatoid arthritis [FA20] [21]
Sulindac DM2QHZU Moderate Antagonize the effect of Amiloride when combined with Sulindac. Rheumatoid arthritis [FA20] [21]
Oxaprozin DM9UB0P Moderate Antagonize the effect of Amiloride when combined with Oxaprozin. Rheumatoid arthritis [FA20] [21]
Flurbiprofen DMGN4BY Moderate Antagonize the effect of Amiloride when combined with Flurbiprofen. Rheumatoid arthritis [FA20] [21]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Amiloride and Quetiapine. Schizophrenia [6A20] [26]
Mesoridazine DM2ZGAN Moderate Additive hypotensive effects by the combination of Amiloride and Mesoridazine. Schizophrenia [6A20] [26]
Thioridazine DM35M8J Moderate Additive hypotensive effects by the combination of Amiloride and Thioridazine. Schizophrenia [6A20] [26]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Amiloride and Aripiprazole. Schizophrenia [6A20] [26]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Amiloride and Iloperidone. Schizophrenia [6A20] [26]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Amiloride and Paliperidone. Schizophrenia [6A20] [26]
Perphenazine DMA4MRX Moderate Additive hypotensive effects by the combination of Amiloride and Perphenazine. Schizophrenia [6A20] [26]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Amiloride and Molindone. Schizophrenia [6A20] [26]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Amiloride and Thiothixene. Schizophrenia [6A20] [26]
Trifluoperazine DMKBYWI Moderate Additive hypotensive effects by the combination of Amiloride and Trifluoperazine. Schizophrenia [6A20] [26]
Risperidone DMN6DXL Moderate Additive hypotensive effects by the combination of Amiloride and Risperidone. Schizophrenia [6A20] [26]
Amisulpride DMSJVAM Moderate Additive hypotensive effects by the combination of Amiloride and Amisulpride. Schizophrenia [6A20] [26]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Amiloride and Asenapine. Schizophrenia [6A20] [26]
Tacrolimus DMZ7XNQ Major Increased risk of hyperkalemia by the combination of Amiloride and Tacrolimus. Transplant rejection [NE84] [33]
Methdilazine DMAUHQX Moderate Additive hypotensive effects by the combination of Amiloride and Methdilazine. Vasomotor/allergic rhinitis [CA08] [26]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Amiloride and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [34]
⏷ Show the Full List of 71 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Quinoline yellow WS E00309 24671 Colorant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Brushite E00392 104805 Diluent
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 12 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Amiloride Hydrochloride 5mg tablet 5mg Tablet Oral
Amiloride 5 mg tablet 5 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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11 In vivo and in vitro dysferlin expression in human muscle satellite cells. J Neuropathol Exp Neurol. 2004 Oct;63(10):1104-13. doi: 10.1093/jnen/63.10.1104.
12 PDX-1 protein is internalized by lipid raft-dependent macropinocytosis. Cell Transplant. 2005;14(9):637-45. doi: 10.3727/000000005783982648.
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14 Role of HER-2/neu signaling in sensitivity to tumor necrosis factor-related apoptosis-inducing ligand: enhancement of TRAIL-mediated apoptosis by amiloride. J Cell Biochem. 2005 Oct 1;96(2):376-89. doi: 10.1002/jcb.20512.
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