Stem definition | Drug id | CAS RN |
---|---|---|
diuretics, furosemide derivatives | 1258 | 54-31-9 |
Dose | Unit | Route |
---|---|---|
40 | mg | O |
40 | mg | P |
40 | mg | O |
Property | Value | Reference |
---|---|---|
BA (Bioavailability) | 71 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
EoM (Fraction excreted unchanged in urine) | 66 % | Benet LZ, Broccatelli F, Oprea TI |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 25.92 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
t_half (Half-life) | 2.50 hours | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 1.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
Vd (Volume of distribution) | 0.12 L/kg | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 0.07 mg/mL | Bocci G, Oprea TI, Benet LZ |
fu (Fraction unbound in plasma) | 0.01 % | Lombardo F, Berellini G, Obach RS |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Acute kidney injury | 3456.16 | 10.57 | 6881 | 494281 | 256534 | 62731326 |
Cardiac failure congestive | 2567.78 | 10.57 | 3399 | 497763 | 89034 | 62898826 |
Drug ineffective | 1856.33 | 10.57 | 3402 | 497760 | 1041363 | 61946497 |
Cardiac failure | 1635.68 | 10.57 | 2698 | 498464 | 86444 | 62901416 |
Hyperkalaemia | 1543.99 | 10.57 | 2019 | 499143 | 52184 | 62935676 |
Pemphigus | 1373.37 | 10.57 | 14 | 501148 | 183712 | 62804148 |
Hyponatraemia | 1197.82 | 10.57 | 2695 | 498467 | 109205 | 62878655 |
Glossodynia | 1161.16 | 10.57 | 61 | 501101 | 178815 | 62809045 |
Hand deformity | 1153.27 | 10.57 | 21 | 501141 | 159436 | 62828424 |
Contraindicated product administered | 1023.74 | 10.57 | 232 | 500930 | 217416 | 62770444 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Cardiac failure congestive | 1934.05 | 11.62 | 3370 | 382693 | 79900 | 34490968 |
Acute kidney injury | 1920.46 | 11.62 | 7532 | 378531 | 297456 | 34273412 |
Cardiac failure | 1344.17 | 11.62 | 3053 | 383010 | 88195 | 34482673 |
Hyperkalaemia | 1022.69 | 11.62 | 2323 | 383740 | 67066 | 34503802 |
Drug ineffective | 997.04 | 11.62 | 2239 | 383824 | 454512 | 34116356 |
Drug abuse | 614.57 | 11.62 | 167 | 385896 | 98929 | 34471939 |
Oedema peripheral | 589.81 | 11.62 | 2753 | 383310 | 117059 | 34453809 |
Off label use | 583.78 | 11.62 | 2521 | 383542 | 417003 | 34153865 |
Renal failure | 534.33 | 11.62 | 2847 | 383216 | 127710 | 34443158 |
Hypotension | 532.99 | 11.62 | 4225 | 381838 | 217424 | 34353444 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Acute kidney injury | 5051.68 | 10.43 | 13448 | 741155 | 505956 | 78483829 |
Cardiac failure congestive | 3981.00 | 10.43 | 5769 | 748834 | 136633 | 78853152 |
Cardiac failure | 2594.66 | 10.43 | 4987 | 749616 | 149855 | 78839930 |
Hyperkalaemia | 2419.19 | 10.43 | 4078 | 750525 | 110320 | 78879465 |
Drug ineffective | 2046.39 | 10.43 | 4511 | 750092 | 1076402 | 77913383 |
Hypotension | 1372.19 | 10.43 | 7965 | 746638 | 432352 | 78557433 |
Renal failure | 1335.32 | 10.43 | 4561 | 750042 | 196407 | 78793378 |
Off label use | 1190.63 | 10.43 | 4498 | 750105 | 902717 | 78087068 |
International normalised ratio increased | 1177.82 | 10.43 | 2527 | 752076 | 82194 | 78907591 |
Oedema peripheral | 1165.73 | 10.43 | 5103 | 749500 | 247185 | 78742600 |
None
Source | Code | Description |
---|---|---|
ATC | C03CA01 | CARDIOVASCULAR SYSTEM DIURETICS HIGH-CEILING DIURETICS Sulfonamides, plain |
ATC | C03CB01 | CARDIOVASCULAR SYSTEM DIURETICS HIGH-CEILING DIURETICS Sulfonamides and potassium in combination |
ATC | C03EB01 | CARDIOVASCULAR SYSTEM DIURETICS DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION High-ceiling diuretics and potassium-sparing agents |
CHEBI has role | CHEBI:35703 | Xenobiotic |
CHEBI has role | CHEBI:77608 | loop diuretics |
CHEBI has role | CHEBI:78298 | environmental contaminants |
FDA EPC | N0000175590 | Loop Diuretic |
FDA PE | N0000175366 | Increased Diuresis at Loop of Henle |
MeSH PA | D004232 | Diuretics |
MeSH PA | D049990 | Membrane Transport Modulators |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Hypertensive disorder | indication | 38341003 | DOID:10763 |
Acute pulmonary edema | indication | 40541001 | |
Decompensated cardiac failure | indication | 195111005 | |
Edema | indication | 267038008 | |
Pulmonary Edema due to Chronic Heart Failure | indication | ||
Edema due to Hepatic Cirrhosis | indication | ||
Peripheral Edema due to Chronic Heart Failure | indication | ||
Hypercalcemia | off-label use | 66931009 | DOID:12678 |
Prevention of Oliguria | off-label use | ||
Metabolic alkalosis | contraindication | 1388004 |
Species | Use | Relation |
---|---|---|
Cats | Edema (pulmonary congestion, ascites) associated with cardiac insufficiency | Indication |
Cats | Acute noninflammatory tissue edema | Indication |
Cattle | Physiological parturient edema of the mammary gland and associated structures | Indication |
Dogs | Edema (pulmonary congestion, ascites) associated with cardiac insufficiency | Indication |
Dogs | Acute noninflammatory tissue edema | Indication |
Horses | Edema (pulmonary congestion, ascites) associated with cardiac insufficiency | Indication |
Horses | Acute noninflammatory tissue edema | Indication |
Product | Applicant | Ingredients |
---|---|---|
Disal | Boehringer lngelheim Animal Health USA Inc. | 1 |
Disal | Boehringer lngelheim Animal Health USA Inc. | 1 |
Disal Injection | Boehringer lngelheim Animal Health USA Inc. | 1 |
Furos-A-Vet | Bimeda Animal Health Limited | 1 |
Furosemide Injection 5% | Elanco US Inc. | 1 |
Furosemide Syrup 1% | First Priority Inc. | 1 |
Furosemide Syrup 1% | Cronus Pharma Specialities India Private Limited | 1 |
Lasix Packets | Intervet Inc. | 1 |
Lasix Syrup 1% | Intervet Inc. | 1 |
Salix Injection 5% | Intervet Inc. | 1 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.69 | acidic |
pKa2 | 10.59 | acidic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
80MG/10ML (8MG/ML) | FUROSCIX | SCPHARMACEUTICALS | N209988 | Oct. 7, 2022 | RX | SOLUTION | SUBCUTANEOUS | 11433044 | April 3, 2034 | USE OF A LIQUID FORMULATION COMPRISING FUROSEMIDE TO TREAT CONGESTION DUE TO FLUID OVERLOAD (EDEMA) IN ADULTS WITH NYHA CLASS II/III CHRONIC HEART FAILURE |
80MG/10ML (8MG/ML) | FUROSCIX | SCPHARMACEUTICALS | N209988 | Oct. 7, 2022 | RX | SOLUTION | SUBCUTANEOUS | 9884039 | April 3, 2034 | USE OF A LIQUID FORMULATION COMPRISING FUROSEMIDE TO TREAT CONGESTION DUE TO FLUID OVERLOAD (EDEMA) IN ADULTS WITH NYHA CLASS II/III CHRONIC HEART FAILURE |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Solute carrier family 12 member 1 | Transporter | INHIBITOR | IC50 | 6.20 | WOMBAT-PK | CHEMBL | |||
Sodium/potassium-transporting ATPase subunit alpha-1 | Transporter | WOMBAT-PK | |||||||
Carbonic anhydrase 2 | Enzyme | Ki | 7.19 | CHEMBL | |||||
ATP-binding cassette sub-family G member 2 | Transporter | IC50 | 5.50 | CHEMBL | |||||
Carbonic anhydrase 1 | Enzyme | Ki | 7.21 | CHEMBL | |||||
Carbonic anhydrase 4 | Enzyme | Ki | 6.25 | CHEMBL | |||||
Carbonic anhydrase 9 | Enzyme | Ki | 6.38 | CHEMBL | |||||
Carbonic anhydrase 12 | Enzyme | Ki | 6.58 | CHEMBL | |||||
Carbonic anhydrase 5A, mitochondrial | Enzyme | Ki | 6.30 | CHEMBL | |||||
Carbonic anhydrase 5B, mitochondrial | Enzyme | Ki | 6.49 | CHEMBL |
ID | Source |
---|---|
FUN | PDB_CHEM_ID |
002307 | NDDF |
1584 | INN_ID |
3440 | PUBCHEM_CID |
387475002 | SNOMEDCT_US |
3962 | MMSL |
4017830 | VUID |
4017830 | VANDF |
4603 | RXNORM |
4769 | MMSL |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3294 | SOLUTION | 10 mg | ORAL | ANDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3294 | SOLUTION | 10 mg | ORAL | ANDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3294 | SOLUTION | 10 mg | ORAL | ANDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3298 | SOLUTION | 40 mg | ORAL | ANDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3298 | SOLUTION | 40 mg | ORAL | ANDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-3298 | SOLUTION | 40 mg | ORAL | ANDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-4297 | TABLET | 20 mg | ORAL | NDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-4297 | TABLET | 20 mg | ORAL | NDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-4297 | TABLET | 20 mg | ORAL | NDA | 21 sections |
Furosemide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-4299 | TABLET | 40 mg | ORAL | NDA | 21 sections |