Stem definition | Drug id | CAS RN |
---|---|---|
antibacterials, nalidixic acid derivatives | 1280 | 112811-59-3 |
Dose | Unit | Route |
---|---|---|
0.40 | g | O |
0.40 | g | P |
Property | Value | Reference |
---|---|---|
BA (Bioavailability) | 96 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 1.70 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 2.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.80 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 10 hours | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 60 mg/mL | Bocci G, Oprea TI, Benet LZ |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
March 28, 2003 | FDA | ALLERGAN |
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 |
---|---|---|---|---|---|---|
Anaphylactic reaction | 135.98 | 30.99 | 51 | 1260 | 66049 | 63421662 |
Hypoglycaemia | 104.28 | 30.99 | 41 | 1270 | 60024 | 63427687 |
Drug hypersensitivity | 98.03 | 30.99 | 67 | 1244 | 310620 | 63177091 |
Drug intolerance | 55.96 | 30.99 | 48 | 1263 | 308613 | 63179098 |
Toxic anterior segment syndrome | 46.19 | 30.99 | 10 | 1301 | 1761 | 63485950 |
Corneal disorder | 45.95 | 30.99 | 10 | 1301 | 1804 | 63485907 |
Visual acuity reduced | 41.66 | 30.99 | 16 | 1295 | 21810 | 63465901 |
Cataract | 40.82 | 30.99 | 21 | 1290 | 57032 | 63430679 |
Hyperglycaemia | 40.70 | 30.99 | 19 | 1292 | 41848 | 63445863 |
Keratitis | 34.73 | 30.99 | 9 | 1302 | 3413 | 63484298 |
Endophthalmitis | 34.29 | 30.99 | 9 | 1302 | 3583 | 63484128 |
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 |
---|---|---|---|---|---|---|
Hypoglycaemia | 262.34 | 25.73 | 101 | 1769 | 54539 | 34900522 |
Hyperglycaemia | 137.10 | 25.73 | 58 | 1812 | 39422 | 34915639 |
Intraocular pressure increased | 82.59 | 25.73 | 24 | 1846 | 5359 | 34949702 |
Clostridium colitis | 76.91 | 25.73 | 17 | 1853 | 1262 | 34953799 |
Visual acuity reduced | 73.97 | 25.73 | 29 | 1841 | 16120 | 34938941 |
Blood glucose decreased | 61.41 | 25.73 | 24 | 1846 | 13213 | 34941848 |
Corneal oedema | 44.38 | 25.73 | 11 | 1859 | 1340 | 34953721 |
Blood glucose increased | 39.78 | 25.73 | 31 | 1839 | 66687 | 34888374 |
Retinal haemorrhage | 37.57 | 25.73 | 13 | 1857 | 5076 | 34949985 |
International normalised ratio increased | 34.92 | 25.73 | 25 | 1845 | 47302 | 34907759 |
Corneal opacity | 30.90 | 25.73 | 7 | 1863 | 579 | 34954482 |
Toxic anterior segment syndrome | 30.89 | 25.73 | 8 | 1862 | 1161 | 34953900 |
Vitreous haemorrhage | 29.50 | 25.73 | 9 | 1861 | 2364 | 34952697 |
Eye pain | 28.31 | 25.73 | 14 | 1856 | 13448 | 34941613 |
Vision blurred | 26.59 | 25.73 | 21 | 1849 | 45942 | 34909119 |
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 |
---|---|---|---|---|---|---|
Hypoglycaemia | 347.20 | 25.45 | 130 | 2600 | 101464 | 79640194 |
Hyperglycaemia | 169.14 | 25.45 | 70 | 2660 | 70265 | 79671393 |
Intraocular pressure increased | 107.16 | 25.45 | 30 | 2700 | 9175 | 79732483 |
Anaphylactic reaction | 99.10 | 25.45 | 51 | 2679 | 83692 | 79657966 |
Visual acuity reduced | 86.81 | 25.45 | 34 | 2696 | 29435 | 79712223 |
Corneal disorder | 63.92 | 25.45 | 15 | 2715 | 2276 | 79739382 |
Corneal oedema | 56.83 | 25.45 | 14 | 2716 | 2606 | 79739052 |
Toxic anterior segment syndrome | 56.09 | 25.45 | 14 | 2716 | 2750 | 79738908 |
Blood glucose decreased | 55.85 | 25.45 | 24 | 2706 | 26210 | 79715448 |
Clostridium colitis | 55.71 | 25.45 | 14 | 2716 | 2825 | 79738833 |
Drug hypersensitivity | 44.74 | 25.45 | 53 | 2677 | 298863 | 79442795 |
Drug intolerance | 41.45 | 25.45 | 48 | 2682 | 264071 | 79477587 |
Corneal opacity | 41.02 | 25.45 | 9 | 2721 | 1011 | 79740647 |
Endophthalmitis | 40.28 | 25.45 | 13 | 2717 | 6415 | 79735243 |
Vision blurred | 37.15 | 25.45 | 30 | 2700 | 105868 | 79635790 |
Blood glucose increased | 34.99 | 25.45 | 30 | 2700 | 114945 | 79626713 |
Conjunctival hyperaemia | 32.09 | 25.45 | 10 | 2720 | 4403 | 79737255 |
Keratitis fungal | 31.78 | 25.45 | 6 | 2724 | 318 | 79741340 |
Corneal endotheliitis | 31.65 | 25.45 | 5 | 2725 | 91 | 79741567 |
Cataract subcapsular | 30.56 | 25.45 | 7 | 2723 | 954 | 79740704 |
International normalised ratio increased | 29.70 | 25.45 | 24 | 2706 | 84697 | 79656961 |
Eye pain | 28.21 | 25.45 | 17 | 2713 | 37561 | 79704097 |
Vitreous opacities | 27.39 | 25.45 | 6 | 2724 | 669 | 79740989 |
Macular oedema | 26.05 | 25.45 | 9 | 2721 | 5465 | 79736193 |
None
Source | Code | Description |
---|---|---|
ATC | J01MA16 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
ATC | S01AE06 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Fluoroquinolones |
FDA CS | M0023650 | Quinolones |
CHEBI has role | CHEBI:33281 | antibiotics |
CHEBI has role | CHEBI:35441 | antiinfective agents |
CHEBI has role | CHEBI:50750 | inhibitors of type II topoisomerase |
MeSH PA | D000900 | Anti-Bacterial Agents |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D009883 | Ophthalmic Solutions |
MeSH PA | D019999 | Pharmaceutical Solutions |
MeSH PA | D059005 | Topoisomerase II Inhibitors |
MeSH PA | D059003 | Topoisomerase Inhibitors |
FDA EPC | N0000175937 | Quinolone Antimicrobial |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Acute gonococcal cervicitis | indication | 20943002 | DOID:10615 |
Staphylococcal pneumonia | indication | 22754005 | |
Acute gonococcal urethritis | indication | 29864006 | |
Pneumonia due to Streptococcus | indication | 34020007 | |
Gonorrhea of rectum | indication | 42746002 | |
Pneumonia due to Mycoplasma pneumoniae | indication | 46970008 | |
Bacterial pneumonia | indication | 53084003 | DOID:874 |
Klebsiella cystitis | indication | 60867007 | |
Haemophilus influenzae pneumonia | indication | 70036007 | |
Acute bacterial sinusitis | indication | 75498004 | |
Bacterial conjunctivitis | indication | 128350005 | DOID:9700 |
Pneumococcal pneumonia | indication | 233607000 | |
Chlamydial pneumonia | indication | 233609002 | |
Escherichia coli urinary tract infection | indication | 301011002 | |
Proteus urinary tract infection | indication | 301012009 | |
Bacterial urinary infection | indication | 312124009 | |
Infection due to Staphylococcus aureus | indication | 406602003 | |
Acute exacerbation of chronic bronchitis | indication | 425748003 | |
Urinary tract infection caused by Klebsiella | indication | 369001000119100 | |
Moraxella Catarrhalis Chronic Bronchitis | indication | ||
E. Coli Pyelonephritis | indication | ||
Haemophilus Parainfluenzae Chronic Bronchitis | indication | ||
Legionella Pneumophila Pneumonia | indication | ||
Moraxella Catarrhalis Pneumonia | indication | ||
Staphylococcus Chronic Bronchitis | indication | ||
Complicated Proteus UTI | indication | ||
Streptococcus Pneumoniae Chronic Bronchitis | indication | ||
Skin and Skin Structure Streptococcus Infection | indication | ||
Haemophilus Influenzae Chronic Bronchitis | indication | ||
Haemophilus Parainfluenzae Pneumonia | indication | ||
Acute tuberculosis | off-label use | 25629007 | |
Pulmonary tuberculosis | off-label use | 154283005 | DOID:2957 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 6.23 | acidic |
pKa2 | 8.39 | Basic |
pKa3 | 1.22 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
DNA topoisomerase 4 | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
DNA gyrase | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
DNA topoisomerase 4 subunit A | Enzyme | IC50 | 5.92 | CHEMBL | |||||
DNA gyrase subunit A | Enzyme | IC50 | 5.03 | CHEMBL | |||||
DNA gyrase | Enzyme | IC50 | 6.30 | CHEMBL |
ID | Source |
---|---|
4021187 | VUID |
N0000148634 | NUI |
D00589 | KEGG_DRUG |
180200-66-2 | SECONDARY_CAS_RN |
4021187 | VANDF |
CHEBI:5280 | CHEBI |
GFN | PDB_CHEM_ID |
CHEMBL31 | ChEMBL_ID |
CHEMBL428581 | ChEMBL_ID |
CHEMBL251670 | ChEMBL_ID |
10816 | IUPHAR_LIGAND_ID |
DB01044 | DRUGBANK_ID |
L4618BD7KJ | UNII |
1546025 | RXNORM |
8587 | MMSL |
d04504 | MMSL |
007995 | NDDF |
116349004 | SNOMEDCT_US |
371238005 | SNOMEDCT_US |
C0753645 | UMLSCUI |
D000077734 | MESH_DESCRIPTOR_UI |
7423 | INN_ID |
5379 | PUBCHEM_CID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
ZYMAXID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-3615 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | NDA | 25 sections |
ZYMAXID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-3615 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | NDA | 25 sections |
ZYMAR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-9218 | SOLUTION/ DROPS | 3 mg | OPHTHALMIC | EXPORT ONLY | 1 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-526 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 20 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-526 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 20 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13668-526 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 20 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50383-189 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 23 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50383-189 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 23 sections |
ZYMAXID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6303 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | NDA | 25 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57297-435 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 24 sections |
gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60758-615 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | NDA authorized generic | 25 sections |
gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60758-615 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | NDA authorized generic | 25 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-672 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 23 sections |
Gatifloxacin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68180-435 | SOLUTION/ DROPS | 5 mg | OPHTHALMIC | ANDA | 24 sections |