gemifloxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, nalidixic acid derivatives | 1286 | 175463-14-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.32 | g | O |
| 0.20 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 3.52 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 7.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.30 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 8.30 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.35 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 4, 2003 | FDA | LG LIFE SCIENCES | |
| Dec. 27, 2002 | Korean Food and Drug Administration (KFDA) |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01MA15 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
| FDA CS | M0023650 | Quinolones |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| MeSH PA | D059003 | Topoisomerase Inhibitors |
| FDA EPC | N0000175937 | Quinolone Antimicrobial |
| CHEBI has role | CHEBI:33281 | antibiotics |
| CHEBI has role | CHEBI:36047 | antibacterial drugs |
| CHEBI has role | CHEBI:53559 | topoisomerase IV inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pneumonia due to Mycoplasma pneumoniae | indication | 46970008 | |
| Bacterial pneumonia | indication | 53084003 | DOID:874 |
| Pneumonia due to Klebsiella pneumoniae | indication | 64479007 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Acute bacterial bronchitis | indication | 233598009 | |
| Pneumococcal pneumonia | indication | 233607000 | |
| Chlamydial pneumonia | indication | 233609002 | |
| Acute exacerbation of chronic bronchitis | indication | 425748003 | |
| Moraxella Catarrhalis Pneumonia | indication | ||
| Torsades de pointes | contraindication | 31722008 | |
| Transplantation of heart | contraindication | 32413006 | |
| Tendinitis | contraindication | 34840004 | DOID:971 |
| Depressive disorder | contraindication | 35489007 | |
| Hypokalemia | contraindication | 43339004 | |
| Bradycardia | contraindication | 48867003 | |
| Transplant of kidney | contraindication | 70536003 | |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Transplant of lung | contraindication | 88039007 | |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Prolonged QT interval | contraindication | 111975006 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Impaired renal function disorder | contraindication | 197663003 | |
| Peripheral nerve disease | contraindication | 302226006 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Congenital long QT syndrome | contraindication | 442917000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.27 | acidic |
| pKa2 | 9.75 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| DNA topoisomerase 4 subunit A | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL | |||||
| DNA topoisomerase 4 subunit A | Enzyme | IC50 | 6.52 | CHEMBL | |||||
| DNA gyrase subunit B | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4021386 | VUID |
| N0000148804 | NUI |
| D02471 | KEGG_DRUG |
| 210353-53-0 | SECONDARY_CAS_RN |
| 4021386 | VANDF |
| 4021387 | VANDF |
| C0533545 | UMLSCUI |
| CHEBI:101853 | CHEBI |
| CHEMBL430 | ChEMBL_ID |
| CHEMBL1200621 | ChEMBL_ID |
| DB01155 | DRUGBANK_ID |
| D000077735 | MESH_DESCRIPTOR_UI |
| 9571107 | PUBCHEM_CID |
| 12406 | IUPHAR_LIGAND_ID |
| 7877 | INN_ID |
| OKR68Y0E4T | UNII |
| 138099 | RXNORM |
| 17216 | MMSL |
| d04859 | MMSL |
| 000543 | NDDF |
| 000557 | NDDF |
| 407086007 | SNOMEDCT_US |
| 407087003 | SNOMEDCT_US |
| 426551002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| FACTIVE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 44001-321 | TABLET | 320 mg | ORAL | NDA | 21 sections |
| FACTIVE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 44004-321 | TABLET | 320 mg | ORAL | NDA | 18 sections |