roxithromycin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, produced by Streptomyces strains 2410 80214-83-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • roxithromycin
  • rotramin
  • claramid
  • roxacin
  • roxeptin
  • Roxithromycin A
Semisynthetic derivative of erythromycin. It is concentrated by human phagocytes and is bioactive intracellularly. While the drug is active against a wide spectrum of pathogens, it is particularly effective in the treatment of respiratory and genital tract infections.
  • Molecular weight: 837.06
  • Formula: C41H76N2O15
  • CLOGP: 2.20
  • LIPINSKI: 2
  • HAC: 17
  • HDO: 5
  • TPSA: 216.89
  • ALOGS: -3.65
  • ROTB: 13

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.19 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 12 % Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability) 50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1987 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Jaundice 38.35 30.12 18 1221 53331 79689818

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01FA06 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
MACROLIDES, LINCOSAMIDES AND STREPTOGRAMINS
Macrolides
CHEBI has role CHEBI:35703 Xenobiotic
CHEBI has role CHEBI:78298 environmental contaminants
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.96 acidic
pKa2 8.65 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Motilin receptor GPCR AGONIST IC50 6.20 IUPHAR
50S ribosomal protein L10 Ribosomal protein WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 6.26 DRUG MATRIX

External reference:

IDSource
N0000168422 NUI
D01710 KEGG_DRUG
C0035891 UMLSCUI
CHEBI:48935 CHEBI
ROX PDB_CHEM_ID
CHEMBL1214185 ChEMBL_ID
D015575 MESH_DESCRIPTOR_UI
DB00778 DRUGBANK_ID
1465 IUPHAR_LIGAND_ID
5815 INN_ID
21KOF230FA UNII
6915744 PUBCHEM_CID
9478 RXNORM
004199 NDDF
713769006 SNOMEDCT_US
96037004 SNOMEDCT_US

Pharmaceutical products:

None