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

Stem definition	Drug id	CAS RN
antibiotics, cefalosporanic acid derivatives	548	61622-34-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

cefotiam
cefotiam hydrochloride
cefotiam HCl

One of the CEPHALOSPORINS that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms.

Molecular weight: 525.62
Formula: C18H23N9O4S3
CLOGP: -3.37
LIPINSKI: 2
HAC: 13
HDO: 3
TPSA: 172.46
ALOGS: -2.61
ROTB: 10

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1.20	g	O
4	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	80 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	190.25 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.26 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.50 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.84 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
None	FDA	TAKEDA

FDA Adverse Event Reporting System (Female)

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
Toxic epidermal necrolysis	67.19	57.78	15	150	25319	63463538

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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
Toxic epidermal necrolysis	56.25	43.27	17	406	44564	79699401

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	J01DC07	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Second-generation cephalosporins
CHEBI has role	CHEBI:36047	antibacterial drugs
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 level	Dissociation constant	Type (acidic/basic)
pKa1	2.63	acidic
pKa2	7.38	Basic
pKa3	4.64	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
Matrix metalloproteinase-9	Enzyme	P14780	MMP9_HUMAN		IC50	4.46		WOMBAT-PK
Vasoactive intestinal polypeptide receptor 1	GPCR	P32241	VIPR1_HUMAN		IC50	4.47		WOMBAT-PK
Bacterial penicillin-binding protein	Enzyme		PBPA_ECOLI PBPB_ECOLI DACC_ECOLI PBP2_ECOLI FTSI_ECOLI DACA_ECOLI DACB_ECOLI	INHIBITOR				CHEMBL	CHEMBL
Penicillin-binding protein 1A	Enzyme		PBPA_CLOPE					WOMBAT-PK

External reference:

ID	Source
N0000166878	NUI
D01819	KEGG_DRUG
2188	RXNORM
C0007556	UMLSCUI
CHEBI:355510	CHEBI
CHEMBL1296	ChEMBL_ID
D015310	MESH_DESCRIPTOR_UI
DB00229	DRUGBANK_ID
12254	IUPHAR_LIGAND_ID
4565	INN_ID
66309-69-1	SECONDARY_CAS_RN
91W6Z2N718	UNII
43708	PUBCHEM_CID
005393	NDDF
005394	NDDF
421700007	SNOMEDCT_US
422345006	SNOMEDCT_US
CHEMBL1200589	ChEMBL_ID

Pharmaceutical products:

None