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

Stem definition	Drug id	CAS RN
antibiotics, cefalosporanic acid derivatives	564	73384-59-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ceftriaxone sodium hydrate ceftriaxone biotrakson rocefin rocephalin rophex ceftriaxone sodium	A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears. Molecular weight: 554.57 Formula: C18H18N8O7S3 CLOGP: -1.24 LIPINSKI: 2 HAC: 15 HDO: 4 TPSA: 208.98 ALOGS: -3.72 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ceftriaxone sodium hydrate
ceftriaxone
biotrakson
rocefin
rocephalin
rophex
ceftriaxone sodium

A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears.

Molecular weight: 554.57
Formula: C18H18N8O7S3
CLOGP: -1.24
LIPINSKI: 2
HAC: 15
HDO: 4
TPSA: 208.98
ALOGS: -3.72
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2	g	P
2	g	P

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	7.60 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	46 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	400 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	120.27 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	0.22 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.12 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.10 %	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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Approvals:

Date	Agency	Company	Orphan
Dec. 21, 1984	FDA

FDA Adverse Event Reporting System (Female)

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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
Drug reaction with eosinophilia and systemic symptoms	736.10	12.38	403	47480	33433	63407706
Acute generalised exanthematous pustulosis	405.71	12.38	188	47695	10911	63430228
Toxic epidermal necrolysis	389.50	12.38	241	47642	25093	63416046
Acute kidney injury	356.58	12.38	679	47204	262736	63178403
Eosinophilia	338.50	12.38	212	47671	22544	63418595
Pseudocholelithiasis	328.64	12.38	54	47829	6	63441133
Rash maculo-papular	291.37	12.38	220	47663	31676	63409463
Fatigue	244.07	12.38	189	47694	887839	62553300
Multiple organ dysfunction syndrome	238.02	12.38	252	47631	56500	63384639
Pain	214.45	12.38	149	47734	740479	62700660

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FDA Adverse Event Reporting System (Male)

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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
Off label use	512.53	12.17	1586	51158	417938	34486249
Drug reaction with eosinophilia and systemic symptoms	445.03	12.17	381	52363	32631	34871556
Postrenal failure	291.90	12.17	78	52666	377	34903810
Jarisch-Herxheimer reaction	262.79	12.17	76	52668	515	34903672
Appendicolith	235.18	12.17	152	52592	8449	34895738
Pseudocholelithiasis	225.43	12.17	41	52703	0	34904187
Rash maculo-papular	197.65	12.17	229	52515	28222	34875965
Appendicitis	197.54	12.17	170	52574	14637	34889550
Multiple organ dysfunction syndrome	185.08	12.17	377	52367	76189	34827998
Fatigue	173.17	12.17	183	52561	370470	34533717

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FDA Adverse Event Reporting System (Geriatric)

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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
Drug reaction with eosinophilia and systemic symptoms	1098.89	11.22	774	93837	63470	79586307
Off label use	719.09	11.22	2529	92082	904686	78745091
Pseudocholelithiasis	532.68	11.22	94	94517	7	79649770
Acute generalised exanthematous pustulosis	486.39	11.22	285	94326	16969	79632808
Acute kidney injury	471.99	11.22	1519	93092	517885	79131892
Rash maculo-papular	441.52	11.22	431	94180	55647	79594130
Eosinophilia	427.06	11.22	385	94226	44960	79604817
Multiple organ dysfunction syndrome	423.05	11.22	612	93999	119634	79530143
Toxic epidermal necrolysis	405.12	11.22	371	94240	44210	79605567
Fatigue	391.57	11.22	319	94292	929408	78720369

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J01DD04	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins
ATC	J01DD54	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins
ATC	J01DD63	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins
CHEBI has role	CHEBI:35625	beta-lactamase inhibitors
CHEBI has role	CHEBI:36047	antibacterial drugs
CHEBI has role	CHEBI:88188	allergenic drug
FDA CS	M0003827	Cephalosporins
FDA EPC	N0000175488	Cephalosporin Antibacterial
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000890	Anti-Infective Agents

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

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Disease	Relation	SNOMED_ID	DOID
Gonococcal meningitis	indication	151004
Streptococcal meningitis	indication	4510004	DOID:11574
Septicemia due to Escherichia coli	indication	9323009
Bacterial septicemia	indication	10001005	DOID:0040085
Staphylococcal meningitis	indication	12166008
Gonorrhea	indication	15628003	DOID:7551
Infection of skin AND/OR subcutaneous tissue	indication	19824006
Acute gonococcal cervicitis	indication	20943002	DOID:10615
Staphylococcal pneumonia	indication	22754005
Streptococcal septicemia	indication	29577008

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	2.65	acidic
pKa2	4.17	acidic
pKa3	13.31	acidic
pKa4	3.29	Basic
pKa5	0.93	Basic

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Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D-amino-acid oxidase	Enzyme	P14920	OXDA_HUMAN		IC50	5	CHEMBL
Alpha-synuclein	Transporter	P37840	SYUA_HUMAN		Kd	6.28	CHEMBL
Peptidoglycan synthase FtsI	Enzyme		FTSI_ECOLI	INHIBITOR	IC50	6.14	WOMBAT-PK	CHEMBL
Penicillin-binding protein 1A	Enzyme		PBPA_ECOLI	INHIBITOR	IC50	6.51	WOMBAT-PK	CHEMBL
Penicillin-binding protein 1B	Enzyme		PBPB_ECOLI	INHIBITOR	IC50	5.74	WOMBAT-PK	CHEMBL
Penicillin-binding protein 2	Enzyme		PBP2_ECOLI	INHIBITOR	IC50	6.21	WOMBAT-PK	CHEMBL

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External reference:

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ID	Source
9F2	PDB_CHEM_ID
002734	NDDF
004849	NDDF
104376-79-6	SECONDARY_CAS_RN
1314	MMSL
19841008	SNOMEDCT_US
203172	RXNORM
33440000	SNOMEDCT_US
372670001	SNOMEDCT_US
4017814	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9678	INJECTION, POWDER, FOR SOLUTION	10 g	INTRAVENOUS	ANDA	26 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9678	INJECTION, POWDER, FOR SOLUTION	10 g	INTRAVENOUS	ANDA	26 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9768	INJECTION, POWDER, FOR SOLUTION	10 g	INTRAVENOUS	ANDA	23 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9856	INJECTION, POWDER, FOR SOLUTION	2 g	INTRAMUSCULAR	ANDA	24 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9856	INJECTION, POWDER, FOR SOLUTION	2 g	INTRAMUSCULAR	ANDA	24 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9856	INJECTION, POWDER, FOR SOLUTION	2 g	INTRAMUSCULAR	ANDA	24 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9857	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAMUSCULAR	ANDA	24 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9857	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAMUSCULAR	ANDA	24 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9857	INJECTION, POWDER, FOR SOLUTION	1 g	INTRAMUSCULAR	ANDA	24 sections
Ceftriaxone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9858	INJECTION, POWDER, FOR SOLUTION	500 mg	INTRAMUSCULAR	ANDA	24 sections

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