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

Stem definition	Drug id	CAS RN
anti-infectives, sulfonamides	2500	68-35-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sulfadiazine sodium sulfadiazine sulfadiazin sulfapyrimidine sulfazine sulphadiazine	One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections. Molecular weight: 250.28 Formula: C10H10N4O2S CLOGP: 0.10 LIPINSKI: 0 HAC: 6 HDO: 2 TPSA: 97.97 ALOGS: -2.62 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sulfadiazine sodium
sulfadiazine
sulfadiazin
sulfapyrimidine
sulfazine
sulphadiazine

One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.

Molecular weight: 250.28
Formula: C10H10N4O2S
CLOGP: 0.10
LIPINSKI: 0
HAC: 6
HDO: 2
TPSA: 97.97
ALOGS: -2.62
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.60	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	7 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	684.95 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	57 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	0.55 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.44 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.29 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.13 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 11, 1941	FDA	LEDERLE

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
Lipase increased	215.61	31.56	50	1564	9850	63477558
Drug hypersensitivity	196.36	31.56	112	1502	310575	63176833
Pancreatitis	140.29	31.56	51	1563	49004	63438404
Drug reaction with eosinophilia and systemic symptoms	92.22	31.56	34	1580	33802	63453606
Pancytopenia	58.01	31.56	34	1580	96899	63390509
Pneumonia aspiration	43.51	31.56	20	1594	34520	63452888
Astigmatism	43.29	31.56	9	1605	1058	63486350
Bone marrow failure	40.17	31.56	18	1596	29272	63458136
Coma	39.57	31.56	23	1591	64341	63423067
Hepatocellular injury	38.10	31.56	17	1597	27364	63460044

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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
Toxic epidermal necrolysis	88.52	27.34	34	1520	21612	34933765
Cerebral toxoplasmosis	43.77	27.34	11	1543	1710	34953667
Stevens-Johnson syndrome	41.45	27.34	19	1535	18620	34936757
Pulmonary venous thrombosis	35.20	27.34	6	1548	135	34955242
Pulmonary vasculitis	32.04	27.34	7	1547	592	34954785
Central pain syndrome	31.58	27.34	5	1549	70	34955307
Drug hypersensitivity	31.31	27.34	27	1527	80502	34874875
Neuritis	28.95	27.34	7	1547	927	34954450
Electric shock	27.82	27.34	5	1549	154	34955223

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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	95.11	25.16	46	2766	64198	79677378
Toxic epidermal necrolysis	75.38	25.16	35	2777	44546	79697030
Pancytopenia	74.58	25.16	55	2757	165690	79575886
Cerebral toxoplasmosis	73.55	25.16	17	2795	2345	79739231
Drug hypersensitivity	46.76	25.16	55	2757	298861	79442715
Astigmatism	39.38	25.16	9	2803	1180	79740396
Pulmonary venous thrombosis	35.90	25.16	6	2806	152	79741424
Pulmonary vasculitis	31.98	25.16	7	2805	754	79740822
Hepatocellular injury	31.30	25.16	20	2792	47573	79694003
Infection protozoal	30.38	25.16	4	2808	17	79741559

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J01EC02	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Intermediate-acting sulfonamides
ATC	J01EE02	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Combinations of sulfonamides and trimethoprim, incl. derivatives
ATC	J01EE06	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE SULFONAMIDES AND TRIMETHOPRIM Combinations of sulfonamides and trimethoprim, incl. derivatives
CHEBI has role	CHEBI:33281	antibiotics
CHEBI has role	CHEBI:35441	antiinfective agents
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:35818	coccidiostats
CHEBI has role	CHEBI:35820	antiprotozoal drugs
CHEBI has role	CHEBI:50502	dihydropteroate synthase inhibitors
CHEBI has role	CHEBI:74234	sepiapterin reductase inhibitors

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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
Chorioretinitis	indication	46627006	DOID:8886
Skin ulcer	indication	46742003
Ulcerative colitis	indication	64766004	DOID:8577
Congenital toxoplasmosis	indication	73893000	DOID:13336
Toxoplasmosis	indication	187192000	DOID:9965
Toxoplasmosis associated with acquired immunodeficiency syndrome	indication	421666009
Rheumatic Fever Prevention	indication
Burn Wound Infections	indication
Encephalitis due to Toxoplasmosis	indication
Minor Bacterial Skin Infections	indication

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🐶 Veterinary Drug Use

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Species	Use	Relation
Dogs	Systemic antibacterial action against sensitive organisms to surgery	Indication
Dogs	Systemic antibacterial action against sensitive organisms to debridement	Indication
Dogs	Control of bacterial infection during the treatment of acute urinary tract infections	Indication
Dogs	Control of bacterial infection during the treatment of acute bacterial complications of distemper	Indication
Dogs	Control of bacterial infection during the treatment of acute respiratory tract infections	Indication
Dogs	Control of bacterial infection during the treatment of acute alimentary tract infections	Indication
Dogs	Control of bacterial infection during the treatment of wound infections	Indication
Dogs	Control of bacterial infection during the treatment of abscesses	Indication
Horses	Systemic antibacterial action against sensitive organisms during treatment of acute strangles	Indication
Horses	Systemic antibacterial action against sensitive organisms during respiratory infections	Indication

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🐶 Veterinary products

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Product	Applicant	Ingredients
Di-Trim 24%	Zoetis Inc.	2
Di-Trim 400 Paste	Zoetis Inc.	2
Di-Trim 48% Injection	Zoetis Inc.	2
Di-Trim Tablets	Zoetis Inc.	2
EQUISUL-SDT	Aurora Pharmaceutical Inc.	2
ReBalance	Pegasus Laboratories Inc.	2
Tribrissen 120 Tablets, Tribrissen 30 Tablets, Tribrissen 480 Tablets, Tribrissen 960 Tablets	Intervet Inc.	2
Tribrissen 24% Injection	Intervet Inc.	2
Tribrissen 400 Oral Paste	Intervet Inc.	2
Tribrissen 48% Injection	Intervet Inc.	2

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.6	acidic
pKa2	2.03	Basic
pKa3	1.41	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		IC50	6.03	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		IC50	4.96	WOMBAT-PK
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		IC50	4.68	CHEMBL
High affinity choline transporter 1	Transporter	Q9GZV3	SC5A7_HUMAN		IC50	4.24	WOMBAT-PK
Dihydropteroate synthase	Enzyme		DHPS_ECOLI	INHIBITOR			CHEMBL	CHEMBL
Dihydroorotate dehydrogenase (quinone), mitochondrial	Enzyme		PYRD_PLAF7				WOMBAT-PK

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External reference:

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ID	Source
002814	NDDF
014626	NDDF
0N7609K889	UNII
10171	RXNORM
12635	IUPHAR_LIGAND_ID
13920	MMSL
2022	MMSL
371400009	SNOMEDCT_US
4017497	VANDF
421	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Sulfadiazine	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0757	TABLET	500 mg	ORAL	ANDA	18 sections
SULFADIAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	42806-757	TABLET	500 mg	ORAL	ANDA	19 sections

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