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

Stem definition	Drug id	CAS RN
vasopressin analogues	2810	113-79-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: vasopressin 8-L-arginine vasopressin synthetic vasopressin 8-L-Arginine-vasopressin argipressin vasopressin tannate vasopressin injection antidiuretic hormone pitressin tannate	Molecular weight: 1084.24 Formula: C46H65N15O12S2 CLOGP: -2.31 LIPINSKI: 3 HAC: 27 HDO: 15 TPSA: 461.43 ALOGS: -3.93 ROTB: 19 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

vasopressin
8-L-arginine vasopressin
synthetic vasopressin
8-L-Arginine-vasopressin
argipressin
vasopressin tannate
vasopressin injection
antidiuretic hormone
pitressin tannate

Molecular weight: 1084.24
Formula: C46H65N15O12S2
CLOGP: -2.31
LIPINSKI: 3
HAC: 27
HDO: 15
TPSA: 461.43
ALOGS: -3.93
ROTB: 19

Status: OFP

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

Drug dosage:

Dose	Unit	Route
40	U	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	2 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
None	FDA	PARKE DAVIS

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 ineffective	228.51	39.35	323	4272	1044442	62439985
Metabolic acidosis	170.29	39.35	77	4518	44992	63439435
Hypotension	141.94	39.35	133	4462	272471	63211956
Intentional overdose	139.41	39.35	79	4516	74073	63410354
Cardiac arrest	123.22	39.35	79	4516	92466	63391961
Shock	121.08	39.35	50	4545	23413	63461014
Multiple organ dysfunction syndrome	105.34	39.35	60	4535	56692	63427735
Acute kidney injury	99.24	39.35	108	4487	263307	63221120
Cardiogenic shock	98.59	39.35	40	4555	17892	63466535
Lactic acidosis	97.66	39.35	50	4545	38237	63446190

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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
Appendicolith	468.24	37.09	141	7647	8460	34940683
Cardiogenic shock	438.78	37.09	179	7609	26439	34922704
Multiple organ dysfunction syndrome	406.85	37.09	237	7551	76329	34872814
Appendicitis	393.01	37.09	141	7647	14666	34934477
Stress	354.52	37.09	160	7628	30187	34918956
Drug ineffective	267.95	37.09	409	7379	456342	34492801
Ascites	256.95	37.09	148	7640	46423	34902720
Ventricular fibrillation	236.45	37.09	111	7677	22843	34926300
Abdominal distension	228.28	37.09	149	7639	58343	34890800
Hyponatraemia	190.47	37.09	153	7635	82538	34866605

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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
Cardiogenic shock	542.24	28.84	214	12139	41700	79690335
Appendicolith	514.58	28.84	140	12213	8411	79723624
Multiple organ dysfunction syndrome	497.54	28.84	279	12074	119967	79612068
Drug ineffective	468.81	28.84	692	11661	1080221	78651814
Appendicitis	392.05	28.84	140	12213	20654	79711381
Ventricular fibrillation	268.16	28.84	120	12233	31806	79700229
Stress	265.87	28.84	161	12192	79451	79652584
Ascites	252.79	28.84	153	12200	75409	79656626
Sepsis	224.93	28.84	241	12112	269187	79462848
Diabetes insipidus	199.17	28.84	60	12293	5177	79726858

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	H01BA01	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES POSTERIOR PITUITARY LOBE HORMONES Vasopressin and analogues
CHEBI has role	CHEBI:35554	cardiovascular agent
CHEBI has role	CHEBI:50248	hematologic agents
CHEBI has role	CHEBI:52290	mitogens
FDA CS	M0022562	Vasopressins
FDA PE	N0000009908	Vasoconstriction
FDA PE	N0000175360	Decreased Diuresis
MeSH PA	D050034	Antidiuretic Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D003029	Coagulants

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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
Nocturnal enuresis	indication	8009008
Hereditary factor VIII deficiency disease	indication	28293008	DOID:12134
von Willebrand disorder	indication	128105004	DOID:12531
Partial Central Diabetes Insipidus	indication
Cardiac arrest	off-label use	410429000	DOID:0060319
Uremic Bleeding Tendency	off-label use
Chronic glomerulonephritis	contraindication	20917003
Migraine	contraindication	37796009	DOID:6364
Hypertensive disorder	contraindication	38341003	DOID:10763
Uremia	contraindication	44730006	DOID:4676

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.65	acidic
pKa2	12.19	acidic
pKa3	12.56	acidic
pKa4	12.85	acidic
pKa5	13.19	acidic
pKa6	13.43	acidic
pKa7	13.76	acidic
pKa8	10.75	Basic
pKa9	6.4	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
200UNITS/10ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	Dec. 17, 2016	RX	SOLUTION	INTRAVENOUS	9375478	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	Dec. 17, 2016	RX	SOLUTION	INTRAVENOUS	9687526	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	Dec. 17, 2016	RX	SOLUTION	INTRAVENOUS	9744209	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	Dec. 17, 2016	RX	SOLUTION	INTRAVENOUS	9744239	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
200UNITS/10ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	Dec. 17, 2016	RX	SOLUTION	INTRAVENOUS	9937223	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/100ML (0.2UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 21, 2021	RX	SOLUTION	INTRAVENOUS	10010575	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/100ML (0.2UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 21, 2021	RX	SOLUTION	INTRAVENOUS	9925233	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/100ML (0.2UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 21, 2021	RX	SOLUTION	INTRAVENOUS	9925234	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/100ML (0.2UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 21, 2021	RX	SOLUTION	INTRAVENOUS	9962422	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES
20UNITS/100ML (0.2UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 21, 2021	RX	SOLUTION	INTRAVENOUS	9968649	Jan. 30, 2035	TO INCREASE BLOOD PRESSURE IN ADULTS WITH VASODILATORY SHOCK (E.G., POST-CARDIOTOMY OR SEPSIS) WHO REMAIN HYPOTENSIVE DESPITE FLUIDS AND CATECHOLAMINES

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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
Vasopressin V1a receptor	GPCR	P37288	V1AR_HUMAN	AGONIST	Ki	9.59	CHEMBL	CHEMBL
Vasopressin V1b receptor	GPCR	P47901	V1BR_HUMAN	AGONIST	Ki	9.31	CHEMBL	CHEMBL
Vasopressin V2 receptor	GPCR	P30518	V2R_HUMAN	AGONIST	Ki	8.92	CHEMBL	CHEMBL
Oxytocin receptor	GPCR	P30559	OXYR_HUMAN		Ki	8.78	CHEMBL
Vasopressin V2 receptor	GPCR		V2R_PIG		IC50	8.48	CHEMBL
Oxytocin receptor	GPCR		OXYR_RAT		Ki	8.93	CHEMBL
Vasopressin V2 receptor	GPCR		V2R_RAT		Ki	9.35	CHEMBL
Vasopressin V2 receptor	GPCR		V2R_BOVIN		Kd	8.82	CHEMBL
Vasopressin V1a receptor	GPCR		V1AR_RAT		Kd	9.19	CHEMBL
Vasopressin V1b receptor	GPCR		V1BR_RAT		Ki	9.54	CHEMBL

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External reference:

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ID	Source
002122	NDDF
002123	NDDF
002126	NDDF
005438	NDDF
005439	NDDF
1098	RXNORM
126192003	SNOMEDCT_US
2168	IUPHAR_LIGAND_ID
3144	MMSL
4018654	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	0517-1020	INJECTION, SOLUTION	20 [USPU]	INTRAVENOUS	NDA	25 sections
Vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	0517-1020	INJECTION, SOLUTION	20 [USPU]	INTRAVENOUS	NDA	25 sections
Vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	0517-1020	INJECTION, SOLUTION	20 [USPU]	INTRAVENOUS	NDA	25 sections
Vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	0517-1030	INJECTION, SOLUTION	20 [USPU]	INTRAVENOUS	NDA	25 sections
Vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	0548-9701	INJECTION	20 [USPU]	INTRAVENOUS	ANDA	24 sections
VASOPRESSIN	HUMAN PRESCRIPTION DRUG LABEL	1	42367-570	INJECTION	20 U	PARENTERAL	ANDA	24 sections
VASOPRESSIN	HUMAN PRESCRIPTION DRUG LABEL	1	42367-570	INJECTION	20 U	PARENTERAL	ANDA	24 sections
VASOPRESSIN	HUMAN PRESCRIPTION DRUG LABEL	1	63323-930	INJECTION, SOLUTION	20 [USPU]	INTRAVENOUS	ANDA	25 sections
VASOPRESSIN	HUMAN PRESCRIPTION DRUG LABEL	1	65219-039	INJECTION, SOLUTION	20 [USPU]	INTRAVENOUS	ANDA	25 sections
vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	70121-1642	INJECTION	20 [USPU]	INTRAVENOUS	ANDA	20 sections

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