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

Stem definition	Drug id	CAS RN
vasoconstrictors, vasopressin derivatives	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: -3.82 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:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI

Approvals:

Date	Agency	Company	Orphan
None	FDA	PARKE DAVIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

Source	Code	Description
MeSH PA	D050034	Antidiuretic Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D003029	Coagulants
MeSH PA	D006401	Hematologic Agents
MeSH PA	D006490	Hemostatics
MeSH PA	D045283	Natriuretic Agents
MeSH PA	D014662	Vasoconstrictor Agents

Drug Use (View source of the data)

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
Heart failure	contraindication	84114007	DOID:6000
Epilepsy	contraindication	84757009	DOID:1826
Asthma	contraindication	195967001	DOID:2841
Disorder of coronary artery	contraindication	414024009

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

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/ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 17, 2014	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
20UNITS/ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 17, 2014	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
20UNITS/ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 17, 2014	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
20UNITS/ML (20UNITS/ML)	VASOSTRICT	PAR STERILE PRODUCTS	N204485	April 17, 2014	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

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
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
Vasopressin V1a receptor	GPCR	P37288	V1AR_HUMAN	AGONIST	Ki	9.59		CHEMBL	CHEMBL
Oxytocin receptor	GPCR	P30559	OXYR_HUMAN		Ki	8.78		CHEMBL
Vasopressin V2 receptor	GPCR		V2R_BOVIN		Kd	8.82		CHEMBL
Vasopressin V1b receptor	GPCR		V1BR_RAT		Ki	9.54		CHEMBL
Vasopressin V1a receptor	GPCR		V1AR_RAT		Kd	9.19		CHEMBL
Vasopressin V1 receptor	GPCR		V1AR_RAT V1BR_RAT		Kd	9.19		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

External reference:

ID	Source
4018654	VUID
N0000179795	NUI
C1705480	UMLSCUI
D00101	KEGG_DRUG
4R069M4O1P	UNII
77671006	SNOMEDCT_US
772208008	SNOMEDCT_US
4018654	VANDF
11149	RXNORM
3144	MMSL
5667	MMSL
d00398	MMSL
002126	NDDF
002122	NDDF
CHEMBL373742	ChEMBL_ID
DB00067	DRUGBANK_ID
CHEBI:9937	CHEBI
1482	INN_ID
CHEMBL1201528	ChEMBL_ID
CHEMBL2108986	ChEMBL_ID
644077	PUBCHEM_CID
2168	IUPHAR_LIGAND_ID
C016671	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
VASOPRESSIN	HUMAN PRESCRIPTION DRUG LABEL	1	52584-302	INJECTION, SOLUTION	20 [USP'U]	INTRAMUSCULAR	unapproved drug other	10 sections
Vasopressin	HUMAN PRESCRIPTION DRUG LABEL	1	63323-302	INJECTION, SOLUTION	20 [USP'U]	INTRAMUSCULAR	unapproved drug other	11 sections