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

Stem definition	Drug id	CAS RN
prostaglandins	138	745-65-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: alprostadil prostaglandin E1 vasaprostan PGE1 prostavasin	A potent vasodilator agent that increases peripheral blood flow. Molecular weight: 354.49 Formula: C20H34O5 CLOGP: 2.50 LIPINSKI: 0 HAC: 5 HDO: 3 TPSA: 94.83 ALOGS: -3.65 ROTB: 13 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alprostadil
prostaglandin E1
vasaprostan
PGE1
prostavasin

A potent vasodilator agent that increases peripheral blood flow.

Molecular weight: 354.49
Formula: C20H34O5
CLOGP: 2.50
LIPINSKI: 0
HAC: 5
HDO: 3
TPSA: 94.83
ALOGS: -3.65
ROTB: 13

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.50	mg	P
20	mcg	P
0.25	mg	urethral

ADMET properties:

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Property	Value	Reference
CL (Clearance)	45.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	2.40 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	15 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	1.90 hours	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Oct. 16, 1981	FDA	PHARMACIA AND UPJOHN

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
Incision site pain	52.89	35.26	10	1015	1148	63486849
Lymphocyte count decreased	51.21	35.26	19	1006	30238	63457759
Red blood cells urine positive	42.99	35.26	10	1015	3116	63484881
Blood urea increased	42.56	35.26	16	1009	26363	63461634
Capillary leak syndrome	40.89	35.26	9	1016	2191	63485806
Neutrophil count increased	37.87	35.26	13	1012	16514	63471483
Haematotoxicity	36.35	35.26	11	1014	9365	63478632

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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
Drug ineffective	224.18	23.23	245	3150	456506	34497030
Erection increased	148.70	23.23	28	3367	499	34953037
Lymphocyte count decreased	141.13	23.23	60	3335	22562	34930974
Incision site pain	139.59	23.23	33	3362	1805	34951731
Priapism	137.21	23.23	40	3355	4954	34948582
Product quality issue	115.62	23.23	48	3347	16987	34936549
Neutrophil count increased	92.24	23.23	41	3354	17105	34936431
Red blood cells urine positive	89.37	23.23	23	3372	1786	34951750
Penile pain	87.70	23.23	22	3373	1541	34951995
Blood urea increased	72.74	23.23	42	3353	30322	34923214

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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
Incision site pain	206.87	23.04	43	3618	2787	79737940
Lymphocyte count decreased	204.32	23.04	78	3583	47211	79693516
Neutrophil count increased	143.25	23.04	53	3608	29343	79711384
Blood urea increased	126.90	23.04	56	3605	48734	79691993
Red blood cells urine positive	126.60	23.04	32	3629	4931	79735796
Priapism	119.64	23.04	30	3631	4475	79736252
Haemoglobin decreased	91.53	23.04	78	3583	222041	79518686
Protein urine present	87.36	23.04	28	3633	10084	79730643
Penile pain	83.44	23.04	17	3644	994	79739733
White blood cell count increased	79.76	23.04	47	3614	74586	79666141

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01EA01	CARDIOVASCULAR SYSTEM CARDIAC THERAPY OTHER CARDIAC PREPARATIONS Prostaglandins
ATC	G04BE01	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs used in erectile dysfunction
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:50249	anticoagulants
CHEBI has role	CHEBI:50427	platelet aggregation inhibitors
CHEBI has role	CHEBI:77746	Homo sapiens metabolite
FDA CS	M0017805	Prostaglandins
FDA EPC	N0000175454	Prostaglandin Analog
FDA EPC	N0000180189	Prostaglandin E1 Agonist
FDA MoA	N0000000106	Prostaglandin Receptor Agonists

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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
Coarctation of aorta	indication	7305005
Congenital atresia of tricuspid valve	indication	63042009
Tetralogy of Fallot	indication	86299006	DOID:6419
Pulmonary artery stenosis	indication	95441000
Congenital atresia of the pulmonary valve	indication	204342004
Ebstein's anomaly of tricuspid valve	indication	204357006	DOID:14289
Impotence	indication	397803000
Aorta Dextratransposition with Intact Ventricular Septum	indication
Congenital Heart Defect Requiring Open Patent Ductus Arteriosus	indication
Pulmonary hypertension	off-label use	70995007	DOID:6432

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.76	acidic

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
Prostaglandin E2 receptor EP2 subtype	GPCR	P43116	PE2R2_HUMAN	AGONIST	EC50	8	WOMBAT-PK	CHEMBL
Prostaglandin E2 receptor EP1 subtype	GPCR	P34995	PE2R1_HUMAN	AGONIST	EC50	6.80	WOMBAT-PK	CHEMBL
Prostacyclin receptor	GPCR	P43119	PI2R_HUMAN		EC50	7.50	WOMBAT-PK
Prostaglandin E2 receptor EP4 subtype	GPCR	P35408	PE2R4_HUMAN	AGONIST	EC50	8.80	WOMBAT-PK
Prostaglandin D2 receptor	GPCR	Q13258	PD2R_HUMAN		EC50	7.30	WOMBAT-PK
Cation channel sperm-associated protein 1	Ion channel	Q8NEC5	CTSR1_HUMAN	ACTIVATOR	EC50	6.30	IUPHAR
Cation channel sperm-associated protein 2	Ion channel	Q96P56	CTSR2_HUMAN	ACTIVATOR	EC50	6.30	IUPHAR
Cation channel sperm-associated protein 3	Ion channel	Q86XQ3	CTSR3_HUMAN	ACTIVATOR	EC50	6.30	IUPHAR
Cation channel sperm-associated protein 4	Ion channel	Q7RTX7	CTSR4_HUMAN	ACTIVATOR	EC50	6.30	IUPHAR
Nuclear receptor subfamily 4 group A member 2	Nuclear other	P43354	NR4A2_HUMAN		EC50	5.52	CHEMBL

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External reference:

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ID	Source
XPG	PDB_CHEM_ID
000704	NDDF
10261	MMSL
109119001	SNOMEDCT_US
11600	MMSL
153020	RXNORM
4018099	VUID
4018099	VANDF
4154	MMSL
4425	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Alprostadil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-1501	INJECTION, SOLUTION, CONCENTRATE	500 ug	INTRAVASCULAR	ANDA	16 sections
Caverject	HUMAN PRESCRIPTION DRUG LABEL	1	0009-3701	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20.50 ug	INTRACAVERNOUS	NDA	27 sections
Caverject	HUMAN PRESCRIPTION DRUG LABEL	1	0009-3701	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20.50 ug	INTRACAVERNOUS	NDA	27 sections
Caverject	HUMAN PRESCRIPTION DRUG LABEL	1	0009-7686	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	41.10 ug	INTRACAVERNOUS	NDA	27 sections
Caverject	HUMAN PRESCRIPTION DRUG LABEL	1	0009-7686	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	41.10 ug	INTRACAVERNOUS	NDA	27 sections
Caverject Impulse	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5181	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 ug	INTRACAVERNOUS	NDA	28 sections
Caverject Impulse	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5181	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 ug	INTRACAVERNOUS	NDA	28 sections
Caverject Impulse	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5182	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20 ug	INTRACAVERNOUS	NDA	28 sections
Caverject Impulse	HUMAN PRESCRIPTION DRUG LABEL	1	0009-5182	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	20 ug	INTRACAVERNOUS	NDA	28 sections
Caverject Impulse	HUMAN PRESCRIPTION DRUG LABEL	1	63539-121	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 ug	INTRACAVERNOUS	NDA	28 sections

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