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

Stem definitionDrug idCAS RN
prostaglandins 138 745-65-3

Description:

MoleculeDescription

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:

DoseUnitRoute
0.50 mg P
20 mcg P
0.25 mg urethral

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
Oct. 16, 1981 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Painful erection 62.24 23.23 12 3383 243 34953293
Device malfunction 59.50 23.23 26 3369 10395 34943141
Protein urine present 57.74 23.23 21 3374 5207 34948329
Device failure 56.37 23.23 17 3378 2359 34951177
Procedural pain 48.25 23.23 18 3377 4788 34948748
Wrong technique in product usage process 42.48 23.23 32 3363 35954 34917582
Blood glucose increased 41.30 23.23 41 3354 66677 34886859
Foreign body in reproductive tract 41.20 23.23 5 3390 0 34953536
Haemoglobin decreased 40.45 23.23 54 3341 120718 34832818
White blood cell count increased 38.68 23.23 32 3363 41119 34912417
Bilirubin conjugated increased 35.59 23.23 13 3382 3258 34950278
Penile burning sensation 34.80 23.23 5 3390 13 34953523
Cytomegalovirus viraemia 34.34 23.23 16 3379 7414 34946122
Harlequin skin reaction 32.96 23.23 4 3391 0 34953536
Complications of transplanted kidney 31.27 23.23 13 3382 4596 34948940
Systolic hypertension 26.50 23.23 6 3389 270 34953266
Kidney transplant rejection 25.22 23.23 13 3382 7484 34946052

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Blood glucose increased 63.49 23.04 48 3613 114927 79625800
Erection increased 59.95 23.04 11 3650 369 79740358
Product quality issue 57.45 23.04 29 3632 33911 79706816
Drug ineffective 57.03 23.04 141 3520 1080772 78659955
Procedural pain 45.85 23.04 22 3639 23062 79717665
Complications of transplanted kidney 44.39 23.04 15 3646 6351 79734376
Kidney transplant rejection 40.93 23.04 16 3645 10230 79730497
Cytomegalovirus viraemia 40.80 23.04 17 3644 12804 79727923
Painful erection 40.49 23.04 7 3654 166 79740561
Gastrointestinal infection 39.20 23.04 16 3645 11445 79729282
Bilirubin conjugated increased 38.42 23.04 13 3648 5526 79735201
Haematotoxicity 34.53 23.04 16 3645 15503 79725224
Penile burning sensation 33.72 23.04 4 3657 3 79740724
Blood albumin decreased 33.25 23.04 18 3643 24225 79716502
Venoocclusive disease 32.77 23.04 11 3650 4562 79736165
Cystitis haemorrhagic 32.03 23.04 13 3648 9159 79731568
Blood triglycerides increased 29.91 23.04 16 3645 21024 79719703
High density lipoprotein decreased 28.68 23.04 10 3651 4645 79736082
Drug reaction with eosinophilia and systemic symptoms 27.24 23.04 23 3638 64221 79676506
Penile haemorrhage 27.00 23.04 6 3655 531 79740196
Systolic hypertension 25.35 23.04 6 3655 702 79740025
Alanine aminotransferase increased 25.12 23.04 34 3627 162536 79578191
Hepatic function abnormal 24.68 23.04 23 3638 73084 79667643
C-reactive protein increased 24.67 23.04 30 3631 128997 79611730
Acute graft versus host disease 24.24 23.04 11 3650 10156 79730571
Delayed graft function 23.42 23.04 8 3653 3499 79737228

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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
FDA CS M0017805 Prostaglandins
FDA MoA N0000000106 Prostaglandin Receptor Agonists
FDA PE N0000009059 Genitourinary Arterial Vasodilation
FDA PE N0000009911 Venous Vasodilation
FDA EPC N0000175454 Prostaglandin Analog
MeSH PA D002317 Cardiovascular Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D064804 Urological Agents
MeSH PA D014665 Vasodilator Agents
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 EPC N0000180189 Prostaglandin E1 Agonist

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

DiseaseRelationSNOMED_IDDOID
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
Peripheral vascular disease off-label use 400047006
Apnea contraindication 1023001
Induratio penis plastica contraindication 1335005 DOID:8616
Priapism contraindication 6273006 DOID:9286
Thrombocytosis contraindication 6631009 DOID:2228
Sickle cell trait contraindication 16402000
Disorder of lung contraindication 19829001 DOID:850
Urethritis contraindication 31822004 DOID:1343
Fibrosis of corpus cavernosum contraindication 32608004
Balanitis contraindication 44882003 DOID:13033
Low blood pressure contraindication 45007003
Respiratory distress syndrome in the newborn contraindication 46775006
Blood coagulation disorder contraindication 64779008 DOID:1247
Urethral stricture contraindication 76618002
Leukemia, disease contraindication 93143009 DOID:1240
Multiple myeloma contraindication 109989006 DOID:9538
Penis implantation contraindication 119996002
Hb SS disease contraindication 127040003 DOID:10923
Erythrocytosis contraindication 127062003
Lymphoid leukemia contraindication 188725004 DOID:1037
Pyloric obstruction contraindication 244815007
Penis bent contraindication 249247007
Deformity of Erection of the Penis contraindication
Hypospadia contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.76 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Prostaglandin E2 receptor EP2 subtype GPCR AGONIST EC50 8 WOMBAT-PK CHEMBL
Prostaglandin E2 receptor EP1 subtype GPCR AGONIST EC50 6.80 WOMBAT-PK CHEMBL
Prostacyclin receptor GPCR EC50 7.50 WOMBAT-PK
Prostaglandin E2 receptor EP4 subtype GPCR AGONIST EC50 8.80 WOMBAT-PK
Prostaglandin D2 receptor GPCR EC50 7.30 WOMBAT-PK
Cation channel sperm-associated protein 1 Ion channel ACTIVATOR EC50 6.30 IUPHAR
Cation channel sperm-associated protein 2 Ion channel ACTIVATOR EC50 6.30 IUPHAR
Cation channel sperm-associated protein 3 Ion channel ACTIVATOR EC50 6.30 IUPHAR
Cation channel sperm-associated protein 4 Ion channel ACTIVATOR EC50 6.30 IUPHAR
Nuclear receptor subfamily 4 group A member 2 Nuclear other EC50 5.52 CHEMBL
Prostaglandin E2 receptor EP3 subtype GPCR AGONIST EC50 9 WOMBAT-PK
Prostaglandin E2 receptor EP1 subtype GPCR Ki 8.22 CHEMBL
Prostaglandin E2 receptor EP2 subtype GPCR Ki 7.66 CHEMBL
Prostaglandin E2 receptor EP3 subtype GPCR Ki 8.30 CHEMBL
Prostaglandin E2 receptor EP4 subtype GPCR Ki 8.51 CHEMBL
Prostaglandin E2 receptor EP2 subtype GPCR AGONIST Ki 8 IUPHAR
Prostaglandin E2 receptor EP4 subtype GPCR AGONIST Ki 9.20 IUPHAR
Prostacyclin receptor GPCR AGONIST Ki 7.50 IUPHAR
Prostaglandin E2 receptor EP3 subtype GPCR AGONIST EC50 9.35 IUPHAR
Prostaglandin E2 receptor EP1 subtype GPCR AGONIST Ki 7 IUPHAR

External reference:

IDSource
4018099 VUID
N0000146437 NUI
D00180 KEGG_DRUG
153020 RXNORM
C0002335 UMLSCUI
CHEBI:15544 CHEBI
XPG PDB_CHEM_ID
CHEMBL495 ChEMBL_ID
DB00770 DRUGBANK_ID
D000527 MESH_DESCRIPTOR_UI
5280723 PUBCHEM_CID
4425 INN_ID
F5TD010360 UNII
d01387 MMSL
109119001 SNOMEDCT_US
48988008 SNOMEDCT_US
4018099 VANDF
10261 MMSL
11600 MMSL
4154 MMSL
000704 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PROSTIN VR PEDIATRIC HUMAN PRESCRIPTION DRUG LABEL 1 0009-0215 INJECTION, SOLUTION 500 ug INTRAVENOUS NDA 17 sections
PROSTIN VR PEDIATRIC HUMAN PRESCRIPTION DRUG LABEL 1 0009-3169 INJECTION, SOLUTION 500 ug INTRAVENOUS NDA 17 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 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 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
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8110 SUPPOSITORY 125 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8110 SUPPOSITORY 125 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8120 SUPPOSITORY 250 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8120 SUPPOSITORY 250 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8130 SUPPOSITORY 500 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8130 SUPPOSITORY 500 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8140 SUPPOSITORY 1000 ug URETHRAL NDA 22 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8140 SUPPOSITORY 1000 ug URETHRAL NDA 22 sections
Alprostadil HUMAN PRESCRIPTION DRUG LABEL 1 0703-1501 INJECTION, SOLUTION, CONCENTRATE 500 ug INTRAVASCULAR ANDA 16 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-010 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 ug INTRACAVERNOUS NDA 23 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-010 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 ug INTRACAVERNOUS NDA 23 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-020 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 ug INTRACAVERNOUS NDA 23 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-020 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 ug INTRACAVERNOUS NDA 23 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-040 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 ug INTRACAVERNOUS NDA 23 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-040 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 ug INTRACAVERNOUS NDA 23 sections
Caverject Impulse HUMAN PRESCRIPTION DRUG LABEL 1 63539-121 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 ug INTRACAVERNOUS NDA 28 sections
Caverject Impulse HUMAN PRESCRIPTION DRUG LABEL 1 63539-221 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 ug INTRACAVERNOUS NDA 28 sections