alprostadil indications/contra

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

Drug dosage:

DoseUnitRoute
0.50 mg P
20 mcg P
0.25 mg urethral

Approvals:

DateAgencyCompanyOrphan
Oct. 16, 1981 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System

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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 606.51 44.00 184 407 115906 3269362
Priapism 155.61 44.00 27 564 1202 3384066
Erection increased 139.74 44.00 20 571 246 3385022
Product quality issue 128.26 44.00 41 550 26694 3358574
Device malfunction 115.27 44.00 26 565 4458 3380810
Penile pain 91.99 44.00 15 576 452 3384816
Device failure 83.56 44.00 18 573 2483 3382785
Painful erection 64.15 44.00 9 582 94 3385174
Erectile dysfunction 54.47 44.00 14 577 4113 3381155
Wrong technique in product usage process 53.46 44.00 19 572 16732 3368536
Infantile cortical hyperostosis 47.81 44.00 5 586 0 3385268

Pharmacologic Action:

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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 PE N0000009059 Genitourinary Arterial Vasodilation
FDA EPC N0000175454 Prostaglandin Analog
FDA EPC N0000180189 Prostaglandin E1 Agonist
FDA MoA N0000000106 Prostaglandin Receptor Agonists
FDA Chemical/Ingredient N0000007706 Prostaglandins
FDA PE N0000009911 Venous Vasodilation
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 agent
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:50249 anticoagulant

Drug Use (View source of the data)

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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
Congenital Heart Defect Requiring Open Patent Ductus Arteriosus indication
Aorta Dextratransposition with Intact Ventricular Septum indication
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 DOID:12716
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 DOID:8432
Lymphoid leukemia contraindication 188725004 DOID:1037
Pyloric obstruction contraindication 244815007 DOID:3122
Penis bent contraindication 249247007
Hypospadia contraindication
Deformity of Erection of the Penis contraindication
Pulmonary hypertension off-label use 70995007 DOID:6432
Peripheral vascular disease off-label use 400047006

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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
Cation channel sperm-associated protein 4 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 1 Ion channel ACTIVATOR EC50 6.30 IUPHAR
Cation channel sperm-associated protein 2 Ion channel ACTIVATOR EC50 6.30 IUPHAR
Prostaglandin E2 receptor EP4 subtype GPCR AGONIST EC50 8.80 WOMBAT-PK
Prostaglandin E2 receptor EP3 subtype GPCR AGONIST EC50 9 WOMBAT-PK
Prostaglandin D2 receptor GPCR EC50 7.30 WOMBAT-PK
Prostacyclin receptor GPCR EC50 7.50 WOMBAT-PK
Prostacyclin receptor Unclassified AGONIST Ki 7.50 IUPHAR
Prostaglandin E2 receptor EP1 subtype Unclassified AGONIST Ki 7 IUPHAR
Prostaglandin E2 receptor EP2 subtype GPCR AGONIST Ki 8 IUPHAR
Prostaglandin E2 receptor EP2 subtype GPCR Ki 7.66 CHEMBL
Prostaglandin E2 receptor EP1 subtype GPCR Ki 8.22 CHEMBL
Prostaglandin E2 receptor EP3 subtype GPCR Ki 8.30 CHEMBL
Prostaglandin E2 receptor EP3 subtype Unclassified AGONIST Ki 9 IUPHAR
Prostaglandin E2 receptor EP4 subtype GPCR Ki 8.51 CHEMBL
Prostaglandin E2 receptor EP4 subtype GPCR AGONIST Ki 9.20 IUPHAR

External reference:

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IDSource
4018099 VUID
N0000146437 NUI
C0002335 UMLSCUI
1882 IUPHAR_LIGAND_ID
D00180 KEGG_DRUG
CHEMBL495 ChEMBL_ID
DB00770 DRUGBANK_ID
11600 MMSL
598 RXNORM
109119001 SNOMEDCT_US
4154 MMSL
d01387 MMSL
48988008 SNOMEDCT_US
4018099 VANDF
N0000146437 NDFRT
N0000006614 NDFRT
000704 NDDF
5280723 PUBCHEM_CID
F5TD010360 UNII
4425 INN_ID
D000527 MESH_DESCRIPTOR_UI
CHEBI:15544 CHEBI
XPG PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
PROSTIN HUMAN PRESCRIPTION DRUG LABEL 1 0009-3169 INJECTION, SOLUTION 500 ug INTRAVENOUS NDA 13 sections
Caverject HUMAN PRESCRIPTION DRUG LABEL 1 0009-3701 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20.50 ug INTRACAVERNOUS NDA 19 sections
Caverject Impulse HUMAN PRESCRIPTION DRUG LABEL 1 0009-5181 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 ug INTRACAVERNOUS NDA 20 sections
Caverject Impulse HUMAN PRESCRIPTION DRUG LABEL 1 0009-5182 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 ug INTRACAVERNOUS NDA 20 sections
Caverject HUMAN PRESCRIPTION DRUG LABEL 1 0009-7686 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 41.10 ug INTRACAVERNOUS NDA 19 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8110 SUPPOSITORY 125 ug URETHRAL NDA 14 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8120 SUPPOSITORY 250 ug URETHRAL NDA 14 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8130 SUPPOSITORY 500 ug URETHRAL NDA 14 sections
MUSE HUMAN PRESCRIPTION DRUG LABEL 1 0037-8140 SUPPOSITORY 1000 ug URETHRAL NDA 14 sections
Alprostadil HUMAN PRESCRIPTION DRUG LABEL 1 0703-1501 INJECTION, SOLUTION, CONCENTRATE 500 ug INTRAVASCULAR ANDA 12 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-010 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 ug INTRACAVERNOUS NDA 13 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-020 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 ug INTRACAVERNOUS NDA 13 sections
Edex HUMAN PRESCRIPTION DRUG LABEL 1 52244-040 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 40 ug INTRACAVERNOUS NDA 13 sections
Caverject Impulse HUMAN PRESCRIPTION DRUG LABEL 1 63539-121 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 ug INTRACAVERNOUS NDA 20 sections
Caverject Impulse HUMAN PRESCRIPTION DRUG LABEL 1 63539-221 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 ug INTRACAVERNOUS NDA 20 sections