Stem definition | Drug id | CAS RN |
---|---|---|
spasmolytics with a papaverine-like action | 2056 | 58-74-2 |
Dose | Unit | Route |
---|---|---|
0.10 | g | O |
0.10 | g | P |
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 25.26 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 28 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 1 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 11 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.07 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 1.80 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
None | FDA |
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 |
---|---|---|---|---|---|---|
Hypotension | 49.44 | 44.16 | 30 | 499 | 250478 | 56041060 |
Sedation complication | 49.34 | 44.16 | 13 | 516 | 11659 | 56279879 |
Creatinine renal clearance decreased | 46.50 | 44.16 | 13 | 516 | 14546 | 56276992 |
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 |
---|---|---|---|---|---|---|
Toxicity to various agents | 248.23 | 67.65 | 91 | 346 | 181396 | 31515511 |
Drug abuse | 88.79 | 67.65 | 36 | 401 | 87722 | 31609185 |
Alcohol interaction | 74.79 | 67.65 | 15 | 422 | 2774 | 31694133 |
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 |
---|---|---|---|---|---|---|
Toxicity to various agents | 186.01 | 42.91 | 94 | 887 | 382078 | 70545385 |
Drug abuse | 103.61 | 42.91 | 47 | 934 | 147209 | 70780254 |
Alcohol interaction | 66.95 | 42.91 | 15 | 966 | 4638 | 70922825 |
None
Source | Code | Description |
---|---|---|
ATC | A03AD01 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS Papaverine and derivatives |
ATC | G04BE02 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs used in erectile dysfunction |
ATC | G04BE52 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs used in erectile dysfunction |
MeSH PA | D002317 | Cardiovascular Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D010726 | Phosphodiesterase Inhibitors |
MeSH PA | D064804 | Urological Agents |
MeSH PA | D014665 | Vasodilator Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Cerebral ischemia | indication | 287731003 | |
Peripheral vascular disease | indication | 400047006 | |
Sinus tachycardia | contraindication | 11092001 | |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Glaucoma | contraindication | 23986001 | DOID:1686 |
Complete atrioventricular block | contraindication | 27885002 | |
Conduction disorder of the heart | contraindication | 44808001 | |
Low blood pressure | contraindication | 45007003 | |
Angina pectoris | contraindication | 194828000 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Chronic myocardial ischemia | contraindication | 413844008 | DOID:3393 |
Disorder of coronary artery | contraindication | 414024009 | |
Cardiac Conduction Delay | contraindication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 6.36 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.14 | CHEMBL | |||||
cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Enzyme | Ki | 6.55 | CHEMBL | |||||
cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Enzyme | WOMBAT-PK | |||||||
Acetylcholinesterase | Enzyme | IC50 | 4.61 | CHEMBL | |||||
cGMP-specific 3',5'-cyclic phosphodiesterase | Enzyme | IC50 | 5.06 | CHEMBL | |||||
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A | Enzyme | IC50 | 7.77 | CHEMBL | |||||
Cytochrome P450 2C19 | Enzyme | IC50 | 6.12 | DRUG MATRIX | |||||
cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Enzyme | IC50 | 6.09 | DRUG MATRIX | |||||
cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Enzyme | IC50 | 5.85 | CHEMBL | |||||
cGMP-dependent 3',5'-cyclic phosphodiesterase | Enzyme | IC50 | 5.64 | CHEMBL | |||||
cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Enzyme | Ki | 6.38 | CHEMBL | |||||
Protein-arginine deiminase type-4 | Enzyme | IC50 | 4.41 | CHEMBL | |||||
Phosphodiesterase 1 | Enzyme | IC50 | 5.05 | CHEMBL | |||||
Serine hydroxymethyltransferase, mitochondrial | Enzyme | IC50 | 5.57 | CHEMBL | |||||
Acetylcholinesterase | Enzyme | IC50 | 4.61 | CHEMBL | |||||
Cyclic nucleotide phosphodiesterase PDE3A | Enzyme | IC50 | 6.21 | CHEMBL | |||||
Cyclic AMP-specific phosphodiesterase SSPDE4A1A | Enzyme | IC50 | 5.77 | CHEMBL | |||||
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A | Enzyme | IC50 | 7.44 | CHEMBL | |||||
Phosphodiesterase 1 | Enzyme | IC50 | 5.06 | CHEMBL | |||||
Phosphodiesterase 1 | Enzyme | IC50 | 4.92 | CHEMBL |
ID | Source |
---|---|
4019875 | VUID |
N0000147960 | NUI |
D02218 | KEGG_DRUG |
61-25-6 | SECONDARY_CAS_RN |
4017430 | VANDF |
4019875 | VANDF |
C0030350 | UMLSCUI |
EV1 | PDB_CHEM_ID |
CHEMBL19224 | ChEMBL_ID |
DB01113 | DRUGBANK_ID |
CHEMBL98123 | ChEMBL_ID |
D010208 | MESH_DESCRIPTOR_UI |
4680 | PUBCHEM_CID |
DAA13NKG2Q | UNII |
203132 | RXNORM |
4553 | MMSL |
5230 | MMSL |
d00695 | MMSL |
000694 | NDDF |
004522 | NDDF |
372784001 | SNOMEDCT_US |
40404004 | SNOMEDCT_US |
58467001 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Papaverine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-4002 | INJECTION, SOLUTION | 30 mg | INTRAVENOUS | UNAPPROVED DRUG OTHER | 16 sections |
Papaverine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 14789-121 | INJECTION | 30 mg | INTRAVENOUS | unapproved drug other | 16 sections |
PAPAVERINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54288-142 | INJECTION, SOLUTION | 30 mg | PARENTERAL | unapproved drug other | 16 sections |
Papaverine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72516-024 | INJECTION, SOLUTION | 30 mg | INTRAVENOUS | UNAPPROVED DRUG OTHER | 16 sections |