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

Stem definitionDrug idCAS RN
spasmolytics with a papaverine-like action 2056 58-74-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • papaverine
  • papaverine hydrochloride
  • papaverin
  • papaverine HCl
An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.
  • Molecular weight: 339.39
  • Formula: C20H21NO4
  • CLOGP: 3.58
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 49.81
  • ALOGS: -4.42
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.10 g O
0.10 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 25.26 µM/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
S (Water solubility) 50 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
None FDA

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
Creatinine renal clearance decreased 78.78 46.22 21 702 16287 63472012
Sedation complication 77.33 46.22 20 703 13802 63474497
Blood calcium decreased 68.73 46.22 21 702 26430 63461869
Orthostatic hypotension 62.28 46.22 21 702 36139 63452160
Hypotension 61.15 46.22 38 685 272566 63215733
Drug abuse 58.07 46.22 24 699 72494 63415805
Sedation 56.96 46.22 20 703 38789 63449510
Cognitive disorder 53.38 46.22 21 702 55794 63432505
Depressed level of consciousness 47.82 46.22 20 703 62058 63426241

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
Toxicity to various agents 308.05 75.53 111 399 200251 34756170
Drug abuse 142.04 75.53 53 457 99043 34857378

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
Toxicity to various agents 241.69 49.70 120 1111 421420 79321737
Drug abuse 177.56 49.70 73 1158 162618 79580539
Creatinine renal clearance decreased 69.16 49.70 21 1210 18981 79724176
Sedation complication 68.70 49.70 20 1211 15649 79727508
Depressed level of consciousness 64.90 49.70 31 1200 96621 79646536
Alcohol interaction 64.59 49.70 15 1216 4859 79738298
Blood calcium decreased 58.53 49.70 21 1210 31798 79711359
Overdose 51.12 49.70 33 1198 184173 79558984

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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

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

DiseaseRelationSNOMED_IDDOID
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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.36 Basic

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
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

External reference:

IDSource
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 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 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 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
Papaverine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 72516-024 INJECTION, SOLUTION 30 mg INTRAVENOUS UNAPPROVED DRUG OTHER 16 sections