capsaicin Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
3064 404-86-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • capsaicin
  • capsaicine
  • qutenza
  • NGX-4010
  • NGX 4010
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
  • Molecular weight: 305.42
  • Formula: C18H27NO3
  • CLOGP: 3.75
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 58.56
  • ALOGS: -4.56
  • ROTB: 9

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 16, 2009 FDA ACORDA

FDA Adverse Event Reporting System

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
Application site pain 642.44 48.23 90 262 2461 4636179
Application site erythema 350.00 48.23 52 300 2029 4636611
Application site burn 174.56 48.23 23 329 350 4638290
Burns second degree 150.18 48.23 20 332 330 4638310
Occupational exposure to product 145.31 48.23 23 329 1308 4637332
Application site vesicles 137.86 48.23 20 332 628 4638012
Complex regional pain syndrome 95.68 48.23 14 338 463 4638177
Pain 81.78 48.23 33 319 92837 4545803
Drug ineffective 80.21 48.23 40 312 186021 4452619
Burning sensation 74.84 48.23 19 333 11853 4626787
Erythema 70.33 48.23 24 328 41916 4596724
Condition aggravated 62.65 48.23 24 328 58147 4580493
Throat irritation 52.58 48.23 13 339 7225 4631415
Hypersensitivity 49.07 48.23 18 334 38403 4600237

Pharmacologic Action:

SourceCodeDescription
ATC M02AB01 MUSCULO-SKELETAL SYSTEM
TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
Capsaicin and similar agents
ATC N01BX04 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Other local anesthetics
CHEBI has role CHEBI:35481 non-narcotic analgesic
MeSH PA D000982 Antipruritics
MeSH PA D003879 Dermatologic Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Postherpetic neuralgia indication 2177002
Neuralgia indication 16269008
Backache indication 161891005
Sprains and Strains indication
Arthritic Pain indication
Gastritis contraindication 4556007 DOID:4029
Bacterial septicemia contraindication 10001005 DOID:0040085
Myocardial infarction contraindication 22298006 DOID:5844
Shock contraindication 27942005
Hypertensive disorder contraindication 38341003 DOID:10763
Gastrointestinal ulcer contraindication 40845000
Body fluid retention contraindication 43498006
Conduction disorder of the heart contraindication 44808001
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Vitamin K deficiency contraindication 52675005 DOID:11249
Nasal polyp contraindication 52756005
Hepatic failure contraindication 59927004
Blood coagulation disorder contraindication 64779008 DOID:1247
Diabetes mellitus contraindication 73211009 DOID:9351
Factor II deficiency contraindication 73975000
Gastrointestinal hemorrhage contraindication 74474003
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Decreased respiratory function contraindication 80954004
Kidney disease contraindication 90708001 DOID:557
Thyrotoxicosis contraindication 90739004 DOID:7997
Hemophilia contraindication 90935002
Disorder of skin contraindication 95320005 DOID:37
Anemia due to enzyme deficiency contraindication 111577008
Open wound contraindication 125643001
Seizure disorder contraindication 128613002
Cerebrovascular accident contraindication 230690007
Heart block contraindication 233916004
Gastroesophageal reflux disease contraindication 235595009 DOID:8534
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Denuded skin contraindication 418242004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.64 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
8% QUTENZA AVERITAS N022395 Nov. 16, 2009 RX PATCH TOPICAL 8263059 Sept. 5, 2023 METHOD OF USING CAPSAICIN IN COMBINATION WITH A GEL COMPOSITION FOR REMOVAL OF CAPSAICIN FROM A TREATMENT AREA OR UNINTENDED AREA
8% QUTENZA AVERITAS N022395 Nov. 16, 2009 RX PATCH TOPICAL 8889113 Sept. 5, 2023 METHOD OF USING CAPSAICIN IN COMBINATION WITH A GEL COMPOSITION FOR REMOVAL OF CAPSAICIN FROM A TREATMENT AREA OR UNINTENDED AREA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Transient receptor potential cation channel subfamily V member 1 Ion channel OPENER Ki 8.22 CHEMBL CHEMBL
Tyrosine--tRNA ligase, cytoplasmic Enzyme Ki 4.38 CHEMBL
Prostaglandin G/H synthase 1 Enzyme IC50 5.42 CHEMBL
Cytochrome P450 1A2 Enzyme IC50 5.52 DRUG MATRIX
Transient receptor potential cation channel subfamily V member 1 Ion channel Ki 5.77 CHEMBL
NADH-ubiquinone oxidoreductase chain 1 Unclassified IC50 4.28 CHEMBL
Transient receptor potential cation channel subfamily M member 8 Unclassified IC50 4.55 CHEMBL
Potassium voltage-gated channel subfamily A member 1 Unclassified BLOCKER IC50 4.50 IUPHAR
Potassium voltage-gated channel subfamily A member 2 Unclassified BLOCKER Kd 4.40 IUPHAR
Potassium voltage-gated channel subfamily A member 7 Unclassified BLOCKER IC50 4.60 IUPHAR
Transient receptor potential cation channel subfamily V member 1 Unclassified ACTIVATOR EC50 8 IUPHAR

External reference:

IDSource
D002211 MESH_DESCRIPTOR_UI
4019506 VUID
N0000147626 NUI
C0006931 UMLSCUI
D00250 KEGG_DRUG
400416009 SNOMEDCT_US
4019506 VANDF
001988 NDDF
6074 MMSL
1992 RXNORM
95995002 SNOMEDCT_US
4346 MMSL
CHEBI:3374 CHEBI
CHEMBL294199 ChEMBL_ID
S07O44R1ZM UNII
10145 INN_ID
4DY PDB_CHEM_ID
DB06774 DRUGBANK_ID
2486 IUPHAR_LIGAND_ID
1548943 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PainBloc HUMAN OTC DRUG LABEL 1 0295-9029 LIQUID 2.50 mg TOPICAL OTC monograph not final 8 sections
Walgreens Capsaicin Hot HUMAN OTC DRUG LABEL 1 0363-9113 PATCH 0.60 mg TOPICAL OTC monograph not final 13 sections
CAPSAICIN HEAT PATCHES BACK AND LARGE AREAS HUMAN OTC DRUG LABEL 1 0363-9902 PATCH 0.03 g TOPICAL OTC monograph not final 13 sections
Castiva Warming HUMAN OTC DRUG LABEL 1 0395-0130 CREAM 0.35 mg TOPICAL OTC monograph not final 8 sections
Rugby Arthritis Pain Relieving HUMAN OTC DRUG LABEL 1 0536-1118 CREAM 0.75 mg TOPICAL OTC MONOGRAPH NOT FINAL 10 sections
Rugby Capsaicin Cream HUMAN OTC DRUG LABEL 1 0536-1264 CREAM 0.10 g TOPICAL OTC monograph not final 13 sections
Rugby Capsaicin HUMAN OTC DRUG LABEL 1 0536-2525 CREAM 0.25 mg TOPICAL OTC MONOGRAPH NOT FINAL 10 sections
Qutenza HUMAN PRESCRIPTION DRUG LABEL 1 10144-928 KIT 640 ug None NDA 17 sections
Qutenza HUMAN PRESCRIPTION DRUG LABEL 1 10144-929 KIT 640 ug None NDA 17 sections
WellPatch Warming Pain Relief HUMAN OTC DRUG LABEL 1 10742-8127 PATCH 25 mg TOPICAL OTC monograph not final 8 sections
RITE AID CAPSICUM HOT HUMAN OTC DRUG LABEL 1 11822-5744 PATCH 0.60 mg TOPICAL OTC monograph not final 12 sections
Capsaicin HUMAN OTC DRUG LABEL 1 11822-7884 CREAM 0.00 g TOPICAL OTC monograph not final 12 sections
ASTRAPHARM CHILLI BRAND HUMAN OTC DRUG LABEL 1 11993-000 PLASTER 0.25 g TOPICAL OTC monograph not final 14 sections
ASTRAPHARM CHILLI BRAND EXTERNAL MEDICATED HUMAN OTC DRUG LABEL 1 11993-001 PLASTER 70 mg TOPICAL OTC monograph not final 13 sections
Dr. OH BALM HUMAN OTC DRUG LABEL 3 17452-430 CREAM 0.02 g TOPICAL OTC monograph not final 9 sections
EARTHS CARE ARTHRITIS HUMAN OTC DRUG LABEL 1 24286-1559 CREAM 0.10 g TOPICAL OTC MONOGRAPH NOT FINAL 9 sections
Overtime HUMAN OTC DRUG LABEL 3 27495-008 LOTION 0.02 g TOPICAL OTC monograph not final 11 sections
Dendracin Neurodendraxcin HUMAN OTC DRUG LABEL 3 27495-014 LOTION 0.02 g TOPICAL OTC monograph not final 11 sections
OVERTIME-X HUMAN OTC DRUG LABEL 2 27495-019 LOTION 0.03 g TOPICAL OTC monograph not final 9 sections
OVERTIME-HMP HUMAN OTC DRUG LABEL 3 27495-020 STICK 0.10 g TOPICAL OTC monograph not final 10 sections
KESSLER FAMILY WELLNESS HUMAN OTC DRUG LABEL 3 27495-021 STICK 0.10 g TOPICAL OTC monograph not final 10 sections
TERPHOUSE HUMAN OTC DRUG LABEL 3 27495-022 STICK 0.10 g TOPICAL OTC monograph not final 10 sections
Flanax HUMAN OTC DRUG LABEL 2 27854-205 LINIMENT 0.03 g TOPICAL OTC monograph not final 11 sections
LONOL Forte Gel HUMAN OTC DRUG LABEL 2 27854-255 GEL 0.00 g TOPICAL OTC monograph not final 9 sections
LaBella Linimento Obrero HUMAN OTC DRUG LABEL 2 31774-8005 CREAM 0.25 mg TOPICAL OTC monograph not final 8 sections
MEDROX HUMAN OTC DRUG LABEL 2 33261-884 PATCH 0.04 g TOPICAL OTC MONOGRAPH NOT FINAL 8 sections
ASSURED PAIN RELIEF HOT PATCH HUMAN OTC DRUG LABEL 2 33992-1889 PATCH 8.30 mg TOPICAL OTC monograph not final 10 sections
Assured Pain Relief Hot Menthol HUMAN OTC DRUG LABEL 2 33992-6156 PATCH 8.30 mg TOPICAL OTC monograph not final 9 sections
Weh-Weh Natural Pain relief oil HUMAN OTC DRUG LABEL 1 35192-023 OIL 0.08 g TOPICAL OTC monograph not final 8 sections
Dendracin Neurodendraxcin HUMAN OTC DRUG LABEL 3 35356-642 LOTION 0.02 mg TOPICAL OTC monograph not final 10 sections