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

Stem definition	Drug id	CAS RN
analgesics, capsaicin analogues	3064	404-86-4

Description:

Molecule	Description
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 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.06 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

Approvals:

Date	Agency	Company	Orphan
Nov. 16, 2009	FDA	ACORDA

FDA Adverse Event Reporting System (Female)

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
Application site pain	286.83	16.72	72	7501	4110	63477339
Body tinea	188.52	16.72	44	7529	1841	63479608
Inhibitory drug interaction	165.60	16.72	43	7530	2806	63478643
Infection susceptibility increased	161.22	16.72	44	7529	3477	63477972
Application site erythema	138.79	16.72	42	7531	4793	63476656
Glucose tolerance impaired	134.09	16.72	44	7529	6533	63474916
Application site burn	118.86	16.72	26	7547	808	63480641
Poor quality sleep	114.06	16.72	53	7520	19882	63461567
Purpura	114.01	16.72	45	7528	11340	63470109
Impaired quality of life	109.02	16.72	46	7527	13737	63467712
Bone density decreased	99.92	16.72	44	7529	14568	63466881
Application site vesicles	94.85	16.72	24	7549	1411	63480038
Hyperlipidaemia	90.61	16.72	45	7528	19526	63461923
Impaired work ability	89.34	16.72	43	7530	17432	63464017
Oral herpes	83.87	16.72	47	7526	26027	63455422
Skin disorder	70.77	16.72	44	7529	29463	63451986
Occupational exposure to product	68.09	16.72	20	7553	2058	63479391
Cataract	60.69	16.72	52	7521	57001	63424448
Burns second degree	55.97	16.72	17	7556	1961	63479488
Application site hyperaesthesia	48.21	16.72	6	7567	0	63481449
Urticaria thermal	47.88	16.72	11	7562	428	63481021
Herpes zoster	42.88	16.72	51	7522	82411	63399038
Cellulitis	41.49	16.72	50	7523	81908	63399541
Insomnia	39.10	16.72	82	7491	215170	63266279
Administration site erythema	37.07	16.72	10	7563	755	63480694
Immune thrombocytopenia	36.59	16.72	20	7553	10536	63470913
Weight increased	34.83	16.72	88	7485	260704	63220745
Hypertension	33.98	16.72	91	7482	279212	63202237
Burns first degree	33.24	16.72	5	7568	15	63481434
Contusion	30.60	16.72	60	7513	149984	63331465
Pigmentation disorder	28.60	16.72	13	7560	4626	63476823
Nail bed tenderness	27.82	16.72	7	7566	402	63481047
Application site swelling	25.42	16.72	7	7566	571	63480878
Complement factor C4 decreased	24.97	16.72	6	7567	284	63481165
Hypercholesterolaemia	23.80	16.72	20	7553	21314	63460135
Dizziness postural	22.90	16.72	13	7560	7363	63474086
Application site oedema	22.46	16.72	4	7569	41	63481408
Burning sensation	22.46	16.72	30	7543	54377	63427072
Cryoglobulinaemia	22.06	16.72	6	7567	467	63480982
Application site warmth	21.93	16.72	5	7568	188	63481261
Skin plaque	21.45	16.72	13	7560	8307	63473142
Vitamin B12 deficiency	21.06	16.72	11	7562	5292	63476157
Throat irritation	20.74	16.72	24	7549	37623	63443826
Autonomic neuropathy	20.61	16.72	7	7566	1152	63480297
Blood pressure systolic increased	19.35	16.72	26	7547	47371	63434078
Scratch	18.86	16.72	11	7562	6554	63474895
Therapy non-responder	18.77	16.72	33	7540	75868	63405581
Illness	18.65	16.72	26	7547	49033	63432416
Urticaria contact	17.41	16.72	3	7570	25	63481424
Blood viscosity abnormal	17.07	16.72	4	7569	170	63481279
Secretion discharge	16.90	16.72	13	7560	12218	63469231
Vulvovaginal swelling	16.73	16.72	5	7568	546	63480903

FDA Adverse Event Reporting System (Male)

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
Application site pain	234.12	20.67	48	2447	1860	34952576
Application site erythema	100.55	20.67	25	2470	2311	34952125
Burning sensation	41.41	20.67	22	2473	18372	34936064
Application site burn	35.48	20.67	7	2488	221	34954215
Application site vesicles	33.61	20.67	8	2487	614	34953822
Application site necrosis	31.96	20.67	4	2491	3	34954433
Swollen tongue	28.78	20.67	16	2479	14589	34939847
Pain	27.64	20.67	51	2444	204624	34749812
Sleep deficit	23.86	20.67	6	2489	579	34953857
Anticholinergic syndrome	23.53	20.67	7	2488	1262	34953174
Drug ineffective	23.07	20.67	78	2417	456673	34497763
Dermatitis exfoliative	20.99	20.67	10	2485	6629	34947807

FDA Adverse Event Reporting System (Geriatric)

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
Application site pain	364.61	16.95	87	8138	4660	79731503
Body tinea	190.17	16.95	43	8182	1811	79734352
Application site erythema	178.30	16.95	50	8175	5060	79731103
Infection susceptibility increased	160.41	16.95	43	8182	3678	79732485
Inhibitory drug interaction	148.23	16.95	42	8183	4411	79731752
Application site burn	138.54	16.95	29	8196	846	79735317
Glucose tolerance impaired	127.49	16.95	43	8182	8041	79728122
Impaired quality of life	110.14	16.95	45	8180	14341	79721822
Poor quality sleep	108.58	16.95	51	8174	22671	79713492
Bone density decreased	106.47	16.95	43	8182	13304	79722859
Application site vesicles	98.23	16.95	24	8201	1416	79734747
Purpura	96.92	16.95	45	8180	19482	79716681
Impaired work ability	90.42	16.95	43	8182	19638	79716525
Hyperlipidaemia	87.38	16.95	46	8179	26047	79710116
Oral herpes	82.40	16.95	45	8180	27409	79708754
Skin disorder	70.97	16.95	44	8181	33899	79702264
Cataract	63.41	16.95	52	8173	62068	79674095
Burns second degree	62.04	16.95	19	8206	2609	79733554
Herpes zoster	50.73	16.95	55	8170	93028	79643135
Urticaria thermal	49.33	16.95	11	8214	434	79735729
Application site hyperaesthesia	49.08	16.95	6	8219	0	79736163
Administration site erythema	45.70	16.95	10	8215	361	79735802
Cellulitis	45.26	16.95	56	8169	109004	79627159
Insomnia	44.78	16.95	86	8139	245084	79491079
Burning sensation	41.69	16.95	40	8185	58592	79677571
Weight increased	40.84	16.95	89	8136	277297	79458866
Occupational exposure to product	34.51	16.95	9	8216	691	79735472
Contusion	33.25	16.95	57	8168	148719	79587444
Burns first degree	30.76	16.95	5	8220	33	79736130
Immune thrombocytopenia	29.62	16.95	20	8205	17785	79718378
Application site swelling	29.16	16.95	8	8217	745	79735418
Nail bed tenderness	28.74	16.95	7	8218	407	79735756
Pigmentation disorder	28.03	16.95	13	8212	5605	79730558
Application site warmth	27.74	16.95	6	8219	205	79735958
Application site necrosis	26.28	16.95	4	8221	16	79736147
Complement factor C4 decreased	24.72	16.95	6	8219	344	79735819
Therapy non-responder	24.17	16.95	38	8187	92267	79643896
Blood pressure systolic increased	24	16.95	32	8193	66954	79669209
Allodynia	22.99	16.95	8	8217	1640	79734523
Illness	21.09	16.95	25	8200	46486	79689677
Application site oedema	20.27	16.95	4	8221	86	79736077
Skin plaque	20.13	16.95	13	8212	10732	79725431
Cryoglobulinaemia	19.57	16.95	6	8219	827	79735336
Application site discolouration	19.35	16.95	6	8219	858	79735305
Vitamin B12 deficiency	19.34	16.95	11	8214	7230	79728933
Drug ineffective	18.99	16.95	182	8043	1080731	78655432
Vulvovaginal swelling	18.85	16.95	5	8220	410	79735753
Autonomic neuropathy	18.25	16.95	7	8218	1888	79734275
Scratch	17.87	16.95	11	8214	8352	79727811
Urticaria contact	17.84	16.95	3	8222	25	79736138
Blood viscosity abnormal	17.53	16.95	4	8221	175	79735988
Sleep deficit	17.53	16.95	6	8219	1170	79734993
Pain	17.38	16.95	128	8097	703674	79032489

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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:38634	voltage-dependent sodium channel blockers
CHEBI has role	CHEBI:140535	capsaicin receptor agonist
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents

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

Disease	Relation	SNOMED_ID	DOID
Postherpetic neuralgia	indication	2177002
Neuralgia	indication	16269008
Backache	indication	161891005
Arthritic Pain	indication
Sprains and Strains	indication
Cannabis hyperemesis syndrome co-occurrent and due to cannabis abuse	off-label use	11047881000119100
Cannabis hyperemesis syndrome co-occurrent and due to cannabis dependence	off-label use	11048011000119100
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.64	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
8%	QUTENZA	AVERITAS	N022395	Nov. 16, 2009	RX	PATCH	TOPICAL	July 17, 2023	TREATMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY (DPN) OF THE FEET

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Transient receptor potential cation channel subfamily V member 1	Ion channel	Q8NER1	TRPV1_HUMAN	OPENER	Ki	8.22	CHEMBL	CHEMBL
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN		IC50	5.42	CHEMBL
Cytochrome P450 1A2	Enzyme	P05177	CP1A2_HUMAN		IC50	5.52	DRUG MATRIX
Arachidonate 5-lipoxygenase	Enzyme	P09917	LOX5_HUMAN		IC50	4.25	CHEMBL
Potassium voltage-gated channel subfamily A member 1	Ion channel	Q09470	KCNA1_HUMAN		IC50	4.54	CHEMBL
Tyrosine--tRNA ligase, cytoplasmic	Enzyme	P54577	SYYC_HUMAN		Ki	4.38	CHEMBL
Lysine-specific histone demethylase 1A	Enzyme	O60341	KDM1A_HUMAN		IC50	6.22	CHEMBL
Transient receptor potential cation channel subfamily V member 1	Ion channel		TRPV1_RAT		Ki	5.77	CHEMBL
NADH-ubiquinone oxidoreductase chain 1	Unclassified		NU1M_BOVIN		IC50	4.28	CHEMBL
Transient receptor potential cation channel subfamily M member 8	Ion channel		TRPM8_MOUSE		IC50	4.55	CHEMBL
Transient receptor potential cation channel subfamily V member 1	Ion channel		TRPV1_MOUSE	ACTIVATOR	EC50	8	IUPHAR
Potassium voltage-gated channel subfamily A member 7	Ion channel		KCNA7_MOUSE	BLOCKER	IC50	4.60	IUPHAR
Potassium voltage-gated channel subfamily A member 1	Ion channel		KCNA1_MOUSE	BLOCKER	IC50	4.50	IUPHAR
Potassium voltage-gated channel subfamily A member 2	Ion channel		KCNA2_RAT	BLOCKER	Kd	4.40	IUPHAR

External reference:

ID	Source
4019506	VUID
N0000147626	NUI
D00250	KEGG_DRUG
4019506	VANDF
C0006931	UMLSCUI
CHEBI:3374	CHEBI
4DY	PDB_CHEM_ID
CHEMBL294199	ChEMBL_ID
DB06774	DRUGBANK_ID
D002211	MESH_DESCRIPTOR_UI
1548943	PUBCHEM_CID
2486	IUPHAR_LIGAND_ID
10145	INN_ID
S07O44R1ZM	UNII
1992	RXNORM
169226	MMSL
4346	MMSL
6074	MMSL
001988	NDDF
400416009	SNOMEDCT_US
95995002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
PainBloc	HUMAN OTC DRUG LABEL	1	0295-9029	LIQUID	2.50 mg	TOPICAL	OTC monograph not final	12 sections
Walgreens Arthritis Pain Relief Capsaicin Analgesic	HUMAN OTC DRUG LABEL	1	0363-0837	CREAM	1 mg	TOPICAL	OTC MONOGRAPH NOT FINAL	14 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
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	12 sections
Rugby Arthritis Pain Relieving Topical Analgesic	HUMAN OTC DRUG LABEL	1	0536-1118	CREAM	0.75 mg	TOPICAL	OTC MONOGRAPH NOT FINAL	15 sections
Rugby Capsaicin Cream	HUMAN OTC DRUG LABEL	1	0536-1264	CREAM	0.10 g	TOPICAL	OTC monograph not final	13 sections
Rugby Capsaicin Cream	HUMAN OTC DRUG LABEL	1	0536-1264	CREAM	0.10 g	TOPICAL	OTC monograph not final	13 sections
Rugby Capsaicin External Analgesic	HUMAN OTC DRUG LABEL	1	0536-2525	CREAM	0.25 mg	TOPICAL	OTC MONOGRAPH NOT FINAL	14 sections
WellPatch Warming Pain Relief	HUMAN OTC DRUG LABEL	1	10742-8127	PATCH	25 mg	TOPICAL	OTC monograph not final	10 sections
WellPatch Warming Pain Relief	HUMAN OTC DRUG LABEL	1	10742-8127	PATCH	25 mg	TOPICAL	OTC monograph not final	10 sections
CAPSAICIN HEAT PATCHES PAIN RELIEF	HUMAN OTC DRUG LABEL	1	11822-4210	PATCH	0.03 g	TOPICAL	OTC monograph not final	14 sections
RITE AID CAPSICUM HOT	HUMAN OTC DRUG LABEL	1	11822-7448	PATCH	0.60 mg	TOPICAL	OTC monograph not final	12 sections
RITE AID CAPSICUM HOT	HUMAN OTC DRUG LABEL	1	11822-7448	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
Capsaicin	HUMAN OTC DRUG LABEL	1	11822-7884	CREAM	0.00 g	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	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
BLUE SPRING Foot and Leg Comfort Cream with Pain Relief	HUMAN OTC DRUG LABEL	2	14448-316	CREAM	0.25 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	13 sections
Overtime	HUMAN OTC DRUG LABEL	3	27495-008	LOTION	0.02 g	TOPICAL	OTC monograph not final	11 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
Dendracin Neurodendraxcin	HUMAN OTC DRUG LABEL	3	27495-014	LOTION	0.02 g	TOPICAL	OTC monograph not final	11 sections
Overtime-HMP	HUMAN OTC DRUG LABEL	3	27495-025	STICK	0.03 g	TOPICAL	OTC monograph not final	12 sections
Power Pain Relief Stick	HUMAN OTC DRUG LABEL	3	27495-026	STICK	0.03 g	TOPICAL	OTC monograph not final	12 sections