Capsaicin

MUSCULO-SKELETAL SYSTEM

Key facts

Capsaicin is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 2009. DrugCentral lists 15 molecular targets, including TRPV1, Trpv1 and KDM1A. Recorded indications include Arthritic Pain, Backache, Neuralgia and Postherpetic neuralgia.

• Approval status: ofp (first approved 2009 by the FDA).
• Molecular targets: TRPV1, Trpv1, KDM1A and TRPM8 (15 listed in DrugCentral).
• Indications: Arthritic Pain, Backache, Neuralgia, Postherpetic neuralgia and Sprains and Strains.
• ATC code: M02AB01 (Capsaicin and similar agents).
• Molecular formula: C18H27NO3; molecular weight 305.42 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (5)

• Arthritic Pain
• Backache
• Neuralgia
• Postherpetic neuralgia
• Sprains and Strains

Off-label uses (2)

• Cannabis hyperemesis syndrome co-occurrent and due to cannabis abuse
• Cannabis hyperemesis syndrome co-occurrent and due to cannabis dependence

Contraindications (34)

• Anemia
• Anemia due to enzyme deficiency
• Bacterial septicemia
• Blood coagulation disorder
• Body fluid retention
• Breastfeeding (mother)
• Cardiovascular event risk
• Cerebrovascular accident
• Conduction disorder of the heart
• Decreased respiratory function
• Denuded skin
• Diabetes mellitus
• Disease of liver
• Disorder of cardiovascular system
• Disorder of skin
• Factor II deficiency
• Gastritis
• Gastroesophageal reflux disease
• Gastrointestinal hemorrhage
• Gastrointestinal ulcer
• Heart block
• Hemophilia
• Hepatic failure
• Hypertensive disorder
• Kidney disease
• Myocardial infarction
• Nasal polyp
• Open wound
• Pregnancy, function
• Seizure disorder
• + 4 more

Mechanism & targets

Molecular targets (15)

Target	Gene	Action	Activity
Transient receptor potential cation channel subfamily V member 1	TRPV1	opener	Ki 8.22
Transient receptor potential cation channel subfamily V member 1	Trpv1	activator	EC50 8.00
Lysine-specific histone demethylase 1A	KDM1A	unknown	IC50 6.22
Transient receptor potential cation channel subfamily M member 8	TRPM8	unknown	IC50 6.00
Transient receptor potential cation channel subfamily V member 1	Trpv1	unknown	Ki 5.77
Cytochrome P450 1A2	CYP1A2	unknown	IC50 5.52
Prostaglandin G/H synthase 1	PTGS1	unknown	IC50 5.42
Potassium voltage-gated channel subfamily A member 7	Kcna7	blocker	IC50 4.60
Transient receptor potential cation channel subfamily M member 8	Trpm8	unknown	IC50 4.55
Potassium voltage-gated channel subfamily A member 1	KCNA1	unknown	IC50 4.54
Potassium voltage-gated channel subfamily A member 1	Kcna1	blocker	IC50 4.50
Potassium voltage-gated channel subfamily A member 2	Kcna2	blocker	Kd 4.40
Tyrosine--tRNA ligase, cytoplasmic	YARS	unknown	Ki 4.38
NADH-ubiquinone oxidoreductase chain 1	MT-ND1	unknown	IC50 4.28
Arachidonate 5-lipoxygenase	ALOX5	unknown	IC50 4.25

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2009-11-16	FDA	—	ACORDA

ATC classification

ATC code	Therapeutic hierarchy
M02AB01	MUSCULO-SKELETAL SYSTEM › TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN › TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN › Capsaicin and similar agents
N01BX04	NERVOUS SYSTEM › ANESTHETICS › ANESTHETICS, LOCAL › Other local anesthetics

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Application site pain	1361.1
Application site erythema	365.6
Application site burn	210.3
Body tinea	204.5
Application site vesicles	166.3
Infection susceptibility increased	166.2
Inhibitory drug interaction	157.9
Bone density decreased	157.8
Burning sensation	147.3
Purpura	144.1
Poor quality sleep	131.3
Glucose tolerance impaired	127.3

Chemical structure

• Molecular formula: C₁₈H₂₇NO₃
• Molecular weight: 305.42 g/mol
• CAS number: —
• InChIKey: YKPUWZUDDOIDPM-SOFGYWHQSA-N
• PubChem CID: 1548943

COC1=C(O)C=CC(CNC(=O)CCCC\C=C\C(C)C)=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Capsaicin used for?

DrugCentral lists the following indications for Capsaicin: Arthritic Pain, Backache, Neuralgia, Postherpetic neuralgia and Sprains and Strains.

How does Capsaicin work?

Its molecular targets in DrugCentral include TRPV1 (opener), Trpv1 (activator), KDM1A and TRPM8.

When was Capsaicin first approved?

Capsaicin was first approved by the FDA in 2009.

What is the chemical formula of Capsaicin?

Capsaicin has the molecular formula C18H27NO3 and a molecular weight of 305.42 g/mol.

Sources

• DrugCentral drug card 3064 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL294199 — compound record and bioactivity
• PubChem CID 1548943 — chemical identifiers
• DrugBank DB06774 — drug record
• FDA UNII S07O44R1ZM — substance identity
• DailyMed: FDA labels for Capsaicin — current prescribing information (label search)
• UniProt Q8NER1 (TRPV1) — target protein
• UniProt O60341 (KDM1A) — target protein
• UniProt Q7Z2W7 (TRPM8) — target protein
• UniProt P05177 (CYP1A2) — target protein
• UniProt P23219 (PTGS1) — target protein
• UniProt Q09470 (KCNA1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.