Capsicum oleoresin

Identification

Name
Capsicum oleoresin
Accession Number
DB11131
Description

Capsicum oleoresin is an oily organic resin derived from the fruit of plants in the Capsicum genus, such as chilli peppers. When the plants are finely ground, capsicum oleoresin is formed after the extraction process of capsaicin using oragnic solvents such as ethanol. It is commonly used as a culinary spice. The intensity of biological actions and toxicological effects of capsicum oleoresin are a direct function of the amount of capsaicinoids, or capsaicin, present in the compound 6. Capsaicinoids comprise of a group of fat-soluble pungent chemical phenols and include Capsaicin, dihydrocapsaicin, nordihydrocapsaicin, homocapsaicin, and homodihydrocapsaicin 3. Capsaicin and dihydrocapsaicin are the most pungent capsaicinoid analogues 3.

Capsicum oleoresin is contained in pepper sprays when suspended in water, and acts an active lachrymatory agent that induces irritation, lacrimation, pain, and temporary blindness when in contact with eyes. Due to its analgesic properties, capsicum oleoresin is used to temporarily relieve of minor aches and pains of muscles and joints as an active ingredient in topical OTC preparations and has been studied for management of different models of neuropathic pain 1. It is suggested that capsicum oleoresin is a rich source of phytochemicals that consist of phenolic compounds with antioxidant and antidiabetic activities 2.

Type
Biotech
Groups
Approved
Synonyms
  • Capsaicin oleoresin
  • Capsicum annuum resin
  • Capsicum capsicum resin
  • Capsicum longum resin
  • Cayenne pepper resin
  • Chili oleoresin
  • Oleoresin capsicum
  • Oleoresins of capsicum

Pharmacology

Indication

Indicated for the temporary relief of minor aches and pains of muscles and joints associated with simple backache, arthritis, strains and sprains.

Contraindications & Blackbox Warnings
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Pharmacodynamics

Capsicum oleoresin is a topical analgesic and inflammatory agent. Capsaicin, an active ingredient in capsicum oleoresin, causes pain and sensitization of both peripheral and central nerves. It induces primary and secondary hyperalgesia and mimics the symptoms associated with neuropathic pain, such as allodynia, secondary hyperalgesia, referred pain area, and viscerovisceral hyperalgesia 4. In opposition, capsaicin also mediates analgesic actions via desensitization and withdrawal of epidermal nerve fibers 4. Systemic reviews of capsaicin-containing topical formulations demonstrate clinical effectiveness for pain reduction in postherpetic neuralgia, postsurgical neuropathies, and diabetic neuropathy, compared to placebo 1.

Mechanism of action

Capsaicin is the active ingredient in capsicum oleoresin that confers the molecule its biological actions. It induces central sensitization to cause pain and depolarizes nociceptors to increases their cytosolic free Ca2+ concentration 4. It is a highly selective agonist and activator at the transient receptor potential vanilloid subfamily member 1 (TRPV1) receptors expressed in afferent neuronal C fibers and some Aδ fibers 1. The aliphatic tail of capsaicin interacts with the channel via nonspecific Van der Waals forces, while hydrogen bonds between its vanillyl “head” and amide “neck” with residues of glutamic acid E571 and T551 of the channel, respectively, confers specificity for ligand binding 5. Binding and local activation of these receptors lead to increased influx of calcium ions and nerve depolarization. Signal propagation to the central nervous system causes local heat, stinging, and/or itching sensations 1. Prolonged activation of TRPV1 receptors results in loss of receptor functionality, causing impaired local nociception for extended periods due to desensitization and inactivation of sensory neurons. It is thought that the activation of TRPV1 receptors is the main mechanism of action of capsaicin. Capsaicin also induces a local depletion of substance P, which is a neuropeptide involved in visceral pain signalling 5; however this effect in the relief of pain remains controversial 1.

TargetActionsOrganism
ATransient receptor potential cation channel subfamily V member 1
agonist
activator
Humans
Absorption

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Volume of distribution

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Protein binding

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Metabolism

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Route of elimination

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Half-life

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Clearance

For pharmacokinetic properties of capsaicin, refer to the drug entry for Capsaicin.

Adverse Effects
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Toxicity

Acute oral LD50, acute dermal LD50 and acute inhalation LD50 in rat are >3000mg/kg, >2500 mg/kg, and >10000 mg/m^3, respectively MSDS. Capsicum oleoresin is not considered to be a carcinogen. There has been no case reports or findings from studies indicating teratogenic potential of capsaicinoid 6.

Capsicum oleoresin can cause serious irritation, conjunctivitis and lacrimation via contact with eyes. It induces a burning sensation and pain in case of contact with eyes and skin. As it is also irritating to the respiratory system, it causes lung irritation and coughing as well as bronchoconstriction. Other respiratory effects include laryngospasm, swelling of the larynx and lungs, chemical pneumonitis,respiratory arrest and central nervous system effects such as convulsions and excitement. In case of ingestion, gastrointestinal tract irritation may be observed along with a sensation of warmth or painful burning MSDS. Symptoms of systemic toxicity include disorientation, fear, loss of body motor control including diminished hand-eye coordination, hyperventilation, tachycardia, and pulmonary oedema 6. Careful early decontamination is recommended and medical intervention should be initiated for any life-threatening symptoms. In case of contact, individual must be removed from the source of exposure and the contacted skin and mucous membranes should be thoroughly washed with copious amounts of water 6.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Products

Active Moieties
NameKindUNIICASInChI Key
CapsaicinunknownS07O44R1ZM404-86-4YKPUWZUDDOIDPM-SOFGYWHQSA-N
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Chakra Aroma Relaxing ColorPatch0.2 g/1Topicalmooni studio2019-01-01Not applicableUs
DermacinRx Penetral CreamCream0.25 mg/1mLTopicalPureTek Corporation2015-06-09Not applicableUs
Diabet AidLotion0.25 mg/1gTopicalInsight Pharmaceuticals LLC2010-06-07Not applicableUs
Fast Arthritis AidGel0.061 g/244gTopicalConcept Laboratories2015-04-17Not applicableUs
Hot StuffCream0.0265 g/106gTopicalMueller Sports Medicine, Inc.2014-06-25Not applicableUs
Sheffield Arthritis and Muscle Pain ReliefCream0.25 mg/1gTopicalSheffield Pharmaceuticals LLC2010-04-14Not applicableUs
Super Arthritis Pain ReliefLiquidTopicalHerbalife International of America, Inc.1999-11-012002-09-17Canada
TrixaicinCream0.25 mg/1gTopicalA-S Medication Solutions1995-12-012018-02-28Us
TrixaicinCream0.25 mg/1gTopicalQualitest1995-12-012018-02-28Us
Trixaicin HPCream0.75 mg/1gTopicalQualitest1995-12-012015-11-26Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Arthricare for Women Ultra StrengthCapsicum oleoresin (0.075 %) + Levomenthol (2 %)CreamTopicalDel Pharmaceuticals Inc.1997-10-212003-07-21Canada
BiobalsamCapsicum oleoresin (0.05 %) + Methyl nicotinate (0.75 %)CreamTopicalBiopharmatech Inc.1997-06-111999-07-07Canada
DeramsilkRx Anodynexa PakCapsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1) + Ranitidine hydrochloride (150 mg/1)KitOral; TopicalPatchwerx Labs2015-06-12Not applicableUs
DermacinRx Inflammatral PakCapsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1) + Ranitidine hydrochloride (150 mg/1)Oral; TopicalPureTek Corporation2015-06-122019-03-05Us
DermacinRx Lexitral PharmaPakCapsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (16.05 mg/1mL)KitTopicalPureTek Corporation2015-11-06Not applicableUs
DermasilkRx DicloPakCapsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1)KitOral; TopicalPatchwerx Labs2015-08-06Not applicableUs
DermasilkRx DicloPakCapsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1)KitOral; TopicalPatchwerx Labs2015-08-05Not applicableUs
Diclotral PakCapsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (16.05 mg/1mL)KitTopicalPatchwerx Labs2014-05-28Not applicableUs
Essentials Herbal Muscle MassageCapsicum oleoresin (0.32 mg/1g) + Methyl salicylate (100 mg/1g) + Racementhol (50 mg/1g)GelTopicalArbonne International, LLC2012-02-22Not applicableUs
Family Care Back Pain TherapyCapsicum oleoresin (16 mg/1) + Levomenthol (24 mg/1) + Synthetic camphor (80 mg/1)PatchTopicalUnited Exchange Corporation2011-12-27Not applicableUs

Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
UW86K581WY
CAS number
8023-77-6

References

General References
  1. Groninger H, Schisler RE: Topical capsaicin for neuropathic pain #255. J Palliat Med. 2012 Aug;15(8):946-7. doi: 10.1089/jpm.2012.9571. [PubMed:22849599]
  2. Sricharoen P, Lamaiphan N, Patthawaro P, Limchoowong N, Techawongstien S, Chanthai S: Phytochemicals in Capsicum oleoresin from different varieties of hot chilli peppers with their antidiabetic and antioxidant activities due to some phenolic compounds. Ultrason Sonochem. 2017 Sep;38:629-639. doi: 10.1016/j.ultsonch.2016.08.018. Epub 2016 Aug 12. [PubMed:27544798]
  3. Yeung MF, Tang WY: Clinicopathological effects of pepper (oleoresin capsicum) spray. Hong Kong Med J. 2015 Dec;21(6):542-52. doi: 10.12809/hkmj154691. Epub 2015 Nov 6. [PubMed:26554271]
  4. O'Neill J, Brock C, Olesen AE, Andresen T, Nilsson M, Dickenson AH: Unravelling the mystery of capsaicin: a tool to understand and treat pain. Pharmacol Rev. 2012 Oct;64(4):939-71. doi: 10.1124/pr.112.006163. [PubMed:23023032]
  5. Fattori V, Hohmann MS, Rossaneis AC, Pinho-Ribeiro FA, Verri WA: Capsaicin: Current Understanding of Its Mechanisms and Therapy of Pain and Other Pre-Clinical and Clinical Uses. Molecules. 2016 Jun 28;21(7). pii: molecules21070844. doi: 10.3390/molecules21070844. [PubMed:27367653]
  6. Oleoresin Capsicum Toxicology Evaluation and Hazard Review [Link]
PubChem Substance
347911130
RxNav
235787
Wikipedia
Pepper_spray
MSDS
Download (58.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentBack Pain Lower Back Chronic1
4CompletedTreatmentSub-acute Back Pain1
4RecruitingTreatmentBack Pain Lower Back Chronic1
3Not Yet RecruitingTreatmentMigraine1
2RecruitingTreatmentCoughing1
2WithdrawnTreatmentPain, Acute1
2, 3WithdrawnTreatmentHuman Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS) / Immune Reconstitution Inflammatory Syndrome / Immune Reconstitution Syndrome / Tuberculosis (TB)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
PatchTopical0.2 g/1
KitOral; Topical
CreamTopical0.25 mg/1mL
LotionTopical0.25 mg/1g
KitTopical
GelTopical
GelTopical0.061 g/244g
LinimentTopical
OintmentTopical
TabletOral
CreamTopical0.0265 g/106g
PatchTopical
OilTopical
LiquidTopical
PlasterTransdermal
CreamTopical
CreamTopical0.25 mg/1g
CreamTopical0.75 mg/1g
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)<60"Oleoresin Capsicum Toxicology Evaluation and Hazard Review.", National Institute of Justice Less-Than-Lethal Force Program, 1995
boiling point (°C)>187"Oleoresin Capsicum Toxicology Evaluation and Hazard Review.", National Institute of Justice Less-Than-Lethal Force Program, 1995
water solubilityFully dispersible"Oleoresin Capsicum Toxicology Evaluation and Hazard Review.", National Institute of Justice Less-Than-Lethal Force Program, 1995

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
Activator
General Function
Transmembrane signaling receptor activity
Specific Function
Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular aci...
Gene Name
TRPV1
Uniprot ID
Q8NER1
Uniprot Name
Transient receptor potential cation channel subfamily V member 1
Molecular Weight
94955.33 Da
References
  1. Groninger H, Schisler RE: Topical capsaicin for neuropathic pain #255. J Palliat Med. 2012 Aug;15(8):946-7. doi: 10.1089/jpm.2012.9571. [PubMed:22849599]

Drug created on December 03, 2015 09:51 / Updated on June 12, 2020 10:53

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