Identification
- Summary
Capsicum oleoresin is a medication used to treat minor aches and pains of muscles and joints.
- Brand Names
- Previdolrx Analgesic Pak
- Generic Name
- Capsicum oleoresin
- DrugBank Accession Number
- DB11131
- Background
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
- Capsicum oleoresin
- 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.
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism ATransient receptor potential cation channel subfamily V member 1 agonistactivatorHumans - 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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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.
- 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
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Active Moieties
Name Kind UNII CAS InChI Key Capsaicin unknown S07O44R1ZM 404-86-4 YKPUWZUDDOIDPM-SOFGYWHQSA-N - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Chakra Aroma Relaxing Color Patch 0.2 g/1 Topical mooni studio 2019-01-01 Not applicable US 
Chilli Brand Porous Capsicum Plaster Plaster ZBT FAR EAST SDN. BHD. 2020-09-08 Not applicable Malaysia 
Circata Cream 0.05 g/100g Topical PureTek Corporation 2021-09-02 Not applicable US Circatrix Cream 0.05 g/100g Topical PureTek Corporation 2022-01-14 Not applicable US DermacinRx Penetral Cream Cream 0.25 mg/1mL Topical PureTek Corporation 2015-06-09 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Arthricare for Women Ultra Strength Capsicum oleoresin (0.075 %) + Levomenthol (2 %) Cream Topical Del Pharmaceuticals Inc. 1997-10-21 2003-07-21 Canada 
Biobalsam Capsicum oleoresin (0.05 %) + Methyl nicotinate (0.75 %) Cream Topical Biopharmatech Inc. 1997-06-11 1999-07-07 Canada CAPSIGEL 30 GR POMAD Capsicum oleoresin (16.67 mg/g) + Methyl salicylate (100 mg/g) Ointment Topical OSEL İLAÇ SAN. VE TİC. A.Ş. 1999-05-05 Not applicable Turkey 
DeramsilkRx Anodynexa Pak Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1) + Ranitidine hydrochloride (150 mg/1) Kit Oral; Topical Patchwerx Labs 2015-06-12 Not applicable US DermacinRx Inflammatral Pak Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1) + Ranitidine hydrochloride (150 mg/1) Kit Oral; Topical PureTek Corporation 2015-06-12 2019-03-05 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image DermacinRx Lexitral PharmaPak Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (16.05 mg/1mL) Cream; Kit; Solution Topical PureTek Corporation 2015-11-06 2024-04-30 US DermacinRx Lexitral PharmaPak II Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (16.05 mg/1mL) Cream; Kit; Solution Topical PureTek Corporation 2022-03-02 2024-04-30 US Inflammacin Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1) Kit Oral; Topical PureTek Corporation 2016-01-11 Not applicable US Lextol Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (16.05 mg/1mL) Cream; Kit; Solution Topical PureTek Corporation 2023-08-30 Not applicable US Lextol Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (16.05 mg/1mL) Cream; Kit; Solution Topical PureTek Corporation 2023-08-25 Not applicable US
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- UW86K581WY
- CAS number
- 8023-77-6
References
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Oleoresin Capsicum Toxicology Evaluation and Hazard Review [Link]
- External Links
- PubChem Substance
- 347911130
- 235787
- Wikipedia
- Pepper_spray
- MSDS
- Download (58.4 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Chronic Lower Back Pain (CLBP) 2 4 Completed Treatment Sub-acute Back Pain 1 3 Recruiting Treatment Migraine 1 2 Active Not Recruiting Treatment Cough 1 2 Withdrawn Treatment Acute Pain 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Patch Topical 0.2 g/1 Plaster Cream Topical 0.05 g/100g Kit Oral; Topical Cream; kit; solution Topical Cream Topical 0.25 mg/1mL Lotion Topical 0.25 mg/1g Kit Topical Gel Topical Gel Topical 0.061 g/244g Liniment Topical Ointment Topical Tablet Oral Cream Topical 0.0265 g/106g Spray Topical Patch Topical Cream; kit; tablet Oral; Topical Oil Topical Cream Topical .075 g/100g Liquid Topical 0.025 % Plaster Plaster Transdermal Cream Topical 0.25 mg/1g Cream Topical 0.75 mg/1g Cream Topical - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source 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 solubility Fully 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
- AgonistActivator
- 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
- 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. [Article]
Drug created at December 03, 2015 16:51 / Updated at May 21, 2021 10:21