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Capsaicin is an active component of chili peppers, which are plants belonging to the genus Capsicum. It is an irritant for mammals, including humans, and produces a sensation of burning in any tissue with which it comes into contact. Capsaicin and several related compounds are called capsaicinoids and are produced as secondary metabolites by chili peppers, probably as deterrents against certain mammals and fungi.Pure capsaicin is a volatile, hydrophobic, colorless, odorless, crystalline to waxy compound.
History
The compound was first extracted (albeit in impure form) in 1816 by Christian Friedrich Bucholz (1770–1818). He called it "capsicin", after the genus Capsicum from which it was extracted. John Clough Thresh (1850–1932), who had isolated capsaicin in almost pure form, gave it the name "capsaicin" in 1876. But it was Karl Micko who first isolated capsaicin in pure form in 1898. Capsaicin's empirical formula (chemical composition) was first determined by E. K. Nelson in 1919; he also partially elucidated capsaicin's chemical structure. Capsaicin was first synthesized in 1930 by E. Spath and S. F. Darling.[ In 1961, similar substances were isolated from chili peppers by the Japanese chemists S. Kosuge and Y. Inagaki, who named them capsaicinoids.
In 1873 German pharmacologist Rudolf Buchheim (1820–1879) and in 1878 the Hungarian doctor Endre HÃ…‘gyes stated that "capsicol" (partially purified capsaicin) caused the burning feeling when in contact with mucous membranes and increased secretion of gastric acid.
Capsaicinoids
Capsaicin is the main capsaicinoid in chili peppers, followed by dihydrocapsaicin. These two compounds are also about twice as potent to the taste and nerves as the minor capsaicinoids nordihydrocapsaicin, homodihydrocapsaicin, and homocapsaicin. Dilute solutions of pure capsaicinoids produced different types of pungency; however, these differences were not noted using more concentrated solutions.
Capsaicin is believed to be synthesized in the interlocular septum of chili peppers by addition of a branched-chain fatty acid to vanillylamine; specifically, capsaicin is made from vanillylamine and 8-methyl-6-nonenoyl CoA.Biosynthesis depends on the gene AT3, which resides at the pun1 locus, and which encodes a putative acyltransferase.
Besides the six natural capsaicinoids, one synthetic member of the capsaicinoid family exists. Vanillylamide of n-nonanoic acid (VNA, also PAVA) is used as a reference substance for determining the relative pungency of capsaicinoids.
Natural function
Capsaicin is present in large quantities in the placental tissue (which holds the seeds), the internal membranes and, to a lesser extent, the other fleshy parts of the fruits of plants in the genus Capsicum. The seeds themselves do not produce any capsaicin, although the highest concentration of capsaicin can be found in the white pith of the inner wall, where the seeds are attached.
The seeds of Capsicum plants are dispersed predominantly by birds: in birds, the TRPV1 channel does not respond to capsaicin or related chemicals (avian vs mammalian TRPV1 show functional diversity and selective sensitivity). This is advantageous to the plant, as chili pepper seeds consumed by birds pass through the digestive tract and can germinate later, whereas mammals have molar teeth which destroy such seeds and prevent them from germinating. Thus, natural selection may have led to increasing capsaicin production because it makes the plant less likely to be eaten by animals that do not help it reproduce.
Mechanism of action
The burning and painful sensations associated with capsaicin result from its chemical interaction with sensory neurons. Capsaicin, as a member of the vanilloid family, binds to a receptor called the vanilloid receptor subtype 1 (TRPV1). First cloned in 1997, TRPV1 is an ion channel-type receptor. TRPV1, which can also be stimulated with heat, protons and physical abrasion, permits cations to pass through the cell membrane and into the cell when activated. The resulting depolarization of the neuron stimulates it to signal the brain. By binding to the TRPV1 receptor, the capsaicin molecule produces similar sensations to those of excessive heat or abrasive damage, explaining why the spiciness of capsaicin is described as a burning sensation.
Use capsaicin cream as directed by your doctor. Check the label on the medicine for exact dosing instructions.
An extra patient leaflet is available with capsaicin cream. Talk to your pharmacist if you have questions about this information.
Apply just enough medicine to cover the affected area. Gently massage the medicine into skin until it disappears.
Wash your hands with soap and water immediately after using capsaicin cream unless your hands are part of the treated area.
If you are using capsaicin cream on your hands, allow 30 minutes for the medicine to absorb before washing. During this time, avoid touching damaged or irritated skin, contact lenses, or your eyes, nose, mouth, or other mucous membranes. Wash hands after 30 minutes.
Do not apply to wounds or damaged, broken (open), or irritated skin.
Do not bandage or wrap the affected area.
Do not use capsaicin cream with a heating pad.
Do not expose the treated area to heat or direct sunlight. Warm or hot water or sunlight may increase the likelihood of burning or itching. Do not use capsaicin cream immediately after bathing, swimming, using a hot tub, sunbathing, or exposure to heat.
If you miss a dose of capsaicin cream, use it as soon as you remember. Continue to use it as directed by your doctor or on the package label.
Ask your health care provider any questions you may have about how to use capsaicin cream
This medication is used to treat minor aches and pains of the muscles/joints (e.g., arthritis, backache, sprains). It may also be used to treat nerve pain. Capsaicin works by decreasing a certain natural substance in your body (substance P) that helps pass pain signals to the brain.
How to use capsaicin in castor oil topical
Use this medication on the skin only. Follow all directions on the product package. If you are uncertain about any of the information, consult your doctor or pharmacist.
For the cream, gel, and lotion forms, apply a thin layer of medication to the affected area and rub in gently and thoroughly. You may want to use a cotton ball/swab or latex glove to apply the medication to avoid touching the medication with your hands.
Do not apply the medication in the eyes, mouth, nostrils, or genitals. If you do get the medication in those areas, flush with plenty of water. Also, do not apply this medication to skin that is injured or irritated (e.g., cut, scraped, sunburned).
Do not apply this medication immediately before or after activities such as bathing, swimming, sun bathing, or heavy exercise. Do not bandage or wrap the affected area or use a heating pad on that area. Doing so may increase the risk of side effects.
After applying the medication, wash your hands unless you are using this medication to treat the hands. If treating the hands, wait at least 30 minutes after applying the medication to wash your hands.
Use this medication regularly to get the most benefit from it. To help you remember, use it at the same times each day.
This medication may sometimes take up to 2 months to work. Tell your doctor if your condition persists for more than 7 days, if it worsens, or if it keeps returning. If you think you may have a serious medical problem, seek immediate medical attention.
Warmth, stinging, or burning on the application site may occur. If any of these effects persist or worsen, contact your doctor or pharmacist promptly.
Coughing, sneezing, watery eyes, or throat irritation may occur if you breathe in the dried residue from the medication. Use caution to avoid inhaling the residue.
If your doctor has directed you to use this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Stop using this medication and tell your doctor right away if you have any serious side effects, including: blistering/swelling at the application site, increased/unusual pain at the application site.
A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
Before using capsaicin, tell your doctor or pharmacist if you are allergic to it; or to zucapsaicin; or to hot peppers (from the Capsicum family); or to lidocaine or other local anesthetics that may be in your brand; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
If you have any of the following health problems, consult your doctor or pharmacist before using this product: injured/irritated skin in the affected area.
If you are going to have an MRI test, tell testing personnel if you are using the patch. Some patches may contain metals that can cause serious burns during an MRI. Ask your doctor whether you will need to remove your patch before the test and apply a new patch afterward, and how to do so properly.
During pregnancy, this product should be used only when clearly needed. Discuss the risks and benefits with your doctor.
It is not known whether this product passes into breast milk. Consult your doctor before breast-feeding.
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
Before using capsaicin products containing lidocaine or other local anesthetics, tell your doctor or pharmacist if you also take class I antiarrhythmic drugs (such as mexiletine, procainamide, quinidine).
Capsaicin is very similar to zucapsaicin. Do not use medications containing zucapsaicin while using capsaicin.
This medicine may be harmful if swallowed. If swallowing or overdose is suspected.
Notes
Keep all regular medical and laboratory appointments.
Missed Dose
If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.
Storage
Refer to storage information printed on the package. If you have any questions about storage, ask your pharmacist. Keep all drug products away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.
Information last revised April 2014. Copyright(c) 2014 First Databank, Inc.
