Capsaicin Actions

• Actions of Capsaicin in details
• Capsaicin pharmacology
• Capsaicin reviews

Actions of Capsaicin in details

Pharmacology: Pharmacodynamics: Mechanism of Action: Capsaicin activates afferent nociceptive neurons and evokes sensations ranging from hotness to burning. Its analgesic properties are mediated by the depletion of substance P that leads to the desensitization of small afferent sensory neurons. Capsaicin binds to a specific nerve membrane receptor, the transient receptor potential V1 (TRPV1) receptor (previously known as vanilloid receptor, VR1). The binding of Capsaicin to TRPV1 receptor in small fiber sensory afferent nerve endings activates the receptor and this leads to an influx of calcium, and the release of inflammatory neuropeptides. This mediates the pungent properties of Capsaicin and limits its tolerability. Following the receptor activation, these neurons are functionally desensitized to further painful stimuli and this leads to analgesia. In addition, there may be degeneration of nociceptive fibers. Capsaicin down regulates these voltage-activated calcium channels by dephosphorylation (via a calcium-dependent activation of calcineurin). This is the mechanism by which Capsaicin reduces inflammatory hyperalgesia.

Pharmacokinetics:

Topical Capsaicin is well-absorbed from the skin. Maximal cutaneous concentrations of Capsaicin are rapidly achieved when Capsaicin is applied topically. These concentrations are greater with isopropyl preparations compared with propylene glycol or mineral oil preparations. The half-life (t_½) of Capsaicin is approximately 24 hrs. In a study of 12 subjects, the topical application of 3% solutions of Capsaicin (Capsaicin 55%, hydrocapsaicin 35% and other analogues 10%) using 3 different vehicle preparations (isopropyl alcohol 70%, mineral oil and propylene glycol which contained alcohol 20%) was evaluated. Capsaicinoids were detected in the stratum corneum within 1 min after application and a steady state was reached shortly. The maximum concentration was almost 3 times greater in the subjects who received the isopropyl alcohol 70% preparation compared with the mineral oil and propylene glycol preparations. This indicated the greater relative solubility of the capsaicinoids in the larger volume of alcohol. The t_½ of Capsaicin was approximately 24 hrs in all 3 preparations. In mice, Capsaicin is distributed widely to the brain, spinal cord and liver after IV administration. Capsaicinoids are metabolised by cytochrome P-450 enzymes to macrocyclic, alkyl dehydrogenated, omega-1 hydroxylated products. Dihydrocapsaicin is the major metabolite of Capsaicin. Dihydrocapsaicin and its metabolites are excreted by the kidney. Capsaicin is also renally cleared.

How should I take Capsaicin?

A nurse or other trained healthcare professional will apply the topical Qutenza™ patch to the affected area.

If you are using the topical cream, gel, lotion, or ointment for neuralgia, muscle pain, or arthritis, follow the instructions on the medicine label.

Be careful not to get any of Capsaicin in your eyes, because it can cause severe eye irritation. If the medicine does get in your eyes, wash the eyes with water and check with your doctor right away.

If Capsaicin gets on your face, scalp, or in your mouth, it may cause a burning sensation. Wash these areas with warm (not hot) soapy water.

If you are using the cream, gel, lotion, or ointment:

• Do not put the medicine on wounds or irritated skin.
• Apply a small amount of medicine and use your fingers to rub it in well so very little or no medicine is left on the skin.
• Wash your hands with soap and water after applying the medicine to avoid getting it in your eyes or on other sensitive areas of the body.
• If you are using Capsaicin for arthritis in your hands, do not wash your hands for at least 30 minutes after applying it.
• If a bandage is being used on the treated area, do not wrap it tightly.
• Use the medicine regularly every day as directed. It may take a full 2 weeks before your pain goes away.
• If your condition gets worse, or does not improve after one month, stop using the medicine and check with your doctor.

Dosing

The dose of Capsaicin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Capsaicin. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For topical dosage form (cream, gel, lotion, or ointment):
  • For arthritis, muscle pain, or neuralgia:
    • Adults and teenagers—Apply regularly 3 or 4 times a day and rub in well.
    • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Capsaicin, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Capsaicin pharmacology

Capsaicin is a TRPV1 receptor agonist. TRPV1 is a trans-membrane receptor-ion channel complex activated by temperatures higher than 43 degrees Celsius, pH lower than 6, and endogenous lipids. When activated by a combination of these factors, the channel can transiently open and initiate depolarization due to the influx of calcium and sodium ions. Because TRPV1 is commonly expressed in A-delta and mostly C fibers, depolarization results in action potentials which send impulses to the brain and spinal cord. These impulses result in Capsaicin effects of warming, tingling, itching, stinging, or burning. Capsaicin also causes more persistent activation of these receptors compared to the environmental agonists, resulting in a loss of response to many sensory stimuli, described as "defunctionalization". Capsaicin is associated with many enzymatic, cytoskeletal, and osmotic changes, as well as disruption of mitochondrial respiration, impairing nociceptor function for extended periods of time.

References

1. DailyMed. "CAPSAICIN: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
2. NCIt. "Capsaicin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
3. EPA DSStox. "Capsaicin: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Capsaicin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Capsaicin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

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Information checked by Dr. Sachin Kumar, MD Pharmacology