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Capsaicin - instructions for use, analogs, reviews and release forms (ointment, cream or gel, patch based on bitter pepper) drug for the treatment of neuropathic pain, neuralgia, warming effect in adults, children and pregnancy. Composition

Capsaicin - instructions for use, analogs, reviews and release forms (ointment, cream or gel, patch based on bitter pepper) drug for the treatment of neuropathic pain, neuralgia, warming effect in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Capsaicin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Capsaicin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Capsaicin in the presence of existing structural analogues.Use for the treatment of neuropathic pain, neuralgia, warming effect in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

 

Capsaicin - a highly selective vanilloid receptor agonist with transient receptor potential of type 1 (TRPV1). The initial effect of capsaicin is the activation of skin pain receptors expressing TRPV1, which leads to the development of burning and redness due to the release of vasoactive neuropeptides.

 

Pharmacodynamic effects

 

After exposure to capsaicin, the skin pain receptors become less sensitive to pain stimuli. Such effects of capsaicin are called sensitivity decrease; probably, they underlie the analgesic effect. It is assumed that the sensitivity of skin nerves that do not express TRPV1, including sensitivity to mechanical and vibration stimuli, remains unchanged. Capsaicin-induced change in cutaneous pain receptors is reversible; according to reports and observations of healthy volunteers, the restoration of normal function (reaction to irritant stimuli) occurs within a few weeks.

 

Clinical efficacy

 

Based on the results of controlled clinical trials conducted in patients with painful HIV-associated neuropathy, the effectiveness of a single 30-minute capsaicin application in the form of a patch on the foot area is shown. According to the results of controlled clinical trials conducted in patients with postherpetic neuralgia, the effectiveness of capsaicin is shown with a single 60-minute application on the painful areas of the skin of other localization. Reduction of pain intensity was noted already in the first week; The effect of the therapy persisted throughout the 12-week study period. The effectiveness of capsaicin is confirmed both in monotherapy and in combination with other systemic drugs for the treatment of neuropathic pain.

 

Composition

 

Capsaicin (a synthetic analogue of a natural compound found in bitter pepper) + excipients.

 

Pharmacokinetics

 

In vitro (when studying the dissolution of the active substance and its penetration into the skin) it is shown that the release rate of capsaicin from the dosage form for external use throughout the period of application is linear.According to the in vitro data, approximately 1% capsaicin is exposed during the 60-minute application of transepidermal and transdermal absorption. The amount of capsaicin released during external application per hour is proportional to the surface area of ​​the application. Therefore, the estimated maximum possible total dose for an application area of ​​1000 cm2 is approximately 7 mg. Assuming that with an external application area of ​​1000 cm2, approximately 1% capsaicin is delivered to a patient weighing 60 kg, the maximum possible exposure of capsaicin is approximately 0.12 mg / kg once every 3 months.

 

According to the pharmacokinetics data, after 60-minute capsaicin application, transient, insignificant (less than 5 ng / ml) systemic exposure of capsaicin was observed in approximately one third of patients with postherpetic neuralgia, in 3% of patients with painful diabetic neuropathy. In patients with HIV-associated neuropathy, systemic exposure was not observed. Data on systemic exposure after a 30-minute application is not available. In general, the percentage of patients with PGN who had a systemic exposure of capsaicin increased with the area of ​​the treated surface and the duration of therapy.Cmax capsaicin, detected in patients after a 60-minute application, was 4.6 ng / ml, this concentration was fixed immediately after removal of the capsaicin patch. In most cases, a quantifiable concentration was detected at the time of removal of the patch with capsaicin. A clear tendency to eliminating capsaicin from the systemic blood flow 3-6 hours after removal of the patch was revealed. None of the patients had capsaicin metabolites.

 

Indications

  • peripheral neuropathic pain, including postherpetic neuralgia, in adults without diabetes mellitus as a monotherapy or in combination with other medications for the treatment of pain.

 

Forms of release

 

Patch.

 

Ointment or cream for external use (sometimes mistakenly called a gel).

 

Balsam oil warming.

 

Instructions for use and how to use them

 

Patch

 

Outwardly. A plaster with capsaicin should be applied to the most painful areas of the skin. The attending physician should identify the painful areas of the skin and note them. A patch with capsaicin should be applied to undamaged, non-irritated dry skin.

 

Ointment or cream

 

Outerly, apply a thin layer on the previously washed dry skin, with joint diseases - 1 time per day for 3 days, then - 2 times a day (morning and evening); for warming up the muscles of athletes during massage - a strip of ointment 3-5 cm long is carefully rubbed into the skin.

 

Warm balm

 

Outerly, 2 times a day, a small amount of balm is applied uniformly onto the skin in the joint area, let it absorb for 2-3 minutes. After applying the balm, wash your hands thoroughly.

 

The course of treatment is 2-3 weeks or until the symptoms of inflammation are removed. If necessary, the course of treatment can be repeated.

 

Side effect

  • perversion of taste;
  • hypoesthesia;
  • burning sensation;
  • eye irritation;
  • AV blockade of 1 degree;
  • tachycardia;
  • a feeling of palpitations;
  • increased blood pressure;
  • cough;
  • irritation of the throat;
  • nasopharyngitis;
  • nausea, vomiting;
  • itching;
  • pain in the limbs;
  • headache;
  • muscle spasms;
  • pain and redness in the place of application;
  • papules, vesicles, swelling, swelling, dryness at the place of application;
  • urticaria, paresthesia, dermatitis, hyperesthesia, inflammation, irritation (hemorrhagic elements) at the place of application;
  • peripheral edema.

 

Contraindications

  • hypersensitivity to capsaicin.

 

Application in pregnancy and lactation

 

There are no clinical data on the use of capsaicin during pregnancy.

 

The results of studies conducted on animals did not reveal teratogenic effects.

 

Based on data from pharmacokinetics studies in humans showing a transient minor systemic absorption of capsaicin, the likelihood of an increased risk of developmental abnormalities due to the use of capsaicin with pregnant women is extremely low. Nevertheless, care must be taken when administering the capsaicin to pregnant women.

 

There are no clinical data on the use of capsaicin in breast-feeding women. In a study on lactating rats exposed to a daily capsaicin patch for 3 hours, the concentration of capsaicin in breast milk of rats was quantifiable.

 

At present, it is not known whether capsaicin penetrates the human breast milk. As a precaution on the day of therapy, it is recommended to refrain from breastfeeding.

 

Use in children

 

Due to the lack of data on safety and efficacy, capsaicin is not recommended for use in children and adolescents.

 

special instructions

 

After rubbing the ointment or cream, you should wash your hands thoroughly with warm water and soap.

 

Do not use with warming compresses.

 

In case of skin irritation, it is recommended to cancel the drug.

 

Avoid contact with mucous membranes (including the eyes), areas of skin irritation.

 

When handling the band-aid and cleaning the areas of application, medical workers should wear nitrile gloves.

 

A patch with capsaicin is allowed to be applied only to dry undamaged skin; Do not use the drug on the skin of the face, on the scalp and (or) close to the mucous membranes. Care should be taken to prevent unintentional contact with the patch or other materials that come into contact with the treated areas of the skin. The effect of capsaicin on the skin leads to the appearance of transient erythema and a burning sensation; especially sensitive to mucous membranes. Inhalation of airborne capsaicin can cause coughing or sneezing.The used patch should be disposed of immediately in an appropriate container for medical waste.

 

If the patch with capsaicin comes into contact with skin that is not planned to be treated, a cleansing gel should be applied to this area of ​​skin for one minute, then wipe the skin with a dry gauze cloth to remove the remaining capsaicin from its surface. After the cleansing gel is removed, the surface of the skin should be gently washed with water and soap. If burning occurs in the eyes, skin or respiratory tract, immediately remove the patch. Eyes and mucous membranes should be rinsed with water. With the development of dyspnea, appropriate medical attention should be provided.

 

In connection with the conditioned therapy, an increase in the intensity of pain during or shortly after the use of a capsaicin patch in patients may experience a transient increase in blood pressure (on average, less than 8 mm Hg). During the period of the treatment procedure, it is necessary to monitor the blood pressure level. Patients who have increased pain intensity should receive symptomatic treatment, for example, local cooling or analgesics for oral administration (eg short-acting opioid analgesics).In patients with unstable or poorly controlled hypertension or with a newly transferred CAS disease, the risk of adverse reactions from the CCC due to potential stress associated with the procedure should be taken into account before starting therapy with capsaicin.

 

Patients taking opioids in high doses may not respond to opioid analgesics for ingestion, used to eliminate acute pain during or after the treatment. Before the start of therapy, you must carefully collect the anamnesis; for patients with suspected high tolerance to opioids, an alternative strategy for reducing pain intensity should be used.

 

Despite the fact that during the clinical studies of the capsaicin patch there was no reduction in the neurological function caused by therapy, after the use of capsaicin, slight and transient changes in sensitivity (for example, thermal sensitivity) were noted. Patients with an increased risk of developing unwanted reactions due to minor changes in sensitivity should be careful when applying a patch with capsaicin.

 

There is limited experience with the use of capsaicin patch in patients with painful diabetic neuropathy (BDN). Long-term therapy with capsaicin in patients with MND has not been studied.

 

The cleansing gel for patch with capsaicin contains butyl hydroxy anisole, which can cause local skin reactions (eg contact dermatitis) or eye or mucous membrane irritation.

 

Drug Interactions

 

Strengthens the absorption of other medicines for external use with simultaneous application (due to reflex enhancement of blood flow).

 

Analogues of the drug Capsaicin

 

Structural analogs for the active substance:

  • Analgos;
  • Kutensa;
  • Nikofleks;
  • Percamp;
  • Peppers of a tincture;
  • Pepper-camphor liniment;
  • Pepper plaster;
  • Pepper plaster Doctor pepper with analgesic action;
  • Espoo.

 

Analogues for the pharmacological group (local-irritants):

  • Alvipsal;
  • Ammonia;
  • Analgos;
  • Apizarthron;
  • Badyaga;
  • Bengay;
  • Betalgon;
  • Bikarmint;
  • Bom-Bengu;
  • Boromentol;
  • Viprosal;
  • Mustard plaster;
  • Gavkamen;
  • Iodine;
  • Cameton;
  • Camphard;
  • Camphor;
  • Camphor ointment;
  • Camphor alcohol;
  • Capsicam;
  • Carmolis;
  • Kim balm is liquid;
  • Kutensa;
  • Levomenthol;
  • Camphor oil;
  • Mentoclar;
  • Miospray;
  • Mucofitin;
  • Nayatoks;
  • Nikofleks;
  • Percamp;
  • Peppers of a tincture;
  • Chilli pepper extract is thick;
  • Provinenol;
  • Risaxyl;
  • Salvisar;
  • Turpentine ointment;
  • Spongylan;
  • Turpentine oil;
  • Ungapiven;
  • Finalgon;
  • Evamenol;
  • Espol;
  • Efkamon.

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Reviews (1):
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According to the latest data, scientists are trying to determine the degree of influence of the active substance capsaicin on cancer cells and allegedly have already received data indicating the effectiveness of this molecule in the treatment of breast cancer.Of course, this does not mean that patients with this disease need to spread the breast with ointment or Capsaicin cream in the hope of getting rid of oncology, except as a burn it will not bring anything. Now scientists are working to confirm this hypothesis and are trying to find a mechanism for transporting the active substance capsaicin into cancer cells. And this business is not one year old.

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