Index of drugs

Treatment of peripheral neuropathic pain in adult patients without diabetes as monotherapy or in combination with other analgesics.

1 patch with an area of ​​280 cm² contains 179 mg capsaicin (640 μg capsaicin / cm² patch).

Painkiller for topical use. Capsaicin, i.e. 6-nonenamide, N- [4-hydroxy-3-methoxyphenyl) methyl] -8-methyl, is a highly selective vanilloid receptor agonist from the group of transient potential receptors (TRPV1). The initial effect of capsaicin is the activation of TPRV1 nociceptors in the skin, which causes irritation and erythema as a result of the release of vasoactive neuropeptides. After exposure to capsaicin, skin nociceptors become less sensitive to different stimuli. Late actions of capsaicin are often referred to as "anesthesia" and it is believed that they are responsible for the resolution of pain. Sensations from the nerves of the skin without expression of TPRV1 remain unchanged, including the ability to feel the mechanical and vibrational stimuli. Capsaicin-induced changes in skin nocicepses are reversible, as demonstrated in studies in healthy volunteers who have been observed to return to normal function (unpleasant sensations) over weeks. In clinical trials, a reduction in pain after 1 week was observed after application of the patch and persisted for the 12th week of the study. Test results andn vitro (studies on the breakdown of active substance and penetration through the skin) indicate a linear course of capsaicin release from patches over time. Based on researchin vitro it is estimated that during a one-hour application, approximately 1% of capsaicin is absorbed into the skin and skin layers. Considering that the amount of capsaicin released from the patch is proportional to the application area, the estimated total maximum possible dose on the surface of 1000 cm² will be approximately 7 mg. Assuming that the patch has an area of ​​1000 cm² about 1% of capsaicin will be delivered to a person with a body weight of 60 kg, the maximum possible dose of capsaicin will be 0.12 mg / kg, once every 3 months. The highest capsaicin levels detected in patients treated for 60 min were 4.6 ng / ml and occurred immediately after removal of the patch. The most measurable concentrations were observed during removal of the patch with a pronounced tendency to disappear within 3-6 h after removal of the patch. No metabolite of capsaicin was detected in any patient. The analysis of pharmacokinetic data in a population of patients treated for 60-90 min indicates that maximum serum capsaicin concentrations occur about 20 minutes after removal of the patch and decrease very rapidly with mean T_0,5 about 130 minutes.

Hypersensitivity to capsaicin or other components of the drug.

Plaster should not be applied on the face, in the area above the hairline and / or in the mucous membrane area. Care should be taken to avoid unintentional contact with the patch or other materials that have been in contact with the treatment site. Exposure of the skin to capsaicin causes transient erythema and burning sensation, which is particularly sensitive to mucous membranes. If the patch comes into contact with the skin in a place other than the treatment area, it should be applied with a cleansing gel for 1 min, then - to remove capsaicin residues from the skin surface - wipe it off with dry gauze and gently wash with soap and water. If burning of the eye, skin or respiratory tract occurs, move away from the place where the medicine is administered. Eyes and mucous membranes should be rinsed or washed with water. If dyspnea occurs, appropriate medical attention should be provided. As a result of treatment of pain intensity, when applying the patch and shortly after its application, a transient increase in blood pressure (on average <8 mmHg) may occur. The blood pressure should be monitored during the treatment. Patients experiencing severe pain should receive symptomatic treatment such as: local cooling or oral analgesics.In patients with unstable or poorly controlled hypertension or recent cardiovascular events, the risk of adverse cardiovascular reactions due to possible stress associated with the surgery should be considered before implementing treatment with a patch. Patients using high doses of opioids may not respond to opioid analgesics used in acute pain during and after the treatment; before the treatment is implemented, an accurate medical history should be obtained in patients suspected of a high degree of tolerance to opioid drugs and an alternative analgesic regimen should be established. During treatment, slight and transient sensory disturbances were reported; caution should be used in patients at high risk of adverse reactions. The experience in the use of patches in patients with painful diabetic neuropathy is limited, no re-evaluation of the drug has been performed. The drug contains butylhydroxyanisole, which can cause local skin reactions or irritation of the eyes and mucous membranes.

Caution should be exercised when using the drug during pregnancy. Based on human pharmacokinetic properties that indicate transient low systemic exposure to capsaicin, the likelihood of patches increasing the risk of developmental abnormalities during pregnancy is low. Breast-feeding is not recommended on the day of applying the patches.

Very common: pain, erythema at the application site. Common: pruritus, papules, blisters, swelling, swelling, dryness at the application site. Uncommon: shingles, taste disorders, hypoaesthesia, burning sensation, eye irritation, first degree atrioventricular block, tachycardia, palpitations, hypertension, cough, throat irritation, nausea, pruritus, limb pain, muscle cramps, high blood pressure , urticaria, paresthesia, dermatitis, hyperaesthesia, inflammation, reaction, irritation, bruising at the application site, peripheral edema.

Adults. Apply the patch to the most painful areas on the skin (using up to 4 patches). Place the patch on undamaged, non-irritated, dry skin and leave for 30 minutes on the feet (eg in neuropathy in the course of HIV infection) and for 60 minutes in other places (eg in herpes zoster neuralgia). If the pain persists or recurs, the treatment with the patch can be repeated every 90 days. Always use nitrile gloves when applying the patch. If necessary, to improve adhesion of the patch, cut the hair at the treatment site (do not shave). In order to reduce the discomfort associated with the application of the patch before the procedure, the local anesthetic should be applied to the entire surface of the treated area and to 1-2 cm around it. The patch can be cut to a specific size and shape of the surface to be treated. To ensure permanent contact of the patch with the treatment site, elastic socks or bandages can be used. After removal of the patch, place the cleansing gel in a large amount and leave for about 1 minute, then, with dry gauze, remove the remains of capsaicin and wash the place with soap and water. In the treatment of acute pain occurring during and after the treatment, the place of administration should be cooled and oral analgesics administered.