Kutensa - instructions for use, doses, side effects, contraindications

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Dosage form: & nbsppatch

Composition:

Active substance: capsaicin 179 mg per 280 cm² (8.0% by weight);

Excipients: silicone adhesive BIO-PSA-4201 1098 mg per 280 cm² (49% by weight), silicone adhesive BIO-PSA4301 470 mg per 280 cm² (21% by weight), diethylene glycol monoethyl ether (MEDG) 430 mg per 280 cm² (19,2% by weight), silicone oil 12500 cSt 45 mg per 280 cm² (2% by weight), ethylcellulose N 50 18 mg by 280 cm² (0,8% by weight).

Cover film

Polyethylene terephthalate with silicone inner side.

Removable protective film

Polyester film, covered with fluoropolymer.

Cleansing gel

Macrogol 300 44.5 g per 50 g (89.1% by weight), carbomer 0.5 g per 50 g (1.0% by weight), water purified 4.9 g per 50 g (9.8% by weight weight), sodium hydroxide pellets (E524) 0.02 g per 50 g (0.03% by weight), disodium edetate 0.05 g per 50 g (0.1% by weight), butyl hydroxy anisole (E320) 0.01 g by 50 g (0.02% by weight).

Description:

Patch: transparent patch on the transparent removable protective layer, the protective layer covers the patch with long and short sides.

Gel: from transparent to opalescent, colorless, semi-solid, without mechanical inclusions.

Pharmacotherapeutic group:anesthetics, other local anesthetics

ATX: & nbsp

Other drugs for local anesthesia

Pharmacodynamics:

Capsaicin, or (E) -N - [(4-hydroxy-3-methoxyphenyl) methyl] -8-methylnon-6-enamide is a highly selective vanilloid receptor agonist with a transient receptor potential of type 1 (TRPV1). The initial effect of capsaicin is to activate skin pain receptors that express TRPV1, which leads to the appearance 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 "decreased sensitivity"; 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 and safety

According to the results of controlled clinical studies conducted in patients with painful HIV-associated neuropathy, the effectiveness of a single 30-minute application of the Kutens plaster band on the foot area is shown.Based on the results of controlled clinical trials conducted in patients with postherpetic neuralgia (PGN), the efficacy of the Kutens plaster is shown with a single 60-minute application to the painful areas of the skin of other localization. Reduction of pain intensity was noted already at 1 week; The effect of the therapy persisted throughout the 12-week study period.

The effectiveness of the Kutens plaster is confirmed both in monotherapy and in combination with other systemic drugs for the treatment of neuropathic pain.

Pharmacokinetics:

Capsaicin, contained in the preparation of Kutensa, is intended for delivery in the thickness of the skin. Data received in vitro (when studying the dissolution of the active substance and its penetration into the skin) showed that the release rate of capsaicin from the Kutensa preparation is linear throughout the entire period of application. According to the data in vitro It has been established that approximately 1% capsaicin is exposed during the 60-minute application of transepidermal and transdermal absorption.

The amount of capsaicin released from the patch in one hour is proportional tosurface area of the application.

Consequently, the estimated maximum possible total dose for an application area of 1000 cm² approximately 7 mg. Assuming that a patch area of 1000 cm² carries out the delivery of approximately 1% capsaicin 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 Scientific Committee of the European Union on Foodstuffs, the average consumption of capsaicin inside Europe is 1.5 mg / day (0.025 mg / kg / day for a person weighing 60 kg), and the maximum intake with food is 25-200 mg / day (up to 3.3 mg / kg / day for a person weighing 60 kg).

According to the pharmacokinetics data, after a 60-minute application of the patch Kutensa, a transitory, insignificant (<5 ng / ml) systemic exposure of capsaicin was observed in approximately one-third of patients with PGN 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.The maximum concentration of capsaicin detected in patients after a 60-minute application was 4.6 ng / ml; this concentration was fixed immediately after removal of the patch Kutensa. In most cases, a quantifiable concentration was detected at the time of removal of the Kutens plaster. 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.

The results of a population pharmacokinetic analysis of patients treated for 60 and 90 minutes demonstrated that the concentration of capsaicin in the blood plasma reaches a maximum value approximately 20 minutes after removal of the Kutens plaster and then rapidly decreases. The average half-life is approximately 130 minutes.

Indications:

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

Contraindications:

Hypersensitivity to the active substance or to any of the excipients.

Pregnancy and lactation:

Information on the use of capsaicin in pregnant women is limited or absent.

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

Based on data from pharmacokinetics studies in humans showing a transient, insignificant systemic absorption of capsaicin, the likelihood of an increased risk of developmental abnormalities resulting from the use of Kutense's patch is extremely low.

Nevertheless, care must be taken when prescribing the drug to pregnant women.

It is not known whether the capsaicin and / or its metabolites into human milk in human milk.

Available pharmacodynamic / toxicological data obtained in vivo, showed that capsaicin its metabolites penetrate the milk of lactating animals. Risk for newborn babies can not be ruled out. When applying Kutens plaster, breastfeeding should be discontinued.

There are no data on the impact on reproductive function of humans.

Toxicological study of reproductive function in rats showed a decrease in the number andpercentage of mobile spermatozoa and the number of pregnancies.

Dosing and Administration:

Only for cutaneous application.

Plaster Kutensa should be imposed on the most painful areas of the skin (at the same time it is allowed to use no more than 4 patches). The attending physician should identify the painful areas of the skin and note them. Kutens plaster should be applied to intact, non-irritated dry skin for 30 minutes in the area of the feet (for example, in HIV-associated neuropathy), and for 60 minutes to other areas (eg, postherpetic neuralgia).

Treatment with Kutens plaster is allowed to be repeated every 90 days, if this is necessary while maintaining or relapsing the pain syndrome.

A Kutens plaster should be applied by a doctor or a medical professional under the supervision of a doctor.

It is possible to use a mask and goggles, especially when sticking and removing the patch. Each time, when contacting the Kutens plaster and cleaning the plaster patch areas, nitrile gloves should be worn. Latex gloves are NOT suitable for this, since they do not provide the necessary protection.

Avoid direct contact of unprotected skin with a Kutens plaster, with used gauze or cleansing gel.

Precautions should be taken to avoid inadvertent contact with the patch or materials in contact with the skin. Failure to take precaution can lead to reversible reddening of the skin and a burning sensation (mucous membranes are especially sensitive), eye pain, irritation of the mucous membranes of the eyes, oral cavity and pharynx, coughing.

Plasters should not be applied to areas located near the eyes or mucous membranes.

If necessary, cut the hairline (not to shave) on the affected areas in order to facilitate a close contact of the skin with the plaster. The surface to be treated should be washed gently with soap and water. After hair removal and rinsing, the skin should be thoroughly dried.

Before applying Kutens plaster, the surface of the skin should be pretreated with a local anesthetic in order to reduce the associated discomfort.Local anesthetic should be treated the entire surface, which is applied to the patch Kutensa, as well as surrounding areas 1-2 cm wide. Local anesthetic should be used in accordance with the instructions for its use. In clinical trials, patients' skin was pre-treated for 4 minutes with 4% lidocaine for external use or a combination of lidocaine (2.5%) and prilocaine (2.5%) for external use.

The medicinal preparation of Kutensa is a plaster intended for single use, from which it is possible to cut out a site suitable for the shape and size of the affected area of the skin.

Plaster Kutensa should be cut before removing the protective film. Do not remove the protective film until the time of application. A diagonal cut on the protective film makes it easier to remove. It is necessary to separate the area of the protective film, bend it and apply an adhesive (adhesive) surface of the patch to the treated area of the skin. The plaster must be fixed immediately. With one hand, the protective film must be slowly and carefully separated from the lower surface,while smoothing the patch with the other hand on the surface of the skin to ensure full contact between the plaster and the skin, preventing the formation of air bubbles and moisture.

When applying Kutens plasters on foot, they can be wrapped around the back, side and plantar surfaces of the foot to completely cover the area being treated.

In order to ensure the contact of the patch Kutensa with the affected surface, it is allowed to use elastic socks or gauze bandage. Remove the patch of Kutensa carefully and slowly, turning it inward to minimize the risk of aerosol formation from capsaicin. After removing the patch of Cootenze, the surface of the skin should be copiously treated with a cleansing gel and leave it for at least one minute. The cleansing gel should be wiped off with a dry gauze cloth to remove the remains of capsaicin from the skin. After the cleansing gel is removed, the surface of the skin should be gently washed with water and soap. If acute pain occurs during and after the procedure, local cooling (eg cold compress) or analgesics for oral administration (eg short-acting opioid analgesics) should be used.

Use in patients with impaired renal or hepatic function

Dose adjustments in patients with impaired renal or hepatic function are not required.

Use in children of childhood

The safety and effectiveness of Kutens plaster in children under 18 years of age is not established. No data.

Instructions for disposal and handling

When handling the Kutens plaster and cleaning the areas of application, medical workers should wear nitrile gloves.

It is possible to use a mask and goggles.

Used and unused patches, as well as other materials that come into contact with the treated areas of the skin, must be disposed of, hermetically packed in a plastic bag for medical waste and placed in a suitable container for medical waste.

Side effects:

Thousand eighty-nine of the 1,826 patients (67%) who received Kutens plaster therapy in randomized controlled trials reported on the development of adverse reactions that the investigator considered drug-mediated. The most frequently reported adverse reactions such as transient burning at the site of application, pain, redness and itching.Unwanted reactions were transient, in most cases mild or moderate severity, and stopped on their own. In all controlled trials, the proportion of patients who discontinued therapy due to adverse events was 2% in the group receiving Kutens, and 0.9% in the control group. Table 1 lists all adverse reactions that occurred at a frequency greater than that in the control group and in more than one patient in controlled clinical trials among patients with postherpetic neuralgia and HIV-associated neuropathy with pain.

Reactions are presented in accordance with the distribution of organ systems and frequency. The frequency of the reaction is classified as follows: very frequent (≥1 / 10), frequent (≥1 / 100, <1/10) and infrequent (≥1 / 1000, <1/100).

Within each frequency category, adverse reactions are presented in order of decreasing severity.

Table 1: Frequency of treatment-related adverse reactions in controlled studies.

System of organs and frequency	Unwanted reaction
Infections and invasions
Infrequent	Shingles Herpes
From the nervous system
Infrequent	Perversion of taste, hypoesthesia, burning sensation
From the side of the organ of vision
Infrequent	Eye Irritation
From the heart
Infrequent	Atrioventricular block of the 1st degree, tachycardia, palpitation
From the side of the vessels
Infrequent	Increased blood pressure
On the part of the respiratory system, the organs of the thorax and the mediastinum
Infrequent	Cough, throat irritation
From the digestive system
Infrequent	Nausea
From the skin and subcutaneous tissues
Infrequent	Itching
From the musculoskeletal system and connective tissue
Infrequent	Pain in the extremities, muscle spasms
General violations and violations in the field of application
Very Frequent	Pain and redness in the place of application
Frequent	Itching, papules, blisters, swelling, swelling, dryness at the place of application
Infrequent	Urticaria, paresthesia, dermatitis, hyperesthesia, inflammation, reaction, irritation, (hemorrhagic elements) at the site of application, peripheral edema
Abnormalities detected during diagnostic studies
Infrequent	High blood pressure
Injuries, poisoning and reactions associated with procedures
Unknown	Second degree burns, accidental exposure components of the plaster (including pain in the eyes, irritation of the mucous membranes of the eyes, mouth and pharynx, cough)

In clinical trials, patients with peripheral neuropathic pain did not experience a reduction in neurologic function due to treatment, as evidenced by the results of a quantitative sensitivity test and a neurological examination. When performing studies on healthy volunteers, transient minimal changes in thermal sensitivity (from 1 to 2 ° C) and tingling sensations at the site of the application of the Kutens plaster patch were noted.

Overdose:

There were no cases of overdose. A Kutens plaster should be applied by a doctor or other medical professional under the supervision of a doctor. In this regard, the likelihood of an overdose is not high.

In case of an overdose, severe reactions can occur at the site of application, for example, pain, redness, itching. If you suspect an overdose, the patch should be carefully removed,apply a cleansing gel for one minute and wipe it with a dry gauze pad, after which the skin area should be gently washed with water and soap. If there are clinical indications, symptomatic treatment should be performed. There is no antidote to capsaicin.

Interaction:

Studies of interaction with other drugs have not been carried out, since only a transient minor systemic absorption of capsaicin was noted with the use of Kutens plaster.

Special instructions:

When handling Kutens plaster and washing the treated areas, medical workers should wear nitrile gloves. It is possible to use a mask and goggles.

Plaster Kutensa allowed to apply only on dry undamaged skin; Do not use the drug on the skin of the face, on the scalp and (or) close to the mucous membranes.

Reactions at the site of application, such as transient burning at the site of application, pain, redness and itching, occur frequently or very often. In addition, cases of burns, including second-degree burns, were reported in patients who used capsaicin patches.In patients with severe pain, the patch should be removed and the skin checked for chemical burns.

If the Kutens plaster is in contact with skin that is not planned for therapy, this skin area needs to be applied with a cleansing gel 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, the person should immediately stop contacting 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 application of the Kutens plaster in patients may experience a transient increase in arterial pressure (on average <8 mm Hg). During the period of the treatment procedure, it is necessary to control the level of blood pressure. 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 recently transferred cardiovascular disease, the risk of adverse cardiovascular reactions should be taken into account before initiating therapy with Kutens plaster because of the potential stress associated with the procedure.

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 patch Kutensa there was no observed reduction in neurological functions caused by therapy, after applying 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 Kutens plaster.

Diabetic Neuropathy

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

Cleansing gel

Cleansing gel for the patch Kutensa contains butylhydroxyanisole, which can cause local skin reactions (for example, contact dermatitis) or eye or mucous membrane irritation.

Effect on the ability to drive transp. cf. and fur:

The Kutens plaster has no or little effect on the ability to drive vehicles and work with various mechanisms.

Form release / dosage:

Plaster, 179 mg / 280 cm² (8.0%) complete with a cleansing gel.

Packaging:

Each patch, provided with a protective film with a slit to separate from the protective film, is packed in a paper sachet, coated with aluminum foil with a thermo-sealant layer of acrylic nitrile acrylic acid copolymer.

50 g of cleansing gel in a tube of high-density polyethylene.

1 patch complete with 1 tuba cleansing gel, liner and instructions for use in a pack of cardboard.

Storage conditions:

Kutens plaster: store on a flat surface in the original sachet and carton box, at a temperature of no higher than 25 ° C.

Cleansing gel: Store at a temperature not higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

After opening the package, Kutens should be applied within 2 hours.

Terms of leave from pharmacies:On prescription

Registration number:LP-002157

Date of registration:26.07.2013 / 19.02.2014

Expiration Date:26.07.2018

Date of cancellation:2017-11-28

The owner of the registration certificate:Astellas Farma Europe BVAstellas Farma Europe BV Netherlands

Manufacturer: & nbsp

LTS LOHMANN THERAPIE-SYSTEME, AG Germany

GP GRENZACH PRODUKTIONS, GmbH Germany

Representation: & nbspASTELLAS PHARMA YUROP BV ASTELLAS PHARMA YUROP BV Netherlands

Information update date: & nbsp28.11.2017

Illustrated instructions

Instructions

Kutenza (Qutenza)