Versatis - instructions for use, dose, side effects, contraindications

Excipients: purified water 3.367 g, glycerol 2.520 g, sorbitol 2,800 g, polyacrylic acid solution 20% 1,400 g, sodium polyacrylate 400-600 mPa·with 0.700 g, carmellose sodium 90-168 mPa·0.700 g, propylene glycol 0.700 g, urea 0.420 g, kaolin 0.210 g, tartaric acid 0.210 g, gelatin 0.147 g, polyvinyl alcohol (75,000) 0.0588 g, Aluminum dihydroxyaminoacetate (aluminum glycinate) 0.0322 g, disodium edetate 0.014 g, methyl parahydroxybenzoate 0.014 g, propyl parahydroxybenzoate 0.007 g, non-woven fabric 1,750 g, plastic film (polyethene terephthalate, PET) 0.742 g

The size of the plaster: length from 13.3 to 14.7 cm, width from 9.5 to 10.5 cm.

Description:

From white to light yellow, polymer adhesive (sticky) material with a weak characteristic odor, evenly distributed on one side of the nonwoven fabric and covered with plastic film. On the non-woven material the inscription is engraved "Lidocaine 5 %".

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B Amides

N.01.B.B.02 Lidocaine

C.01.B.B.01 Lidocaine

C.01.B.B Antiarrhythmic drugs Ib class

Pharmacodynamics:

Versatis contains lidocaine, an acetamide derivative. The mechanism of action is associated with the stabilization of neuronal membranes, which is believed to be the result of blockade of sodium channels.

When applied locally to intact skin, a therapeutic effect is sufficient to relieve the pain syndrome.

Pharmacokinetics:

Suction:

With a single or multiple application of the Versasitis patch in the maximum recommended dose (simultaneous application of three patches of 12 hours), only 3 ± 2% of lidocaine contained in patch, enters the systemic circulation. The concentration in the blood plasma after applying the maximum recommended dose of the drug in patients without a postherpetic neuralgia clinic was 84-125 ng / ml. In patients with postherpetic neuralgia - 52 ng / ml.

Distribution:

The volume of distribution does not depend on age and is lower in patients with chronic heart failure, increases with hepatic insufficiency.

Blood plasma proteins are associated with 70 % lidocaine, penetrating into the systemic circulation after the cutaneous application.Penetrates through blood-brain and placental barriers through passive diffusion.

Metabolism:

Lidocaine is rapidly metabolized in the liver with the formation of several metabolites. The main pathway of metabolism N-dealkylation to form monoethylglycinexylidide (MEGC) and glycinexylidide (HA), metabolites have less pharmacological activity than lidocaine and are present in lower concentrations. Metabolites are hydrolyzed to 2,6-xylidine, which is converted to 4-hydroxy-2,6-xylidine by conjugation.

It is not established whether 2.6-xilidine is pharmacologically active, however, when studying on biological models, 2,6-xylidine potentially has a carcinogenic effect. Kinetic analysis revealed that with daily applications lasting up to one year, the maximum concentration of 2,6-xylidine on average is 9 ng / ml. Lidocaine and its metabolites (monoethylglycinexylidide, glycinexylidide and 2,6-xylidine) do not accumulate in the body, equilibrium concentration is reached within the first four days of use.

With an increase in the number of simultaneously applied patches from one to three, the concentration of lidocaine in the plasma increases more slowly proportional relationship.

Excretion:

Lidocaine and its metabolites are excreted in the urine (more than 85% in the form of metabolites, less than 10% in unchanged form). The main metabolite in urine is the conjugate of 4-hydroxy-2,6-xylidine, which is approximately 70-80% of the dose excreted in the urine. Metabolite 2,6-xylidine is excreted in the urine at a concentration of less than 1% of the dose received. The half-life of lidocaine after skin patch application is 7.6 hours.

With cardiac, renal or hepatic insufficiency, it is possible slowing the excretion of lidocaine and its metabolites.

Indications:

Hneuropathic pain associated with a previous history of herpetic infection (herpes zoster), postherpetic neuralgia.

Contraindications:

- hypersensitivity of allergic and non-allergic genesis to the active and auxiliary substances of the drug;

- hypersensitivity of allergic and non-allergic genesis to local anesthetics of the amide group (eg, bupivacaine, etidokain, mepivacaine and prilocaine);

- inflammation or disruption of skin integrity at the site of the patch application (eg, rashes herpes zoster, atopic dermatitis or wounds).

Carefully:It is used with caution in severe heart, kidney or liver failure (cm. "Special instructions").

Pregnancy and lactation:

Lidocaine penetrates the placenta. Data on the use of lidocaine in pregnant women are absent, so during pregnancy the drug is used if the expected benefit to the mother exceeds the potential risk to the fetus. Lidocaine excreted in breast milk. Since the metabolism of lidocaine occurs relatively quickly and predominantly in the liver, it can be expected that very small amounts of lidocaine can be excreted in breast milk. There are no data on the application of the Versasitis plaster in nursing mothers, so during breastfeeding the drug is used only if the expected benefit for the mother exceeds the potential risk for the child.

Dosing and Administration:

The patch is for external use only. The patch is glued to the skin in the area of pain once a day for up to 12 hours. At the same time, no more than 3 patches can be used. If necessary, the patch can be cut into pieces before removing the plastic protective film.The patch should be glued on intact, dry, non-inflamed skin (after complete healing of herpetic eruptions) covering the area of pain.

Then remove the adhesive tape and take a break for at least 12 hours. Do not reuse the removed adhesive.

The plaster is adhered to the skin immediately after extraction from the sachet and removal of the plastic film from the adhesive layer. Hair must be cut with scissors (do not shave). The effectiveness of therapy should be reassessed after 2-4 weeks from the start of treatment. If, at these times, the response to therapy is insufficient or the therapeutic effect is determined only by the protective properties of the patch, treatment should be discontinued. It is necessary to regularly evaluate the effectiveness of therapy to determine the optimal number of simultaneously applied patches needed to cover the area pain, or to increase the periods of time between patch applications.

The use of plaster Versasitis in the age of 18 years is not recommended.

There is no data on the safety and efficacy of the Versatitis patch in patients under the age of 18 years.

After sticking the patch, hands and eyes should be avoided, hands should be washed immediately.

The used patch contains the active substance. Dispose of the adhesive immediately after use.

After removal from the skin, the patch should be folded in half an adhesive side inward, so that the surface containing the active substance is not visible. Used patches should not be available to children or pets.

Side effects:

Adverse reactions were noted in about 16 % patients who used Versatis. Since the drug is applied externally, in most cases, undesirable reactions are local in nature and occur in the area of application of the patch. The most frequent adverse reactions are the following local reactions in the field of patch application: erythema, rash (before vesicular), itching, burning sensation, dermatitis at the site of application.

The table below shows the adverse reactions identified in the clinical use of the drug in postherpetic neuralgia. They are listed by organ systems and frequency of occurrence. The frequency of occurrence is defined as follows: "very often" (≥ 1/10), "often" (≥ 1/100 - <1/10), "infrequently" (≥ 1/1000 - <1/100), "rarely" (≥ 1/10000 - <1/1000), "very rarely" (<1/10000), "insufficient data" (based on the available data, it is impossible to estimate the frequency).

System of organs	Adverse Reactions
Disturbances from the skin and subcutaneous tissues
Infrequently	Lesions and damage to the skin
General disorders and local reactions
Often	Reactions in the place of application

The following adverse reactions were noted in the post-marketing application of the drug:

System of organs	Adverse Reactions
Immune system disorders
Rarely	Anaphylactic reaction, hypersensitivity
General disorders and local reactions
Rarely	Breach of the integrity of the skin

All adverse reactions had a weak or moderate intensity. In less than 5% of cases, the development of adverse reactions was the reason for discontinuation of the drug.

With the correct use of the drug, the development of systemic adverse reactions is unlikely, since when treated with a patch containing 5% lidocaine, the inflow of active substance into the systemic blood flow is insignificant (see section "Pharmacokinetics"). Systemic adverse reactions associated with the use of lidocaine are identical to reactions characteristic of local anesthetics of the amide group (see section "Overdose").

If any of the following adverse reactions appear in the manual, or any other side effects not indicated in the instructions are noted, tell your doctor.

Overdose:

Overdose of lidocaine with the use of a patch Versasitis is unlikely. Overdose can not be excluded due to incorrect use of the drug (e.g., use more than 3 plasters simultaneously applique patch for more than 12 hours, or the use of adhesive in areas of damaged skin), in such cases, the plasma concentration of lidocaine may be increased. Symptoms of overdose can be: dizziness, vomiting, drowsiness, convulsions, mydriasis, bradycardia, arrhythmia and shock. In case of overdose, lidocaine may interact with β-blockers, inhibitors of the isoenzyme CYP3A4 (for example, imidazole derivatives, macrolides) and antiarrhythmic drugs.

When suspected of an overdose, the patch should be removed from the skin and measures taken to maintain the vital functions of the body. There is no antidote to lidocaine.

Interaction:

In the accumulated experience of using the drug, there was no clinically significant interaction with other drugs.

Since the maximum concentration of lidocaine in the blood plasma is low, the occurrence of clinically significant pharmacokinetic interaction is unlikely.

Although the absorption of lidocaine through the skin is usually low, caution when using a patch containing lidocaine 5%, in patients receiving class I antiarrhythmic drugs (eg, tocaine, mexiletine) or other local anesthetics, since the risk of developing an additive systemic effect is not ruled out.

Special instructions:

The patch should not be used on mucous membranes. Avoid contact with the area of the eyes.

The patch contains propylene glycol, which can cause skin irritation, as well as methyl parahydroxybenzoate and propyl parahydroxybenzoate, which can cause allergic reactions (possibly delayed). Caution should be exercised when using the Versatitis patch in patients with severe cardiac, renal or hepatic insufficiency. After the first opening of the sachet, the drug should be used within 14 days, the opened sachet must be stored tightly closed. The drug should not be stored in the refrigerator or frozen.

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

Since systemic absorption is minimal,There is no reason to assume that there is an effect on the ability to drive and the ability to work with machinery.

Form release / dosage:Patch.

Packaging:

5 patches in the sachet. 1, 2 or 6 sachets in a cardboard pack together with instructions for use.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Do not store in the refrigerator and do not freeze. After opening, store the sachet tightly closed. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date indicated on the package. The patches should be used within 14 days after the opening of the sachet.

Terms of leave from pharmacies:On prescription

Registration number:LS-001775

Date of registration:23.09.2011

Expiration Date:Unlimited

The owner of the registration certificate:Grünenthal GmbHGrünenthal GmbH Germany

Manufacturer: & nbsp

TEIKOKU SEIYAKU, Co. Ltd. Japan

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Versatis (Versatis)