Versatis

General characteristics. Structure:

Active agent: lidocaine of 700 mg / plaster;

Excipients: the water purified 3367 mg, глицерол 2520 mg, sorbitol of 2800 mg, solution of the polyacrylic acid of 20% 1400 mg, sodium polyacrylate 400-600 мПас 700 mg a karmelloza of sodium 90-168 мПас 700 mg, propylene glycol of 700 mg, urea of 420 mg, a kaolin 21O of mg, tartaric acid (tartarovy) 210 mg, gelatin of 147 mg, polyvinyl alcohol (75 000) 58,8 of mg, aluminum dihydroxyaminoacetate (aluminum глицинат) 32,2 mg, dinatrium эдетат 14 mg, methylparahydroxybenzoate of 14 mg, пропилпарагидроксибензоат 7 mg, nonwoven fabric of 1750 mg, plastic foil (полиэтилентерфталат, PET) 742 g.
Plaster size: length is from 13,3 to 14,7 mm, width is from 9,5 to 10,5 mm.

Pharmacological properties:

Pharmacodynamics. Versatis contains lidocaine, derivative acetamide. The mechanism of action is connected with stabilization of membranes of neurons that as believe, is result of blockade of natrium channels. At topical administration on the unimpaired skin there is a therapeutic effect sufficient for removal of a pain syndrome.

Pharmacokinetics. Absorption: at single or repeated use of a plaster Versatis in the maximum recommended dose (simultaneous application of three plasters lasting 12 watch), only 3 ± 2% of the lidocaine which is contained in a plaster comes to a system blood stream. Concentration in a blood plasma after use of the maximum recommended drug dose for patients without clinic of post-herpetic neuralgia made 84 - 125 ng/ml. Patients with post-herpetic neuralgia have 52 ng/ml.

Distribution: the volume of distribution does not depend on age and is reduced at patients with chronic heart failure, increases at a liver failure. 70% lidocaine and, getting into a system blood stream after cutaneous application contact proteins of a blood plasma. Gets through hematoencephalic and placental barriers by passive diffusion.

Metabolism: lidocaine is quickly metabolized in a liver with formation of several metabolites. The main way of metabolism N-dealkylation with formation of a monoetilglitsinksilidid (MEGK) and glitsinksilidid (Civil Code), metabolites have smaller pharmacological activity, than lidocaine and are present at smaller concentration. Metabolites are hydrolyzed to 2,6 xylidine and which will be transformed by conjugation in 4-gidroksi-2,6 xylidine. It is not established whether 2,6 xylidine have pharmacological activity, however, when studying on biological models 2,6-xylidine potentially has cancerogenic effect. The kinetic analysis revealed that at daily applications by duration up to one year, the maximum concentration 2,6 xylidines on average makes 9 ng/ml. Lidocaine and its metabolites (моноэтилглицинксилидид, глицинксилидид and 2,6 xylidine) do not collect in an organism е, equilibrium concentration is reached within the first four days of use. At increase in quantity of at the same time applied plasters from one to three, concentration of lidocaine in plasma increases more slowly than a proportional ratio.

Removal: lidocaine and its metabolites are removed with urine (more than 85% in the form of metabolites, less than 10% in not changed look). The main metabolite in urine - the conjugate of 4-hydroxy-2,6-xylidine making about 70 — 80% of the dose removed with urine. The metabolite 2,6 xylidine is removed with urine in concentration of less than 1% of the received dose. The lidocaine elimination half-life after skin application of a plaster makes 7,6 h. At a heart, renal or liver failure delay of removal of lidocaine and its metabolites is possible.

Indications to use:

- the neyropatichesky pain associated with earlier postponed herpes infection (Herpes zoster), post-herpetic neuralgia.

Route of administration and doses:

The plaster is intended for external use. The plaster is pasted on skin in the field of pain for the period till 12 o'clock once a day. It is at the same time possible to apply no more than 3 plasters. If necessary the plaster can be cut on a part before removal of a plastic protective foil. The plaster has to be pasted on the unimpaired, dry, uninflammed skin (after full healing of herpetic rashes) covering area of pain.

Then the plaster is removed and not less than 12 hours do a break. Do not reuse the removed plaster.

The plaster is pasted to skin right after extraction from a sachet and removal of plastic foil from a sticky layer. Hair need to be sheared scissors (not to shave off). Efficiency of therapy needs to be estimated repeatedly in 2-4 weeks from an initiation of treatment. If in these terms the response to therapy is insufficient or the therapeutic effect is defined only by protective properties of a plaster, treatment should be stopped. It is regularly necessary to estimate efficiency of therapy for determination of optimum quantity of at the same time applied plasters necessary for a covering of area of pain, or for increase in spans between applications of a plaster. Use of a plaster Versatis aged up to 18 years is not recommended.

Patients have no data on safety and efficiency of a plaster Versatis aged up to 18 years.

After gluing of a plaster it is necessary to avoid contact of hands with eyes, it is necessary to wash up hands at once.

The used plaster contains active ingredient. Utilize a plaster right after use.

After removal about skin, a plaster it has to be put in half by the sticky party inside so that the surface containing active ingredient was not visible. The used plasters should not be available to children or domestic animals.

Features of use:

The plaster should not be applied on mucous membranes. It is necessary to avoid contact of a plaster with area of eyes.

The plaster contains propylene glycol which can cause irritation of skin, and also methylparahydroxybenzoate and пропилпарагидроксибензоат which can cause the allergic reactions which are (perhaps delayed).

It is necessary to be careful when using a plaster Versatis at patients with a heavy heart, renal or liver failure. After the first opening of a sachet, drug needs to be used within 14 days, densely closed need to store the opened sachet. Drug should not be stored in the refrigerator or to freeze.

Influence on ability to drive the car and to work with mechanisms:
As system absorption is minimum, there are no bases to assume existence of influence on ability to drive the car and an opportunity to work with mechanisms.

Side effects:

Side reactions were noted approximately at 16% of the patients applying Versatis. As drug is used outwardly, in most cases undesirable reactions have local character and arise in a plaster scope. The most frequent undesirable reactions are the following local reactions in the field of application of a plaster: an erythema, rash (to vesicular), a skin itch, burning sensation, dermatitis in the place of application.

In the table the side reactions revealed at a clinical use of drug at post-herpetic neuralgia are included below. They are listed on systems of bodies and frequency of emergence. Frequency of emergence is defined as follows: "it is very frequent" (≥ 1/1 0), is "frequent" (≥ 1/100 - <1/10), "infrequently" (≥ 1/1000 - <1/100), is "rare" (≥ 1/10000 - <1/1000), "it is very rare" (≤ 1/1 0000), "there are not enough data" (on the basis of the available data it is impossible to estimate frequency).

System of bodies	Side reaction
Disturbances from skin and hypodermic fabrics
Infrequently	Defeats and injury of skin
General frustration and local reactions
Very often	Reactions in the place of application

The following side reactions were noted at post-marketing use of drug.

System of bodies	Side reaction
Disturbances from immune system
Very seldom	Anaphylactic reaction, hypersensitivity
General frustration and local reactions
Very seldom	Disturbance of integrity of an integument

All side reactions had weak or average intensity. Less than in 5% cases development of side reactions was the cause of phase-out of drug.

At the correct use of drug development of system side reactions is improbable as at treatment by the plaster containing 5% lidocaine, intake of active ingredient in a system blood stream is insignificant (see the section "Pharmacokinetics"). The system undesirable reactions connected using lidocaine are identical to the reactions characteristic of local anesthetics of amide group (see the section "Overdose").

If there were any side reactions specified in the instruction, or any other side effects which are not specified in the instruction are noticed, report about it to the doctor.

Interaction with other medicines:

In the accumulated experience of use of drug clinically significant interaction with other drugs was not noted.

As the maximum concentration of lidocaine in a blood plasma is low, emergence of clinically significant pharmacokinetic interaction is improbable.

Though absorption of lidocaine through skin is usually low, it is necessary to be careful at use пластыр I, containing lidocaine of 5%, at the patients receiving antiarrhytmic drugs I of a class (for example, tokain д, мексилетин) or others local anesthetic and as the risk of development of the additive system effect is not excluded.

Contraindications:

- hypersensitivity of allergic and not allergic genesis to acting and to excipients of drug;
- hypersensitivity of allergic and not allergic genesis to local anesthetics of group of amides (for example, to bupivacaine, an etidokain, a mepivakain and a prilokain);
- an inflammation or disturbance of integrity of integuments in the place of application of a plaster (for example, herpes zoster rashes, atopic dermatitis or wounds).

With care:
It is applied with care at a heavy heart, renal or liver failure (see. "Special instructions").

Use at pregnancy and feeding by a breast:
Lidocaine gets through a placenta. Data on use of lidocaine for pregnant women are absent therefore during pregnancy drug is used if the expected advantage for mother exceeds potential risk for a fruit. Lidocaine is emitted with breast milk. As metabolism of lidocaine happens rather quickly and preferential in a liver, it is possible to expect that extremely insignificant amounts of lidocaine can be removed with breast milk. Nursing mothers have data on use of a plaster no Versatis therefore during breastfeeding drug is used, only if the expected advantage for mother exceeds potential risk for the child.

Overdose:

The overdose of lidocaine at use of a plaster Versatis is improbable. The overdose cannot be excluded at the wrong use of drug (for example, use more than 3 plasters at the same time, application of a plaster more than for 12 hours or use of a plaster on sites of the injured skin), in such cases concentration of lidocaine in a blood plasma can increase. Can be symptoms of overdose: dizziness, vomiting, drowsiness, spasms, mydriasis, bradycardia, arrhythmia and shock. At overdose interaction of lidocaine with p - adrenoblockers, CYP3A4 isoenzyme inhibitors (for example, derivatives an imidazole and, macroleads) and antiarrhytmic drugs is possible.

At suspicion on overdose the plaster has to be removed from skin and measures of maintenance of vital signs of an organism are taken. There is no antidote to lidocaine.

Storage conditions:

To store at a temperature not above 25 °C. Not to store in the refrigerator and not to freeze. After opening to store the sachet which are densely closed. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Plaster. 5 plasters in a sachet. 1, 2 or 6 sachets in a cardboard pack together with the application instruction.