Versatis, 700 mg patch 30 pcs

Versatis contains lidocaine, an acetamide derivative.

The mechanism of action is associated with stabilization of neuronal membranes, which is believed to be the result of blockade of sodium channels.

When applied topically to intact skin a therapeutic effect sufficient to relieve pain syndrome occurs.

Pharmacokinetics

Absorption:

When Versatis patch is administered once or repeatedly at the maximum recommended dose (simultaneous application of three patches lasting 12 hours), only 3 ± 2% of the lidocaine contained in the patch enters the systemic bloodstream.

Plasma concentrations after application of the maximum recommended dose of the drug in patients without postherpetic neuralgia clinic were 84 – 125 ng/ml.

In patients with postherpetic neuralgia – 52 ng/ml.

Distribution:

Distribution volume is independent of age and decreased in patients with chronic heart failure, increased in liver failure.

70% of lidocaine is bound to blood plasma proteins and penetrates into the systemic bloodstream after cutaneous application.

It penetrates through the blood-brain and placental barriers by passive diffusion.

Metabolism:

Lidocaine is rapidly metabolized in the liver to form several metabolites.

The main metabolic pathway is N-dealkylation to form monoethylglycinkylidide (MEGC) and glycinkylidide (GC), the metabolites have less pharmacological activity than lidocaine and are present in lower concentrations.

The metabolites are hydrolyzed to 2,6-xylidine, which is converted to 4-hydroxy-2,6-xylidine by conjugation.

It has not been determined whether 2,6-xylidine has pharmacological activity; however, when studied in biological models, 2,6-xylidine is potentially carcinogenic.

Kinetic analysis revealed that with daily applications lasting up to one year, the maximum concentration of 2,6-xylidine averaged 9 ng/mL.

Lidocaine and its metabolites (monoethylglycincylidide, glycincylidide and 2,6-xylidine) do not accumulate in the body, with equilibrium concentration reached within the first four days of application.

As the number of patches used simultaneously increases from one to three, plasma lidocaine concentrations increase more slowly than the proportional ratio.

Excretion:

Lidocaine and its metabolites are excreted in the urine (over 85% as metabolites, less than 10% unchanged).

The main metabolite in the urine is 4-hydroxy-2,6-xylidine conjugate, accounting for approximately 70% to 80% of the dose excreted with the urine.

The metabolite 2,6-xylidine is excreted in the urine at a concentration of less than 1% of the dose received.

The elimination half-life of lidocaine after skin application of the patch is 7.6 h.

Cardiac, renal or hepatic insufficiency may slow the elimination of lidocaine and its metabolites.

Indications

Neuropathic pain associated with a previous herpetic infection (Herpes zoster), postherpetic neuralgia.

Pharmacological effect

Versatis contains lidocaine, an acetamide derivative.

The mechanism of action is related to the stabilization of neuronal membranes, which is believed to be the result of blockade of sodium channels.

When applied topically to intact skin, a therapeutic effect occurs sufficient to relieve pain.

Pharmacokinetics

Suction:

With single or repeated use of the Versatis patch at the maximum recommended dose (simultaneous application of three patches for 12 hours), only 3 ± 2% of the lidocaine contained in the patch enters the systemic circulation.

The concentration in blood plasma after using the maximum recommended dose of the drug in patients without clinical symptoms of postherpetic neuralgia 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 reduced in patients with chronic heart failure and increases in liver failure.

70% of lidocaine, which penetrates into the systemic circulation after cutaneous application, binds to blood plasma proteins.

Penetrates through the blood-brain and placental barriers by passive diffusion.

Metabolism:

Lidocaine is rapidly metabolized in the liver to form several metabolites.

The main route of metabolism is N-dealkylation to form monoethylglycine xylidide (MEGC) and glycine xylidide (GK), metabolites that have less pharmacological activity than lidocaine and are present in lower concentrations.

Metabolites are hydrolyzed to 2,6-xylidine, which is converted by conjugation to 4-hydroxy-2,6-xylidine.

It has not been established whether 2,6-xylidine has pharmacological activity, however, when studied in biological models, 2,6-xylidine has a potential carcinogenic effect.

Kinetic analysis revealed that with daily applications for up to one year, the maximum concentration of 2,6-xylidine averaged 9 ng/ml.

Lidocaine and its metabolites (monoethylglycine xylidide, glycine xylidide and 2,6-xylidine) do not accumulate in the body; equilibrium concentration is achieved within the first four days of use.

When the number of simultaneously applied patches increases from one to three, the concentration of lidocaine in plasma increases more slowly than the proportional ratio.

Removal:

Lidocaine and its metabolites are excreted in the urine (more than 85% in the form of metabolites, less than 10% unchanged).

The main metabolite in urine is a 4-hydroxy-2,6-xylidine conjugate, accounting for approximately 70 – 80% of the dose excreted in the urine.

The metabolite 2,6-xylidine is excreted in the urine in a concentration of less than 1% of the dose received.

The half-life of lidocaine after skin application of the patch is 7.6 hours.

In case of cardiac, renal or liver failure, the elimination of lidocaine and its metabolites may be delayed.

Special instructions

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

Versatis patch contains propylene glycol, which may cause skin irritation, as well as methyl parahydroxybenzoate and propyl parahydroxybenzoate, which may cause allergic reactions (possibly delayed).

Caution should be exercised when using the Versatis patch in patients with severe cardiac, renal or hepatic impairment.

After the first opening of the sachet, the drug must be used within 14 days; the opened sachet must be stored tightly closed. The drug should not be stored in the refrigerator or frozen.

Impact on the ability to drive vehicles and operate machinery

Since systemic absorption is minimal, there is no evidence to suggest an effect on the ability to drive or operate machinery.

Active ingredient

Lidocaine

Composition

One patch contains:

Active substance:

Lidocaine 700 mg/patch;

Excipients:

Purified water 3367 mg,

Glycerol 2520 mg,

Sorbitol 2800 mg,

Polyacrylic acid solution 20% 1400 mg,

Sodium polyacrylate 400-600 mPa s 700 mg,

Carmellose sodium 90-168 mPa s 700 mg,

Propylene glycol 700 mg,

Urea 420 mg,

Kaolin 210 mg,

Tartaric acid (tartaric) 210 mg,

Gelatin 147 mg,

Polyvinyl alcohol (75,000) 58.8 mg,

Aluminum dihydroxyaminoacetate (aluminum glycinate) 32.2 mg,

Disodium edetate 14 mg,

Methyl parahydroxybenzoate 14 mg,

Propyl parahydroxybenzoate 7 mg,

Nonwoven fabric 1750 mg,

Plastic film (polyethylene terephthalate, PET) 742 g.

Patch size: length from 13.3 to 14.7 cm, width from 9.5 to 10.5 cm.

Pregnancy

Versatis should not be used during pregnancy and lactation (breastfeeding).

Contraindications

Increased sensitivity of allergic and non-allergic origin to the active and excipients of the drug;
increased sensitivity of allergic and non-allergic origin to local anesthetics of the amide group (for example, bupivacaine, etidocaine, mepivacaine and prilocaine);
inflammation or disruption of the integrity of the skin at the site of application of the patch (for example, herpes zoster rash, atopic dermatitis or wounds).
With caution
Use with caution in severe cardiac, renal or hepatic impairment (see “Special Instructions”).

Side Effects

headache,
dizziness,
numbness of the tongue and oral mucosa,
lowering blood pressure,
decrease in heart rate,
a burning sensation when the aerosol hits the anesthetized surface (stops a few seconds after the onset of anesthesia).

Interaction

In the accumulated experience of using the drug, there were no clinically significant interactions with other drugs.
Because the maximum plasma concentration of lidocaine is low, a clinically significant pharmacokinetic interaction is unlikely to occur.

Although the absorption of lidocaine through the skin is usually low, caution should be exercised when using the lidocaine 5% patch in patients receiving class I antiarrhythmic drugs (eg, tocainide,

mexiletine) or other local anesthetics, since the risk of additive systemic effects cannot be excluded.

Overdose

An overdose of lidocaine when using the Versatis patch is unlikely.

Overdose cannot be excluded if the drug is used incorrectly (for example, using more than 3 patches at the same time, applying the patch for more than 12 hours, or using the patch on areas of damaged skin); in such cases, the concentration of lidocaine in the blood plasma may increase.

Symptoms of overdose may include: dizziness, vomiting, drowsiness, convulsions, mydriasis, bradycardia, arrhythmia and shock. In case of overdose, interaction of lidocaine with β-blockers, inhibitors of the CYP3A4 isoenzyme (for example, imidazole derivatives, macrolides) and antiarrhythmic drugs is possible.

If an overdose is suspected, 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.

Storage conditions

Store at a temperature not exceeding 25 °C.

Do not refrigerate or freeze.

After opening, keep the sachet tightly closed.

Keep out of the reach of children.

Shelf life

3 years. Do not use after the expiration date stated on the package.

The patches must be used within 14 days after opening the sachet.

Manufacturer

Grünenthal GmbH, Germany