Relief® [Lidocaine, fluocortolone]

Pharmacological properties

fluocortolone pivalate suppresses inflammatory and allergic skin reactions, and also facilitates subjective manifestations, such as itching, burning and pain; reduces capillary expansion, interstitial cell edema and tissue infiltration, inhibits capillary proliferation.

Lidocaine hydrochloride is a standard local anesthetic that has been used in medical practice for many years. Due to the analgesic effect, it is effective in the use of suppositories and ointments intended for the treatment of disorders associated with hemorrhoidal pathology. A decrease in the severity of pain and itching is associated with inhibition of afferent nerve impulses.

Pharmacokinetics After a single rectal administration by healthy male volunteers, the maximum systemic absorption was about 5% for suppositories and 15% for a cream dose of fluocortolone pivalate and about 24 and 30%, respectively, of a dose of lidocaine hydrochloride (active substances labeled with a radioactive isotope).

Indications

Rectal cream. for symptomatic treatment of pain and inflammation with:

• hemorrhoids;
• proctitis;
• eczema in the anus.

Suppositories. For symptomatic treatment of pain and inflammation with:

• hemorrhoids;
• proctite.

Application

Rectal cream should be used 2 times a day, morning and evening (approximately 1 g per 1 application). in the first days of treatment, the drug can be used 3 times a day. after improvement, the use of the drug 1 time per day is often sufficient. Relif® Pro rectal cream is recommended after defecation. Before using the drug, the anal area should be carefully cleaned.

The duration of the full course of treatment should not exceed 2 weeks.

Apply rectal cream Relief^® Pro on the tip of the finger to the anus, overcoming the sphincter resistance with the tip of the finger. One dose of application at the tip of the finger is the amount that is obtained after a single extrusion from the tube and applied to the surface of the index finger of an adult. If necessary, the introduction of rectal cream Relief^® About the inside of the rectum, screw the applicator onto the tube and insert the tip into the anus. A small amount of cream can be entered by lightly pressing the tube.

Suppositories. Apply 1 suppository 2 times a day, morning and evening. After improvement, 1 suppository 1 time per day or 1 time per 2 days is often sufficient. Relif suppositories recommended^® Pro after defecation. Before the introduction of the suppository, the anal area should be carefully cleaned.

Insert the suppository deep into the anus. Duration of treatment with Relif suppositories^® Pro should not exceed 2 weeks.

If the suppositories become soft due to the influence of high temperature, dip them in cold water before removing the shell.

Contraindications

Relif® is contraindicated in case of local infections in the injection zone, as well as in the presence of clear symptoms of the following pathological conditions in the respective zones:

• specific skin lesions (syphilis, tuberculosis);
• chickenpox;
• reactions after vaccination;
• genital herpes;
• smallpox;
• other viral infections;
• primary bacterial or fungal infections;
• secondary skin infections in the absence of appropriate antibiotic therapy;
• patients with hypersensitivity to other local amide type anesthesia (e.g. bupivacaine, mepivacaine and lidocaine).

Relief^® Pro should not be used with hypersensitivity to active substances or any of the excipients.

Side effects

Cases of undesirable effects are determined on the basis of a combination of clinical trials conducted with 661 patients.

On the part of the skin and subcutaneous tissue, including allergic reactions, often - pain and burning sensation at the site of application; infrequently - irritation at the site of use.

After prolonged therapy with Relief^® Pro (which exceeds 4 weeks) there is a risk of developing local pathological conditions of the skin, such as atrophy, striae or telangiectasia.

Adverse reactions due to lidocaine hydrochloride: anaphylactic reactions. The development of systemic adverse reactions is unlikely, since with the use of the drug, the intake of lidocaine into the systemic circulation is negligible; systemic adverse reactions associated with lidocaine, identical in manifestations to those associated with local anesthetics of the amide group.

special instructions

When using Relif® Pro rectal cream in the genital area or anus, excipients such as soft white paraffin and mineral oil can reduce the strength of latex condoms and thus compromise their reliability.

With fungal infections, additional special antifungal therapy is required.

Avoid contact of the cream with the eyes. Wash hands thoroughly after use.

Cetostearyl alcohol can cause local skin reactions (contact dermatitis).

The use of drugs for topical use, especially for a long period, can cause sensitization phenomena. In this case, the use of these drugs should be discontinued and appropriate treatment should begin. If topical preparations are applied to large areas of the body, to damaged skin, or under an airtight dressing, corticosteroids can be absorbed in amounts that can cause unwanted systemic effects. Do not use under occlusive dressings on the perineum. Inhibition of adrenal function may develop even without occlusion. Local use of corticosteroids in high doses can lead to the absorption of a systemically active amount of corticosteroids. There is literature data on the development of cataracts in patients using corticosteroids for a long period, therefore, in order to exclude manifestations of the systemic effect of corticosteroids, one should be aware of their possible role in the development of cataracts.

Use with caution in acute diseases, in debilitated patients, elderly patients; patients with severe heart, kidney, and liver failure.

Relif suppository contact should be avoided.^® About with eyes. After their use, it is recommended to wash your hands thoroughly.

With fungal infections, additional special antifungal therapy is required.

There is literature data on the development of cataracts in patients using corticosteroids for a long period, therefore, in order to exclude manifestations of the systemic effect of corticosteroids, one should be aware of their possible role in the development of cataracts.

Use with caution in debilitated patients, elderly patients; patients with severe heart, kidney, and liver failure.

Use during pregnancy and lactation. Relief Application Data^® Pros during pregnancy are inadequate. Studies of glucocorticoids that have been conducted in animals have revealed the presence of reproductive toxicity.

Some epidemiological studies indicate the possibility of increasing the risk of palatoschisis in newborns if their mothers received treatment with systemic use of glucocorticoids in the first trimester of pregnancy. Palatoschisis (cleft palate) is a rare pathology and, despite the fact that the systemic use of glucocorticoids causes a teratogenic effect, their use can be considered the cause of this pathology only if the number of cases increases to 1 or 2 per 1000 women taking this treatment during pregnancy.

Data related to the topical use of glucocorticoids during pregnancy are insufficient, but the risk can be considered low, since glucocorticoids, when applied topically, are characterized by very low systemic bioavailability.

In general, topical preparations containing glucocorticoids should not be used in the first trimester of pregnancy.

When prescribing treatment to pregnant women and women during lactation, a careful assessment of the clinical indications for use should be made.^® Pro, as well as the ratio of risk and benefit. In particular, prolonged use of the drug should be avoided.

Children. It is not recommended for use in children due to the lack of data on safety and effectiveness.

The ability to influence the reaction rate when driving vehicles and other mechanisms. Does not affect.

Interactions

No interaction studies have been performed. Relif® Pro should be used with caution in patients taking antiarrhythmic drugs because it contains lidocaine as an active ingredient.

Use with caution in patients taking other local anesthetics, since there is a risk of an increase in the severity of adverse reactions; MAO inhibitors enhance the local anesthetic effect of lidocaine.

It is believed that concomitant use with CYP 3A inhibitors, including cobicistat in tablet form, may increase the risk of systemic side effects. Such a combination should be avoided unless the benefit exceeds the risk of systemic side effects associated with taking GCS. In the case of concomitant use, it is necessary to monitor the patients condition to make sure that there are no systemic side effects associated with the use of GCS.

Overdose

The results of studies of potential acute toxicity associated with the active substances of Relig® Pro indicate that there is no risk of developing symptoms associated with acute toxicity, which develops as a result of accidental overdose due to a single rectal use of the drug.

In case of accidental swallowing of the drug (for example, swallowing several suppositories or several grams of cream), the main symptoms that are expected to occur are systemic symptoms caused by the use of lidocaine hydrochloride, and, depending on the dose, they can manifest in the form of severe cardiovascular disorders (decreased blood pressure, increased sweating, pallor of the skin, bradycardia, arrhythmia, inhibition of heart function, shock, or, in severe cases, cardiac arrest), or reactions associated disorders with the central nervous system (headache, dizziness, blurred visual perception, diplopia, tinnitus, drowsiness, numbness of the limbs, chills, anxiety, vomiting, cramps, shortness of breath or, in especially severe cases, respiratory failure). Methemoglobinemia is possible.

Treatment in case of overdose involves careful monitoring of vital functions, supporting actions that provide oxygen levels, as well as symptomatic treatment of disorders of the central nervous system and cardiovascular system, for example, the appointment of short-acting barbiturates, β-sympathomimetics and atropine. Dialysis does not provide sufficient effect.

Storage conditions

Relif® Pro cream - at a temperature not exceeding 30 ° C, Relif® pro cream - at a temperature not exceeding 25 ° C.