Relief^® Pro (Cream, Suppositories) Instructions for Use

ATC Code

C05AX03 (Preparations for the treatment of hemorrhoids and anal fissures in combination)

Active Substances

Lidocaine (Rec.INN registered by WHO)

Fluocortolone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

A drug with anti-inflammatory and local anesthetic action for topical use in proctology

Pharmacotherapeutic Group

Combined topical glucocorticosteroid

Pharmacological Action

Fluocortolone – a glucocorticosteroid (GCS) that, when applied to the skin, prevents the marginal accumulation of neutrophils, leads to a decrease in the number of lymphokines and inhibition of macrophage migration, helping to reduce the processes of infiltration, exudation, and granulation. It suppresses inflammatory and allergic skin reactions and relieves itching, burning, and pain; reduces capillary dilation, interstitial edema, and tissue infiltration.

Lidocaine – a local anesthetic; analgesic and antipruritic action is achieved by suppressing the formation and conduction of nerve impulses along afferent nerve fibers through the depolarization of sodium channels.

Pharmacokinetics

Local therapeutic effect is achieved with a low level of active components in the blood plasma.

Fluticasone propionate micronized

Absorption

After a single rectal application of 1 g of rectal cream, the absorption of fluocortolone pivalate was a maximum of 5% of the applied or administered amount of the drug.

Metabolism

Fluticasone propionate micronized is hydrolyzed by esterases and enzymes at the site of inflammation to form fluocortolone, 11-ketofluocortolone, and trimethylacetic acid.

Elimination

The T_1/2 of fluocortolone and its metabolites after rectal administration were approximately 1, 3, and 4 hours, respectively. Fluocortolone is eliminated from the body in the form of metabolites mainly with urine.

Lidocaine

Absorption

The absorption and bioavailability of lidocaine after rectal administration of the cream is about 30%.

Metabolism and Elimination

T_1/2 is 1-2 hours. Lidocaine is metabolized by oxidative N-dealkylation, hydrolysis of the amide bond, and hydroxylation of the aromatic ring to form 4-hydroxy-2,6-xylidine, which is the main metabolite. 70% of the drug is excreted in the urine as this metabolite.

Indications

For the symptomatic treatment of pain, swelling, burning, itching in:

• Hemorrhoids;
• Proctitis;
• Eczema in the anal area.

ICD codes

Dosage Regimen

Cream

Relief^® Pro is recommended to be used after defecation. Before using the drug, hygiene of the anus should be performed.

The duration of treatment should not exceed 2 weeks.

The rectal cream should be applied 2 times/day (morning and evening). In the first days of treatment, the cream can be applied 3 times/day. As symptoms improve, it is often sufficient to use the drug 1 time/day.

After squeezing a small amount of cream (about the size of a pea) onto a finger, it is necessary to lubricate the area around the anus and inside the anal ring. To overcome the resistance of the sphincter, the cream should be applied with the fingertip.

Protruding hemorrhoids should be generously lubricated with cream, gently pushing them back with a finger.

To introduce the cream into the rectum, it is necessary to screw the supplied applicator onto the tube and insert it into the anus. Then, by gently pressing the tube, squeeze a small amount of cream into the rectum.

Use of the applicator.

Do not use the applicator if it is damaged. Screw the applicator completely onto the tube. After each use, the applicator should be cleaned externally with a paper towel, then remove the remaining drug with a cotton swab and clean it again with a paper towel. Rinse the applicator under warm water for 1 minute and dry with a paper towel.

Suppositories

Rectally. Relief^® Pro is recommended to be used after defecation. Before using the drug, hygiene of the anus should be performed.

The duration of treatment should not exceed 2 weeks.

Rectal suppositories (1 pc.) are inserted into the anus 2 times/day, in the morning and evening, however, in severe cases of the disease, 1 suppository is inserted 3 times/day during the first 3 days. With stable improvement, in many cases it is sufficient to administer 1 suppository/day or every other day.

The suppository should be inserted so that it remains in the anal canal (at the level of the anal orifice), without completely immersing in the rectum. The base of the suppository should be held with a gauze pad for a few minutes until it is completely dissolved.

For severely inflamed and therefore painful hemorrhoids, it is recommended to start treatment with Relief^® Pro rectal cream.

Adverse Reactions

The frequency of adverse reactions reported during clinical trials of the drug is given below. Within each frequency group, adverse reactions are presented in order of decreasing severity. By frequency, they are divided into very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and <1/100) and rare (≥1/10000 and <1/1000) and very rare (≥1/100000 and <1/10000).

General disorders and administration site conditions common – burning, uncommon – irritation.

Immune system disorders uncommon – allergic reactions.

Skin and subcutaneous tissue disorders with prolonged treatment (more than 4 weeks) there is a risk of developing local skin changes, such as atrophy, striae, or telangiectasia.

Contraindications

• Hypersensitivity to lidocaine and/or fluocortolone and/or to any of the excipients;
• Specific skin diseases (syphilitic, tuberculous process);
• Viral diseases (e.g., chickenpox, shingles) in the area of application of the drug;
• Reaction to vaccination;
• Childhood and adolescence under 18 years of age (no clinical trial data);
• First trimester of pregnancy.

Use in Pregnancy and Lactation

Clinical data on the use of Relief^® Pro during pregnancy and breastfeeding are insufficient.

The appointment of drugs containing GCS in the first trimester of pregnancy should be avoided. A number of studies have shown an increased risk of cleft palate in newborns whose mothers took GCS in the first trimester of pregnancy.

Prescribing the drug in the second and third trimester of pregnancy and during breastfeeding is possible only if the potential benefit to the mother outweighs the risk to the fetus and infant. Long-term use of Relief^® Pro should be avoided when prescribed during pregnancy and breastfeeding.

Animal studies have shown reproductive toxicity of fluocortolone pivalate.

Pediatric Use

The use of the drug in children and adolescents under 18 years of age is contraindicated, since clinical trial data are lacking.

Special Precautions

Ingestion of Relief^® Pro and contact of the drug with the eyes should be avoided. Hands should be washed thoroughly after applying the drug.

Cetearyl alcohol may cause a local skin reaction (e.g., contact dermatitis).

Contact of the drug with latex products (contraceptive diaphragms and condoms) should be avoided to prevent a decrease in their effectiveness.

Effect on ability to drive vehicles and mechanisms

The drug does not affect the ability to drive vehicles or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Studies of the active substances of Relief^® Pro show that there are no risks of acute intoxication as a result of accidental overdose with a single rectal or perianal application of Relief^® Pro.

Symptoms

It is assumed that in case of accidental ingestion of the drug (for example, swallowing several grams of cream), the most severe symptoms may occur from the cardiovascular system (depression of heart function, cardiac arrest) and the central nervous system (convulsions, respiratory depression, respiratory arrest) depending on the dose.

Treatment

Treatment of overdose includes careful monitoring of vital functions, the use of supportive procedures (oxygen supply), as well as symptomatic treatment of the central nervous system and cardiovascular system, for example, with fast-acting barbiturates, beta-sympathomimetic drugs and atropine. The use of dialysis does not show sufficient effectiveness.

Drug Interactions

Patients receiving antiarrhythmic drugs should use lidocaine with caution. With simultaneous use of lidocaine with antiarrhythmic drugs, prolongation of the QT interval is possible and, in very rare cases, the development of AV block or ventricular fibrillation is possible.

Concomitant use of the drug and cytochrome P450 3A4 inhibitors may increase the risk of developing systemic side effects from the use of corticosteroids, including suppression of the hypothalamic-pituitary-adrenal system. The combination of these drugs should be avoided, except in cases where the benefit of therapy outweighs the risk of developing systemic side effects from corticosteroids. If it is necessary to use Relief^® Pro in combination with cytochrome P450 3A4 inhibitors, careful monitoring of the patient should be carried out due to the risk of developing systemic reactions to corticosteroids.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C (86°F).

Shelf Life

The shelf life is 3 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.