Relief Pro, rectal 40 mg+1 mg 12 pcs

Pharmacotherapeutic group

Glucocorticosteroid for topical use combined.

ATC code:

C05AX03

Pharmacological properties

Pharmacodynamics

Fluocortolone. Fluocortolone, when applied to the skin, prevents marginal accumulation of neutrophils, leads to a decrease in lymphokines and inhibition of macrophage migration, helping to reduce infiltration, exudation and granulation processes.

Fluocortolone suppresses inflammatory and allergic skin reactions and relieves itching, burning and pain; reduces capillary dilatation, interstitial edema and tissue infiltration.

Lidocaine. Lidocaine is a local anesthetic; analgesia is achieved by inhibition of nerve impulse formation and conduction along afferent nerve fibers by depolarization of sodium channels.

Pharmacokinetics
Local therapeutic effect is achieved at low plasma levels of active ingredients.

Fluocortolone pivalate. After a single rectal application of 1 g of cream or administration of one suppository, absorption of the glucocorticosteroid was maximum 5% of the applied or injected amount of the drug.

At the time of daily administration of 2 suppositories 3 times a day for 4 weeks, plasma levels of fluocortolone did not reach levels with systemic effects.

Fluocortolone pivalate is hydrolyzed by esterases, enzymes of the inflammation focus, to form fluocortolone, 11-ketofluocortolone and trimethylacetic acid.

The plasma elimination half-lives of fluocortolone and its metabolites after rectal administration were approximately 1.3 and 4 hours, respectively.

Fluocortolone is excreted as metabolites mainly in the urine. Lidocaine. Absorption and bioavailability of lidocaine after rectal administration of the cream and suppository are about 30% and 24%, respectively.

The elimination half-life of lidocaine from blood plasma is 1-2 hours. In humans, 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 and the urine excretes 70% of the drug as this metabolite.

Indications

Pain, HemorrhoidsHemorrhoids, Proctitis.

Active ingredient

Lidocaine, Fluocortolone

Composition

1 suppository contains:

fluocortolone pivalate 1 mg,

lidocaine hydrochloride in terms of anhydrous substance 40 mg.

Excipients:

Solid fat (Vitepsol W35) – 1775 mg.

How to take, the dosage

Relief Pro is recommended to be used after defecation. Before using the drug, anus (anus) hygiene should be performed.

One suppository is inserted deep into the anus twice a day, morning and evening, but if the disease is severe, the first three days, one suppository three times a day. With steady improvement, it is often sufficient to administer one suppository a day or every other day.

Interaction

Patients receiving antiarrhythmic drugs should use lidocaine with caution.

If lidocaine is used simultaneously with antiarrhythmic drugs, prolongation of the QT interval and, in very rare cases, AV blockade or ventricular fibrillation may occur.

Special Instructions

In the presence of fungal infections in addition to Relief Pro requires appropriate antifungal therapy.

Avoid getting Relief Pro inside or contact with the eyes. After applying the cream it is recommended to wash hands thoroughly.

Contraindications

Tuberculosis and syphilitic processes in the area of application.

Viral diseases (e.g., chickenpox, reaction to vaccination, shingles) in the area of application.

The treatment of children and adolescents is not recommended due to lack of clinical trial data.

The first trimester of pregnancy.

High sensitivity to the components of the drug.

Side effects

With prolonged treatment with both Relief Pro cream and suppositories (more than four weeks) there is a risk of local skin changes such as atrophy, stretch marks or telangiectasia.

Burning: 1-10%, rarely – irritation and allergic reactions – 0.1-1%.

Overdose

If the drug is accidentally ingested (e.g., if several grams of cream or more than one suppository is swallowed), the most severe symptoms may occur from the cardiovascular system (depressed heart function, cardiac arrest) and CNS (seizures, respiratory depression, respiratory arrest) depending on the dose.

Similarities

Relief Pro, Hemorrhoid Remedies