Relief About rectal suppositories, No. 12

hemorrhoids;

proctitis.

ReliefЃ Pro is recommended for use after a bowel movement. Before using the drug, hygiene of the anus (anus) should be performed.

The duration of treatment should not exceed 2 weeks.

Rectal suppositories (1 pc.) Are injected deep into the anus 2 times / day, in the morning and in the evening, however, in the case of a severe form of the disease in the first 3 days, 1 suppository is administered 3 times / day. With a stable improvement, in many cases it is sufficient to administer 1 suppository / day or every other day. However, for severely inflamed and, therefore, painful hemorrhoids, it is recommended to start treatment with Rectal ReliefЃ Pro cream.

Protruding hemorrhoids should be generously lubricated with cream, gently setting them back with your finger.

1 suppository contains:

Active ingredients: fluocortolone pivalate 1 mg, lidocaine hydrochloride in terms of anhydrous substance 40 mg.

Excipient: solid fat (Witepsol W 35) 1775 mg.

• tuberculous and syphilitic processes in the area of ??drug application;

• viral diseases (for example, chickenpox, reaction to vaccination, shingles) in the area of ??application of the drug;

• I trimester of pregnancy;

• hypersensitivity to the components of the drug.

• Treatment of children and adolescents is not recommended due to the lack of data from clinical trials.

pharmachologic effect

A drug with anti-inflammatory and local anesthetic action for local use in proctology. Fluocortolone - GCS, when exposed to the skin, prevents the marginal accumulation of neutrophils, leads to a decrease in the production of lymphokines and inhibition of the migration of macrophages, helping to reduce the processes of infiltration, exudation and granulation. Suppresses inflammatory and allergic skin reactions and relieves itching, burning and pain; reduces capillary dilation, interstitial edema and tissue infiltration. Lidocaine is a local anesthetic; anesthesia is achieved by suppressing the formation and conduction of nerve impulses along afferent nerve fibers by depolarizing sodium channels.

Pharmacokinetics

The local therapeutic effect is achieved with a low level of active components in the blood plasma. Fluocortolone pivalate

Suction

With the daily administration of 2 suppositories 3 times / day for 4 weeks, the content of fluocortolone in the blood plasma did not reach the level that has a systemic effect.

Metabolism

Fluocortolone pivalate is hydrolyzed by esterases and enzymes of the inflammatory focus to form fluocortolone, 11-ketofluocortolone and trimethylacetic acid. Excretion T1 / 2 of fluocortolone and its metabolites after rectal administration was approximately 1.3 and 4 hours, respectively. Fluocortolone is excreted from the body in the form of metabolites, mainly in the urine.

Lidocaine

Suction

The absorption and bioavailability of lidocaine after rectal administration of the cream and suppository is about 30% and 24%, respectively.

Metabolism and excretion

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 in the form of this metabolite. T1 / 2 is 1-2 hours.

With prolonged treatment (more than 4 weeks), there is a risk of developing local skin changes such as atrophy, striae or telangiectasia. Local reactions: burning sensation (1-10%); rarely - irritation and allergic reactions (0.1-1%).

Application during pregnancy and lactation

Epidemiological studies suggest a possible increased risk of developing cleft palate in newborns whose mothers received oral GCS in the first trimester of pregnancy. Insufficient data have been accumulated on the use of local corticosteroids during pregnancy, however, in this case, the likelihood of adverse effects is very low due to the minimal bioavailability of corticosteroids when applied topically. ReliefЃ Pro should be used with caution during pregnancy. When prescribing to pregnant and lactating women, it is necessary to compare the expected benefits of treatment for the mother with the possible risk to the fetus and infant.

The use of the drug during pregnancy and lactation should be short-term.

Application in children

Treatment of children and adolescents is not recommended due to the lack of data from clinical trials.

special instructions

In the presence of fungal infections, in addition to ReliefЃ Pro, appropriate antifungal therapy is required. Avoid ingestion of ReliefЃ Pro or contact with eyes. Influence on the ability to drive vehicles and mechanisms

Not found.

Overdose

Symptoms: if the drug is accidentally taken by mouth (for example, if more than one suppository is swallowed), 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 dose. Treatment: carrying out symptomatic therapy.

Drug interactions

Patients receiving antiarrhythmic drugs should use RelifЃ Pro with caution, given that the drug contains lidocaine. With the simultaneous use of lidocaine with antiarrhythmic drugs, the QT interval may be prolonged and, in very rare cases, the development of AV blockade or ventricular fibrillation is possible