Composition, form of production and packaging
Suppositories rectal yellowish-white, torpedo-shaped, with a smooth surface.
1 supp.
fluocortolone pivalate 1 mg
lidocaine hydrochloride 40 mg
[PRING] fat solid (Witepsol W35) - 1775 mg.
5 pieces. - strips of aluminum foil (1) - packs of cardboard.
5 pieces. - strips of aluminum foil (2) - packs of cardboard.
6 pcs. - strips of aluminum foil (1) - packs of cardboard.
6 pcs. - strips of aluminum foil (2) - packs of cardboard.
Rectal cream white, opaque.
1 g
fluocortolone pivalate 1 mg
lidocaine hydrochloride 20 mg
[PRING] sodium hydrophosphate dodecahydrate - 0.7 mg, disodium edetate - 1 mg, sodium dihydrogen phosphate dihydrate - 4.5 mg, benzyl alcohol - 5 mg, sorbitan stearate - 10 mg, polysorbate 60 - 35 mg, cetostearyl alcohol - 60 mg, paraffin liquid - 90 mg, white petrolatum - 100 mg, purified water - 672.8 mg.
10 g - aluminum tubes (1) complete with applicator - packs cardboard.
15 g - aluminum tubes (1) complete with applicator - packs of cardboard.
30 g - aluminum tubes (1) complete with applicator - packs of cardboard.
50 g - aluminum tubes (1) complete with applicator - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
PHARMACHOLOGIC EFFECT
The drug with anti-inflammatory and local anesthetic action for topical application in proctology.
Fluorocortolone - GCS, when exposed to the skin, prevents the accumulation of neutrophils, leads to a decrease in the production of lymphokines and inhibition of migration of macrophages, contributing to a reduction in the processes of infiltration, exudation and granulation. Suppresses inflammatory and allergic skin reactions and relieves itching, burning and pain; reduces dilatation of capillaries, interstitial edema and tissue infiltration.
Lidocaine is a local anesthetic; anesthesia is achieved by suppressing the formation and carrying out of nerve impulses along afferent nerve fibers by depolarizing the sodium channels.
PHARMACOKINETICS
Local therapeutic effect is achieved with a low level of active components in the blood plasma.
Fluorocortolone pivalate
Suction
After a single application of 1 g of rectal cream or the administration of one suppository rectal, the absorption of fluocortolone pivalate was at most 5% of the applied or administered amount of the drug.
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 exerts systemic influence.
Metabolism
Fluorocortolone pivalate is hydrolyzed by esterases and enzymes of the inflammatory focus with the formation of fluocortolone, 11-ketofluocortolone and trimethylacetic acid.
Excretion
T 1/2 of fluocortolone and its metabolites after rectal administration were approximately 1.3 and 4 hours, respectively. Fluorocortolone is excreted from the body in the form of metabolites mainly along with urine.
Lidocaine
Suction
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. With urine, 70% of the drug is excreted in the form of this metabolite. T 1/2 is 1-2 hours.
INDICATIONS
- hemorrhoids;
- proctitis;
- eczema in the anus (for rectal cream).
DOSING MODE
Relief Pro is recommended after defecation. Before using the drug should be hygiene anus (anus).
Duration of treatment should not exceed 2 weeks.
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 relief of symptoms is often enough to apply the drug 1 time / day.
Pressing on the finger a small amount of cream (about the size of a pea), you need to lubricate the area around the anus and inside the anal ring. To overcome the resistance of the sphincter, you need to apply the cream with the tip of your finger.
To inject the cream into the rectum, the attached applicator should be screwed onto the tube and inserted into the anus. Then, lightly pressing the tube, squeeze a small amount of cream into the rectum.
Suppositories rectal (1 unit) are injected deep into the anus 2 times / day, in the morning and in the evening, however, for a severe form of the disease in the first 3 days, 1 suppository is administered 3 times / day. With stable improvement, in many cases it is enough to administer 1 suppository / day or every other day.
However, in cases of severely inflamed and, consequently, painful hemorrhoids, it is recommended to begin treatment with a cream. The protruding hemorrhoids should be greased with a lot of cream, gently pushing them back with your finger.
SIDE EFFECT
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%).
CONTRAINDICATIONS
- tuberculosis and syphilitic processes in the application area;
- viral diseases (eg chicken pox, vaccination reaction, 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 on clinical trials.
PREGNANCY AND LACTATION
Epidemiological studies suggest a possible increased risk of development of the wolf mouth in newborns whose mothers received SCS inside the first trimester of pregnancy. Data on the use of local GCS during pregnancy is not accumulated enough, but in this case the likelihood of adverse effects is very low due to the minimal bioavailability of GCS in topical application.
Relief Pro should be administered with caution in pregnancy. When appointing pregnant and lactating women, it is necessary to compare the expected benefit of treatment for the mother with a possible risk to the fetus and the baby.
The purpose of the drug during pregnancy and during lactation should be short-lived.
APPLICATION FOR CHILDREN
Treatment of children and adolescents is not recommended, due to the lack of data on clinical trials.
SPECIAL INSTRUCTIONS
In the presence of fungal infections in addition to Relief Pro, appropriate antifungal therapy is required.
It is necessary to avoid getting Relief Pro inside or contact with the eyes. After applying the cream, we recommend that you wash your hands thoroughly.
Impact on the ability to drive vehicles and manage mechanisms
Not found.
OVERDOSE
In case of accidental ingestion of the drug inside (for example, if several grams of cream or more than one suppository are swallowed), the most severe symptoms may arise from the cardiovascular system (heart function depression, cardiac arrest) and CNS (convulsions, respiratory depression, respiratory arrest) in dose dependence.
DRUG INTERACTION
Patients receiving antiarrhythmic drugs should use Relief Pro with caution, given that the preparation contains lidocaine. With the simultaneous use of lidocaine with antiarrhythmic drugs, the QT interval may be prolonged and, in very rare cases, AV blockade or ventricular fibrillation may develop.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. The shelf life of rectal cream is 3 years, rectal suppositories - 4 years.
