Instruction for use: Doloproct

Active substance Fluocortolone + Lidocaine

ATX code C05AX03 Preparations for the treatment of hemorrhoids and anal fissures in combination

Pharmacological group

Glucocorticosteroids in combinations

Nosological classification (ICD-10)

I84 Hemorrhoids

Painful hemorrhoids, External hemorrhoids, Internal hemorrhoids, Inflammation of hemorrhoids, Aggravation of hemorrhoids, Chronic bleeding hemorrhoids, Acute hemorrhoidal attack

K62.8.1 * Proctitis

Atrophic proctitis, Anusitis

L29.0 anus Itching

Anal eczema, Anal itching, anogenital pruritus, Dermatitis and eczema in the anal area, Perianal dermatitis, anal Itching, Itching anogenital, Itching anorectal, Itching in the genital area and the anus, Itching in the anus, Eczema anal area, perianal dermatitis

L30.9 Dermatitis, unspecified

Allergic dermatoses complicated by a secondary bacterial infection, Anal eczema, Bacterial maturation, Varicose Eczema, Venous dermatitis, Inflammation of the skin, Inflammation of the skin upon contact with plants, Inflammatory Skin Diseases, Inflammatory skin reactions, Inflammatory processes of the skin, Hypostatic dermatitis, Fungal Eczema, Fungal dermatosis, Dermatitis, Dermatitis is stagnant, Dermatitis and eczema in the anal area, Dermatitis acute contact, Perianal dermatitis, Dermatosis, Dermatosis of the scalp, Dermatosis of psoriasis, Dermatosis with persistent itching, Dermatoses, Dermatoses itchy, Other itching dermatoses, Significant eczematous manifestations, Itching with, dermatoses, Itching eczema, True eczema, Skin reaction to insect bites,Skin itching with dermatosis, Constitutional eczema, Weeping eczema, Drowsing inflammatory skin disease, Dying Infectious-Inflammatory Skin Disease, Non-allergic dermatitis, Nummular eczema, Acute contact eczema, Acute inflammatory skin disease, Acute dermatosis, Acute severe dermatosis, Perianal dermatitis, Superficial dermatosis, Subacute Contact Eczema, Simple dermatitis, Occupational dermatitis, Psychogenic dermatosis, Bubble dermatitis of newborns, Pustular eruptions, Irritation and redness of the skin, Low-flammable eczema, Dry atrophic eczema, Dry eczema, Toxic dermatitis, Ear eczema like dermatitis, Chronic eczema, Chronic dermatosis, Chronic common dermatosis, Scaly papular dermatosis, Eczema, Eczema anal region, Eczema of the hands, Eczema Contact, Eczema lichenized, Eczema Nummular, Eczema acute, Eczema acute contact, Eczema subacute, Eczematous dermatitis, Eczema-like rashes, Ecome exogenous, Endogenous eczema, Gluteal dermatitis, Restricted itchy dermatitis

Composition and form of release

Rectal cream 1 mg + 20 mg 1 tube

Fluocortolone pivalate 1 mg

Lidocaine hydrochloride (in terms of anhydrous substance) 20 mg

Auxiliary substances: sodium hydrophosphate dodecahydrate; Disodium edetate; Sodium dihydrogen phosphate dihydrate; Benzyl alcohol; Sorbitan stearate; Polysorbate 60; Cetostearyl alcohol; Paraffin liquid; Petroleum jelly white; purified water

In an aluminum tube 10, 15, 30 or 50 g with an applicator; In a pack of cardboard 1 tuba.

Suppositories for rectal administration 1 mg + 40 mg 1 supp.

Fluocortolone pivalate 1 mg

Lidocaine hydrochloride (in terms of anhydrous substance) 40 mg

Excipients: fat solid (Witepsol W 35) - 1775 mg

In a 5 or 6 piece; In a pack of cardboard 1 or 2 strip.

Description of dosage form

Cream: white opaque.

Suppositories: a yellowish-white suppository torpedo-shaped with a smooth surface.

pharmachologic effect

Pharmacological action - antipruritic, anti-inflammatory local, local anesthetic.

Pharmacodynamics

Fluorocortolone pivalate

Fluorocortolone when exposed to the skin prevents the accumulation of neutrophils, leads to a decrease in the level of lymphokines and inhibition of migration of macrophages, contributing to a reduction in the processes of infiltration, exudation and granulation.

Fluorocortolone suppresses inflammatory and allergic skin reactions and relieves itching, burning and pain; Reduces dilatation of capillaries, interstitial edema and tissue infiltration.

Lidocaine

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

After a single rectal application of 1 g of cream or the administration of one suppository, the absorption of the glucocorticosteroid was at most 5% of the applied or administered amount of the drug.

In the period of daily administration of 2 soups. 3 times a day for 4 weeks the content of fluocortolone in the blood plasma did not reach the level that exerts systemic influence.

Fluorocortolone pivalate is hydrolyzed by esterases, enzymes of the inflammatory focus with the formation of fluocortolone, 11-ketofluocortolone and trimethylacetic acid.

T1 / 2 from the plasma 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

Absorption and bioavailability of lidocaine following rectal administration of the cream and suppository is about 30% and 24%, respectively.

T1 / 2 lidocaine from the blood plasma is 1-2 hours. In the human body, 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 with Urine output 70% of the drug in the form of this metabolite.

Indications

hemorrhoids;

Proctitis;

Eczema in the anus (rectal cream).

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;

Treatment of children and adolescents is not recommended due to the lack of data on clinical trials;

I trimester of pregnancy;

Hypersensitivity to the components of the drug.

pregnancy and lactation

A number of 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 sufficiently accumulated, but in this case the likelihood of adverse effects is very low due to the minimal bioavailability of GCS in topical application.

Doloproct cream and suppositories should be administered with caution in pregnant women. 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.

When prescribed by a doctor during pregnancy and lactation, the drug should be used for a short time.

Side effects

With prolonged treatment with both cream and suppositories of the preparation Doloproct (more than 4 weeks), there is a risk of developing local skin changes, such as atrophy, striae or telangiectasia.

Rectal cream: burning - 1-10%, rarely - irritation and allergic reactions.

Suppositories rectal: burning - 1-10%, rarely - irritation and allergic reactions (0.1-1%).

Interaction

Patients receiving antiarrhythmic drugs should use lidocaine with caution. 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.

Dosing and Administration

Externally, rectally.

Doloproct is recommended after defecation. Before using the drug should be hygiene anus (anus).

The duration of treatment should not exceed 2 weeks.

Rectal cream

Rectal cream should be applied 2 times a day: morning and evening. In the first days of treatment, the cream can be applied 3 times a day. As relief of symptoms often enough, one application per day is enough.

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.

Rectal suppositories

For 1 dose. Injected deep into the anus 2 times a day, in the morning and in the evening, however, in the severe form of the disease, the first 3 days are administered 1 supp. 3 times a day. With stable improvement in many cases it is enough to introduce 1 soup. Per day or every other day.

In cases of severely inflamed and, therefore, painful hemorrhoids, it is recommended to begin treatment with a cream. The protruding hemorrhoids should be greased with a lot of cream, gently back with your finger.

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 can arise from the cardiovascular system (heart function depression, cardiac arrest) and CNS (convulsions, respiratory depression, respiratory arrest) Of the dose.

special instructions

In the presence of fungal infections in addition to the preparation of Doloproct, appropriate antifungal therapy is required. Avoid ingestion or contact with the eyes. After applying the cream, we recommend that you wash your hands thoroughly.

Influence on the ability to drive and machinery. Not found.

storage Conditions

At a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life

Rectal cream 1 mg + 20 mg - 3 years.

Suppositories rectal 1 mg + 40 mg - 4 years.

Do not use after the expiry date printed on the package.