Hepazolone rectal suppositories, No. 10

External and internal hemorrhoids, including acute, thrombophlebitis of hemorrhoidal veins of the perianal region, fistulas, eczema, itching in the anus caused by inflammation, anal fissures, preparation for surgery in the anorectal area, as part of the complex therapy of thrombosed and operated hemorrhoids.

In case of internal hemorrhoids, the suppository should be injected into the rectal cavity 1-2 times a day. With external hemorrhoids, the suppository is not fully inserted into the anus - its base must be felt from the outside. Hold the anus with a gauze napkin until the suppository melts completely (2-3 minutes), otherwise the suppository will 'fall' into the rectum without having a therapeutic effect. The course of treatment is 7 days. On the recommendation of a doctor, the course can be extended up to 14 days.

1 suppository contains:
Active ingredients: sodium heparin 120 ME, prednisolone 1.7 mg, lidocaine hydrochloride 10 mg
Excipients: witepsol H 15 - a sufficient amount to obtain a suppository weighing 1.0 g.

Hypersensitivity to the components of the drug.

Viral, fungal, tuberculous and other infectious processes of the anorectal region, disorders of the coagulation system with a predisposition to bleeding. Pregnancy and lactation. Children under 12 years of age.

Trade name: Hepazolone

Dosage form:

Rectal suppositories

Composition of the preparation:

1 suppository contains:
Active ingredients: sodium heparin 120 ME, prednisolone 1.7 mg, lidocaine hydrochloride 10 mg
Excipients: witepsol H 15 - a sufficient amount to obtain a suppository weighing 1.0 g.

Description:

Suppositories of torpedo-shaped white or white with a yellowish or creamy shade.

Pharmacotherapeutic group:

Hemorrhoids are a cure. -

Pharmachologic effect:

The pharmacological action is determined by the properties of the components included in the drug. Heparin prevents the formation of blood clots, prevents blood coagulation in hemorrhoids, has an anti-edema effect, promotes the regeneration of connective tissue, accelerates healing and reduces the number of disease relapses. Heparin inhibits reactions that cause blood coagulation and form a fibrin thrombus. Heparin at this dosage in combination with plasma antithrombin III inhibits thrombosis, deactivating factor Xa, and also inhibiting the conversion of prothrombin to thrombin. Heparin prevents the formation of a stable fibrin thrombus by inhibiting the activation of fibrin-stabilizing factor. Heparin also exhibits an anti-inflammatory effect, affecting the vascular endothelium, and prevents edema.

Prednisolone belongs to the group of synthetic glucocorticosteroids of medium duration of action, reduces the formation, release and activity of an inflammatory mediator (histamine, kinin, prostaglandin, lysosomal enzymes). Suppresses cell migration to the site of inflammation; reduces vasodilation and increased vascular permeability in the focus of inflammation. Reduces exudation due to vasoconstrictor action. Suppresses the action of macrophages, target cells, cytokines, which are involved in the development of allergic reactions. Prevents access of sensitized 1 lymphocytes and macrophages to target cells. It has anti-inflammatory, anti-exudative and anti-allergic effects, reduces inflammation and associated subjective sensations (itching, burning, pain,feeling of moisture due to eczematous changes) in the anorectal region.

Lidocaine has a local anesthetic effect, which is due to the blockade of voltage-dependent sodium channels, which prevents the generation of impulses at the endings of the sensory nerves and the conduction of pain impulses along the nerve fibers. The best effect is achieved by the combined action of the components of the preparation.

Pharmacokinetics:
Heparin and prednisolone are effectively absorbed after rectal administration, penetrate into the intestinal wall for several hours, and then are gradually transported through portal circulation to the liver, where they are biotransformed by oxidizing enzymes into metabolites and excreted through the kidneys. The half-life of heparin is 1-1.5 hours, for prednisolone, 18-36 hours.

When administered rectally, part of lidocaine (35%) undergoes systemic absorption. The maximum concentration in the blood of lidocaine reaches after 2 hours. Lidocaine is rapidly metabolized in the liver and excreted through the kidneys. Part of the lidocaine undergoes enterohepatic circulation and is excreted in the feces. The half-life is 1 to 3 hours.

Indications for use:

External and internal hemorrhoids, including acute, thrombophlebitis of hemorrhoidal veins of the perianal region, fistulas, eczema, itching in the anus caused by inflammation, anal fissures, preparation for surgery in the anorectal area, as part of the complex therapy of thrombosed and operated hemorrhoids.

Contraindications:

Hypersensitivity to the components of the drug.

Viral, fungal, tuberculous and other infectious processes of the anorectal region, disorders of the coagulation system with a predisposition to bleeding. Pregnancy and lactation. Children under 12 years of age.

Method of administration and dosage:

In case of internal hemorrhoids, the suppository should be injected into the rectal cavity 1-2 times a day. With external hemorrhoids, the suppository is not fully inserted into the anus - its base must be felt from the outside. Hold the anus with a gauze napkin until the suppository melts completely (2-3 minutes), otherwise the suppository will 'fall' into the rectum without having a therapeutic effect. The course of treatment is 7 days. On the recommendation of a doctor, the course can be extended up to 14 days.

Side effect:

The drug is usually well tolerated. At the recommended dose of the drug, no side effects have been identified.

When using the drug for more than 5 weeks, systemic side effects associated with the action of prednisolone are possible:

From the endocrine system: decreased glucose tolerance, 'steroid' diabetes mellitus, suppression of adrenal function, Itsenko-Cushing's syndrome. On the part of the cardiovascular system, arrhythmias, bradycardia (in predisposed patients), ECG changes characteristic of hypokalemia, and increased blood pressure are possible.

From the nervous system: insomnia, dizziness.

From the side of metabolism: increased excretion of calcium ions, hypocalcemia, increased sweating.

Allergic reactions are possible caused by lidocaine and heparin in the form of itching and irritation of the anus.

Release form:

Rectal suppositories. 5 pieces in a blister strip made of polyvinyl chloride film. Two contour packs together with instructions for use in a cardboard box.

Storage conditions:

In a dry, dark place at a temperature not exceeding 25 ? C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use the drug after the expiration date.

Terms of dispensing from pharmacies:

On prescription.