Gepazolon

General characteristics. Structure:

Active ingredients: heparin sodium 120 ME, Prednisolonum of 1,7 mg, lidocaine of a hydrochloride of 10 mg;
Excipients: a vitepsola of N 15 – enough for receiving suppository weighing 1,0 g.

Description. Suppositories of color, white or white with a yellowish or creamy shade, torpedo-shaped form.

Pharmacological properties:

Pharmacodynamics. Pharmacological action is defined by properties of the components entering drug.
Heparin interferes with formation of blood clots, prevents blood coagulation in hemorrhoidal nodes, possesses antiedematous action, promotes regeneration of connecting fabric, accelerates healing and reduces number of a recurrence of a disease. Heparin inhibits the reactions causing blood coagulation and forming fibrinous blood clot. Heparin in this dosage in a combination with antithrombin III of a blood plasma inhibits thrombosis, deactivating a factor Ha, and also inhibiting conversion of a prothrombin in thrombin. Heparin interferes with formation of stable fibrinous blood clot, inhibiting activation of a fibrinstabiliziruyushchy factor. Heparin shows also antiinflammatory action, influencing an endothelium of vessels, interferes with hypostasis.
Prednisolonum belongs to group of synthetic glucocorticosteroids of average duration of action, reduces education, release and activity of mediators of an inflammation (a histamine, a kinin, prostaglandin, lizosomalny enzymes). Suppresses migration of cells to the place of an inflammation; reduces a vazodilatation and a hyperpermeability of vessels in the inflammation center. Reduces exudation thanks to vasopressor action. Suppresses action of macrophages, target cells, cytokines who participate in development of allergic reactions. Prevents access of sensibilized T lymphocytes and macrophages to target cells. Has antiinflammatory, antiexudative and antiallergic effect, reduces an inflammation and the accompanying subjective feelings (an itch, burning, pain, feeling of humidity owing to eczematic changes) in anorectal area.
Lidocaine possesses mestnoanesteziruyushchy action which is caused by blockade of voltazhzavisimy natrium channels that interferes with generation of impulses in the terminations of sensory nerves and to carrying out painful impulses on nerve fibrils. The combined action of components of drug reaches the best effect.  

Pharmacokinetics. Heparin and Prednisolonum are effectively absorbed after rectal administration, get into an intestines wall at several o'clock, and then are gradually transported by means of portal circulation in a liver, there biotransformirutsya by the oxidizing enzymes in metabolites and are removed through kidneys. The elimination half-life of heparin makes 1 – 1,5 h, Prednisolonum - 18-36 hours. Heparin and Prednisolonum are effectively absorbed after rectal administration, get into an intestines wall at several o'clock, and then At rectal use a part of lidocaine (35%) is exposed to system absorption. The maximum concentration in blood of lidocaine reaches in 2 h. Lidocaine is quickly metabolized in a liver and removed through kidneys. A part of lidocaine is exposed to enterogepatichesky circulation and is removed with a stake. The elimination half-life makes from 1 to 3 hours.

Indications to use:

Outside and internal hemorrhoids, including acute, thrombophlebitis of hemorrhoidal veins of perianal area, fistulas, eczema, the itch in the field of the anus caused by an inflammation, proctal cracks, preparation for an operative measure in an anorectal zone, as a part of complex therapy thrombosed and the operated hemorrhoids.

Route of administration and doses:

At internal hemorrhoids to enter suppository into a rectum cavity 1-2 times a day.
At outside hemorrhoids to enter suppository into an anus short – its basis has to be probed outside. Hold an anus with a gauze napkin before full thawing of suppository (2–3 min.), otherwise suppository "will fail" in a rectum, without having had medical effect.
Course of treatment – 7 days.
According to the recommendation of the doctor the course can be prolonged up to 14 days.

Features of use:

The patients who had earlier allergic reactions to other selection blockers of 5-HT3-receptors have the increased risk of their development against the background of an ondansetron.
Ondansetron can slow down motility of a large intestine in this connection, its appointment as the patient with signs of impassability of intestines demands special observation.

Side effects:

Drug is usually well transferred. At the recommended dose of drug of side effects it is not revealed.
At drug use more than 5 weeks the system side effects connected with effect of Prednisolonum are possible:
From endocrine system: decrease in tolerance to glucose, a "steroid" diabetes mellitus, oppression of function of adrenal glands, an Icenco-Cushing syndrome.
From cardiovascular system arrhythmias, bradycardia (at predisposed patients), the ECG changes characteristic of a hypopotassemia, increase in arterial pressure are possible.
From a nervous system: sleeplessness, dizziness.
From a metabolism: the increased removal of calcium ions, a hypocalcemia, the increased sweating.
The allergic reactions caused by lidocaine and heparin in the form of an itch and irritation of an anus are possible.

Contraindications:

- Hypersensitivity to drug components.
- Virus, fungal, tubercular and other infectious processes of anorectal area, disturbance of coagulative system with predisposition to bleedings.
- Pregnancy and period of a lactation.
- Children's age up to 12 years.

Storage conditions:

In the dry place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Period of validity - 2 years. After a period of validity not to use drug.

Issue conditions:

According to the recipe

Packaging:

Suppositories rectal. On 5 pieces in a blister strip packaging from a film polyvinyl chloride. Two planimetric packagings together with the application instruction in a pack cardboard.