Hepazolone, rectal suppositories, 10pcs

Composition

1 suppository contains:

Active ingredients:

heparin sodium 120 IU,

prednisone 1.7 mg,

lidocaine hydrochloride 10 mg

Auxiliary substances:

vitepsol H 15 – sufficient amount to obtain a suppository weighing 1.0 g

Pharmacological action

Pharmacotherapeutic group:

Hemorrhoid treatment tool.

ATX code: C05BA53

Pharmacological action:

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

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

Lidocaine has a local anesthetic effect, which is caused by the blockade of voltage-dependent sodium channels, which prevents the generation of impulses in the endings of sensitive nerves and the conduct of pain impulses along nerve fibers. The combined action of the components of the drug achieves the best effect.

Pharmacokinetics:

Heparin and prednisone are effectively absorbed after rectal use, enter the intestinal wall for several hours, and then 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, prednisone-18-36 hours.

With rectal use, part of lidocaine (35%) undergoes systemic absorption. The maximum concentration of lidocaine in the blood reaches 2 h. Lidocaine is rapidly metabolized in the liver and excreted through the kidneys. Part of lidocaine undergoes enterohepatic circulation and is excreted in the faeces. The elimination half-life is 1 to 3 hours.

Indications

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

Contraindications

• Hypersensitivity to the components of the drug.
• Viral, fungal, tuberculosis and other infectious processes of the anorectal area, disorders of the coagulation system with a predisposition to bleeding.
• Pregnancy and lactation.
• Children under 12 years of age.

Side effects

The drug is usually well tolerated. No side effects were detected at the recommended dose of the drug.

If the drug is used for more than 5 weeks, systemic side effects associated with the action of prednisone may occur. :

From the endocrine system: reduced glucose tolerance, “steroid” diabetes mellitus, adrenal suppression, Itsenko-Cushing syndrome. From the cardiovascular system, arrhythmias, bradycardia (in predisposed patients), ECG changes characteristic of hypokalemia, increased blood pressure are possible.

Nervous system disorders: insomnia, dizziness.

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

Possible allergic reactions caused by lidocaine and heparin in the form of itching and irritation of the anus.

How to take, course of use and dosage

For internal hemorrhoids, the suppository should be inserted into the rectal cavity 1-2 times a day.

With external hemorrhoids, the suppository is not fully inserted into the anus – its base should be palpated from the outside.

Hold the anus with a gauze cloth until the suppository completely melts (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 doctor’s recommendation, the course can be extended up to 14 days.

Form of production

Rectal suppositories

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf life

2 years

Active ingredient

Heparin Sodium, Lidocaine, Prednisone

Conditions of release from pharmacies

By prescription

Dosage form

rectal suppositories

Description

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 12 years of age

Indications

Hemorrhoid