Hepazolone, rectal, 10 pcs.

Pharmacotherapeutic group:

Hemorrhoid treatment.

ATX code: C05BA53

Pharmacological action:

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

Prednisolone belongs to the group of synthetic glucocorticosteroids of medium duration of action; it reduces formation, release and activity of inflammatory mediators (histamine, kinin, prostaglandin, lysosomal enzymes). Suppresses cell migration to the site of inflammation; reduces vasodilation and increased vascular permeability in the inflammation focus. Reduces exudation due to vasoconstrictor action. Inhibits the action of macrophages, target cells, cytokines, which are involved in the development of allergic reactions. Prevents the access of sensitized 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 moistness due to eczematous changes) in the anorectal area.

Lidocaine has a local anesthetic effect due to blockade of voltage-dependent sodium channels, which prevents generation of impulses in the endings of sensitive nerves and conduct of pain impulses along the nerve fibers. By the combined action of the ingredients of the drug the best effect is achieved.

Pharmacokinetics:

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

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

Indications

Active ingredient

Composition

1 suppository contains:

The active ingredients:

Heparin sodium 120 ME,

Prednisolone 1.7 mg,

Lidocaine hydrochloride 10 mg

Auxiliary substances:

Vitepsol H 15 – enough to produce a suppository weight of 1.0 g.

How to take, the dosage

In case of internal hemorrhoids, insert the suppository into the rectal cavity 1-2 times a day.

In external hemorrhoids, insert the suppository incompletely into the anus – its base should be palpable on the outside.

To prevent the suppository from “falling” into the rectum without producing its therapeutic effect, hold the anus with a gauze towel until the suppository has completely melted (2-3 minutes).

The course of treatment is 7 days. The course may be prolonged up to 14 days, if recommended by the doctor.

Contraindications

Side effects

When using the drug for more than 5 weeks there may be systemic side effects associated with the action of prednisolone:

Endocrine system disorders: decreased glucose tolerance, “steroid” diabetes, inhibition of adrenal function, Icenko-Cushing’s syndrome. Cardiovascular system disorders may include arrhythmias, bradycardia (in predisposed patients), ECG changes characteristic of hypokalemia, increased arterial pressure.

Nervous system disorders: insomnia, dizziness.

Metabolism disorders: increased excretion of calcium ions, hypocalcemia, increased sweating.

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