Helepazocol (Ointment) Instructions for Use

Marketing Authorization Holder

Tula Pharmaceutical Factory, LLC (Russia)

ATC Code

C05BA53 (Heparin in combination with other drugs)

Active Substances

Heparin sodium (Rec.INN registered by WHO)

Prednisolone (Rec.INN registered by WHO)

Lauromacrogol 400 (Rec.INN registered by WHO)

Dosage Form

Helepazocol

Ointment for rectal and external use 65 IU+30 mg+2.233 mg/1 g: tube 20 g

Dosage Form, Packaging, and Composition

Ointment for rectal and external use of a yellowish-white color, semi-transparent, homogeneous, gel-like, with a characteristic odor.

* at a heparin sodium activity of 180 IU/mg.

Excipients: hard paraffin – 50 mg, anhydrous lanolin – 50 mg, colloidal silicon dioxide – 70 mg, purified water – 1.5 mg, propylparaben – 0.5 mg, liquid paraffin – up to 1 g.

20 g – tubes (1) with nozzles – cardboard packs.

Clinical-Pharmacological Group

A drug with antithrombotic, anti-inflammatory, and venosclerosing action for topical use in proctology

Pharmacotherapeutic Group

Direct-acting anticoagulant for topical use + other drugs

Pharmacological Action

A combined medicinal product with antithrombotic, anti-inflammatory, and venosclerosing action for topical use in proctology.

Heparin sodium is a direct-acting anticoagulant. When applied externally, it exerts a local antithrombotic, anti-exudative, and moderate anti-inflammatory effect; promotes the regeneration of connective tissue; prevents blood coagulation in hemorrhoids.

Prednisolone is a glucocorticosteroid that exerts anti-inflammatory, anti-exudative, and anti-allergic effects, reducing itching, burning sensation, and pain in the anorectal area.

Laureth-9 exerts a local anesthetic effect and provides sclerosing of hemorrhoids.

Pharmacokinetics

Heparin sodium

After absorption, plasma protein binding is 95%. It is slowly released from tissues with a T_1/2 of about 1 hour. 50% of the active substance remains on the skin after administration. The rate of release is dose-dependent. After absorption, it is metabolized in the liver (partially by the enzyme hepatic heparinase) and in the reticuloendothelial system. 20-50% is excreted in the urine unchanged and partially as uroheparin, which has a weak anticoagulant effect. The degree of excretion is dose-dependent (at lower doses, the plasma T_1/2 is shorter).

Prednisolone

Prednisolone is metabolized in the liver after absorption. About 1% is excreted in the urine unchanged. The biological T_1/2 is 18-36 hours, and the plasma T_1/2 is 115-212 minutes.

Indications

External and internal hemorrhoids; thrombophlebitis of the hemorrhoidal veins of the anus; fistulas, eczema, and itching in the anal area; anal fissures; preparation for surgical intervention in the anorectal area; as part of the complex therapy of thrombosed or operated hemorrhoids.

ICD codes

Dosage Regimen

Apply externally and rectally. The dose and treatment regimen depend on the clinical indications and severity of symptoms.

For external application, apply a thin layer of ointment to the affected perianal area 2 to 4 times daily. Gently rub in until absorbed. For rectal administration, use the supplied applicator nozzle. Attach the nozzle securely to the tube.

Insert the nozzle gently into the anal canal and squeeze the tube to deliver the ointment. Apply 2 to 4 times daily, typically after bowel movements and at bedtime. The duration of treatment is usually 1 to 2 weeks, or as directed by a physician.

For the management of acute thrombosed hemorrhoids, apply the ointment every 4 to 6 hours during the initial 24-48 hours. For anal fissures, apply a sufficient amount to cover the fissure. Use consistently to maintain a protective layer and promote healing.

For pre-operative preparation, use as directed by the surgeon, typically for several days prior to the scheduled procedure. In post-operative care, apply to the operated area to reduce inflammation and prevent thrombosis.

Do not exceed the recommended frequency or duration of application. Discontinue use and consult a physician if no improvement is observed within 7 days, or if symptoms worsen. Avoid contact with eyes and mucous membranes other than the anorectal area.

Adverse Reactions

Local reactions: allergic reactions, skin hyperemia.

With prolonged use and/or application to large surfaces, systemic side effects are possible: slowing of the regeneration processes of fissures, edema.

Contraindications

Hypersensitivity to the components of the combination; bacterial, viral, fungal skin lesions; tuberculosis;
Syphilis; skin tumors (anorectal zone); predisposition to bleeding; reactions to vaccination;
The first trimester of pregnancy.

With caution

Childhood, the second and third trimesters of pregnancy, the period of breastfeeding.

Use in Pregnancy and Lactation

Use in the first trimester of pregnancy is contraindicated. In the second and third trimesters of pregnancy, use with caution when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

During breastfeeding, use with caution when the expected benefit for the mother outweighs the potential risk for the breastfed infant.

Special Precautions

As with the treatment with other corticosteroids, caution should be exercised, and this agent should not be used in large quantities or for a long time.

Drug Interactions

Concomitant use with other drugs for rectal use is not recommended.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.