Anestelax (Suppositories) Instructions for Use

Marketing Authorization Holder

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

ATC Code

C05AX03 (Preparations for the treatment of hemorrhoids and anal fissures in combination)

Active Substances

Heparin sodium (Rec.INN registered by WHO)

Benzocaine (Rec.INN registered by WHO)

Dosage Form

Anestelax

Rectal suppositories 1000 IU+50 mg: 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Rectal suppositories white or white with a yellowish tint, torpedo-shaped; the appearance of a coating on the surface of the suppository and the presence of an air core and a funnel-shaped depression on the cut are allowed.

Excipients: purified water, hard fat (witepsol grade H 15: witepsol W 35 (1:1), suppocire grade NA 15: suppocire NAS 50 (1:1)), distilled monoglycerides (Palsgaard 0093).

5 pcs. – contour cell packaging (1) – cardboard packs.
5 pcs. – contour cell packaging (2) – cardboard packs.

Clinical-Pharmacological Group

A drug with antithrombotic and local anesthetic action for topical use in proctology

Pharmacotherapeutic Group

Hemorrhoid treatment agent

Pharmacological Action

Combined drug for rectal use.

Heparin is a direct-acting anticoagulant belonging to the group of medium molecular weight heparins.

When applied externally, it has a local anticoagulant, anti-exudative, and moderate anti-inflammatory effect.

It blocks the formation of thrombin.

Heparin reduces the inflammatory process and has an anticoagulant effect, indirectly improves microcirculation, which promotes the process of resorption of hematomas and blood clots and reduces tissue swelling.

Benzocaine is a local anesthetic for superficial anesthesia.

By reducing the permeability of the cell membrane to sodium ions, it blocks the conduction of nerve impulses.

It prevents the occurrence of pain impulses in the endings of sensory nerves and their conduction along nerve fibers.

Pharmacokinetics

Heparin. It is absorbed insignificantly. Plasma protein binding is up to 95%, V_d is 0.06 l/kg.

It does not cross the placental barrier and into breast milk.

It is intensively captured by endothelial cells and cells of the mononuclear-macrophage system, concentrated in the liver and spleen.

It is metabolized in the liver by N-desulfamidase and platelet heparinase, which is involved in the metabolism of heparin at later stages.

Desulfated molecules are converted into low molecular weight fragments under the influence of renal endoglycosidase.

T_1/2 is 1-6 hours (on average – 1.5 hours); it increases with obesity, hepatic and/or renal failure; it decreases with pulmonary embolism, infections, malignant tumors.

It is excreted by the kidneys mainly in the form of inactive metabolites, and only when used in high doses is excretion (up to 50%) in unchanged form possible. It is not excreted by hemodialysis.

Benzocaine is practically not absorbed when applied externally.

It is hydrolyzed by plasma and hepatic cholinesterase to metabolites of para-aminobenzoic acid and is excreted in the urine.

Indications

Thrombosis of external and internal hemorrhoids.

ICD codes

Dosage Regimen

Administer rectally.

Use one suppository twice daily, typically in the morning and evening.

The standard treatment course is 10 to 14 days.

Continue use for the full prescribed duration, even if symptoms improve earlier.

Do not exceed the recommended dosage and duration of use.

For administration, ensure hands are clean. Remove the suppository from its packaging immediately before use.

Insert the suppository completely into the rectum, pointed end first.

If symptoms persist after 7 days of treatment, discontinue use and consult a physician.

Adverse Reactions

Possible allergic reactions.

There are isolated reports of cases of methemoglobinemia with the use of drugs containing Benzocaine.

Contraindications

Hypersensitivity to the components of the combination; increased tendency to bleeding, thrombocytopenia; children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding, because the safety of this combination in this category of patients has not been established.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

In case of heavy bloody discharge from the rectum or if painful symptoms persist for more than 7 days, it is necessary to additionally consult a proctologist.

When using this product, it is necessary to monitor the hygiene of the anal area, avoid excessive straining, and take measures to maintain a soft stool consistency.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.