Proctosan® neo

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PROCTOSAN® NEO (PROCTOSAN® NEO)

Composition:

Active substances: sodium heparin, prednisolone acetate, lauromacrogol 400;

1 g of ointment contains: sodium heparin 65 IU, prednisolone acetate 2.233 mg; lauromacrogol 400 30 mg;

Excipients: paraffin, mineral oil, lanolin, colloidal anhydrous silicon dioxide.

Pharmaceutical form. Rectal ointment.

Main physicochemical properties: yellowish-white semi-transparent ointment resembling a gel, with a characteristic odor.

Pharmacotherapeutic group. Agents for the treatment of hemorrhoids and anal fissures for topical use. ATC code C05AX03.

Pharmacological Properties

Pharmacodynamics. Proctosan® NEO provides effective treatment for the characteristic symptoms and consequences of hemorrhoids. The medication rapidly reduces inflammation in the anorectal area, as well as associated discomfort such as itching, burning, stinging, pain, and the sensation of moisture.

Proctosan® NEO, due to its pure heparin content, prevents thrombus formation in hemorrhoidal plexuses.

Prednisolone exerts anti-inflammatory and antiallergic effects.

Laurocaprate 400 (laureth-9) provides local analgesic action and relieves itching.

Pharmacokinetics. After topical application, heparin is detectable in the bloodstream at relatively low concentrations, which do not result in systemic effects. In the blood, it binds to plasma proteins (95%). It is metabolized in the liver (partially by the enzyme hepatic heparinase) and in the reticuloendothelial system. Elimination occurs via the kidneys. Between 20% and 50% of the administered dose is excreted unchanged in the urine. The half-life depends on the dose (increasing with higher dosages).

Prednisolone is present in the formulation and is absorbed in small amounts insufficient to produce systemic effects.

Laurocaprate 400 (laureth-9) acts exclusively locally.

Clinical characteristics.

Indications.

For symptomatic treatment of hemorrhoids and pruritus in the perianal area for a short period of time.

Contraindications.

Hypersensitivity to the components of the drug; infections in the perianal area; tendency to bleeding; specific skin lesions (e.g., syphilis); genital herpes; other viral infections; secondary skin infections in the absence of appropriate antibiotic therapy; first trimester of pregnancy. Tuberculous lesions of the anorectal zone.

Special precautions.

The product contains lanolin, which may cause local skin reactions (e.g., contact dermatitis).

Interaction with other medicinal products and other forms of interaction.

Interaction studies with the ointment have not been conducted.

CYP3A4 inhibitors, such as erythromycin, clarithromycin, ketoconazole, diltiazem, aprepitant, itraconazole, oleandomycin, and also cobicistat increase the elimination and plasma levels of prednisolone, thereby enhancing the therapeutic and adverse effects of the active substance prednisolone.

Proctosan® NEO, ointment for rectal and topical use, should not be used concomitantly with other medicinal products intended for rectal administration.

Special precautions for use.

If skin irritation or allergic reactions occur, the use of the drug should be discontinued immediately, and appropriate symptomatic therapy should be initiated. To avoid local or systemic toxicity, the drug should not be used for prolonged periods.

Cases of pheochromocytoma crisis have been reported after systemic corticosteroid use, which may lead to fatal outcomes. The drug should be prescribed to patients with suspected or confirmed pheochromocytoma only after a proper risk-benefit assessment.

Prolonged application of the drug to the same skin area may cause skin atrophy, particularly in younger patients.

The drug should be used with particular caution in patients with glucocorticoid-induced suppression of the hypothalamic-pituitary system.

Due to the presence of prednisolone in the formulation, prolonged use of Proctosan® NEO should be avoided, as it may cause dryness and microfissures in the anal canal. The drug is also contraindicated in infectious skin diseases of the perianal area and during pregnancy.

Visual disturbances have been reported with both systemic and topical use of corticosteroids. If symptoms such as blurred vision or other visual disturbances occur, patients should be referred to an ophthalmologist to identify possible causes, including cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which has been reported after both systemic and topical corticosteroid use. Central serous chorioretinopathy may lead to retinal detachment.

Use during pregnancy or breastfeeding. The drug is contraindicated during the first trimester of pregnancy. Caution is recommended during later stages of pregnancy (second and third trimesters).

The drug is not recommended during breastfeeding. Corticosteroids pass into breast milk and may thus affect adrenal cortex function in the newborn and impair growth.

Ability to influence reaction rate while driving or operating machinery. Proctosan® NEO ointment does not affect reaction speed while driving or operating machinery.

Method of administration and dosage.

Apply Proctosan® NEO, ointment for rectal and local use, to the affected areas of the skin twice daily after defecation. On the first day of treatment, to relieve symptoms, the ointment may be applied 4 times daily. The duration of therapy should not exceed 7 days.

For internal hemorrhoids, to ensure deep insertion of the ointment, attach the applicator to the tube, insert it into the rectum, and gently squeeze a small amount of ointment by pressing the lower part of the tube.

Children. Clinical experience with the use of the drug in children is lacking.

Overdose.

Since the drug, when applied topically, reaches only relatively low concentrations in systemic circulation, no toxic effects are expected.

Prolonged use of the drug in high doses may lead to symptoms of hypercorticism.

Symptoms: headache, heart failure, urticaria, rash, severe itching.

Treatment: symptomatic. The drug should be discontinued and medical advice sought.

In severe cases, emergency medical assistance is required.

In cases of skin atrophoderma associated with overdose during topical application of the drug, treatment should be discontinued. Symptoms usually regress within 10–14 days.

Adverse reactions.

The product is usually well tolerated; only in isolated cases may hypersensitivity reactions and local skin irritation occur (there is a slight possibility of allergic reactions to lauromacrogol 400).

Local treatment with corticosteroids may cause local adverse events such as dermatitis, folliculitis (at the application site), acneiform eruptions (steroid acne), contact dermatitis; dryness, thinning, and fragility of the skin; erythema, rash, urticaria, hirsutism, hyperhidrosis, intertrigo, pruritus, skin atrophy, hypopigmentation, skin irritation, striae formation, telangiectasias, burning sensation on the skin, purpura, delayed healing of fissures.

With prolonged local use, suppression of adrenal cortex function, hypercorticism, growth retardation, steroid myopathy, osteonecrosis, osteoporosis (as a manifestation of the resorptive effect of prednisolone), blurred vision, and choroidoretinopathy are possible.

Shelf life.

3 years.

Storage conditions. Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 20 g of ointment in a tube; 1 tube with an applicator in a cardboard box.

Availability. Over-the-counter.

Manufacturer. «Hemofarm» AD / «Hemofarm» AD.

Manufacturer's address and location of business activity.

Beogradski put bb, 26300, Vrsac, Republic of Serbia / Beogradski put bb, 26300, Vrsac, Republic of Serbia.