Procto-ointment

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PROCTO-OINTMENT

Composition:

Active substances: prednisolone; lidocaine; dexpanthenol;

1 g of the preparation contains 1.755 mg of prednisolone acetate, 20 mg of lidocaine hydrochloride, 20 mg of dexpanthenol;

Excipients: propylparaben (E 216), methylparaben (E 218), polysorbate 60, mineral oil, polyethylene glycol stearate, cetostearyl alcohol, glycerin, propylene glycol, medium-chain triglycerides, dimethicone, stearic acid, purified water.

Pharmaceutical form. Ointment.

Main physicochemical properties: homogeneous ointment of white or almost white color, practically odorless.

Pharmacotherapeutic group.

Agents for the treatment of hemorrhoids and anal fissures for topical use.

ATC code C05A X03.

Pharmacological properties.

Pharmacodynamics.

A combination drug containing substances that are effective in the treatment of inflammatory processes and pain in the perianal area, in an optimal ratio.

Prednisolone is a non-halogenated glucocorticoid with local anti-inflammatory action. It reduces vascular permeability, increases vascular wall tone, and decreases inflammation symptoms.

Lidocaine rapidly relieves pain and burning sensations.

Dexpanthenol promotes regeneration of damaged epithelium and mucous membranes.

Pharmacokinetics.

Pharmacokinetic studies with the ointment have not been conducted. The active substances of the medicinal product exert primarily local effects.

Prednisolone

Absorption. Topically applied prednisolone may be absorbed and may cause systemic effects (especially when applied under occlusive dressing, to damaged skin, or administered via rectal enema).

Distribution. Prednisolone is rapidly distributed into all tissues of the body. It binds strongly to plasma proteins. Prednisolone rapidly crosses the placenta and is excreted into breast milk.

Elimination. It is excreted in the urine as conjugated metabolites.

Lidocaine

Absorption. Lidocaine is well absorbed from mucous membranes and damaged skin.

Distribution. It binds strongly to plasma proteins. It crosses the placenta and the blood-brain barrier and penetrates into breast milk.

Biological transformation. Metabolized in the liver.

Elimination. Elimination half-life is 1–2 hours.

Renal impairment

Renal impairment does not affect lidocaine elimination, but may lead to accumulation of its active metabolite.

Clinical characteristics.

Indications.

Conditions associated with inflammation of the perianal area: pruritus, eczema and dermatitis of the perianal area, hemorrhoids, anal fissures.

Contraindications.

Hypersensitivity (allergy) to any of the active substances or to any of the excipients of the medicinal product.

Hypersensitivity to other amide-type local anesthetics (e.g., bupivacaine, etidocaine, mepivacaine, and prilocaine).

Treatment of eyes or periorbital area.

Primary bacterial, viral, or fungal skin infections, including herpes simplex.

Facial rosacea, common acne, perioral dermatitis, diaper rash, skin tuberculosis, cutaneous manifestations of syphilis, dryness, skin desquamation.

Concomitant treatment with lidocaine for other indications.

Age under 1 year.

First trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction.

Interaction studies with the use of the ointment have not been conducted.

The medicinal product should not be used if lidocaine is being used concomitantly for other indications.

Concomitant use with other antiarrhythmic agents requires caution.

Special precautions for use

If skin irritation or allergic reactions occur, the use of the medicinal product should be discontinued immediately and appropriate symptomatic therapy should be initiated.

To avoid local or systemic toxicity, the product should not be applied to large affected areas of skin, in skin folds, under occlusive dressings, and/or for prolonged periods.

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

In case of fungal or bacterial infections, appropriate local or systemic treatment should be administered.

The product should be used with special caution in patients with cataract, diabetes mellitus, glaucoma, tuberculosis, or anemia, as well as in patients with glucocorticoid-induced suppression of the hypothalamic-pituitary-adrenal axis.

Visual disturbances

Visual disturbances may occur 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 for evaluation. Cases of cataract, glaucoma, or the rare condition known as central serous chorioretinopathy have been reported following systemic and topical corticosteroid use. Central serous chorioretinopathy may lead to retinal detachment.

The medicinal product contains propylparaben (E 216) and methylparaben (E 218), which may cause allergic reactions (possibly delayed); cetostearyl alcohol, which may cause local skin reactions (e.g., contact dermatitis); and propylene glycol, which may cause skin irritation.

Use during pregnancy or breastfeeding

Pregnancy. The medicinal product is contraindicated during the first trimester of pregnancy. When prescribing the product during the second and third trimesters of pregnancy, the benefit-risk ratio must be carefully evaluated.

Breastfeeding. Corticosteroids and lidocaine pass into breast milk. Thus, corticosteroids may affect the adrenal cortex function in the newborn and impair growth. Small amounts of lidocaine appear in breast milk. Although in practice this poses no significant risk to the infant, caution should be exercised when the product is used in breastfeeding women.

Ability to affect reaction speed when driving or operating machinery

The potential effect of the medicinal product on the ability to drive vehicles or operate machinery has not been studied.

Dosage and Administration.

For external use only. Prolonged application and use over large areas of skin should be avoided regardless of patient age. Use under occlusive dressing is not recommended.

Adults and elderly patients. Apply a thin layer of the ointment to the affected area 2–4 times daily. As symptoms improve, the ointment should be applied less frequently. Treatment duration should not exceed 5–7 days.

Children. In children aged 1 year and older, the product may be used only in exceptional cases, in the minimal dose required to achieve therapeutic effect, and no more than twice daily. Treatment duration in children should not exceed 5 days.

Children.

The ointment is contraindicated in children under 1 year of age.

Overdose.

May manifest with local or systemic symptoms depending on the amount of absorbed corticosteroid and lidocaine. There is no specific antidote; supportive therapy should be administered.

Adverse reactions.

Local treatment with corticosteroids may cause local adverse events.

With prolonged topical use or application over large skin areas, suppression of adrenal cortex function may occur. This is particularly common when the ointment is used in children or under occlusive dressings. Protein catabolism may lead to a negative nitrogen balance.

Systemic absorption of a large amount of lidocaine after topical application may result in stimulation and/or depression of the central nervous system.

Depending on the amount of absorbed corticosteroid and lidocaine, the following adverse effects may occur:

Infections and infestations: activation of subclinical infections, masking of infection signs, opportunistic infections;

Immune system disorders: hypersensitivity reactions;

Endocrine system disorders: suppression of adrenal cortex function, hypercorticism (as a manifestation of the resorptive effect of prednisolone);

Metabolism and nutrition disorders: hypokalemic alkalosis, sodium and fluid retention, hypokalemia;

Psychiatric disorders: insomnia, psychiatric disturbances;

Central nervous system disorders: seizures, dizziness, headache, increased intracranial pressure;

Eye disorders: cataract (children have a higher risk of developing cataract), subcapsular cataract, exophthalmos, glaucoma, optic disc edema, corneal ulcer, chorioretinopathy, blurred vision (see section "Special precautions");

Cardiac disorders: heart failure, cardiac conduction disturbances;

Vascular disorders: arterial hypertension, peripheral vasodilation;

Gastrointestinal disorders: gastric bleeding, gastrointestinal hemorrhage, perforation of gastrointestinal organs, esophagitis, pancreatitis, peptic ulcer;

Skin and subcutaneous tissue disorders: dermatitis, folliculitis (at the application site), acneiform eruptions (steroid acne), contact dermatitis; dryness, thinning and fragility of the skin; erythema, urticaria, hirsutism, hyperhidrosis, intertrigo, pruritus, skin atrophy, hypopigmentation, skin irritation, striae formation, telangiectasia, burning sensation, purpura;

Musculoskeletal and connective tissue disorders: growth retardation (in children), steroid myopathy, osteonecrosis, osteoporosis;

General disorders and administration site conditions: delayed wound healing;

Investigations: increased intraocular pressure, negative nitrogen balance, suppressed response in skin provocation tests.

Reporting of adverse reactions.

Reporting suspected adverse reactions after drug registration is important. It allows continuous monitoring of the benefit-risk ratio of the medicinal product. Healthcare professionals and patients or their legal representatives should report any suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature between 2 °C and 8 °C.

Keep out of reach of children.

Packaging. 20 g in a tube; 1 tube per cardboard box.

Prescription status. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and location of business activity.

Ukraine, 61013, Kharkiv Oblast, Kharkiv, Shevchenko Street, 22.

Ukraine, 08301, Kyiv Oblast, Boryspil, Shevchenka Street, 100, lit. B-II (Building 4).