Posterisan forte

INSTRUCTIONS
for medical use of medicinal product

POSTERISAN FORTE

Composition:

Active substances: 1 suppository contains 387.10 mg of standardized bacterial culture suspension (containing 1.0 × 10⁹ E. coli, killed and preserved in 6.6 mg of liquid phenol), 5.00 mg of hydrocortisone;

Excipients: hard fat, acetylcysteine, polyoxylated hydrogenated castor oil, alpha-tocopherol, disodium edetate (Trilon B).

Pharmaceutical form. Suppositories.

Basic physicochemical properties: homogeneous, white to beige suppositories with a characteristic phenol odor.

Pharmacotherapeutic group.

Agents for treatment of hemorrhoids and anal fissures for local use.

ATC code C05A A.

Pharmacological properties.

Pharmacodynamics.

The active substances of the medicinal product are standardized bacterial culture suspension (SBC), obtained from E. coli, and hydrocortisone.

For SBC production, bacteria are inactivated with phenol. The aqueous suspension is then processed into a galenical form. Thus, the final product contains intact cells, cellular degradation products, and metabolites, but no live bacteria.

After rectal administration (in rats and dwarf pigs), SBC is rapidly absorbed through the intestinal mucosa. When applied to the skin and mucous membranes, SBC stimulates non-specific and specific immune mechanisms. In vitro tests and animal models have shown that SBC induces T-lymphocyte proliferation and production of immunoglobulins (IgA and IgG). Thus, a polyclonal stimulation of the immune response is initiated, natural immune defense is enhanced, and susceptibility of affected tissues to infections is reduced.

In an in vitro model using human cell systems, lymphocyte proliferation is induced in an antigen-specific manner by Langerhans antigen-presenting cells. In vitro, SBC lyophilisates exert an inhibitory effect on provoked histamine release from mast cells and basophils, demonstrating anti-inflammatory properties. In vitro induction of various cytokines indicates possible involvement in tissue regeneration and thus promotes wound healing.

Animal and human studies also demonstrate immunogenic effects on inflammatory skin changes and wound-healing activity. Swelling decreases more rapidly when therapy includes SBC.

Hydrocortisone is a natural adrenal hormone and a precursor of synthetic glucocorticoids. Compared to them, hydrocortisone is classified as a low-potency glucocorticoid.

When applied locally to the skin or mucous membranes, hydrocortisone exerts acute anti-inflammatory, antipruritic, anti-allergic, and immunosuppressive effects, although the latter is less pronounced. However, there is no antiproliferative effect.

Hydrocortisone inhibits the release of lysosomal enzymes, migration of inflammatory cells, and synthesis of inflammatory mediators such as prostaglandins and leukotrienes. This leads to vasoconstriction and reduced vascular permeability in mesenchyme. Reactivity of connective tissue vessels is reduced, and inflammatory processes are suppressed.

Hydrocortisone affects the immune system by reducing immunogenic activity of T-lymphocytes, Langerhans cells, and macrophages. Antibody-mediated immediate reactions are diminished.

The action of hydrocortisone results from binding to cytosolic corticosteroid receptors, influencing RNA and protein synthesis.

The above-described effects of SBC and hydrocortisone complement each other in the medicinal product Postersan Forte.

Experiments have shown that hydrocortisone does not eliminate the immunopharmacological effects of SBC. Hydrocortisone does not impair the beneficial effect of SBC on wound healing. Anti-inflammatory and antipruritic effects of hydrocortisone support the enhanced immune defense mechanisms induced by SBC.

Pharmacokinetics.

Studies on absorption, systemic presence, and excretion are not feasible after local application of SBC. However, penetration of immunogenic components of SBC has been demonstrated in immunohistological studies of the rectal mucosa in animals (rats and dwarf pigs).

Topically applied hydrocortisone penetrates through the skin and accumulates in the epidermis and dermis. The degree of penetration varies by body site. Only a small amount of hydrocortisone enters the bloodstream from the dermis, thus not causing systemic side effects.

After local application, absorption of hydrocortisone through the rectal mucosa is significantly higher than through the skin. However, after therapeutic doses, the concomitant increase in blood concentration is transient, with peak levels reaching below the lower physiological range. There are no systemic side effects or impact on hormonal regulation.

Quantitative data on absorption and elimination of hydrocortisone are lacking.

Hydrocortisone is hydrogenated in the liver in the ring system and in keto groups, thus being rapidly inactivated. Elimination occurs predominantly via the kidneys as glucuronides and sulfate esters.

Clinical characteristics.

Indications.

Local treatment of hemorrhoid symptoms.

Contraindications.

Increased sensitivity to the active substance or to any component of the preparation.

Specific skin conditions (tuberculosis, syphilis, gonorrhea) in the application area, varicella, vaccination reaction, fungal infections, inflammatory skin diseases of the face (perioral dermatitis, rosacea), other bacterial, viral, parasitic infections at the application site, ulcerative lesions and atrophic changes at the application site, tumors of the anorectal zone.

Interaction with other medicinal products and other types of interactions.

Concomitant use of Postersan Forte suppositories with other corticosteroid-containing preparations (in tablet, drop, or injection form) may enhance both therapeutic and adverse effects of corticosteroids.

Special precautions for use.

Treatment should continue until symptoms disappear, but not longer than 5–7 days.

When using any topical steroids, systemic absorption should be considered possible.

In case of fungal infections, a topical antifungal medicinal product should be used concomitantly.

Contains polyoxylated hydrogenated castor oil. May cause local skin reactions.

Use during pregnancy or breastfeeding.

Pregnancy. There are no adequate data on the use of the medicinal product in pregnant women. Therefore, the drug should be used during pregnancy only if strictly indicated and after careful assessment of benefit/risk ratio.

Breastfeeding. Hydrocortisone is excreted in breast milk. Breastfeeding should be avoided during continuous use or use of high doses of hydrocortisone.

Ability to affect reaction speed when driving or operating machinery.

Data are lacking.

Method of administration and dosage.

Hygienic procedures of the anal area should be performed before administration.

For rectal use in adults: 1 suppository twice daily (in the morning and evening), preferably after defecation.

The duration of treatment is determined by the physician depending on the nature and course of the disease. Usually, the treatment period is 5–7 days.

Children.

Not to be used in children.

Overdose.

No cases of overdose or intoxication have been reported. Overdose may cause suppression of the hypothalamic-pituitary-adrenal system. Accidental oral administration of suppositories (e.g., by children) may result in gastrointestinal disturbances (abdominal pain, nausea).

Long-term use in high doses enhances absorption and increases the risk of systemic effects of hydrocortisone, such as menstrual cycle disturbances, increased blood pressure, delayed wound healing, muscle weakness, insomnia, elevated blood glucose levels.

If symptoms of hypercorticism occur, treatment should be discontinued.

Adverse reactions.

In individual cases, patients with increased sensitivity to components of PosteRISAN forte suppositories may experience hypersensitivity reactions, including itching and burning.

May cause contact dermatitis (e.g., due to hypersensitivity to phenol).

With prolonged use of the drug in high doses, the following dermatological reactions are possible: dermatitis, eczema, delayed healing of wounds and fissures, development of secondary infection, mucosal atrophy, skin atrophy, adrenocortical suppression, capillary dilation (telangiectasia), development of skin striae and steroid acne. Cushing's syndrome, hyperglycemia, glucosuria, growth retardation, intracranial hypertension, dry skin, "rebound effect" which may lead to steroid dependence.

Shelf life. 2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C, in a dry, light-protected place, out of reach of children.

Packaging.

5 suppositories per strip.

2 strips per cardboard pack.

Availability.

Over-the-counter.

Manufacturer.

Dr. Kade Pharmazeutische Fabrik GmbH.

Manufacturer's address and location of its business activities.

Riethstraße, 2, 12277 Berlin, Germany.