Instructions Posterizan forte suppositories strip No. 10
Composition
active ingredients: 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 liquefied phenol), 5.00 mg of hydrocortisone;
excipients: solid fat, acetylcysteine, polyethoxylated hydrogenated castor oil, alpha-tocopherol, disodium edetate (Trilon B).
Dosage form
Suppositories.
Main physicochemical properties: homogeneous suppositories from white to beige in color with a characteristic odor of phenol.
Pharmacotherapeutic group
Means for the treatment of hemorrhoids and anal fissures for topical use. ATX code C05A A.
Pharmacological properties
Pharmacodynamics. The active substances of the drug are standardized bacterial culture suspension (SBS) obtained from E. coli and hydrocortisone.
To produce SKB, bacteria are inactivated with phenol. The aqueous suspension is then processed into a galenic form. Therefore, the finished preparation contains intact cells, cell breakdown products, and metabolites, but does not contain live bacteria.
After rectal administration (in rats and dwarf piglets), SKB is rapidly absorbed through the intestinal mucosa. After application to the skin and mucosa, SKB stimulates nonspecific and specific immune mechanisms. In vitro tests and animal models have shown that SKB induces T-lymphocyte proliferation and the production of immunoglobulins (IgA and IgG). This triggers a polyclonal stimulation of the immune response, enhances natural immune defenses, and reduces the susceptibility of affected tissues to infections.
In an in vitro model on human cell systems, lymphocyte proliferation is induced in an antigen-specific manner by antigen-presenting Langerhans cells. In vitro, SKB lyophilizates have an inhibitory effect on the provoked release of histamine from mast cells and basophilic granulocytes, demonstrating anti-inflammatory properties. In vitro induction of various cytokines indicates a possible involvement in tissue regeneration and, accordingly, promotes wound healing.
Animal and human experiments also demonstrate an immunogenic effect on inflammatory skin changes, as well as a wound-healing effect. Swelling decreases more quickly when therapy includes SKB.
Hydrocortisone is a natural hormone of the adrenal gland and a precursor to synthetic glucocorticoids. Compared to them, hydrocortisone is classified as a low-potency glucocorticoid.
When applied topically to the skin or mucous membrane, hydrocortisone exhibits acute anti-inflammatory, antipruritic, antiallergic, and immunosuppressive effects, although the latter are less pronounced. However, there is no antiproliferative effect.
Hydrocortisone inhibits the release of lysosomal enzymes, the migration of inflammatory cells, and the synthesis of inflammatory mediators such as prostaglandins and leukotrienes. This causes vasoconstriction and a decrease in vascular permeability in the mesenchyme. The reactivity of connective tissue vessels is reduced, and inflammatory processes are suppressed.
Hydrocortisone affects the immune system, reducing the immunogenic activity of T-lymphocytes, Langerhans cells and macrophages. Immediate antibody-related reactions are reduced.
The action of hydrocortisone is a consequence of binding to the cytosolic corticosteroid receptor, which affects the synthesis of ribonucleic acid and protein.
The effects of SKB and hydrocortisone described above complement each other in the composition of the drug Posterisan forte.
Experiments have shown that hydrocortisone does not eliminate the immunopharmacological effects of SKB. Hydrocortisone does not impair the desired effect of SKB on wound healing. The anti-inflammatory and antipruritic effects of hydrocortisone support the enhanced immune defense mechanisms induced by SKB.
Pharmacokinetics.
Absorption, blood presence, and excretion studies cannot be performed after topical application of SKB. However, penetration of immunogenic components of SKB has been determined in immunohistological studies on the rectal mucosa of animals (rats and dwarf piglets).
Topically applied hydrocortisone penetrates the skin and accumulates in the epidermis and dermis. The degree of penetration through the skin varies depending on the site. Only a small amount of hydrocortisone enters the bloodstream from the dermis and therefore does not cause systemic side effects.
After topical application, the absorption of hydrocortisone through the rectal mucosa is significantly higher than through the skin. However, after the use of therapeutic doses, the concomitant increase in blood concentration is short-lived, with peak levels reaching lower physiological ranges. There are no systemic side effects or effects on hormonal regulation.
Quantitative data on the absorption and release of hydrocortisone are not available.
Hydrocortisone is hydrogenated in the liver at the ring system and at the keto groups and is thus rapidly inactivated. Excretion occurs mainly by the kidneys in the form of glucuronides and sulfate esters.
Indication
Local treatment of hemorrhoid symptoms.
Contraindication
Specific skin conditions (tuberculosis, syphilis, gonorrhea) in the area of application, chickenpox, reaction to vaccination, fungal diseases, inflammatory diseases of the facial skin (oral dermatitis, rosacea), other bacterial, viral, parasitic infections at the site of application, ulcerative lesions and atrophic changes at the site of application, tumors of the anorectal area.
Interaction with other medicinal products and other types of interactions
When Posterisan Forte suppositories are used simultaneously with other drugs containing corticosteroids (in the form of tablets, drops or injections), the therapeutic and side effects of corticosteroids may be enhanced.
Application features
Continue treatment until symptoms disappear, but not longer than 5–7 days.
When using any topical steroids, the possibility of systemic absorption should be kept in mind.
In case of fungal infections, a topical antifungal medication should be used simultaneously.
Contains polyethoxylated hydrogenated castor oil. May cause local skin reactions.
Use during pregnancy or breastfeeding
Pregnancy: There are no adequate data on the use of the drug in pregnant women. Therefore, the drug should be used during pregnancy only under strict indications and after a careful risk/benefit assessment.
Breastfeeding. Hydrocortisone is excreted in breast milk. Breastfeeding should be avoided during continuous use or use of high doses of hydrocortisone.
Ability to influence reaction speed when driving vehicles or other mechanisms
Data is missing.
Method of administration and doses
Before use, it is necessary to carry out hygienic procedures of the anal area.
Apply rectally to adults 1 suppository 2 times a day (morning and evening), if possible after defecation.
The duration of treatment is determined by the doctor depending on the nature and course of the disease. Usually the duration of use is 5–7 days.
Children.
Do not use on children.
Overdose
No cases of overdose or intoxication have been reported. Overdose causes suppression of the function of the hypothalamic-pituitary-adrenal system. In case of accidental oral administration of suppositories (e.g. by children), gastrointestinal disorders (abdominal pain, nausea) are possible.
Prolonged use in large doses increases resorption and increases the risk of developing systemic effects of hydrocortisone, such as menstrual irregularities, increased blood pressure, delayed wound healing, muscle weakness, insomnia, and increased blood sugar levels.
If symptoms of hypercorticism are observed, treatment should be discontinued.
Side effects
In some cases, patients with hypersensitivity to the 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 cracks, development of secondary infection, atrophy of the mucous membrane, atrophy of the skin, adrenocortical suppression, dilation of capillaries (telangiectasia), the appearance of stretch marks on the skin (striae) and steroid acne. Cushing's syndrome, hyperglycemia, glycosuria, growth retardation, intracranial hypertension, dry skin, "ricochet effect", which can lead to steroid dependence.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C, out of the reach of children and in a dry place, protected from light.
Packaging
5 suppositories per strip.
2 strips in a cardboard pack.
Vacation category
Without a prescription.
Producer
Dr. Kade Pharmaceutical Factory GmbH.
Address
Rigistrasse 2, 12277 Berlin, Germany.
