Properties
What is it?
1. Product Name CREPITANO Rectal Suppositories 2. Qualitative and Quantitative Composition Each suppository contains active substances, Heparin Sodium - 120 IU, Prednisolone Acetate - 1.675 mg and Lauromacrogol 400 - 30 mg. For a full list of excipients, see section 6.1. 3. Pharmaceutical Form Rectal suppositories. Cylindrical suppositories, white or white with a yellowish tint. The presence of air and porous inclusions and a funnel-shaped depression is allowed on the longitudinal section. 4. Clinical Data 4.1 Indications for Use Short-term symptomatic treatment of hemorrhoids and perianal itching. 4.2 Posology and Method of Administration Rectally, 1 suppository once a day after defecation. In case of pronounced symptoms, only on the first day of treatment, 1 suppository 2-3 times a day is possible. The course of treatment should not exceed 7 days. If symptoms persist, a proctological examination should be performed and the treatment reviewed. 4.3 Contraindications - Hypersensitivity to the active substances or any of the excipients listed in section 6.1; - Infections in the perianal area; - Tendency to bleeding; - First trimester of pregnancy; - Children under 12 years of age. 4.4 Special Warnings and Precautions for Use As with other corticosteroids, caution should be exercised to avoid using the product in large quantities or for prolonged periods. 4.5 Interactions with Other Medicinal Products and Other Forms of Interaction No interactions with other medicinal products have been described. Simultaneous use with other rectal preparations is not recommended. 4.6 Fertility, Pregnancy and Lactation Pregnancy Use in the first trimester of pregnancy is contraindicated. Caution is recommended in the II and III trimesters of pregnancy. Breastfeeding period The use of Crepitano suppositories during lactation is possible after careful assessment of the benefit/risk ratio (as prescribed by a doctor). 4.7 Effects on Ability to Drive and Use Machines The product does not affect the ability to drive vehicles and operate potentially dangerous machinery. 4.8 Undesirable Side Effects Undesirable side effects are classified according to organ systems and frequency of occurrence (MedDRA classification): very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10,000, <1/1,000), very rare (<1/10,000), frequency unknown (cannot be estimated from available data). Immune system disorders: Very rare - hypersensitivity reactions. General disorders and administration site reactions: Very rare - local irritation (there is a small chance of allergic reactions to Lauromacrogol 400). Prolonged use of the product may lead to delayed wound healing, as well as systemic adverse effects due to the use of prednisolone, manifested by edema. Reporting of suspected adverse reactions Continuous monitoring of the benefit-risk balance of the medicinal product is important. Reporting of suspected adverse reactions after the medicinal product is authorized. 4.9 Overdose Due to low absorption into the systemic circulation, overdose is unlikely. 5. Pharmacological Properties Pharmacotherapeutic group: Angioprotectors, agents for the treatment of hemorrhoids and anal fissures for topical use, ATC code: C05AX03. 5.1 Pharmacodynamic Properties Combined preparation for the treatment of hemorrhoids. The action is determined by the properties of the components included in the preparation. Heparin sodium is a direct-acting anticoagulant. When applied topically, it has local antithrombotic, antiexudative, and moderate anti-inflammatory effects, promotes connective tissue regeneration, and inhibits reactions that cause blood coagulation and thrombus formation in hemorrhoidal nodes. Prednisolone acetate is a synthetic glucocorticosteroid of medium duration of action, has anti-inflammatory, antiexudative, and antiallergic effects, reduces inflammation, itching, burning sensation, and pain in the anorectal area. Lauromacrogol 400 - a compound of the polyethylene glycol group, has a local anesthetic effect and promotes the sclerotherapy of hemorrhoidal nodes. 5.2 Pharmacokinetic Properties Heparin Sodium After topical application, a relatively small amount of heparin sodium is absorbed into the systemic circulation. Plasma protein binding is 95%. It is metabolized in the liver (partially by the liver heparinase enzyme) and in the reticuloendothelial system. 20-50% is excreted unchanged in the urine and partially as uroheparin, which has a weak anticoagulant effect. The elimination half-life is dose-dependent (increases with dose). Prednisolone Acetate The degree of subcutaneous absorption of glucocorticoids and systemic concentration depends on several factors, including the physicochemical properties of the preparation, the dose administered, the frequency of administration, and the duration of treatment. Some topical corticosteroids, including prednisolone acetate, are esterified in the skin by non-specific esterases. When released into the systemic circulation, they are mainly bound to plasma globulins (transcortin) and albumins. Induction of liver enzymes increases the clearance of prednisolone acetate. Approximately 1% is excreted unchanged in the urine. Clearance depends on the concentration level in blood plasma. The half-life from tissues is 18-36 hours, and from blood plasma - 115-212 minutes. Lauromacrogol 400 There is no data in the reference literature on the pharmacokinetics of Lauromacrogol 400 after topical application to the skin and mucous membranes. 5.3 Preclinical Safety Data Heparin is characterized by a relatively low level of toxicity. Acute toxicity experiments in rabbits showed that toxic effects occur at doses of 1000 mg or more. In chronic toxicity tests, 40 injections at 20 mg/kg in dogs and 30 injections at 40 mg/kg in rabbits did not lead to any organ changes in test animals. Studies in sheep have shown that heparin does not cross the placental barrier and does not exhibit embryotoxicity or teratogenicity. The very good tolerability of heparin in humans has been confirmed by medical practice. Given that the recommended single dose of heparin for intravenous and drip administration is from 5000 IU to 20000 IU, it is almost impossible to expect a toxic effect from a preparation containing 120 IU of heparin sodium in one suppository and used topically. There is limited data in the literature on the toxic effects of topical glucocorticoids. However, it is known that high doses of topical corticosteroids, under occlusive dressings and for prolonged periods, can cause fetal damage in experimental animals, although epidemiological studies of the use of these preparations during pregnancy in humans have not revealed an increased frequency of fetal malformations. Given that corticosteroids are absorbed into the systemic circulation in relatively small amounts after topical use, significant toxic effects should not be expected. There is no data in the literature on the toxicity of Lauromacrogol 400, except for isolated cases of allergic reactions when used as a sclerosing agent. 6. Pharmaceutical Properties 6.1 List of Excipients Colloidal anhydrous silica Medium-chain triglycerides Glyceryl tristearate Hard fat 6.2 Incompatibilities Not presented 6.3 Shelf Life 3 years 6.4 Special Precautions for Storage Store at a temperature not exceeding 25°C. 6.5 Nature and Contents of Packaging 5 suppositories in a PVC/PE blister pack. 2 blister packs with a leaflet in a cardboard box. 6.6 Special Precautions for Disposal of Unused Medicinal Product or Waste Materials Derived from Such Medicinal Products There are no special requirements for the disposal of unused medicinal product or waste materials derived from such medicinal products. Dispensing regime: Pharmaceutical product group - Group III, available without a prescription