Instructions for use POLCORTOLON

Pharmacological properties of the drug Polcortolone

Triamcinolone (9α-fluoro-11β,16α, 17α, 21-tetrahydroxy-1,4-pregnadieno-3,20-dione) is a synthetic fluorinated corticosteroid, a prednisolone derivative with a pronounced anti-inflammatory effect. Triamcinolone at a dose of 4 mg is equivalent in anti-inflammatory activity to 4 mg methylprednisolone, 5 mg prednisolone, 0.75 mg dexamethasone, 0.6 mg betamethasone and 20 mg hydrocortisone. It has a weak mineralocorticoid effect. Triamcinolone inhibits the development of symptoms of inflammation without affecting the cause of its occurrence, inhibits the accumulation of macrophages, leukocytes and other cells at the site of inflammation. Inhibits phagocytosis, the release of lysosomal enzymes, as well as the synthesis and release of inflammatory mediators. Reduces the expansion and permeability of capillaries, which leads to a decrease in edema. The drug has an immunosuppressive effect, that is, it inhibits cellular immune reactions, reduces the number of T-lymphocytes, monocytes and acidophilic granulocytes. It may also inhibit the penetration of immune complexes through membranes and reduce the concentration of complement components and immunoglobulins. Triamcinolone inhibits the release of ACTH by the pituitary gland, which leads to a decrease in the synthesis of GCS in the adrenal cortex: after a single dose of triamcinolone in a dose of 60–100 mg, the suppression of adrenal function persists for 24–48 hours and returns to the original level after 30–40 days. Almost every patient taking the drug at a dose of 12–16 mg/day for more than 10 days may develop adrenal insufficiency. After long-term use of triamcinolone in high doses, adrenal function can recover within a year, and in some cases, its impairment is irreversible. Triamcinolone enhances protein catabolism, inhibits the synthesis and enhances the breakdown of proteins in lymphatic, connective, muscle tissue and skin, which can lead to their atrophy. The drug causes an increase in the concentration of glucose in the blood serum, affects fat metabolism, and increases the concentration of fatty acids in the blood plasma. With prolonged use, improper distribution of adipose tissue may occur. The drug slows down the synthesis of bone tissue, reduces the concentration of calcium in the blood plasma, can inhibit bone growth in children and adolescents and lead to the development of osteoporosis at any age. Enhances the effect of endo- and exogenous catecholamines. The bioavailability of triamcinolone after oral administration is 20–30%. The effect appears after 1-2 hours and lasts for 6-8 hours. The half-life of triamcinolone from blood serum is ≥2-5 hours, from tissues - 18-36 hours. The period of action is 54 hours, food inhibits the absorption of triamcinolone in the initial phase , but does not affect the overall bioavailability of the drug. About 40% of triamcinolone is bound to serum proteins (mainly globulins). The volume of distribution of the free fraction of the drug is 0.6–2 dm3/kg body weight. The drug is metabolized in the liver, and to a lesser extent in the kidneys. It is excreted from the body mainly in the urine in the form of inactive metabolites, ≤15% is unchanged triamcinolone. Three metabolites of triamcinolone acetate have been identified: 6β-hydroxytriamcinolone acetate, 21-carboxy-6β-hydroxytriamcinolone acetate, and 21-carboxytriamcinolone acetate. Triamcinolone penetrates the placental barrier and into breast milk.

Analogs

There are several analogues of Polcortolone:

1. "Kenalog" in the form of a solution for injection. Has the same composition. Its price is five hundred seven rubles per pack of five ampoules. Or you can purchase the drug in tablets for three hundred and ten rubles per pack of fifty pieces.
2. "Polcortolone" in tablet form has a similar composition. The price of the drug is three hundred and seventy rubles.

   

Indications for use of the drug Polcortolon

Endocrine diseases: primary (Addison's disease) and secondary adrenal insufficiency, adrenogenital syndrome (congenital, adrenal hyperplasia), acute adrenal insufficiency, use before surgical interventions in severe diseases and injuries with adrenal insufficiency, thyroiditis (non-purulent). Severe allergic diseases, when other treatment methods are ineffective: contact and atopic dermatitis, serum sickness, hypersensitivity reaction to medications, persistent or seasonal allergic rhinitis, anaphylactic reactions (GCS - as an auxiliary treatment when other treatment methods are ineffective), vasomotor edema, acute non-infectious edema larynx (drug of choice - epinephrine). Collagenoses (during an exacerbation or in some cases as maintenance therapy): rheumatic or non-rheumatic myocarditis, dermatomyositis, systemic lupus erythematosus, giant cell inflammation of the temporal artery, some connective tissue diseases, nodular inflammation of the arteries, recurrent polycartilaginous inflammation, polymyalgia rheumatica, vascular inflammation. Dermatological diseases: skin inflammation - atopic, contact, desquamation, severe polymorphic erythema (Stevens-Johnson syndrome), granuloma fungoides, pemphigus, severe psoriasis, severe eczema, pemphigoid. Gastrointestinal diseases (during exacerbation; long-term treatment is contraindicated): ulcerative colitis, Crohn's disease, severe celiac disease. Hematological diseases: hemolytic acquired anemia (due to autoimmunization), congenital aplastic anemia, hypoplastic anemia, secondary thrombocytopenia in adults, idiopathic thrombocytopenic purpura (Werlhof's disease) in adults, hemolysis. Liver diseases (there are doubts regarding the use of GCS): alcoholic hepatitis with encephalopathy, active chronic hepatitis, non-alcoholic hepatitis in women, subacute liver necrosis. Hypercalcemia associated with cancer or sarcoidosis. Non-rheumatic diseases of the joints (short-term, as an auxiliary treatment, during exacerbations): acute and subacute inflammation of the synovial membrane, inflammation of the epicondyle, nonspecific acute inflammation of the tendon sheaths, post-traumatic inflammation of bones and joints. Oncological diseases (as palliative treatment, in combination with antitumor treatment): lymphoblastic acute and chronic leukemia, warty and non-warty lymphangiomas, breast cancer, prostate cancer, multiple myeloma, fever associated with cancer. Nephrotic syndrome Neurological diseases: tuberculous inflammation of the meninges with subarachnoid block (simultaneously with anti-tuberculosis treatment), multiple sclerosis during an exacerbation, muscle weakness. Ophthalmological diseases: inflammation of the iris and ciliary body, inflammation of the choroid and retina, diffuse inflammation of the choroid of the posterior chamber of the eye, inflammation of the optic nerve, sympathetic inflammation of the vascular wall, inflammation of the anterior chamber of the eye, allergic inflammation of the conjunctiva, inflammation of the cornea (unrelated to viral infection herpes or fungal infection), marginal ulceration of the cornea associated with allergies. Oral diseases: desquamative gingivitis. Inflammation of the pericardium. Diseases of the respiratory system: asthma, beryliosis, Lefler's syndrome, pneumonia, symptomatic sarcoidosis, fulminant or miliary form of pulmonary tuberculosis (with simultaneous anti-tuberculosis treatment), COPD. Rheumatic diseases (as an auxiliary treatment during exacerbation): ankylosing spondylitis, psoriatic arthropathy, desquamative inflammation of the joints, rheumatoid inflammation of the joints, juvenile rheumatoid inflammation of the joints (if other treatment methods are ineffective), acute gouty inflammation of the joints, bursitis in osteoarthritis, Reiter's disease, rheumatic fever fever. Prevention and treatment of transplant rejection (simultaneously with other immunosuppressive drugs).

Use of the drug Polcortolon

The course and dose are selected individually depending on the course of the disease and clinical effect. It is recommended to use the drug in accordance with the circadian rhythm once a day in the morning. In some cases, it may be necessary to take triamcinolone more frequently. Adults and children over 14 years of age: 4–48 mg/day in one or more divided doses. Children over 6 years of age: 0.1–0.5 mg/kg body weight per day in one or more divided doses.
For adrenal insufficiency - 4-12 mg/day in one dose in the morning or in two doses (morning and afternoon), children - 0.1 mg/kg body weight per day once in the morning or in two doses. The maximum daily dose for children weighing up to 25 kg is 12–14 mg.

Release form and composition

Dosage forms of Polcortolone:

• Tablets: flat, round, white or almost white, chamfered, engraved “O” on one side, “4/mg” on the other (25 pcs. in a PVC/aluminum foil blister, 2 blisters in a cardboard pack );
• Ointment for external use: translucent, white or almost white fatty mass with the smell of an ointment base (15 g in an aluminum tube, 1 tube in a cardboard box).

Composition of 1 tablet:

• Active ingredient: triamcinolone – 4 mg;
• Additional components: lactose, magnesium stearate, potato starch.

Composition of 1 g ointment:

• Active ingredient: triamcinolone acetonide – 1 mg;
• Additional components: white petroleum jelly, propylene glycol, citric acid, lanolin.

Side effects of the drug Polcortolone

With short-term use of triamcinolone, side effects are rare. With long-term use, the following side effects are possible: From the side of water-electrolyte balance: sodium and fluid retention, congestive circulatory failure, calcium loss, hypokalemic alkalosis, increased blood pressure. From the musculoskeletal system: muscle weakness, steroid myopathy, decreased muscle mass, osteoporosis, bone fragility. From the gastrointestinal tract: peptic ulcers and their complications: bleeding, perforation of the large or small intestine, especially in patients with an inflammatory process in the small intestine, pancreatitis, flatulence, ulcerogenic inflammation of the esophagus, indigestion, increased appetite. Skin: rash, delayed wound healing, thinning of the skin, ecchymoses and hematomas, erythema, increased sweating, allergic skin inflammation, urticaria, vasomotor edema. From the nervous system: convulsions, increased intracranial pressure with papillary edema, dizziness and headache. Endocrine disorders: menstruation disorders, Cushing's syndrome, growth retardation in children, secondary insufficiency of the adrenal cortex and pituitary gland, in diseases, injuries, surgical interventions, diabetes, increased need for insulin and antidiabetic drugs in patients with diabetes; hirsutism. From the organ of vision: cataracts, increased intraocular pressure, glaucoma, exophthalmos. Metabolic disorders: negative nitrogen balance, increased concentrations of glucose in the blood and urine. Others: hypersensitivity reactions, thromboembolic syndromes, weight gain, nausea, poor health, mental disorders, sleep disorders.

Reviews

Polcortolon has mixed reviews. Some patients have a negative attitude towards the drug, as it provokes a large list of adverse reactions. That not everything is suitable even when taken correctly. Nevertheless, it is quite strong and can eliminate the unpleasant symptoms of various diseases. Doctors recommend undergoing an examination before starting treatment in order to minimize the risk of adverse reactions.

Since the drug is hormonal, it often leads to weight gain in females, which is why they do not like this drug. But in the presence of severe pathologies that cannot be treated with other medications, they are ready to use Polcortolone, despite the huge number of negative phenomena.

The aerosol, when used correctly and for a short course of therapy, is usually well tolerated. Moreover, it also contains an antibacterial substance. This significantly improves the results of therapy. Skin manifestations can be eliminated after just two weeks of using the spray. But it is recommended to use it in minimal quantities and for a short time.

The drug has many contraindications and adverse reactions, but it is widely used in medicine, as it has proven its high effectiveness.

Special instructions for the use of Polcortolon

Sudden discontinuation may cause symptoms of adrenal insufficiency, so the dose of triamcinolone should be reduced gradually. Patients taking triamcinolone are not recommended to be vaccinated with live viral vaccines. The use of an inactivated viral or bacterial vaccine may not be accompanied by the expected increase in antibody titer. In case of active tuberculosis, the use of triamcinolone should be limited and carried out simultaneously with antibacterial therapy. Patients with latent tuberculosis or a positive tuberculin test should be under medical supervision due to the possibility of exacerbation of the tuberculosis process, and with long-term use of the drug, take prophylactic antibacterial drugs. Sudden cessation of use after long-term use can cause GCS withdrawal syndrome , manifested by fever, myalgia, arthralgia, and poor health. These symptoms can occur even in the absence of adrenal insufficiency. Triamcinolone may mask symptoms of infection by reducing resistance to infection and the ability to contain the lesion. In persons arriving from tropical countries, infection with dysenteric amoeba should be excluded before using the drug. Triamcinolone in high doses can cause an increase in blood pressure, water and sodium retention, and increase the excretion of potassium and calcium. In people with thyroid deficiency and liver cirrhosis, triamcinolone is more active, so the drug should be used in lower doses. For herpetic eye infections, triamcinolone is used with caution due to the risk of corneal perforation. Long-term use of the drug can cause clouding of the lens, glaucoma with damage to the optic nerve, and also increase the risk of secondary fungal or viral eye infections. With prolonged use, the drug should be prescribed in the minimum effective doses. Use triamcinolone with caution in combination with acetylsalicylic acid for hypoprothrombinemia. Triamcinolone should be used only for reasonable indications and with great caution in cases of ulcerative colitis, intestinal diverticula, peptic ulcers of the stomach or duodenum, renal failure, hypertension, osteoporosis, muscle fatigue, diabetes, hypofunction of the liver, glaucoma, candidiasis or viral infection. Animal studies have established a risk of teratogenicity. Polcortolone used during pregnancy can cause placental insufficiency, fetal adrenal insufficiency, low birth weight or fetal death. The use of GCS by women of reproductive age and pregnant women is permissible only for health reasons or in cases where the benefit of the drug outweighs the potential threat to the fetus. Polcortolone is excreted into breast milk and causes undesirable effects in the baby. In newborns and infants whose mothers took triamcinolone for a long time or in high doses, the drug may cause inhibition of growth and development. Breastfeeding should be stopped while taking triamcinolone.

Contraindications

Tablets Absolute:

• Age up to 3 years;
• Systemic mycoses;
• Hypersensitivity to the components of the drug.

Relative (should be used with extreme caution due to the high risk of complications):

• Parasitic and infectious diseases of fungal, viral or bacterial origin (including recent ones, as well as recent contact with a patient): chicken pox, herpes zoster (viremic phase), herpes simplex, measles, systemic mycosis, strongyloidiasis (diagnosed or suspected), amebiasis, latent and active tuberculosis (use for the treatment of severe infectious lesions is permissible only with specific therapy);
• Post-vaccination period (including 56 days before and 14 days after vaccination), lymphadenitis that developed after BCG vaccination; immunodeficiency conditions (including AIDS and HIV infection);
• Lesions of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, nonspecific ulcerative colitis with the threat of abscessation or perforation, gastritis, esophagitis, diverticulitis, peptic ulcer (acute and latent), newly formed intestinal anastomosis;
• Diseases of the cardiovascular system: arterial hypertension, chronic heart failure in the stage of decompensation, recent myocardial infarction (acute and subacute form), hyperlipidemia;
• Diseases of the endocrine system: hypothyroidism, thyrotoxicosis, diabetes mellitus (including impaired carbohydrate tolerance), Itsenko-Cushing's disease;
• Severe form of chronic renal and/or liver failure nephrourolithiasis;
• Hypoalbuminemia and conditions leading to its appearance;
• Systemic osteoporosis, myasthenia gravis, poliomyelitis (except for the form of bulbar encephalitis);
• Acute psychosis;
• Open- and closed-angle glaucoma;
• Obesity III-IV degree.

Ointment for external use

• Age up to 2 years;
• Trophic ulcers of the legs against the background of varicose veins;
• Fungal and viral skin lesions;
• Lupus;
• Chicken pox;
• Precancerous skin conditions;
• Skin neoplasms;
• Perioral dermatitis;
• Rosacea and vulgar acne;
• Hypersensitivity to the components of the drug.

During breastfeeding and pregnancy, Polcortolone can be used in exceptional cases when the expected benefits of therapy outweigh the possible risk of side effects. When prescribing the drug during lactation, breastfeeding should be stopped.

The ointment should not be applied to the skin of the mammary glands.

Interactions of the drug Polcortolone

The combination of triamcinolone with the following drugs causes: NSAIDs, alcohol - an increased risk of ulcers and gastrointestinal bleeding. Amphotericin B, carbonic anhydrase inhibitors - hypokalemia, myocardial hypertrophy, congestive circulatory failure. Paracetamol - hypernatremia, edema, increased calcium excretion, increased hepatotoxicity of paracetamol. Anabolic steroids, androgens - swelling, rash. Anticholinergic drugs (mainly atropine) - increase intraocular pressure. Anticoagulants, coumarin derivatives, indadione, heparin, streptokinase, urokinase - decreased, in some patients - increased effect; increased risk of ulceration and gastrointestinal bleeding. Tricyclic antidepressants - increased mental disorders. Oral antidiabetic drugs, insulin - weakening of the antidiabetic effect. Triamcinolone alters thyroid function, so it may be necessary to change the dose or stop taking anti-thyroid medications or thyroid hormones. Oral contraceptives containing estrogens enhance the effect of triamcinolone. Digitalis glycosides - tachycardia and increased toxicity of glycosides. Diuretics - weakening of the effect of diuretics, hypokalemia. Folic acid - increasing the need for this product. Immunosuppressive drugs - increased risk of infection, development of lymphangiomas and other lymphoproliferative diseases. Isoniazid - a decrease in the concentration of isoniazid in the blood serum, mainly in individuals with rapid acetylation, dose adjustment may be necessary. Mexiletine - accelerated metabolism of mexiletine and a decrease in its concentration in the blood serum. Sodium salts - edema, increased blood pressure; You may need to limit your intake of high sodium medications and the amount of sodium in your diet; Vaccines containing live viruses - during the use of GCS in immunosuppressive doses, the development of viral diseases and a decrease in the effectiveness of vaccination are possible. Other vaccines increase the risk of developing neurological complications, as well as reduce the formation of antibodies.