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.
Polcortolone
The incidence and severity of side effects depend on the duration of use, the size of the dose used and the ability to comply with the circadian rhythm of the prescription.
With short-term use of Polcortolone, like other glucocorticosteroids, side effects are rarely observed. When using Polcortolone for a long time, the following side effects may develop:
From the endocrine system:
Secondary adrenal and hypothalamic-pituitary insufficiency (especially during stressful situations such as illness, injury, surgery); Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae), delayed sexual development and growth suppression in children, menstrual irregularities, decreased glucose tolerance, manifestation of latent diabetes mellitus and increased need for insulin or oral hypoglycemic drugs in patients with diabetes mellitus, hirsutism.
From the digestive system:
“Steroid” ulcer of the stomach and duodenum with possible perforation and bleeding, pancreatitis, flatulence, erosive esophagitis, indigestion, nausea, vomiting, increased or decreased appetite, hiccups. In rare cases, increased activity of liver transaminases and alkaline phosphatase.
From the cardiovascular system:
Arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, arterial hypertension, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
From the nervous system:
Delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure with congestive papilla syndrome (pseudotumor cerebri - most often in children, usually after too rapid dose reduction; symptoms - headache, worsening of acuity vision or double vision); vertigo, pseudotumor of the cerebellum, convulsions, dizziness, headache, nervousness or anxiety, sleep disturbances.
From the senses:
Posterior subcapsular catarct, increased intraocular pressure with possible damage to the optic nerve, glaucoma, exophthalmos, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea.
From the side of metabolism:
Negative nitrogen balance as a result of protein catabolism, hyperglycemia, glycosuria, increased Ca2+ excretion, hypocalcemia, weight gain, increased sweating, sodium and fluid retention in the body (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).
From the musculoskeletal system:
Slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, compression fracture of the spine, aseptic necrosis of the head of the humerus and femur, pathological fractures of long tubular bones), rupture of muscle tendons, muscle weakness, “steroid” myopathy, decreased muscle mass (atrophy).
From the skin and mucous membranes:
Steroid acne, stretch marks, delayed wound healing, thinning of the skin, petechiae, ecchymoses, hematomas, a tendency to develop pyoderma and candidiasis.
Allergic reactions:
skin rash, itching, anaphylactic shock.
Other:
Development and exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.
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).
Polcortolon
With the simultaneous use of Polcortolone and cardiac glycosides, the risk of developing heart rhythm disturbances and other toxic effects of glycosides associated with hypokalemia increases.
When used simultaneously with Polcortolone, barbiturates, anticonvulsants (phenytoin, carbamazepine), rifampicin, glutethimide accelerate the metabolism of triamcinolone (due to the induction of microsomal enzymes) and weaken its effect.
When used simultaneously, histamine H1 receptor blockers weaken the effect of Polcortolone.
When using Polcortolone together with amphotericin B, carbonic anhydrase inhibitors, the risk of developing hypokalemia, left ventricular myocardial hypertrophy and circulatory failure increases.
With simultaneous use of Polcortolone with paracetamol, the likelihood of hypernatremia, peripheral edema, increased calcium excretion increases, and the risk of hypocalcemia, osteoporosis, and hepatotoxicity of paracetamol increases.
When using Polcortolone together with anabolic steroids or androgens, the risk of developing peripheral edema and acne increases (this combination requires caution, especially in the case of liver and heart diseases).
When used in combination, hormonal contraceptives containing estrogens enhance the effect of Polcortolone by increasing the concentration of globulins that bind corticosteroids in the blood serum, slowing their metabolism and increasing T1/2.
With simultaneous use of Polcortolone with anticholinergic drugs (atropine), intraocular pressure may increase.
Anticoagulants (coumarin derivatives, indanedione, heparin), streptokinase, urokinase reduce (in some patients increase) the effectiveness of Polcortolone. The dose should be determined based on prothrombin time and take into account the increased risk of ulcerative lesions and gastrointestinal bleeding.
The combined use of tricyclic antidepressants may increase the mental disorders associated with taking Polcortolone (this combination is not recommended).
With simultaneous use, Polcortolone weakens the effect of oral hypoglycemic drugs, insulin, increases the concentration of glucose in the blood (dosage adjustment of hypoglycemic drugs may be required).
When using Polcortolone together with antithyroid drugs and thyroid hormones, changes in thyroid function may occur (dose adjustment or discontinuation of the antithyroid drug or thyroid hormones may be required).
Polcortolone weakens the effect of potassium-sparing diuretics. Concomitant use may cause hypokalemia.
Polcortolone reduces the effectiveness of laxatives, thereby increasing the risk of hypokalemia.
When used simultaneously, ephedrine accelerates the biotransformation of triamcinolone, which may require dose adjustment of Polcortolone.
When using Polcortolone and immunosuppressants together, the risk of developing infections, lymphomas and other lymphoproliferative diseases increases.
When used together with isoniazid, a decrease in the concentration of isoniazid in the blood plasma may occur (mainly in individuals with rapid acetylation), in which case a dose change is necessary.
When used together, the metabolism of mexiletine accelerates and its concentration in the blood plasma decreases.
When used concomitantly with depolarizing muscle relaxants, hypocalcemia associated with the use of Polcortolone may increase the duration of neuromuscular blockade.
Polcortolone reduces the effect of NSAIDs (including acetylsalicylic acid), alcohol, while increasing the risk of ulcerative lesions and the development of bleeding from the gastrointestinal tract.
When using Polcortolone simultaneously with medications or foods containing sodium, peripheral edema and arterial hypertension may occur. In such a situation, it is necessary to limit sodium in the diet and discontinue medications with a high sodium content.
When using vaccines containing live viruses, against the background of the use of immunosuppressive doses of GCS, replication of viruses and the development of viral diseases, a decrease in the production of antibodies are possible (the combination is not recommended). When used simultaneously with other vaccines, the risk of neurological complications increases and the production of antibodies decreases.
When used together with folic acid, the need for this drug may increase.
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.
Description of the drug POLCORTOLON
GKS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. It disrupts the ability of macrophages to phagocytose, as well as to form interleukin-1. Helps stabilize lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability due to the release of histamine. Suppresses fibroblast activity and collagen formation.
Inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses the formation of antibodies.
Suppresses the release of ACTH and β-lipotropin by the pituitary gland, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.
When directly applied to blood vessels, it has a vasoconstrictor effect.
It has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys and increases the activity of gluconeogenesis enzymes. In the liver, it enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose levels activates the release of insulin.
Suppresses the uptake of glucose by fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which promotes fat accumulation.
It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue.
Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, growth suppression in children is possible.
In high doses, it can increase the excitability of brain tissue and help lower the threshold for convulsive readiness. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.
When used systemically, the therapeutic activity is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.
When applied externally and locally, the therapeutic activity of triamcinolone acetonide is due to its anti-inflammatory, antiallergic and antiexudative (due to the vasoconstrictor effect) effect.
In terms of anti-inflammatory activity, triamcinolone acetonide is 6 times more active than hydrocortisone. Triamcinolone acetonide has virtually no mineralocorticoid activity.
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.
Polcortolone Tablets, box, 50 pcs., 4 mg, for oral administration
Side effect
From the endocrine system: secondary adrenal and hypothalamic-pituitary insufficiency (especially during stressful situations such as illness, injury, surgery), Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae), delayed sexual development and suppressed growth in children, menstrual irregularities, decreased tolerance to carbohydrates, manifestation of latent diabetes mellitus and increased need for insulin or oral hypoglycemic drugs in patients with diabetes mellitus, hirsutism. From the digestive system: steroid ulcer of the stomach and duodenum with possible perforation and bleeding, pancreatitis, flatulence, erosive esophagitis, indigestion, nausea, vomiting, increased or decreased appetite, hiccups; in rare cases - increased activity of liver transaminases and alkaline phosphatase. From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest), development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, arterial hypertension, hypercoagulation, thrombosis; in patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle. From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased ICP with congestive optic nipple syndrome (pseudotumor of the brain - more often in children, usually after too rapid dose reduction, symptoms - headache, decreased visual acuity or double vision), vertigo, pseudotumor of the cerebellum, convulsions, dizziness, headache, nervousness or restlessness, sleep disturbances. From the senses: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, glaucoma, exophthalmos, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea. Metabolism: negative nitrogen balance as a result of protein catabolism, hyperglycemia, glycosuria, increased excretion of Ca2+, hypocalcemia, increased body weight, increased sweating, sodium and fluid retention in the body (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasms, unusual weakness and fatigue). From the musculoskeletal system: slowing of growth and ossification processes in children (premature closure of the epiphyseal growth plates), osteoporosis (very rarely - pathological bone fractures, compression fracture of the spine, aseptic necrosis of the head of the humerus and femur, pathological fractures of long tubular bones), muscle tendon rupture, muscle weakness, steroid myopathy, decreased muscle mass (atrophy). On the part of the skin and mucous membranes: steroid acne, stretch marks, delayed wound healing, thinning of the skin, petechiae, ecchymosis, hematomas, a tendency to develop pyoderma and candidiasis. Allergic reactions: skin rash, itching, anaphylactic shock. Other: development and exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.
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.
Polcortolone, 50 pcs., 4 mg, tablets
Polcortolone is contraindicated in patients with systemic fungal infections, but in some cases it can be used in this category of patients simultaneously with amphotericin B to reduce its side effects. In these cases, circulatory failure, left ventricular myocardial hypertrophy, and severe hypokalemia may develop. Polcortolone is prescribed with caution for nonspecific ulcerative colitis (due to the risk of developing intestinal perforation, abscess or other purulent infections), fresh intestinal anastomoses, erosive and ulcerative lesions of the gastrointestinal tract, renal failure, arterial hypertension, osteoporosis, myasthenia gravis, diabetes mellitus, liver dysfunction , glaucoma, viral infections, hyperlipidemia, hypoalbuminemia. If perforation of the gastrointestinal tract occurs during the use of Polcortolone in high doses, symptoms of peritonitis may be absent or mildly expressed. In patients with hypothyroidism or liver cirrhosis, the effect of Polcortolone is enhanced. With the use of Polcortolone, the patient's pre-existing emotional instability or psychotic personality may intensify. Prescribing Polcortolone to patients with an active form of tuberculosis is possible only in cases of disseminated or fulminant tuberculosis and only in combination with anti-tuberculosis chemotherapy. If it is necessary to prescribe Polcortolone to patients with latent tuberculosis or with a positive tuberculin test, the patient's condition should be carefully monitored due to the high risk of activation of the tuberculosis process. With long-term use of GCS, such patients should receive anti-tuberculosis chemoprophylaxis. Patients with hypoprothrombinemia should be prescribed Polcortolone and acetylsalicylic acid with caution. Polcortolone can mask the symptoms of infectious diseases and reduce the body's resistance to infection. During the use of the drug, latent amoebiasis may occur. In patients with dysentery of unknown etiology or arriving from tropical countries, dysenteric amoebiasis should be excluded. Long-term use of Polcortolone increases the risk of developing a secondary fungal or viral infection. In stressful situations, parenteral administration of GCS is recommended for patients receiving the drug. It should be taken into account that drug withdrawal must be carried out gradually. If the drug is suddenly discontinued, especially after long-term therapy, withdrawal syndrome may develop, characterized by anorexia, fever, myalgia and arthralgia, and general weakness (these symptoms may occur in the absence of signs of adrenal insufficiency). When using Polcortolone in high doses, it is necessary to control blood pressure and monitor the patient’s body weight. When using Polcortolone, vaccination with live viral vaccines should not be performed due to the possibility of viral replication and the development of viral diseases, as well as a decrease in the production of antibodies. Administration of inactivated viral or bacterial vaccines may not produce the expected increase in antibody titer. It is possible to vaccinate patients receiving Polcortolone as replacement therapy, but it must be taken into account that the risk of developing neurological complications increases. With the use of Polcortolone, the need for folic acid increases. In some patients, while using Polcortolone, sperm motility or sperm count may be impaired. Monitoring laboratory parameters When using Polcortolone in high doses, it is necessary to periodically determine the concentration of electrolytes in the blood plasma. In some cases, it may be necessary to put the patient on a diet that limits sodium intake and increases potassium levels. Use in pediatrics Long-term use of Polcortolone in pediatric practice requires careful monitoring of the growth and development of children.
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.
Instructions for use POLCORTOLON
Polcortolone is contraindicated in patients with systemic fungal infections due to the risk of worsening the infection. In some cases, it can be used in this category of patients simultaneously with amphotericin B to reduce its side effects, however, circulatory failure, left ventricular myocardial hypertrophy, and severe hypokalemia may develop.
Sudden cessation of treatment may cause the development of adrenal insufficiency, so the dose of triamcinolone should be reduced gradually. Interruption of treatment after long-term use of the drug may cause symptoms of the so-called glucocorticoid withdrawal syndrome, such as fever, muscle and joint pain, and poor health. These symptoms can appear even in cases where there is no adrenal insufficiency.
Administration of triamcinolone to patients with active tuberculosis should be limited to cases of disseminated or fulminant tuberculosis and only with concomitant antibacterial treatment. Patients with latent tuberculosis or a positive tuberculin test taking triamcinolone should be monitored for the possibility of developing tuberculosis. In the case of long-term treatment with GCS, such patients should receive prophylactic antibacterial drugs.
Polcortolone can mask the symptoms of infectious diseases and reduce the body's resistance to infection.
During the use of the drug, latent amoebiasis may occur. In patients with dysentery of unknown etiology or arriving from tropical countries, dysenteric amoebiasis should be excluded.
When using Polcortolone, vaccination with live viral vaccines should not be performed due to the possibility of viral replication and the development of viral diseases, as well as a decrease in the production of antibodies. Administration of inactivated viral or bacterial vaccines may not produce the expected increase in antibody titer. Patients receiving Polcortolone as replacement therapy, for example, with Addison's disease, can be vaccinated.
In case of increased stress in patients taking corticosteroids, an increased dose of fast-acting corticosteroids should be administered.
Triamcinolone in high doses can cause an increase in blood pressure, water and sodium retention, and also increase potassium excretion. During treatment, sodium restriction and increased potassium in the diet may be required. Triamcinolone also causes an increase in calcium excretion.
In patients with hypothyroidism or liver cirrhosis, the effect of triamcinolone is enhanced.
In the case of ocular herpes zoster, triamcinolone should be used with caution due to the risk of corneal perforation.
Triamcinolone should be used in the lowest effective doses. If a dose reduction is possible, it should be reduced gradually.
Long-term use of triamcinolone can cause cataracts, glaucoma with the possibility of damage to the optic nerves, and also increases the risk of secondary fungal or viral infections.
During treatment with triamcinolone, mental disorders such as euphoria, insomnia, sudden mood changes, personality changes, severe depression, and symptoms of psychosis may appear. Pre-existing emotional instability or psychotic tendencies may increase during treatment.
Caution should be exercised when treating patients with hypoprothrombinemia with both triamcinolone and acetylsalicylic acid.
Triamcinolone should be used with caution in UC if there is a risk of perforation; abscesses or other purulent infections, intestinal diverticulosis, fresh intestinal anastomoses, active or latent peptic ulcers, renal failure, arterial hypertension, osteoporosis, myasthenia gravis, diabetes mellitus, deterioration of liver function, glaucoma, fungal or viral infections, hyperlipidemia, hypoalbuminemia.
In the case of perforation of the digestive tract in patients taking high doses of triamcinolone, symptoms of peritonitis may be minor or not appear at all.
In some patients, GCS can increase or decrease the number and motility of sperm.
The use of GCS may in some cases be useful in the adjuvant treatment of certain diseases associated with HIV infection. However, due to the risk of developing severe, treatment-resistant infections and neoplasms, the decision to prescribe GCS to HIV-infected patients with clinical manifestations of AIDS should be made after a thorough assessment of the benefits and risks of treatment.
Use in pediatrics
With long-term use of Polcortolone in pediatric practice, careful monitoring of the growth and development of children is necessary.
Impact on the ability to drive vehicles and operate machinery
No data available.
Laboratory results
Subacute toxicity studies have shown that Polcortolone administered at doses of 1/30 and 1/100 LD50 causes significant atrophy of the lymphatic system, especially noticeable in the area of the peribronchial lymphatic system, white parenchyma and spleen and intestinal lymphatic system.
The consequence of involution of the lymphatic system is a decrease in immunity, manifested in rapidly developing purulent bronchitis. After several days of administration of the studied doses of the drug, diffuse fatty liver was observed.
