POLKORTOLON

Active material: Triamcinolone
When ATH: H02AB08
CCF: GCS for oral use
ICD-10 codes (testimony): A15, A17.0, B18.1, B18.2, C82, C83, C84.0, Q91, Q92, D59, D59.1, D60, D61, D69.3, D69.5, D86, E06, E25, E27.1, E27.4, G35, H10.1, H10.2, H10.4, H10.5, H16, H16.2, H20.0, H20.1, H30, H44.1, H46, I01, J30.1, J30.3, J45, J63.2, J69, J82, K70, K72, K73, L10, L12, L13.0, L20.8, L21, L23, L24, L26, L40, L51.1, M05, M07, M08, M10, M15, M30, M31.6, M32, M33, M34, M35.3, M45, M65, M71, M77, T78.2, T78.3, T80.6, T88.7, Z94
Manufacturer: Pharmaceutical Works Polfa in Pabianice Joint-Stock Company (Poland)

Pharmaceutical form, composition and packaging

Pills white or nearly white, round, flat, chamfered, with engravings “O” on one side and “4/mg” – another.

Excipients: potato starch, magnesium stearate, lactose.

25 PC. – blisters (2) – packs cardboard.

Pharmacological action

The synthetic glucocorticoid drugs, It is a fluorinated derivative of prednisolone. It has strong anti-inflammatory effect and is a weak mineralocorticoid effect.

Inhibits the development of the symptoms of inflammation by reducing capillary permeability and reduce the accumulation of macrophages, leukocytes and other cells in the area of ​​inflammation. It has immunosuppressive effect, incl. due to suppression of cellular immune response.

It inhibits the secretion of ACTH by the pituitary gland, which reduces the production of androgens and corticosteroids by the adrenal cortex.

Enhances protein catabolism, It causes an increase in blood glucose concentration, impact on lipid metabolism, increases the concentration of fatty acids in the serum. Prolonged treatment possible fat redistribution.

Triamcinolone inhibits bone formation and reduces the concentration of calcium in blood serum, and therefore the intake of the drug may suppress bone growth in children and adolescents and the development of osteoporosis in patients of all age groups.

It is believed, what 4 mg triamcinolone has anti-inflammatory action, equivalent 4 mg of methylprednisolone, 5 mg prednisolone, 0.75 mg dexamethasone, 0.6 mg betamethasone and 20 mg hydrocortisone.

Pharmacokinetics

Absorption

After ingestion readily absorbed from the gastrointestinal tract. Bioavailability – 20-30%. Taking the drug with food slows the absorption of triamcinolone in the initial phase, but it does not affect the overall bioavailability.

Distribution

Plasma protein binding (predominantly globulins) is 40%. It penetrates through the placental barrier and is excreted in breast milk.

Metabolism and excretion

Biotransformiroetsa mainly in the liver. The biological half-life is approximately 5 no. Write mainly kidneys as inactive metabolites.

Testimony

- Endocrine diseases: adrenocortical insufficiency (primary or secondary), congenital adrenal hyperplasia, subacute thyroiditis;

- Hard proceeding allergic diseases, resistant to other treatments: contact dermatitis, atopic dermatitis, serum sickness, hypersensitivity reactions to drugs, year-round or seasonal allergic rhinitis;

- Diseases of the musculoskeletal system: psoriaticheskiy arthritis, ankylosing spondylitis, acute and subacute bursitis, epicondylitis, acute tenosynovitis, posttravmaticheskiy osteoarthritis;

- Rheumatic diseases: acute rheumatic fever, rheumatic myocarditis, rheumatoid arthritis, juvenile rheumatoid arthritis (in cases, resistant to other therapies), polymyalgia rheumatica, Horton's disease;

- Systemic connective tissue disease: dermatomyositis, SLE, mezoarteriit granulomatous giant, systemic scleroderma, periarteritis nodosa, relapsing polychondritis;

- Dermatological diseases: exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe erythema multiforme (Stevens-Johnson syndrome), granulosarcoid, pemphigus, severe psoriasis, severe eczema, pemfigoid;

- Hematologic diseases: priobretennaya autoimmunnaya gemoliticheskaya anemia, Congenital (erythroid) gipoplasticheskaya anemia, anemia due to bone marrow hypoplasia, secondary thrombocytopenia in adults, idiopaticheskaya trombotsitopenicheskaya purpura (idiopathic thrombocytopenic purpura) adult, gemoliz;

- Liver disease: alcoholic hepatitis with encephalopathy, chronic active hepatitis;

- Hypercalcemia of malignancy;

- Cancer: leukemias and lymphomas in adults, acute leukemia in children;

- Neurological diseases: tuberculous meningitis with subarachnoid block or the threat of its occurrence (in combination with anti-tuberculosis therapy), multiple sclerosis during exacerbation;

- Severe acute and chronic inflammatory diseases of the eye: heavy sluggish front and posterior uveitis, optic neuritis, transferred ophtalmia;

- Respiratory diseases: bronchial asthma (severe form), berylliosis, Loffler's syndrome, symptomatic sarcoidosis, lightning or disseminated pulmonary tuberculosis (in combination with anti-tuberculosis therapy), aspiration pneumonitis;

- To prevent and treat graft rejection during transplantation of organs and tissues (in combination with other immunosuppressive agents).

Dosage regimen

Set individually, depending on indications, efficacy and condition of the patient.

It is recommended to take the entire daily dose 1 time / day in the morning while eating (in accordance with the diurnal rhythm of secretion of endogenous glucocorticoids), however, in some cases it may be required more frequent administration.

Adults and adolescents over 14 years administered at a dose of 4-48 mg / day in single or divided doses.

Babies prescribed drug dose 100-500 ug / kg body weight / day 1 or more steps.

When you miss taking a dose of the drug should be taken as soon as possible. If you are approaching the next admission, do not take the missed dose. Do not take a double dose at once.

Polkortolon should be prescribed in the lowest effective dose. If necessary, the dose can be gradually reduced.

Side effect

On the part of the endocrine system: secondary adrenal and hypothalamic-pituitary insufficiency (especially in stressful situations, such as disease, trauma, surgery), Cushing's syndrome (incl. moon face, obesity, pituitary type, girsutizm, increased blood pressure, dysmenorrhoea, amenorrhea, myasthenia, striae), delayed sexual development and growth suppression in children; menstrual irregularities, reduced glucose tolerance, a manifestation of latent diabetes mellitus and increase the need for insulin or oral hypoglycemic agents in patients with diabetes, girsutizm.

From the digestive system: steroid ulcer and duodenal ulcer with possible perforation and hemorrhage, pancreatitis, erosive esophagitis, flatulence, digestive disorders, nausea, vomiting, increased or decreased appetite, Ikotech; rarely – increase in liver transaminases and alkaline phosphatase.

Cardio-vascular system: Arrhythmia, bradycardia (up to heart failure), development (in predisposed patients) or increased severity of chronic heart failure, ECG changes, typical of hypokalemia, arterial hypertension, hypercoagulation, thrombosis. Patients with acute and subacute myocardial infarction – spread necrosis and slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

From the central and peripheral nervous system: delirium, disorientation, euphoria, hallucinations, affective insanity, depression, paranoia, increased intracranial pressure syndrome stagnant nipples optic nerve (pseudotumor of the brain – most often in children, usually after too rapid dose reduction; symptoms – headache, deterioration of visual acuity or double vision); vertigo, pseudotumor cerebellum, convulsions, dizziness, headache, nervousness or anxiety, sleep disturbance.

On the part of the organ of vision: zadnyaya subkapsulyarnaya cataracts, increased IOP with possible damage to the optic nerve, glaucoma, exophthalmos, propensity to develop secondary bacterial, fungal or viral infections of the eye, trophic changes of the cornea.

Metabolism: negative nitrogen balance as a result of protein catabolism, giperglikemiâ, glycosuria, increased excretion of calcium, hypocalcemia, weight gain, desudation, sodium and fluid retention in the body (peripheral edema), gipernatriemiya, gipokaliemichesky syndrome (kaliopenia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

On the part of the musculoskeletal system: slowing growth and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (rarely – pathological fractures, a compression fracture of the spine, aseptic necrosis of the humeral head and femur, pathological fractures of long bones), muscle tendon rupture, muscular weakness, steroidnaya myopathy, reduced muscle mass (atrophy).

Dermatological reactions: steroid acne, striae, slow wound healing, thinning of the skin, petechiae, ecchymosis, hematoma, the tendency to the development of pyoderma and candidiasis.

Allergic reactions: skin rash, itch, anaphylactic shock.

Other: the development and aggravation of infection (the appearance of this side effect contribute jointly used immunosuppressants and vaccination), leucocyturia, withdrawal.

The frequency and severity of side effects depend on the duration of their application, the value of the dosage used and the possibility of compliance circadian rhythm of destination.

With short-term use of triamcinolone, like other corticosteroids, side effects are rare. Side effects are usually, there are long-term use of the drug.

Contraindications

- Systemic mycosis;

- Children up to age 3 years;

- Hypersensitivity to the drug.

FROM caution Polkortolon prescribed in parasitic and infectious diseases of viral, fungal or bacterial origin (occurring now or recently transferred, including the recent contact with a patient): herpes simplex, herpes zoster (viremicheskaya phase), enable vetryanaya, kor, ameʙiaz, strongiloidoz (established and the suspect), systemic mycosis, active and latent tuberculosis. Application for serious infectious diseases is permissible only against the background of specific therapy.

FROM caution should be prescribed in the post-vaccination period (period duration 8 weeks before and 2 weeks after vaccination), when lymphadenitis after BCG vaccination, with immunodeficiency (incl. AIDS, HIV infection).

Observe caution in the treatment of individuals, gastrointestinal diseases such as the esophagitis, gastritis, UC with the threat of perforation or abscess, diverticulitis, gastric ulcer and duodenal ulcer, acute or latent peptic ulcer, recently established intestinal anastomosis.

FROM caution prescribe the drug to patients with diseases of the cardiovascular system, incl. during recent myocardial infarction (in patients with acute and subacute myocardial infarction may spread necrosis, slowing the formation of scar tissue and therefore – rupture of the heart muscle), In chronic heart failure decompensation, with hypertension and hyperlipidemia.

Need caution the appointment of persons with Polkortolona endocrine diseases (diabetes / incl. in violation of carbohydrate tolerance /, thyrotoxicosis, gipotireoz, pituitary basophilia), chronic renal and / or liver failure, severe, nefrourolitiaze, with hypoalbuminemia and conditions, predisposing to its occurrence, systemic osteoporosis, myasthenia gravis, Ostrom psychosis, obesity grade III-IV, poliomielite (except bulbar form of encephalitis), openly- and angle-closure glaucoma, Pregnancy and lactation.

Pregnancy and lactation

Use of the drug during pregnancy is possible only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus.

If necessary, the appointment during lactation should decide the issue of termination of breastfeeding.

Cautions

In case of stress patients, receiving Polkortolon, recommended that parenteral administration of corticosteroids.

The sudden discontinuation of treatment can cause the development of adrenal insufficiency, therefore, the dose should be reduced gradually Polkortolona.

Polkortolon may mask symptoms of infection, to reduce resistance to infection and ability to limit its spread. Long-term use increases the risk of Polkortolona secondary fungal or viral infections.

Long-term use can cause Polkortolona cataracts, glaucoma with possible lesions of the optic nerve.

Patients, taking Polkortolon, do not vaccinate live virus vaccines. Introduction inactivated viral or bacterial vaccines could not cause the expected increase in the amount of antibodies. Besides, patients, taking corticosteroids, there is an increased risk of neurological complications during vaccination.

It should be remembered, that a sudden discontinuation of treatment can cause the development of adrenal insufficiency, therefore, the dose should be reduced gradually Polkortolona.

With the sudden cancellation Polkortolona, especially after long-term use, possible development of the so-called withdrawal, manifesting anorexia, fever, muscle and joint pain, general weakness. These symptoms may appear even in the case of, When not marked adrenal insufficiency. In patients with hypothyroidism or cirrhosis intensifies the action of triamcinolone.

During the application may appear Polkortolona mental disorders, such as euphoria, insomnia, mood changes, personality changes, severe depression, simptomы psychosis. Pre-existing emotional instability or psychotic tendencies may intensify during treatment.

In the treatment of patients with gipoprotrombinemiey be used with caution while triamcinolone and acetylsalicylic acid.

Use in Pediatrics

With prolonged use Polkortolona pediatric careful monitoring of growth and development of children.

Overdose

Symptoms: increased blood pressure, peripheral edema; may increase the side effects described above.

Treatment: gradual dose reduction and elimination of the drug; if necessary, symptomatic therapy.

Taking large doses of the drug does not cause acute intoxication. But long-term use Polkortolona, especially in large doses, there is a risk of overdose.

Drug Interactions

With simultaneous application of cardiac glycosides Polkortolona and increases the risk of cardiac arrhythmias and other toxic effects of glycosides, associated with hypokalemia.

In an application with barbiturates Polkortolonom, anticonvulsants (phenytoin, Carbamazepine), rifampicin, glutetimid accelerate the metabolism of triamcinolone (by induction of microsomal enzymes) and weaken its effect.

With simultaneous use of histamine H₁-receptors weaken the effect Polkortolona.

When combined with amphotericin B Polkortolona, carbonic anhydrase inhibitors increase the risk of hypokalemia, left ventricular hypertrophy, and circulatory failure.

In an application Polkortolona with paracetamol increases the risk of hypernatremia, peripheral edema, increasing the excretion of calcium, increased risk of hypocalcemia, osteoporosis, gepatotoksičnosti paracetamol.

In a joint application Polkortolona with anabolic steroids or androgens increases the risk of peripheral edema, blackheads (this combination requires caution, especially in the case of liver diseases and heart).

If concomitant use of hormonal contraceptives, containing estrogen, Polkortolona enhance the effect by increasing the concentration of globulins, binding of GCS in serum, slowing down their metabolism and increase T_1/2.

In an application with Polkortolona holinoblokatorami (atropynom) may increase intraocular pressure.

Antykoahulyantы (coumarin derivatives, indadion, Heparin), streptokinase, urokinase reduce (some patients raise) efficiency Polkortolona. The dosage should be determined on the basis of the prothrombin time, and take into account the increased risk of ulceration and bleeding from the gastrointestinal tract.

The combined use of tricyclic antidepressants may enhance mental disorders, associated with taking Polkortolona (this combination is not recommended).

In an application Polkortolon reduces the effect of oral hypoglycemic agents, insulin, potassium-sparing diuretics, increases the concentration of glucose in the blood (may require dose adjustment of hypoglycemic drugs).

In a joint application Polkortolona and antithyroid drugs, and thyroid hormones may change the function of the thyroid gland (It may require a dosage adjustment or cancellation of antithyroid medication or thyroid hormones).

Polkortolon reduces the effect of potassium-sparing diuretics. Combined use may cause hypokalemia.

Polkortolon reduces the effectiveness of laxatives, potassium-sparing diuretics, it increases the risk of hypokalemia.

With simultaneous use of ephedrine accelerates biotransformation triamcinolone, which may require dose adjustment Polkortolona.

In a joint application Polkortolona and immunosuppressants increases the risk of infections, lymphomas and other lymphoproliferative disorders.

When used in conjunction with isoniazid may occur isoniazid decreased concentration in the blood plasma (mainly in patients, with rapid acetylation), in this case, variation in dosage.

In a joint application accelerates the metabolism of mexiletine and reduce its concentration in the blood plasma.

While the use of depolarizing muscle relaxants hypocalcemia, associated with Polkortolona, may increase the duration of neuromuscular blockade.

Polkortolon reduces the effect of NSAIDs (incl. acetylsalicylic acid), alcohol, it increases the risk of ulcerative lesions and bleeding from the gastrointestinal tract development.

In an application Polkortolona with drugs or food, containing sodium, may cause peripheral edema and hypertension. In such a situation it is necessary to limit sodium diet and cancellation of drugs with a high content of sodium.

When the vaccines, containing live viruses, during treatment with immunosuppressive doses of corticosteroids replication of viruses and development of viral diseases, reduction in antibody production (the combination is not recommended). When applied simultaneously with other vaccines increases the risk of neurological complications, and reduced production of antibodies.

When combined with the use of folic acid may increase the need for this preparation.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in a dry, protected from light, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 3 year.