2010/06/06

Triamcinolone

International name:
Triamtsinolon (Triamcinolone)

Group Affiliation:
Glucocorticosteroids

Description of the active substance (INN):
Triamtsinolon

Dosage form:
Tablets

Mode of action:
GCS, inhibits the release of interleykina1, interleykina2, interferon gamma from lymphocytes and macrophages. Has anti-inflammatory, antiallergic, desensitizing, antishock, anti-toxic and immunosuppressive effect. Absorbs release of pituitary ACTH and beta-lipotropina, but does not reduce the concentration of circulating beta-endorphin. Inhibits the secretion of TSH and FSH. Increase the excitability of the CNS, reduces the number of lymphocytes and eosinophils, increases - erythrocytes (stimulates the production of erythropoietin). Interaction with specific cytoplasmic receptors, forming a complex that penetrates the cell nucleus, and stimulates the synthesis of mRNA, the latter induces the formation of proteins, Including lipokortina, mediating cellular effects. Lipokortin inhibits phospholipase A2, inhibits arachidonic acid and inhibits the synthesis of endoperekisey, Pg, leukotrienes that contribute to inflammation, allergies and other protein metabolism: it reduces the amount of protein in the plasma (due to globulin) with an increase in the coefficient of albumin / globulin, albumin synthesis increases in liver and kidneys, increases catabolism of protein in muscle tissue. Lipid metabolism: increased synthesis of fatty acids and triglycerides, redistributes fat (fat accumulation mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia. Carbohydrate metabolism: increases the absorption of carbohydrates from GIT; increases the activity of glucose-6-phosphatase, which leads to an increase of glucose from the liver to blood increases the activity of fosfoenolpiruvatkarboksilazy and synthesis of aminotransferases, resulting in the activation of gluconeogenesis. Water-electrolyte metabolism: retards Na + and water in the body, stimulates the excretion of K + (ISS activity ), reduces the absorption of Ca2 + from the gastrointestinal tract, "washes out" Ca2 + from the bones, increases the excretion of Ca2 + by the kidneys. Antiinflammatory effect associated with inhibition of the release of eosinophils inflammatory mediators, induction, education lipokortina and reduce the number of mast cells that produce hyaluronic acid, a decrease in capillary permeability, stabilization of cell membranes and membrane organelles (especially the lysosomal). antiallergic effect is due to suppression of synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, reducing the number of circulating basophils, suppress the development of lymphoid and connective tissue, reducing the number of T-and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to the mediators of allergy, inhibition of antibody production, changes in immune response. With COPD action is mainly based on inhibition of inflammatory processes, inhibition of growth or prevention of swelling of mucous membranes, inhibition of eosinophilic infiltration of the submucous layer of bronchial epithelium, deposition in the bronchial mucosa of circulating immune complexes, as well as braking erozirovaniya and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic bronchial small-and medium-sized to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus due to suppression or reduction of its products. Antishock and anti-toxic effect associated with elevated blood pressure (by increasing the concentration of circulating catecholamines and recovery of sensitivity to them adrenoceptor, and vasoconstriction), decrease the permeability of the vascular wall, membrano properties, activation of liver enzymes involved in the metabolism of endo-and xenobiotics. immunosuppressive effect is caused by inhibition of the release of cytokines (interleykina1, interleykina2, interferon gamma) from lymphocytes and macrophages. suppresses the synthesis and secretion of ACTH and secondary - the synthesis of endogenous GCS. Hinders connective tissue reaction in the inflammatory process and reduces the possibility of formation of scar tissue. The anti-inflammatory activity triamtsinolon similar to hydrocortisone, triamtsinolona acetonide in 6 times more active. ISS activity is virtually absent. Maximum effect is observed after 1-2 hours, duration - 2.5 days.

Indications:
Systemic connective tissue disorders (SLE, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis). Acute and chronic inflammatory joint diseases: gout and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, humeroscapular periarthritis, ankylosing spondylitis (Bechterew's disease ), juvenile arthritis, Still syndrome in adults, bursitis, nonspecific peritendinitis, synovitis, and epicondylitis. Rheumatic fever, acute rheumatic heart disease. Bronchial asthma, asthmatic status. Acute and chronic allergic diseases: allergic reactions to drugs and foods, serum sickness, urticaria, Allergic rhinitis, angioedema, drug exanthema, pollinosis. Skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis, diffuse neurodermatitis, contact dermatitis (with the defeat of the large surface of the skin), toksidermiya, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome ), bullous Dermatitis herpetiformis, a malignant exudative erythema multiforme (Stevens-Johnson syndrome). Cerebral edema (also on the background of a brain tumor or associated with surgery, radiotherapy, or head trauma) after a preliminary parenteral use. ocular allergy: allergic corneal ulcer, and allergic forms of conjunctivitis. Inflammatory eye diseases: sympathetic ophthalmia, severe lingering front and rear uveitis, optic neuritis. primary or secondary adrenal insufficiency (including the state after the removal of the adrenal glands). Congenital adrenal hyperplasia. Kidney disease of autoimmune origin (including acute glomerulonephritis), nephrotic syndrome. Subacute thyroiditis. Diseases of blood - agranulocytosis, panmielopatiya, autoimmune hemolytic anemia, acute lymphocytic and myeloid leukemia, venereal disease, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocytic anemia) , congenital (erythroid) anemotrophy. Lung diseases: acute alveolitis, pulmonary fibrosis, sarcoidosis II-III century. Tuberculous meningitis, pulmonary tuberculosis, pneumonia, aspiration (in conjunction with specific chemotherapy). Berylliosis syndrome Leffler (not amenable to other therapies) . Lung cancer (in combination with cytotoxic drugs). Multiple sclerosis. gastrointestinal diseases: ulcerative colitis, Crohn's disease, a local enteritis. Hepatitis. Prevention of graft rejection reactions. hypercalcemia on the background of cancer, nausea and vomiting during the cytostatic therapy. Multiple myeloma.

Contraindications:
For short-term use according to the life only contraindication is giperchuvstvitelnost.C caution. Parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, including the recent contact with a patient) - Herpes simplex, herpes zoster (viremicheskaya phase), chicken pox, measles, amoebiasis, strongyloidiasis (or suspected); system mycosis; active and latent tuberculosis. Application for serious infectious diseases is permissible only against the background of specific therapy. Postvaccination period (the period of duration 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency states (including AIDS or HIV infection). Diseases of the digestive tract - stomach ulcer and 12 duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis of the intestine, ulcerative colitis, with the threat of perforation or abscess formation , diverticulitis. Diseases of the SSA, including recent myocardial infarction (in patients with acute and subacute myocardial necrosis may spread the fire, slowing the formation of scar tissue and therefore rupture of the heart muscle), decompensated chronic heart failure, hypertension, hyperlipidemia). Endocrine disease - diabetes mellitus (including breach of tolerance to carbohydrates), hyperthyroidism, hypothyroidism, pituitary Cushing's. Severe chronic renal and / or liver failure, nefrourolitiaz. Hypoalbuminaemia and conditions that predispose to its occurrence. Systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV century .), polio (except bulbar form of encephalitis), open-and-closure glaucoma, pregnancy, lactation.

Side effects:
The frequency and severity of side effects depend on the duration of application, size of the dosage used and the possibility of preserving the circadian rhythm of destination. On the part of the endocrine system: reduction of glucose tolerance, "steroid" diabetes or a manifestation of latent diabetes mellitus, adrenal suppression, Cushing's syndrome Itsenko- (moon face, obesity, pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae), delay sexual development in children. On the part of the digestive system: nausea, vomiting, pancreatitis, "steroid" stomach ulcers and 12 duodenal ulcer, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - increased activity of "liver" transaminase and alkaline phosphatase. On the part of the SSA: arrhythmia, bradycardia (down to heart failure), development (in predisposed patients) or increased severity of CHF, ECG changes typical of hypokalemia, increased blood pressure, hypercoagulation , thrombosis. In patients with acute and subacute myocardial infarction - the spread foci of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle. The nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, headache, convulsions. On the part of the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, the propensity to develop secondary bacterial, fungal or viral eye infection trophic changes of the cornea, exophthalmos. On the part of metabolism: increased excretion of Ca2 +, hypocalcemia, increased body weight, negative nitrogen balance (an increased breakdown of proteins), increased sweating. The resulting ISS activity - fluid retention, and Na + (peripheral edema), hypernatremia, gipokaliemichesky syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness, and fatigue). From the musculoskeletal system: slowing growth and ossification in children (premature closure of epiphyseal growth zones), osteoporosis (very rare - pathological fractures, aseptic necrosis of the head humerus and femur), muscle tendon rupture, "steroid" myopathy, reduced muscle mass (atrophy). On the part of the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, skin thinning, hyper-or hypopigmentation, steroid acne, striae , the propensity to develop pyoderma and candidiasis. Allergic reactions: generalized (skin rash, itching, anaphylactic shock), local allergic reactions. Other: development or exacerbation of infection (the appearance of this side effect contribute jointly used immunosuppressants, and vaccination), Pyuria, syndrome cancel . Overdosage. Symptoms: Cushing's syndrome Itsenko-, hyperglycemia, Glycosuria. Treatment: symptomatic on the background of gradual abolition.

Dosage and administration:
Inside, after eating: initial dose - 4-40 mg / day for 2-3 reception, after the improvement of the daily dose is gradually reduced by 1-2 mg every 2-3 days to reach a minimum maintenance dose (1 mg) or completely abolished. Adults and teenagers (aged 12 years) with adrenal insufficiency - 4-12 mg once (morning) or in 2 divided doses (morning and lunch). In Hodgkin's disease, lymphosarcoma, chronic leukemia initial dose - 30-60-75 mg / day. Children from 6 to 12 years in case of insufficiency of the adrenal cortex - 0.117 mg / kg in the morning or in 2 divided doses, and in other cases - 0.416-1.7 mg / kg. Children weighing up to 25 kg - 0.1-0.5 mg / kg / day in 1 or more receptions. The maximum daily dose - 12-14 mg.

Cautions:
Oral use of doses exceeding 4 mg / day, suppression of the hypothalamic-pituitary system may develop in 6-12 weeks. Gradually remove the drug spend. Do not apply within 8 weeks prior to vaccination, and within 2 weeks after their implementation. In order to prevent failure of the adrenal cortex after treatment with corticotropin appointed within a few days. During the period of treatment is recommended to take vitamin D supplements and eat foods rich in Ca2 +. The children in the period of growth GCS should be used only if absolutely indicated and under very close supervision of a doctor.

Interaction:
Triamtsinolon pharmaceutical incompatible with other drugs (can form insoluble compounds). Triamtsinolon increases the toxicity of cardiac glycosides (because of the emerging hypokalemia increases the risk of arrhythmias). Accelerates Launch ACK, reduces its concentration in the blood (if you cancel triamtsinolona concentration of salicylates in the blood increases increases the risk of side effects). If applied simultaneously with live vaccines and antiviral against a background of other types of immunization increases the risk of virus activation and development of infections. Increases the metabolism of isoniazid, meksiletina (especially in "fast atsetilyatorov"), which leads to a decrease in their plasma concentrations . increases the risk of hepatotoxic reactions of paracetamol (induction of "liver" enzymes and formation of a toxic metabolite of paracetamol). Increases (with prolonged therapy) the concentration of folic acid. Hypokalemia caused by SCS, may increase the severity and duration of muscle blockade against the background of muscle relaxants. In high doses reduces the effect somatropina. Antacids reduce the absorption of the SCS. Triamtsinolon reduces hypoglycemic effect of drugs; enhances anticoagulant effect of coumarin derivatives. weakens the influence of vitamin D on the absorption of Ca2 + in the lumen of the intestine. Ergocalciferol and parathyroid hormone hinder the development of osteopathy caused by SCS. Reduces the concentration of praziquantel in blood. Ciclosporin (inhibits metabolism) and ketoconazole (lowers the ride height) increases the toxicity. Thiazide diuretics, inhibitors of carbonic anhydrase, etc. SCS and amphotericin B increase the risk of hypokalemia, Na +-containing HP - swelling and increase blood pressure. NSAIDS and ethanol increases the risk of gastrointestinal ulcerations and bleeding, in combination with NSAIDs to treat arthritis may reduce the dose of GCS due to summation of the therapeutic effect. indomethacin, displacing triamtsinolon from its association with albumin, increases the risk of its side effects. Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis. The therapeutic effect of SCS is reduced under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers, hepatic, microsomal enzymes (increased metabolic rate). Mitotan inhibitors and other functions adrenal cortex may necessitate increasing the dose of GCS. Clearence GCS rises against a background of drugs - thyroid hormones. Immunodepresanty increase the risk of infection and lymphoma or other lymphoproliferative disorders associated with Epstein-Barr virus. estrogens (including oral contraceptives estrogensoderzhaschie) reduce the clearance of GCS , extend T1 / 2 and their therapeutic and toxic effects. The appearance of hirsutism and acne promotes the simultaneous use of other steroid hormone drugs - androgens, estrogens, anabolic steroids, oral contraceptives. Tricyclic antidepressants may increase the severity of depression caused by GCS (not shown for the treatment of data side effects). The risk of developing cataracts increases with the application in the background, etc. SCS, antipsychotic drugs (neuroleptics), karbutamida and azathioprine. Simultaneous with the appointment of m-holinoblokatorami (including antihistamine drugs, tricyclic antidepressants), nitrates contribute to the development of increased intraocular pressure.