2010/06/05

TRIAMCINOLONE ACETONIDE

Pharmacological action

SCS. Inhibits the function of leukocytes and tissue macrophages. The migration of leukocytes in the area of inflammation. Impair the capacity of macrophages to phagocytosis and the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the field of inflammation. Decreases capillary permeability due to histamine release. Inhibits activity of fibroblasts and collagen formation.

Inhibits the activity of phospholipase A 2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce production of prostaglandins.

Reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the vascular bed to lymphoid tissue, suppresses the formation of antibodies.

Suppresses the release of pituitary ACTH and β-lipotropina, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

With direct application of the receptacles has a vasoconstrictor effect.

It has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the capture of amino acids by the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, increases glycogen deposition by stimulating the activity glikogensintetazy and synthesis of glucose from the products of protein metabolism. Increased blood glucose activates the secretion of insulin.

Suppresses the seizure of glucose by fat cells that leads to activation of lipolysis. However, due to increased secretion of insulin is stimulation of lipogenesis, which contributes to the accumulation of fat.

Has catabolic effect in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue.

Osteoporosis and Cushing's syndrome Itsenko-are the main factors limiting the long-term therapy of GCS. As a result of catabolic actions may suppress growth in children.

In high doses may increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. It stimulates the excessive production of hydrochloric acid and pepsin in the stomach that promotes the development of peptic ulcers.

The systems use therapeutic activity due to anti-inflammatory, anti-allergic, immunosuppressive and antiproliferative action.

When external and local application of therapeutic activity triamtsinolona acetonide caused by anti-inflammatory, anti-allergic and antiexudative (due to vasoconstrictor effect) action.

For anti-inflammatory activity triamtsinolona acetonide in 6 times more active than hydrocortisone. Mineralocorticoid activity in triamtsinolona acetonide is virtually absent.


Pharmacokinetics

When the system application is metabolized primarily in the liver and partially - in the kidneys. The main route of metabolism is a 6-β-hydroxylation. T 1 / 2 - 3.5 hours is derived by the kidneys.


Statement

For regular use: asthma, chronic bronchitis with bronchoobstructive syndrome, pemphigoid, psoriasis, dermatitis.

Intraarticular injection: chronic inflammatory disease of the joints, exudative arthritis, gout, dropsy of the joints, the blockade of the shoulder joint, chronic inflammation of the inner layer of articular capsule.

For external use: eczema, psoriasis, atopic dermatitis, various types of dermatitis and other inflammatory and allergic skin diseases non-microbial etiology (combined therapy).


Dosage regimen

Solo, depending on the evidence and applied dosage form.


Side effect

On the part of the endocrine system: the redistribution of body fat, menstrual irregularities, increased blood glucose, adrenal suppression, moon face, striae, hirsutism, acne.

From the Metabolic: edema, electrolyte imbalance, negative nitrogen balance, growth retardation in children.

On the part of the digestive system: steroid ulcer, erosive and ulcerative lesions gastrointestinal acute pancreatitis.

From the CNS: convulsions, sleep disorders, mental disorders, headaches and dizziness, weakness.

On the part of the musculoskeletal system: myopathy, osteoporosis.

Since the cardiovascular system: hypertension.

From the blood coagulation system: thromboembolism.

On the part of the organ of vision: visual impairment, back subcapsular cataracts, increased intraocular pressure, or exophthalmos, anaphylactic reactions.

Reactions due to immunosuppressive effect: intensification of infectious diseases.

With intraarticular injection: possible joint pain, irritation at the injection site, hyperpigmentation, sterile abscess, atrophy of the skin, with the introduction of doses over 40 mg resorptive possible side effects.

For exterior use: possible itching, skin irritation, the late reaction of the type of eczema, steroid acne, purpura. Prolonged use of the ointment may develop secondary infectious lesions and atrophic changes of the skin.


Contraindications

Acute psychosis, a history of active TB disease, myasthenia gravis, tumor metastases, diverticulitis, stomach ulcer and duodenal ulcer, hypertension, Cushing's syndrome Itsenko-, renal failure, thrombosis and embolism in history, osteoporosis, diabetes, latent foci of infection, amyloidosis, syphilis, fungal diseases, viral infections (including those caused by Herpes simplex and Varicella zoster), amoebic infections, polio (except bulbar encephalitis-form), gonococcal or tuberculous arthritis, the period of vaccination lymphadenitis after BCG vaccination, glaucoma infected skin lesions.


Application of pregnancy and breastfeeding

If necessary, use during pregnancy (especially in the I trimester) and during lactation should assess the perceived benefit to the mother and the risk of side effects in the fetus or child.


Cautions

Not designed for to / in the introduction.

With caution and under strict medical supervision is used in edema, obesity, mental illness and gastrointestinal diseases. In the period of treatment is recommended to take vitamin D supplements and consume foods rich in calcium.

When applied externally to prevent local infectious complications is recommended in combination with antimicrobials.

Parenteral use in children under 6 years not recommended; aged 6-12 years - according to strict indications.

Should avoid prolonged outdoor use in children regardless of age.


Drug Interactions

With the simultaneous use of anabolic steroids, androgens increase the risk of peripheral edema, acne.

At simultaneous application with antithyroid drugs and thyroid hormones may change thyroid function.

With simultaneous application of histamine H 1 blocker receptors decreases action triamtsinolona; with hormonal contraception - potentsiruet triamtsinolona.

Hypocalcemia associated with the use of triamtsinolona may lead to an increase in the duration of neuromuscular blockade caused by the action of the depolarizing muscle relaxants in their simultaneous application.

With the simultaneous use of immunosuppressants increases the risk of bacterial and viral infections.

With the simultaneous use of potassium-sparing diuretics can hypokalaemia.

With the simultaneous use may decrease the effectiveness of indirect anticoagulants, heparin, streptokinase, urokinase, increasing the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract.

With the simultaneous use of NSAIDs (including with acetylsalicylic acid) increases the risk of erosive-ulcerative lesions and bleeding from the gastrointestinal tract.

With simultaneous application of attenuated effect of oral hypoglycemic funds insulin; with laxatives - can hypokalaemia; with cardiac glycosides - increase the risk of cardiac arrhythmias and other toxic effects of glycosides.

With the simultaneous use of tricyclic antidepressants may gain mental disorders associated with the reception triamtsinolona.



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