Pharmacological action Triamcinolone Acetonide Ointment
SCS. Inhibits the function of leukocytes and tissue macrophages. Restricts the migration of leukocytes in the area of inflammation. Interfere with the ability of macrophages to phagocytosis and the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes on inflammation. Decreases capillary permeability caused by histamine release. Inhibits the activity of fibroblasts and collagen formation.
Inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Inhibits the release of COX (especially 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 to lymphoid tissue, inhibits the formation of antibodies.
Triamcinolone inhibits the release of pituitary ACTH and β-lipotropin, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.
With a direct application to the vessels has a vasoconstrictor effect.
Triamcinolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, amino acid contributes to the seizure of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver glycogen deposition triamcinolone increases, stimulating the activity glikogensintetazy and synthesis of glucose from products of protein metabolism. Increased blood glucose activates insulin secretion.
Triamcinolone inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis, which contributes to the accumulation of fat.
It has a catabolic effect in the lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue.
Osteoporosis and Cushing’s syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result, the catabolic actions may suppress growth in children.
In high doses, can increase the excitability of triamcinolone brain tissue and helps to reduce the threshold of convulsive readiness. Stimulates excess production of hydrochloric acid and pepsin in the stomach that promotes the development of peptic ulcers.
In the systemic use of therapeutic activity of triamcinolone caused by anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.
For external and local application of therapeutic activity of triamcinolone caused by anti-inflammatory, anti-allergic and antiexudative (due to vasoconstriction effect) effect.
With inhalation use anti-inflammatory effect on bronchial mucosa in patients with asthma. With constant use reduces the number of mast cells, macrophages, T lymphocytes and eosinophils in the epithelium and submucosal layer of bronchi, suppresses airway hyperresponsiveness.
By anti-inflammatory activity similar to hydrocortisone triamcinolone, and triamcinolone acetonide in 6 times more potent. Mineralocorticoid activity in triamcinolone and triamcinolone acetonide is virtually nonexistent.
Pharmacokinetics Triamcinolone Acetonide Ointment
Metabolized primarily in the liver and partially – in the kidneys. The main route of metabolism is a 6-beta-hydroxylation. T1 / 2 – 3.5 hours the kidneys.
Statement Triamcinolone Acetonide Ointment
For oral administration: rheumatism, rheumatoid arthritis, systemic lupus erythematosus and other connective tissue diseases, severe allergic reactions, allergic skin diseases, severe asthma, erythema multiforme, hemorrhagic diathesis, hemolytic anemia, lymphoma, leukemia.
For parenteral application for rheumatoid arthritis, connective tissue disease, systemic lupus erythematosus, dermatitis, pulmonary emphysema and pulmonary fibrosis, lymphoma, Hodgkin’s disease, lymphatic leukemia, nephrotic syndrome, sprue.
For inhalation: Asthma exacerbation. Lack of efficacy of bronchodilators and / or stabilizing mast cell membranes in the treatment of asthma. Hormone-dependent bronchial asthma (with a view to reducing the dose of oral corticosteroids). Allergic rhinitis.
For external use: eczema, psoriasis, atopic dermatitis, various types of dermatitis and other inflammatory and allergic skin diseases nemikrobnoy etiology (in the combined therapy).
Dosage regimen Triamcinolone Acetonide Ointment
Into adults – 4-20 mg per day in 2-3 doses. After improving the daily dose is gradually reduced by 1-2 mg every 2-3 days to the minimum maintenance dose – 1 mg, and the complete abolition of therapy.
V / m at the beginning of treatment – 40 mg 1 every 4 weeks. Then, depending on the indications and patient response to treatment can be administered at 40-80 mg every 2-4 weeks. If necessary, a single dose may be increased to 100 mg. In order to avoid atrophy of subcutaneous injected deep into the muscle.
With intraarticular injection and the introduction of the lesion dose is 10-40 mg. The interval between the injections at least 1 week.
For application by inhalation dose depends on the dosage form and patient’s age.
Topically applied 1-3 times / day. The duration of treatment is determined individually and is usually 5-10 days. If persistent disease course treatment can be extended to 25 days. We do not recommend the use of more than 4 weeks.
Side effect Triamcinolone Acetonide Ointment
With 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.
From the digestive system: steroid ulcer, erosive and ulcerative lesions of the gastrointestinal tract, acute pancreatitis.
CNS: convulsions, sleep disorders, mental disorders, headaches and dizziness, and weakness.
On the part of the musculoskeletal system: myopathy, osteoporosis.
Cardio-vascular diseases: hypertension.
With the blood coagulation system: thromboembolism.
On the part of the vision: blurred vision, posterior subcapsular cataracts, increased intraocular pressure, or exophthalmos, anaphylactic reactions.
Reactions due to immunosuppressive effects: exacerbation of infectious diseases.
With intraarticular injection: possible joint soreness and irritation at the injection site, depigmentation, sterile abscess, atrophy of the skin, when administered in doses of 40 mg possible side effects of resorptive.
With inhalation use: possible headache, sneezing, coughing, dry mucous membranes of the mouth or nose, a feeling of irritation in the nose, hoarseness, rarely – fungal infection of the throat caused by Candida albicans.
For exterior use: possible itching, skin irritation, eczema-type reaction later, steroid acne, purpura. With prolonged use the ointment may develop secondary infectious lesions and atrophic skin changes.
Contraindications Triamcinolone Acetonide Ointment
Acute psychosis in the history of active TB disease, myasthenia gravis, cancer metastases, diverticulitis, stomach ulcer and duodenal ulcer, hypertension, Itsenko – Cushing, renal failure, thrombosis and embolism, a history of osteoporosis, diabetes, hidden pockets of infection, amyloidosis, syphilis, fungal infections, viral infections (including caused by Herpes simplex and Varicella zoster), amoebic infections, polio (with the exception of the bulbar-encephalitic form), gonococcal or tuberculous arthritis, the period of vaccination lymphadenitis after BCG vaccination, glaucoma infected skin lesions.
Pregnancy and breastfeeding Triamcinolone Acetonide Ointment
If necessary, use during pregnancy (especially in the I trimester) and lactation should assess the expected benefits to the mother and the risk of side effects in the fetus or child.
Cautions Triamcinolone Acetonide Ointment
It is not intended for on / in a.
With caution and under strict medical supervision is used for edema, obesity, mental diseases and diseases of the gastrointestinal tract. During the period of treatment is recommended to take vitamin D and eat foods rich in calcium.
After a single i / m injection at a dose of 60-100 mg over 24-48 hours may be a suppression of adrenal function, which is usually restored within 30-40 days.
When applied topically to prevent local infection is recommended in combination with antimicrobial agents.
Parenteral administration in children under the age of 6 years is not recommended, at the age of 6-12 years – under strict indications.
Should avoid prolonged outdoor use in children regardless of age.
Drug Interactions
While the use of anabolic steroids, androgens increases the risk of peripheral edema, acne.
While the use of antithyroid drugs and thyroid hormones may change thyroid function.
While the use of histamine H1-blockers reduced receptor action of triamcinolone, with hormonal contraceptives – potentiates the effect of triamcinolone.
Hypocalcemia associated with the use of triamcinolone may lead to an increase in the duration of neuromuscular blockade induced by the action of depolarizing muscle relaxants during their simultaneous application.
While the use of immunosuppressive drugs increases the risk of bacterial and viral infections.
While the use of potassium-sparing diuretics can hypokalemia.
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 acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract.
When applied simultaneously weakens the effect of oral hypoglycemic agents, insulin, with a laxative – it is possible hypokalemia, with cardiac glycosides – increase the risk of heart rhythm disturbances and other toxic effects of glycosides.
With the simultaneous use of tricyclic antidepressants may increase mental health problems associated with taking triamcinolone.
While the use of m-holinoblokatorami (including with atropine) may increase the intraocular pressure.
While the use of amphotericin B, carbonic anhydrase inhibitors, the risk of hypokalemia, left ventricular hypertrophy and heart failure.
While the use of isoniazid may decrease the concentration of isoniazid in blood plasma, mainly in patients with rapid acetylation.
With the simultaneous use may accelerate the biotransformation and decreased concentration meksiletina in blood plasma.
While the use of paracetamol increases the risk of hypernatremia, edema, increased excretion of calcium, hypocalcemia, osteoporosis, liver toxicity of paracetamol.
In an application with rifampin, phenytoin, carbamazepine, barbiturates accelerated the metabolism of triamcinolone through the induction of microsomal liver enzymes, diminishes its effect.
While the use of ephedrine accelerates the metabolism of triamcinolone.
