Kenalog - instructions for use, dose, side effects, contraindications

Glucocorticosteroid (GCS) inhibits the release of interleukin-1, 2, gamma-interferon from lymphocytes and macrophages. Has anti-inflammatory, antiallergic, desensitizing, anti-shock, antitoxic and immunosuppressive action.

Suppresses the release of pituitary adrenocorticotropic hormone and beta-lipotropin, but does not reduce the level of circulating beta-endorphin.Oppressing the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Increases the excitability of the central nervous system (CNS), reduces the number of lymphocytes and eosinophils, increases the number of erythrocytes (by increasing the production of erythropoietins).

Interacts with specific cytoplasmic receptors, forming a complex that penetrates into the nucleus of the cell. Synthesized mRNA induces the formation of proteins, (including lipocortin), mediating cellular effects. Lipocortin depresses phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperoxides, prostaglandins, leukotrienes, contributing to the process of inflammation.

Protein metabolism: reduces the amount of protein in the blood plasma (due to globulins) with an increase in the albumin / globulin ratio, increases the synthesis of albumins in the liver and kidneys; enhances the catabolism of the beige in the muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat mainly in the area of the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, which leads to an increase in the intake of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases leading to the activation of gluconeogenesis.

Water-electrolyte exchange: detains sodium ions and water in the body, stimulates the excretion of potassium ions (mineralocorticosteroid activity), reduces the absorption of calcium ions from the gastrointestinal tract, increases their renal excretion.

The anti-inflammatory effect is associated with the inhibition of eosinophil release by inflammatory mediators; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes and membranes of organelles (especially lysosomal).

The antiallergic effect develops as a result of 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, a decrease in the number of circulating basophils,inhibition of lymphoid and connective tissue development, decrease in the number of T- and B-lymphocytes, mast cells, reduction of the sensitivity of effector cells to mediators of allergy, inhibition of antibody formation. The anti-shock and antitoxic effect is associated with increased blood pressure (by increasing the concentration of circulating catecholamines and restoring the sensitivity of adrenoreceptors to them, as well as vasoconstriction), reducing the permeability of the vascular wall, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics. Immunodepressive effect is due to inhibition of the release of cytokines (interleukin-1,2, gamma-interferon) from lymphocytes and macrophages. It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

For anti-inflammatory activity triamcinolone is close to hydrocortisone, triamcinolone 6 times more active. Mineralocorticosteroid activity is low.

Pharmacokinetics:After oral administration, it is easily absorbed from the gastrointestinal tract (GIT). Bioavailability - 20-30%.Connection with plasma proteins - 40%. Metabolized in the liver with the formation of inactive metabolites. The half-life (T1 / 2) of blood plasma is -2-5 hours, from tissues -18-36 hours. It is excreted by the kidneys in the form of inactive metabolites.

Indications:

- Rhematoid arthritis;

- rheumatic fever, acute rheumatic heart disease;

- systemic diseases of connective tissue (systemic lupus erythematosus, scleroderma, etc.);

- Acute allergic reactions;

- severe form of bronchial asthma;

- erythema multiforme;

- hemorrhagic diathesis;

- hemolytic anemia;

- lymphoma, leukemia.

Contraindications:

For short-term use according to vital indications, the only contraindication is hypersensitivity.

Peptic ulcer of the stomach or duodenum, osteoporosis, tuberculosis, newly created anastomosis, diverticulitis, glaucoma, diabetes mellitus, thrombophlebitis, acute viral, bacterial, fungal systemic infections (when no appropriate therapy is performed), Iscenko-Cushing syndrome, post-surgical condition and severe injuries, children under 3 years (for this dosage form), galactosemia, lactase deficiency, glucose-galactose malabsorption syndrome.

Carefully:Chronic renal failure, cirrhosis, chronic hepatitis, hypothyroidism, hyperthyroidism, esophagitis, gastritis, ulcerative colitis, psychosis or psychoneurosis, immunodeficiency (including AIDS or HIV infection), cardiovascular diseases, in tons .h. the recently transferred myocardial infarction (in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle), hyperlipidemia, nephrourolythiasis, hypoalbuminemia and conditions predisposing to its onset (nephrotic syndrome), systemic osteoporosis, obesity (grade III-IV), poliomyelitis (except for the form of bulbar encephalitis), pregnancy, lactation, elderly age.

Pregnancy and lactation:

Preparation Kenalog® should be used with caution in pregnancy, as animal studies indicate a teratogenic effect of triamcinolone (in the first 3 months of use), and data on the safety of the drug during pregnancy in humans are absent.

With prolonged use of the preparation Kenalog®, it is impossible to exclude the violation of intrauterine development.When triamcinolone is used in the last trimester of pregnancy, there is a risk of developing fetal adrenal atrophy. Glucocorticosteroids (GCS) penetrate into breast milk, so during the period of breastfeeding during the treatment with Kenalog® it is necessary to evaluate the benefit / risk ratio.

Dosing and Administration:

Inside, during or after a meal, once a day (preferably in the morning) or in several doses during the day, especially if the daily dose exceeds 16 mg.

The usual daily intake for adults is 4 to 32 mg. When the desired effect is achieved, the dose of the drug should be gradually reduced (by 4 mg every 2-3 days) until the optimal maintenance dose (usually 4 mg per day) is achieved. In children older than 3 years, weighing more than 25 kg apply the same dose as in adults. For children weighing less than 25 kg, the starting dose is 12 mg (3 tablets) per day. The therapeutic effect should develop within 2-3 weeks. In some cases, it may take more than 6 weeks for the clinical effect to be manifested.

Side effects:

Undesirable effects are classified by organs and systems:

Violations of the blood and lymphatic system

Lymphopnea, monocytopenia, polyglobulia and eosinopenia.

Immune system disorders

Skin rash, itchy skin, hives, angioedema, bronchospasm, respiratory arrest, anaphylactic shock.

Disorders from the endocrine system

The delay in the growth and sexual development in children (with prolonged therapy), the decrease in glucose tolerance, steroid diabetes mellitus or the manifestation of latent diabetes mellitus, oppression of the adrenal gland function, the Itenko-Kushngung syndrome (lunar face, pituitary-type obesity, hirsutism, dysmenorrhea, amenorrhea, myasthenia gravis, striae).

Disorders from the metabolism and nutrition

Porphyria, increase serum cholesterol, low-density lipoprotein (LDL) and triglycerides, hypocalcemia, weight gain, negative nitrogen balance, fluid retention and sodium ions (peripheral edema), hypernagraemia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

Disorders of the psyche

Manic-depressive psychosis, depression, disorientation, euphoria, hallucinations, paranoia, nervousness or anxiety, insomnia.

Disturbances from the nervous system

Dizziness, pseudotumor of the cerebellum, headache, increased intracranial pressure, convulsions. Visual impairment of the posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve (glaucoma¹), a tendency to develop secondary bacterial, fungal or viral infections of the eyes, the progression of trophic disorders in the corneal ulcer, exophthalmos, sudden loss of vision (possibly deposition of triamcinolone crystals in the eye chambers), central serous chorioriopathy (see section "Special instructions"), visual perception.

Heart Disease

Arrhythmia, bradycardia (up to cardiac arrest), development (in predisposed patients) or progression of chronic heart failure, changes in ECG, characteristic of hypokalemia. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

Vascular disorders

Increased blood pressure, hypercoagulation, thrombosis, vasculitis.

Disturbances from the respiratory system, chest and mediastinal organs

Decreased voice, irritation and dryness of the oral and pharyngeal mucosa.

Disorders from the digestive system

Nausea, vomiting, pancreatitis, erosive esophagitis, "steroid" stomach and / or duodenal ulcer, bleeding and perforation of the gastrointestinal tract, increase or decrease in appetite, flatulence, hiccups, increased activity of "liver" transaminases and alkaline phosphatase in blood plasma.

Disturbances from the skin and subcutaneous tissues

"Steroid" acne, subcutaneous hemorrhage, dermatitis, ecchymosis, facial erythema, skin atrophy, delayed wound healing, increased sweating, striae, telangiectasia and thinning of the skin, hyper- or hypopigmentation, candidiasis of the oral and pharyngeal mucosa, septic necrosis (especially in patients with systemic lupus erythematosus or rheumatoid arthritis), avascular necrosis, perioral dermatitis (rosacea), hypertrichosis.

Disturbances from musculoskeletal and connective tissue

"Steroid" myopagia, osteonecrosis, osteoporosis² (the maximum loss of bone tissue occurs at the beginning of therapy and mainly affects the spongy (trabecular) bone tissue),slowing growth and ossification processes in children (premature closure of epiphyseal growth zones), decreased muscle mass (atrophy), rupture of tendons.

Violations of the genitals and mammary gland

Violations of the menstrual cycle, impotence.

Laboratory and instrumental data

Leukocytosis (more than 20000 / mm³) without signs of inflammation or neoplastic process.

¹The effect of systemic GCS on an existing glaucoma is usually weak, "steroid" glaucoma often develops in a year or more against the background of systemic application of GCS.

²For the prevention of osteoporosis, it is necessary to apply the minimum effective doses of GCS, and if possible, the forms for external use.

Overdose:

Symptoms: nausea, vomiting, sleep disorder, euphoria, agitation, depression, Itenko-Cushing syndrome, hyperglycemia, glucosuria.

Treatment: symptomatic, amid a gradual withdrawal of the drug.

There is no specific antidote.

Hemodialysis is not effective.

Interaction:

Triamcinolone increases the toxicity of cardiac glycosides (because of the resulting hypokalemia, the risk of arrhythmias increases).

Accelerates the excretion of acetylsalicylic acid (ASA), reduces its concentration in the blood plasma (with the elimination of triamcinolone, the concentration of salicylates in the blood plasma increases and the risk of side effects increases).

With simultaneous use of triamcinolone with live viral vaccines and against the background of other types of immunization, the risk of virus activation and infection development increases. Increases the metabolism of isoniazid, mexiletine (especially in "fast acetylators"), which leads to a decrease in their plasma concentrations.

Increases the risk of hepatotoxic reactions of paracetamol (induction of "hepatic" enzymes and the formation of a toxic metabolite of paracetamol).

Increases (with prolonged therapy) the concentration of folic acid.

In high doses reduces the effect of somatropin.

Triamcinolone reduces the effect of hypoglycemic drugs, increases the anticoagulant effect of coumarin derivatives.

Weaken the influence of vitamin D on the absorption of calcium ions in the lumen of the intestine.

Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase the toxicity of griamcinolone. Indomethacin. displacing triamcinolone from association with albumin, increases the risk of developing its side effects. The simultaneous use of triamcinolone with m-holinoblokatorami (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.

Simultaneous use of inhibitors of the isoenzyme CYP3A, including preparations containing a co-cystitis, may increase the risk of systemic side effects. Simultaneous use should be avoided, except when the benefits of use exceed the risk of systemic side effects of GCS, in which case patients should be monitored for systemic effects of GCS.

Special instructions:

Before and during the treatment of GCS, it is necessary to monitor the total blood test, the concentration of blood glucose, the content of electrolytes in the blood plasma. The use of the drug in acute viral infections (herpes simplex, herpes simplex, herpetic keratitis), chronic active viral hepatitis B, poliomyelitis, systemic mycoses, parasitic invasions, a history of tuberculosis (possible reactivation of the disease) is possible only on strict indications and against the use of specific antimicrobial or antiviral therapy.

Vaccination with live viral vaccines is contraindicated during SCS therapy. Immunization with inactivated viral or bacterial vaccines against the background of SCS does not provide the expected increase in the number of antibodies and does not give the expected protective effect. Therefore, these drugs should not be used 8 weeks before and within 2 weeks after vaccination.

Care should be taken in case of contact of the patient receiving SCS treatment with patients with chicken pox, measles and other contagious diseases, as the risk of the above mentioned infectious diseases increases by accidental contact with infected persons. In such cases, passive immunization is recommended.

It is necessary to perform a specific geranium against the background of using (only by strict indications) the preparation of Kenalog® in patients with gastric and intestinal ulcer, severe osteoporosis, uncontrolled arterial hypertension or diabetes, mental disorders, narrow and wide-angle glaucoma, ulcerative lesion or trauma of the cornea. Caution is necessary in patients after operations and fractures of bones,because SCS can slow the healing of wounds and fractures.

The effect of SCS is enhanced in patients with cirrhosis or hypothyroidism. The use of the drug Kenalog "can change the parameters of skin allergic tests for hypersensitivity.

In children during the period of growth, GCS should be used only in absolute indications and under the close supervision of the attending physician.

Visual impairment

Possible appearance of visual impairment in systemic and local application of GCS. If blurred vision or other visual impairment should consider the possibility of consulting an ophthalmologist to exclude causes such as cataract, glaucoma or rare eye diseases, such as central serous chorioretinopathy (CSCR), reported after systemic and topical application of GCS. With prolonged use of the drug, an ophthalmologist is recommended to be examined every 3 months. Secondary adrenal cortex insufficiency develops against the background of SCS therapy and persists depending on the dose and duration of therapy for several months, and in some cases up to 1 year after discontinuation of therapy.

In patients who are exposed to stress (surgery, traffic accident, etc.), consider increasing the dose of GCS.

A careful medical observation is recommended when using the drug in patients with chronic heart failure and in patients with acute ulcerative colitis, diverticulitis, newly formed intestinal anastomosis (due to the risk of intestinal perforation).

Perhaps masking the symptoms of perforation of the walls of the stomach or intestine, peritonitis.

When conducting a doping control against the background of therapy with GCS, a false positive result is possible.

Effect on the ability to drive transp. cf. and fur:In connection with the possibility of developing dizziness, visual impairment, convulsions, disorientation, inhibition, hallucinations with the use of the Kenalog® drug, patients should refrain from managing vehicles and mechanisms requiring increased concentration of attention and rapidity of motor reactions.

Form release / dosage:

Tablets, 4 mg.

Packaging:

For 50 tablets in a bottle of dark glass (type III), with a lid of polyethylene, free space is filled with hygroscopic cotton wool.

1 bottle is placed in a pack of cardboard along with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C, in the original packaging. Keep out of the reach of children.

Shelf life:

5 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N012381 / 01

Date of registration:12.10.2010 / 11.12.2017

Expiration Date:Unlimited

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Information update date: & nbsp11.01.2018

Illustrated instructions

Instructions

Kenalog® (Kenalog®)