Кеналог®

General characteristics. Structure:

Active ingredient: 40 mg of Triamcinolonum of acetonide.

Excipients: benzyl alcohol, sodium chloride, a karmelloza of sodium, polysorbate 80, Acidum hydrochloricum, sodium hydroxide, water for injections.

Pharmacological properties:

Pharmacodynamics. The glucocorticosteroid (GKS), slows down release interleykina-1,2, gamma interferon from lymphocytes and macrophages. Renders the antiinflammatory, antiallergic, desensibilizing, antishock, anti-toxic and immunodepressive effect.

Suppresses release by a hypophysis of adrenocorticotropic hormone and beta липотропина, but does not reduce the level of the circulating beta endorphine. Oppresses secretion of thyritropic hormone and follicle-stimulating hormone. Increases excitability of the central nervous system, reduces quantity of lymphocytes and eosinophils, increases number of erythrocytes (due to strengthening of production of erythropoetins).

Interacts with specific cytoplasmatic receptors, forming the complex getting into a cell kernel. The synthesized MRNK induces formation of the proteins (in a t.ch.lipokortin) mediating cellular effects. Lipokortin oppresses A2 phospholipase, suppresses release of arachidonic acid and inhibits synthesis of endoperoxides, prostaglandins, the leukotrienes promoting process of an inflammation.

Protein metabolism: reduces amount of protein in plasma (at the expense of globulins) with increase in coefficient albumine/globulin, increases synthesis of albumine in a liver and kidneys; strengthens a protein catabolism in muscular tissue.

Lipidic exchange: increases synthesis of polyunsaturated fatty acids and triglycerides, redistributes fat (accumulation of fat is preferential in the field of a shoulder girdle, the person, a stomach), leads to development of a hypercholesterolemia.

Carbohydrate metabolism: increases absorption of carbohydrates from digestive tract; increases activity of glkzhozo-6-phosphatase that leads to increase in intake of glucose from a liver in blood; increases activity of a fosfoenolpiruvatkarboksilaza. and synthesis of the aminotransferases leading to activation of a gluconeogenesis.

Water and electrolytic exchange: detains ions of sodium and water in an organism, stimulates removal of potassium ions (mineralokortikosteroidny activity), reduces absorption of calcium ions from digestive tract, raises their renal excretion.

The antiinflammatory effect is connected with release oppression by eosinophils of mediators of an inflammation; induction of formation of lipokortin and reduction of quantity of the mast cells producing hyaluronic acid; with reduction of permeability of capillaries; stabilization of cellular membranes and membranes of organellas (especially lizosomalny).

The antiallergic effect develops as a result of suppression of synthesis and secretion of mediators of an allergy, braking of release from sensitized mast cells and basophiles of a histamine, etc. biologically active agents, reduction of number of the circulating basophiles, suppression of development of adenoid and connecting tissue, decrease in number of T - and V-lymphocytes, mast cells, decrease in sensitivity of effector cells to mediators of an allergy, antibodyformation oppression. At obstructive respiratory diseases action is based, mainly, on braking of inflammatory processes, oppression of eosinophilic infiltration of a submucosal layer of an epithelium of bronchial tubes and adjournment in mucous bronchial tubes of the circulating cell-bound immune complexes, and also braking of an erozirovaniye and desquamation mucous. Increases sensitivity of beta adrenoceptors of bronchial tubes of small and average caliber to endogenous catecholamines and exogenous sympathomimetics, reduces viscosity of slime due to oppression or reduction of its products.

Antishock and anti-toxic action is connected with increase in arterial pressure (due to increase in concentration of the circulating catecholamines and recovery of sensitivity to them of adrenoceptors, and also vasoconstrictions), decrease in permeability of a vascular wall, membranoprotektivny properties, activation of the enzymes of a liver participating in metabolism endo-and xenobiotics. The immunodepressive effect is caused by braking of release of cytokines (interleykinov-1,2; gamma interferon) from lymphocytes and macrophages. Slows down connective tissue reactions during inflammatory process and reduces a possibility of formation of cicatricial fabric.

On antiinflammatory activity Triamcinolonum is close to a hydrocortisone, acetonide is 6 times more active than Triamcinolonum. Mineralokortikosteroidny activity low.

Pharmacokinetics. At intramuscular introduction slowly, but it is completely absorbed. Communication with proteins of plasma - 40%. It is metabolized in a liver in the way 6 - beta hydroxylations to inactive metabolites; partial metabolism is carried out in kidneys. It is removed by kidneys in the form of inactive transmutation products.

After intramuscular introduction at most of effect action duration at intramuscular introduction - 1-6 weeks, in a joint cavity - several weeks is observed later 24-48 h.

Indications to use:

System treatment
- As short-term additional therapy of a posttraumatic osteoarthritis, a synovitis, an osteoarthritis, a pseudorheumatism, an acute and podsotry bursitis, an epicondylitis, acute неспецифическогог a tenosinovita, bad attacks of gout, psoriasis arthritis, an ankylosing spondylitis, a juvenile pseudorheumatism;
- At aggravations or as a maintenance therapy of a system lupus erythematosus, an acute rhematoid carditis;
- Pemphigoid, heavy multiformny erythema (Stephens-Jones's syndrome), exfoliative dermatitis, heavy psoriasis
- The expressed allergic diseases: allergic rhinitis, .bronkhialny asthma, Quincke's edema, contact dermatitis, atopic dermatitis, allergic reactions to medicines and serums, stings of insects;
- Serious chronic allergic and inflammatory illness of organs of sight: herpes, iritis, iridocyclitis, chorioretinitis, diffusion, back uveitis, neuritis of an optic nerve, sympathetic ophthalmia, inflammation of a front segment;
- Diseases of respiratory bodies: symptomatic sarcoidosis, berylliosis, aspiration pneumonia;
- Hematologic diseases: the acquired autoimmune anemia;
- Oncological diseases: palliative treatment of leukemia and leukosis at adults; acute leukemia at children;
- At hypostases: for strengthening of a diuresis and treatment of a proteinuria at a nephrotic idiopathic syndrome without uraemia or the nephrotic syndrome caused by a system lupus erythematosus.

Topical treatment. Intra joint or circumarticular introduction and introduction to a sinew vagina as additional short-term therapy at a synovitis, an osteoarthritis, a pseudorheumatism, an acute and subacute bursitis, bad attacks of gout, an epicondylitis, an acute nonspecific tenosinovit, a posttraumatic osteoarthritis.

Route of administration and doses:

Drug is not intended for intravenous, intradermal, intraocular, epidural and intrathecal use. It is necessary to be careful also concerning inadvertent intravascular introduction, first of all to the area of the left side of the person, head skin, and also in a buttock.

Before use contents of an ampoule to stir up and be convinced of lack of particles or conglomerates. At prolonged use drug withdrawal should be carried out gradually.

System treatment (intramuscular introduction). The dosage for adults and teenagers is more senior than 12 years is defined individually and depends on the nature of a disease, usually varying from 40 mg to 80 mg (1 - 2 ml of drug). The drug is administered by a slow deep intramuscular injection to the area of a buttock, using a needle not less than 3,8 cm long. After an injection it is necessary to press densely for 1-2 minutes a sterile napkin to a drug injection site. For treatment of hay fever and other seasonal allergic diseases one injection of drug (40 - 100 mg) suffices usually during a blossoming season. In need of several injections it is necessary to observe an interval between introductions not less than 4 weeks.

Children are 6-12 years old: an initial dose - 40 mg, with repetition of an injection in 4 weeks as required.

Topical treatment
a) At intra joint introduction the dose is defined by the sizes of a joint and weight of symptoms. Usually for adults and children 12 years are more senior (see Contraindications) the following doses of drug are used: small joints (for example, phalanxes of fingers of hands and legs) to 10 mg; joints of the average size (for example, humeral, elbow) 20 mg; large joints (for example, coxofemoral, knee) 20-40 mg.

At damage of several joints the general dose of drug can make up to 80 mg. At excess amount of synovial fluid a part it should be removed by means of the syringe to avoid drug dilution. For ensuring more bystry stopping of symptoms the drug can be administered in a combination with the local anesthetic (which is not containing vasoconstrictive drug). Injections should be carried out so that to avoid creation of depot of drug in hypodermic fatty tissue. At injections it is necessary to meet conditions of the most strict asepsis. Before carrying out an intra joint injection the site of skin is prepared, as before carrying out surgeries. Repeatedly it is necessary to use drug not earlier than in 2 weeks.

b) At intra focal introduction at the small centers of defeat: inflammations of a joint bag (bursitis), periostites to adults and children 12 years depending on the size and localization of the defeats subjected to treatment are aged more senior enter up to 10 mg of drug and at defeats of the big size - from 10 to 40 mg of drug, dilute with normal saline solution of sodium of chloride and fanlikely enter into the area which is characterized by the greatest morbidity. It is necessary to avoid creation of big depots drug. Kenalogum can also be mixed with local anesthetic. Repeatedly it is necessary to use drug not earlier than in two weeks.

c) At introduction to area of skin defeats, 1 ml of drug in concentration of 40 mg/ml dilute with the local anesthetic which is not containing vasoconstrictive substance and mix in the syringe. The injection is carried out horizontally to the area between skin and a hypodermic for providing anesthesia of infiltrate. As an approximate dose 1 mg of drug on 1 cm3 of a surface of skin defeat is recommended. At treatment of several centers of defeat in one step the daily dose of drug by the adult should not exceed 30 mg, and to children (see Contraindications) - 10 mg. At keloid cicatrixes the drug can be administered directly without dilution in hem fabric; not to enter subcutaneously. Repeatedly it is necessary to use drug not earlier than in 2 weeks.

Features of use:

Pregnancy and lactation. The drug Kenalogum uses by pregnant women given on safety are absent. At prolonged use of the drug Pregnant Woman's Kenalogum by the woman it is impossible to exclude disturbance of pre-natal fetation. At use of drug at the end of pregnancy there is a danger of development of an atrophy of adrenal glands of a fruit.

At use of drug during pregnancy (and also women of childbearing age out of pregnancy) it is necessary to compare in each case estimated advantage for the woman and possible risk for the child. GKS at system use get into maternal milk therefore it is necessary to compare in each case estimated advantage for the woman and possible risk for the child.

Drug is not intended for intravenous, intradermal, intraocular, epidural and intrathecal use. The serious undesirable phenomena were noted at epidural and intrathecal ways of introduction.
For the prevention of an atrophy of fabrics in the place of an intramuscular injection it is necessary to drive drug deeply in a gluteus.

Drug renders therapeutic effect during a long span after introduction, however, it is not intended for use in emergency situations. At topical administration of drug it is necessary to estimate its compatibility with at the same time entered local anesthetics.

Mixing with an equal volume of solutions of local anesthetics (1% solution of Procainum or 1% lidocaine solution) in the syringe, but not in an ampoule is allowed.

Prior to the beginning of and during GKS of therapy it is necessary to control the general blood test, a glycemia, content of electrolytes in a blood plasma.

At prolonged use of GKS the risk of development of a subcapsular cataract and glaucoma, sometimes with injury of an optic nerve increases. Frequency of consecutive infections of eyes can also increase.

The research of synovial fluid in each joint is necessary for an exception of septic process. The considerable strengthening of pains which is followed by local hypostasis, further restriction of mobility of a joint, fever and an indisposition gives the grounds to assume development of septic arthritis. If sepsis is confirmed, performing the corresponding antimicrobic therapy is necessary. At therapy during intercurrent infections, septic states, tuberculosis - at the same time carry out treatment by antibiotics.

It is not necessary to enter into "unstable" joints, into the area of an Achilles tendon (risk of a gap). Vaccination by live virus vaccines is contraindicated during therapy of GKS. Immunization by the killed virus or bacterial vaccines against the background of use of GKS does not provide the expected growth of quantity of antibodies and does not give the expected protective effect. Therefore it is not necessary to appoint similar drugs in 8 weeks prior to and within 2 weeks after vaccination.

At the patients who did not have chicken pox and receiving treatment of GKS the risk of a disease of chicken pox or a herpes infection at accidental contact with the infected persons increases. In such cases passive immunization is recommended. Care is necessary at patients after operations and fractures of bones as glucocorticosteroids can slow down healing of wounds and changes in connection with strengthening of removal of calcium from an organism.

Action of GKS amplifies at patients with cirrhosis or a hypothyroidism. Use of the drug Kenalogum can change indicators of tests for hypersensitivity.

GKS can mask some symptoms of the available infectious diseases, and also emergence of an infection in the course of treatment. At their reception decrease in immunity and weakening of process of localization of an infection can be noted.

Use of GKS can provoke an aggravation of symptoms and strengthening of migration of larvae at patients with a strongyloidosis that can bring to a heavy coloenteritis and a lethal outcome owing to a gram-negative septicaemia.

At use of GKS (especially high and average doses of a hydrocortisone and cortisol) increase in arterial pressure, a delay of liquid and salts, the strengthened potassium removal can be observed. Though these phenomena are less expressed at purpose of synthetic GKS (such as drug Kenalogum), however, can be required restriction of salt in food and additional administration of drugs of potassium. At prolonged use of drug it is necessary to provide sufficient consumption of the proteinaceous food necessary for maintenance of nitric balance of an organism.

In the presence the patient of a peptic ulcer of a stomach against the background of treatment of GKS can have asymptomatic its aggravation until a perforation of the ulcer or began bleedings. Considering also that fact, that GKS at prolonged use cause a hyperoxemia of a gastric juice that can lead to stomach ulceration, it is necessary to appoint the corresponding scheme of treatment of a peptic ulcer.

At children in a growth period of GKS have to be applied only according to absolute indications and under especially careful observation of the attending physician.

At treatment of GKS disturbances of a menstrual cycle can be observed. Due to the risk of development heavy allergic reactions (up to an acute anaphylaxis) against the background of parenteral administration of GKS, it is necessary to observe extra care at treatment of patients with allergies in the anamnesis.

Drug contains the benzyl alcohol capable to cause serious side reactions (including with a lethal outcome), especially in children. It should be considered at appointment to patients (especially to children) high doses of the drug Kenalogum and long courses of treatment.

Influence on ability to manage vehicles and mechanisms. mother during treatment needs to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of development and expressiveness of side effects depends on duration of use, size of the used dose and a possibility of observance of a circadian rhythm of appointment.

From endocrine system: disturbances of a menstrual cycle (a dysmenorrhea, an amenorrhea), decrease in tolerance to glucose, a glucosuria, a steroid diabetes mellitus or manifestation of a latent diabetes mellitus, increase in need for insulin or peroral glucose-lowering drugs in the presence of diabetes, oppression of function of adrenal glands and a hypophysis, an Icenco-Cushing syndrome (a crescent-shaped face, obesity of pituitary type, a hirsutism, increase in the ABP, muscular weakness, striya), a delay of sexual development at children.

From the alimentary system: pancreatitis, an erosive esophagitis, an ulcer with possible bleedings and perforation, a meteorism.

From cardiovascular system: arrhythmias, bradycardia (up to a cardiac standstill); development (at predisposed patients) or strengthening of expressiveness of heart failure, change on the ECG characteristic of a hypopotassemia, increase in the ABP, a necrotizing angiitis, hypercoagulation, a thromboembolism, thrombophlebitis.

From a nervous system: increase in intracranial pressure, pseudoneoplasm of a brain, spasm, dizziness, headache, sleeplessness, paresthesia, deterioration in a course of psychiatric diseases, depression (sometimes heavy), euphoria, differences of mood, psychoses, change of the personality.

From sense bodys: sudden loss of sight (adjournment of crystals of drug in chambers of the eye is possible), a back subkapsulyarny cataract, glaucoma, increase in intraocular pressure with possible injury of an optic nerve, tendency to development of consecutive bacterial, fungal or viral infections of eyes, trophic changes of a cornea, an exophthalmos.

From a metabolism: hypocalcemia, increase in body weight, negative nitrogenous balance, delay of liquid and sodium (peripheral hypostases), hypernatremia, hypopotassemia.

From a musculoskeletal system: delay of growth and processes of ossification at children, osteoporosis (it is very rare - pathological fractures of bones, an aseptic necrosis of a head humeral and a femur), a rupture of sinews of muscles, a steroid myopathy, decrease in muscle bulk (atrophy).

From integuments and mucous membranes: petechias, ecchymomas, hyper - or hypopigmentation, tendency to development of a pyoderma and candidiases, a hirsutism, the slowed-down healing of wounds, thinning of skin, steroid eels, striya, an erythema in a face, the increased sweating, volchanko-like injuries of skin.

Allergic reactions: generalized (skin rash, itch, acute anaphylaxis), local allergic reactions.

The general: development or an exacerbation of infections, a leukocyturia, a syndrome of "cancellation" after the sharp termination of use of drug.

In an injection site: burning, a onemeneniye, pain, a pricking, infections (sterile abscess), a necrosis of surrounding fabrics, formation of hems in the place of an injection, an atrophy of skin and hypodermic cellulose at introduction in oil (introduction to a deltoid muscle is especially dangerous).

Interaction with other medicines:

The combined use with non-steroidal anti-inflammatory drugs increases risk of developing of gastrointestinal bleedings and formation of ulcers. Kenalogum can increase renal clearance of salicylates therefore on their background concentration of salicylates in blood serum can decrease. On the other hand, therapy cancellation by the drug Kenalogum against the background of reception of high doses of salicylates can lead to toxic action of the last. It is necessary to observe extra care at co-administration of GKS and acetylsalicylic acid to patients with a prothrombinopenia.

At combined use of GKS and ketokonazol the clearance of GKS decreases that leads to strengthening of their effect. Serumal concentration of an isoniazid can decrease at its use together with GKS.

Simultaneous use of cyclosporine and GKS leads to strengthening of effect of ody drugs. Tricyclic antidepressants can increase expressiveness of the depression caused by reception of GKS therefore they are not shown for therapy of these side effects.

At a concomitant use with oral contraceptives the elimination half-life of GKS can be extended, their effect to amplify, and the frequency of side effects to increase.

Efficiency of the drug Kenalogum can decrease if it is entered along with inductors of liver enzymes (rifampicin, barbiturates, Phenytoinum, carbamazepine, Primidonum, ephedrine and аминоглутетимид).

GKS reduce therapeutic effect of antidiabetic means, strengthen or weaken effect of anticoagulants.

At co-administration of Amphotericinum In and the means which are washing away potassium from an organism, GKS can strengthen a hypopotassemia.

Inhibitors of acetylcholinesterase and GKS show antagonism at combined use.

The combined use of GKS and drugs of a foxglove can lead to strengthening of toxicity of the last.

Action of a growth hormone can be weakened under the influence of GKS.

The effect of not depolarizing muscle relaxants can amplify or be weakened under the influence of GKS.

At simultaneous use of GKS with live antiviral vaccines and against the background of other types of immunizations the risk of activation of viruses and development of infections increases. At therapy of GKS false-negative results of tests for existence of a bacterial infection can be observed.

Contraindications:

- Hypersensitivity to any component of drug;
- acute viral, bacterial, fungal system infections;
- at intramuscular use - an idiopathic Werlhof's disease;
- children's age up to 6 years (intramuscular introduction).

With care. Chronic renal failure, acute glomerulonephritis; chronic nephrite; thrombophlebitis; thromboembolism; osteoporosis; dieback; the metastasizing carcinoma; myasthenia гравис; cirrhosis; chronic liver failure, hypothyroidism, thyrotoxicosis, Itsenko-Cushing's disease, diabetes mellitus, esophagitis, gastritis, peptic ulcer of a stomach (active or latent phases); nonspecific ulcer colitis with threat of perforation or abscessing, sleeplessness, a depression, euphoria, psychosis or a psychoneurosis, immunodeficiency (including AIDS or HIV infection), displays of herpes on a mucous membrane of eyes; abscess, a diverticulitis, recently undergone operation on an intestines neostomy; recently postponed myocardial infarction), dekompensirovanny chronic heart failure, arterial hypertension, a lipidemia); pregnancy, period, feedings by a breast; advanced age.

Overdose:

Symptoms: confusion of consciousness, nausea, vomiting, frustration of a dream, euphoria, excitement, depression, gastrointestinal bleedings, nasal bleedings, crescent-shaped face, arterial hypertension. At prolonged use and bystry drug withdrawal - gneteny functions of bark of adrenal glands, Cushing's syndrome.

In cases of overdose it is necessary to reduce a dose to gradual drug withdrawal and to carry out a symptomatic treatment. There is no specific antidote. Effects of overdose can remain several weeks.

Storage conditions:

At a temperature from 15 to 25 °C in the place protected from light. To store in the place, unavailable to children. List B. A period of validity - 3 years. Not to use drug after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Suspension for injections of 40 mg/ml. Packaging: on 5 ampoules (1 ml) in a tray. 1 tray together with the application instruction is placed in a cardboard pack.