Hydrocortisoni acetas susp. for infection. 2.5% of amp. 2 ml No. 10

Pharmacological properties

Pharmacodynamics. Hydrocortisoni acetas belongs to group gks natural origin. possesses the antishock, anti-toxic, immunosuppressive, anti-exudative, antipruritic, anti-inflammatory, desensibilizing, antiallergenic action. slows down reaction of hypersensitivity, proliferative and exudative processes in the inflammation center. action of Hydrocortisoni acetas is mediated through specific intracellular receptors. anti-inflammatory action is based on braking of all phases of inflammation: stabilization of cellular and subcellular membranes, reduction of release of proteolytic enzymes from lysosomes, slowing down of formation of superoxidic anion and other free radicals. the hydrocortisone slows down release of mediators of inflammation, including interleukin-1, a histamine, serotonin, bradykinin, reduces release of arachidonic acid from phospholipids and synthesis of prostaglandins, leukotrienes, thromboxane. reduces inflammatory cellular infiltrates, reduces migration of leukocytes and lymphocytes in the inflammation center. slows down connective tissue reactions during inflammatory process and reduces intensity of formation of cicatricial fabric. reduces quantity of mast cells which produce hyaluronic acid, the activity of hyaluronidase oppresses and promotes reduction of permeability of capillaries. slows down producing a collagenase and activates synthesis of inhibitors of proteases. reduces synthesis and strengthens catabolism of proteins in muscle tissue. stimulating steroid receptors, induces formation of a special class of proteins — lipokortin in which antiedematous action is inherent. has kontrinsulyarny action, increasing glycogen level in a liver and causes development of a hyperglycemia. detains sodium and water in an organism, increasing at the same time otsk and raising hell (antishock action).

is Stimulated by potassium removal, reduces absorption of calcium from a GIT, reduces a mineralization of a bone tissue.

As well as other glucocorticoids, a hydrocortisone are reduced by quantity of T lymphocytes in blood, reducing thereby impact T-helperov on V-lymphocytes, slows down formation of cell-bound immune complexes, reducing manifestations of allergic reactions.

Pharmacokinetics. The hydrocortisone which is applied locally can be soaked up and show systemic action. It is rather slowly soaked up from the injection site. Up to 90% of medicine contacts blood proteins (with transcortinum — 80%, with albumine — 10%), about 10% represent free fraction. Metabolism is carried out in a liver. Unlike synthetic derivatives, through a placenta the insignificant amount of medicine (up to 67% collapses in the placenta to inactive metabolites) gets. Metabolites of a hydrocortisone are removed mainly with urine.

Indication

Osteoarthritis, different monoarthroses (knee, elbow, coxofemoral joints), a pseudorheumatism and arthritises of other origin (except for tubercular and gonorrheal arthritises). humeroscapular periarthritis, bursitis, epicondylitis, tendovaginitis. before ankylotic joint surgery.

as local addition to system corticosteroid therapy.

Use

Before application contents of an ampoule to stir up

before formation of homogeneous suspension.

to Adults and children aged since 14 years: the single dose depends on the size of a joint and on disease severity — 5–50 mg of a hydrocortisone vnutrisustavno and periartikulyarno.

adult can carry out by

for 24 h injections no more than to three joints.

to Children: the single dose of a hydrocortisone depends on the size of a joint and on disease severity — 5–30 mg vnutrisustavno and periartikulyarno.

Medical effect at intra articulate introduction of medicine occurs for 6–24 h and remains from several days to several weeks. Repeated introduction of medicine is possible in 3 weeks.

Drug cannot be administered directly in a sinew therefore at a tendinitis the medicament needs to be administered in a tendinous vagina.

Drug cannot be used for system corticosteroid therapy.

Contraindication

Hypersensitivity to active ingredient or any of auxiliary components; general fungus diseases; use of live or attenuirovanny vaccines is contraindicated to the patients receiving corticosteroids in immunosuppressive doses (see special instructions); corticosteroid medicines in oil are contraindicated at an idiopathic Werlhof's disease; contraindicated for intrathecal introduction.

Side effects

side reactions Given below are typical for all system corticosteroids. their inclusion in this list not necessarily means that the direct phenomenon was observed at application of this specific dosage form.

Disturbance of laboratory and tool indicators: after treatment the corticosteroids observed increase in the AlAT, AsAT and SF level. Usually these little changes, they are not connected with one clinical syndrome and have reversible character at the treatment termination. Increase in intraocular pressure. Decrease in tolerance to carbohydrates, increase in need for insulin or oral antidiabetic cure for diabetes. Negative nitrogenous balance owing to catabolism of proteins. Increase or decrease in mobility and quantity of spermatozoa.

from metabolism and food: sodium delay, liquid delay, potassium loss, gipokaliyemichesky Alkalosis, increase in excretion of calcium, increase in appetite, abnormal fat deposits, increase in body weight.

from heart: bradycardia, cardiac arrest, violations of a heart rhythm, expansion of borders of heart, hypertrophic cardiomyopathy, fluid lungs, syncope, tachycardia. Stagnant heart failure at susceptible patients.

Vascular frustration: petechias and ecchymomas, bruises, AG, vascular collapse, a fat embolism, a rupture of a myocardium after recently postponed myocardial infarction, a thrombembolia, thrombophlebitis, a vasculitis.

from skin and hypodermic cellulose: urticaria, an acne, allergic dermatitis, a skin and hypodermic atrophy, thin weak skin, dryness and peeling of skin, hypostasis, an erythema, a hyperpegmentation, hypopigmentation, a hypertrichosis, the increased sweating, rashes, striya, thinning of hair on the head; at the patients receiving corticosteroid therapy it was reported about development of Kaposi sarcoma.

General violations and violations in the injection site: reactions in the injection site, including burning or pricking, infections in the place of an injection, sterile abscess, oppression of reaction to skin tests, false skin reactions, a delay of healing of wounds, a demonstration of latent diabetes, masking of infections, activation of latent infections, including repeated activation of tuberculosis, the opportunistic infections caused by any pathogens, any localization from lungs to lethal, decrease in resistance to infections, an indisposition.

from nervous system: benign intracranial hypertensia, convulsive attacks, dizziness, headache, neuritis, neuropathies, paresthesias. The arachnoiditis, meningitis, a paraparesis/paraplegia, touch frustration developed after intrathecal application.

from an organ of sight: back subkapsulyarny cataracts, an exophthalmos, glaucoma, the exceptional cases of a blindness associated with injections in a periokulyarny zone.

from the respiratory system, bodies of a thorax and mediastinum: if at preparation of suspension to apply benzyl alcohol, it is necessary to take into account that benzyl alcohol can lead to development of a syndrome of an asthma with a lethal outcome at premature children.

from a GIT: a hiccups, development of a round ulcer with possible perforation and bleeding, gastric bleeding, pancreatitis, an esophagitis, perforation of intestines, an abdominal distension, intestines dysfunction, nausea.

from kidneys and an urinary system: glucosuria, bladder dysfunction.

from a gepatobiliarny system: hepatomegalia.

from a musculoskeletal system and connective tissue: a corticosteroid myopathy, an arthropathy, loss of muscle bulk, muscle weakness, osteoporosis, pathological changes, compression spinal fractures, aseptic necrosis, a rupture of a sinew, in particular an Achilles tendon, a growth inhibition at children.

Endocrine violations: irregular menstrual cycle, development of a cushingoid state, hirsutism, oppression of a system hypophysis adrenal glands.

from the immune system: reactions of hypersensitivity, including anaphylaxis and anaphylactoid reactions (for example bronchospasm, Quincke's disease).

Mental disorders: euphoria, insomnia, changes of mood, change of the personality, depression, mental disorders; sharpening of the existing emotional instability or tendencies to development of psychosis.

Special instructions

to Patients who receive corticosteroid therapy and transfer an unusual stress, to, in time and after a stressful situation the application of corticosteroids in the raised doses or corticosteroids of fast action is shown.

Corticosteroids can mask some symptoms of an infection, and at their application there can be new infections. At application of corticosteroids resistance of an organism to infections and ability of an organism localize an infection can be reduced.

Development of the infections of any localization caused by any pathogens (including viral, bacterial, fungal, protozoan or gelmintny infections), can be connected with application of corticosteroids as monotherapy or in a combination with other immunosuppressive means influencing a cellular link of immunity, a humoral link of immunity or function of neutrophils. Such infections can be lungs, but can be heavy degree and sometimes lethal. With increase in doses of corticosteroids the frequency of development of infectious complications increases.

In active, disseminate or fulminantny tuberculosis a hydrocortisone can be applied only to treatment of a disease together with the corresponding antitubercular scheme of treatment. If application of corticosteroids is shown to patients with latent tuberculosis or tuberkulinovy reactivity, careful observation as the disease can be activated again is necessary. During long corticosteroid therapy such patients have to receive chemoprophylaxis.

to the Patients receiving corticosteroids in immunosuppressive doses use of live or attenuirovanny vaccines is contraindicated to

; at such patients it is necessary to apply the killed or inactivated vaccines. However the answer to such vaccines can be reduced. Holding procedures of immunization is shown to the patients receiving corticosteroids in not immunosuppressive doses.

Hydrocortisone can cause increase in the ABP, a delay of sodium and water in an organism and increase in excretion of potassium. Therefore observance of a diet with restriction of amount of table salt and the use of nutritional supplements on the basis of potassium can be required. All corticosteroids increase calcium excretion.

As in isolated cases at the patients receiving treatment by corticosteroids parenterally anaphylactoid reactions developed (for example a bronchospasm), before their application it is necessary to take the appropriate measures of precaution, especially when in the anamnesis of the patient there is an allergy to any medicine.

In spite of the fact that recent researches were not conducted using a hydrocortisone or other steroids, results of researches of use of Methylprednisolonum of sodium of succinate at septic shock demonstrate that in some subgroups of patients of high risk (that is patients with increase in level of creatinine more than 2 mg/dl or consecutive infections) increase in lethality can be noted.

Effect of a hydrocortisone can be strengthened at patients with a liver disease as at them metabolism and removal of a hydrocortisone are considerably reduced.

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At the children receiving long-term treatment by glucocorticoids in the divided daily doses the growth inhibition can be noted. Use of such scheme of treatment has to be limited to the most serious indication.

Corticosteroids should be applied with care at patients with the herpes simplex of eyes which is followed by risk of perforation of a cornea.

At application of corticosteroids mental disorders which vary from euphoria, insomnia, changes of mood, changes of the personality before obvious demonstrations of psychosis can arise. Also corticosteroids can cause aggravation of the existing emotional instability or a trend of development of psychosis.

Corticosteroids should be applied with care at nonspecific ulcer colitis if there is a perforation likelihood of development in the presence of abscess or other piogenic infections and also at a diverticulitis, a fresh intestinal anastomosis, an active or latent round ulcer, a renal failure, AG, osteoporosis and a myasthenia gravis.

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At application of high doses of corticosteroids described cases of development of a sharp myopathy which arises at patients with neuromuscular transmission violations more often (in particular myasthenias gravis) or at the patients receiving therapy by neuromuscular blockers (such as pankuroniya). Such sharp myopathy is generalized, can affect respiratory muscles and muscles of eyes and to lead to development of a kvadriparez. Increase in the KFK level can be noted. Before clinical improvement or recovery after phase-out of corticosteroids can pass from several weeks to several years.

messages about development of Kaposi sarcoma in the patients receiving therapy by corticosteroids Were available, however the termination of therapy can lead to its clinical remission.

for the purpose of reduction of a possibility of development of an atrophy of skin in the injection site should not exceed the recommended doses. It is necessary to avoid an injection in a deltoid muscle because of high risk of development of a hypodermic atrophy.

should not apply High doses of corticosteroids to treatment at a craniocereberal injury.

Published data confirm probable communication between application of corticosteroids and a rupture of a myocardium after recently postponed myocardial infarction; therefore these patients should perform therapy using corticosteroids with extra care.

oppression gipotalamo - a hypophysial and adrenal system Can cause, development of a syndrome of Cushing and a hyperglycemia.

Secondary adrenocortical insufficiency caused by use of medicine can be reduced by a gradual dose decline. Insufficiency such can remain within several months after the therapy termination. Therefore in any situation of manifestation of a stress during this period the hormonal therapy has to be restored.

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At simultaneous application with Amphotericinum B noted cases of expansion of borders of heart and development of heart failure (see INTERACTIONS).

exacerbation of the intercurrent infections caused by Amoeba, Candida, Cryptoccocus, Mycobacterium, Nocardia, Pneumocystis and Toxoplasma Can cause

. Before therapy the corticosteroids recommend to exclude a latent or active amebiasis at the patients visiting the tropical countries or at patients with diarrhea of not clear genesis.

not to apply

at cerebral malaria as is not present for this time of proofs of advantage of application of corticosteroids at this state.

Chicken pox and measles: there can be serious or even lethal complications at adults and children. Patients who had no these diseases in the past should be protected carefully from risk of distribution on them these diseases.

Use of corticosteroids can cause a back subkapsulyarny cataract, glaucoma, injury of optic nerves, can contribute to the development of the consecutive eye infections caused by bacteria, mushrooms or viruses.

to Apply

with extra care at patients with the known or suspected defeat of Strongyloides. At such patients the immunosuppression can lead to a hyper infection and distribution of migration of larvae that can cause a heavy coloenteritis and a lethal gram-negative septicaemia.

With care should be applied at patients with stagnant heart failure, AG.

to Patients with a hypothyroidism a dose of corticosteroids needs to be adjusted.

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At patients with cirrhosis notes stronger effect due to decrease in metabolism of corticosteroids.

At therapy by corticosteroids increase in the intraocular pressure demanding control, especially at long therapy is possible

.

It is medicine contains sorbite. If at the patient the intolerance of some sugars is established, it is necessary to consult with the doctor before taking this drug.

It is medicine contains benzyl alcohol therefore it cannot be applied at premature children and newborns. Can cause toxic and allergic reactions in babies and children up to 3 years.

It is medicine contains less than 1 mmol (23 mg) / a sodium dose, that is it is almost free from sodium.

Use during pregnancy and feeding by a breast

Use during pregnancy. Researches on animals showed that corticosteroids in case of their application for a pregnant female in high doses can cause fruit malformations. Adequate researches of influence on reproductive function of the person were not conducted. Therefore use of this medicine during pregnancy or demands careful assessment of advantage of application in comparison with potential risks for the pregnant woman from the women wishing to become pregnant and a fruit. As proofs of safety of application for the person during pregnancy are indirect, the hydrocortisone can be applied at pregnancy, only if the advantage of therapy for mother exceeds risk for a fruit.

Corticosteroids easily pass

through a placental barrier. The children born by women who received high doses of corticosteroids during pregnancy should be examined carefully concerning signs of insufficiency of bark of adrenal glands.

Use during feeding by a breast. Corticosteroids get into breast milk. The hydrocortisone can be applied during feeding by a breast, only if the advantage of therapy for mother exceeds risk for the child.

Carcinogenicity, mutagenicity, influence on fertility. Adequate researches on animals of existence or absence at corticosteroids of cancerogenic or mutagen action were not conducted.

Corticosteroids can raise or reduce mobility and quantity of spermatozoa at some patients.

Children. At children medicament is used only according to absolute indications.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Influence of corticosteroids on ability to operate trasportny means or to work with other automated systems was not estimated. After treatment by corticosteroids development of such undesirable effects as to a syncope, vertigo and spasms is possible. With the above-stated effects the patients should not steer vehicles or to work with other automated systems.

Interaction

Medicines — inductors of liver enzymes, such as phenobarbital, Phenytoinum and rifampicin, can increase clearance of corticosteroids, and at their application the increase in a dose of corticosteroids can be required to receive the desirable response to treatment.

Such medicines as troleandomitsin and ketokonazol, can inhibit metabolism of corticosteroids and reduce their clearance. Therefore it is necessary to titrate a dose of corticosteroids in order to avoid development of their toxicity.

Corticosteroids can increase clearance of aspirin which apply a long time and in high doses. It can cause decrease in levels of salicylate in blood serum or increase in risk of development of salitsilatny toxicity at cancellation of corticosteroids. Acetylsalicylic acid should be applied with care together with corticosteroids to patients with a gipotrombinemiya.

Influence of corticosteroids on oral anticoagulants substantially varies

; they can both weaken, and to strengthen their action. Therefore it is necessary to carry out regular monitoring of indicators of a koagulogramma for the purpose of maintenance of desirable anticoagulating effect.

With care should be applied with the medicines influencing potassium level (for example diuretics). Not to apply with Amphotericinum B.

Corticosteroids can cause a hyperglycemia therefore it is necessary to apply with antidiabetic means with care.

Antibiotics. It was reported that makrolidny antibiotics caused significant decrease in clearance of corticosteroids.

Cyclosporines. At simultaneous use of these medicines the increase in activity and cyclosporine, and a corticosteroid is noted. It was reported also about cases of developing of spasms.

Antikholinesterazny medicines. Simultaneous application can lead to development of heavy weakness in patients with a myasthenia gravis. Therefore it is necessary to stop use of these medicines not less than for 24 h prior to therapy by corticosteroids.

Anti-diabetic means. As corticosteroids can increase concentration of glucose in blood, there can be a need for dose adjustment of anti-diabetic means.

Antituberculous remedies. Decrease in concentration of an isoniazid in blood plasma is possible.

Holestiramin can increase clearance of corticosteroids.

Aminoglyutemid can cause loss of the adrenalny suppression induced by corticosteroids.

Cardiac glycosides. At the patients applying cardiac glycosides the increased risk of developing arrhythmia because of a hypopotassemia is noted.

Are oestrogenic

, including oral contraceptives. Estrogen can cause decrease in metabolism of certain corticosteroids in a liver, being the reason of increase in their effect.

Skin tests. Corticosteroids can suppress reactions to skin tests.

Vaccine. At the patients who are on long therapy by corticosteroids the slight answer to the toksoidny and live or inactivated vaccines because of oppression of the answer of antibodies can be shown. Corticosteroids can also exponentiate the answer of some organisms which are contained in live attenuirovanny vaccines.

At use of vaccines or toxoids according to the plan of vaccination should consider the possibility to postpone vaccination until completion of therapy by corticosteroids.

Overdose

Clinical syndrome of overdose of a hydrocortisone does not exist.

Hydrocortisone is removed by

by dialysis.

Storage conditions

In original packing at a temperature not above 25 °C. not to freeze.