Hydrocortisoni acetas

General characteristics. Structure:

Active ingredient: hydrocortisone;

1 ml of suspension contains Hydrocortisoni acetas in terms of 100% dry matter of 25 mg;

excipients: propylene glycol, sorbite (Е 420), povidone, sodium chloride, benzyl alcohol, water for injections.

Pharmacological properties:

Pharmacodynamics. Hydrocortisoni acetas concerns to group of glucocorticosteroids of a natural origin. Possesses the antishock, anti-toxic, immunosuppressive, anti-exudative, antipruritic, antiinflammatory, desensibilizing, antiallergenic action. Slows down hypersensitivity reaction, proliferative and exudative processes in the inflammation center. Action of Hydrocortisoni acetas is mediated through specific intracellular receptors. Antiinflammatory action is based on braking of all phases of an inflammation: stabilization of cellular and subcellular membranes, reduction of release of proteolytic enzymes from lysosomes, braking of formation of superoxidic anion and other free radicals. The hydrocortisone slows down release of mediators of an inflammation, including interleykina-1 (IL-1), a histamine, serotonin, bradikinin, etc., 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, activity of hyaluronidase oppresses and promotes reduction of permeability of capillaries. Brakes products of a collagenase and activates synthesis of inhibitors of proteases. Reduces synthesis and strengthens a catabolism of proteins in muscular 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 causing development of a hyperglycemia. Detains sodium and water in an organism, increasing at the same time the volume of the circulating blood and increasing the arterial pressure (antishock action).

Stimulates potassium removal, reduces absorption of calcium from a digestive tract, 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 an injection site. To 90% of drug 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 drug (to 67% collapses in the placenta to inactive metabolites) gets. Metabolites of a hydrocortisone are removed preferential by kidneys.

Pharmaceutical characteristics

Main physical and chemical properties: drug after agitation within 2 minutes represents suspension of color, white or white with a yellowish shade, which when standing accumulates, with a specific smell.

Indications to use:

Osteoarthritis, different monoarthroses (knee, elbow, coxofemoral joints), pseudorheumatism and arthritises of other origin (except for tubercular and gonorrheal arthritises). Humeroscapular periarthritis, bursitis, epicondylitis, tendovaginitis. Before ankylotic joint operation. As local addition to system corticosteroid therapy.

Route of administration and doses:

Before the use contents of ampoules are stirred up before formation of homogeneous suspension.

To adults and children 14 years are more senior: the single dose depends on the size of a joint and on disease severity – 5-50 mg of a hydrocortisone vnutrisustavno and periartikulyarno.

For 24 hours adults can carry out 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.

The medical effect at intra joint administration of drug occurs for 6-24 hours and remains from several days to several weeks. Repeated administration of drug is possible in 3 weeks.

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

Drug cannot be used for system corticosteroid therapy.

Features of use:

Use during pregnancy or feeding by a breast

Purpose of drug in the I trimester of pregnancy is contraindicated. Further drug is appointed only when the advantage of use for mother exceeds risk of negative effects for a fruit.

Corticosteroids are excreted with milk therefore during treatment feeding by a breast should be stopped.

Children

For treatment of children in a growth period drug is used only according to absolute indications. Drug contains benzyl alcohol therefore it is not recommended to children under 2 years for use.

 

Vnutrisustavno the entered corticosteroid can increase a possibility of resuming of inflammatory processes. Drug can provoke bacterial infection of a joint therefore Hydrocortisoni acetas can be entered only in aseptic conditions.

During treatment it is impossible to carry out by a hydrocortisone vaccination in connection with high risk of development of neurologic complications and oppressions of antibody formation.

During therapy by corticosteroids ability of an organism to localization of an infection can decrease.

Introduction of the standard and high doses of corticosteroids can cause increase in arterial pressure, strengthen a delay of sodium and water in an organism and to stimulate release of potassium from an organism. All corticosteroids strengthen removal of calcium from an organism.

At the latent tuberculosis it is possible to apply only together with tuberculostats.

At infectious diseases to apply with care and only jointly with specific antibacterial therapy.

During performing therapy by the Hydrocortisone acetate it is necessary to adjust a dose of peroral antidiabetic means and anticoagulants.

It is necessary to control electrolytic exchange in an organism at simultaneous use of diuretic means.

At prolonged use it is necessary to appoint in addition potassium drugs for prevention of a hypopotassemia.

At children's and teenage age it is necessary to use drug shorter course in minimum effective dosage because of a possibility of a growth inhibition.

During treatment it is regularly desirable to measure arterial pressure, to carry out the analysis of urine and a calla.

It is necessary to finish treatment with a gradual dose decline of drug and the solution of a question of need of use of AKTG (skin test).

At combined use with salicylates if the corticosteroid dose decreases, it is necessary to reduce a salicylate dose at the same time.

It is necessary to appoint carefully drug to patients with psychosis in the anamnesis, a diabetes mellitus (including in the family anamnesis), arterial hypertension, glaucoma, a steroid myopathy, epilepsy, tuberculosis in the anamnesis.

Ability to influence speed of response at control of motor transport or work with other mechanisms

 

There are no data which would confirm that use of drug influences speed of response at control of motor transport or work with other mechanisms. In case during treatment drug observes dizziness, spasms, etc., it is necessary to refrain from control of vehicles and performance of work which require attention.

Side effects:

At intra joint use of steroid drug can be one of by-effects swelled or pain in the place of an injection. Usually this phenomenon passes independently in several hours after introduction.

Against the background of prolonged and uncontrollable use of suspension of Hydrocortisoni acetas side reactions which are typical for all corticosteroids (systemic action) can be observed.

Disturbances of water and electrolytic balance: a delay of sodium and liquid in an organism; hypopotassemia, gipokaliyemichesky alkalosis; heart failure, arterial hypertension.

Disturbances from a musculoskeletal system: aseptic necrosis; steroid myopathy; osteoporosis; a growth inhibition at children.

Disturbances from digestive tract: a round ulcer with possible perforation and bleeding; gastric bleeding; pancreatitis; esophagitis; the increased appetite, nausea, vomiting.

Dermatological disturbances: hirsutism, hypopigmentation, delay of healing of wounds, atrophy of skin, striya, eels, skin itch, folliculitis, irritation, dryness, thinning and hypersensitivity of skin, expansion of skin capillaries.

Metabolic disturbances: negative nitrogenous balance.

Neurologic frustration: increase in intracranial pressure with a papilledema (papillary stasis sign); mental disorders; spasms, dizziness, headache, sleeplessness, excitement, euphoria, depression.

Endocrine disturbances: oppression of function of adrenal glands, especially at prolonged use or at use of high doses; Icenco-Cushing syndrome; decrease in tolerance to carbohydrates and increase in need for insulin or in peroral hypoglycemic drugs; a delay of sexual development at children, disturbance of a menstrual cycle.

Ophthalmologic disturbances: increase in intraocular pressure, glaucoma; exophthalmos; helcoma; the probability of development of a cataract in children increases.

Others: opportunistic infections, exacerbation of latent tuberculosis, leukocytosis, hypersensitivity, thromboembolism, feeling sick; allergic reactions are in some cases possible.

Withdrawal: fervescence, mialgiya, arthralgia, oppression of function of bark of adrenal glands.

At advanced age side effects of corticosteroids can be shown more intensively.

Interaction with other medicines:

It is necessary to avoid a combination with barbiturates at treatment of patients who have Addison's disease (there can come crisis).

It is necessary to be careful at co-administration:
with barbiturates, phenylbutazone, Phenytoinum and rifampicin (the effect of corticosteroids can decrease);
with peroral antidiabetic means (it is necessary to change their dose taking into account hyper glycemic effect of corticosteroids);
with anticoagulants (strengthening or easing of anticoagulating effect);
with salicylates (can reduce the level of salicylates in plasma, arise the concealed gastrointestinal hemorrhage or a possibility of emergence of ulcers);
with Amphotericinum, diuretics, theophylline, cardiac glycosides (the risk of development of a hypopotassemia increases);
with oral contraceptives (concentration of corticosteroids in blood increases);
with anti-hypertensive means (corticosteroids reduce efficiency of anti-hypertensive means);
with mefipristony (efficiency of corticosteroids decreases).

Contraindications:

Hypersensitivity to drug components. Intra joint infection. I trimester of pregnancy. Infectious diseases and sepsis without antibacterial therapy. Icenco-Cushing syndrome. Treatment of an Achilles tendon. Vaccination period. Round ulcer of a stomach and duodenum. Osteoporosis. Tendency to a thromboembolism. Renal failure. Arterial hypertension of a heavy current. Herpes simplex. Chicken pox. Active tuberculosis. Syphilis.

Overdose:

There is no characteristic clinical syndrome at overdose of Hydrocortisoni acetas.

At overdose strengthening of both local, and system side reactions can be observed.

Treatment: symptomatic. There is no specific antidote. At considerable overdose dialysis use is possible.

Storage conditions:

Period of validity. 3 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature not above 15 °C. Freezing is not allowed. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule. On 10 ampoules in a pack.