Hydrocortisone

General characteristics. Structure:

Active agents: Hydrocortisoni acetas - 125 mg, lidocaine a hydrochloride monohydrate - 26,66 mg (it is equivalent to lidocaine to a hydrochloride of 25 mg).

Excipients: пропилпарагидроксибензоат; methylparahydroxybenzoate; sodium chloride; sodium phosphate; sodium dihydrophosphate; povidone; polysorbate 80; N, N-dimethylacetamide; water for injections.

Pharmacological properties:

Pharmacodynamics. Hydrocortisoni acetas - glucocorticosteroid means. Has antiinflammatory effect. The hydrocortisone slows down release of cytokines (interleykin and interferon) from lymphocytes and macrophages, release by eosinophils of mediators of an inflammation oppresses, reduces intensity of metabolism of arachidonic acid and synthesis of prostaglandins. Activates steroid receptors, induces formation of the lipokortin having antiedematous activity. Reduces inflammatory cellular infiltration, interferes with migration of leukocytes and lymphocytes to places of an inflammation. In high doses slows down development of adenoid and connecting tissue. Reducing quantity of mast cells, reduces formation of hyaluronic acid; suppresses hyaluronidase, promotes decrease in permeability of capillaries. It is intended for intramuscular, inside - and circumarticular introduction, for the purpose of rendering systemic or local antiinflammatory action. At intra joint introduction the medical effect occurs during 6-24 h and to last several days or weeks.
Lidocaine - mestnoanesteziruyushchy means with membrane stabilizing effect, in a short space of time has the anesthetizing effect.

Pharmacokinetics. At intra joint and circumarticular introduction the hydrocortisone gets into a system blood stream. Communication with proteins - more than 90%. It is metabolized in a liver in a tetrahydrocortisone and tetrahydrocortisol which are removed by kidneys in the conjugated form. Gets through a placental barrier.
Lidocaine is well soaked up, has high affinity with proteins of plasma.
It is metabolized mainly in a liver. An elimination half-life - 1-2 h.
Lidocaine gets into breast milk, through placental and hematoencephalic barriers.

Indications to use:

The rheumatic diseases which are followed by arthritises including osteoarthrosis in the presence of a synovitis (except for tubercular, gonorrheal, purulent and other infectious arthritises); pseudorheumatism, humeroscapular periarthritis, bursitis, epicondylitis, tendovaginitis.

Route of administration and doses:

Intra-and periartikulyarno. In one day it is possible to enter the Hydrocortisone Richter no more than into 3 joints. The repeated injection is possible at observance of a 3 weeks interval. Introduction of the Hydrocortisone Richter directly in a joint can exert adverse impact on a hyaline cartilage therefore the same joint it is possible to treat no more than 3 times a year.
At a tendinitis the injection needs to be done in a sinew vagina - directly it is impossible to enter into a sinew.

Adult: depending on the size of a joint and disease severity, 5-50 mg intra-and periartikulyarno.
To children: 5-30 mg/days, having divided into several doses. A single dose at periartikulyarny introduction to children aged from 3 months till 1 year: 25 mg; from 1 year to 6 years: 25-50 mg; from 6 to 14 years: 50-75 mg.

Features of use:

The injection is entered at observance of rules of antiseptics and an asepsis in order to avoid development of bacterial infection.
During treatment by the Hydrocortisone Richter, especially high doses, any vaccination is contraindicated as there can be an insufficient synthesis of antibodies.
During treatment the Hydrocortisone Richter recommends a diet with restriction of sodium and the increased content of potassium, providing enough protein in food.
It is regularly necessary to control the arterial pressure, concentration of glucose in blood, coagulability of blood, a diuresis and body weight of the patient.
Relative adrenal insufficiency can proceed within several months after cancellation of a hydrocortisone therefore in conditions of the raised stress it is necessary to resume hormonal therapy with co-administration of mineralokortikosteroid and salts.
Children whose mothers received a hydrocortisone during pregnancy are subject to careful observation for the purpose of identification of signs of adrenal insufficiency.
At a latent form of tuberculosis and in the period of a bend of tuberkulinovy tests careful control of a condition of the patient and, in case of need, performing chemoprophylaxis is necessary.
The hydrocortisone Richter slows down growth and development of children and teenagers.
It is recommended to appoint drug in the smallest therapeutic doses and, whenever possible, during short term.

Side effects:

From endocrine system: decrease in tolerance to glucose and increase in need for hypoglycemic drug; manifestation of a latent diabetes mellitus; steroid diabetes mellitus. At prolonged treatment - oppression of function of adrenal glands; Icenco-Cushing syndrome; a growth inhibition at children and teenagers.

From digestive tract: nausea; vomiting; pancreatitis; round ulcer; esophagitis; bleedings and perforation of digestive tract; increase in appetite; meteorism; hiccups; in rare instances - increase in activity of transaminases of a liver and an alkaline phosphatase.

From cardiovascular system: lidocaine can cause conductivity disturbance (in the doses exceeding therapeutic), peripheral vasodilation; at high doses of a hydrocortisone: increase in arterial pressure; hypopotassemia and changes of an ECG, inherent for it; thromboembolism; heart failure.

From a nervous system: sleeplessness, irritability, concern, excitement, euphoria, epileptiform spasms; mental disorders; delirium; disorientation; hallucinations; an exacerbation of maniac-depressive psychosis against the background of administration of drug; depression; paranoia; increase in intracranial pressure with a papilledema, dizziness; cerebellum pseudoneoplasm; headache.

From a metabolism: increase in body weight, negative nitrogenous balance, the strengthened sweating.

From an organ of sight: keratohelcosis; a back kapsulyarny cataract (is more probable at children); increase in intraocular pressure with possible injury of an optic nerve; consecutive bacterial, fungal, viral infections of eyes; trophic changes of a cornea; exophthalmos, glaucoma.

From a musculoskeletal system: delay of growth and processes of ossification at children (premature closing of epiphyseal regions of growth); osteoporosis; very seldom - pathological fractures of bones; aseptic necrosis of a head humeral and femur; rupture of sinews of muscles; steroid myopathy; decrease in muscle bulk; arthralgias.

The effects caused by mineralokortikoidny activity of drug: delay of liquid and sodium with formation of peripheral hypostases; hypernatremia; a hypopotassemia, arrhythmia, a mialgiya, a spasm of muscles, the increased weakness, fatigue.

From immune system: opportunistic infections, exacerbation of latent tuberculosis, hypersensitivity reaction; local and generalized: skin rash, itch; acute anaphylaxis; the slowed-down healing of wounds; tendency to development of a pyoderma and candidiases, an exacerbation of infections, especially at vaccination and simultaneous treatment by immunosuppressive means.

From skin and mucous covers: petechias; ecchymomas; hyper - or hypopigmentation; steroid eels; striya; folliculitis, hirsutism, teleangiectasia. Local reactions: swelled fabrics and pain in the place of an injection which spontaneously disappear several hours later, strengthening of pains in a joint at administration of drug in a joint, burning, numbness, paresthesia in an injection site, an atrophy of skin and hypodermic cellulose in an injection injection site (at accidental introduction to a deltoid muscle), it is rare - a necrosis of surrounding fabrics, formation of hems in the place of an injection.

Others: indisposition, syndrome of "cancellation" (high temperature of a body, mialgiya, arthralgia, adrenal insufficiency); leukocyturia, leukocytosis.
At elderly patients the risk of development of side reactions is higher.
At prolonged treatment and use of high doses of a hydrocortisone and lidocaine development of systemic side effects is possible.

Interaction with other medicines:

The hydrocortisone increases toxicity of cardiac glycosides (because of the arising hypopotassemia the risk of development of arrhythmias increases).
Accelerates removal of acetylsalicylic acid, reduces the maintenance of its metabolites in blood (at its cancellation concentration of salicylates in blood increases and the risk of development of by-effects increases).
At simultaneous use with live (attenuirovanny) vaccines and against the background of other types of immunizations increases risk of activation of viruses and development of infections.
Increases metabolism of an isoniazid, meksiletin (especially at "bystry acetylizers") that leads to decrease in their plasma concentration.
Increases risk of development of a hepatotoxic action of paracetamol (induction of "hepatic" enzymes and formation of a toxic metabolite of paracetamol).
The hypopotassemia caused by a hydrocortisone can increase expressiveness and duration of muscular blockade against the background of muscle relaxants.
In high doses reduces effect of a somatropin.
The hydrocortisone reduces effect of peroral hypoglycemic medicines.
Strengthens anticoagulating action of derivatives of coumarin.
Weakens influence of vitamin D on absorption of calcium in an intestines gleam.
Ketokonazol (reduces clearance) increases toxicity of a hydrocortisone.
Thiazide diuretics, karboangidraza inhibitors, other glucocorticoids and Amphotericinum In increase risk of development of a hypopotassemia, sodium - the containing medicines - hypostases and increase in arterial pressure.
Non-steroidal anti-inflammatory drugs and ethanol increase danger of development of an ulceration of a mucous membrane of the digestive tract (DT) and bleeding. In a combination with nonsteroid antiinflammatory means for treatment of arthritis the hydrocortisone dose decline because of summation of therapeutic effect is possible.
Indometacin, forcing out a hydrocortisone from communication with albumine, increases risk of development of its side effects.
Amphotericinum In and inhibitors of a karboangidraza increase risk of development of osteoporosis.
Therapeutic action of a hydrocortisone decreases under the influence of Phenytoinum, barbiturates, ephedrine, theophylline, rifampicin and other inductors of "hepatic" microsomal enzymes (increase in speed of metabolism).
Mitotanum and other inhibitors of synthesis of steroids can cause need of increase in a dose of a hydrocortisone.
The clearance of a hydrocortisone increases against the background of drugs of hormones of a thyroid gland.
Immunodepressants increase risk of development of infections and a lymphoma or other limfoproliferativny disturbances connected with a virus Epstein - Barrel.
Estrogen (including oral estrogensoderzhashchy contraceptives) reduces clearance of a hydrocortisone, extends T1/2 and their therapeutic and toxic effects.
Emergence of a hirsutism and eels is promoted by simultaneous use of a hydrocortisone and steroid hormonal medicines - androgens, estrogen, anabolic steroids, oral contraceptives.
Tricyclic antidepressants can increase expressiveness of the depression caused by reception of a hydrocortisone (are not shown for therapy of these side effects).
The risk of development of a cataract increases at use against the background of other glucocorticoids, antipsychotic medicines (neuroleptics), Carbutamidum and Azathioprinum.
Co-administration with nitrates, m-holinoblokatorami (including antihistaminic medicines, tricyclic antidepressants), promotes increase in intraocular pressure.

Contraindications:

Hypersensitivity to any of drug components; the infected joint; Icenco-Cushing syndrome; tendency to a thrombogenesis; I trimester of pregnancy; a system infection without specific treatment; Achilles tendon diseases.
Intra joint introduction is contraindicated at the postponed arthroplasty, pathological bleeding (endogenous or caused by anticoagulants), an intra joint fracture of bones, infectious (septic) arthritis and a periartikulyarny infection (including in the anamnesis), the general infectious disease, the expressed circumarticular osteoporosis, an osteoarthrosis without synovitis (so-called to Sukhoi a joint), an unstable joint, an aseptic necrosis of the epiphysis of bones creating a joint, the expressed bone destruction and deformation of a joint (considerable narrowing of a joint crack, an anchylosis).

With care: peptic ulcer of a stomach and duodenum; herpes simplex, including eye (possibility of perforation of a cornea of an eye); arterial hypertension; a diabetes mellitus, including in the family anamnesis; osteoporosis (the risk of osteoporosis increases in a postmenopause); chronic psychotic reactions; tuberculosis in the anamnesis; glaucoma; steroid myopathy; epilepsy; measles; chronic heart failure; advanced age (it is more than 65 years), pregnancy (the II-III trimesters), the lactation period.

Pregnancy and period of a lactation
Purpose of the Hydrocortisone Richter is contraindicated to pregnant women in the first trimester due to the lack of sufficient data on safety of drug in this group. In the second and third trimesters of pregnancy and to the feeding women reception of the Hydrocortisone Richter is possible when the estimated advantage for mother exceeds potential risk for a fruit or the child.
Use of the Hydrocortisone Richter in the period of a lactation can lead to dysfunction of adrenal glands and lag in development of babies since the hydrocortisone and lidocaine get into breast milk.

Overdose:

Exceeding of a dose or long introduction of the Hydrocortisone Richter can lead to oppression of own products of glucocorticoids, increase in arterial pressure, ulcer bleedings of a digestive tract, a sharpening of persistent infections, arthralgias, development of a syndrome of Itsenko-Cushing. There is no specific antidote. Treatment - symptomatic.

Storage conditions:

To store at a temperature from 15 °C to 30 °C in the place protected from light. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Suspension for intra joint and circumarticular introduction, 25 mg +5mg/ml:
5 ml of drug in a colourless glass bottle. 1 bottle together with the application instruction in a cardboard pack.