Gidrokortizon (When ATH A07EA02)

When ATH:
A07EA02

Characteristic.

Hydrocortisone-hormone, secreted by the adrenal cortex, -glukokortikoid. In medical practice for systemic and topical use natural hydrocortisone or its esters (hydrocortisone acetate and hydrocortisone sodium hemisuccinate).

Hydrocortisone is white or almost white powder odourless, bitter taste. Solubility (mg / ml) at 25 °C: water 0,28; ethanol 15,0; methanol 6,2; acetone 9,3; chloroform 1,6; propylene glycol 12,7; stream — about 0,35. Soluble in concentrated sulfuric acid solution to produce a fluorescent intense green color. Molecular weight 362,47.

Hydrocortisone acetate is a synthetic steroid, White or white with a slightly yellowish white, crystalline powder;. Slightly hygroscopic. Solubility in water: 1 mg / 100ml, ethanol: 0,45 g / 100ml, methanol: 3,9 mg / ml, acetone: 1,1 mg / g, on the air: 0,15 mg / ml, chloroform: 1 g / 200ml, is highly soluble in dimethylformamide, dioxane solution. Molecular weight 404,50.

Hydrocortisone gemisuktinat sodium is a synthetic steroid, white or white with a slightly yellowish tinge porous mass or a hygroscopic amorphous white powder; solubility in water is about 500 mg / ml. Easily soluble in methanol, ethanol, it is soluble in chloroform. Molecular weight 484,51.

Hydrocortisone 17-butyrate is a molecular weight 432,55.

Pharmacological action.
Glucocorticoid, protivoshokovoe, anti-inflammatory, antiallergic, immunosuppressive, antiexudative, protivozudnoe.

Application.

For systemic use: severe allergic reactions, a severe attack of asthma, asthmatic condition, serum sickness, hypersensitivity reaction to the administration of drugs; urgent-hypotension, incl. orthostatic, collapse in Addison's disease, myocardial infarction, hemorrhagic stroke, Adams' disease, Coma in cerebral circulation disorders and inflammatory diseases of the brain, gipotireoidnaya and pechenochnaya coma, Multiple bleeding, acute liver failure in case of poisoning, laryngeal edema in allergic and inflammatory lesions, burns and injuries, poisoning vitamin D, strong acids, organophosphorus compounds, xininom, chlorine, post-transfusion complications, Mendelson's syndrome, snake bites and scorpion; anaphylactic, hemorrhagic, cardiogenic shock and traumatic; Endocrine diseases-watenausa-Frideriksena, primary or secondary adrenocortical insufficiency (Preferred natural cortisone and hydrocortisone, Synthetic analogs to be applied in conjunction with mineralocorticoids), congenital adrenal hyperplasia with loss of sodium, tireoidit; hypercalcemia, associated with cancer; rheumatic disease psoriatic, rheumatoid, juvenile and acute gouty arthritis, ankiloziruyushtiy spondylitis, acute and subacute bursitis, frozen shoulder, systemic lupus erythematosus, acute rheumatic carditis, dermatomyositis; sarkoidoz, Loffler's syndrome, berylliosis, fulminant or disseminated pulmonary tuberculosis, aspiration pneumonitis (in combination with a specific chemotherapy); idiopathic thrombocytopenic purpura in adults, autoimmune hemolytic anemia and congenital hypoplastic, erythroblastopenia, palliative therapy of leukemia and lymphomas in adults, acute leukemia in children; nephrotic syndrome without signs of uremia (to reduce proteinuria and inducing diuresis), severe exacerbations of ulcerative colitis and Crohn's disease, tuberculous meningitis with subarachnoid block, trichinosis with neurological manifestations and myocardial, acute manifestations of multiple sclerosis, disseminated lung cancer (complementary therapies), differential diagnosis of idiopathic and drug induced leukopenia.

Intra-articular and periarticular administration (gidrokortizona acetate): reactive synovitis (incl. when deforming osteoarthritis), rheumatoid arthritis, acute and subacute bursitis, acute gouty arthritis, epicondylitis, acute nonspecific tenosynovitis, carpal tunnel syndrome, post-traumatic osteoarthritis.

When applied to the skin: inflammatory and allergic skin disease etiology nemikrobnoy, incl. eczema, dermatitis (allergic, atopic, bullosa herpetiformis, exfoliative, seborrheal, contact); pruritic dermatoses, photodermatosis, anogenital itching, insect bites, pemphigus, erythroderma, psoriasis.

In ophthalmology (hydrocortisone acetate in the form of an eye ointment): allergic conjunctivitis, .Aloe, dermatitis century, keratit, recovery of corneal transparency and suppression of neovascularization after an keratitis, chemical and thermal burns (after complete epithelialization of the cornea); Irit, iridocyclitis, inflammation of the anterior segment, diffuse posterior uveitis and choroiditis, transferred ophtalmia, condition after surgery.

VC when keloids, localized hypertrophic, infiltrative, inflammatory lesions, flat lichen, psoriatic plaques, granuloma annulare, neurodermatitis, discoid lupus erythematosus, diabetic lipoid necrobiosis, alopecia areata, cystic tumors fascia and tendons.

Contraindications.

Hypersensitivity (for short-term use of the system for health is the only contraindication).

For systemic use. Systemic fungal infections, parasitic and infectious diseases of viral or bacterial origin (currently without appropriate chemotherapy or recently transferred, including the recent contact with a patient), incl. herpes simplex, herpes zoster (viremicheskaya form), enable vetryanaya, kor, ameʙiaz, strongiloidoz (or suspected), active and latent tuberculosis; immunodeficiency states (incl. AIDS or HIV infection), post-vaccination period, acute psychosis, severe hypertension, decompensated severe diabetes; gastric ulcer and duodenal ulcer in the acute stage, diverticulitis; the recent imposition of intestinal anastomoses; pepticheskaya ulcer; osteoporosis, myastenia gravis, pituitary basophilia, trombofilicescie state, renal failure, pregnancy, lactation.

For intra-articular and periarticular use: previous arthroplasty, status after surgery overlay intestinal anastomosis, pregnancy, breast-feeding.

When applied to the skin: Bacterial, viral and fungal skin disease, cutaneous manifestations of syphilis, lupus, skin tumors, violation of the integrity of the skin (ulcers, wounds), Rosacea, acne vulgaris, perioral dermatitis, post-vaccination period, pregnancy, breast-feeding.

For ophthalmic ointment: purulent, Viral, tuberculosis and fungal diseases of the eye, trachoma, pervichnaya glaucoma, violation of the integrity of the corneal epithelium; during vaccination, pregnancy, breast-feeding.

Pregnancy and breast-feeding.

The use of corticosteroids during pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety of not performed). Women of childbearing age should be warned about the potential risk to the fetus (Corticosteroids cross the placenta). It should be carefully monitored for newborns, whose mothers during pregnancy were treated with corticosteroids (adrenal insufficiency may develop in the fetus and newborn). Do not use often, large doses, over a long period of time.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Nursing women should stop any breastfeeding, or use of drugs, especially in high doses (corticosteroids penetrate into breast milk and could suppress growth, production of endogenous corticosteroids and cause undesirable effects in the newborn). When using the external forms of hydrocortisone medication should not be applied to the skin of the breast.

Side effects.

The frequency and severity of side effects depend on the way, the duration of use, the dosage used and the possibility of compliance circadian rhythm of destination PM.

Systemic effects

Metabolism: delay Na⁺ and body fluid, kaliopenia, hypokalemic alkalosis, negative nitrogen balance, giperglikemiâ, glycosuria, weight gain.

On the part of the endocrine system: secondary adrenal and hypothalamic-pituitary insufficiency (particularly during times of stress, such as illness, trauma, surgery); Cushing's syndrome; growth suppression in children; menstrual irregularities; reduced tolerance to carbohydrates; a manifestation of latent diabetes mellitus, increase the need for insulin or oral antidiabetic drugs in patients with diabetes.

Cardio-vascular system and blood (hematopoiesis, hemostasis): increased blood pressure, development (in predisposed patients) or increased severity of chronic heart failure, hypercoagulation, thromboembolism, ECG changes, typical of hypokalemia; in patients with acute and subacute myocardial infarction is necrosis lesion distribution, slowing the formation of scar tissue with a possible rupture of the heart muscle, occlusive disease, hematological changes.

On the part of the musculoskeletal system: muscular weakness, steroidnaya myopathy, loss of muscle mass, osteoporosis, a compression fracture of the spine, aseptic necrosis of the femoral head and the shoulder bones, pathological fractures of long bones, tendon rupture, especially Achilles.

From the digestive tract: steroid ulcer with possible perforation and hemorrhage, pancreatitis, flatulence, ulcerative esophagitis, indigestion, nausea, vomiting, increase / decrease of appetite; observed after treatment with corticosteroids increased ALT, AST and ALP in serum; Typically these changes are minor, not associated with any clinical syndrome and are reversible after discontinuation of treatment.

For the skin: atrophic band, acne, delayed wound healing, thinning of the skin, petechiae and ecchymosis, эritema, increased sweating.

From the nervous system and sensory organs: convulsions, increased intracranial pressure syndrome stagnant nipples optic nerve (pseudotumor of the brain — more often in children, usually after too rapid dose reduction, the symptoms — headache, deterioration of visual acuity or double vision); vertigo, headache, malaise, mental disorders; posterior subcapsular cataract formation, an increase in intraocular pressure, glaucoma; steroid exophthalmos.

Allergic reactions: Generalized (atopic dermatitis, hives, anaphylactic shock) and local.

Other: masking of symptoms of communicable diseases, withdrawal; reactions at the injection is burning, numbness, pain, paraesthesia and infitsirovanie, Hyper- or hypopigmentation, scarring; atrophy of the skin and subcutaneous tissue, sterile abscess.

If application to the skin: irritation, burning, xerosis, Local allergic reactions, incl. hyperemia, puffiness, itch; prolonged use, especially under impermeable dressings or large parts of the skin — systemic side effects; steroid acne, purpura, teleangiэktazii; development as a manifestation of Cushing resorptive action (In these cases, medication overturned); long-term use may also develop secondary infections of skin lesions, atrophic changes, hypertryhoza.

Eye ointment: allergic reactions, burning, injection sclera, increased intraocular pressure, exophthalmos; in violation of the integrity of the corneal epithelium may be a delay healing, and perforation of the cornea; with long-term use may develop steroid-glaucoma; frequent repeated courses of treatment can lead to the formation of posterior subcapsular cataracts; the accession of secondary infection.

Cooperation.

Barbiturates, antiepileptics and antihistamines reduce efficiency. NSAIDs increase the risk of ulceration in the gastrointestinal tract, paracetamol-gepatotoksicnosti. Hydrocortisone reduces blood salicylates (increases clearance) activity and antidiabetic agents, alters the effectiveness of anticoagulants. Cardiac glycosides and diuretics potentiate hypokalemia nekaliysberegayuschie, anabolic steroids — enhancing hydrophilic properties of fabrics. When combined with amfoteritinom in perhaps the dilatacionnogo heart failure and heart failure.

Dosing and Administration.

B /, / m, inside, intra-articular and periarticular, VC, locally. The route of administration and dosage regimen are selected individually depending on the nature and severity of the disease, patient's condition and response to therapy.

When emergencies for adults I / at an initial dose 100 mg (administered over 30 from); 500 mg (administered over 10 m), then repeated every 2-6 hours depending on the condition of the patient. In high doses prescribed only to stabilize the patient's condition, usually not more than 48-72 hours; if necessary longer glucocorticoid replacement therapy is suitable for other drugs with less mineralocorticoid activity.

/ M, in a dose of 125-250 mg/day.

Inside, during replacement therapy is 20-30 mg/day.

Vnutrisustavno and peryartykulyarno, adults-10-50 mg, depending on the size of the joint, and the severity of the lesion (in acute conditions — to 100 mg), repeat injections every 1-3 weeks (sometimes 3-5 days); Children designate smaller doses (However, the dose is largely determined by the severity of the effect and, than the age and body weight).

Locally. Forms for local use are applied in a thin layer on the skin in the affected areas 2-3 times a day. Duration of treatment averages 6-14 days (to 20 days). In chronic lihenizirovannyh, hypertrophic cutaneous manifestations in adults are used under occlusive dressings, alternate every 24-48 h.

Eye ointment is administered into the conjunctival sac of 2-3 times per day. The course of treatment is not more than 2 Sun (course may be extended by a physician).

Precautions.

During the period of treatment is not recommended vaccination (due to an immunosuppressive effect of hydrocortisone). Intra should be done under strict aseptic and antiseptic, and only after exclusion of infection in a joint. / M administration is made as deep as possible into the gluteal muscle to prevent the development of muscle atrophy. When long-term therapy is recommended control of the content of potassium in the blood (and his appointment) and regular ECG study. To prevent the development of secondary hypocorticoidism, caused by the cancellation of the treatment, the dose should be reduced gradually. Corticosteroids may mask some of the manifestations of infection, possible accession of new infections due to lower resistance. In the treatment of corticosteroid, or combination thereof with other drugs, inhibit cell, humoral immunity or neutrophil function may manifest various viral, Bacterial, Fungal, protozoal infections and worm infestation, flows previously latent. The risk of infection and the heavier its current increases in proportion to increase the dose.

The sudden discontinuation of treatment can cause the development of acute adrenal insufficiency; long-term use can not suddenly cancel the drug, the dose should be reduced gradually. With the sudden cancellation after long-term use may develop withdrawal, manifested by fever, myalgia and arthralgia, malaise. These symptoms may appear even in the case of, When not marked adrenal insufficiency.

Eye ointment. When, If after the application of eye ointment temporarily lost the clarity of vision, not recommended immediately after application to drive a car or operate complex mechanisms. During treatment should refrain from wearing contact lenses. Excessive and frequent use of eye ointment for a day or applying it in children is possible systemic effects of hydrocortisone (to remove the drug symptoms alone are). The use of other drugs in the form of eye drops, the time interval between their applications and use of the ointment should be at least 15 m. In applying the ointment more 2 weeks or a history of openly- or angle-closure glaucoma requires monitoring of intraocular pressure. The children have a higher probability of systemic effects of hydrocortisone, than in adults. In this connection it should apply the ointment in children, possibly, short courses (5-7 Days).

Forms for outdoor use. Children up 12 years, the drug is prescribed only under strict medical supervision. When using the ointment in children older 1 the year should be limited to the total duration of treatment and eliminating conditions, leading to increased resorption of the drug (Warming, fixing and occlusive dressings). Avoid contact with eyes ointment. With extreme caution should be used drug in the skin due to the possibility of side effects (teleangiэktazii, atrophy, perioral dermatitis), even after short-term use. For the prevention of infectious skin lesions hydrocortisone ointment recommended given in combination with antibacterial and antifungal agents.

Cooperation