Hydrocortisone - instructions for use, dose, side effects, contraindications

Excipients: propylene glycol 0.2 ml, sorbitol 20 mg, povidone 10 mg, sodium chloride 1.4 mg, alcohol gasoline 0.015 ml, water for injection up to 1 ml.

Description:The drug after shaking for 2 minutes is a suspension of white or white with a yellowish hue, with a specific odor that settles on standing.

Pharmacotherapeutic group:Glucocorticosteroid

ATX: & nbsp

S.01.B.A.02 Hydrocortisone

H.02.A.B.09 Hydrocortisone

D.07.A.A.02 Hydrocortisone

Pharmacodynamics:Hydrocortisone belongs to the group of glucocorticosteroids of natural origin. Has anti-inflammatory, antiallergic and immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

Interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids (GCS) are present in all tissues,especially a lot of them in the liver) with the formation of a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells).

Protein metabolism: reduces the number of globulins in the plasma, increases the synthesis of albumins in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs predominantly in the region shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increased intake of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and synthesis aminotransferase (activation of gluconeogenesis); promotes the development of hyperglycemia. Water-electrolyte., Exchange: delays Na + and water in the body, stimulates derivation of K + (miMr.euralocorticoid activity), decreases the absorption of Ca²⁺ of gastrointestinal tract, causes "washing away" of calcium from the bones and increasing its renal excretion, reduces the mineralization of bone tissue.

The anti-inflammatory effect is associated with the inhibition of the release of mediators of inflammation by zosinophils and mast cells; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. It works on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin oppresses phospholipase A2, inhibits the liberation of arachidonic acid. It inhibits, biosynthesis, endoperexides, leukotrienes, promoting inflammation, allergies, etc.), the synthesis of "pro-inflammatory cytokines" (interleukin 1, tumor necrosis factor alpha, ); increases the resistance of the cell membrane to the action of various damaging factors.

Immunosuppressive effect is caused by induced lymphoid tissue involution, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, 2, gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies.

The antiallergic effect develops as a result of a decrease in: synthesis, and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in the number of circulating basophils, T- and B-lymphocytes, mast cells, suppression of lymphoid and connective tissue, reducing the sensitivity of effector cells to mediators, allergies, inhibition of antibody formation, changes in the body's immune response.

In obstructive airway diseases, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of the degree of edema of the mucous membranes, a decrease in eosinophilic infiltration submucosal layer of the epithelium of the bronchi and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.

Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS. It inhibits joint tissue reaction during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics:Relatively slowly absorbed from the injection site. Communication with blood proteins - up to 90% (from transcortin - 80% and albumin - 10%), about 10%, is in the form of "free fraction metabolism in the liver minor amount of the drug penetrates through the placenta (up to 67% destroyed in itself.. placenta to inactive metabolites) in contrast to synthetic derivatives.The hydrocortisone metabolites are excreted mainly through the kidneys.

Indications:

- Endocrine diseases: acute insufficiency, adrenal cortex, congenital hyperplasia adrenal cortex, subacute, thyroiditis, thyrotoxic crisis;

- shock, resistant to standard therapy; anaphylactic shock;

- edema of the brain (with a brain tumor, head injury, Neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation damage);

- asthmatic status; severe bronchospasm (exacerbation of bronchial asthma chronic obstructive bronchitis);

- severe allergic reactions;

- rheumatic diseases;

- systemic connective tissue diseases;

- acute severe dermatoses;

- Malignant diseases: palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; hypercalcemia in patients with malignant tumors;

- Blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;

- severe infectious diseases (in combination with antibiotics);

- Intra-articular and intrasynovial administration - diseases of the musculoskeletal system: non-infectious arthritis, synovitis in osteoarthritis, bursitis, epicondylitis, tendovaginitis, inflammatory contracture of joints.

Contraindications:

For short-term use according to vital indications, the only contraindication is hypersensitivity to hydrocortisone acetate and the components of the drug.

In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.

Carefully:

With caution, the drug should be administered in the following conditions and conditions:

- Diseases of the gastrointestinal tract - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing threat, diverticulitis.

Parasitic and infectious diseases - viral, fungal or - bacterial (current or recent, including recent contact with the patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amoebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis. Application with severe infectious diseases is permissible only against the background of specific therapy.

- Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination.

- Immunodeficiency conditions (including AIDS, or HIV infection).

- Diseases of the cardiovascular system (including the recently transferred heart attack myocardium - in patients with acute and subacute myocardial infarction is possible the spread of the foci of necrosis, slowing the formation of scar tissue and, as a consequence, rupture of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia.

- Endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV c).

- Severe chronic renal and / or hepatic insufficiency, nefrourolithiasis.

- Hypoalbuminemia and conditions predisposing to its occurrence.

- Systemic osteoporosis, myasthenia gravis gravis, acute psychosis, poliomyelitis (except / forms of bulbar encephalitis), open and closed angle glaucoma.

- Pregnancy is the period of breastfeeding.

- For intraarticular administration: the general severe condition of the patient, Ineffectiveness (or short-term) of the previous two taking into account the individual properties of the GCS used).

Pregnancy and lactation:When pregnancy (especially in the first trimester) is used only for life indications. Since glucocorticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Dosing and Administration:

Before use, the contents of the ampoules are shaken until a homogeneous suspension is formed. Intramuscularly injected deep into the gluteus muscle at a dose of 50-300 mg to 1000 -1500 mg per day. In acute, life-threatening conditions, 100-150 mg is administered every 4 hours for 48 hours; then every 8-12 hours. Children - every 4 hours 1-2 mg / kg, the optimal daily dose of 6-9 mg / kg.

In the joint cavity, 5-25 mg 0.1-1 ml (depending on the size of the joint) are administered 1 time per week, 3-5 injections per course). The drug begins 6 to 25 hours after the administration and lasts for several days or weeks.

Side effects:

The frequency of development and severity of side effects depends on the duration of application, the amount of dose used and the possibility of observing circadian rhythm. administration of hydrocortisone.

From the endocrine system: reduction of glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, oppression of the adrenal gland function, Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delayed sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, steroid stomach ulcer andduodenal ulcer, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal wall, increased or decreased appetite, digestive disorders, flatulence, hiccups. In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

From the cardiovascular system: arrhythmia bradycardia (up to cardiac arrest); development (in predisposed patients) or - increased severity heart failure, changes in the electrocardiogram, characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the "formation" of scar tissue, which can lead to a rupture of the cardiac muscle.

From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or restlessness, insomnia, dizziness, vertigo, pseudotumor, cerebral palsy, headache, convulsions.

Co side of the senses: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to development - secondary bacterial fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos, sudden loss of vision (when parenteral administration in the head, neck, nasal concha, scalp it is possible to deposit crystals of the drug in the vessels of the eye).

From the side of metabolism: increased excretion of calcium, hypocalcemia, increase in body weight, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticoid activity: fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: Deceleration of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological fractures of bones, aseptic! necrosis of the head of the humeral and femoral head bones), rupture of muscle tendons, steroid myopathy, reduction of muscle mass (atrophy), with intra-articular injection - increased pain in the joint.

From the skin and mucous membranes: delayed healing of wounds, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, acne, striae, propensity to develop pyoderma and candidiasis.

Allergic reactions: skin rash, itching, anaphylactic shock.

Other: development - or exacerbation of infections (the emergence of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:It is possible to strengthen the above described side effects. It is necessary to reduce the dose of hydrocortisone. Treatment is symptomatic.

Interaction:Simultaneous administration of hydrocortisone with:

inducers of "hepatic" microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;

diuretics (especially "thiazide" and inhibitors of carbonic anhydrase), and amphotericin B - can lead to increased excretion of K + from the body and an increased risk of developing heart failure;

with sodium-containing preparations - to development of edema and increased blood pressure;

cardiac glycosides - their tolerance is worsened and the likelihood of developing ventricular extrasystole (due to induced hypokalemia) increases; indirect anticoagulants - weakens (less intensifies) their effect (dose adjustment is required); anticoagulants and thrombolytics - Increased risk of bleeding from ulcers in the gastrointestinal tract;

ethanol and non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding (in combination with NSAIDs in the treatment of arthritis, a reduction in the dose of glucocorticosteroids due to the summation of the therapeutic effect);

paracetamol - The risk of hepatotoxicity increases (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol);

acetylsalicylic acid - accelerates its excretion and reduces the concentration in the blood (with the abolition of hydrocortisone, the level of salicylates in the blood increases and increases _;risk of side effects);

insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness is reduced;

vitamin D - decreases its effect on the absorption of Ca²⁺ in the intestine;

somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration;

- M-holinoblokatorami - (including antihistamines and tricyclic antidepressants) and nitrates - promotes increased intraocular pressure;
isoniazid and mexiletine - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations;

Inhibitors of carbonic anhydrase and, "loop" diuretics may increase the risk of osteoporosis.

- Indomethacin displacing hydrocortisone from association with albumin, increases the risk development of its side effects.

AKTG strengthens the action of hydrocortisone.

Ergocalciferol, and parathyroid hormone. prevent the development of osteopathy, caused by hydrocortisone.

- Cyclosporine and ketoconazole, slowing the metabolism of hidrocortisone, may in some cases increase its toxicity. Simultaneous appointment of androgens and steroid anabolic drugs with hydrocortisone promotes the development of peripheral edema andhirsutism, the appearance of blackheads.

Estrogens and oral estrogen-containing contraceptives lower the clearance hydrocortisone, which may be accompanied by an increase in the severity of its action.

Mitotane and other inhibitors of adrenal cortex function may necessitate an increase in the dose of hydrocortisone.

With simultaneous use with live, antiviral vaccines against the background of other types of immunization increases the risk of virus activation and the development of infections.

Antipsychotic drugs (antipsychotics) - and azathioprine increase the risk of developing cataract in the appointment of hydrocortisone.

With simultaneous use with antithyroid drugs is reduced, and with thyroid hormones - increases the clearance of hydrocortisone.

Special instructions:During treatment with hydrocortisone (especially long-term) it is necessary to observe the oculist, control blood pressure, condition of water-electrolyte balance, as well as pictures of peripheral blood and blood glucose level.

In order to reduce side effects, antacids can be prescribed, as well as increased intake of K⁺ in the body (diet, potassium preparations). Food should be rich in proteins, vitamins,with restriction of the maintenance of fats; carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may enhance existing emotional instability or psychotic violations. When referring to a psychosis in an anamnesis hydrocortisone in high doses prescribed under the strict supervision of a doctor.

With caution should be used for acute and subacute myocardial infarction, it is possible to spread a foci of necrosis, slow the formation of scar tissue and rupture of the heart muscle.

In stressful situations during maintenance treatment (eg, surgical surgery, trauma, or infectious diseases) should adjust the dose of the drug due to increased demand for glucocorticosteroids.

In case of sudden cancellation, especially in case of prior application of high doses, the syndrome of "cancellation" (anorexia, nausea, blocking, generalized musculoskeletal pain, general weakness), as well as aggravation of the disease, about which it was prescribed hydrocortisone.

- During treatment with hydrocortisone, vaccination should not be performed due to a decrease in its effectiveness (immune response).

Assigning with intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously perform antibiotic treatment of bactericidal action.

Children during prolonged hydrocortisone treatment need careful monitoring of the dynamics of growth and development. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.

As a result, insufficiently expressed mineralocorticoid effect for replacement therapy for adrenal insufficiency hydrocortisone used in combination with mineralocorticoids. Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.

An x-ray control of the osteoarticular system (images of the spine, hands) is shown.

Hydrocortisone in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which can have diagnostic value.

Hydrocortisone increases the metabolites content of 11- and 17-oxyketocorticosteroids.

Effect on the ability to drive transp. cf. and fur:Not described.

Form release / dosage:

Suspension for intramuscular and intraarticular administration.

Packaging:

2 ml per ampoule with or without a ring ring.

For 5 or 10 ampoules together with instructions for medical, use and knife an ampoule ceramic or a cutting ceramic disc is placed in a pack of cardboard with corrugated liners.

Or 5 ampoules (with a break ring) are put into the blister of a polymer film. For 1 or 2 blisters with ampoules, together with instructions for medical use, put in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 15 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N016113 / 01

Date of registration:16.10.2009 / 09.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:FARMAK, JSC FARMAK, JSC Ukraine

Manufacturer: & nbsp

FARMAK, JSC Ukraine

Information update date: & nbsp04.04.2017

Illustrated instructions

Instructions

Hydrocortisone (Hydrocortisone)