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

Clinical and pharmacological group: & nbsp

Included in the formulation

pills inwards

АТХ:

H.02.A.B.10 Cortisone

Pharmacodynamics:Interaction with intracellular glucocorticoid receptors - the formation of dimers of the glucocorticoid-glucocorticoid receptor complex (release of the receptor from the bonds with heat shock proteins 70 and 90 and immunophilin). Penetration of the activated receptor into the nucleus, binding to glucocorticoid-sensitive regulatory elements of DNA - a specific effect on gene expression (activation and suppression). Interaction with other protein transcription factors, including NFκB and AP-1, regulating the expression of many proteins of the immune system, which leads to suppression of the expression of genes encoding some cytokines, collagenase and stromelysins.

Pharmacokinetics:

Absorption is rapid and complete in the upper parts of the jejunum, slowing the rate of absorption with food. Relationship with plasma proteins 90%. Biotransformation in the liver to the active metabolite - hydrocortisone (11β-hydroxysteroid dehydrogenase type 1). Half-life ~ 1.5 hours. Elimination of metabolites by the kidneys.

Indications:

Chronic adrenal insufficiency (Addison's disease, hypokorticism after bilateral total adrenalectomy, hypopituitarism with secondary hypocorticism), congenital dysfunction of the adrenal cortex - in combination with mineralocorticoids.

ICD-10

IV.E70-E90.E89.3 Hypopituitarism, which arose after medical procedures

IV.E20-E35.E23.0 Hypopituitarism

XII.L60-L75.L64.8 Other androgenetic alopecia

IV.E70-E90.E89.6 Hypofunction of the adrenal cortex (medulla), which arose after medical procedures

IV.E20-E35.E27.4 Other and unspecified adrenocortical insufficiency

IV.E20-E35.E27.3 Medication adrenocortical insufficiency

IV.E20-E35.E27.1 Primary insufficiency of the adrenal cortex

Contraindications:

Hypersensitivity (for short-term use according to vital indications is the only contraindication). Parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, including the recent contact with the patient) - herpes simplex, herpes zoster (viremicheskaya phase), chicken pox, measles; amoebiasis, strongyloidiasis (or suspected); systemic mycosis, tuberculosis. The vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection). 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 the threat of perforation or abscess formation, diverticulitis. Diseases of the cardiovascular system, including the recently transferred myocardial infarction, decompensated chronic heart failure, severe arterial hypertension, hyperlipidemia. Endocrine diseases - diabetes (including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Cushing's disease. Tendency to thromboembolism, renal and / or hepatic insufficiency, nephrourolythiasis, hypoalbuminemia and conditions predisposing to its occurrence, myasthenia gravis, obesity (III-IV degree), poliomyelitis (with the exception of the form of bulbar encephalitis), open and closed angle glaucoma.

Carefully:

In patients with ulcerative colitis, with diverticulitis, newly created anastomosis of the intestine, peptic ulcer of the stomach and duodenum, renal failure, myasthenia gravis, arterial hypotension, diabetes mellitus, mental illness, hypoalbuminemia. With hypothyroidism, as well as with cirrhosis, the effect of cortisone can be enhanced.With initial emotional instability or psychotic tendencies, these phenomena can intensify.

When using cortisone in patients with herpes simplex cornea, one should keep in mind the possibility of perforation.

During treatment, it is necessary to monitor the intraocular pressure and the condition of the cornea. With sudden withdrawal of treatment, especially in the case of previous use in high doses, there is a so-called glucocorticosteroid cancellation syndrome (not due to hypocorticism): anorexia, nausea, blocking, generalized musculoskeletal pain, general weakness. After cancellation of cortisone within a few months, relative insufficiency of the adrenal cortex may persist. If during this period there are stressful situations, prescribe (for indications) for a time glucocorticosteroids, if necessary in combination with mineralocorticoids.

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

Pregnancy and lactation:

Category FDA - FROM.

Adequate and well-controlled studies in humans have not been conducted. In pharmacological doses can cause placental insufficiency, deficiency of fetal body weight, stillbirth. Teratogenic effect is not confirmed. Hormone replacement therapy does not adversely affect the fetus and the newborn. Studies in animals have revealed an increase in the frequency of cleft palate, placental insufficiency, spontaneous abortion and delayed intrauterine development of the fetus.

Penetrates into breast milk. Violations are not registered. The appointment of physiological or low pharmacological doses (equivalent to ~ 25 mg cortisone or 5 mg prednisone) does not cause abnormalities on the part of the child. The appointment of higher doses is not recommended due to possible violations on the part of the child (stunting, disruption of the production of its own glucocorticoids).

Dosing and Administration:

Inside, the initial dose is 100-200 mg in 2 divided doses. When the effect is achieved, the dose is gradually reduced to a maintenance dose (usually 25 mg per day). Higher doses for adults: single dose - 150 mg, daily - 300 mg. For children, the initial dose of 12.5-25 mg 2 times a day. Supportive doses are selected individually.

Side effects:

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

From the endocrine system: depression 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, increase in blood pressure, dysmenorrhea, amenorrhea, myasthenia, strias), delay in sexual development in children .

On the part of the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increase or decrease in appetite, flatulence, hiccough; in rare cases - increased activity of hepatic transaminases and alkaline phosphatase.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): arrhythmia, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased manifestation of heart failure, changes in ECG, 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 rupture of the heart muscle.

From the nervous system and sensory organs: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of cerebellum, headache, convulsions, posterior subcapsular cataract, increased intraocular pressure with possible damage to the visual nerve, a tendency to develop secondary bacterial, fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos.

From the side of metabolism: increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating. Effects due to 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: slowing the growth and processes of ossification in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and thigh bone), rupture of tendons, steroid myopathy, decrease in muscle mass (atrophy).

From the skin: delayed wound healing, petechiae, ecchymoses, skin thinning, hyper- or hypopigmentation, steroid acne, striae, propensity to develop pyoderma and candidiasis.

Allergic reactions: generalized (skin rash, itching, anaphylactic shock), local allergic reactions.

Others: development or exacerbation of infections (the appearance of this side effect is promoted by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

Overdose:

Symptoms: Nausea, vomiting, sleep disorders, euphoria, agitation, depression. With prolonged use in high doses - osteoporosis, fluid retention in the body, increased blood pressure and other signs of hypercorticism, including Itenko-Cushing syndrome, secondary adrenal insufficiency.

Treatment: against the background of a gradual discontinuation of the drug maintenance of vital functions, correction of electrolyte balance, antacids, phenothiazines, lithium preparations; with the syndrome of Itenko-Cushing - aminoglutethimide.

Interaction:

Alcohol, non-steroidal anti-inflammatory drugs - increased risk of bleeding (including hemorrhagic stroke) and ulceration of the gastric mucosa.

Aminoglutethimide - oppression of the adrenal glands (additional glucocorticoid administration is required).

Amphotericin B (parenterally), inhibitors of carbonic anhydrase - the risk of severe hypokalemia.

Antiglaucoma means - correction of the dose due to glaucocorticoids glaucoma.

Anticholinergics, especially atropine - risk of intraocular hypertension.

Acetazolamide - the risk of hypernatremia, edema, hypocalcemia (osteoporosis).

Anabolic steroids, androgens - the risk of edema, severe acne.

Antidepressants tricyclics - aggravation of steroid-dependent disorders of the psyche. Do not apply!

Anticoagulants indirect (coumarin and indanedione derivatives), anticoagulants direct, thrombolytics - risk of hemorrhagic stroke.

Antithyroid drugs, thyroid hormones - correction of the dose of glucocorticoids due to reduced clearance in hypothyroidism and increased - in the hyperthyroid state.

Asparaginase - increasing its toxic effects.

Vaccines, live viruses or other immunization - pharmacological (immunosuppressive) doses of glucocorticoids lead to stimulation of the replication of live viruses, an increased risk of developing viral diseases, a decrease in the formation of antibodies to the vaccine.

Diuretics - reduction of their natriuretic and diuretic effects, hypokalemia.

Inhibitors of acetylcholinesterase - a risk of severe weakness in myasthenia gravis (cancellation 24 hours before the start of glucocorticoid therapy).

Isoniazid, mexiletine - Increase in clearance of isoniazid, mexiletine, decrease in plasma concentration (dose adjustment).

Other immunosuppressants are the risk of infection.

Carbamazepine, ephedrine, phenobarbital, phenytoin, rifampicin - increased clearance of glucocorticoids.

Ketoconazole - reduced clearance of glucocorticoids (increased risk of side effects).

Special instructions:

The use in severe infectious diseases is permissible only against the background of specific therapy.

Instructions

Cortisone (Cortisonum)