Cortisone (Cortisone)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceCortisoneCortisone
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  • Cortisone
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
    • Dosage form: & nbsppills
    Composition:

    One tablet contains:

    active substance: cortisone acetate in terms of 100 % - 25 mg;

    Excipients: sucrose 34.5 mg, potato starch 40 mg, stearic acid 0.5 mg.

    Description:

    Tablets are white or white with a yellowish tint of color, flat-cylindrical, with a bevel.

    Pharmacotherapeutic group:Glucocorticosteroid
    ATX: & nbsp

    H.02.A.B.10   Cortisone

    Pharmacodynamics:

    Cortisone is a biologically inactive compound, which in the liver turns into a hydrocortisone, affecting the carbohydrate, lipid and protein metabolism. It has mineralocorticoid activity (sodium ion retention, fluid retention, elimination of potassium ions), but weaker than the true mineral ocorticoids.

    Promotes the accumulation of glycogen in the liver, increases the concentration of glucose in the blood, causes an increase in the excretion of nitrogen in the urine. Has anti-inflammatory, immunosuppressive and anti-allergic effect. The anti-inflammatory effect is caused by the inhibition of phospholipase A2, which leads to inhibition of the synthesis of prostaglandins, a decrease in the release of macrophage chemotactic factor, a decrease in the migration of macrophages and lymphocytes to the focus of inflammation, stabilization of lysosomal membranes and prevention of lysosomal enzymes.

    The immunosuppressive effects associated with decreased amount of immunocompetent cells, decrease the binding of immunoglobulins to cellular receptors, suppression of blast transformation of B-lymphocytes, reducing the amount of interleukins, cytokines, circulating immune complexes, complement fractions.

    Increases the excretion of calcium ions in the urine, activates the resorption of bone tissue, increases the activity of osteoclasts, reduces osteoblasts.

    Stimulating enzyme systems of the liver, activates gluconeogenesis. Having catabolic action, increases the breakdown of proteins. Lipolytic effect increases the concentration of fatty acids in the blood. Reduces the production of adrenocorticotropic hormone in the anterior pituitary gland (the principle of negative feedback), which determines suppression activity and subsequent atrophy of the adrenal cortex. The duration of action is 6-8 hours.

    Pharmacokinetics:

    Absorption is rapid and almost complete in the upper parts of the jejunum. Food somewhat slows down the absorption rate, but does not reduce its degree. Time to reach the maximum concentration in blood plasma - 0.5-1.5 h.It is first subjected to presystemic metabolism, at which conversion into an active metabolite - hydrocortisone. Connection with plasma proteins - 90 %. Rapidly metabolized in the liver, kidneys, peripheral tissues with the formation of inactive metabolites, which are excreted mainly by the kidneys. Half-life is about 1.5 hours.

    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 mineralocorticosteroids.

    For the rest of the indications, typical for glucocorticosteroids, is not currently applied.

    Contraindications:

    For short-term use according to "vital" indications, the only contraindication is hypersensitivity.

    Carefully:

    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; active or latent tuberculosis.Application in severe infectious diseases is permissible only against the background of specific antimicrobial therapy.

    Post-vaccination period (period of 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including acquired immunodeficiency syndrome (AIDS) or HIV infection). Diseases of the gastrointestinal tract: peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with threat of perforation or abscess formation, diverticulitis. Diseases of the cardiovascular system, incl. recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction, the spread of the necrosis foci, slowing the formation of scar tissue and, as a result, rupture of the heart muscle), decompensated chronic heart failure, hypertension, hyperlipidemia. Endocrine diseases-diabetes mellitus (including a violation of carbohydrate tolerance), obesity (III-IV century), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease.

    Severe chronic renal and / or hepatic insufficiency, nephrourolythiasis.

    Hypoalbuminemia and conditions predisposing to its occurrence.

    Systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open- and an angle-closure glaucoma.

    Pregnancy and lactation:

    Cortisone penetrates the placental barrier and into breast milk.

    During pregnancy (especially in the first trimester) the drug can be used only in cases where the benefit to the mother: exceeds the potential risk to the fetus. With prolonged therapy during pregnancy, the possibility of intrauterine growth retardation is not ruled out. Also, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

    If it is necessary to carry out treatment with the drug during breastfeeding, then breastfeeding should be discontinued.

    Dosing and Administration:

    Cortisone is administered orally.

    In chronic adrenal insufficiency, the usual average maintenance dose is 25-50 mg per day.The daily dose of the drug is prescribed in 2 divided doses, reproducing the daily rhythm of cortisone secretion - 2/3 of the daily dose in the morning (6-8 hours) and 1/3 of the daily dose in the evening (17-18 hours). With a threat of stress, the daily dose is increased 2-3 times and is prescribed in 3-4 doses (in 6-8 hours).

    With congenital dysfunction of the adrenal cortex cortisone apply in a dose of 25 mg per day in combination with other glucocorticosteroid drugs (prednisolone, dexamethasone). Maximum doses for adults: single dose - 150 mg, daily - 300 mg.

    Children cortisone prescribe in smaller doses depending on the age. Maximum doses for children: up to 5 years: single dose - 25 mg, daily - 75 mg; from 5 to 10 years: single - 50 mg, daily - 150 mg; over 10 years: single dose - 75 mg, daily - 225 mg. If it is necessary to replace cortisone with other drugs with glucocorticosteroid activity, remember that 25 mg of cortisone is equivalent to 20 mg of hydrocortisone; 5 mg of prednisolone or prednisone; 4 mg of methylprednisolone or triamcinolone; 0.75 mg of dexamethasone.

    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, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia, striae), delay in sexual development in children.

    From 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 "liver" transaminases and alkaline phosphatase.

    From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased cardiac insufficiency, ECG changes, 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: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor, cerebral palsy, headache, convulsions.

    From the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic 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 excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating. Caused by mineralocorticoid activity: fluid retention and sodium ions (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue.

    From the side of the musculoskeletal system: slowing growth and processes of ossification in children (premature closure epiphyseal growth zones), osteoporosis (very rarely pathological bone fractures,aseptic necrosis of the head of the humerus and thigh bone), rupture of the tendons of the muscles, steroid myopathy, decrease in muscle mass (atrophy).

    From the skin and mucous membranes: slow wound healing, petechiae, ecchymosis, thinning of the skin, hyper or hypopigmentation, "steroid" acne, striae, a tendency to develop pyoderma and candidiasis.

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

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

    Interaction:

    Strengthens the effect of anticoagulants, antiaggregants, the severity of side effects of nonsteroidal anti-inflammatory drugs, cardiac glycosides, estrogens, androgens, steroid anabolic, amphotericin B, asparaginase.

    Reduces the effectiveness of hypoglycemic, hypotensive drugs and diuretics.

    With simultaneous use with live antiviral vaccines and against other types of immunizations, increases the risk of virus activation and the development of infections.- Hypokalemia caused by glucocorticosteroids may increase the severity and duration of muscle blockade against the background of muscle relaxants.

    The therapeutic effect of glucocorticosteroids decreases under the influence of phenytoin,. .barbiturates, ephedrine, theophylline, rifampicin * and other inducers of "hepatic" microsomal enzymes (increased metabolic rate).
    Special instructions:

    During treatment it is necessary to control intraocular pressure and the condition of the cornea. The abolition is carried out by a gradual decrease in the dose (danger of the "withdrawal" syndrome): the longer the course of treatment, the slower the dose reduction should be.

    In time treatment of glucocorticosteroids should not be vaccinated due to a decrease in its effectiveness (immune response).

    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 chickenpox, prophylactically appoint specific immunoglobulins.

    In children during growth, glucocorticosteroids should be used only in absolute indications and under the close supervision of the treating physician.

    Effect on the ability to drive transp. cf. and fur:

    In connection with the possibility of developing dizziness, disorientation, hallucinations, seizures, damage to the optic nerve, the drug should be administered with caution to persons administering transport means and dealing with other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets 25 mg.

    Packaging:

    For 10 tablets in a planar cell package.

    8 contour mesh packages together with instructions for use in a pack of cardboard.

    Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:

    5 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003710 / 01
    Date of registration:22.07.2009 / 18.05.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp05.02.2018
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