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Active ingredients
Fludrocortisone
Release form
Pills
Composition
Active ingredient: Fludrocortisone acetate; Concentration of active ingredient (mg): 0.1
Pharmacological effect
Synthetic analogue of the hormone of the adrenal cortex, fluorinated hydrocortisone derivative. It has high mineralocorticoid activity .; Cortineff enhances the reabsorption of sodium and water in the renal tubules, and also increases the excretion of potassium and hydrogen ions. The increase in extracellular fluid volume and sodium retention in the body lead to an increase in blood pressure .; Cortineff in doses exceeding therapeutic can inhibit the activity of the adrenal cortex, the activity of the thymus gland and the secretion of ACTH by the pituitary gland. The drug can also increase the deposition of glycogen in the liver, and, with an insufficient amount of protein in the diet, leads to a negative nitrogen balance .; Cortineff has a 100-fold stronger mineralocorticoid effect and 10-15-fold stronger anti-inflammatory effect than hydrocortisone.
Pharmacokinetics
Absorption; After ingestion is rapidly and completely absorbed from the gastrointestinal tract. The active substance is detected in the blood serum 10–20 minutes after a dose of 0.1 mg. Cmax of the active substance in plasma is reached approximately 1.7 hours after administration. Distribution; Plasma protein binding - 70-80% .; Metabolism; Metabolized mainly in the liver, partly in the kidney .; Withdrawal; T1 / 2 - about 3.5 hours. Excreted in the urine in the form of inactive metabolites. T1 / 2 of tissue is 18-36 hours.
Indications
Primary insufficiency of the adrenal cortex (Addison's disease, condition after complete adrenalectomy). Secondary insufficiency of the adrenal cortex. ; Adrenogenital syndrome (congenital adrenal hyperplasia). ; Hypovolemia and arterial hypotension of various genesis.
Contraindications
Systemic mycoses; Hypersensitivity to fludrocortisone or other components of the drug.
Use during pregnancy and lactation
Use of Cortineff during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus .; In case of insufficiency of the adrenal cortex, the reception of Corineffe during pregnancy should be continued, while its dose may increase .; If necessary, the use of the drug during lactation is recommended to stop breastfeeding.
Dosage and administration
The dose of the drug is set individually, depending on the evidence, the effectiveness of therapy and the patient's condition. In the course of treatment, when the clinical picture changes or during stressful situations, such as surgery, trauma or infection, dose adjustment may be necessary. ; Adults with replacement therapy: Depending on the clinical situation, the dose varies from 100 mcg 3 times a week to 200 mcg / day. ; In adrenogenital syndrome in children: It is prescribed at an initial dose of 300 mcg / day, then within a few months the dose is reduced to 50-100 mcg / day. The maintenance dose for infants ranges from 100 to 200 mcg / day, for children over the age of 1 year - 50-100 mcg / day. ; Tablets should be taken in the morning after meals with plenty of fluids. In the case of use in high doses, it is recommended to take 2/3 doses in the morning and 1/3 doses in the afternoon. ; If you miss a dose, you should take the drug as soon as possible. If the time of the next intake is approaching, the missed dose should not be taken. Do not take a double dose right away. ; Cortineff should be taken in minimum effective doses. If necessary, the dose should be reduced gradually. ;
Side effects
On the part of the musculoskeletal system: muscle weakness, steroid myopathy (more common in women; usually begins with pelvic muscles of the femoral belt and spreads to proximal arm muscles; rarely affects the respiratory muscles), muscle loss, muscle tendon rupture, osteoporosis, compression fracture spine, aseptic necrosis of the heads of the femur and humerus, pathological fractures of the long tubular bones. ; On the part of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest), ECG changes characteristic of hypokalemia, hypercoagulation, thrombosis, endarteritis obliterans; in patients with acute and subacute myocardial infarction - the spread of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle. ; On the part of the digestive system: steroid ulcer with possible perforation and bleeding, pancreatitis, flatulence, ulcerative esophagitis, digestive disorders, nausea, increased or decreased appetite, vomiting, hiccups; in rare cases - increased activity of hepatic transaminases and alkaline phosphatase.; On the part of the skin and mucous membranes: atrophic bands, acne, delayed wound healing, thinning of the skin, petechia and hematomas, erythema, increased sweating, allergic dermatitis, urticaria, angioedema, ecchymosis, hyper- or hypopigmentation, tendency to develop pyoderma . ; On the part of the nervous system: increased ICP with optic nerve congestive nipple syndrome (brain pseudotumor - most often in children, usually after too fast a dose reduction, symptoms - headache, decreased visual acuity or double vision), convulsions, dizziness, headache, sleep disorders. ; Endocrine status: secondary adrenal and hypothalamic-pituitary insufficiency (especially in stressful situations such as illness, trauma, surgery), Cushing's syndrome, growth suppression in children, menstrual disorders, decrease in carbohydrate tolerance, manifestation of latent diabetes mellitus, and increased demand in insulin or oral hypoglycemic agents, hirsutism. ; On the part of the senses: posterior subcapsular cataract (usually goes away after stopping treatment, but may require surgical treatment), increased intraocular pressure, glaucoma (usually after treatment for at least a year), exophthalmos, a tendency to develop secondary bacterial, fungal or viral infections eye, trophic changes of the cornea. ; Mental disorders: most often appear during the first 2 weeks of treatment, symptoms can mimic schizophrenia, mania or delirious syndrome (women are most susceptible). ; Metabolism: negative nitrogenous balance as a result of protein catabolism, hyperglycemia, glycosuria, increased excretion of Ca2 +, hypocalcemia; caused by mineralocorticoid activity - hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue). ; Others: anaphylactic reactions, weight gain, masking of symptoms of infectious diseases, fainting, development or exacerbation of infections (jointly used immunosuppressants and vaccination contribute to the manifestation of this side effect), leukocyturia, withdrawal syndrome. ;
Overdose
Symptoms: arterial hypertension, peripheral edema, hypokalemia, a significant increase in body weight, myocardial hypertrophy .; Treatment: cancel the drug. Symptoms usually go away within a few days. Then treatment should be continued, reducing the dose of Florinef. In the case of muscle weakness associated with potassium loss, the administration of potassium preparations is necessary. For the prevention of overdose should regularly monitor blood pressure and the concentration of electrolytes in the serum.
Interaction with other drugs
With simultaneous use of Corineffe with cardiac glycosides, the risk of developing cardiac arrhythmias increases and the toxicity of glycosides increases on the background of hypokalemia .; With the simultaneous use of barbiturates, antiepileptic drugs (phenytoin, carbamazepine), rifampicin, gluthethimide weaken the action of Cortineff by accelerating the metabolism of fludrocortisone .; Antihistamines weaken the action of Cortineff .; Amphotericin B, carbonic anhydrase inhibitors, when used simultaneously with Cortineff, can cause hypokalemia, left ventricular hypertrophy of the heart, circulatory failure .; With simultaneous use of Kortineff with anabolic steroids, androgens, the risk of developing peripheral edema and the occurrence of acne increases (use with caution, especially in patients with diseases of the liver and heart) .; Oral contraceptives containing estrogens increase the serum level of globulins that bind corticosteroids, increase the effect of Cortineff by slowing the metabolism of fludrocortisone and increasing its T1 / 2 .; Anticoagulants (coumarin derivatives, indadione, heparin), streptokinase, urokinase reduce (in some patients increase) the effectiveness of Corineffe. The dose should be determined on the basis of prothrombin time and take into account the increased risk of ulceration and bleeding from the gastrointestinal tract .; Tricyclic antidepressants can exacerbate the mental disorders associated with taking Cortineff (these drugs should not be used to treat these disorders) .; With the simultaneous use of Kortineff weakens the action of oral hypoglycemic drugs, insulin, potassium-sparing diuretics,increases the concentration of glucose in the blood (may require correction of the dose of hypoglycemic drugs) .; Cortineff reduces the effectiveness of laxatives, potassium-sparing diuretics, and the risk of hypokalemia increases .; Ephedrine can accelerate the metabolism of fludrocortisone (correction of the dose of Cortineff may be required) .; With the simultaneous use of Kortineff with immunosuppressive drugs increases the risk of developing infection, lymphoma and other lymphoproliferative diseases .; Cortineff when used simultaneously with depolarizing muscle relaxants may increase the duration of the neuromuscular blockade, since hypocalcemia associated with the use of Cortineff may increase the blockade of synapses .; Cortineff reduces the effect of NSAIDs (including acetylsalicylic acid), while increasing the risk of ulcerative lesions and the development of bleeding from the gastrointestinal tract .; With the simultaneous use of Corineffe and drugs and foods containing sodium, peripheral edema, arterial hypertension are possible .; With the use of vaccines containing live viruses, against the background of the use of immunosuppressive doses of Cortineff, replication of viruses and the development of viral diseases are possible, a decrease in antibody production (the combination is not recommended) .; With simultaneous use with other vaccines increases the risk of neurological complications and reduces the production of antibodies.
special instructions
In stressful situations (including surgery, trauma or infection), parenteral administration of GCS is recommended for patients receiving the drug; Sudden cessation of treatment can cause the development of adrenal insufficiency, so the dose of Corineffe should be reduced gradually .; Kortineff can mask the symptoms of infectious diseases, reduce the body's resistance to infection and the ability to localize it .; Prolonged use of Florinef increases the risk of developing a secondary fungal or viral infection .; With prolonged use of Cortineff, it may be necessary to transfer the patient to a diet with limited sodium intake and an increase in the potassium content, as well as an increase in the protein content .; With the use of Kortineff should not be vaccinated with live virus vaccines.The introduction of an inactivated viral or bacterial vaccine may not cause the expected increase in antibody titer. In addition, patients receiving corticosteroids, increases the risk of neurological complications during vaccination .; It should be borne in mind that the abolition of the drug should be carried out gradually. With the sudden withdrawal of the drug, especially after long-term therapy, the development of withdrawal syndrome characterized by anorexia, fever, myalgia and arthralgia, general weakness (these symptoms may appear even in the absence of signs of adrenal insufficiency) may occur .; In patients with hypothyroidism or cirrhosis of the liver, the action of Corineffe is enhanced .; Against the background of the use of Cortineff, the previously existing emotional instability or psychotic warehouse of the patient’s personality may increase. Patients with hypoprothrombinemia should be carefully prescribed Corineff at the same time as acetylsalicylic acid .; Use in pediatrics; With long-term use of Kortineff in children, careful monitoring of their growth and development is necessary.