DR. DOPING

Instructions

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Instructions / Instruction for use: Fludrocortisone (Fludrocortisonum)

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Pharmacological group

Mineralocorticosteroids

Nosological classification (ICD-10)

E25 Adrenogenital disorders

Macroghenytozomy in boys, Adrenogenital syndrome, Decreased function of the sex glands, Congenital dysfunction of the adrenal cortex, Apera-Halle Syndrome, Crook-Apera-Halle Syndrome

E27.1 Primary insufficiency of the adrenal cortex

Addison's Disease, Addisonism, Adrenocortical insufficiency, Hypofunction of the adrenal cortex, Collapse with Addison's Disease, Insufficiency of the adrenal cortex primary, Primary adrenocortical insufficiency, Primary adrenal insufficiency

E27.4 Other and unspecified adrenocortical insufficiency

Hypocorticism, Hypoaldosteronism, Adrenal insufficiency, Insufficiency of the adrenal cortex, Insufficiency of the adrenal cortex, Secondary adrenocortical insufficiency, Secondary adrenal insufficiency, Secondary insufficiency of the adrenal cortex, Temporary decrease in the function of the adrenal cortex, Dysfunction of the adrenal cortex

E86 Decreased fluid volume [hypovolaemia] Water deficit compensation, Indemnification of isotonic deficiency of water, Compensation for isotonic sodium deficiency, Compensation BCC, Replenishment of water deficit with stored KShS, Replenishment of fluid volume, Replenishment of BCC, Replenishment of electrolytes with stored KHS, Hypovolemic condition, Hypovolemia, Hypotonic form of hypohydration, Hypochloremia with dehydration, Dehydration of different origin, Dehydration in children, Replacing the volume of plasma with blood loss in pediatrics, Replacing the plasma with its losses and burns, Isotonic dehydration, Isotonic form of hypohydration, Violation of the water-salt balance, Dehydration, Dehydration in acute intestinal infections, Acute hypovolemia, Loss of fluid during burns, Toxicosis with exsycosis

I95.9 Hypotension, unspecified

Hypotensive reactions in case of weather changes, Hypotension in septic shock, Arterial hypotension with spinal anesthesia, Hypotonic state, Hypotension

Code CAS127-31-1

Characteristics

It is a synthetic hormone of the adrenal cortex, a fluorinated derivative of hydrocortisone, which has a high mineralocorticoid activity.

Pharmacology

Pharmacological action - glucocorticoid, mineralocorticoid.

Raises blood pressure (BP), reabsorption of sodium, water and secretion of potassium in the renal tubules. Oppresses the production of ACTH (adrenocorticotropic hormone), adrenal function, stimulates gluconeogenesis, breakdown of proteins (causes a negative nitrogen balance), shows immunosuppressive and anti-inflammatory activity; When applied locally reduces itching and exudation. Well absorbed from the digestive tract (gastrointestinal tract). T1 / 2 from the plasma - 3.5 hours Easily passes the histohematological barriers. It is excreted in the urine in the form of metabolites. T1 / 2 - 18-36 hours. An insignificant part is excreted during lactation.

Application of Fludrocortisone

Primary insufficiency of the adrenal cortex (Addison's disease, condition after complete adrenalectomy), secondary adrenocortical insufficiency, adrenogenital syndrome (congenital adrenal hyperplasia), hypovolemia and hypotension of various genesis.

Contraindications

Hypersensitivity, systemic fungal infections.

Restrictions for use

Nonspecific ulcerative colitis, intestinal diverticulosis, stomach ulcer or duodenal ulcer, acute or latent peptic ulcer, newly developed intestinal anastomosis, esophagitis, gastritis, gastrointestinal surgery in history, impaired liver function, renal failure, hypertension , Osteoporosis, myasthenia gravis, hypoalbuminemia and conditions predisposing to its occurrence, hyperlipidemia; Diabetes mellitus (including a violation of carbohydrate tolerance), hypothyroidism, Itenko-Cushing's disease, thyrotoxicosis, obesity (III-IV century), acute psychosis and mental disorders, poliomyelitis (with the exception of the form of bulbar encephalitis); Cardiovascular diseases, incl. Recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction, a necrosis foci may spread, a delay in the formation of scar tissue and, as a consequence, a rupture of the heart muscle), decompensated chronic heart failure; Parasitic and infectious diseases of bacterial nature (currently or recently transferred, including contact with the patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles, amebiasis, strongyloidiasis (established or suspected); Active and latent tuberculosis; Severe infectious diseases (permissible only against specific therapy); A period of 8 weeks before and 2 weeks after vaccination, lymphadenitis after BCG vaccination; HIV (human immunodeficiency virus) -infection and AIDS (acquired immunodeficiency syndrome) (decision on the use of corticosteroids should be taken after careful consideration of the benefit and risk to the patient).

pregnancy and lactation

Acceptance of corticosteroids by women of childbearing age and pregnant women is allowed only if their potential benefit to the mother exceeds the potential risk to the fetus. If the adrenal cortex is deficient, fludrocortisone should be taken during pregnancy, but the dose may increase.

Action category for fetus by FDA - C.

If it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Side effects

From the side of the cardiovascular system and blood (blood, hemostasis): arterial hypertension, peripheral edema, left ventricular hypertrophy of the heart, circulatory insufficiency, arrhythmia, bradycardia (up to cardiac arrest), ECG changes (electrocardiogram, electrocardiography), characteristic of hypokalemia ; Hypercoagulation, thrombosis, obliterating endarteritis; 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.

On the part of the gastrointestinal tract: steroid ulcer with possible perforation and bleeding, pancreatitis, flatulence, ulcerative esophagitis, indigestion, nausea, increased or decreased appetite, vomiting, hiccough; In rare cases - increased activity of hepatic transaminases and alkaline phosphatase (alkaline phosphatase).

On the part of the skin: atrophic bands, acne, delayed wound healing, thinning of the skin, petechia and hematoma, erythema, excessive sweating, ecchymosis, hyper- or hypopigmentation, propensity to develop pyoderma and candidiasis.

From the side of the nervous system and sensory organs: increased intracranial pressure with the syndrome of the congestive nipple of the optic nerve (pseudotumor of the brain - most often in children, usually after too rapid reduction of the dose, symptoms - headache, reduced visual acuity or double vision), convulsions, dizziness , Headache, sleep disturbance, mental disorders (most often appear within the first 2 weeks of treatment, symptoms can mimic schizophrenia, mania or delirious syndrome, women are most susceptible), posterior subcapsular I cataract (usually passes after stopping treatment but may require surgical treatment), increased intraocular pressure, glaucoma (usually after treatment for at least one year), exophthalmos, the tendency to the development of secondary bacterial, fungal or viral infections of the eyes, trophic changes of the cornea.

On the part of the endocrine system: secondary adrenal and hypothalamic-pituitary insufficiency (especially in stressful situations such as illness, trauma, surgery), Itenko-Cushing syndrome, growth inhibition in children, menstrual irregularities, decreased glucose tolerance, steroid diabetes mellitus Or the manifestation of latent diabetes mellitus, hirsutism.

On the part of metabolism: hypocalcemia, negative nitrogen balance due to protein catabolism, hyperglycemia, glucosuria, increased excretion of Ca2 +; Conditioned by mineralocorticoid activity - hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: muscle weakness, steroid myopathy (more often in women), loss of muscle mass, rupture of tendons, osteoporosis, compression fracture of the spine, aseptic necrosis of the femoral and humerus head, pathological fractures of long tubular bones.

Allergic reactions: allergic dermatitis, hives, anaphylactic reactions, angioedema.

Other: weight gain, masking of symptoms of infectious diseases, syncope, development or exacerbation of infections (manifestation of this side effect is promoted by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

Interaction

Increases the efficiency (and toxicity) of systemic gluco- and mineralocorticoids, reduces anabolic steroids (but increases their hepatotoxicity). Anabolic steroids, androgens increase the risk of peripheral edema, acne (use cautiously, especially in diseases of the liver and heart).

Increases the likelihood of side effects in the appointment of cardiac glycosides and drugs that cause hypokalemia (diuretics, amphotericin B). Against the background of sodium-containing drugs, the risk of peripheral edema and hypertension increases. Against the background of acetylsalicylic acid and other NSAIDs, the risk of ulceration of the gastric mucosa increases. Barbiturates, antiepileptic drugs (phenytoin, carbamazepine), rifampicin accelerate the metabolism of corticosteroids (by induction of microsomal enzymes) and weaken their action.

Oral contraceptives containing estrogens slow down metabolism, increase T1 / 2 and increase the effect of fludrocortisone. Antihistamines reduce the effect of fludrocortisone. With the simultaneous use of fludrocortisone and anticoagulants (coumarin derivatives, indanedione, heparin), streptokinase, urokinase, there is a decrease, and in some cases - an increase in the effectiveness of anticoagulants (the dose of anticoagulants should be determined on the basis of PV); The risk of ulceration and bleeding from the digestive tract increases.

Tricyclic antidepressants can enhance mental disorders associated with the administration of fludrocortisone (should not be prescribed for treatment of these disorders). Ephedrine can accelerate the metabolism of corticosteroids (possible correction of the dose of fludrocortisone).

Weaken the hypoglycemic effect of oral hypoglycemic agents and insulin (it is possible to correct the dose of hypoglycemic drugs), the effect of potassium-sparing diuretics, laxatives.

With simultaneous use with immunosuppressants, the risk of infection, lymphoma and other lymphoproliferative diseases increases. Hypocalcemia associated with the use of fludrocortisone may contribute to strengthening the blockade of synapses and lead to an increase in the duration of neuromuscular blockade when combined with depolarizing muscle relaxants.

With the simultaneous use of immunosuppressive doses of corticosteroids and vaccines containing live viruses, virus replication (development of viral diseases) and a decrease in antibody production (simultaneous use is not recommended), other vaccines increase the risk of neurological complications and reduce the production of antibodies.

Overdose

Symptoms: arrhythmia, hypokalemia, arterial hypertension, peripheral edema, significant increase in body weight, cardiac muscle hypertrophy.

Treatment: withdrawal of the drug (symptoms usually last for several days), symptomatic therapy. Then the treatment should be continued, reducing the dose of the drug.

Routes of administration

Inside.

Precautions

Regular monitoring of blood pressure, potassium and glucose levels in the blood is necessary. It is necessary to limit the intake of salt, prophylactically prescribe potassium preparations, control the functions of the adrenal cortex. Elongation of the course is possible only with a lower dose. After a long reception, cancellation is made gradually (the risk of adrenal insufficiency).

The frequency 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.