Pharmacodynamics and pharmacokinetics
Pharmacodynamics
A synthetic fluorine-containing corticosteroid is an analogue of adrenal hormone . It has a stronger (100 times) mineralocorticoid effect than hydrocortisone . The use of Cortineff enhances the reabsorption of water and sodium and increases the excretion of potassium. Retention of sodium and fluid in the body leads to an increase in blood pressure .
In high doses, it can inhibit the activity of the adrenal cortex , thymus gland and the production of ACTH by the pituitary gland . If there is insufficient protein intake from food, it causes a negative nitrogen balance.
Intended for replacement therapy for adrenal insufficiency (acute or chronic).
Pharmacokinetics
When taken orally, it is completely absorbed. The active substance is determined in the blood after 10-20 minutes, and Cmax is reached after 1.7 hours. It binds to proteins by 70-80%. Metabolized in the liver and kidneys (partially). The half-life from the blood is 3.5 hours, from tissues - 18-36 hours. Excreted in urine.
Cortef
From the endocrine system:
decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (including moon face, pituitary type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, stretch marks), delay sexual development in children.
From the side of metabolism:
increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, fluid and sodium ion retention (peripheral edema), hypernatremia, hypokalemic syndrome (including hypokalemia, arrhythmia, myalgia or spasm muscles, unusual weakness and fatigue).
From the side of the central nervous system:
delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions.
From the cardiovascular system:
arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle; with intracranial administration - nosebleeds.
From the digestive system:
nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups; rarely - increased activity of liver transaminases and alkaline phosphatase.
From the senses:
sudden loss of vision (with parenteral administration in the head, neck, nasal turbinates, scalp, deposition of drug crystals in the vessels of the eye is possible), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral infections eye, trophic changes in the cornea, exophthalmos.
From the musculoskeletal system:
slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, steroid myopathy, decrease in muscle mass (atrophy; with intra-articular injection - increased joint pain
Dermatological
reactions:
delayed wound healing, petechiae, ecchymosis, skin thinning, hyper- or hypopigmentation, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis.
Allergic reactions:
generalized (including skin rash, skin itching, anaphylactic shock), local allergic reactions.
Effects due to immunosuppressive effects
: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination).
Local reactions:
with parenteral administration - burning, numbness, pain, paresthesia and infection at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; with intramuscular injection (especially into the deltoid muscle) - atrophy of the skin and subcutaneous tissue.
Other:
leukocyturia, withdrawal syndrome.
With intravenous administration - blood flow to the face, convulsions.
For external use:
rarely - itching, hyperemia, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, skin maceration, secondary infection, skin atrophy, stretch marks, prickly heat. With long-term use or application to large areas of skin, systemic side effects characteristic of GCS may develop.
Contraindications
- increased sensitivity;
- systemic mycoses .
Prescribed with caution for peptic ulcer disease , intestinal diverticulosis , ulcerative , esophagitis , operations on the gastrointestinal tract , gastritis liver and kidney dysfunction, arterial hypertension , diabetes mellitus , osteoporosis , hypothyroidism , myasthenia gravis , thyrotoxicosis , acute psychosis , obesity (III-IV degrees) .
Use caution in patients with acute and subacute infarction , cardiovascular diseases, viral and bacterial diseases, and in patients with HIV infection .
Cortineff, 20 pcs., 0.1 mg, tablets
The main undesirable effects include: arterial hypertension, peripheral edema, left ventricular hypertrophy, circulatory failure, hypernatremia, hypocalcemia.
When using Cortineff for a long time or using it simultaneously with other corticosteroids, the following side effects are possible.
From the musculoskeletal system:
muscle weakness, steroid myopathy (more common in women; usually begins with the pelvic muscles of the femoral girdle and spreads to the proximal muscles of the arms; rarely affects the respiratory muscles), loss of muscle mass, rupture of muscle tendons, osteoporosis, compression fracture of the spine, avascular necrosis of the femoral and humerus, pathological fractures of long tubular bones.
From the SSS side:
arrhythmias, bradycardia (up to cardiac arrest), ECG changes characteristic of hypokalemia, hypercoagulation, thrombosis, obliterating endarteritis; in patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
From 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 liver transaminases and alkaline phosphatase.
From the skin and mucous membranes:
atrophic stripes, acne, delayed wound healing, thinning of the skin, petechiae and hematomas, erythema, increased sweating, allergic dermatitis, urticaria, angioedema, ecchymosis, hyper- or hypopigmentation, a tendency to develop pyoderma and candidiasis.
From the nervous system:
increased ICP with congestive optic nipple syndrome (pseudotumor cerebri - most often in children, usually after too rapid dose reduction, symptoms - headache, decreased visual acuity or double vision), convulsions, dizziness, headache, sleep disturbances.
Endocrine status:
secondary adrenal and hypothalamic-pituitary insufficiency (especially in stressful situations such as illness, injury, surgery), Cushing's syndrome, growth suppression in children, menstrual irregularities, decreased tolerance to carbohydrates, manifestation of latent diabetes mellitus and increased need for insulin or oral hypoglycemic agents, hirsutism.
From the senses:
posterior subcapsular cataract (usually resolves after cessation of treatment, but surgical treatment may be required), increased intraocular pressure, glaucoma (usually after treatment for at least a year), exophthalmos, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea .
Mental disorders:
most often appear during the first 2 weeks of treatment, symptoms can mimic schizophrenia, mania or delirium (women are most susceptible).
From the side of metabolism:
negative nitrogen balance as a result of protein catabolism, hyperglycemia, glucosuria, increased excretion of Ca2+, hypocalcemia; caused by mineralocorticoid activity - hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).
Other:
anaphylactic reactions, weight gain, masking the symptoms of infectious diseases, fainting, development or exacerbation of infections (the manifestation of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.
Side effects
Cortineff may cause unwanted reactions:
- arterial hypertension;
- swelling;
- hypokalemia , hypocalcemia ;
- bradycardia;
- arrhythmias;
- muscle weakness, myopathy ;
- tendon rupture;
- loss of muscle mass;
- osteoporosis and pathological fractures;
- steroid ulcer and perforation;
- pancreatitis , ulcerative esophagitis , acne , petechiae , skin thinning;
- tendency to develop candidiasis ;
- urticaria , Quincke's edema ;
- dizziness , convulsions, sleep disturbances, severe depression ;
- Itsenko-Cushing syndrome , diabetes mellitus , hirsutism ;
- withdrawal syndrome;
- weight gain.
Cortineff
The main undesirable effects include: arterial hypertension, peripheral edema, left ventricular hypertrophy, circulatory failure, hyponatremia, hypocalcemia.
When using Cortineff for a long time or simultaneously with other corticosteroids, the following side effects may develop:
From the musculoskeletal system
:
Muscle weakness, steroid myopathy (more common in women; usually begins in the femoral girdle muscles and spreads to the proximal muscles of the arms; rarely affects the respiratory muscles), loss of muscle mass, rupture of tendons, muscles, osteoporosis, compression fracture of the spine, avascular necrosis of the femoral and humerus, pathological fractures of long tubular bones.
From the cardiovascular system
:
Arrhythmias, bradycardia (up to cardiac arrest), ECG changes characteristic of hypokalemia, hypercoagulation, thrombosis, obliterating endarteritis. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
From 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 liver transaminases and alkaline phosphatase.
From the skin and mucous membranes
:
Atrophic stripes, acne, delayed wound healing; thinning of the skin; petechiae and hematomas, erythema, increased sweating, allergic dermatitis, urticaria, angioedema, ecchymoses, hyper- or hypopigmentation, a tendency to develop pyoderma and candidiasis.
From the nervous system
:
Increased intracranial pressure with optic papilla congestion syndrome (pseudotumor cerebri - most often in children, usually after too rapid dose reduction, symptoms - headache, decreased visual acuity or double vision); convulsions, dizziness, headache, sleep disturbances.
From the endocrine system
:
Secondary adrenal and hypothalamic-pituitary insufficiency (especially during stressful situations such as illness, injury, surgery); Cushing's syndrome; growth suppression in children; menstrual irregularities; decreased tolerance to carbohydrates; manifestation of latent diabetes mellitus and increased need for insulin or oral hypoglycemic drugs in patients with diabetes mellitus; hirsutism.
From the senses
:
Posterior subcapsular cataract (usually resolves after cessation of treatment, but may require surgical treatment); increased intraocular pressure; glaucoma (usually after treatment for at least a year); exophthalmos, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea.
Mental disorders
:
Most often appear during the first two weeks of treatment; symptoms may mimic schizophrenia, mania, or delirium; Women are most susceptible to mental disorders.
Metabolism
:
Negative nitrogen balance as a result of protein catabolism; hyperglycemia; glucosuria, increased excretion of Ca2+, hypocalcemia. Caused by mineralcorticoid activity - hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).
Other:
Anaphylactic reactions; weight gain; masking symptoms of infectious diseases; fainting; development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination); leukocyturia; withdrawal syndrome.
Cortineff, instructions for use (Method and dosage)
The dose depends on the disease and the effectiveness of therapy. During treatment, dose adjustments are made during stressful situations, infections, injuries or operations. Often it is necessary to increase the dose in the summer, which is associated with large losses of sodium and water by the body.
Adults are prescribed 0.05-0.1 mg once a day in the morning, after breakfast, with plenty of water. The maximum daily dose is 0.2 mg. When prescribing high doses, take 2/3 of the dose in the morning, and the remaining 1/3 of the dose in the afternoon. Do not take a double dose if you miss a dose.
For children with adrenogenital syndrome - 300 mcg/day, with a gradual dose reduction. Maintenance dose for children - 50-100 mcg/day. In children, growth and development must be monitored.
With long-term use, the patient should follow a diet with limited sodium and increased potassium and protein. Long-term use poses a risk of fungal infection. The dose is reduced gradually, since sudden cessation of treatment causes adrenal insufficiency.
Use of the drug Cortineff
The dose of the drug is selected individually, depending on the severity of the disease and the response to the therapy. During treatment, it may be necessary to adjust the dose depending on the course of the disease or in a stressful situation (for example, during surgery, trauma or an infectious disease). Recommended doses for adults are 0.1-0.2 mg/day, for children with congenital adrenal dysplasia - initially 0.3 mg/day, then over several months the dose is reduced to 0.05-0.1 mg/day. The daily maintenance dose in infants is 0.1-0.2 mg, in older children - 0.05-0.1 mg/day. The tablets should be taken in the morning after meals with plenty of liquid. When using the drug in high doses, it is recommended to use 2/3 of this dose in the morning and 1/3 at noon. If you miss a dose, take the drug as quickly as possible or, if the time for your next dose is approaching, do not take the missed dose. Do not take two doses at the same time. In patients taking corticosteroids, in a stressful situation, fast-acting corticosteroids should be used in a higher dose. Sudden discontinuation of the drug may lead to adrenal insufficiency, so the dose of fludrocortisone must be reduced gradually.
Interaction
When used with cardiac glycosides, their toxicity increases and the risk of hypokalemia and arrhythmias increases. Use with NSAIDs gastrointestinal ulcers .
Barbiturates, rifampicin , phenytoin , carbamazepine and antihistamines weaken the effect of Cortineff.
Hypokalemia and left ventricular hypertrophy are caused by concomitantly administered amphotericin B and carbonic anhydrase .
When used with androgens and anabolic steroids, the risk of edema and acne increases.
Estrogens slow down metabolism and enhance the effect of the active substance. Anticoagulants, urokinase and streptokinase , on the contrary, reduce effectiveness. Accelerates the metabolism of the drug ephedrine .
Tricyclic antidepressants increase mental disorders.
Cortineff weakens the effect of insulin , hypoglycemic drugs and potassium-sparing diuretics.
When used with muscle relaxants, the duration of neuromuscular blockade increases.
Increased edema and hypertension are observed when eating foods with large amounts of sodium.
When used with vaccines, there is a risk of neurological complications.
Drug interactions Cortineff
patients with hypoprothrombinemia should be prescribed fludrocortisone with caution in combination with acetylsalicylic acid. With simultaneous use of Cortineff with digitalis glycosides, the risk of developing cardiac arrhythmias and glycoside toxicity increases; with barbiturates, antiepileptic drugs (phenytoin, carbamazepine), rifampicin, glutethimide, antihistamines, the potency of fludrocortisone is weakened; with amphotericin B, carbonic anhydrase inhibitors - hypokalemia, myocardial hypertrophy, congestive circulatory failure; with anabolic steroids, androgens - the risk of developing edema and rash increases; with estrogens - metabolism slows down and the effect of fludrocortisone increases; with antithrombotic agents (coumarin and indadione derivatives, heparin, streptokinase, urokinase) - it decreases, and in some people the effectiveness of fludrocortisone increases; with tricyclic antidepressants - the development of mental disorders is possible; with immunosuppressants - increased risk of developing infections, lymphangiomas and lymphoproliferative diseases; with oral hypoglycemic drugs, insulin - weakening of the antidiabetic effect; with diuretics - decreased diuretic effect, hypokalemia; with laxatives - weakening of the effect, hypokalemia; with NSAIDs - decreased effectiveness, increased risk of ulcerogenic effects and gastrointestinal bleeding; with sodium salts - peripheral edema, increased blood pressure (it may be necessary to limit sodium in the diet); In some patients, the use of GCS sometimes requires additional sodium intake.
Reviews of Cortineffe
For adrenal insufficiency, hydrocortisone is prescribed , and with a slight decrease in mineralocorticoid function, taking one drug is sufficient. a corticosteroid with more pronounced mineralocorticoid activity is added to the treatment This combination ideally compensates for the lack of hormones and is used constantly. Minimum doses are prescribed that ensure satisfactory well-being, performance, and the required level of electrolytes and blood pressure . The adequacy of treatment is assessed by these parameters, as well as by ECG . Patients with adrenal dysfunction who receive adequate therapy live full lives. Severe course is observed only in untreated patients.
There are many reviews from patients with congenital dysfunction of the adrenal cortex or parents of children suffering from this pathology. Everyone reports that they take this drug together with Cortineff constantly, 2 times a day. Sometimes there are difficult situations when the drug is not available in the pharmacy chain. For such patients it is vital.
- “... Addison's disease, I take Cortineff and dexamethasone. When there were interruptions in the supply of this drug, they switched to prednisolone. I immediately realized that he was not a good fit: he had convulsions, his blood pressure dropped, and he gained weight.”
- “... The child has adrenogenital syndrome, a salt-wasting form. Lifelong replacement therapy is required. How difficult it is when Cortineff disappears from pharmacies. In order not to bring the child to a crisis, I look everywhere—friends bring them from Poland or I order from online pharmacies.”
Special instructions for the use of Cortineff
May have a teratogenic effect and cause adrenal insufficiency in the fetus and newborn. Systemic use of GCS in women of reproductive age and during pregnancy is permissible only if the expected therapeutic effect of the drug outweighs the potential threat to the fetus. Fludrocortisone is excreted in breast milk and may cause unwanted reactions in the baby. Breastfeeding should be discontinued while taking fludrocortisone. Fludrocortisone can mask the symptoms of infectious diseases and also reduce the body's resistance to infections. Patients taking fludrocortisone should not be vaccinated with live viral vaccines. The use of inactivated bacterial or viral vaccines may not produce the expected immune response. Individuals receiving treatment with corticosteroids are at increased risk of developing neurological complications associated with vaccination. A break in treatment after prolonged use of the drug can cause the development of GCS withdrawal syndrome, manifested by fever, myalgia and arthralgia, and general malaise. In patients with hypothyroidism or liver cirrhosis, the effect of fludrocortisone is more pronounced. Fludrocortisone should be used in the lowest effective doses. Fludrocortisone should be used with extreme caution in case of nonspecific ulcerative colitis, diverticulosis of the small intestine, a history of peptic ulcer of the stomach or duodenum, renal failure, hypertension (arterial hypertension), osteoporosis, myasthenia gravis, diabetes mellitus, liver disease, glaucoma, fungal or viral infections , recently undergone surgery on the gastrointestinal tract. In children taking the drug for a long time, the dynamics of growth and development should be monitored.
Cortineffa price, where to buy
You can buy Cortineff in pharmacies in regional cities. The cost of 20 tablets ranges from 107-119 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Cortineff tablets 0.1 mg 20 pcs. Adamed Pharma JSC
RUB 129 order
Pharmacy Dialogue
- Cortineff (tablet 0.1 mg No. 20)Polfa
114 RUR order
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Pharmacy24
- Cortineff 0.1 mg N20 tablets Pub Yanitsky FZ, Polfa A.T., Poland
131 UAH.order
