Solu-Cortef
Solu-Cortef: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Solu-Cortef
ATX code: H02AB09
Active ingredient: hydrocortisone (hydrocortisone)
Manufacturer: Pfizer MFG. Belgium N. V. (Belgium)
Description and photo update: 2018-27-11
Solu-Cortef is a systemic glucocorticosteroid (GCS).
Release form and composition
Dosage form - lyophilisate for the preparation of a solution for intravenous (i / v) and intramuscular (i / m) administration: powder or porous mass of almost white or white color [in colorless glass vials or in double-volume ACT-O-VIAL vials (GCS lyophilisate and solvent * in two separate containers of one bottle), in a cardboard box 1 bottle and instructions for use of Solu-Cortef].
* Solvent is a clear, colorless liquid.
Solution after reconstitution: transparent, slightly opalescent, colorless or slightly yellowish.
Composition of the preparation in colorless glass vials:
- active substance: hydrocortisone (in the form of sodium succinate) - 100 mg;
- auxiliary components: sodium dihydrogen phosphate monohydrate - 0.9 mg, sodium hydrogen phosphate - 8.8 mg.
Composition of the preparation in two-volume ACT-O-VIAL vials:
- lower container: active substance - hydrocortisone (in the form of sodium succinate) - 100 mg; auxiliary components: sodium dihydrogen phosphate monohydrate - 0.9 mg, sodium hydrogen phosphate - 8.8 mg;
- upper container: benzyl alcohol - 18 mg, water for injection - 2 ml.
Pharmacological properties
Pharmacodynamics
Penetrating through cell membranes, hydrocortisone forms complexes with specific cytoplasmic receptors. These complexes penetrate into the cell nucleus, where they bind to deoxyribonucleic acid (chromatin). Subsequently, the formed complexes stimulate the transcription of mRNA (matrix ribonucleic acid), followed by the synthesis of various enzymes. This mechanism of action explains the systemic effect of Solu-Cortef. Hydrocortisone has a significant effect not only on the immune response and the inflammatory process, but also on protein, fat and carbohydrate metabolism.
The maximum pharmacological activity of hydrocortisone is manifested not at the peak of plasma concentration, but after it, therefore, the effect of the glucocorticosteroid is mainly due to its effect on enzyme activity.
Solu-Cortef has anti-shock, anti-inflammatory, immunosuppressive, anti-toxic, desensitizing, anti-allergic and anti-metabolic effects.
The immunosuppressive activity of hydrocortisone, in contrast to cytostatics, is not associated with a mitostatic effect, but is the total result of the suppression of various stages of immunogenesis: migration of B cells, migration of stem cells (bone marrow), interaction of T and B lymphocytes. Solu-Cortef inhibits the release of cytokines (interferon and interleukins) from macrophages and lymphocytes, inhibits the release of inflammatory mediators by eosinophils, reduces the synthesis of prostaglandins and the metabolism of arachidonic acid. Hydrocortisone stimulates steroid receptors, as a result of which it induces the formation of lipocortin. Reduces the synthesis of histamine, increases blood glucose, enhances the excretion of potassium ions from the body, inhibits the excretion of sodium and water ions, and promotes the deposition of glycogen in the liver.
Hydrocortisone reduces the migration of lymphocytes and leukocytes to the area of inflammation, reduces inflammatory cell infiltrates. In high doses, it inhibits the development of connective and lymphoid tissue (including the reticuloendothelial system). Suppresses hyaluronidase, reduces capillary permeability, and also reduces the number of mast cells, where hyaluronic acid is formed. It inhibits the synthesis of proteins and accelerates their breakdown. Acting on the pituitary gland, hydrocortisone inhibits the production of corticotropin.
With prolonged use of Solu-Cortef, suppression and atrophy of the adrenal cortex, suppression of the formation of gonadotropic and thyroid-stimulating hormones of the pituitary gland are possible.
Pharmacokinetics
C max (maximum plasma concentration) of hydrocortisone after i / m administration is observed after about 30-60 minutes.
The connection of the substance with plasma proteins is 40–90%. Most of the hydrocortisone binds to one of the globulins (transcortin), only a small part binds to albumin.
The biological activity of hydrocortisone is determined by the free unbound fraction of the hormone. The associated faction acts as a reserve.
The drug is metabolized primarily in the liver.
With urine, 22–30% of hydrocortisone administered intramuscularly or intravenously is excreted within 24 hours.
Hydrocortisone is almost completely excreted from the body within 12 hours, therefore, if it is necessary to maintain high concentrations in the blood, Solu-Cortef should be administered every 4-6 hours.
Indications for use
Emergency conditions:
- shock due to adrenal insufficiency;
- shock resistant to standard therapy in patients with possible adrenal insufficiency;
- hemorrhagic, traumatic and surgical shock that cannot be corrected by standard therapy;
- acute allergic manifestations (reactions to insect bites, anaphylactic reactions, status asthmaticus) - after the use of epinephrine.
Severe and disabling allergic conditions in which conventional therapy has proven ineffective:
- drug hypersensitivity reactions;
- post-transfusion reactions such as urticaria;
- serum sickness;
- acute non-infectious laryngeal edema;
- asthmatic status;
- seasonal and perennial allergic rhinitis;
- contact dermatitis;
- atopic dermatitis.
Hematological diseases:
- erythrocytic anemia (erythroblastopenia);
- erythroid (congenital) hypoplastic anemia;
- autoimmune (acquired) hemolytic anemia;
- secondary thrombocytopenia in adults;
- idiopathic thrombocytopenic purpura in adults (the drug is administered only intravenously, intramuscular use is contraindicated).
Edematous syndrome: proteinuria in nephrotic syndrome without uremia, in idiopathic nephrotic syndrome or lupus erythematosus - to stimulate diuresis and achieve remission.
Endocrine diseases:
- acute adrenal insufficiency (hydrocortisone and cortisone are the drugs of choice; sometimes the simultaneous use of mineralocorticoids is required);
- primary and secondary adrenal insufficiency (hydrocortisone and cortisone are the drugs of choice; if necessary, their synthetic analogues are used in combination with mineralocorticoids, especially in the treatment of children).
Systemic connective tissue diseases (with exacerbation or, in some cases, as a maintenance drug):
- systemic lupus erythematosus;
- systemic dermatomyositis (polymyositis);
- acute rheumatic heart disease.
Respiratory tract diseases:
- disseminated and fulminant pulmonary tuberculosis (simultaneously with the corresponding anti-tuberculosis chemotherapy);
- aspiration pneumonitis;
- Leffler's syndrome, resistant to therapy with other drugs;
- beryllium disease;
- clinically significant sarcoidosis.
Diseases of the gastrointestinal tract (short-term use until the patient is removed from a critical condition):
- regional enteritis;
- ulcerative colitis.
Rheumatic diseases (briefly as an adjunct therapy for an exacerbation of the disease, as well as for removing the patient from an acute condition):
- psoriatic arthritis;
- acute gouty arthritis;
- rheumatoid arthritis, including juvenile arthritis (in some cases, maintenance therapy with the use of the drug in low doses may be required);
- synovitis with osteoarthritis;
- post-traumatic osteoarthritis;
- acute nonspecific tendosynovitis;
- acute and subacute bursitis;
- ankylosing spondylitis;
- epicondylitis.
Ophthalmic diseases (severe acute / chronic inflammatory and allergic processes with eye damage):
- keratitis;
- inflammation of the anterior segment;
- diffuse posterior uveitis and choroiditis;
- allergic edge corneal ulcers;
- ocular form of herpes zoster (Herpes zoster);
- allergic conjunctivitis;
- iritis and iridocyclitis;
- chorioretinitis;
- sympathetic ophthalmia;
- optic neuritis.
Dermatological diseases:
- severe psoriasis;
- exfoliative dermatitis;
- bullous dermatitis herpetiformis;
- severe seborrheic dermatitis;
- pemphigus;
- fungal mycosis;
- malignant exudative erythema (Stevens-Johnson syndrome).
Oncological diseases (as palliative therapy):
- lymphomas and leukemias in adults;
- acute leukemia in children.
As symptomatic therapy:
- subacute thyroiditis;
- congenital adrenal hyperplasia;
- the period of preparation for surgery, serious illness or severe trauma, diagnosed or suspected adrenal insufficiency;
- hypercalcemia against the background of cancer.
Other indications for use:
- trichinosis with damage to the myocardium or nervous system;
- tuberculous meningitis in the presence of a subarachnoid block or the threat of its formation (simultaneously with the corresponding anti-tuberculosis chemotherapy).
Contraindications
- systemic fungal infections;
- the presence of individual hypersensitivity to any component of the drug.
Solu-Cortef is not recommended for use in acute and subacute myocardial infarction, since hydrocortisone can promote the spread of the necrosis focus, inhibition of the formation of scar tissue and, as a result, rupture of the heart muscle.
The drug in two-volume vials ACT-O-VIAL should not be administered to newborns, since the solvent contains benzyl alcohol, which can cause respiratory system disturbances in the form of suffocation, or even death.
During the period of use of the drug in immunosuppressive doses, it is contraindicated to immunize with live and live attenuated vaccines.
Solu-Cortef should be used with caution in the following cases:
- eye damage caused by the herpes simplex virus (corneal perforation may develop);
- ulcerative colitis in the presence of a threat of abscess, perforation or other purulent infection;
- active or latent peptic ulcer;
- the presence of fresh intestinal anastomoses;
- renal failure;
- myasthenia gravis;
- osteoporosis;
- arterial hypertension.
Solu-Cortef, instructions for use: method and dosage
The solution prepared from the lyophilisate is indicated for intramuscular injection and intravenous administration / infusion. Before administration, the solution must be visually inspected for precipitation, particles or discoloration. It is allowed to use only a clear solution.
In case of emergency conditions, treatment is recommended to begin with intravenous administration of the drug. After the end of the acute period, parenteral dosage forms of hydrocortisone with a longer duration of action or oral forms of hydrocortisone are prescribed.
At the beginning of treatment, the administration of Solu-Cortef is started from 30 seconds (for example, a dose of 100 mg) and up to 10 minutes (for example, a dose of 500 mg or more, if necessary). In high doses, the drug can be used only until the patient's condition stabilizes, but no more than 48–72 hours.
The initial dose is determined by the severity of the patient's condition and may be 100–500 mg or more. Every 2, 4 or 6 hours, the drug is re-administered at a dose that the doctor determines individually, depending on the clinical picture and the patient's response to therapy.
For children, Solu-Cortef is administered at lower doses (but not less than 25 mg per day), however, when determining the dose, they are guided primarily not by age and body weight, but by the severity of the condition and the child's response to therapy.
Preparation of a solution from a lyophilisate in a transparent glass vial
For intramuscular and intravenous administration of the drug into a vial with a lyophilisate, observing the rules of asepsis, add no more than 2 ml of water for injection or an aqueous solution of sodium chloride for injection with a bacteriostatic additive. For intravenous infusion, the reconstituted solution can be added to 100-1000 ml of an aqueous solution of 5% dextrose (or a solution of sodium chloride 0.9%, or a solution of dextrose 5% in a solution of sodium chloride 0.9%, if there is no need to limit the patient's amount of sodium).
Preparation of a solution from a lyophilisate in a two-volume ACT-O-VIAL vial
- Press the plastic activator so that the solvents from the upper container are poured into the lower one.
- Gently shake the bottle until the lyophilisate is completely dissolved.
- Remove the plastic disc from the center of the plug.
- Treat the surface of the cork with an antiseptic solution.
- Pierce the center of the plug with a needle so that its tip is visible.
- Turn the bottle over and withdraw the required volume of solution with a syringe.
For intramuscular and intravenous injection of the drug, further dilution is not required.
For intravenous infusion, a solution prepared as described above is added to 100-1000 ml of an aqueous solution of 5% dextrose (or a solution of sodium chloride 0.9%, or a solution of dextrose 5% in a solution of sodium chloride 0.9%, if not necessary limit the amount of sodium to the patient). If a small amount of liquid is required, then 100-3000 mg of sodium hydrocortisone succinate can be added to 50 ml of any of the solutions listed.
Ready solutions remain stable for 4 hours. They can be administered directly into a vein or through a second dropper.
If solutions are prepared according to the scheme described above, then their pH = 7-8, osmolarity = 0.36 osmol (osmolarity of 0.9% sodium chloride solution is 0.28 osmol).
Side effects
The side effects listed below are characteristic not only of hydrocortisone, but also of all glucocorticosteroids administered parenterally:
- on the part of metabolism: negative nitrogen balance (due to protein catabolism);
- on the part of the water and electrolyte balance: fluid / sodium retention in the body, potassium loss, increased calcium excretion, hypokalemic alkalosis, arterial hypertension, chronic heart failure in patients with a predisposition to this disease;
- on the part of the endocrine system: increased need for insulin or oral hypoglycemic agents in patients with diabetes mellitus, manifestation of latent diabetes mellitus, decreased glucose tolerance, development of Itsenko-Cushing syndrome, suppression of the function of the pituitary-adrenal system, menstrual irregularities in women, growth retardation in children;
- from the digestive system: esophagitis, gastric bleeding, bowel perforation, pancreatitis, peptic ulcer with possible perforation and bleeding (antacid therapy can be prescribed as a prophylaxis), increased serum alkaline phosphatase, increased activity of liver enzymes (alanine aminotransferase and aspartate aminotransferase);
- from the immune system: hypersensitivity reactions (including anaphylaxis and anaphylactic reactions, for example, urticaria, laryngeal edema, bronchospasm), suppression of reactions during skin tests, activation of latent infections (including tuberculosis reactivation), erased clinical picture in infectious diseases, the development of infections of any localization caused by opportunistic pathogens (can occur both in a mild form and in a severe form with a risk of death);
- from the nervous system: pseudotumor of the brain, increased intracranial pressure with edema of the optic nerve head, seizures, acute psychotic manifestations, mental disorders (including mood instability, insomnia, depression, personality change, euphoria), increased existing emotional instability or propensity for psychotic reactions;
- from the senses: increased intraocular pressure, posterior subcapsular cataract, exophthalmos;
- on the part of the musculoskeletal system: muscle weakness, tendon ruptures (especially the Achilles tendon), steroid myopathy, aseptic necrosis of the epiphyses of tubular bones, osteoporosis, compression fractures of the vertebrae, pathological fractures;
- on the part of the skin: decreased strength and thinning of the skin, ecchymosis, petechiae, slow healing, Kaposi's sarcoma (after the cancellation of Solu-Cortef, clinical remission may occur);
- others: when using the drug in two-volume ACT-O-VIAL vials in newborns - gasping Syndrome with a possible fatal outcome (due to the presence of benzyl alcohol in the solvent).
Overdose
The clinical symptoms of acute hydrocortisone overdose have not been described.
The drug is excreted during dialysis.
special instructions
Patients who may be exposed to stress during GCS therapy, before stress, during and after a stressful situation, require an increase in the dose of Solu-Cortef. Patients need strict medical supervision, which is associated with the risk of developing adrenal insufficiency.
With active tuberculosis, the use of Solu-Cortef should be limited to cases of disseminated or fulminant course of the disease, while the drug must be administered against the background of appropriate anti-tuberculosis chemotherapy. When corticosteroids are prescribed to patients with positive tuberculin tests or latent tuberculosis, reactivation of the disease is possible, therefore, careful medical supervision of the treatment is required. With prolonged use of Solu-Cortef, appropriate preventive treatment is indicated.
Hydrocortisone can increase blood pressure, retain salt and water in the body, and enhance the excretion of potassium. During the period of therapy, some patients require salt restriction and additional potassium supplementation. All glucocorticosteroids increase the excretion of calcium from the body.
Parenteral therapy with GCS in rare cases can cause anaphylactoid reactions (for example, bronchospasm), therefore, before the administration of Solu-Cortef, appropriate preventive measures should be taken, especially in patients with a history of allergic reactions to drugs.
Patients receiving Solu-Cortef in immunosuppressive doses are contraindicated to administer live and live attenuated vaccines. If necessary, inactivated or killed vaccines should be used, however, the likelihood of a decrease in the response to their administration should be considered. When using the drug in doses that do not have an immunosuppressive effect, vaccination is not contraindicated.
Against the background of glucocorticosteroid therapy, some infectious processes can proceed in an erased form (without obvious clinical manifestations), the development of new infections is possible due to a decrease in the body's resistance, a decrease in the body's ability to localize the infectious process. The development in various systems of the body of infections caused by pathogenic organisms (bacteria, viruses, fungi, protozoa, helminths) may be associated with the use of both Solu-Cortef and concomitant immunosuppressants that affect the function of neutrophils, cellular and humoral immunity. These diseases can be moderate, but in some cases they can be severe, even fatal. The higher the doses of GCS are used, the greater the risk of developing infectious complications.
When high doses of hydrocortisone are used for more than 48–72 hours, hypernatremia may develop. In this case, Solu-Cortef is replaced with another corticosteroids, against the background of treatment with which sodium retention in the body does not occur or occurs to an insignificant extent (for example, methylprednisolone sodium succinate).
In violation of neuromuscular transmission (for example, in patients with myasthenia gravis) and with the simultaneous use of peripheral muscle relaxants (for example, pancuronium), high doses of GCS often cause acute myopathy. This disease is generalized in nature, can affect the muscles of the eyes and the respiratory system, sometimes leads to tetraparesis, an increase in the content of creatine phosphokinase is also possible. After the abolition of GCS, improvement and recovery can occur only after a few weeks and even years.
In children, with prolonged daily use of Solu-Cortef, growth retardation is possible, therefore, treatment of pediatric patients for a long time can only be carried out in the presence of serious, threatening indications.
Influence on the ability to drive vehicles and complex mechanisms
Solu-Cortef can cause side effects on the part of the organ of vision and the nervous system, therefore, during the period of therapy, special care should be taken in any work with potentially dangerous consequences if they require a speed of reactions and / or a high concentration of attention, including driving vehicles and control of complex mechanisms.
Application during pregnancy and lactation
According to the results of animal studies, it was found that when using GCS in pregnant females in high doses, the fetus may develop deformities. Appropriate studies on the effect of GCS on human reproductive function have not been conducted, therefore, the use of all glucocorticosteroids in pregnant women and women of childbearing age is possible only if there are absolute indications and if the expected benefit is definitely higher than the potential risks.
Hydrocortisone easily crosses the placenta. Newborns whose mothers received high doses of Solu-Cortef during pregnancy should be carefully examined in order to identify signs of possible adrenal insufficiency in time. The effect of GCS on the course of labor and delivery is unknown.
Hydrocortisone passes into breast milk. If Solu-Cortef is required during lactation, breastfeeding should be discontinued.
Pediatric use
Newborns are contraindicated in the appointment of Solu-Cortef in two-volume ACT-O-VIAL vials, which is due to the content of benzyl alcohol in the solvent, a compound that can cause suffocation, fraught with death.
With impaired renal function
If the patient has impaired renal function, Solu-Cortef should be used with caution, under the supervision of a physician.
Drug interactions
Solu-Cortef can increase the clearance of acetylsalicylic acid (ASA), which is used for a long time in high doses, as a result of which the concentration of salicylates in the serum may decrease, and the risk of salicylate toxicity after corticosteroid withdrawal is also possible. This combination should be used with caution in patients with hypoprothrombinemia.
Hydrocortisone can have different effects on indirect anticoagulants: increase or decrease their effect. In this regard, during the period of combined therapy, it is required to constantly determine the indicators of blood clotting.
Some drugs, such as ketoconazole and troleandomycin, can inhibit metabolism and reduce the clearance of hydrocortisone, which requires a decrease in the Solu-Cortef dose to avoid the development of an overdose.
Inducers of liver microsomal enzymes, such as rifampicin, phenobarbital, and phenytoin, can increase the clearance of hydrocortisone, which requires an increase in its dose to obtain the desired therapeutic effect.
Analogs
Solu-Cortef analogs are: Betaspan Depot, Hydrocortisone, Dexazone, Dexamed, Dexamethasone, Ivepred, Metipred, Prednisol, Prednisolone, Solu-Medrol, etc.
Terms and conditions of storage
Keep out of the reach of children at a temperature of 15-25 ° C. The reconstituted solution can be stored in a place protected from light at room temperature for no more than 72 hours.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Solu-Cortefe reviews
The drug is used mainly in hospitals and often as part of complex therapy, therefore, there are no reviews on Solu-Kortefe on specialized medical sites that would allow assessing its effectiveness and tolerance.
The price of Solu-Cortef in pharmacies
The approximate price for Solu-Cortef is 90-101 rubles. for 1 colorless glass or double-volume bottle.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
