Celeston

The drug Celestone belongs to the pharmacological group of synthetic adrenocortical steroids (adrenal cortex hormones). ATC code H02A B01.

Other trade names: Betamethasone, Diprospan, Betaspan Depot, Minizon, Supercorten, Flosteron.

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Indications Celeston

Due to its strong anti-inflammatory, anti-allergic and anti-itching effects, Celestone is used:

• for allergic conditions and reactions of various etiologies, asthma, atopic and contact dermatitis, serum sickness;
• for dermatological diseases (bullous herpetiform dermatitis, exfoliative erythroderma, pemphigus, erythema multiforme);
• in case of endocrine disorders (congenital adrenal hyperplasia, adrenocortical insufficiency, hypercalcemia, inflammation of the thyroid gland);
• for gastrointestinal pathologies (enteritis, ulcerative colitis);
• in hematology (with autoimmune hemolytic anemia, secondary thrombocytopenia, etc.);
• in nephrology (for inflammation and various dysfunctions of inflammatory etiology);
• in the treatment of rheumatic diseases (gouty arthritis, acute rheumatic carditis, ankylosing spondylitis, systemic lupus erythematosus, psoriatic and rheumatoid arthritis, etc.).

Celestone can also be prescribed to cancer patients for palliative therapy of leukemia and lymphoma, metastatic brain tumors; patients with exacerbation of multiple sclerosis or cerebral edema; in anti-tuberculosis therapy, for inflammatory processes in otolaryngology and ophthalmology.

Intramuscular or intravenous administration of Celestone is indicated in cases of shock, acute cerebral edema and tetanus. As a prophylactic agent, the drug is used in kidney transplantation and to prevent respiratory distress in newborns during premature birth.

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Release form

Tablets of 0.5 mg; solution for parenteral use in ampoules of 1 ml.

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Pharmacodynamics

The active ingredient of Celestone is a long-acting fluorinated corticosteroid, betamethasone sodium phosphate. Its mineralocorticoid activity is less pronounced due to the presence of a β-methyl group, which enhances the anti-inflammatory effect and reduces the ability of fluorine to retain water and sodium.

The pharmacodynamics of this drug is based on the binding of the active substance to specific cell receptors and penetration into the cell nucleus, after which the synthesis of lipocortin protein increases, which suppresses the anti-inflammatory activity of cyclogenases, phospholipases and other inflammatory factors. This stabilizes the cytoplasmic membranes of inflamed tissues and reduces the formation of antibodies.

Like all GCS, Celestone has an immunosuppressive effect, helping to reduce the synthesis of T- and B-lymphocytes, reduce the production of γ-interferon and interleukins by lymphocytes and macrophages, and block the release of mediators of allergic reactions, in particular histamine, synthesized by mast cells into the systemic bloodstream.

As a result of intracellular biochemical changes, there is a neutralization of intercellular adhesion molecules on the membranes of endothelial cells and a stop in the movement of leukocytes to the site of inflammation, as well as the production of proteolytic enzymes and tissue plasminogen activator.

The use of Celestone in shock conditions not only restores the sensitivity of receptors to adrenaline, noradrenaline and dopamine, but also increases the level of catecholamines in the blood, stimulating the functions of the most important organs and general metabolism.

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Pharmacokinetics

With any method of application, Celestone penetrates well into tissues and enters the bloodstream, reaching maximum concentrations in plasma after 60-90 minutes.

Betamethasone sodium phosphate undergoes biotransformation by liver enzymes to form inactive metabolites. The drug is excreted from the body in the urine (the half-life is approximately five hours). But its biological activity at a standard dosage is manifested within one and a half to two days.

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Dosing and administration

Celestone can be administered intravenously, intramuscularly, into joint cavities and soft tissues (intralesional); in emergency cases (shock, cerebral edema) - intravenously 2-4 mg three times a day (with sodium chloride or glucose solution).

At the beginning of treatment, the daily dose of the drug in tablet form is 0.25-8 mg for adults and 0.02-0.25 mg per kilogram of body weight for children.

The dose is determined for each patient individually – in accordance with the diagnosis and severity of the disease.

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Use Celeston during pregnancy

Celestone, like any other corticosteroid, should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Children born to women who took corticosteroids during pregnancy should be closely monitored for signs of hypoadrenalism (Addison's disease).

According to the FDA, Celestone's effects on the fetus are classified as risk category C.

Contraindications

Contraindications to the use of the drug Celestone include:

• systemic fungal infection;
• infection with herpes virus (HSV, Herpes zoster), chickenpox virus (zoster virus) or rubella virus (Rubella virus);
• latent or active amebiasis;
• active form of tuberculosis;
• HIV infection;
• severe functional insufficiency of the kidneys or liver;
• inflammation of the lining of the stomach (gastritis) or esophagus (esophagitis);
• acute stage of gastric ulcer and duodenal ulcer;
• inflammation of the diverticula of the colon;
• myocardial infarction, acute heart failure, hypertension;
• diabetes mellitus;
• autoimmune myasthenia gravis;
• acute forms of mental disorders;
• recent vaccination.

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Side effects Celeston

The use of the drug Celestone may cause the following side effects:

• allergic reactions, anaphylactic shock, Quincke's edema;
• exacerbation of intercurrent infections;
• heart rhythm disturbances (bradycardia or tachycardia), increased blood pressure, pulmonary edema, fainting, thromboembolism, myocardial rupture after a recent infarction, cardiac arrest;
• acne, allergic dermatitis, atrophy of the skin and subcutaneous tissue (at the site of parenteral administration), increased dryness of the skin with hyperkeratosis, hematomas and petechiae, erythema, hyper- or hypopigmentation, poor wound healing, hyperhidrosis, striae, thinning of the skin and hair;
• decreased glucose tolerance, glucosuria, hirsutism, growth retardation in children;
• nausea, bloating and intestinal distension, increased appetite, hepatomegaly; inflammation of the pancreas, stomach ulcer with possible perforation and bleeding;
• loss of muscle mass and muscle weakness, osteoporosis (with pathological bone fractures), steroid myopathy;
• headaches and dizziness, convulsions and paresthesia, increased intracranial pressure, neuropathy, depression, emotional instability, mental disorders.

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Overdose

An overdose is possible if the dosage regimen is not followed and is fraught with not only an increase in all side effects, but also the development of secondary (medicinal) adrenal insufficiency.

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Interactions with other drugs

The instructions for Celestone note that its combined use with NSAIDs or ethanol can cause gastrointestinal ulceration, with diuretics - hypokalemia, and with cardiac glycosides - increase the risk of cardiac arrhythmia.

Macrolide antibiotics and barbiturates reduce the effectiveness of Celeston, while estrogen-containing agents (including oral contraceptives) increase its effect.

Concomitant use of anticholinesterase drugs and GCS may worsen the condition of patients with myasthenia. Since corticosteroids increase blood glucose levels, it may be necessary to adjust the dose of drugs for the treatment of diabetes. Vaccinations should not be performed during the administration of Celeston due to the immunosuppressive effect of corticosteroids.

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Storage conditions

Store away from daylight, t +15-30°C.

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Shelf life

Tablets – 36 months, solution – 24 months.