Celeston

The drug Celeston refers to the pharmacological group of synthetic adrenocortical steroids (adrenal cortex gonads). ATS code H02A B01.

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

[1], [2], [3]

Indications Celeston

Due to its strong anti-inflammatory, anti-allergic and itching action, Celeston is used:

• at allergic conditions and reactions of different etiology, asthma, atopic and contact dermatitis, serum sickness;
• with dermatological diseases (bullous herpetiform dermatitis, exfoliative erythroderma, pemphigus, erythema multiforme);
• in the case of endocrine disorders (congenital adrenal hyperplasia, adrenocortical insufficiency, hypercalcemia, inflammation of the thyroid gland);
• with pathologies of the gastrointestinal tract (enteritis, ulcerative colitis);
• in hematology (with autoimmune hemolytic anemia, secondary thrombocytopenia, etc.);
• in nephrology (with 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.).

Also, Celeston can be prescribed by the oncology for palliative therapy of leukemias and lymphomas, a metastatic brain tumor; patients with exacerbation of multiple sclerosis or edema of the brain; in anti-tuberculosis therapy, in inflammatory processes in otolaryngology and ophthalmology.

Intramuscular or intravenous administration of Celeston is indicated in the case of shock, acute cerebral edema and tetanus. As a preventive agent, the drug is used for kidney transplantation and to prevent the breathing disorder of newborns during premature birth.

[4], [5], [6], [7]

Release form

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

[8], [9], [10]

Pharmacodynamics

The active substance of the drug Celeston is a fluorinated corticosteroid with long-acting betamethasone sodium phosphate. Its mineral corticoid activity is less pronounced due to the presence of the β-methyl group, which enhances the anti-inflammatory effect and reduces the property of fluoride to retain water and sodium.

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 the lipocortin protein, which suppresses the anti-inflammatory activity of cyclogenases, phospholipase and other inflammatory factors, is increased. At the same time, the cytoplasmic membranes of inflammatory tissues are stabilized and the formation of antibodies is reduced.

Like all GCS, Celeston has an immunosuppressive effect, contributing to a decrease in the synthesis of T and B lymphocytes, a reduction in the production of lymphocytes and macrophages of γ-interferon and interleukins and a blockade of the output of the mediators of allergic reactions, in particular histamine, in the systemic circulation of the mast cells.

As a result of intracellular biochemical changes, the molecules of intercellular adhesion on membranes of endotheliocytes are neutralized and the movement of leukocytes to the site of inflammation stops, as well as the production of proteolytic enzymes and a tissue activator of plasminogen.

The use of Celeston in shock states not only restores receptor sensitivity to adrenaline, noradrenaline and dopamine, but also increases the level of catecholamines in the blood, stimulating the functions of the major organs and the overall metabolism.

[11], [12], [13], [14]

Pharmacokinetics

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

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

[15], [16], [17], [18], [19], [20]

Use Celeston during pregnancy

The Celeston preparation - like any other corticosteroid - should be used during pregnancy only if the potential benefits justify the possible risk to the fetus. Children born to women taking corticosteroids during pregnancy should be carefully monitored for signs of hypoadrenalism (Addison's disease).

According to the FDA, the effect of Celeston on the fetus has a risk category of C.

Contraindications

Among the contraindications to the use of the preparation Celeston are noted:

• systemic fungal infection;
• Herpesvirus (HSV, Herpes zoster), virus zoster or rubella virus;
• latent or active amoebiasis;
• active form of tuberculosis;
• HIV infection;
• severe renal or hepatic insufficiency;
• inflammation of the gastric mucosa (gastritis) or esophagus (esophagitis);
• acute stage of peptic ulcer of stomach and duodenum;
• inflammation of the diverticulum of the large intestine;
• myocardial infarction, acute heart failure, hypertension;
• diabetes;
• autoimmune myasthenia gravis;
• acute forms of mental disorders;
• recent vaccination.

[21], [22], [23]

Side effects Celeston

The use of the drug Celeston can 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 heart attack, cardiac arrest;
• acne, atopic dermatitis, skin and subcutaneous atrophy (where parenteral administration), improved skin dryness with hyperkeratosis, hematoma and petechiae, erythema, hyper or hypopigmentation, poor wound healing, hyperhidrosis, striae, thinning of the skin and hair;
• a decrease in glucose tolerance, glucosuria, hirsutism, growth retardation in children;
• nausea, bloating and intestines, increased appetite, hepatomegaly; inflammation of the pancreas, stomach ulcers with possible perforation and bleeding;
• loss of muscle mass and weakness in muscles, osteoporosis (with pathological bone fractures), steroid myopathy;
• headaches and dizziness, seizures and paresthesia, increased intracranial pressure, neuropathy, depression, emotional imbalance, mental disorders.

[24], [25], [26]

Dosing and administration

Celeston can be administered intravenously, intramuscularly, into the joint cavity and soft tissue (intralesional); in case of emergency (shock, cerebral edema) - intravenously 2-4 mg three times a day (with a solution of sodium chloride or glucose).

At the beginning of the treatment, the daily dose of the drug in the form of tablets 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.

[27], [28]

Overdose

Overdose is possible if the regime of application is violated and is fraught not only by the intensification of all side effects, but also by the development of secondary (medicamentous) insufficiency of the adrenal glands.

[29], [30], [31], [32]

Interactions with other drugs

Celeston's instruction notes that its combined use with NSAIDs or ethanol can cause ulceration of the gastrointestinal tract, with diuretics - hypokalemia, and with cardiac glycosides - increase the risk of cardiac arrhythmia.

Reduce the effectiveness of Celeston antibiotics-macrolides and barbiturates, and increase the impact of estrogen-containing drugs (including oral contraceptives).

Simultaneous use of anticholinesterase drugs and GCS can worsen the condition of patients with myasthenia gravis. Since corticosteroids increase blood glucose levels, it may be necessary to adjust the dose of drugs to treat diabetes. During the reception of Celeston, vaccination can not be carried out because of the immunosuppressive effect of corticosteroids.

[33], [34], [35], [36], [37]

Storage conditions

Store without access to daylight, t + 15-30 ° C.

[38], [39], [40]

Shelf life

Tablets - 36 months, solution - 24 months.