Rectodelt

Rectodelt is a drug from the GCS group (for systemic use), which has a non-fluorinated form.

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Indications Rectodelt

It is used in children – for intensive combined treatment of false croup (acute croup syndrome), as well as true croup (diphtheria form) and bronchial obstruction.

Release form

The drug is released in the form of rectal suppositories, which contain 0.1 g of prednisone. Inside a separate pack there are 2, 4 or 6 suppositories.

Pharmacodynamics

The drug has an effect, the severity of which depends on the size of the portion of the drug; in addition, it affects tissue metabolism processes. With its help, the body's homeostasis processes can be maintained under stress and at rest. At the same time, the drug is a participant in immunoregulation processes.

When the dose used for replacement therapy is exceeded, the drug causes a powerful anti-inflammatory effect (anti-exudative and antiproliferative activity), and at the same time a delayed immunosuppressive effect. The substance suppresses the activity of immune cells and chemotaxis, and in addition, the processes of releasing inflammatory conductors and the body's immune response (leukotrienes, PG and lysosome enzymes).

When used during bronchial obstruction, the active element of the drug potentiates the power of bronchodilation that develops under the influence of β-mimetics.

Long-term administration in large doses leads to involution of the adrenal cortex with immunity.

The mineralocorticoid effect of Rectodelt (less intense than with hydrocortisone) requires monitoring of plasma electrolyte values during therapy.

The active component of the drug helps improve the patency of the respiratory tract - reducing the intensity of inflammation, preventing the development of mucosal edema, slowing the onset of bronchial spasm and reducing the force of mucus secretion (while simultaneously weakening its viscosity). Such effects develop by strengthening vascular membranes and stabilizing cell walls, and at the same time increasing the susceptibility of the bronchial muscles to β2-sympathomimetics and suppressing type 1 immune responses (develops from the 2nd week of drug use).

Pharmacokinetics

Blood indicators of GCS are noted quite quickly after the administration of the suppository, from which it can be concluded that the drug has a high level of bioavailability and active absorption.

Prednisone inside the body is quickly transformed into an active metabolic product - prednisolone. Both of these elements can be mutually transformed, but inside the human body, prednisolone is mostly contained. The bioavailability of the drug is about 29%.

Prednisolone is synthesized with transcortin and plasma protein. The drug clearance rate is about 1.5 ml/minute/kg. About 2-5% of the substance is excreted unchanged in the urine, and up to 24% is excreted as prednisolone. The remainder is excreted as other metabolic products.

Dosing and administration

The medicine is prescribed to infants and children over 6 months of age, in the amount of 1 suppository per day (the maximum daily dose is thus 0.1 g of the substance). The duration of such treatment is determined by the course of the pathology.

To stop an acute lesion, a 2-day treatment cycle is required. If there is an extreme need, the therapy can be repeated once. It is not recommended to conduct longer courses of therapy. A maximum of 0.2 g of the drug is allowed to be used over 2 days.

Suppositories are inserted deep into the rectum.

It is recommended to use suppositories in children who cannot undergo intravenous, intramuscular or oral administration of drugs (due to stress, inadmissibility of use or development of complications).

If the optimal dose is exceeded or the recommended treatment regimen is deviated from, complications may develop, expressed in the form of severe negative manifestations.

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Use Rectodelt during pregnancy

There have been no adequate tests of the use of the drug in pregnant and breastfeeding women. The drug has only been studied in animals. In this case, the occurrence of a teratogenic and embryotoxic effect was discovered - abnormal development of the skeletal structure, slowing of fetal development in the womb, and death of the embryo.

In addition, an increase in the likelihood of developing deformities was observed in the case of using the drug in the first trimester.

The use of Rectodelt in animals has also demonstrated that the introduction of subteratogenic doses increases the likelihood of delays in intrauterine development, metabolic disorders in adults, and in addition, the appearance of pathologies in the cardiovascular system and changes in the duration of transmission of neural reactions with impulses.

Administration of the drug in the 3rd trimester in animals revealed that the infant may develop adrenal cortex atrophy. In such cases, replacement therapy for the newborn is required.

The drug can be prescribed during pregnancy, but only in extreme cases and when it is determined that the likelihood of risk to the fetus is lower than the benefit to the woman.

Prednisone with prednisolone, which are the components of the drug, pass into the mother's milk, although there is no information that they cause harm to the baby. However, if there is an urgent need to use the drug in large portions, it is necessary to stop breastfeeding for this period.

Contraindications

It is contraindicated to prescribe the drug if the patient has been diagnosed with intolerance to any of its components.

There are no contraindications for short-term treatment to relieve urgent, acute and life-threatening conditions.

Side effects Rectodelt

In the case of administration of the drug in emergency cases, the only negative symptom may be an immune reaction - the development of severe sensitivity.

Long-term use of the drug can provoke the development of various side effects:

• endocrine dysfunction: the appearance of cushingoid of varying severity. Symptoms such as obesity, metabolic syndrome against the background of diabetes, moon face, growth retardation, hyperglycemia (which may result in steroid diabetes), disorder of sex hormone secretion, depletion of the adrenal cortex (which may lead to atrophy), changes in hemogram readings and hirsutism may also occur;
• problems with metabolic processes: negative nitrogen balance values, sodium and fluid retention in the body, as well as hypokalemia;
• disturbances in the functioning of the cardiovascular system: weakening of the strength of blood vessels and increased blood pressure;
• damage to the blood system: increased blood clotting;
• disorders of the musculoskeletal structure: muscle atrophy, osteoporosis, and also bone necrosis of aseptic origin;
• epidermal lesions: acne, striae, skin atrophy, and telangiectasia;
• disorders affecting visual activity: steroid-induced cataracts and manifestation of latent glaucoma;
• problems with the central nervous system: mental disorders;
• manifestations from the gastrointestinal tract: pancreatitis or ulcers in the gastrointestinal tract (associated with an ulcerogenic effect on the gastrointestinal tract and an increase in gastric pH values);
• symptoms associated with the immunosuppressive effect: slowing of wound healing processes and decreased resistance of the body to various infections.

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Overdose

There is no information on the development of acute overdose with any form of GCS. In case of poisoning, it is necessary to take into account the existing probability of developing pronounced symptoms - mainly related to endocrine function, as well as metabolic disorders and salt balance.

The medication has no antidote, so if any problems occur, symptomatic measures are taken.

Interactions with other drugs

Various enzyme inducers (including phenytoin with barbiturates and rifampicin with primidone) reduce the therapeutic properties of Rectodelt.

Use with estrogen agents leads to increased effects of the drug.

Combination with atropine or other anticholinergics may lead to an increase in IOP.

Combination with salicylates or NSAIDs increases the likelihood of bleeding in the gastrointestinal tract.

When using the drug, it should be remembered that it reduces the effectiveness of insulin, hypoglycemic agents and coumarin derivatives.

Combination with SG enhances their therapeutic effect due to the loss of potassium, which is induced by the activity of steroids.

Concomitant use with saluretics may lead to potentiation of potassium excretion.

When using the medication, the blood level of the substance praziquatel may decrease.

Administration together with ACE inhibitors significantly increases the likelihood of changes in hemogram readings.

Chloroquine and mefloquine with hydrochloroquine, used together with the drug, increase the risk of developing cardiomyopathy and myopathy.

The drug weakens the medicinal effect of the substance STH.

Use in combination with protirelin leads to a slowdown in the elimination processes of Rectodelt.

The drug increases blood levels of cyclosporine, which increases the likelihood of developing a convulsive syndrome of central origin.

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Storage conditions

Rectodelt should be kept in a place protected from moisture and sunlight. Temperature indicators are a maximum of 25°C.

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Shelf life

Rectodelt is allowed to be used within 36 months from the date of manufacture of the therapeutic agent.

Application for children

The medicine is not used for therapy in infants under 6 months of age.

Analogues

The drug's analogs include such medications as Betaspan, Medrol, Dexon and Hydrocortisone acetate with Metipred, as well as Dexamethasone, Celestone, Depo-medrol, Primacort with Diprospan, Prednisolone with Kenalog and Solu-medrol. Also on the list are Cort-s, Flosteron with Polcortolone and Methylprednisolone with Solu-cortef.

Reviews

Rectodelt is considered a very effective drug, but the reviews also say that it is necessary to take into account the presence of a large number of side effects - this is the main disadvantage of the drug, because otherwise the commentators agree that it really quickly and efficiently improves the patient's condition.