Deltacortril

CLASSIFICATION
Glucocorticosteroid
DOSAGE
20-30 mg/day
ACNE
No
WATER RETENTION
No
HBR
Possible
HEPATOTOXICITY
No
AROMATIZATION
No
MANUFACTURER
Pfizer
WAREHOUSE
International Warehouse 2
SUBSTANCE
Prednisolone

Deltacortril is a powerful glucocorticosteroid that expertly modulates leukocyte and macrophage activity. By restricting leukocyte migration to inflamed areas, it hampers macrophages' phagocytic capabilities and interleukin-1 production. Deltacortril also stabilizes lysosomal membranes, reducing the concentration of inflammatory proteolytic enzymes. Additionally, it effectively diminishes capillary permeability caused by histamine, while inhibiting fibroblast activity and collagen production.

This medication operates by inhibiting phospholipase A2, thereby lowering prostaglandin and leukotriene production. Its action extends to suppressing COX enzyme release, particularly COX-2, further curtailing prostaglandin synthesis.

Deltacortril significantly reduces circulating lymphocyte levels (both T and B cells), monocytes, eosinophils, and basophils by redirecting them from the bloodstream into lymphoid tissues and inhibiting antibody production.

It also curtails ACTH and beta-lipotropin release from the pituitary gland, without affecting beta-endorphin levels, and inhibits TSH and FSH secretion.

When administered directly to blood vessels, Deltacortril exhibits a vasoconstrictive effect.

Metabolically, Deltacortril has profound, dose-dependent effects on carbohydrate, protein, and fat metabolism. It promotes gluconeogenesis, enhances amino acid uptake in the liver and kidneys, and boosts gluconeogenesis enzyme activity. In the liver, it facilitates glycogen storage and glucose synthesis from protein metabolism products, leading to increased blood glucose levels and heightened insulin secretion.

While it reduces glucose absorption in fat cells, promoting lipolysis, this surge in insulin can also lead to fat accumulation through lipogenesis.

Moreover, Deltacortril exhibits catabolic effects on lymphoid and connective tissues, muscles, adipose tissue, skin, and bone. Compared to hydrocortisone, its influence on water and electrolyte metabolism is milder, promoting potassium and calcium loss while retaining sodium and fluid. Prolonged corticosteroid therapy can lead to conditions like osteoporosis and Cushing's syndrome, and may hinder growth in children.

At elevated doses, prednisone can heighten brain tissue excitability and lower convulsive thresholds, while potentially increasing hydrochloric acid and pepsin production in the stomach, raising the risk of peptic ulcers.

Deltacortril's therapeutic advantages stem from its anti-inflammatory, antiallergic, immunosuppressive, and antiproliferative properties. When used topically, its efficacy is attributed to its anti-inflammatory and vasoconstrictive effects.

Notably, Deltacortril's anti-inflammatory effects are four times more potent than those of hydrocortisone, while exhibiting approximately 60% less mineralocorticoid activity.

Administered orally or parenterally, Deltacortril is prescribed for a variety of conditions including rheumatism, rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, asthma, acute and chronic allergic reactions, anaphylaxis, Addison's disease, acute adrenal insufficiency, adrenal-genital syndrome, liver disorders, and more. It is effective for skin conditions such as pemphigus, eczema, psoriasis, systemic lupus erythematosus (SLE), and hair loss.

For intra-articular administration, it effectively treats chronic arthritis, post-traumatic arthritis, and osteoarthritis in larger joints.

When infiltrated into tissues, it addresses epicondylitis, tenosynovitis, bursitis, frozen shoulder, keloids, sciatica, and other joint and soft tissue disorders.

In the field of ophthalmology, Deltacortril is utilized for allergies, chronic conjunctivitis, blepharitis, corneal inflammation, anterior choroid inflammation, and post-injury care.

For adults requiring replacement therapy, the initial oral dose ranges from 20-30 mg, with maintenance doses of 10-15 mg daily. Adjustments may involve initial doses of 15-100 mg per day, tapering down to maintenance doses of 5-15 mg. For children, a starting dose of 1-2 mg/kg divided into 4-6 doses is recommended, with a maintenance dose of 3-6 mg/kg per day.

For intramuscular or intravenous administration, the frequency and duration are tailored to individual needs.

For intra-articular treatments, doses of 25-50 mg are used for larger joints, 10-25 mg for medium joints, and 5-10 mg for smaller joints. Tissue infiltration doses may range from 5 mg to 50 mg based on severity.

In ophthalmology, Deltacortril is applied three times daily for no more than 14 days; in dermatology, it can be used once to three times daily.

Endocrine side effects may include menstrual irregularities, adrenal suppression, Cushing's syndrome, and growth retardation in children. Digestive issues can manifest as nausea, vomiting, ulcers, and gastrointestinal bleeding. Metabolic disturbances may lead to weight gain, hypocalcemia, and increased sweating.

Cardiovascular effects include potassium loss, arrhythmias, elevated blood pressure, and risks associated with myocardial infarction. Musculoskeletal effects may involve inhibited growth in children, osteoporosis, and muscle weakness.

Central nervous system reactions can range from headaches to mood fluctuations, while ocular risks include cataracts and increased intraocular pressure. Dermatological effects may involve skin thinning, bruising, and increased susceptibility to infections.

Immunosuppressive reactions can result in slower healing and reduced infection resistance, with rare cases of anaphylaxis and allergic reactions for parenteral use.