Product Classification:
Glucocorticosteroid
Recommended Dosage:
20-30 mg per day
Acne:
No
Water Retention:
No
HBR:
Possible
Hepatotoxicity:
No
Aromatization:
No
Manufacturer:
Pfizer
Warehouse Location:
International Warehouse 2
Active Substance:
Prednisolone
Deltacortril is a potent glucocorticosteroid designed to effectively modulate leukocyte and macrophage activity. By limiting leukocyte migration to inflamed regions and disrupting the phagocytic and interleukin-1 production capabilities of macrophages, Deltacortril plays a crucial role in managing inflammation. Additionally, it stabilizes lysosomal membranes, reducing the concentration of proteolytic enzymes during inflammatory responses. This remarkable medication also decreases capillary permeability triggered by histamine and inhibits the activity of fibroblasts and collagen synthesis.
The mechanism of action involves inhibiting phospholipase A2, which subsequently lowers the production of prostaglandins and leukotrienes. Furthermore, Deltacortril suppresses the release of COX enzymes, particularly COX-2, leading to a significant reduction in prostaglandin synthesis.
This powerful medication is known to decrease circulating levels of lymphocytes (both T and B cells), monocytes, eosinophils, and basophils by directing them from the bloodstream into lymphoid tissues, simultaneously suppressing antibody formation.
Deltacortril also reduces ACTH and beta-lipotropin release from the pituitary gland without affecting beta-endorphin levels in circulation, while inhibiting TSH and FSH secretion.
When administered directly into blood vessels, Deltacortril exhibits a vasoconstrictive effect.
Metabolically, Deltacortril has significant, dose-dependent impacts on carbohydrate, protein, and fat metabolism. It promotes gluconeogenesis and enhances amino acid uptake in the liver and kidneys, boosting gluconeogenesis enzyme activity. In the liver, it increases glycogen storage while facilitating glucose synthesis from protein metabolite products. This leads to elevated blood glucose levels and stimulates insulin secretion.
Deltacortril also reduces glucose absorption in adipocytes, resulting in heightened lipolysis, though the increased insulin secretion ultimately encourages lipogenesis, contributing to fat accumulation.
Moreover, Deltacortril exhibits catabolic effects on lymphoid and connective tissues, muscle, 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. Long-term use of corticosteroids can lead to complications such as osteoporosis and Cushing's syndrome, with potential growth inhibition in children.
At high doses, prednisone may elevate brain tissue excitability and lower the convulsive threshold, alongside increasing hydrochloric acid and pepsin production in the stomach, which raises the risk of peptic ulcers.
Deltacortril?s therapeutic efficacy is derived from its anti-inflammatory, antiallergic, immunosuppressive, and antiproliferative properties. When used topically or externally, its effectiveness is mainly attributed to its anti-inflammatory and vasoconstrictive effects.
In comparison to hydrocortisone, Deltacortril's anti-inflammatory potency is four times greater, while its mineralocorticoid activity is approximately 60% less.
Indications for Deltacortril:
For both oral and parenteral administration, it is indicated for various 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, hypoglycemia, lipid nephrosis, agranulocytosis, certain leukemias, lymphomas, thrombocytopenic purpura, hemolytic anemia, chorea, and multiple skin conditions such as pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, seborrheic dermatitis, systemic lupus erythematosus (SLE), erythroderma, and hair loss.
For intra-articular use, it is beneficial for chronic arthritis, post-traumatic arthritis, osteoarthritis in larger joints, and rheumatic joint destruction.
For tissue infiltration, it is indicated for epicondylitis, tenosynovitis, bursitis, frozen shoulder, keloids, sciatica, Dupuytren's contracture, and various joint and soft tissue disorders.
In ophthalmology, it is prescribed for allergies, chronic and atypical conjunctivitis, blepharitis, corneal inflammation with intact mucosa, acute and chronic anterior choroid inflammation, sclera and episcleritis, sympathetic eye inflammation, and post-injury or post-surgery care.
Dosage and Administration:
For oral administration in adults requiring replacement therapy, the initial dose is 20-30 mg, with a maintenance dose of 10-15 mg daily. Initial doses may vary from 15-100 mg per day, with maintenance doses between 5-15 mg daily, necessitating gradual tapering. For children, a starting dose of 1-2 mg/kg divided into 4-6 doses is advised, with maintenance doses of 3-6 mg/kg per day.
For intramuscular or intravenous administration, the frequency and duration are personalized based on individual needs.
For intra-articular administration: 25-50 mg is used for larger joints, 10-25 mg for medium-sized joints, and 5-10 mg for smaller joints. For tissue infiltration, doses from 5 mg to 50 mg are applied depending on the severity of the condition.
In ophthalmology, Deltacortril is typically administered three times daily for no more than 14 days; in dermatology, it is used once to three times daily.
Side Effects and Adverse Reactions:
Endocrine system: May cause menstrual irregularities, adrenal suppression, Cushing's syndrome, pituitary-adrenal suppression, decreased carbohydrate tolerance, steroid diabetes, growth retardation in children, and delayed sexual development.
Digestive system: Possible side effects include nausea, vomiting, steroid-induced peptic and duodenal ulcers, pancreatitis, esophagitis, gastrointestinal bleeding, appetite changes, flatulence, and hiccups. There may also be rare increases in liver transaminases and alkaline phosphatase levels.
Metabolic effects: Can lead to negative nitrogen balance due to protein catabolism, increased calcium excretion resulting in hypocalcemia, weight gain, and hyperhidrosis (excessive sweating).
Cardiovascular system: Risks include potassium depletion, hypokalemic alkalosis, arrhythmias, bradycardia, steroid myopathy, worsening heart failure symptoms, ECG changes indicative of hypokalemia, elevated blood pressure, increased risk of thrombosis, and potential complications following an acute myocardial infarction.
Musculoskeletal system: Potential impacts include inhibited growth and ossification in children (risk of early epiphyseal closure), osteoporosis, rare pathological fractures, necrosis of the shoulder head and femur, tendon ruptures, muscle weakness, steroid myopathy, and muscle wasting.
Central nervous system: Symptoms may include headaches, increased intracranial pressure, confusion, mood swings (from euphoria to depression), anxiety, insomnia, dizziness, vertigo, pseudo-tumors of the brain, and seizures.
Vision: Risks involve posterior subcapsular cataracts, increased intraocular pressure potentially affecting the optic nerve, corneal trophic changes, exophthalmos, and increased susceptibility to secondary infections (bacterial, fungal, and viral).
Dermatological effects: Possible reactions include small red spots (petechiae), bruising (ecchymosis), thinning and fragility of the skin, pigmentation changes, acne, stretch marks, and heightened risk of skin infections like pyoderma and candidiasis.
Immunosuppressive reactions: May manifest as slower healing rates and reduced infection resistance. Rare cases following parenteral administration may involve anaphylactic and allergic reactions, skin pigmentation changes, tissue atrophy, exacerbation of existing conditions, sterile abscess formation, and complications from intrasynovial injections that could lead to blindness.