Mildison - General Information
The main glucocorticoid secreted by the adrenal cortex. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions. [PubChem]
Pharmacology of Mildison
Mildison is the most important human glucocorticoid. It is essential for life and regulates or supports a variety of important cardiovascular, metabolic, immunologic and homeostatic functions. Topical hydrocortisone is used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Glucocorticoids are distinguished from mineralocorticoids and sex steroids by having different receptors, target cells, and effects. Technically, the term corticosteroid refers to both glucocorticoids and mineralocorticoids, but is often used as a synonym for glucocorticoid. Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and TNF-alpha, the most important of which is the IL-2. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, causing B cells to express lower amounts of IL-2 and IL-2 receptors. This diminishes both B cell clonal expansion and antibody synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte cells being activated.
Mildison for patients
Patients using topical corticosteroids should receive the following information and instructions:
- This medication is to be used as directed by the physician. It is for external use only. Avoid contact with the eyes.
- Patients should be advised not to use this medication for any disorder other than that for which it has been prescribed.
- The treated skin area should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by the physician.
- Patients should report any signs of local adverse reactions especially under occlusive dressing.
- Parents of pediatric patients should be advised not to use tight-fitting diapers or plastic pants on a child being treated in the diaper area, as these garments may constitute occlusive dressings.
No information available.
Topical corticosteroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.
Additional information about Mildison
Mildison Indication: For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addisons disease). It is also used to treat many immune and allergic disorders, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.
Mechanism Of Action: Mildison binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In another words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Drug Interactions: Ambenonium The corticosteroid decreases the effect of anticholinesterases
Edrophonium The corticosteroid decreases the effect of anticholinesterases
Neostigmine The corticosteroid decreases the effect of anticholinesterases
Pyridostigmine The corticosteroid decreases the effect of anticholinesterases
Aspirin The corticosteroid decreases the effect of salicylates
Bismuth Subsalicylate The corticosteroid decreases the effect of salicylates
Salicylate-magnesium The corticosteroid decreases the effect of salicylates
Salicylate-sodium The corticosteroid decreases the effect of salicylates
Salsalate The corticosteroid decreases the effect of salicylates
Trisalicylate-choline The corticosteroid decreases the effect of salicylates
Warfarin The corticosteroid alters the anticoagulant effect
Acenocoumarol The corticosteroid alters the anticoagulant effect
Dicumarol The corticosteroid alters the anticoagulant effect
Anisindione The corticosteroid alters the anticoagulant effect
Cholestyramine Cholestyramine decreases the effect of hydrocortisone
Colestipol Cholestyramine decreases the effect of hydrocortisone
Amobarbital The barbiturate decreases the effect of the corticosteroid
Aprobarbital The barbiturate decreases the effect of the corticosteroid
Butabarbital The barbiturate decreases the effect of the corticosteroid
Butalbital The barbiturate decreases the effect of the corticosteroid
Butethal The barbiturate decreases the effect of the corticosteroid
Dihydroquinidine barbiturate The barbiturate decreases the effect of the corticosteroid
Heptabarbital The barbiturate decreases the effect of the corticosteroid
Hexobarbital The barbiturate decreases the effect of the corticosteroid
Methohexital The barbiturate decreases the effect of the corticosteroid
Methylphenobarbital The barbiturate decreases the effect of the corticosteroid
Pentobarbital The barbiturate decreases the effect of the corticosteroid
Phenobarbital The barbiturate decreases the effect of the corticosteroid
Primidone The barbiturate decreases the effect of the corticosteroid
Quinidine barbiturate The barbiturate decreases the effect of the corticosteroid
Secobarbital The barbiturate decreases the effect of the corticosteroid
Talbutal The barbiturate decreases the effect of the corticosteroid
Rifampin The enzyme inducer decreases the effect of the corticosteroid
Phenytoin The enzyme inducer decreases the effect of the corticosteroid
Mephenytoin The enzyme inducer decreases the effect of the corticosteroid
Fosphenytoin The enzyme inducer decreases the effect of the corticosteroid
Ethotoin The enzyme inducer decreases the effect of the corticosteroid
Midodrine Increased arterial pressure
Food Interactions: Take with food to reduce irritation. Calcium, phosphorous, potassium, Vitamin A, C, D and zinc needs increased with long term use.
Generic Name: Hydrocortisone
Synonyms: 11beta-Hydroxycortisone; 17alpha-Hydroxycorticosterone; Anti-inflammatory hormone; Dihydrocostisone; Hidrocortisona [INN-Spanish]; Hydrocorticosterone; Hydrocortisone Acetate; Hydrocortisone alcohol; Hydrocortisone Base; Hydrocortisone Butyrate; Hydrocortisone free alcohol; Hydrocortisone Sodium Phosphate; Hydrocortisone Valerate; Hydrocortisonum [INN-Latin]; Hydroxycortisone; Idrocortisone [DCIT]
Drug Category: Anti-inflammatory Agents
Drug Type: Small Molecule; Approved
Absorption: Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.
Toxicity (Overdose): Side effects include inhibition of bone formation, suppression of calcium absorption and delayed wound healing
Protein Binding: 95%
Biotransformation: Primarily hepatic via CYP3A4
Half Life: 6-8 hours
Dosage Forms of Mildison: Liquid Topical
Powder, for solution Intramuscular
Powder, for solution Intravenous
Chemical IUPAC Name: (8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
Chemical Formula: C21H30O5
Hydrocortisone on Wikipedia: https://en.wikipedia.org/wiki/Hydrocortisone
Organisms Affected: Humans and other mammals