Product Information
Registration Status: ActiveXEPASONE TABLET 5mg is approved to be sold in Singapore with effective from 1990-04-17. It is marketed by APEX PHARMA MARKETING PTE LTD, with the registration number of SIN04190P.
This product contains Prednisolone 5mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by XEPA-SOUL PATTINSON (MALAYSIA) SDN BHD in MALAYSIA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. [PubChem]
Indication
For the treatment of primary or secondary adrenocortical insufficiency, such as congenital adrenal hyperplasia, thyroiditis. Also used to treat psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis and epicondylitis. Also indicated for treatment of systemic lupus erythematosus, pemphigus and acute rhematic carditis. Can be used in the treatment of leukemias, lymphomas, thrombocytopenia purpura and autoimmune hemolytic anemia. Can be used to treat celiac disease, insulin resistance, ulcerative colitis and liver disorders.
Mechanism of Action
Glucocorticoids such as Prednisolone can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisolone reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Prednisolone is a glucocorticoid receptor agonist. On binding, the corticoreceptor-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 an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.
Pharmacokinetics
- Absorption
- Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration.
- Distribution
- Metabolism
- Excreted in the urine as either free or glucoconjugate.
- Elimination
Toxicity
LD50=500 mg/kg (oral, rat), short-term side effects include high blood glucose levels and fluid retention. Long term side effects include Cushing's syndrome, weight gain, osteoporosis, glaucoma, type II diabetes and adrenal suppression.
Active Ingredient/Synonyms
(11beta)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione | 1,4-Pregnadiene-11beta,17alpha,21-triol-3,20-dione | 1,4-Pregnadiene-3,20-dione-11beta,17alpha,21-triol | 3,20-dioxo-11beta,17alpha,21-Trihydroxy-1,4-pregnadiene | delta-dehydrocortisol | delta-dehydrohydrocortisone | delta-hydrocortisone | delta(1)-Dehydrocortisol | delta(1)-Dehydrohydrocortisone | delta(1)-Hydrocortisone | Hydroretrocortine | Metacortandralone | PRDL | Prednisolona | Prednisolonum | Prednisolone |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.