Radiocin - General Information
A glucocorticoid derivative used topically in the treatment of various skin disorders. It is usually employed as a cream, gel, lotion, or ointment. It has also been used topically in the treatment of inflammatory eye, ear, and nose disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732). It is also being investigatied by pSivida and Alimera, under the brand name Medidur, as a sustained release intraocular implant for the treatment of diabetic macular edema.
Pharmacology of Radiocin
Radiocin for patients
RETISERT is designed to locally treat inflammation in the eye, but it is not known to treat the underlying disease. Medication to treat the underlying disease may be prescribed concurrently as deemed appropriate by a physician. Patients should be advised to have ophthalmologic follow-up examinations of both eyes at appropriate intervals following implantation of RETISERT.
As with any surgical procedure, there is risk involved. Potential complications accompanying intraocular surgery to place RETISERT into the vitreous cavity may include, but are not limited to, the following: cataract formation, choroidal detachment, temporary decreased visual acuity, endophthalmitis, hypotony, increased intraocular pressure, exacerbation of intraocular inflammation, retinal detachment, vitreous hemorrhage, vitreous loss, and wound dehiscence.
Following implantation of RETISERT, nearly all patients will experience an immediate and temporary decrease in visual acuity in the implanted eye which lasts for approximately one to four weeks postoperatively. This decrease in visual acuity is likely a result of the surgical implant procedure.
Based on clinical trials with RETISERT, within 34 weeks post-implantation, approximately 60% of patients will require IOP lowering medications to control intraocular pressure. Within an average post-implantation period of approximately 2 years, approximately 32% of patients are expected to require filtering procedures to control intraocular pressure.
No information provided.
RETISERT is contraindicated in most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infections of the eye and fungal diseases of ocular structures. RETISERT is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.
Additional information about Radiocin
Radiocin Indication: For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Also for the treatment of chronic non-infectious uveitis affecting the posterior segment of the eye (Retisert).
Mechanism Of Action: Radiocin is a corticosteroid that 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. 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. Like other glucocorticoid agents Fluocinolone acetonide acts as a physiological antagonist to insulin by decreasing glycogenesis (formation of glycogen). It also promotes the breakdown of lipids (lipolysis), and proteins, leading to the mobilization of extrahepatic amino acids and ketone bodies. This leads to increased circulating glucose concentrations (in the blood). There is also decreased glycogen formation in the liver.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Fluocinolone Acetonide
Synonyms: Fluocinolonacetonidum; Fluocinolone acetonide [DCIT]; Fluocinoloni acetonidum [INN-Latin]
Drug Category: Anti-inflammatory Agents; Glucocorticoids; Antipruritics
Drug Type: Small Molecule; Approved; Investigational
Absorption: Rapidly absorbed (15 minutes)
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Primarily hepatic, corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys.
Half Life: 1.3-1.7 hours
Dosage Forms of Radiocin: Liquid Topical
Chemical IUPAC Name: Not Available
Chemical Formula: C24H30F2O6
Fluocinolone Acetonide on Wikipedia: https://en.wikipedia.org/wiki/Fluocinolone_acetonide
Organisms Affected: Humans and other mammals