Cortibiotan

Uses

Prednisolone is a glucocorticoid used to treat adrenocortical insufficiency, inflammatory conditions, and some cancers.

Prednisolone is indicated to treat endocrine, rheumatic, and hematologic disorders; collagen, dermatologic, ophthalmic, respiratory, and gastrointestinal diseases; allergic and edematous states; and other conditions like tuberculous meningitis.

Sulfacetamide sodium ophthalmic solution is used for the treatment of conjunctivitis and other superficial ocular infections due to susceptible microorganisms, and as an adjunctive in systemic sulfonamide therapy of trachoma: Escherichia coli, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus (viridans group), Haemophilus influenzae, Klebsiella species, and Enterobacter species.

Topically applied sulfonamides do not provide adequate coverage against Neisseria species, Serratia marcescens and Pseudomonas aeruginosa. A significant percentage of staphylococcal isolates are completely resistant to sulfa drugs.

Cortibiotan is also used to associated treatment for these conditions: Acne Rosacea, Acute Gouty Arthritis, Allergic Bronchopulmonary Aspergillosis, Allergic Contact Dermatitis, Allergic corneal marginal ulcers, Alveolitis, Extrinsic Allergic, Anal Fissures, Ankylosing Spondylitis (AS), Aspiration Pneumonitis, Atopic Dermatitis (AD), Bell's Palsy, Berylliosis, Bullous dermatitis herpetiformis, Burns, Chorioretinitis, Choroiditis, Chronic Obstructive Airways Disease Exacerbated, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Conjunctivitis, Corneal Inflammation, Corneal injuries, Corneal ulceration, Crohn's Disease (CD), Cyclitis, Dermatitis exfoliative generalised, Dermatitis, Contact, Dermatomyositis, Dermatosis of the Ear Canal, Drug hypersensitivity reaction, Edema of the cerebrum, Epicondylitis, Erythroblastopenia, Exacerbation of asthma, Eye inflammation caused by Cataract Surgery, Eye inflammation caused by Infection, Herpes Zoster Keratitis, Hot Water Burns (Scalds), Hypercalcemia of Malignancy, Idiopathic Pulmonary Fibrosis (IPF), Idiopathic Thrombocytopenic Purpura, Inflamed External Hemorrhoid, Inflamed Hemorrhoids, Internal, Inflammatory Reaction caused by susceptible Bacterial Infections, Iridocyclitis, Iritis, Itching caused by susceptible Bacterial Infections, Leukemia, Acute, Loeffler's syndrome, Malignant Lymphomas, Multiple sclerosis exacerbation, Mycosis Fungoides (MF), Ocular Inflammation, Ophthalmia, Sympathetic, Optic Neuritis, Otic Eczema, Pemphigus, Perennial Allergic Rhinitis (PAR), Pericarditis, Pneumocystis Jirovecii Pneumonia, Pneumonia, Aspiration, Polymyalgia Rheumatica, Post-traumatic Osteoarthritis, Proctitis, Proteinuria, Pruritus, Pruritus Ani, Psoriatic Arthritis, Pulmonary Tuberculosis (TB), Pure Red Cell Aplasia, Rash, Rejection, Transplant, Relapsing Polychondritis, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis, Secondary Adrenal Insufficiency, Secondary thrombocytopenia, Serum Sickness, Severe Asthma, Sjögren's Syndrome, Skin Infections, Bacterial, Stevens-Johnson Syndrome, Superficial punctate keratitis, Synovitis, Systemic Lupus Erythematosus (SLE), Trichinosis, Tuberculosis (TB), Tuberculous Meningitis, Ulcerative Colitis, Uveitis, Vasculitis, Acquired immune hemolytic anemia, Acute Bursitis, Acute Rheumatic heart disease, unspecified, Acute Tenosynovitis, Allergic skin manifestations, Anal eczema, Exfoliative erythroderma, Idiopathic Bronchiolitis obliterans with organizing pneumonia, Idiopathic eosinophilic pneumonias, Non-suppurative Thyroiditis, Primary adrenocoritical insufficiency, Severe Psoriasis, Severe Seborrhoeic dermatitis, Severe alcoholic liver disease, Steroid-responsive inflammation of the eye, Subacute Bursitis, Susceptible Bacterial Infections, Symptomatic Sarcoidosis, Varicella-zoster virus acute retinal necrosisAcne Vulgaris, Conjunctivitis, Trachoma, Superficial ocular infections

How Cortibiotan works

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Sulfacetamide is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), an essential component for bacterial growth (according to the Woods-Fildes theory). The inhibited reaction is necessary in these organisms for the synthesis of folic acid.

Dosage

Cortibiotan dosage

For conjunctivitis and other superficial ocular infections: Instill one or two drops into the conjunctival sac(s) of the affected eye(s) every two to three hours initially. Dosages may be tapered by increasing the time interval between doses as the condition responds. The usual duration of treatment is seven to ten days.

For trachoma: Instill two drops into the conjunctival sac(s) of the affected eye(s) every two hours. Topical administration must be accompanied by systemic administration.

Side Effects

Bacterial and fungal corneal ulcers have developed during treatment with sulfonamide ophthalmic preparations. The most frequently reported reactions are local irritation, stinging and burning. Less commonly reported reactions include non-specific conjunctivitis, conjunctival hyperemia, secondary infections and allergic reactions.

Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias

Toxicity

The intraperitoneal LD₅₀ in rats is 2g/kg and 65mg/kg in mice. The subcutaneous LD₅₀ in rats is 147mg/kg and >3500mg/kg in mice. The oral LD₅₀ in mice is 1680mg/kg. In humans, the oral TDLO in men is 9mg/kg/2W and in women is 14mg/kg/13D.

Patients experiencing an overdose of prednisolone may present with gastrointestinal disturbances, insomnia, and restlessness. Overdose of oral prednisolone may be treated by gastric lavage or inducing vomiting if the overdose was recent, as well as supportive and symptomatic therapy. Chronic overdosage may be treated by dose reduction or treating patients on alternate days. An overdose by the ophthalmic route is not expected to cause problems.

Oral LD₅₀ Mouse : 16500 mg/kg. Side effects include moderate to severe erythema (redness) and moderate edema (raised kin), nausea, vomiting, headache, dizziness, and tiredness. Higher exposure causes unconsciousness.

Precaution

Prolonged use of topical anti-bacterial agents may give rise to overgrowth of nonsusceptible organisms including fungi. Bacterial resistance to sulfonamides may also develop.

The effectiveness of sulfonamides may be reduced by the para-aminobenzoic acid present in purulent exudates.

Sensitization may recur when a sulfonamide is readministered irrespective of the route of administration, and cross-sensitivity between different sulfonamides may occur.

At the first sign of hypersensitivity, increase in purulent discharge, or aggravation of inflammation or pain, the patient should discontinue use of the medication and consult a physician

Interaction

Sulfacetamide preparations are incompatible with silver preparations.

Volume of Distribution

A 0.15mg/kg dose of prednisolone has a volume of distribution of 29.3L, while a 0.30mg/kg dose has a volume of distribution of 44.2L.

Elimination Route

Oral prednisolone reaches a C_max of 113-1343ng/mL with a T_max of 1.0-2.6 hours. Oral prednisolone is approximately 70% bioavailable.

Half Life

Prednisolone has a plasma half life of 2.1-3.5 hours. This half life is shorter in children and longer in those with liver disease.

7-12.8 hours

Clearance

A 0.15mg/kg dose of prednisolone has a clearance of 0.09L/kg/h, while a 0.30mg/kg dose has a clearance of 0.12L/kg/h.

Elimination Route

Prednisolone is over 98% eliminated in urine.

Pregnancy & Breastfeeding use

Pregnancy Category C. Animal reproduction studies have not been conducted with sulfonamide ophthalmic preparations. Kernicterus may occur in the newborn as a result of treatment of a pregnant woman at term with orally administered sulfonamides. There are no adequate and well controlled studies of sulfonamide ophthalmic preparations in pregnant women and it is not known whether topically applied sulfonamides can cause fetal harm when administered to a pregnant woman. Sulfacetamide sodium should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing mothers: Systemically administered sulfonamides are capable of producing kernicterus in infants of lactating women. Because of the potential for the development of kernicterus in neonates, a decision should be made whether to discontinue nursing or discontinue the drug taking into account the importance of the drug to the mother.

Contraindication

Sulfacetamide sodium ophthalmic solution is contraindicated in individuals who have a hypersensitivity to sulfonamides or to any ingredient of the preparation.

Special Warning

Pediatric use: Safety and effectiveness in infants below the age of two months have not been established.

Storage Condition

Store below 25° C.

Innovators Monograph

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