Unisulf-S

Uses

Prednisolone eye drops is used for the treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

Prednisolone tablet, Injection is used forAllergy and anaphylaxis: bronchial asthma, drug hypersensitivity reactions, serum sickness, angioneurotic oedema, anaphylaxis.

Respiratory disease: allergic pneumonitis, asthma, occupational asthma, pulmonary aspergillosis, pulmonary fibrosis, pulmonary alveolitis, aspiration of foreign body, aspiration of stomach contents, pulmonary sarcoid, drug induced lung disease, adult respiratory distress syndrome, spasmodic croup.

Rheumatic disorders: rheumatoid arthritis, polymyalgia rheumatica, juvenile chronic arthritis, systemic lupus erythematosus, dermatomyositis, mixed connective tissue disease.

Arteritis/collagenosis: giant cell arteritis/polymyalgia rheumatica, mixed connective tissue disease, polyarteritis nodosa, polymyositis.

Blood disorders: haemolytic anaemia (auto-immune), leukaemia (acute and chronic lymphocytic), lymphoma, multiple myeloma, idiopathic thrombocytopenic purpura.

Cardiovascular disorders: post-myocardial infarction syndrome, rheumatic fever with severe carditis.

Endocrine disorders: primary and secondary adrenal insufficiency, congenital adrenal hyperplasia.

Gastro-intestinal disorders: Crohn's disease, ulcerative colitis, persistent coeliac syndrome (coeliac disease unresponsive to gluten withdrawal), auto-immune chronic active hepatitis, multisystem disease affecting liver, biliary peritonitis.

Infections (with appropriate chemotherapy): helminthic infestations, Herxheimer reaction, infectious mononucleosis, miliary tuberculosis, mumps orchitis (adult), tuberculous meningitis, rickettsial disease.

Muscular disorders: polymyositis, dermatomyositis.

Neurological disorders: infantile spasms, Shy-Drager syndrome, sub-acute demyelinating polyneuropathy.

Ocular disease: scleritis, posterior uveitis, retinal vasculitis, pseudo-tumours of the orbit, giant cell arteritis, malignant ophthalmic Graves disease.

Renal disorders: lupus nephritis, acute interstitial nephritis, minimal change glomerulonephritis.

Skin disorders: pemphigus vulgaris, bullous pemphigoid, systemic lupus erythematosus, pyoderma gangrenosum.

Miscellaneous: sarcoidosis, hyperpyrexia, Behçets disease, immunosuppression in organ transplantation.

Prednisolone is used for the treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

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.

Unisulf-S is also used to associated treatment for these conditions: Inflammation, Inflammatory Conditions, Ocular Infections, Irritations and Inflammations, Ocular Inflammation, Organ Transplant RejectionAcne Vulgaris, Conjunctivitis, Trachoma, Superficial ocular infections

How Unisulf-S 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

Unisulf-S dosage

The initial dosage of Prednisolone may vary from 5 mg to 60 mg daily depending on the disorder being treated. Divided daily dosage is usually used.

The appropriate individual dose must be determined by trial and error and must be re-evaluated regularly according to activity of the disease.

In general, initial dosage shall be maintained or adjusted until the anticipated response is observed. The dose should be gradually reduced until the lowest dose, which will maintain an adequate clinical response is reached.

During prolonged therapy, dosage may need to be temporarily increased during periods of stress or during exacerbations of the disease. When the drug is to be stopped, it must be withdrawn gradually and not abruptly.

Intermittent dosage regimen: A single dose of Prednisolone in the morning on alternate days or at longer intervals is acceptable therapy for some patients. When this regimen is practical, the degree of pituitary-adrenal suppression can be minimized.

Use in children: Corticosteroids cause growth retardation in infancy, childhood and adolescence, which may be irreversible. Treatment should be administered where possible as a single dose on alternate days.

Specific dosage guidelines-

Allergic and skin disorders: initial doses of 5-15 mg daily are commonly adequate.

Collagenosis: Initial doses of 20-30 mg daily are frequently effective. Those with more severe symptoms may require higher doses.

Rheumatoid arthritis: The usual initial dose is 10-15 mg daily. The lowest daily maintenance dose compatible with tolerable symptomatic relief is recommended.

Blood disorders and lymphoma: An initial daily dose of 15-60 mg is often necessary with reduction after an adequate clinical or haematological response. Higher doses may be necessary to induce remission in acute leukaemia.

Adult: Instill one drop into the conjunctival sac two to four times daily. During the initial 24 to 48 hours, the dosing frequency may be increased if necessary. Care should be taken not to discontinue the therapy before completing the course.

Paediatri: Safety and effectiveness in pediatric patients have not been established.

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

Elevation of intraocular pressure (IOP) with possible development of glaucoma and infrequent optic nerve damage, posterior subcapsular cataract formation and delayed wound healing. Fungal and viral infections of the cornea are particularly may develop coincidentally with long-term applications of steroid.

General side-effects include leucocytosis, hypersensitivity including anaphylaxis, thromboembolism, nausea, and malaise.

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 oral LD₅₀ of prednisolone acetate in mice is 1680 mg/kg. Patients experiencing an overdose of oral prednisolone acetate may experience an increased severity in the adverse effects of corticosteroids. Overdose of oral prednisolone acetate 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

Shake the bottle well before use. Prolonged use of corticosteroids may result in damage to the optic nerve and defects in vision. If this product is used for longer period of time, intraocular pressure should be routinely monitored.

Caution is necessary when oral corticosteroids, including Prednisolone, are prescribed in patients with the following conditions like-Tuberculosis, Hypertension, Congestive heart failure, Liver failure, Renal insufficiency, Diabetes mellitus or in those with a family history of diabetes, Osteoporosis, Patients with a history of severe affective disorders and particularly those with a previous history of steroid-induced psychoses, Epilepsy, Peptic ulceration, Previous Steroid Myopathy.

Undesirable effects may be minimized by using the lowest effective dose for the minimum period and by administering the daily requirement as a single morning dose on alternate days. Frequent patient review is required to titrate the dose appropriately against disease activity.

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

Hepatic microsomal enzyme inducers: Drugs which can cause liver enzyme induction such as phenobarbitone, phenytoin, rifampicin, rifabutin, carbamazepine, primidone and aminoglutethimide may reduce the therapeutic efficacy of corticosteroids by increasing the rate of metabolism.

Non-steroidal anti-inflammatory drugs: Concomitant administration of ulcerogenic drugs such as indomethacin during corticosteroid therapy may increase the risk of Gl ulceration.

Anticoagulants: Response to anticoagulants may be reduced or, less often, enhanced by corticosteroids.

Vaccines: Live vaccines should not be given to individuals with impaired immune responsiveness. The antibody response to other vaccines may be diminished.

Oestrogens: Oestrogens may potentiate the effects of glucocorticoids and dosage adjustment may be required if oestrogens are added to or withdrawn from a stable dosage regimen.

Other: The desired effects of hypoglycaemic agents (including insulin), anti-hypertensives and diuretics are antagonised by corticosteroids and the hypokalaemic effect of acetazolamide, loop diuretics, thiazide diuretics and carbenoxolone are enhanced.

Sulfacetamide preparations are incompatible with silver preparations.

Volume of Distribution

The volume of distribution of the active metabolite, prednisolone, is 0.22/0.7L/kg.

Elimination Route

Prednisolone acetate oral suspension given at a dose equivalent to 15mg prednisolone has a C_max of 321.1ng/hr, a T_maxof 1-2 hours, and an AUC of 1999.4ng*hr/mL. The absorption pharmacokinetics of prednisolone acetate are not significantly different from a comparable dose of prednisolone.

Half Life

Oral prednisolone acetate has a plasma half life of 2-3 hours.

7-12.8 hours

Clearance

Data regarding the clearance of prednisolone acetate is not readily available.

Elimination Route

Prednisolone acetate is predominantly excreted in the urine.

Pregnancy & Breastfeeding use

Pregnancy: Prednisolone Acetate is pregnancy category C. So, this drug should be used during pregnancy only if clearly needed.

Lactation: Corticosteroids are excreted in small amounts in breast milk and infants of mothers taking pharmacological doses of steroids should be monitored carefully for signs of adrenal suppression.

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

Prednisolone (Eye drops) is contraindicated in viral diseases of the cornea, conjunctiva and known hypersensitivity to any of the ingredients of Prednisolone (Eye drops) or other corticosteroids.

Systemic infections unless specific anti-infective therapy is employed. Hypersensitivity to any ingredient. Ocular herpes simplex because of possible perforation.

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

Special Warning

Use in the elderly: Treatment of elderly patients, particularly if long term, should be planned bearing in mind the more serious consequences of the common side effects of corticosteroids in old age, especially osteoporosis, diabetes, hypertension, hypokalemia, susceptibility to infection and thinning of the skin. Close clinical supervision is required to avoid life-threatening reactions.

May need to increase dose in patients with hyperthyroidism to achieve therapeutic effects.

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

Acute Overdose

A one-time accidental overdose of Prednisolone Ophthalmic Suspension generally will not cause acute problems. Long time overdose may show general side-effects. In accidental overdose sufficient water should be taken to dilute the medication.

Report of acute toxicity and/or death following overdose of glucocorticoids are rare. No specific antidote is available; treatment is supportive and symptomatic. Serum electrolytes should be monitored.

Storage Condition

Store in a cool, dry place and protect from light. Keep out of the reach of children. Protect from freezing. Shake well before using.

Store below 25° C.

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