Medasulf
Medasulf Uses, Dosage, Side Effects, Food Interaction and all others data.
Prednisolone is a glucocorticoid similar to cortisol used for its anti-inflammatory, immunosuppressive, anti-neoplastic, and vasoconstrictive effects.
Prednisolone was granted FDA approval on 21 June 1955.
Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals. Prednisolone has a short duration of action as the half life is 2.1-3.5 hours. Corticosteroids have a wide therapeutic window as patients make require doses that are multiples of what the body naturally produces. Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.
The sulfonamides are bacteriostatic agents and the spectrum of activity is similar for all. Sulfonamides inhibit bacterial synthesis of dihydrofolic acid by preventing the condensation of the pteridine with aminobenzoic acid through competitive inhibition of the enzyme dihydropteroate synthetase. Resistant strains have altered dihydropteroate synthetase with reduced affinity for sulfonamides or produce increased quantities of aminobenzoic acid.
Topically applied sulfonamides are considered active against susceptible strains of the following common bacterial eye pathogens: 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.
Sulfacetamide is a sulfonamide antibiotic with bacteriostatic actions and broad-spectrum activity against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus.
Trade Name | Medasulf |
Generic | Prednisolone + sulfacetamide |
Weight | 0.2% + 10%, 0.23% + 10%, 0.2% + 10% |
Type | Ophthalmic ointment, ophthalmic solution, ophthalmic suspension, ophthalmic |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
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.
Medasulf 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 Medasulf 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
Medasulf 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 Cmax of 113-1343ng/mL with a Tmax 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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