Takmide
Takmide Uses, Dosage, Side Effects, Food Interaction and all others data.
Boric acid, also known as hydrogen borate, is a weak monobasic Lewis acid of boron with the chemical formula H3BO3. Boric acid is typically utilized in industrial processing and manufacturing, but is also used as an additive in pharmaceutical products, cosmetics, lotions, soaps, mouthwash, toothpaste, astringents, and eyewashes . It is known to exhibit some antibacterial activity against infections such as bacterial vaginosis and candidiasis .
Boric acid exhibits minimal bacteriostatic and antifungal activities . Boric acid is likely to mediate antifungal actions at high concentrations over prolonged exposures .
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 | Takmide |
Generic | Boric Acid + Sulfacetamide |
Weight | 1.9%, 12.5% |
Type | Eye Drops |
Therapeutic Class | |
Manufacturer | Pharmatak Opthalmics I Pvt Ltd |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
No FDA- or EMA-approved therapeutic indications on its own.
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.
Takmide is also used to associated treatment for these conditions: Acne, Asthenopia, Ocular Irritation, Skin Mycoses, Eye discomfort, Skin disinfection, Irrigation of the ocular surface therapyAcne Vulgaris, Conjunctivitis, Trachoma, Superficial ocular infections
How Takmide works
Information regarding the mechanism of action of boric acid in mediating its antibacterial or antifungal actions is limited. Boric acid inhibits biofilm formation and hyphal transformation of Candida albicans, which are critical virulence factors . In addition, arrest of fungal growth was observed with the treatment of boric acid .
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
Takmide 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
Acute oral LD50 is 2660 mg/kg in rat . Individuals are likely to be exposed to boric acid from industrial manufacturing or processing. Local tissue injury from boric acid exposure is likely due to caustic effects. Systemic effects from boric acid poisoning usually occur from multiple exposures over a period of days and involve gastrointestinal, dermal, CNS, and renal manifestations. Gastrointestinal toxicity include persistent nausea, vomiting, diarrhea, epigastric pain, hematemesis, and blue-green discoloration of the feces and vomit . Following the onset of GI symptoms, a characteristic intense generalized erythroderma follows . Management of mild to moderate toxicity should be supportive. In case of severe toxicity, dialysis may be required in addition to supportive treatment.
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
Volume of distribution ranges from 0.17 to 0.5 L/kg in humans, where large amounts of boric acid are localized in brain, liver, and kidney .
Elimination Route
Boric acid is well absorbed from the gastrointestinal tract, open wounds, and serous cavities but displays limited absorption in intact skin . Following intraperitoneal injection in mice, the peak concentration was reached in about 1.0-1.5 hr in the brain whereas the value was 0.5 hr in other tissues .
Half Life
According to human cases of poisoning, the elimination half-life of boric acid ranges from 13 to 24 hours .
7-12.8 hours
Clearance
A case report of acute boric acid poisoning following oral ingestion of 21 g of boric acid presents the total body clearance of 0.99 L/h before hemodialysis .
Elimination Route
Regardless the route of administration, boric acid predominantly undergoes rapid renal excretion of >90% of total administered dose as unchanged form. Small amounts are also excreted into sweat, saliva, and feces. Following administration as ointment, urinary excretion of boric acid accounted for only 1% of the administered dose .
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.
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