Flutoz
Flutoz Uses, Dosage, Side Effects, Food Interaction and all others data.
Fluticasone propionate is a glucocorticoid with high topical anti-inflammatory potency, but a low HPA-axis suppressive activity after dermal administration. It, therefore, has a therapeutic index which is greater than most of the commonly available steroids. Fluticasone propionate has a high degree of selectivity for the glucocorticoid receptor. In vitro studies show that fluticasone propionate has a strong affinity for, and agonist activity at, human glucocorticoid receptors. This receptor is believed to be responsible for the anti-inflammatory properties of glucocorticoids.
Fluticasone propionate has weak affinity for the progesterone receptor, and virtually no affinity for the mineralocorticoid, estrogen, or androgen receptors. The therapeutic potency of glucocorticoids is related to the half-life of the glucocorticoid-receptor complex. The half-life of the Fluticasone propionate glucocorticoid-receptor complex is approximately 10 hours.
Systemically, in vitro experiments show Fluticasone furoate activates glucocorticoid receptors, inhibits nuclear factor kappa b, and inhibits lung eosinophilia in rats. Fluticasone propionate performs similar activity but is not stated to affect nuclear factor kappa b. Fluticasone propionate as a topical formulation is also associated with vasoconstriction in the skin.
Mupirocin inhibits protein synthesis of the bacteria by binding to isoleucyl transfer ribonucleic acid (RNA)-synthetase. It has bacteriostatic properties at Min inhibitory concentrations and bactericidal properties at the higher concentrations.
Mupirocin is reported to be active against susceptible aerobic gram-positive cocci, such as Staphylococcus aureus, Staphylococcus epidermidis, and other beta-hemolytic streptococciStreptococcus pyogenes. It mediates its antibacterial activity by inhibiting the bacterial protein synthesis and formation of bacterial proteins essential for survival. The minimum bactericidal concentration (MBC) against relevant pathogens is generally eight-fold to thirty-fold higher than the minimum inhibitory concentration (MIC). In one clinical study investigating the therapeutic effectiveness of topical mupirocin in impetigo, the therapeutic response rate was about 94 to 98% after one week following the end of therapy. In clinical studies of patients with primary and secondary skin infections, both elimination of the bacterial pathogen and clinical cure or improvement hav been demonstrated in over 90% of patients receiving topical mupirocin. Mupirocin resistance as high as 81% has been reported previously. Resistance to mupirocin, which occurs more frequently in methicillin-resistant than methicillin-susceptible staphylococci, may occur with the production of a modified isoleucyl-tRNA synthetase, or the acquisition of, by genetic transfer, a plasmid mediating a new isoleucyl-tRNA synthetase.
Trade Name | Flutoz |
Generic | Fluticasone + Mupirocin |
Weight | 0.005% |
Type | Cream |
Therapeutic Class | |
Manufacturer | Cytoz Pharmaceuticals |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
![Flutoz Flutoz](https://www.medicinesfaq.com/media/png/flutoz.png)
Uses
Fluticasone Propionate is used for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive eczema or dermatitis.
Mupirocin ointment or cream is used for the topical treatment of impetigo due to Staphylococcus aureus and Streptococcus pyogenes. It is also used for folliculitis and furunculosis.
Flutoz is also used to associated treatment for these conditions: Asthma, Bronchostenosis, Skin discomfort, Moderate, severe Chronic Obstructive Pulmonary Disease (COPD)Impetigo, Impetigo caused by Staphylococcus aureus, Impetigo caused by streptococcus pyogenes, Secondary infection Skin infection, Staphylococcus aurea colonization of the nasal passage
How Flutoz works
Fluticasone furoate and Fluticasone propionate work through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show Fluticasone furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats. Fluticasone propionate performs similar activity but is not stated to affect nuclear factor kappa b.
Mupirocin specifically and reversibly binds to bacterial isoleucyl transfer-RNA (tRNA) synthetase, which is an enzyme that promotes the conversion of isoleucine and tRNA to isoleucyl-tRNA. Inhibition of this enzyme subsequently leads to the inhibition of the bacterial protein and RNA synthesis. Mupirocin is bacteriostatic at lower concentrations but it exerts bactericidal effects with prolonged exposure, killing 90-99% of susceptible bacteria over a 24 hour period.
Dosage
Flutoz dosage
Cream: Apply a thin layer of Fluticasone propionate cream to the affected skin areas once daily.
Ointment: Apply a thin layer of Fluticasone propionate Ointment to the affected skin areas twice daily.
Secondary skin infections:
- Adult: As 2% cream: Apply to affected area three times daily for up to 10 days; re-evaluate after 3-5 days if no clinical response.
- Child: ≥3 mth Same as adult dose.
Impetigo:
- Adult: As 2% oint: Apply to affected area three times daily for 5-10 days; re-evaluate after 3-5 days if no clinical response.
- Child: ≥2 mth Same as adult dose.
Side Effects
The fluticasone propionate preparations are usually well tolerated; local burning and pruritus have been reported. If signs of hypersensitivity appear, application should be stopped immediately. Prolonged and intensive treatment with potent corticosteroid preparations may cause local atrophic changes in the skin such as thinning, striae, dilatation of the superficial blood vessels, hypertrichosis and hypopigmentation.
Secondary infection, particularly when occlusive dressings are used or when skin folds are involved and allergic contact dermatitis have also been reported with corticosteroid use. Exacerbation of the signs and symptoms of the dermatoses have been reported with corticosteroid use.
Prolonged use of large amounts of corticosteroids, or treatment of extensive areas, can result in sufficient systemic absorption to produce the features of hypercorticism. This effect is more likely to occur in infants and children, and if occlusive dressings are used. In infants, the napkin may act as an occlusive dressing.
Burning, stinging, pruritus, pain, rash, erythema, dry skin, tenderness, cellulitis, pain or bleeding secondary to eczema, secondary wound infection, urticaria, swelling, increased exudates, contact dermatitis, furunculosis, exfoliative dermatitis. Rarely, systemic reactions (e.g. nausea, headache, dizziness, abdominal pain, ulcerative stomatitis, systemic allergic reactions).
Toxicity
Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studies. Fluticasone furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertility. There are no well controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milk. Generally, there are no reported adverse effects with fluticasone in pregnancy. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocity. There is insufficient evidence to determine whether geriatric patients respond differently to other patients. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatment.
Fluticasone propionate's use in specific populations has not been well studied. Fluticasone propionate is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studies. Subcutaneous Fluticasone propionate has been shown to produce teratogenic effects in rats though oral administration does not. Generally, there are no reported adverse effects with fluticasone in pregnancy. Fluticasone propionate in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effects. Pediatric patients treated with Fluticasone propionate ointment experienced adrenal suppression. Geriatric patients treated with Fluticasone propionate did not show any difference in safety or efficacy compared to other patient groups, though older patients may be more sensitive to adverse effects. There is no difference in the clearance of Fluticasone propionate across genders or race. Patients with hepatic impairment should be closely monitored due to the elimination mechanism.
LD50 and Nonclinical Toxicity
The oral LD50 value in rats is 5000 mg/kg. Studies evaluating the carcinogenic potential of mupirocin have not been performed. In various in vivo animal and in vitro bacterial assays, there was no evidence of genotoxicity caused by mupirocin. In reproduction studies using male and female rats, there were no signs of impaired fertility upon subcutaneous administration of mupirocin.
Use in special populations
Mupirocin was found to be excreted in human milk. As there is limited data on the use of topical mupirocin in pregnant women, the use of this drug in these patients should be undertaken with caution. Based on the findings in clinical trials, topical mupirocin was shown to be safe and effective in pediatric patients aged 2 months to 16 years.
Precaution
Fluticasone propionate has a very low propensity for systemic absorption, nevertheless, prolonged application of high doses to large areas of body surface, especially in infants and small children might lead to adrenal suppression. Children may absorb proportionally larger amounts of topical corticosteroids and thus be more susceptible to systemic toxicity.
The face, more than other areas of the body, may exhibit atropic changes after prolonged treatment with potent topical corticosteroids. This must be borne in mind when treating severe eczema.
Appropriate antimicrobial therapy should be used whenever treating inflammatory lesions which have become infected. Any spread of infection requires withdrawal of topical corticosteroid therapy and systemic administration of antimicrobial agents. Bacterial infection is encouraged by the warm, moist conditions induced by occlusive dressing, and so the skin should be cleansed before a fresh dressing is applied.
Mupirocin is not suitable for ophthalmic or intra-nasal use. When Mupirocin ointment is used on the face, care should be taken to avoid the eyes. In common with other polyethylene-based ointments, this drug should be used with caution if there is evidence of moderate or severe renal impairment. As with other antibacterial products, prolonged use may result in overgrowth of nonsusceptible organisms, including fung.
Interaction
Chloramphenicol may interfere with the antibacterial action of mupirocin in RNA synthesis.
Volume of Distribution
608L at steady state for intravenous administration of Fluticasone furoate. Other reports suggest the mean volume of distribution at steady state is 661L. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration.
The volume of distribution of intravenous Fluticasone propionate is 4.2L/kg. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 577L following intravenous administration.
No information available.
Elimination Route
["\"Fluticasone Propionate (Flonase) Nasal Spray FDA Label\" href=\"#reference-F4358Fluticasone propionate is very low but can change depending on a number of factors including integrity of the skin and the presence of inflammation or disease. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 9.0%.<\/p>\n"]Systemic or percutaneous absorption of mupirocin following dermal application is expected to be minimal in adults and children. Occlusive dressings do not significantly enhance drug absorption, but damaged skin may allow enhanced penetration of the drug across the skin barrier.
Half Life
15.1 hours for intranasal Fluticasone furoate and 24 hours for the inhaled formulation. A study of 24 healthy Caucasian males showed a half life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation.
7.8 hours for intravenous Fluticasone propionate. A study of 24 healthy Caucasian males shows a half life of 14.0 hours following intravenous administration and 10.8 hours following inhalation.
In healthy male volunteers, the elimination half-life of mupirocin was about 20 to 40 minutes following intravenous administration. The elimination half-life of monic acid was about 30 to 80 minutes.
Clearance
57.8L/h for Fluticasone furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.
1093mL/min for Fluticasone propionate. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration.
No information available.
Elimination Route
Fluticasone furoate is eliminated ≥90% in the feces and 1-2% in the urine.
Contraindication
Fluticasone propionate is contraindicated in Rosacea, Acne vulgaris, Peri-oral dermatitis, Primary cutaneous viral infections (e.g., herpes simplex, chicken pox), Hypersensitivity to any of the ingredients, Perianal and genital pruritus, etc. The use of Fluticasone propionate is not indicated in the treatment of primarily infected skin lesions caused by infection with fungi or bacteria and dermatoses in children under one year of age, including deramtitis and napkin eruptions.
This drug is contraindicated in individuals with a history of sensitivity reactions to Mupirocin or any of the components of the preparation.
Special Warning
Pediatric Use: The safety and effectiveness of Mupirocin ointment have been established in the age range of 2 months to 16 years. Use of the ointment in these age groups is supported by evidence from adequate and well-controlled studies of Mupirocin in impetigo in pediatric patients.
Acute Overdose
Acute overdosage is very unlikely to occur, however, in case of cronic overdosage or misuse the features of hypercorticism may appear, and in this situation, as with any corticosteroid, application should be discontinued. Overdosage by ingestion of fluticasone propionate cream or ointment is extremely unlikely to occur due to the very low oral bioavailability of fluticasone propionate.
Storage Condition
Store below 30˚ C. Do not freeze.
Store at or below 25° C. Do not freeze.
Innovators Monograph
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