Fluticasona

Uses

Fluticasona Propionate is used for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive eczema or dermatitis.

Fluticasona is also used to associated treatment for these conditions: Asthma, Bronchostenosis, Skin discomfort, Moderate, severe Chronic Obstructive Pulmonary Disease (COPD)

How Fluticasona works

Fluticasona furoate and Fluticasona propionate work through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show Fluticasona furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats. Fluticasona propionate performs similar activity but is not stated to affect nuclear factor kappa b.

Dosage

Fluticasona dosage

Cream: Apply a thin layer of Fluticasona propionate cream to the affected skin areas once daily.

Ointment: Apply a thin layer of Fluticasona propionate Ointment to the affected skin areas twice daily.

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.

Toxicity

Fluticasona 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. Fluticasona furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasona 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.

Fluticasona propionate's use in specific populations has not been well studied. Fluticasona propionate is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studies. Subcutaneous Fluticasona 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. Fluticasona propionate in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effects. Pediatric patients treated with Fluticasona propionate ointment experienced adrenal suppression. Geriatric patients treated with Fluticasona 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 Fluticasona propionate across genders or race. Patients with hepatic impairment should be closely monitored due to the elimination mechanism.

Precaution

Fluticasona 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.

Food Interaction

Fluticasona Drug Interaction

Minor: fluticasone / salmeterol, fluticasone / salmeterol, albuterol, albuterol, budesonide / formoterol, budesonide / formoterolUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, montelukast, montelukast, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, cetirizine, cetirizine

Fluticasona Disease Interaction

Moderate: hepatic impairment, hyperadrenocorticism, infections, ocular herpes simplex, ocular toxicities, osteoporosis

Volume of Distribution

608L at steady state for intravenous administration of Fluticasona 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 Fluticasona 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.

Elimination Route

Half Life

15.1 hours for intranasal Fluticasona 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 Fluticasona 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.

Clearance

57.8L/h for Fluticasona furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.

1093mL/min for Fluticasona propionate. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration.

Elimination Route

Fluticasona furoate is eliminated ≥90% in the feces and 1-2% in the urine.

Fluticasona propionate is mainly eliminated in the feces with

Pregnancy & Breastfeeding use

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