Fluticasone Inhalation
Fluticasone Inhalation Uses, Dosage, Side Effects, Food Interaction and all others data.
Fluticasone Inhalation 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 Inhalation 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 Inhalation 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 Inhalation propionate glucocorticoid-receptor complex is approximately 10 hours.
Systemically, in vitro experiments show Fluticasone Inhalation furoate activates glucocorticoid receptors, inhibits nuclear factor kappa b, and inhibits lung eosinophilia in rats. Fluticasone Inhalation propionate performs similar activity but is not stated to affect nuclear factor kappa b. Fluticasone Inhalation propionate as a topical formulation is also associated with vasoconstriction in the skin.
Trade Name | Fluticasone Inhalation |
Availability | Prescription only |
Generic | Fluticasone |
Fluticasone Other Names | Fluticason, Fluticasona, Fluticasone, Fluticasonum |
Related Drugs | Dupixent, Xolair, ProAir Digihaler, dexamethasone, prednisolone, Symbicort, Breo Ellipta, Decadron, Ventolin, Xopenex |
Type | Inhalation aerosol, inhalation powder |
Formula | C22H27F3O4S |
Weight | Average: 444.51 Monoisotopic: 444.158215012 |
Protein binding | Fluticasone furoate is >99% protein bound in serum and may be as high as 99.6%. Fluticasone propionate is 99% protein bound in serum. Topical Fluticasone propionate is only 91% protein bound in serum however. |
Groups | Approved, Experimental |
Therapeutic Class | Fluticasone & combined preparations topical |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fluticasone Inhalation Propionate is used for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive eczema or dermatitis.
Fluticasone Inhalation is also used to associated treatment for these conditions: Asthma, Bronchostenosis, Skin discomfort, Moderate, severe Chronic Obstructive Pulmonary Disease (COPD)
How Fluticasone Inhalation works
Fluticasone Inhalation furoate and Fluticasone Inhalation propionate work through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show Fluticasone Inhalation furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats. Fluticasone Inhalation propionate performs similar activity but is not stated to affect nuclear factor kappa b.
Dosage
Fluticasone Inhalation dosage
Cream: Apply a thin layer of Fluticasone Inhalation propionate cream to the affected skin areas once daily.
Ointment: Apply a thin layer of Fluticasone Inhalation 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
Fluticasone Inhalation 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 Inhalation furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasone Inhalation 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 Inhalation propionate's use in specific populations has not been well studied. Fluticasone Inhalation propionate is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studies. Subcutaneous Fluticasone Inhalation 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 Inhalation propionate in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effects. Pediatric patients treated with Fluticasone Inhalation propionate ointment experienced adrenal suppression. Geriatric patients treated with Fluticasone Inhalation 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 Inhalation propionate across genders or race. Patients with hepatic impairment should be closely monitored due to the elimination mechanism.
Precaution
Fluticasone Inhalation 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
No interactions found.Fluticasone Inhalation 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
Fluticasone Inhalation Disease Interaction
Moderate: hepatic impairment, hyperadrenocorticism, infections, ocular herpes simplex, ocular toxicities, osteoporosis
Volume of Distribution
608L at steady state for intravenous administration of Fluticasone Inhalation 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 Inhalation 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
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15.1 hours for intranasal Fluticasone Inhalation 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 Inhalation 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 Fluticasone Inhalation furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.
1093mL/min for Fluticasone Inhalation propionate. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration.
Elimination Route
Fluticasone Inhalation furoate is eliminated ≥90% in the feces and 1-2% in the urine.
Fluticasone Inhalation propionate is mainly eliminated in the feces with
Administration of fluticasone propionate during pregnancy should only be considered if the expected benefit to the mother is greater than any possible risk to the fetus. The excretion of fluticasone propionate into human breast milk has not been investigated. Plasma levels in patients following dermal application of fluticasone propionate at recommended doses are likely to be low. When fluticasone propionate is used in breast feeding mothers, the therapeutic benefits must be weighed against the potential hazards to mother and baby.Pregnancy & Breastfeeding use
Contraindication
Fluticasone Inhalation 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 Inhalation 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.
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.
Innovators Monograph
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