Propionate medical

No metabolites of fluticasone propionate were detected in an in vitro study of radiolabeled fluticasone propionate incubated in a human skin homogenate. The total blood clearance of systemically absorbed fluticasone propionate averages 1,093 mL/min (range, 618 to 1,702 mL/min) after a 1-mg intravenous dose, with renal clearance accounting for less than % of the total. Fluticasone propionate is metabolized in the liver by cytochrome P450 3A4-mediated hydrolysis of the 5- fluoromethyl carbothioate grouping. This transformation occurs in 1 metabolic step to produce the inactive17-ß-carboxylic acid metabolite, the only known metabolite detected in man. This metabolite has approximately 2,000 times less affinity than the parent drug for the glucocorticoid receptor of human lung cytosol in vitro and negligible pharmacological activity in animal studies. Other metabolites detected in vitro using cultured human hepatoma cells have not been detected in man.

Distribution : Following intravenous administration of 1 mg of fluticasone propionate in healthy volunteers, the initial disposition phase for fluticasone propionate was rapid and consistent with its high lipid solubility and tissue binding. The apparent volume of distribution averaged L/kg (range, - L/kg). The percentage of fluticasone propionate bound to human plasma proteins averaged 91%. Fluticasone propionate is weakly and reversibly bound to erythrocytes. Fluticasone propionate is not significantly bound to human transcortin.

Eligible patients with a valid prescription for ADVAIR DISKUS (fluticasone propionate and salmeterol inhalation powder) or ADVAIR HFA (fluticasone propionate and salmeterol) Inhalation Aerosol who present this savings card at participating pharmacies will pay the first $10, and receive up to $50 off each 30-day prescription or refill of ADVAIR DISKUS or ADVAIR HFA applied to your out-of-pocket cost. This offer is good for up to 12 uses, and each 30-day supply counts as 1 use. Patient is responsible for applicable taxes, and remaining out of pocket cost, if any. This offer is limited to one per person and is nontransferable and cannot be combined with any other coupon, free trial or similar offer. No substitutions are permitted. Patients, pharmacists, and prescribers cannot seek reimbursement from health insurance or any third party for any part of the amount received by the patient through this offer. Offer must be presented along with a valid prescription for ADVAIR DISKUS or ADVAIR HFA at the time of purchase. Your acceptance of this offer must be consistent with the terms of any drug benefit plan provided to you by your health insurer. You agree to report your use of this coupon to your health insurer if required.

Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen , estrogen , or mineralocorticoid receptors , thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (. mast cell , eosinophil , neutrophil , macrophages , and lymphocytes ) and mediators (. histamine , eicosanoids , leukotrienes , and cytokines ) involved in inflammation . Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemic bioavailability .

Propionate medical

propionate medical

Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen , estrogen , or mineralocorticoid receptors , thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (. mast cell , eosinophil , neutrophil , macrophages , and lymphocytes ) and mediators (. histamine , eicosanoids , leukotrienes , and cytokines ) involved in inflammation . Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemic bioavailability .

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