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General Description:

Fluticasone, identified by CAS number 90566-53-3, is a notable compound with significant therapeutic applications. Fluticasone is a synthetic glucocorticoid available as 2 esters, and . These drugs are available as inhalers, nasal, sprays, and topical treatments for various inflammatory indications. was first approved in 1990 and was approved in 2007.

Indications:

This drug is primarily indicated for: Fluticasone's 2 esters are indicated as inhalers for the treatment and management of asthma by prophylaxisas well as inflammatory and pruritic dermatoses. A nasal spray is indicated for managing nonallergic rhinitis while the nasal spray is indicated for treating season and perennial allergic rhinitis. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Fluticasone undergoes metabolic processing primarily in: and are cleared from hepatic metabolism by cytochrome P450 3A4. Both are hydrolysed at the FIVE-S-fluoromethyl carbothioate group, forming an inactive metabolite. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Fluticasone are crucial for its therapeutic efficacy: Intranasal exposure of results in patients swallowing a larger portion of the dose. However, absorption is poor and metabolism is high, therefore there is negligible systemic exposure with a nasal bioavailability of 0.50% and oral bioavialability of 1.26%. Inhaled bioavailability is 13.9%. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 6.3-18.4%. Intranasal bioavailability of is <2%, and oral bioavailability is <1%. Intranasal exposure results in the majority of the dose being swallowed. Topical absorption of 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%. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Fluticasone is an important consideration for its dosing schedule: 15.1 hours for intranasal 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 . A study of 24 healthy Caucasian males shows a half life of 14.0 hours following intravenous administration and 10.8 hours following inhalation. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Fluticasone exhibits a strong affinity for binding with plasma proteins: is >99% protein bound in serum and may be as high as 99.6%. is 99% protein bound in serum. Topical is only 91% protein bound in serum however. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Fluticasone from the body primarily occurs through: is eliminated ≥90% in the feces and 1-2% in the urine. is mainly eliminated in the feces with <5% eliminated in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Fluticasone is distributed throughout the body with a volume of distribution of: 608L at steady state for intravenous administration of . 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 is 4.2L/kg. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 577L following intravenous administration. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Fluticasone is a critical factor in determining its safe and effective dosage: 57.8L/h for . A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration. 1093mL/min for . A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Fluticasone exerts its therapeutic effects through: Systemically, in vitro experiments show activates glucocorticoid receptors, inhibits nuclear factor kappa b, and inhibits lung eosinophilia in rats. performs similar activity but is not stated to affect nuclear factor kappa b. as a topical formulation is also associated with vasoconstriction in the skin. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Fluticasone functions by: and work through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats. performs similar activity but is not stated to affect nuclear factor kappa b. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Fluticasone belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans, classified under the direct parent group Androgens and derivatives. This compound is a part of the Organic compounds, falling under the Lipids and lipid-like molecules superclass, and categorized within the Steroids and steroid derivatives class, specifically within the Androstane steroids subclass.

Categories:

Fluticasone is categorized under the following therapeutic classes: Adrenal Cortex Hormones, Androstadienes, Androstanes, Androstenes, Anti-Allergic Agents, Anti-Asthmatic Agents, Anti-Inflammatory Agents, Autonomic Agents, Bronchodilator Agents, Corticosteroid Hormone Receptor Agonists, Corticosteroids, Corticosteroids, Dermatological Preparations, Corticosteroids, Potent (Group III), Cytochrome P-450 CYP2C8 Inhibitors, Cytochrome P-450 CYP2C8 Inhibitors (strong), Cytochrome P-450 CYP3A Inducers, Cytochrome P-450 CYP3A Inhibitors, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Inducers, Cytochrome P-450 CYP3A4 Inducers (strength unknown), Cytochrome P-450 CYP3A4 Inhibitors, Cytochrome P-450 CYP3A4 Inhibitors (strength unknown), Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 CYP3A5 Inducers, Cytochrome P-450 CYP3A5 Inducers (strength unknown), Cytochrome P-450 CYP3A5 Inhibitors, Cytochrome P-450 CYP3A5 Inhibitors (strength unknown), Cytochrome P-450 CYP3A5 Substrates, Cytochrome P-450 CYP3A7 Substrates, Cytochrome P-450 Enzyme Inducers, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Substrates, Dermatologicals, Drugs for Obstructive Airway Diseases, Fused-Ring Compounds, Glucocorticoids, Hyperglycemia-Associated Agents, Immunosuppressive Agents, Nasal Preparations, OATP1B1/SLCO1B1 Inhibitors, P-glycoprotein substrates, Peripheral Nervous System Agents, Respiratory System Agents, Steroids, Thyroxine-binding globulin inhibitors. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.