フルチカゾンプロピオン酸エステル
Fluticasone Propionate
Fluticasone propionate (trifluorinated glucocorticoid)
別名: Flovent · Advair Diskus · Cutovate · Flixotide · Flixonase · Flutivate · CCI-18781 · fluticasoni propionas
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Adjunctive treatment of chronic tracheobronchial disease (excessive side effects from oral steroids) | 110 microgram or 220 microgram (1 puff) | Inhalation | q12h | — | 🌎 NA |
| Adjunctive treatment of chronic tracheobronchial disease | 2 puffs of the 220 micrograms/puff MDI | Inhalation | q12h | — | 🌎 NA |
- Adjunctive treatment of chronic tracheobronchial disease (excessive side effects from oral steroids): Use a delivery device (e.g., AeroDawg). Ensure a tightly fitting face mask and count 7-10 respirations after actuating the MDI into the spacer.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Treatment of feline 'asthma' | one puff of the 44 micrograms/puff MDI | Inhalation | q12h | — | 🌎 NA |
| Feline asthma (signs occurring more than once per week) | one puff of 110 micrograms fluticasone MDI | Inhalation | q12h | — | 🌎 NA |
- Treatment of feline 'asthma': Initially try this dose. Study showed 44, 110, and 220 mcg all significantly reduced eosinophils in airway lavage fluid.
- Feline asthma (signs occurring more than once per week): Use a delivery device (e.g., AeroKat) with a spacer. Cats with more serious disease may require the 220 micrograms MDI. Breathe in and out 7-10 times with mask in place. Give prednisolone at 1-2 mg/kg PO twice daily for 5-7 days initially, then taper over 2-3 months.
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Inflammatory airway disease (IAD) in young racehorses | Weeks 1 and 2: 2200 micrograms (10 puffs) twice daily. Weeks 3 and 4: 2200 micrograms (10 puffs) once daily. | Inhalation | q12h then q24h | 4 weeks | 🌎 NA |
| Moderate recurrent airway obstruction (RAO/heaves) | Week 3: 2200 micrograms (10 puffs) twice daily. Week 4: 2200 micrograms (10 puffs) once daily. End of 4 weeks (if good response): 2200 micrograms (10 puffs) once every other day. | Inhalation | q12h, then q24h, then EOD | Maintenance | 🌎 NA |
| Prevention of exacerbations of RAO | 6 mg | Inhalation | q12h | — | 🌎 NA |
- Inflammatory airway disease (IAD) in young racehorses: Use a delivery device (e.g., Aeromask or Equine-haler). Recheck in 4 weeks to determine further treatment.
- Moderate recurrent airway obstruction (RAO/heaves): Begin stringent environmental control and systemic prednisone. Add fluticasone at week 3 with salmeterol 210 mcg (10 puffs).
- Prevention of exacerbations of RAO: Using the EquineHaler. Highly likely that a lower dose can be used.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
フルチカゾンプロピオン酸エステルは、獣医療において主に吸入エアロゾルとして使用される強力な合成糖質コルチコイドです。
- 主な用途: 猫喘息、犬の慢性気管支疾患、馬の回帰性気道閉塞（RAO）や炎症性気道疾患（IAD）などの慢性炎症性気道疾患の管理に極めて有効です。点鼻薬はアレルギー性の慢性鼻副鼻腔炎にも使用されることがあります。
- 臨床的利点: 定量噴霧式吸入器（MDI）と動物種専用のスペーサーを介して気道粘膜に直接送達されるため、経口または注射用ステロイドに通常伴う全身性の副作用を大幅に最小限に抑えつつ、優れた局所抗炎症効果を発揮します。
- 効力: ヒト糖質コルチコイド受容体に対する親和性は、デキサメタゾンの18倍です。
作用機序
Fluticasone exerts its effects by binding to cytosolic glucocorticoid receptors in the respiratory mucosa.
Mechanism Pathway: Receptor binding → Translocation of the receptor-ligand complex to the nucleus → Alteration of gene transcription → Inhibition of pro-inflammatory mediators (such as cytokines, prostaglandins, and leukotrienes) → Decreased airway inflammation, reduced mucosal edema, and lowered airway hyperreactivity.
Note: The drug is highly lipophilic, allowing for prolonged retention in lung tissue, and undergoes extensive first-pass metabolism, which limits systemic bioavailability if swallowed.
安全性・警告
禁忌
- Hypersensitivity to fluticasone
- Acute bronchospasm or status asthmaticus (not a rescue inhaler)
有害事象
- Pharyngitis (reported in humans)
- Upper respiratory infections (reported in humans)
- Hypothalamic-pituitary-adrenal (HPA) axis suppression (rare with inhaled therapy, but possible with chronic high doses)
- Cushingoid effects (with chronic overdosage)
- Paradoxical bronchospasm (rare)
注意事項
When transferring patients from systemic steroid therapy to inhaled steroids, wean slowly off systemic therapy to avoid acute adrenal insufficiency. Prepare to cover patients with additional systemic steroid therapy during periods of acute stress, severe asthma attacks occurring during the withdrawal stage, or after transfer to inhaled steroids. Fluticasone is not useful for acute bronchospasm. Use with caution in nursing dams. FDA Category C for pregnancy; use only when benefits clearly outweigh risks.
医薬品相互作用
Inhibits CYP3A4 isoenzymes; theoretically could increase systemic fluticasone levels.
May decrease the metabolism of fluticasone, potentially increasing systemic exposure.
監視
- Clinical efficacy (reduction in coughing, wheezing, or respiratory effort)
- Signs of HPA axis suppression or cushingoid changes (rare with inhaled therapy)
薬物動態
吸収
In humans, when administered via the lung, about 30% is absorbed into the systemic circulation. Peak plasma concentrations of 0.1 to 1 ng/mL seen after 880 mcg dose.
分布
Volume of distribution averages 4.2 L/kg. It is 91% bound to human plasma proteins.
代謝
Metabolized via hepatic cytochrome P450 3A4 isoenzymes to a metabolite with negligible pharmacologic activity.
消失
Terminal elimination half-life is about 8 hours (in humans). Most of the drug is excreted in the feces as parent drug and metabolites.
過剰投与
Acute overdoses of this medication are unlikely to require treatment. Chronic overdoses could result in significant HPA axis suppression and cushingoid effects.
製品
製剤
- Metered dose inhaler (MDI) aerosol
- Dry powder for inhalation
- Nasal spray/solution
- Topical cream and ointment
ヒト用医薬品
- Fluticasone Propionate aerosol for inhalation: 44 mcg, 110 mcg, and 220 mcg per actuation (Flovent HFA)
- Fluticasone Propionate/Salmeterol Powder for Inhalation: 100/50 mcg, 250/50 mcg, 500/50 mcg (Advair Diskus)
- Fluticasone Propionate/Salmeterol Aerosol for Inhalation: 45/21 mcg, 115/21 mcg, 230/21 mcg
- Nasal solutions, topical creams, and ointments
規制ステータス
規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store between 2-30°C (36-86°F); protect from freezing and direct sunlight. Store canister with the mouthpiece down.
飼主向け情報
重要: この薬は気道の炎症をコントロールするための予防薬です。急性の喘息発作に対するレスキュー吸入器としては使用できません。
- 準備: 使用前に事前によく振ってください。可能であれば、投与前にキャニスターを室温に戻してください。
- 投与方法: ペットの動物種に適したスペーサー（AeroKat®やAeroDawg®など）を必ず使用してください。マスクを動物の鼻と口に優しく当て、吸入器を押してスペーサー内に薬を放出します。マスクを外す前に、動物に7〜10回通常の呼吸をさせてください。
- 保管: キャニスターに穴を開けたり、焼却したりしないでください。
- 使用期間: 1日2回、1回1噴霧の標準的な処方で、約2ヶ月間使用できます。
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