フルメタゾン
Flumethasone
6alpha, 9alpha-difluoro-16alpha methylprednisolone
別名: Flucort · Cerson · Locacortene · Locortene · Lorinden · flumetasone · glumetasoni pivalas · NSC-107680
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 |
|---|---|---|---|---|---|
| Labeled indications (musculoskeletal conditions, dermatoses, allergic states, shock) | 0.0625-0.25 mg daily in divided doses | PO | daily in divided doses | — | 🌎 NA |
| Labeled indications | 0.0625-0.25 mg daily; may repeat | IV, IM, SC | daily | — | 🌎 NA |
| Labeled indications (joint inflammation) | 0.166-1 mg | Intra-articularly | — | — | 🌎 NA |
| Labeled indications (localized lesions) | 0.125-1 mg | Intra-lesionally | — | — | 🌎 NA |
| General anti-inflammatory/immunosuppressive | 0.06-0.25 mg once daily | IV, IM, SC, or PO | once daily | — | 🌎 NA |
- Labeled indications (musculoskeletal conditions, dermatoses, allergic states, shock): Tablets no longer marketed in the USA
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Labeled indications (acute and chronic dermatoses) | 0.03125-0.125 mg daily in divided doses | PO | daily in divided doses | — | 🌎 NA |
| Labeled indications (acute and chronic dermatoses) | 0.03125-0.125 mg. If necessary, may repeat. | IV, IM, or SC | If necessary, may repeat | — | 🌎 NA |
| General anti-inflammatory/immunosuppressive | 0.03-0.125 mg once daily | IV, IM, SC, or PO | once daily | — | 🌎 NA |
- Labeled indications (acute and chronic dermatoses): Tablets no longer marketed in the USA
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Labeled indications (musculoskeletal conditions, allergic states) | 1.25-2.5 mg daily. If necessary, the dose may be repeated. | IV, IM or intra-articular | daily | — | 🌎 NA |
| General anti-inflammatory | 1-2.5 mg/450 kg | IV or IM | — | — | 🌎 NA |
- Labeled indications (musculoskeletal conditions, allergic states): ARCI UCGFS Class 4 Drug
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
フルメタゾンは、獣医学において強力な抗炎症作用および免疫抑制作用を目的として使用される、非常に強力で長時間作用型のフッ素化糖質コルチコイドです。
主な薬理学的特徴は以下の通りです：
- 高力価：ヒドロコルチゾンの約15〜30倍の効力を持ちます。
- 鉱質コルチコイド作用の欠如：鉱質コルチコイド（ナトリウム貯留）作用がほとんどないため、古いステロイドと比較して浮腫や高血圧のリスクが軽減されます。
- 臨床的有用性：急性炎症反応（虫刺されによる過敏症、ワクチン反応、ショック）、筋骨格系の炎症（滑液包炎、筋炎、変形性関節症）、および様々な急性または慢性の皮膚疾患に対して非常に有効です。
臨床のポイント：すべての全身性コルチコイドと同様に、フルメタゾン治療の最大の目標は、医原性副腎皮質機能亢進症（クッシング症候群）および副腎軸抑制のリスクを最小限に抑えるために、「必要な量を、可能な限り少なく、可能な限り短期間」使用することです。
作用機序
Flumethasone exerts its effects via classic genomic and non-genomic steroid pathways:
- Genomic Pathway: Free flumethasone crosses the cell membrane and binds to cytosolic glucocorticoid receptors (GR).
- The receptor-ligand complex translocates to the nucleus and binds to glucocorticoid response elements (GREs) on DNA.
- Transactivation: Upregulates the expression of anti-inflammatory proteins, notably lipocortin-1 (annexin A1). Lipocortin-1 inhibits phospholipase A2 → blocking the release of arachidonic acid from membrane phospholipids → profoundly decreasing the synthesis of pro-inflammatory prostaglandins and leukotrienes.
- Transrepression: Downregulates the expression of pro-inflammatory cytokines (e.g., IL-1, IL-6, TNF-alpha) by inhibiting transcription factors like NF-κB and AP-1.
- Non-genomic Pathway: Rapid physicochemical interactions with cellular membranes provide immediate effects, which is particularly beneficial in shock or acute hypersensitivity states.
安全性・警告
禁忌
- Last trimester of pregnancy (may induce parturition)
- Systemic fungal infections (unless used for Addison's replacement therapy)
- Idiopathic thrombocytopenia (specifically contraindicated for IM administration)
- Known hypersensitivity to the compound
- Chronic corticosteroid therapy of systemic diseases using sustained-release injectable forms
有害事象
- Polydipsia (PD), polyuria (PU), and polyphagia (PP)
- Weight gain and lipidemias
- Dull, dry haircoat and dermatological thinning
- Panting
- Gastrointestinal effects: vomiting, diarrhea, GI ulceration
- Hepatopathy: elevated liver enzymes (ALP, ALT)
- Pancreatitis
- Endocrine: activation or worsening of diabetes mellitus, iatrogenic hyperadrenocorticism (Cushingoid effects) with sustained use
- Musculoskeletal: muscle wasting, retarded growth in young animals
- Behavioral changes: depression, lethargy, viciousness
- Immunosuppression: increased susceptibility to infections
注意事項
Tapering Required: Animals that have received systemic glucocorticoids (other than short 'burst' therapy) must be tapered off slowly to allow endogenous ACTH and corticosteroid function to recover.
Stress Dosing: If an animal undergoes a 'stressor' (e.g., surgery, trauma, illness) during the tapering process or before normal adrenal/pituitary function resumes, additional glucocorticoids should be administered.
Pregnancy Warning: Corticosteroid therapy may induce parturition in large animal species during the latter stages of pregnancy. Categorized as Class C for canine and feline pregnancy (use cautiously as a last resort when benefits clearly outweigh risks).
医薬品相互作用
Administered concomitantly with glucocorticoids may cause hypokalemia
In patients with myasthenia gravis, concomitant administration may lead to profound muscle weakness. Discontinue anticholinesterase at least 24 hours prior if possible.
Glucocorticoids may reduce salicylate blood levels
May increase the metabolism of glucocorticoids and decrease flumethasone blood levels
Glucocorticoids may inhibit the hepatic metabolism of cyclophosphamide; dosage adjustments may be required
Concomitant administration may increase the blood levels of each by mutually inhibiting hepatic metabolism
Flumethasone may decrease diazepam levels
Administered concomitantly with glucocorticoids may cause hypokalemia
May reduce flumethasone blood levels
Insulin requirements may increase in patients receiving glucocorticoids
May decrease the metabolism of glucocorticoids and increase flumethasone blood levels; ketoconazole may induce adrenal insufficiency when glucocorticoids are withdrawn
May decrease the metabolism of glucocorticoids and increase flumethasone blood levels
May alter the metabolism of steroids; higher than usual doses of steroids may be necessary to treat mitotane-induced adrenal insufficiency
Administration of ulcerogenic drugs with glucocorticoids may increase the risk of gastrointestinal ulceration
May increase the metabolism of glucocorticoids and decrease flumethasone blood levels
May increase the metabolism of glucocorticoids and decrease flumethasone blood levels
Patients receiving immunosuppressive dosages should not receive live attenuated-virus vaccines (augmented virus replication); diminished immune response may occur with any vaccine
監視
- Weight, appetite, and signs of edema
- Serum and/or urine electrolytes
- Total plasma proteins, albumin
- Blood glucose
- Growth and development in young animals
- ACTH stimulation test if necessary (to assess adrenal axis suppression)
過剰投与
Short-term administration of massive dosages of glucocorticoids is unlikely to cause harmful effects. There is one reported incidence of a dog developing acute CNS effects after accidental ingestion. If acute clinical signs occur, provide supportive treatment as required.
Chronic overdosage or sustained high-dose usage leads to serious adverse effects, primarily manifesting as iatrogenic hyperadrenocorticism (Cushing's syndrome), characterized by severe polyuria/polydipsia, muscle wasting, alopecia, pot-bellied appearance, and immunosuppression.
製品
製剤
- Injection: 0.5 mg/mL solution
- Tablets (Note: Oral formulations are generally no longer marketed in the USA)
動物用医薬品
- Flumethasone Injection: 0.5 mg/mL in 100 mL vials; Flucort Solution (Pfizer); (Rx)
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
Flumethasone injection should be stored at room temperature; avoid freezing.
飼主向け情報
フルメタゾンは、炎症を急速に抑えたり、重度のアルレルギーを治療したり、特定の皮膚や関節の疾患を管理するために使用される強力なステロイド薬です。
- 指示に注意深く従ってください：処方された正確な用量を与えてください。獣医師に相談せずに突然この薬を中止しないでください。突然の投与中止は、体が自身の天然ステロイドを一時的に生成できなくなるため、生命を脅かす危機を引き起こす可能性があります。
- 予想される副作用：ペットの飲水量が増えたり、排尿の回数が増えたり、食欲が増したりすることに気づくかもしれません。犬ではパンティング（あえぎ呼吸）もよく見られます。
- 獣医師に連絡すべき場合：副作用がひどくなった場合、またはペットが嘔吐、下痢、黒色/タール状の便（胃潰瘍の兆候）、極度の無気力、または行動の変化（異常な攻撃性やうつ状態など）を示した場合は、獣医師に連絡してください。
- 免疫系：この薬は免疫系を抑制するため、ペットを病気の動物から遠ざけ、ワクチン接種を行う前には獣医師に相談してください。
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