メチルプレドニゾロン
Methylprednisolone
6alpha-methylprednisolone
別名: Depo-Medrol · Solu-Medrol · A-Methapred · Depo-Medrone · Solu-Medrone · 6alpha-methylprednisolone · methylprednisolonum · NSC-19987 · Methylprednisolone acetate · Methylprednisolone sodium succinate
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 uses (Oral) | Dogs weighing 5-15 lbs: 2 mg; Dogs weighing 15-40 lbs: 2-4 mg; Dogs weighing 40-80 lbs: 4-8 mg; these total daily doses should be divided | PO | q6-10h | — | 🌎 NA |
| Labeled uses (Injectable) | 2-120 mg (average 20 mg) | IM | May repeat at weekly intervals | — | 🌎 NA |
| Intralesional (sub-lesional) use | 10-40 mg total dose | intralesional | — | — | 🌎 NA |
- Labeled uses (Oral): Divide total daily dose and give 6-10 hours apart.
- Labeled uses (Injectable): Depending on breed (size), severity of condition, and response.
- Intralesional (sub-lesional) use: A sufficient volume of 20 mg/mL methylprednisolone acetate is used to undermine the lesion.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Labeled uses (Oral) | Cats weighing 5-15 lbs: 2 mg; Cats weighing >15 lbs: 2-4 mg; these total daily doses should be divided | PO | q6-10h | — | 🌎 NA |
| Labeled uses (Injectable) | up to 20 mg (average 10 mg) | IM | May repeat at weekly intervals | — | 🌎 NA |
| Intralesional (sub-lesional) use | 10-40 mg total dose | intralesional | — | — | 🌎 NA |
- Labeled uses (Oral): Divide total daily dose and give 6-10 hours apart.
- Labeled uses (Injectable): Depending on breed (size), severity of condition, and response.
- Intralesional (sub-lesional) use: A sufficient volume of 20 mg/mL methylprednisolone acetate is used to undermine the lesion.
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Antiinflammatory (glucocorticoid effects) | 200 mg | IM | repeated as necessary | — | 🌎 NA |
| Intra-articular use | 100 mg | IA | — | — | 🌎 NA |
- Antiinflammatory (glucocorticoid effects): Labeled use.
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
メチルプレドニゾロンは、ヒドロコルチゾンの約4〜5倍の効力を持ち、鉱質コルチコイド作用をほとんど持たない合成の中時間作用型糖質コルチコイドです。強力な抗炎症作用および免疫抑制作用のため、獣医学で広く使用されています。
臨床のポイントと剤形:
- メチルプレドニゾロン塩基: 維持療法または漸減療法のための経口錠剤。
- 酢酸メチルプレドニゾロン (Depo-Medrol®): 筋肉内、病変内、または関節内注射用の微結晶懸濁液。吸収が遅く、長期の持続効果（数週間から数ヶ月）を提供します。注意: 深刻で長期にわたる視床下部-下垂体-副腎 (HPA) 軸の抑制を引き起こす可能性があります。
- コハク酸エステルナトリウムメチルプレドニゾロン (Solu-Medrol®): 急性危機（脊髄損傷、重度の過敏反応、ショックなど）での急速静脈内投与用に設計された高水溶性エステル。ただし、ショック/外傷に対する高用量使用は近年議論の的となっています。
非常に有効ですが、糖質コルチコイド療法の目標は常に、全身性の副作用、特に医原性副腎皮質機能亢進症（クッシング症候群）を最小限に抑えるために、可能な限り短期間で最低有効量を使用することです。
作用機序
Glucocorticoids exert their effects by diffusing across cell membranes and binding to specific cytoplasmic glucocorticoid receptors (GR).
- Genomic Pathway: The receptor-ligand complex translocates to the nucleus → binds to glucocorticoid response elements (GREs) on target genes → alters gene transcription.
- Anti-inflammatory Mechanism: They induce the synthesis of lipocortin-1 (annexin-1) → inhibits phospholipase A2 → blocks the release of arachidonic acid from membrane phospholipids → profoundly decreases the synthesis of pro-inflammatory prostaglandins and leukotrienes.
- Immunosuppressive Mechanism: They suppress the transcription of inflammatory cytokines (e.g., IL-1, IL-2, IL-6, TNF-alpha), inhibit macrophage and neutrophil migration/function, and induce apoptosis in lymphocytes.
- Metabolic Effects: Stimulate hepatic gluconeogenesis, promote protein catabolism, and redistribute lipid stores.
安全性・警告
禁忌
- Systemic fungal infections (unless used for Addison's replacement)
- Viral infections
- Arrested tuberculosis
- Peptic or corneal ulcers
- Acute psychoses
- Cushingoid syndrome
- Idiopathic thrombocytopenia (for IM administration)
- Acute local infections (for intrasynovial/intratendinous use)
- Chronic systemic therapy using sustained-release injectable forms
- Pregnant animals
- Renal disease
- Diabetes mellitus
有害事象
- Polyuria (PU), polydipsia (PD), polyphagia (PP)
- Iatrogenic hyperadrenocorticism (Cushingoid signs) with sustained use
- Weight gain and lipidemias
- Dull, dry haircoat and alopecia
- Muscle wasting and weakness
- Gastrointestinal ulceration, vomiting, diarrhea, melena, hematochezia
- Elevated liver enzymes (ALP, ALT) and hepatopathy
- Pancreatitis
- Activation or worsening of diabetes mellitus (especially in cats)
- Behavioral changes (depression, lethargy, viciousness, panting)
- Extracellular hyperglycemia leading to volume expansion and potential CHF (cats)
- Hypothalamic-pituitary-adrenal (HPA) axis suppression
- Adrenal atrophy
- Weight loss (catabolic effect)
- Cutaneous atrophy (thinning of skin)
- Iatrogenic hyperadrenocorticism (Cushing's syndrome)
- Diarrhoea
- Increased urine glucose levels
- Decreased serum T3 and T4 levels
- Impaired wound healing
- Delayed recovery from infections
注意事項
Tapering Required: Animals receiving systemic glucocorticoids (other than short 'burst' therapy) must be tapered off slowly to allow endogenous ACTH and corticosteroid function to recover. Abrupt withdrawal can precipitate an Addisonian crisis.
- Stress Dosing: Additional glucocorticoids may be needed during stressors (surgery, trauma, illness) during the tapering process.
- Use with Caution: In patients with diabetes mellitus, osteoporosis, predisposition to thrombophlebitis, hypertension, congestive heart failure (CHF), and renal insufficiency.
- Pregnancy: FDA Category C. May cause teratogenic effects in early pregnancy. Exogenous steroids can induce parturition in the latter stages of pregnancy in horses and ruminants.
- Nursing Dams: Glucocorticoids enter milk and may inhibit growth or interfere with endogenous corticosteroid production in nursing offspring.
医薬品相互作用
May cause hypokalemia; potential for CHF and cardiac enlargement
Combination in epidurals has caused serious CNS injuries and death
May lead to profound muscle weakness in myasthenia gravis patients
Glucocorticoids may reduce salicylate blood levels
May increase the metabolism of glucocorticoids and decrease blood levels
Glucocorticoids may inhibit hepatic metabolism of cyclophosphamide
May mutually inhibit hepatic metabolism, increasing blood levels of both drugs
May cause hypokalemia
May reduce methylprednisolone blood levels
May potentiate the effects of methylprednisolone
Insulin requirements may increase due to glucocorticoid-induced insulin resistance
May decrease metabolism of glucocorticoids; ketoconazole may induce adrenal insufficiency upon withdrawal
May decrease metabolism of glucocorticoids and increase blood levels
May alter steroid metabolism; higher steroid doses may be needed
Increased risk of severe gastrointestinal ulceration
May increase metabolism of glucocorticoids and decrease blood levels
May increase metabolism of glucocorticoids and decrease blood levels
Virus replication may be augmented; diminished immune response to vaccines
May affect INR values; requires monitoring
Increased risk of hypokalaemia
Enhanced metabolism of corticosteroids, potentially reducing their efficacy
Decreased metabolism of corticosteroids, potentially increasing their effects and toxicity
監視
- Weight, appetite, and signs of edema
- Serum and/or urine electrolytes
- Total plasma proteins, albumin
- Growth and development in young animals
- ACTH stimulation test (if iatrogenic Cushing's or Addison's is suspected)
- Clinical signs of iatrogenic hyperadrenocorticism (PU/PD, polyphagia, weight gain)
- Blood glucose levels (especially in diabetic or pre-diabetic patients)
- Serum electrolytes (specifically potassium)
- Thyroid panel (T3 and T4 may be artificially decreased)
- Signs of gastrointestinal ulceration (melena, vomiting blood)
薬物動態
半減期
吸収
Orally administered methylprednisolone is relatively well absorbed. The acetate IM injection is slowly absorbed and can have a duration of effect of weeks to months. The sodium succinate IV injection is water soluble and very fast acting.
分布
Extensively distributed throughout the body.
代謝
The liver is the primary site for metabolism (oxidation).
消失
Most of the drug is excreted renally as metabolites.
過剰投与
Short-term administration of massive doses is unlikely to cause harmful effects, though one case of acute CNS effects in a dog after accidental ingestion has been reported. If acute overdose occurs, provide supportive treatment as required.
Chronic Overdosage: Chronic usage leads to serious adverse effects, primarily iatrogenic hyperadrenocorticism (Cushing's syndrome), characterized by profound metabolic, dermatologic, and immunosuppressive changes.
製品
製剤
- Injectable suspension (Acetate)
- Powder for injection (Sodium Succinate)
- Injectable depot suspension: 40 mg/ml
- Injectable powder for reconstitution: 125 mg, 500 mg
- Oral tablets: 2 mg, 4 mg
動物用医薬品
- Methylprednisolone Tablets: 4 mg (Medrol®)
- Methylprednisolone Acetate Injection: 20 mg/mL, 40 mg/mL (Depo-Medrol®)
- Depo-Medrone 40 mg/ml depot suspension
- Solu-Medrone 125 mg powder for reconstitution
- Solu-Medrone 500 mg powder for reconstitution
- Medrone 2 mg tablets
- Medrone 4 mg tablets
ヒト用医薬品
- Methylprednisolone Oral Tablets: 2 mg, 4 mg, 8 mg, 16 mg, 24 mg, 32 mg (Medrol®)
- Methylprednisolone Acetate Injection: 20 mg/mL, 40 mg/mL, 80 mg/mL (Depo-Medrol®)
- Methylprednisolone Sodium Succinate Powder for Injection: 40 mg, 125 mg, 500 mg, 1 gram, 2 grams per vial (Solu-Medrol®, A-Methapred®)
規制ステータス
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store commercially available products at room temperature (15-30°C). Avoid freezing the acetate injection. After reconstituting the sodium succinate injection, store at room temperature and use within 48 hours; only use solutions that are clear.
飼主向け情報
飼い主様への重要なガイドライン:
- 急に服用を中止しないでください: 獣医師に相談することなく、突然この薬の投与を中止しないでください。この薬を服用している間、体内の自然なステロイド産生は休止しており、急に中止すると生命を脅かす危機を引き起こす可能性があります。獣医師が徐々に減量するスケジュールを指示します。
- 予想される副作用: この薬の服用中、ペットの飲水量が増え、頻尿になり、食欲が増すことは非常に一般的です。常に新鮮な水を用意し、頻繁にトイレに行けるようにしてあげてください。
- 重篤な症状に注意: 嘔吐、黒色/タール状の便、血便、極度の無気力、パンティング（あえぎ呼吸）、または著しい行動の変化などの重篤な副作用に気づいた場合は、すぐに獣医師に連絡してください。
- 指示に従ってください: 処方された通りに正確に薬を与えてください。隔日投与のスケジュールを使用している場合は、投与忘れを防ぐためにカレンダーに印を付けると便利です。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。