ドキソルビシン
Doxorubicin
Doxorubicin Hydrochloride
別名: Doxil · Adriamycin RDF · Adriamycin PFS · Rubex · Caelyx · Myocet · cloridrato de doxorrubicina · doxorubicin hydrochloride liposome · doxorubicini hydrochloridum · liposomal doxorubicin hydrochloride · NSC-123127 · Hydroxydaunorubicin
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
これは体表面積(mg/m²)に基づく用量です。投与前に体重を体表面積へ換算してください。
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 |
|---|---|---|---|---|---|
| Antineoplastic | 30 mg/m2 IV every 2-3 weeks | IV | every 2-3 weeks | — | 🌎 NA |
| Lymphoma, sarcomas, carcinomas | 30 mg/m2 (Use 1 mg/kg in dogs weighing <10 kg) | IV | q3wk | Maximum total cumulative dose not to exceed 240 mg/m2 | 🌍 EU |
- Antineoplastic: Depending on the protocol used. Maximum cumulative dose = 240 mg/m2.
- Lymphoma, sarcomas, carcinomas: Administer over a minimum of 10 minutes into side port of freely running 0.9% NaCl.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Antineoplastic | 20-30 mg/m2 IV every 2-4 weeks | IV | every 2-4 weeks | — | 🌎 NA |
| Lymphoma, soft tissue sarcomas | 1 mg/kg or 20-25 mg/m2 | IV | q3-5wk | Maximum total cumulative dose not to exceed 240 mg/m2 | 🌍 EU |
- Antineoplastic: Depending on the protocol used. Maximum cumulative dose is usually 240 mg/m2.
- Lymphoma, soft tissue sarcomas: Nephrotoxicity is a major risk in cats, especially at cumulative dosages >100 mg/m2.
フェレット
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Antineoplastic | 30 mg/m2 IV every 3 weeks | IV | every 3 weeks | — | 🌎 NA |
- Antineoplastic: Depending on the protocol 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
ドキソルビシンは、小動物の獣医腫瘍学において最も広く使用されているアントラサイクリン系抗悪性腫瘍薬の一つです。その鮮やかな赤色と強力な副作用から、しばしば「赤い悪魔 (Red Devil)」と俗称されます。単剤または多剤併用プロトコルの一部として利用されます。
- 広範な有効性: 犬および猫のリンパ腫、癌腫、白血病、肉腫など、さまざまな悪性腫瘍に対して高い効果を示します。
- 起源: 元々は Streptomyces peucetius から分離されました。
- 臨床上のポイント: 抗菌特性を持っていますが、その強力な細胞毒性のため、抗感染症薬としての使用は完全に除外されます。重度の壊死起因物質 (vesicant)であり、壊滅的な血管外漏出損傷を防ぐために、確実な静脈内アクセスの確保に細心の注意を払う必要があります。
作用機序
Doxorubicin is a cell-cycle non-specific cytotoxic agent with multiple mechanisms of action:
- Topoisomerase II Inhibition: Intercalates between DNA base pairs and inhibits topoisomerase II → prevents DNA resealing → causes double-strand DNA breaks → triggers apoptosis.
- Macromolecular Synthesis Inhibition: Directly inhibits DNA synthesis, DNA-dependent RNA synthesis, and protein synthesis.
- Free Radical Generation: Undergoes electron reduction to form anthracycline semiquinone free radicals (often iron-mediated) → causes severe oxidative stress and lipid peroxidation.
- Clinical Pearl: The heart is particularly susceptible to doxorubicin-induced oxidative damage because cardiac tissue has inherently low levels of catalase, an enzyme necessary to neutralize hydrogen peroxide. This is the primary mechanism behind its cumulative cardiotoxicity.
安全性・警告
禁忌
- Pre-existing severe myelosuppression
- Impaired cardiac function
- Patients who have reached the total cumulative dose limit of doxorubicin and/or daunorubicin
- Cats with pre-existing renal insufficiency
有害事象
- Bone marrow suppression (nadir 5-10 days)
- Cardiac toxicity (acute arrhythmias and cumulative cardiomyopathy)
- Nephrotoxicity (particularly in cats)
- Gastroenteritis (anorexia, vomiting, diarrhea)
- Alopecia
- Stomatitis
- Immediate hypersensitivity/anaphylaxis (primarily in dogs)
- Severe tissue ulceration and necrosis (if extravasated)
注意事項
WARNING: Severe Vesicant & Cardiotoxin
- Extravasation Risk: Doxorubicin is extremely irritating to tissues. Perivascular administration can cause severe tissue ulceration and necrosis. Must be administered IV slowly (over at least 10 minutes) via a perfectly placed, free-flowing catheter. If extravasation occurs, treat immediately (e.g., topical DMSO or IV dexrazoxane).
- Cardiotoxicity: Risk increases greatly when cumulative dose exceeds 240 mg/m2 in dogs (and likely cats). Breeds predisposed to cardiomyopathy (Dobermans, Great Danes, Rottweilers, Boxers) require extremely careful monitoring.
- MDR1/ABCB1 Mutation: Actively transported by p-glycoprotein. Dogs with MDR1 mutations (Collies, Australian Shepherds, etc.) are at high risk for severe toxicity. Dose reduction of 25-30% is recommended.
- Hypersensitivity: Immediate reactions (urticaria, facial swelling, hypotension) can occur, especially in dogs. Pretreatment with antihistamines (e.g., diphenhydramine) or dexamethasone is often recommended.
- Handling: Teratogenic and embryotoxic. Prepare in a biological safety cabinet. Wear gloves. Wash immediately if skin contact occurs.
医薬品相互作用
May potentiate the toxic effects of doxorubicin
Potentially could increase risk for cardiotoxicity associated with doxorubicin
Decreased carbamazepine levels
Increased risk of toxicity for both agents; carefully weigh risks versus benefits
May increase doxorubicin blood levels (AUC); doxorubicin may potentiate and prolong hematologic toxicity; coma and seizures have been reported in human patients
Can increase doxorubicin and doxorubicinol (active metabolite) levels
May reduce doxorubicin effectiveness; use together not recommended in humans
Doxorubicin may decrease phenytoin levels
May increase elimination and reduce blood levels of doxorubicin
May inhibit doxorubicin metabolism
May increase doxorubicin levels
Increased risk for bleeding
Increased risk for neutropenia
Increases plasma clearance of doxorubicin
Causes a reduction in serum digoxin levels
Incompatible in syringe/line; leads to precipitate formation
Incompatible in syringe/line; leads to precipitate formation
Incompatible in syringe/line; leads to precipitate formation
Increased risk of toxicity
監視
- Efficacy of tumor response
- CBC with platelets (monitor for myelosuppression, nadir at 5-10 days)
- ECG and/or echocardiogram (especially in dogs with pre-existing heart disease or predisposed breeds)
- Hepatic function prior to and during therapy
- Urinalysis, serum creatinine, and BUN (especially in cats due to nephrotoxicity risk)
薬物動態
半減期
吸収
Not absorbed from the GI tract. Must be administered IV. Extremely irritating to tissues if administered SC or IM.
分布
Rapidly and widely distributed after IV injection. Does not appreciably enter the CSF. Highly bound to tissue and plasma proteins. Probably crosses the placenta and is distributed into milk.
代謝
Metabolized extensively by the liver and other tissues via aldo-keto reductase primarily to doxorubicinol, which is active; other inactive metabolites are also formed.
消失
Primarily excreted in the bile and feces. Only about 5% is excreted in the urine within 5 days of dosing. Eliminated in a triphasic manner.
過剰投与
Inadvertent acute overdosage may be manifested by severe exacerbations of adverse effects (profound myelosuppression, severe GI toxicity, acute cardiotoxicity). A lethal dose for dogs has been reported as 72 mg/m2.
Treatment: Supportive and symptomatic therapy is required. Dexrazoxane may be useful to help prevent cardiac toxicity and should be considered in cases of massive overdose.
製品
製剤
- Lyophilized powder for injection
- Aqueous injection
- Liposomal injection
ヒト用医薬品
- Doxorubicin HCl (Conventional) Lyophilized Powder for Injection: 10 mg, 20 mg, 50 mg, and 150 mg vials (Adriamycin RDF, generic)
- Doxorubicin HCl (Conventional) Injection (aqueous): 2 mg/mL in 5 mL, 10 mL, 25 mL, and 100 mL (Adriamycin PFS, generic)
- Doxorubicin, Liposomal Injection: 20 mg in 10 mL & 50 mg in 30 mL single-use vials (Doxil)
規制ステータス
POM (Prescription Only Medicine). Must be handled by trained personnel.
POM-V. Cytotoxic handling precautions apply.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Lyophilized powder: Store away from direct sunlight in a dry place. Reconstituted powder (with 0.9% NaCl) is stable for 24 hours at room temperature and 48 hours refrigerated. Aqueous injection: Stable for 18 months when refrigerated (2-8°C) and protected from light.
飼主向け情報
ドキソルビシン治療を受けるペットの飼い主様への重要な情報:
- 赤い尿: ドキソルビシンは赤色の薬であり、治療後1〜2日間、ペットの尿がオレンジ色から赤色になるのは完全に正常です。これは血液ではなく、無害です。
- 排泄物の安全な取り扱い: 薬はペットの排泄物から排出されます。尿や便に直接皮膚が触れないようにしてください。治療を受けた犬の尿には最大21日間、便には数日間、薬の残留物が含まれる可能性があります。粗相を片付ける際は手袋を着用し、手をよく洗ってください。
- 身体的接触: 化学療法を受けている間は、ペットが人間の皮膚、特に子供や免疫力の低下している人の顔を舐めないようにしてください。
- 予想される副作用: 治療後2〜5日で、軽度の食欲不振や時折の嘔吐がよく見られます。
- 獣医師に連絡すべき場合: ペットに極度の元気消失、異常な出血、あざ、または血便が見られた場合は、直ちに獣医師にご連絡ください。
- 脱毛: 一部のペット(特にプードルやテリアなど、毛が伸び続ける犬種)では、脱毛や毛が薄くなることがあります。
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