デクスラゾキサン
Dexrazoxane
2,6-Piperazinedione
別名: Zinecard · Cardioxane · Eucardion · Totect · ADR-529 · ICRF187 · NSC-169780 · ICRF-187
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 |
|---|---|---|---|---|---|
| Treatment of anthracycline (doxorubicin, epirubicin, etc.) extravasation | 1000 mg/m2 | IV | within 6 hours and again on day 2. Infuse 500 mg/m2 on day 3 | 3 days | 🌎 NA |
| Treatment of anthracycline extravasation | 10 times the doxorubicin dose | IV | within 3 hours and again at 24 and 48 hours after extravasation | 48 hours | 🌎 NA |
| Prevention of doxorubicin-induced cardiomyopathy | 10:1 ratio (e.g., 300 mg/m2 of dexrazoxane to 30 mg/m2 doxorubicin) | IV | starting 30 minutes of, and prior to the doxorubicin dose | — | 🌎 NA |
| Prevention of doxorubicin-induced cardiomyopathy | 10:1 ratio (e.g., 300 mg/m2 of dexrazoxane to 30 mg/m2 doxorubicin) | IV | starting 30 minutes before doxorubicin is administered | — | 🌎 NA |
- Treatment of anthracycline (doxorubicin, epirubicin, etc.) extravasation: Terminate doxorubicin infusion immediately, and infuse intravenously in a separate infusion. Acute surgical evaluation is performed. Dosage recommendations are for human patients, but may apply to veterinary patients.
- Treatment of anthracycline extravasation: Anecdotally; significantly reduces local tissue injury.
- Prevention of doxorubicin-induced cardiomyopathy: Given as slow IV bolus (as a short, IV bolus).
- Prevention of doxorubicin-induced cardiomyopathy: Given as slow IV bolus. Use can be considered in breeds at risk (Shelties, Collies, Australian Shepherds, etc.), dogs exceeding usual cumulative dose cutoff, and cases with preexisting cardiac disease where no effective chemo options exist.
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
デクスラゾキサンは、主に獣区腫瘍学で使用される細胞内鉄キレート剤および化学防護剤です。
- 心臓保護：アントラサイクリン系薬（ドキソルビシンなど）に関連する累積的かつ用量依存的な心毒性を軽減するために使用されます。
- 血管外漏出の管理：ドキソルビシンの誤った血管外投与（漏出）によって引き起こされる重知な組織壞死に対する重要な解毒剤として機能します。
臨床のポイント：
- 心臓保護には非常に有効ですが、非常に高価であり、多くの飼い主にとって費用がネックになる場合があります。
- デクスラゾキサンががん細胞を部分的に保護し、化学療法の抗腫瘍効果を低下させる可能性があるという理論的懸念と人での証拠があります。
作用機序
Dexrazoxane is a cyclic derivative of EDTA that readily penetrates cell membranes.
- Once intracellular, it is hydrolyzed into an active ring-opened chelating metabolite.
- Active Metabolite → Chelates intracellular iron → Prevents the formation of the highly reactive anthracycline-iron complex.
- This prevents the generation of destructive superoxide free radicals → Protects the myocardium from oxidative stress and irreversible anthracycline-induced cardiomyopathy.
- Mechanistic Note: It also acts as a reversible inhibitor of Topoisomerase II, which is believed to contribute to its protective effects against severe tissue necrosis during extravasation injuries.
安全性・警告
禁忌
- Should not be used unless an anthracycline antineoplastic agent is being used
- Unknown based on monograph, but generally avoid in patients not receiving anthracyclines
有害事象
- Additive myelosuppression
- Potential reduction in efficacy of anthracycline antitumor agents
- Testicular atrophy (observed in dogs)
- Myelosuppression (documented in humans)
- Decreased clinical efficacy of anthracycline antineoplastic agents
注意事項
Important: Dexrazoxane should not be used unless an anthracycline antineoplastic agent is being administered.
- Species Limitations: Efficacy and safety for use in cats is not known.
- Reproductive Safety: Causes testicular atrophy in dogs when administered at usual doses for 13 weeks. Teratogenic in rats and rabbits at doses lower than human doses (FDA Category C). Nursing mothers should discontinue nursing.
- Handling Warnings: Wear gloves when handling. Use normal procedures for handling and disposal of anti-cancer medications. If unreconstituted powder contacts skin or mucous membranes, wash off thoroughly with soap and water.
医薬品相互作用
Additive myelosuppression may occur when used concurrently.
May decrease the clinical efficacy of the chemotherapy
監視
- Echocardiogram (if used for cardioprotection)
- ECG (if used for cardioprotection)
- Complete blood count (CBC) for myelosuppression
- Cardiac monitoring (ECG, echocardiogram) if used for cardiotoxicity
- Extravasation site for healing or necrosis
薬物動態
半減期
分布
Steady-state volume of distribution is 0.67 L/kg. The drug showed low tissue and protein binding.
代謝
Hydrolyzed to an active metabolite.
消失
Clearance is about 11 mL/min/kg (dose-independent). Primarily excreted in the urine as unchanged drug and metabolites.
過剰投与
Because of the method of administration and drug expense, overdoses are unlikely in veterinary medicine. As there is no known antidote, treatment would be supportive. Potentially, the drug could be removed via hemodialysis.
製品
製剤
- Lyophilized Powder for Injection Solution
- Intravenous: 500 mg vials (reconstituted to 20 mg/ml solution for infusion)
ヒト用医薬品
- Dexrazoxane Lyophilized Powder for Injection Solution: 250 mg in single-use vials with 25 mL vial of sodium lactate injection
- Dexrazoxane Lyophilized Powder for Injection Solution: 500 mg regular & preservative free in single-use vials with 50 mL vial of sodium lactate injection
- Cardioxane 500 mg vials
- Zinecard 500 mg vials
規制ステータス
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Unreconstituted vials should be stored at 25°C (77°F); excursions permitted to 15-30°C (59-86°F). Once reconstituted with supplied diluent, stable for 6 hours at room temperature or refrigerated. Unused solutions after that time should be discarded. After reconstitution, may be diluted with 0.9% sodium chloride or D5W to 1.3-5 mg/mL. Do not mix with any other drug.
飼主向け情報
- 目的：あなたのペットは、特定の抗がん剤（ドキソルビシンなど）の副作用から心臓を守るため、または抗がん剤が誤って血管外に漏れた場合の重知な組織損傷を治療するためにこの薬を投与されています。
- 費用と期待される効果：これは非常に専門的で高価な薬です。心臓のダメージや組織損傷のリスクを大幅に軽減しますが、すべてのケースで完全に効果があるわけではありません。
- 副作用：白血球数が減少し、感染症にかかりやすくなる可能性があります。血液検査を慎重にモニタリングします。
- 安全性：この薬は抗がん剤と共に投与されるため、自宅でのペットの排泄物の安全な処理については、獣区区師の指示に従ってください。
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