替魯膦酸二鈉
Tiludronate Disodium
Tiludronic Acid
別名: Tildren · Skelid · Tiludronic acid · ME-3737 · SR-41319 · acidum tiludronicum
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Navicular disease | 0.1 mg/kg tiludronic acid slow IV (over 20-30 seconds per 10 mL given) | IV | once daily | 10 days | 🌎 NA |
- Navicular disease: Alternate injection sites from day to day.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
替魯膦酸二鈉（Tiludronate disodium）是一種非含氮雙膦酸鹽類藥物，主要用於馬匹醫學以抑制骨吸收。
它最常用於靜脈注射治療馬匹的舟狀骨病（navicular disease）及遠端跗關節骨關節炎。透過調節骨骼重塑並減少局部發炎，它能顯著改善與這些疾病相關的跛行，特別是在疾病早期給藥時效果更佳。
臨床要點： 作為一種非含氮雙膦酸鹽，替魯膦酸的效力通常被認為低於較新的含氮雙膦酸鹽（如唑來膦酸），但它在馬匹骨關節疾病中具有公認的安全性和療效。在人類醫學中，其口服製劑用於治療佩吉特氏病（Paget's disease）。
作用機制
Tiludronate works by inhibiting osteoclastic bone resorption.
- Binding: The drug has a high affinity for calcium and binds strongly to hydroxyapatite crystals in the bone matrix, preferentially at sites of active bone turnover (cancellous bone > cortical bone).
- Cellular Uptake: During bone resorption, osteoclasts take up the bisphosphonate.
- Intracellular Mechanism: As a non-nitrogenous bisphosphonate, tiludronate is intracellularly metabolized into a non-hydrolyzable ATP analogue.
- Apoptosis: This toxic ATP analogue accumulates within the osteoclast → disrupts cellular energy metabolism (inhibiting ATP-dependent intracellular enzymes) → induces osteoclast apoptosis (programmed cell death).
- Result: Decreased osteoclast function and lifespan lead to a net reduction in bone resorption and stabilization of bone remodeling.
安全性與警告
禁忌症
- Renal dysfunction
- Horses producing milk for human consumption
- Horses less than 3 years old (due to lack of data on growing skeletons)
- Pregnant or lactating mares
不良反應
- Colic (reduced appetite, abdominal discomfort, pawing, restlessness)
- Muscle tremor (associated with hypocalcemia)
- Fatigue/lassitude
- Sweating
- Injection site reactions (e.g., phlebitis, especially after repeated injections)
- Salivation
- Tail hypertonia
注意事項
Important Warnings:
- Hypocalcemia Risk: Use with extreme caution in horses with pre-existing hypocalcemia or cardiac dysfunction. Bisphosphonates can acutely lower serum calcium levels.
- Administration Rate: If used in high-risk patients, slow the rate of injection significantly and monitor closely for the first few hours post-injection.
- Age Restrictions: Avoid use in young, growing animals (< 3 years old) as the effects on skeletal development are not fully established.
- Renal Clearance: The drug is eliminated unchanged by the kidneys; avoid in patients with renal impairment.
藥物相互作用
May complex with tiludronate and reduce its availability; do not mix or administer concurrently.
監測
- Clinical Efficacy (improvement in lameness)
- Serum Calcium levels
- Adverse Effects (particularly within the first 4 hours after dosing, watching for colic or muscle tremors)
藥物動力學
半衰期
吸收
Rapidly distributed to bone after intravenous injection.
分佈
Binds strongly to bone hydroxyapatite, with greater binding to cancellous bone than cortical bone. Plasma protein binding is approximately 85%.
代謝
Not extensively metabolized; acts directly on osteoclasts.
排除
Unbound drug is eliminated unchanged in the urine. Approximately 25-50% of a single IV dose is eliminated in the urine over 96 hours. Repeated daily doses do not result in plasma accumulation.
過量
Limited information is available regarding massive overdose.
- Clinical Signs: The manufacturer reports that doses of 3X the therapeutic dose in horses caused an increased frequency of adverse effects, particularly signs of colic and muscle tremor.
- Treatment: Intravenous calcium administration should be considered for signs associated with acute hypocalcemia (e.g., severe muscle fasciculations/tremors). Conventional colic treatments are recommended if gastrointestinal signs persist.
可用產品
劑型
- Injection (veterinary)
- Oral tablets (human)
獸醫用
- Tiludronic Acid: 50 mg (as tiludronate disodium) per vial, with one 10 mL vial of sterile water for reconstitution; Tildren (Sanofi/Ceva)
人用標示
- Tiludronate Disodium Oral Tablets: 240 mg (equiv. to 200 mg tiludronic acid); Skelid (Sanofi-Aventis)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store the unreconstituted powder and diluent at room temperature (15-30°C) in the outer carton. Shelf life of properly stored unreconstituted product is generally 3 years. Reconstitute the powder by aseptically adding 10 mL of the provided diluent and mix gently (resulting in 5 mg/mL). After reconstitution, use immediately and discard any remaining product. Do not mix or administer with intravenous fluids containing calcium or magnesium.
飼主須知
馬主重要須知
- 專業給藥： 本藥物必須由合格的獸醫師進行靜脈注射。
- 治療後觀察： 注射後應密切觀察您的馬匹長達 4小時。
- 注意事項： 如果您發現馬匹出現 腹痛（疝痛） 的跡象（如扒地、看著側腹、焦躁不安、食慾不振）或 肌肉顫抖/抽搐（這可能表示血鈣暫時下降），請立即聯繫您的獸醫師。
- 休息與恢復： 在舟狀骨病治療期間，請遵循獸醫師關於運動和休息的具體指示。
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