替魯膦酸二鈉
**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.
各物種劑量
- Navicular disease · 0.1 mg/kg tiludronic acid slow IV (over 20-30 seconds per 10 mL given) · IV · once daily · 10 days · Alternate injection sites from day to day.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
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
藥物相互作用
- Calcium or Magnesium-containing IV fluids (e.g., LRS, Ringer's, Plasma-Lyte, Normasol) · 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)
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.
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。