阿崙膦酸鈉
Alendronate Sodium
(4-amino-1-hydroxy-1-phosphono-butyl) phosphonic acid
別名: Fosamax · Adronat · Alendros · Arendal · Onclast · Alendronic acid · Acide Alendronique · Acido Alendronico · Acidum Alendronicum
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
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Refractory hypercalcemia | 0.5-1 mg/kg | PO | once daily | — | 🌎 NA |
| Investigational treatment of histiocytic sarcoma complex | Loading dose of 70 mg/m 2 (NOT mg/kg) | PO | daily for 14 days, then every other day for 14 days, then once weekly | — | 🌎 NA |
- Investigational treatment of histiocytic sarcoma complex: Monitor for esophageal problems (excessive salivation, regurgitation).
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Feline odontoclastic resorptive lesions (FORLs) | 3 mg/kg | PO | q12h | — | 🌎 NA |
| Idiopathic hypercalcemia (after dietary change has been attempted) | Initially 2 mg/kg. Most cats respond to 10 mg (total dose). | PO | once weekly | — | 🌎 NA |
- Feline odontoclastic resorptive lesions (FORLs): Note: Use for this indication in cats is at present very controversial. (Plumb 2006)
- Idiopathic hypercalcemia (after dietary change has been attempted): Administer at least 6 mL of water after administration and butter the lips to increase salivation and increase transit. If efficacious, effects usually seen in 3-4 weeks. Monitor via serum ionized calcium.
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
阿崙膦酸鈉 (Alendronate sodium) 是一種口服含氮雙膦酸鹽類藥物，主要用於抑制破骨細胞的骨吸收作用。
主要臨床重點：
- 主要適應症： 在獸醫學中用於治療難治性高血鈣症（例如貓的特發性高血鈣症、惡性腫瘤引起的高血鈣症）、貓破牙細胞性齒吸收病灶 (FORLs)，以及作為骨肉瘤或組織細胞肉瘤的輔助治療。
- 試驗性狀態： 在小動物的臨床經驗仍然非常有限。劑量和安全性資料仍在建立中。
- 生物利用度挑戰： 口服吸收率極差（<2%），且會因食物而大幅降低，需要嚴格的禁食計畫。
- 食道風險： 已知在人類會引起嚴重的食道刺激和糜爛；在寵物中需要特定的給藥技巧（例如餵水、在嘴唇塗抹奶油）以確保藥物快速通過胃腸道。
作用機制
Alendronate is a nitrogenous bisphosphonate that strongly binds to hydroxyapatite crystals in the bone matrix.
- Mechanism: During bone resorption, the drug is locally released and endocytosed by osteoclasts.
- Intracellular Pathway: Inside the osteoclast, alendronate inhibits the enzyme farnesyl pyrophosphate synthase (FPPS) within the mevalonate pathway → prevents the prenylation (lipid modification) of small GTP-binding proteins (such as Ras, Rho, and Rab) → disrupts osteoclast cytoskeletal organization and ruffled border formation → induces osteoclast apoptosis.
- Secondary Effects: By inhibiting osteoclastogenesis and promoting apoptosis, it indirectly reduces angiogenesis and may inhibit cancer cell proliferation in osteogenic neoplasms.
安全性與警告
禁忌症
- Esophageal abnormalities (e.g., strictures, achalasia) that delay esophageal emptying
- Inability to stand or sit upright for 30 minutes post-administration (human guideline; veterinary relevance is managed via water chasers/activity)
- Severe renal dysfunction (Creatinine Clearance < 35 mL/min)
- Known hypersensitivity to alendronate or other bisphosphonates
不良反應
- Upper GI irritation and erosions
- Esophageal stricture or ulceration
- Vomiting
- Inappetence
- Jaw osteonecrosis (rare but documented in humans)
- Musculoskeletal pain
- Hypocalcemia (with overdose)
- Hypophosphatemia (with overdose)
注意事項
Esophageal Toxicity Warning: Alendronate can cause severe local irritation to the upper gastrointestinal mucosa.
- Administration Technique: To minimize esophageal transit time and prevent erosions, ensure the patient swallows the medication completely. In dogs, walking or playing for 30 minutes post-dose is recommended. In cats, administering at least 6 mL of water and buttering the lips to induce salivation is advised.
- Renal Impairment: Use with extreme caution or avoid in patients with severe renal dysfunction.
- Investigational Use: Inform owners that the use of this drug in veterinary medicine is largely investigational, and long-term safety data is lacking.
藥物相互作用
Increased risk of upper GI adverse effects and erosions.
Likely to significantly decrease the already low oral bioavailability of alendronate.
Increased oral alendronate bioavailability two-fold in a human study.
Humans taking NSAIDs with alendronate had no higher rates of GI adverse reactions than when NSAIDs were used with placebo, though caution is still advised.
Significantly decreases alendronate absorption
Decreases alendronate absorption
監測
- Serum ionized calcium
- Serum phosphorus
- Serum potassium and sodium
- Signs of GI adverse effects (excessive salivation, regurgitation, dysphagia, inappetence)
藥物動力學
半衰期
吸收
Oral bioavailability is extremely low (<2% in all studied species; <1% in humans). The presence of food, coffee, or juice can reduce bioavailability further to negligible amounts.
分佈
Absorbed drug is rapidly distributed to bone or excreted into the urine. Accumulates on subgingival tooth surfaces and bordering alveolar bone. Not highly plasma protein bound in dogs (but is in rats). Plasma concentrations are virtually undetectable after therapeutic dosing.
代謝
Alendronate is not metabolized.
排除
Drug taken up by bone is very slowly eliminated. Once incorporated into bone, alendronate is no longer active.
過量
Toxicity Profile: No lethality was observed in dogs receiving doses up to 200 mg/kg. Lethality in rodents occurs at >550 mg/kg.
Clinical Signs of Overdose: Hypocalcemia, hypophosphatemia, and severe upper GI reactions (ulceration, erosions).
Treatment:
- DO NOT induce vomiting due to the risk of severe esophageal irritation.
- Administer oral antacids or milk immediately to bind the drug and prevent systemic absorption.
- Monitor serum calcium and phosphorus levels closely.
- Provide supportive care as needed.
可用產品
劑型
- Oral tablets
- Oral solution
人用標示
- Alendronate Sodium Oral Tablets: 5 mg, 10 mg, 35 mg, 40 mg, & 70 mg (Fosamax, generic)
- Alendronate Oral Solution: 70 mg (as base) in 75 mL; raspberry flavor (Fosamax)
各地核准狀態
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Alendronate tablets should be stored in well-closed containers at room temperature. The oral solution should be stored at room temperature; do not freeze.
飼主須知
寵物主人的重要給藥指示：
- 嚴格禁食： 如果與食物一起服用，此藥物將不會被吸收。必須在空腹時給藥，且給藥後至少 30 分鐘內必須禁食。
- 預防食道損傷： 如果阿崙膦酸鈉卡在食道中，可能會引起嚴重的潰瘍。
- 對於狗： 給藥後與您的狗散步或玩耍 30 分鐘，讓牠們保持直立姿勢，確保藥丸到達胃部。
- 對於貓： 給藥後立即用注射器餵食至少 6 毫升（約一茶匙）的水。之後在貓的嘴唇上塗抹奶油可以鼓勵吞嚥和分泌唾液，幫助藥丸安全吞下。
- 注意副作用： 如果您的寵物出現流口水、反胃、吞嚥困難、嘔吐或食慾不振的跡象，請立即聯繫您的獸醫師。
- 試驗性使用： 請了解此藥物在獸醫學中的使用相對較新，寵物的長期影響仍在研究中。
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