司維拉姆
司維拉姆(Sevelamer)是一種不含鈣和鋁的**磷結合劑**,主要用於治療與**慢性腎臟病 (CKD)** 相關的高血磷症。 * **臨床優勢**:與傳統的磷結合劑(如氫氧化鋁或碳酸鈣)不同,司維拉姆不會引起鋁中毒或醫源性高血鈣症的風險。 * 對於無法耐受鋁鹽或使用鈣結合劑可能加重轉移性組織鈣化的晚期 CKD 患畜特別有用。 * **注意**:與傳統的鋁或鈣製劑相比,其價格通常較為昂貴。
作用機制: Sevelamer is a cross-linked polymeric amine that acts locally in the gastrointestinal tract. * **Mechanism**: The polymer contains multiple amine groups that become partially protonated in the acidic environment of the stomach and intestine. These protonated amines interact with dietary phosphate ions via **ionic and hydrogen bonding** → preventing phosphate absorption across the gut wall → increasing fecal excretion of phosphate → ultimately lowering serum phosphorus levels. * **Secondary Effects**: It also binds bile acids in the gut, which can lead to a reduction in serum low-density lipoproteins (LDL) and total cholesterol.
各物種劑量
- Hyperphosphatemia · 200 mg 2-3 times daily · PO · q8-12h · Anecdotally appears to be safe and effective.
- Chronic kidney disease (hyperphosphataemia) · 30-40 mg/kg · PO · q8h · Titrated to the desired serum phosphate concentration · Should be given with meals and at least 1 hour before or 3 hours after other medications.
- Hyperphosphatemia · 400 mg PO with meals · PO · with meals · For medium to large sized dog
- Chronic kidney disease (hyperphosphataemia) · 30-40 mg/kg · PO · q8h · Titrated to the desired serum phosphate concentration · Should be given with meals and at least 1 hour before or 3 hours after other medications.
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給藥途徑
禁忌症
- Hypophosphatemia
- Bowel obstruction
- Known hypersensitivity to sevelamer
- Gastrointestinal obstruction
不良反應
- Gastrointestinal upset (nausea, vomiting, diarrhea, or constipation)
- Decreased absorption of fat-soluble vitamins (A, D, E, K) and folic acid
- Constipation
- Pills are hygroscopic and will expand (potential risk of esophageal obstruction if not swallowed quickly)
藥物相互作用
- Anticonvulsants (oral) · Sevelamer may reduce oral absorption; give at least 1 hour before or 3 hours after sevelamer.
- Antiarrhythmics (oral) · Sevelamer may reduce oral absorption; give at least 1 hour before or 3 hours after sevelamer.
- Ciprofloxacin (and other oral fluoroquinolones) · Concurrent administration may decrease absorption by 50%; administer at least 1 hour before or 3 hours after sevelamer.
- Oral Medications (Narrow Therapeutic Index) · May reduce absorption; consider dosing other oral drugs separately.
- Vitamins · Sevelamer may reduce vitamin absorption from food; consider administering vitamin supplements separately.
- Other oral medications · May bind to and decrease the absorption of concurrently administered oral drugs. Should be given at least 1 hour before or 3 hours after other medications. · moderate
- Fat-soluble vitamins (e.g., Vitamin K) · May inhibit vitamin absorption; consider monitoring prothrombin time. · moderate
監測
- Serum phosphorus
- Serum calcium
- Serum bicarbonate
- Serum chloride
- Baseline coagulation screening test (before and after therapy implementation, due to potential Vitamin K malabsorption)
- Serum phosphate levels (at 4-6 week intervals to adjust dosage)
- Prothrombin time (due to potential vitamin K malabsorption)
- Bowel movements (monitor for constipation)
過量
Because sevelamer is not absorbed systemically, the potential for acute toxicity from an overdose appears to be **negligible**. Overdose would likely result in gastrointestinal distress (constipation or diarrhea) and potential hypophosphatemia.
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