部份中文唑来膦酸处方资料（仅供参考） 
药品英文名
Zoledronic Acid
药品别名
Zometa
药物剂型
注射用唑来膦酸冻干粉针剂：4mg/支。30℃以下保存。
药理作用
本品是一种特异性地作用于骨的二磷酸化合物，主要是抑制骨的再吸收。在体外可抑制破骨细胞凋亡，还可通过与骨的结合阻断破骨细胞对矿化骨和软骨的吸收。还可以抑制由肿瘤释放的多种刺激因子引起的破骨细胞活动增强和钙释放。
药动学
本品2mg、4mg、8mg、16mg单剂量输注，药代动力学数据有剂量依赖性。本品经体循环快速双相消除，半衰期为t1/2α0.23h和t1/2β1.75h，继之以终点半衰期为167h的长相消除；本品经肾脏以原形排出。在给药后的24h内，44%±18%的给药量从尿中排泄，其余主要与骨组织结合，随后缓慢释放进入全身循环再经过肾脏消除。本品与血浆蛋白结合率约为22%，且与药物浓度无关。本品全身清除率为(5.6±2.5)ml/(kg·h)，与剂量无关，也不受性别、年龄、种族和体重的影响。输注时间从5min增加到15min，输注终点本品浓度可下降30%，但不影响AUC。药动学参数的个体差异显著。
适应证
用于骨转移瘤及恶性肿瘤引起的高钙血症。
禁忌证
1.对本品及赋形剂或其他双膦酸盐过敏者禁用。
2.有严重肾功能不全的骨转移瘤患者[血清肌酸酐浓度≥3mg/(L·min)]禁用。
3.本品的妊娠安全性分级为D级，孕妇禁用。
4.尚不明确本品是否能分泌入乳汁，哺乳期妇女禁用。
注意事项
1.轻中度肾损害者(血清肌酸酐＜400µmol/L)，无需调整剂量；严重肾损害者(血清肌酸酐＞400µmol/L)者，需在权衡利弊后才可使用。
2.伴有恶性高钙血症的患者给予本品前应充分补水。
3.尚未确定儿童用药的安全性和有效性。
4.冻干粉经无菌溶解和稀释后，应立即使用。从溶解、稀释、在2～8℃冰箱内贮存至最后使用的全过程不应超过24h。
5.给药前应监测血清肌酸酐浓度，定期监测血钙、血磷、血镁浓度。长期用药者，应每3～6个月检查患者是否患有白蛋白尿和氮质血症。
6.药物过量可致血清中钙、磷、镁水平过低，可静脉给予葡萄糖酸钙、磷酸钾或磷酸钠、硫酸镁补充。
不良反应
1.心血管系统：约10.5%的患者出现低血压。
2.中枢神经系统：骨质溶解性骨转移瘤和佩吉特病患者用药后，常见疲劳，且与剂量无关。恶性肿瘤高钙血症患者用药后，可引起焦虑和失眠。
3.代谢/内分泌系统：在出现早期抗吸收作用时，可见血磷浓度降低和无症状性低钙血症，且与剂量呈相关性。罕见低镁血症。
4.肌肉骨骼系统：有出现下颌骨、上颌骨或上下颌骨的痛性骨外露的报道。
2004年FDA警告：本品可致颌骨坏死。
5.泌尿生殖系统：有肾功能恶化进展为肾衰竭并需要透析的报道。
6.肝脏：罕见肝酶升高。
7.胃肠道：偶见念珠菌性感染(念珠菌病)引起的口腔痛或咽喉痛。
8.眼：偶见眼激惹和结膜炎，罕见巩膜炎。
9.其他：约30%～44%的患者出现剂量相关性发热，多在用药后5天内出现，但大多数症状较轻。曾有引起非特异性流感样症状(包括发热、寒战、骨痛、关节痛和肌肉痛)的报道。
用法用量
静滴。
1.治疗骨转移瘤：每次4mg，时间至少15min，3～4周1次。建议应同时联用标准的抗肿瘤治疗，且应口服补充钙(500mg)和维生素D(400U)。对前列腺癌患者，至少应同时进行1个疗程的激素治疗。
2.恶性肿瘤高钙血症：每次4mg，时间至少15min。若初次治疗后血清钙浓度没有恢复到正常范围内，建议再给予4mg，但两次治疗至少应间隔7天，以便充分发挥第一次治疗的疗效。
3.肾功能不全时剂量：有肾脏疾病但血清肌酸酐浓度低于265µmol/L[或低于3mg/(L·min)]的患者，无需调整剂量和给药时间。
4.将4mg本品用5ml无菌注射用水重新配制，然后用100ml 0.9%生理盐水(或5%葡萄糖注射液)稀释。1次剂量不宜超过4mg，给药时间至少15min。
药物相应作用
1.本品与氨基糖苷类同时使用能够产生降低血钙的叠加作用，从而导致长期低血钙，需格外小心。在治疗过程中也应注意低血镁的发生。
2.本品不得与含钙溶液配伍使用，应与其他药品分开进行单次静脉输注。
3.有肾功能恶化的恶性肿瘤高钙血症患者，合用沙利度胺，可增加引起肾功能不全的危险性。
4.利尿药与本品合用时只能在充分补水后使用。
INDICATION
ZOMETA is also used to reduce and delay bone complications due to multiple myeloma and bone metastases from solid tumors; used with anti-cancer medicines. ZOMETA is not an anti-cancer therapy. If you have prostate cancer, you should have failed treatment with at least one hormonal therapy prior to taking ZOMETA.
IMPORTANT SAFETY INFORMATION
Do not use ZOMETA if you have had a severe allergic reaction to zoledronic acid or any components of ZOMETA. These reactions, including rare cases of hives and angioedema (swelling often near your eyes and lips), and very rare cases of life-threatening allergic reactions, have been reported. ZOMETA is in a class of drugs called bisphosphonates, and contains the same active ingredient as that found in Reclast® (zoledronic acid). If you are treated with ZOMETA, you should not be treated with Reclast.
If you have kidney problems, tell your doctor. The risk of adverse reactions (especially related to the kidney) may be greater for you. ZOMETA treatment is not for patients with severe kidney problems. Patients with kidney problems on multiple cycles of ZOMETA or other bisphosphonates are at greater risk for further kidney problems. It is important to get your blood tests while you are receiving ZOMETA. Your doctor will monitor your kidney function before each dose. Tell your doctor if you are on other drugs, including aminoglycosides, loop diuretics, and drugs which may be harmful to the kidney.
Osteonecrosis of the jaw (ONJ) has been reported mainly in cancer patients treated with intravenous bisphosphonates, including ZOMETA®. Many of these patients were also receiving anti-cancer drugs and corticosteroids, which may make it more likely to get ONJ. If you have advanced breast cancer or a type of cancer called multiple myeloma, or if you have had dental extraction, periodontal disease, local trauma, including poorly fitting dentures, you may be at greater risk of getting ONJ. Many reports of ONJ involved patients with signs of local infection, including bone/bone marrow inflammation. You should maintain good oral hygiene and have a dental examination with preventive dentistry prior to beginning ZOMETA®. While on treatment, avoid invasive dental procedures, if possible, as recovery may take longer. If you develop ONJ while on bisphosphonate therapy, dental surgery may worsen the condition. If you require dental procedures, there are no data available to suggest whether stopping ZOMETA® treatment reduces the risk of ONJ. A causal relationship between bisphosphonate use and ONJ has not been established. Based on your condition, your doctor will determine the treatment plan you will receive.
Do not use ZOMETA if you are pregnant or plan to become pregnant, or if you are breast-feeding.
Severe and occasionally incapacitating bone, joint, and/or muscle pain has been reported in patients taking bisphosphonates, including ZOMETA. Do not continue using ZOMETA if severe symptoms develop, as some patients had the symptoms reappear after taking ZOMETA or another bisphosphonate again. In aspirin sensitive patients, bronchoconstriction (tightening of the airways in the lungs) has been observed while taking bisphosphonates.
Common side effects include bone pain, nausea, fatigue, anemia, fever, vomiting, constipation, shortness of breath, diarrhea, weakness, muscle pain, anorexia, cough, joint pain, lower-limb swelling, worsening of your cancer, headache, dizziness (excluding vertigo), insomnia, decreased weight, back pain, numbness/tingling, and abdominal pain.
Eye-related side effects may occur with bisphosphonates, including ZOMETA. Cases of swelling related to fluid build-up in the eye, as well as inflammation of the uvea, sclera, episclera, conjunctiva, and iris of the eye have been reported.
You should be taking an oral calcium supplement of 500mg and a multiple vitamin containing 400 IU of vitamin D daily.


唑来膦酸一年用一次即可防治骨质疏松
唑来膦酸（zoledronic acid）最近获欧盟批准上市，用于停经期后女性的骨质疏松治疗。与一天、一周或一月给药一次的口服二膦酸盐治疗药不同，唑来膦酸是一年给药一次，静脉滴注15分钟。有调查数据显示，70%的病人更倾向于这种给药方式。对髋骨骨折的骨质疏松病人所作的迄今惟一的研究表明，与安慰剂组比较，一年静脉滴注唑来膦酸一次的患者可使随后发生的任何形式的骨质疏松性骨折风险降低35%。一项涉及2100例男性和女性的再发骨折临床试验也显示，治疗组病人的死亡风险比安慰剂组降低28%。  

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