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【药品名称】
通用名:骨化三醇胶丸
商品名称:罗盖全
英文名:Calcitriol Soft Capsules
汉语拼音:Luogaiquan
【性状】本品为胶丸，内含黄色或谈黄色的油状液体。
【药理作用】骨化三醇是维生素D3的最重要活性代谢产物之一，通常在肾脏内由其前体25-羟基维生素D3（25-HCC）转化而成，正常生理性每日生成量为0.5~1.0ug，并在骨质合成增加期内（如生长期或妊娠期）其生长量稍有增加。骨化三醇促进肠道对钙的吸收并调节骨的矿化。单剂量骨化三醇的药理作用大约可持续3~5天。骨化三醇在调节钙平衡方面的关键作用，包括对骨骼中成骨细胞活性的刺激作用，为治疗骨质疏松症提供充分的药理基础。肾性骨营养不良的患者，口服本品使肠道吸收钙的能力恢复正常，纠正低血钙，及过高的血碱性磷酶和血甲状旁腺素浓度。本品能减轻骨与肌肉疼痛，并矫正发生在纤维性骨炎和其他矿化不足病人中的组织学改变。维生素D依赖性佝偻病人，血中骨化三醇水平降低或缺失，由于肾脏内生产骨化三醇不足，可考虑本品作为一种替代性治疗。维生素D抵抗性佝偻病病人和低磷血症的病人中，血钙水平降低，本品治疗能降低磷的管式消除，并结合磷制剂的治疗，恢复骨的生长。即使在很高剂量，无证据表明维生素D对人具有致畸作用。
【药代动力学】
a) 活性成分的一般性质：吸收：骨化三醇在肠道内被迅速吸收，口服单剂本品0.25~1.0ug，3-6小时内达血药峰浓度。多次用药后，在7日内血清骨化三醇浓度达到稳态，同给药剂量有关。分布： 单剂量口服本品0.5ug2小时后，骨化三醇平均血药浓度从基础值40.0±4.4pg/ml升高到60 ±4.4pg/ml，4小时后降至53.0±6.9pg/ml，8小时后降至50.0±7.0 pg/ml,12小时后降至44±4.6pg/ml，24小时后降至41.5±5.1pg/ml。在血液转运过程中，骨化三醇和其他维生素D代谢产物同特异血浆蛋白结合。可以设想，外源性骨化三醇通过母体血液进入到胎儿的血和乳汁中。代谢：已鉴别出数种骨化三醇的代谢产物，各有不同的维生素D的活性。1a,25-二羟-24-氧代-维生素D3、1a,23,25-三羟-24-氧代-维生素D3、1a,24R，25-三羟基维生素D3、1a,25R=二羟基维生素D3-26，23S-26-三羟维生素D3、1a，25=二羟-23-氧代-维生素D3、1a,25R-26-三羟-23-氧代-维生素D3和1a-羟基-24，25，26，27-四去甲维生素D3。排泄：血中骨化三醇消除半衰期为3-6小时，但单剂量骨化三醇的药理作用大约可持续3~5天。骨化三醇被分泌进入胆汁并参与肝肠循环。健康志愿者静脉使用放射标记的骨化三醇后，24小时内，大约27%的放射活性在粪便中发现，大约7%的放射活性在尿中发现。健康志愿者口服1ug放射标记的骨化三醇， 24小时内大约10%的放射活性在尿中发展。静脉使用放射标记骨化三醇第6天，尿中和粪便中平均累积排泄量分别是16%和49%。
b) 病人的特性：肾病综合症或血液透析的病人中，骨化三醇血药浓度降低，达峰时间延长。
【适应证】
1、绝经后骨质疏松；
2、慢性肾功能低下；
3、术后甲状腺功能低下；
4、特发性甲状旁腺功能低下；
5、假性甲状腺功能低下；
6、维生素D依赖性佝偻病；
7、低血磷性维生素D抵抗型佝偻病等。
【用法用量】应根据每个病人血钙水平小心制定本品的每日最佳剂量。开始以本品治疗时，应尽可能使用最小剂量，并且不能在没有监测血钙水平的情况下增加用量。确定了本品的最佳剂量后，应每月复查一次血钙水平（或参照下面有关个别适应症之详细说明）。采集血钙标本时，不能使用止血带。若血钙超过正常范围（9~11mg/100ml或2250~2750u mol/l）1mg/100ml（250u mol/l ），或血肌酐大于120u mol/l，则必须减少剂量或完全中止治疗直至血钙正常。在血钙增高期间，必须每日测定血钙及血磷水平，血钙正常后可服用本品，但日剂量应低于前剂量0.25ug。每日应估计钙摄入量并酌情进行调整。本平最佳疗效的先决条件是足够但不过量的钙摄入量（成人：每日约800毫克），治疗开始时，补钙是必要的。因为胃肠道对钙的吸收的改善，有些病人可能宜保持较低的钙摄入量。有高血钙倾向的病人，可能只需要小剂量补钙或完全不需要补钙。每日钙总摄取量（如从食物和药物）平均大约为800mg，不应超过1000mg。口服，具体方法如下：
1、绝经后骨质疏松：推荐剂量为每次0.25ug，每日三次。服药后分别于第4周、第3个月、第6个月监测血钙和血肌酐浓度，以后每六个月监测一次。
2、肾习性骨营养不良（包括透析病人）：起始阶段的每日剂量为0.25u g血钙正常或略有降低的病人隔日0.25ug即可。如2~4周内生化指标及病情未见明显改善，则每隔2~4周将本品的每日用量增加0.25ug，在此期间至少每周测定血钙两次。大多数病人最佳用量为每日0.5至1.0ug之间。
3、甲状腺功能低下和佝偻病：推荐起始剂量为每日0.25ug，晨服。如生化指标和病情未见明显改善，则每隔2~4周增加剂量。在此期间，每捉至少测定血钙浓度两次。甲状旁腺功能低下者，偶见吸收不佳现象，因此这种病人需要较大剂量或遵医嘱.
【不良反应】由于骨化三醇能产生维生素D的作用，所以可能发生的不良反应与维生素D过量相似。如高血钙综合症或钙中毒（取决于高钙的严重程度及持续时间）。偶见的急性症状包括食欲减退、头痛、呕吐和便秘。慢性症状包括营养不良、感觉障碍，拌有口渴的发热、尿多、脱水、情感谈漠，发育停止及泌尿道感染。长达15年临床使用本品治疗所有适应症。结果显示不良反应发生率很低，包括高钙血症在内的发生率为0.111%或更低。并发高钙和高磷血症的病人（浓度大于6mg/100mmol/l）可能发生软组织钙化，这些表现可通过放射学检查而观察到。肾功能正常的病人，慢性高钙血症也许与血肌酐增高有关。由于骨化三醇的生物半衰期较短，其药代动力学研究表明，停药或减量数天后升高的血钙即回复正常范围，这一过程要比维生素D3快许多。对敏感体质的病人可能会发生过敏反应。
【禁忌】本品禁用有维生素D中毒迹象的病人。
【注意事项】
1、高血钙同本品的治疗密切相关。对尿毒症骨营养不良病人的研究表明，高达40%使用骨化三醇治疗的病人中发现高血症。饮食改变（例如：增加奶制品的摄入）以至钙摄入量迅速增加或不加控制的服用钙制剂均可导致高血钙。应告知病人及其家属，必须严格遵守处方饮食，并教会他们如何识别高钙血症的症状。一旦血钙浓度比正常值（9~11mg/100ml，或2250~2750ug mol/l）高出1ml/100ml，或血肌酐升高到大于120umol/ml，应立即停止服用本品直至血钙正常。（祥见“用法用量”）肾功能正常的患者，慢性高血钙可能与血酐增加有关。卧床病人，如术后卧床病人发生高钙血机会更大些。
2、骨化三醇能增加血无机磷水平，这时低磷血症的病人是有益的，但对肾功能衰竭的病人来说则要小心不正常的钙沉淀所造成的危险，在这种情况下，要通过口服适量的磷结合剂或减少磷质摄入量将血磷保持在正常水平（2~5mg/100ml或0.65~1.62mmol/l）。患维生素D抵抗性佝偻病人（家族性低磷血症），以本品治疗时应继续口服磷制剂。但必须考虑本品可能促进肠道对磷的吸收，这种作用可能使磷的摄入需要量减少。因此需要定期进行稳定期，每周至少测定血钙两次。（详见“用法用量”）
3、由于骨化三醇是现有的最有效的维生素D代谢产物，故不需要其他维生素D制剂与其合用，从而避免高维生素D血症。如果病人由服用维生素D3改服用骨化三醇时，则可能需要数月时间使血中维生素D3恢复至基础水平。（详见“用答用量”）
4、肾功能正常的患者服用本品时必须避免脱水，故应保持适当的水摄入量。5、对驾驶车辆和操作机器的影响基于所报道的不良反应的药效学特性，推测本品对驾驶车辆及操作机器是安全的或者说影响很小。
【相互作用】由于骨化三醇的维生素D3的最重要的代谢产物之一，因此在骨化三醇治疗期间禁止使用药理学剂量的维生素D及其衍生物制剂，以避免可能发生的附加作用和高钙血症。要对病人进行饮食指导，特别是要观察钙质的摄入情况并要对含钙制剂的使用进行控制。与噻唑类利尿剂合用会增加高钙血症的危险，对正在进行洋地黄类药物治疗的病人，应谨慎制定骨化三醇的用量，因为这类病人如发生高钙血症可能会透发新律失常。在维生素D类似物和激素之间存在功能性拮抗的关系，维生素D类制剂能促进钙的吸收，而激素类制剂则抑制钙的吸收。含镁药物（如抗酸药）可能导致高镁血症，故长期接受透析的病人使用本品进行治疗时，不能服用这类药物。由于本品影响磷在肠道、肾脏及骨髓内的输送，故应依据血磷浓度（正常值2~5mg/100ml或0.6~1.6mmol/l），调节磷结合型制剂的用量。维生素D对抗型佝偻病人（家族性低磷血症）应继续口服磷制剂。但应考虑骨化三醇可能刺激肠道磷吸收，因为该影响可能改变磷的需要量。使用二苯乙内酰胺或苯巴比妥等酶诱导剂可能会增加三醇在肠道的吸收不良。
【孕妇及哺乳期妇女用药】致畸作用：在给予家兔骨化三醇最大推荐量的2~6倍时，胎儿出现外表和骨骼畸形；同样剂量对大鼠没有致畸作用；目前没有适当的和很好被控制的试验研究本品对孕妇的影响，因而孕妇使用本品，需要衡利弊。哺乳期妇女用药：骨化三醇吸收后骨化三醇可以进行乳汁。因为许多药物都可以进入乳汁，而且骨化三醇的潜在副作用还没有确定。因此哺乳期妇女在服用骨化三醇的期间不应哺乳。
【儿童用药】本品儿童用药的安全性和有效性尚未建立。
【老人用药】老年病人无需特殊剂量，但建议监测血钙和血肌苷浓度，对于正进行透析的老年病人使用的安全性和有效性尚未建立。
【贮藏】避光，密闭，阴凉处保存。
Rocaltrol
Generic Name: calcitriol (oral) (kal si TRYE ol)
Brand Names: Rocaltrol
What is calcitriol?
Calcitriol is vitamin D3. Vitamin D is important for the absorption of calcium from the stomach and for the functioning of calcium in the body.
Calcitriol is used to treat calcium deficiency with hypoparathyroidism (decreased functioning of the parathyroid glands) and metabolic bone disease in people with chronic kidney failure.
Calcitriol may also be used for other purposes not listed in this medication guide.
What is the most important information I should know about calcitriol?
Do not use this medication if you have ever had an allergic reaction to vitamin D, or if you have high levels of calcium or vitamin D in your blood. Drink plenty of fluids unless your doctor has told you to restrict your fluid intake. Call your doctor if you have ongoing vomiting or diarrhea, or if you are sweating more than usual. Becoming dehydrated while taking calcitriol can lead to an electrolyte imbalance. Do not take other vitamin or mineral supplements unless your doctor has told you to.
Avoid using antacids without your doctor's advice. Use only the specific type of antacid your doctor recommends. Antacids contain different minerals and some types can cause serious side effects if you take them together with calcitriol.
To be sure this medication is helping your condition, your blood will need to be tested on a regular basis. Do not miss any scheduled appointments.
Calcitriol is only part of a complete program of treatment that may also include a special diet. It is very important to follow the diet plan created for you by your doctor or nutrition counselor. You should become very familiar with the list of foods you must eat or avoid to help control your condition.
What should I discuss with my healthcare provider before taking calcitriol?
Do not use this medication if you have ever had an allergic reaction to vitamin D, or if you have:
high levels of calcium in your blood (hypercalcemia); or
high levels of vitamin D in your body (hypervitaminosis D).
Before taking calcitriol, tell your doctor about all of your medical conditions. You may not be able to take calcitriol, or you may need a dose adjustment or special tests to safely take this medication.
FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Calcitriol can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.
How should I take calcitriol?
Take this medication exactly as prescribed by your doctor. Do not take it in larger amounts or for longer than recommended. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results from this medication.
Measure liquid medicine with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Drink plenty of fluids unless your doctor has told you to restrict your fluid intake. Call your doctor if you have ongoing vomiting or diarrhea, or if you are sweating more than usual. Becoming dehydrated while taking calcitriol can lead to an electrolyte imbalance.
To be sure this medication is helping your condition, your blood will need to be tested on a regular basis. You may need blood tests as often as twice a week when you first start taking calcitriol. Do not miss any scheduled appointments.
Calcitriol is only part of a complete program of treatment that may also include a special diet. It is very important to follow the diet plan created for you by your doctor or nutrition counselor. You should become very familiar with the list of foods you must eat or avoid to help control your condition.
If you need to be on bed-rest or have any type of surgery, your dose or testing needs may change. Follow your doctor's instructions. Store this medication at room temperature away from moisture, light, and heat.
What happens if I miss a dose?
Take the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine.
Overdose symptoms may include increased thirst or urination, uneven heart rate, weakness, behavior changes, bone pain, nausea, weight loss, decreased appetite, constipation, or a metallic taste in the mouth.
What should I avoid while taking calcitriol?
Do not take other vitamin or mineral supplements unless your doctor has told you to.
Avoid using antacids without your doctor's advice. Use only the specific type of antacid your doctor recommends. Antacids contain different minerals and some types can cause serious side effects if you take them together with calcitriol.
Calcitriol side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking calcitriol and call your doctor at once if you have any of these serious side effects:
increased thirst,
urinating more than usual;
pain in your lower back;
fast, slow, or uneven heart rate;
weakness, drowsiness, changes in behavior;
bone pain, muscle weakness, loss of height;
nausea, constipation, loss of appetite, weight loss;
slow growth (in a child taking calcitriol); or
dry mouth or a metallic taste.
This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.
What other drugs will affect calcitriol?
Before taking calcitriol, tell your doctor if you are taking any of the following medicines:
digoxin (digitalis, Lanoxin, Lanoxicaps);
cholestyramine (Questran, Prevalite);
sevelamer (Renagel);
ketoconazole (Nizoral);
lanthanum (Fosrenol);
seizure medication such as phenytoin (Dilantin) or phenobarbital (Solfoton);
steroids such as prednisone, fluticasone (Advair), mometasone (Asmanex, Nasonex), dexamethasone (Decadron, Hexadrol) and others; or
a (water pill) diuretic such as hydrochlorothiazide (HCTZ, Esidrix, Hydrodiuril, Microzide,Oretic), chlorothiazide (Diuril), chlorthalidone (Hygroton, Thalitone), indapamide (Lozol), metolazone (Mykrox, Zaroxolyn), and others.
This list is not complete and there may be other drugs that can interact with calcitriol. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.
Where can I get more information?
Your pharmacist can provide more information about calcitriol.
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
【原产地英文商品名】Generic ROCALTROL 0.25mcg/cap 30caps/box
【原产地英文药品名】CALCITRIOL
【中文参考商品译名】罗盖全仿制药 0.25微克/胶囊 30胶囊/盒
【中文参考药品译名】骨化三醇
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【原产地英文商品名】ROCALTROL-0.5mcg/Capsule,100Capsules
【原产地英文药品名】CALCITRIOL
【中文参考商品译名】罗盖全-0.5微克/胶囊，100胶囊/瓶
【中文参考药品译名】骨化三醇
【生产厂家中文参考译名】罗氏
【生产厂家英文名】Roche Pharma (Switzerland) Ltd.
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【原产地英文商品名】ROCALTROL-0.25mcg/Capsule,100Capsules
【原产地英文药品名】CALCITRIOL
【中文参考商品译名】罗盖全-0.25微克/胶囊，100胶囊/瓶
【中文参考药品译名】骨化三醇
【生产厂家中文参考译名】罗氏
【生产厂家英文名】Roche Pharma (Switzerland) Ltd. | 
