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部分中文他克莫司处方资料（仅供参考）
药品英文名
Tacrolimus
药品别名
普乐可复、他克莫司 Prograf、FK-506
药物剂型
1.胶囊：1mg，5mg；
2.注射剂：5mg(1ml)。
药理作用
与CsA相似，FK506能够抑制T细胞活性。其免疫抑制作用是CsA的10～100倍。此外，FK506还能抑制嗜碱粒细胞及肥大细胞释放组胺，阻止前列腺素D2的合成，抑制5-HT及白三烯的生成，因而也具有良好的抗炎作用。
药动学
他克莫司口服吸收良好，系统应用主要通过细胞色素P450同工酶3A4代谢。代谢产物的主要成分为13-氧去甲基代谢物，其药理活性是他克莫司的6.4%。他克莫司以胆汁排泄为主，清除率每小时2.25L，血浆半衰期40h。他克莫司外用后，13%～23%存在于表皮，0.5%～1%在真皮层，1%～4%透皮进入血液。他克莫司的透皮药量较CsA更大。
适应证
1.全身用药：适用于严重银屑病、白塞病、坏疽性脓皮症、移植物抗宿主病、类风湿性关节炎等。
2.局部用药：用于遗传过敏性皮炎(异位性皮炎)、银屑病、坏疽性脓皮症等。
禁忌证
1.对本药或其他大环类药物过敏。
2.孕妇禁用。
注意事项
1.慎用：
(1)肝肾功能不全；
(2)糖尿病；
(3)高钾血症；
(4)心室肥大；
(5)有神经性毒性表现者(如震颤、头痛、共济失调、精神状态改变等)；
(6)哺乳期妇女。肾功能不全及高血压患者慎用；
2.避免与保钾利尿药合用。
不良反应
1.长期系统应用有肾毒性，可减少肾小球滤过率，损伤肾小管，血清肌酐升高，引起高钾血症、低镁血症等。
2.神经精神症状：焦虑、暂时性失浯、癫痫、躁狂等。
3.其他不良反应有高血压、血胆固醇及三酰甘油升高。
4.外用有轻微刺激，不引起皮肤萎缩。
用法用量
1.口服：每天0.05～0.3mg/kg，分2～3次口服，根据病种及病情轻重调整剂量,一般疗程数周到数月。
2.他克莫司软膏外用，浓度为0.03%～0.4%，每天2次。对斑块型银屑病可用封包疗法,每2～3天更换1次。
药物相应作用
1.本药为强效药酶抑制药，可抑制环孢素、红霉素、交沙霉素、酮康唑、咪康唑，克霉唑、氟康唑、伊曲康唑、地尔硫，硝苯地平，皮质激素(如可的松、睾酮)、溴隐亭、维拉帕米、奥美拉唑、麦角胺、咪达唑仑等的代谢，使上述药物血药浓度升高。
2.抑制细胞色素P4503A4酶系统的药物，如溴隐亭、可的松、氨苯砜、麦角胺、炔雌醇、甲地孕酮、依他康唑、交沙霉素、利多卡因、甲妥因、咪康唑，咪唑安定、尼卡地平、尼鲁地平、尼伐地平、炔诺酮、奎尼丁、他莫昔芬、三醋酸竹桃霉素、维拉帕米、柑桔素(Naringenine)等，可能抑制本药的代谢，使本药血药浓度升高。
3.诱导细胞色素P4503A4酶系统的药物，如巴比妥
专家点评
他克莫司系统应用治疗严重的顽固性银屑病疗效高且耐受性好，但减量或停药后仍可复发，故应注意选择病例。对糖皮质激素、CsA等治疗无效的白塞病、坏疽性脓皮病，他克莫司亦有较好效果。他克莫司外用较CsA有更好的透皮性，对异位性皮炎、银屑病、坏疽性脓皮病等有较好疗效。尤其在治疗异位性皮炎方面效果显著，未发现严重不良反应。
What is Prograf (Tacrolimus) ?
Prograf (Tacrolimus) lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats it as an invader.Prograf (Tacrolimus) is used together with other medicines to prevent your body from rejecting a heart, liver, or kidney transplant.Prograf (Tacrolimus) may also be used for other purposes not listed here.
Important information about Prograf (Tacrolimus)
Taking Prograf (Tacrolimus) may increase your risk of developing certain types of cancer, especially skin cancer. The risk may be higher in people who are treated over long periods of time with drugs that weaken the immune system. Talk with your doctor about your individual risk.While taking Prograf (Tacrolimus) avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Use a sunscreen (minimum SPF 15) and wear protective clothing if you must be out in the sun.There are many other medicines that can interact with Prograf (Tacrolimus) . Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.Do not consume grapefruit or grapefruit juice during treatment with Prograf (Tacrolimus) unless your doctor has told you do. Prograf (Tacrolimus) can have a dangerous interaction with grapefruit or grapefruit juice.Prograf (Tacrolimus) can lower the blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. To be sure your blood cells do not get too low, your blood will need to be tested on a regular basis. Your kidney or liver function may also need to be tested. Do not miss any scheduled appointments.Some people receiving Prograf (Tacrolimus) after a kidney transplant have developed diabetes, most often in people who are Hispanic or African-American. Talk with your doctor about your individual risk of diabetes.
Before taking Prograf (Tacrolimus)
You should not take Prograf (Tacrolimus) if you are allergic to tacrolimus or hydrogenated castor oil.If you have certain conditions, you may need a dose adjustment or special tests to safely use this medication. Before taking Prograf (Tacrolimus) , tell your doctor if you have:kidney disease; liver disease; high blood pressure; orif you have used cyclosporine (Neoral, Sandimmune, Gengraf) within the past 24 hours.Some people receiving Prograf (Tacrolimus) after a kidney transplant have developed diabetes. This effect has been seen most often in people who are Hispanic or African-American. Talk with your doctor about your individual risk of diabetes if you have concerns.Taking Prograf (Tacrolimus) may increase your risk of developing certain types of cancer, especially skin cancer. The risk may be higher in people who are treated over long periods of time with drugs that weaken the immune system. Talk with your doctor about your individual risk.
How should I take Prograf (Tacrolimus) ?
Take Prograf (Tacrolimus) exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.You may receive an injection of Prograf (Tacrolimus) shortly after your transplant. The injection is given around-the-clock until you are ready to take the pill form of Prograf (Tacrolimus) .The Prograf (Tacrolimus) capsule is usually taken every 12 hours. Your doctor may occasionally change your dose to make sure you get the best results from this medication.Prograf (Tacrolimus) can lower the blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. To be sure your blood cells do not get too low, your blood will need to be tested on a regular basis. Your kidney or liver function may also need to be tested. Do not miss any scheduled appointments.Store this medication at room temperature away from moisture and heat.
What happens if I miss a dose?
Take the medication as soon as you remember. If it is almost time for the next dose, skip the missed dose and take the medicine at the next regularly scheduled time. 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. Symptoms of a Prograf (Tacrolimus) overdose are unknown.
What should I avoid while taking Prograf (Tacrolimus) ?
Avoid contact with people who have colds, the flu, or other contagious illnesses. Contact your doctor immediately if you develop signs of infection.Do not consume grapefruit or grapefruit juice during treatment with Prograf (Tacrolimus) unless your doctor has told you do. Prograf (Tacrolimus) can have a dangerous interaction with grapefruit or grapefruit juice. Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Prograf (Tacrolimus) may increase the risk of skin cancer. Use a sunscreen (minimum SPF 15) and wear protective clothing if you must be out in the sun.Do not receive a "live" vaccine while you are being treated with Prograf (Tacrolimus) . Vaccines may not work as well during your treatment with this medicine.
Side effects of Prograf (Tacrolimus):
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. Call your doctor at once if you have any of these serious side effects:pain in the lower back or side;urinating less than usual or not at all;painful urination, blood in your urine;problems with your vision, speech, or coordination;tremor (shaking), headache, confusion, numbness or tingly feeling;pale skin, easy bruising or bleeding, unusual weakness;fever, chills, body aches, flu symptoms;slow heart rate, weak pulse, muscle weakness;tiredness, fast or pounding heartbeat, mild shortness of breath; orincreased urination, thirst, or hunger.
Less serious Prograf (Tacrolimus) side effects may include:swelling in your hands or feet;nausea, vomiting, diarrhea, constipation, stomach pain, loss of appetite;sleep problems (insomnia); oritching skin or mild rash.
What other drugs will affect Prograf (Tacrolimus) ?
Prograf (Tacrolimus) can be harmful to the kidneys, and this effect is increased when Prograf (Tacrolimus) is used together with other medicines that can harm the kidneys.Before taking Prograf (Tacrolimus) , tell your doctor if you are receiving chemotherapy, or using medicines to treat a bowel disorder, antiviral medications, pain or arthritis medicines, any injected antibiotics, or other medications to prevent organ transplant rejection. You may need dose adjustments or special tests when taking any of these medications together with Prograf (Tacrolimus) .Many drugs can interact with Prograf (Tacrolimus) . Below is just a partial list. Tell your doctor if you are using:birth control pills or hormone replacement;metoclopramide (Reglan);mycophenolate mofetil (CellCept);sirolimus (Rapamune);St John's wort;lansoprazole (Prevacid), omeprazole (Prilosec, Zegrid)rifampin (Rifadin, Rimactane, Rifater) or rifabutin (Mycobutin);a potassium supplement or a diuretic (water pill);a calcium channel blocker such as verapamil (Calan, Verelan), diltiazem (Cardizem, Dilacor XR, Tiazac), nifedipine (Adalat, Procardia), or nicardipine (Cardene);antifungal medicines such as ketoconazole (Nizoral), itraconazole (Sporanox), fluconazole (Diflucan), caspofungin (Cancidas), clotrimazole (Mycelex Troche), voriconazole (VFEND);erythromycin (Ery-Tab, E-Mycin, E.E.S.), clarithromycin (Biaxin), or troleandomycin (TAO);HIV medicines such as lopinavir/ritonavir (Kaletra), nelfinavir (Viracept), or ritonavir (Norvir);an antacid containing magnesium or aluminum such as Rulox, Amphojel, Milk of Magnesia; orseizure medicine such as carbamazepine (Carbatrol, Tegretol), phenobarbital (Luminal), phenytoin (Dilantin).
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产地国家: 美国
原产地英文商品名:
PROGRAF 0.5mg/cap 100caps/box
原产地英文药品名:
TACROLIMUS ANHYDROUS
中文参考商品译名:
普乐可复 0.5毫克/胶囊 100胶囊/盒
中文参考药品译名:
无水他克莫司
生产厂家中文参考译名:
安斯泰来
生产厂家英文名:
ASTELLAS
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产地国家: 美国
原产地英文商品名:
PROGRAF 1mg/cap 100caps/box
原产地英文药品名:
TACROLIMUS ANHYDROUS
中文参考商品译名:
普乐可复 1毫克/胶囊 100胶囊/盒
中文参考药品译名:
无水他克莫司
生产厂家中文参考译名:
安斯泰来
生产厂家英文名:
ASTELLAS
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产地国家: 美国
原产地英文商品名:
PROGRAF 5mg/cap 100caps/box
原产地英文药品名:
TACROLIMUS ANHYDROUS
中文参考商品译名:
普乐可复 5毫克/胶囊 100胶囊/盒
中文参考药品译名:
无水他克莫司
生产厂家中文参考译名:
安斯泰来
生产厂家英文名:
ASTELLAS
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