部份中文他克莫司水合物处方资料（仅供参考）
英文药名：Tacrolimus Hydrate
商品药名：Protopic Ointment 0.03％ for Pediatric
中文药名：他克莫司水合物
剂    型：乳膏剂
生产厂家：Maruho Corporation
プロトピック軟膏0.03％小児用
药物分类名称
治疗特应性皮炎
批准日期：1999年11月
商標名
Protopic Ointment 0.03％ for Pediatric
一般名
タクロリムス水和物（Tacrolimus Hydrate）
化学名
（3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS ）-5,19-Dihydroxy-3-｛（1E ）-2-［（1R,3R,4R ）-4-hydroxy-3-methoxycyclohexyl］-1-methylethenyl｝-14,16-dimethoxy-4,10,12,18-tetramethyl-8-（prop-2-en-1-yl）-15,19-epoxy-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3H -pyrido［2,1-c］［1,4］oxaazacyclotricosine-1,7,20,21（4H,23H ）-tetrone monohydrate
構造式
分子式
C44H69NO12・H2O
分子量
822.03
融点
130～133℃
分配係数
1000以上（1-オクタノール／水系）
性状
他克莫司水合物是白色晶体或结晶粉末。 它极易溶于甲醇或乙醇（99.5），易溶于N，N-二甲基甲酰胺或乙醇（95），几乎不溶于水。
批准条件
对于该药的长期使用情况，调查伴随免疫抑制作用的不良事件的发展状况。
药用药理学
1.实验性抑制过敏性皮炎
（1）皮肤局部大鼠皮炎和NC小鼠炎症反应自发地发展皮炎形成人类特应性皮炎的类似条件，抑制在真皮炎症细胞的增加。
（2）强烈抑制IV型过敏反应（延迟过敏反应）。
（3）对I型过敏反应的即刻型反应无效，但对晚期反应具有温和的抑制作用。
2.行动机制
（1）细胞因子产生抑制作用
IL-2通过人力辅助性T细胞，IL-3，IL-4，IL-5，干扰素γ，GM-CSF抑制比相同或类固醇，以细胞因子的产生，如（体外）更强。
（2）对肥大细胞脱颗粒的抑制作用
通过抗IgE抗体刺激刺激人肥大细胞释放的组胺比类固醇（体外）更强。
（3）抑制嗜酸性粒细胞脱颗粒
它强烈抑制钙离子载体刺激引起的人嗜酸性粒细胞碱性蛋白（ECP）的释放，而不是类固醇（体外）。
（4）抗原呈递能力抑制作用
用他克莫司预处理人皮肤朗格汉斯细胞使用朗格汉斯细胞作为抗原呈递细胞（体外）抑制混合淋巴细胞反应。
适应症
特应性皮炎
用法与用量
成年人；每天一次或两次向受影响的区域使用适当的量。 每次申请量限制为5克。
临床结果
对于患有特应性皮炎的儿科患者的软膏基质的比较试验5和长期观察试验的结果如表3所示。 针对每个患者的体重类别确定的单次施用量的上限如表4所示。
包装
5克×10管/盒
制造销售
Maruho Corporation
注：以上中文资料不够完整，使用者以原处方资料为准。
完整说明资料附件：
1）：http://www.info.pmda.go.jp/go/pack/2699709M2024_3_03/
2）：http://www.pmda.go.jp/PmdaSearch/iyakuDetail/ResultDataSetPDF/730155_2699709M1028_4_03 
Brand Names: Protopic
What is Protopic?
Protopic (tacrolimus)is a topical macrolide immunosuppressant. It works by decreasing cell activity in the body's immune system which helps to slow down the growth of atopic dermatitis (eczema) on your skin.
Protopic is used to treat severe atopic dermatitis (eczema).
Protopic may also be used for purposes not listed in this medication guide.
Important information
You should not use Protopic if you are allergic to tacrolimus.
Before using Protopic, tell your doctor if you have skin cancer or a skin infection (including herpes or chickenpox), any genetic skin disorder (such as Netherton's syndrome), a weak immune system, kidney disease, or swelling, redness, or irritation of large areas of your skin.
Protopic can lower the blood cells that help your body fight infections. This can make it easier for you to get sick from a virus such as chicken pox or herpes (cold sores or shingles). Tell your doctor if you have been exposed to any illness.
Avoid sunlight, sun lamps, tanning beds, and phototherapy treatments with UVA or UVB light. If you must be outdoors, wear loose clothing over the skin areas treated with Protopic. Do not use sunscreen on treated skin unless your doctor has told you to.
Talk to your doctor if your skin condition does not improve after using Protopic for 6 weeks.
Do not use this medication on a child younger than 2 years old. Some people have developed skin cancer or lymphoma after using Protopic or pimecrolimus (Elidel). However, it is not known if either of these medicines causes skin cancer or lymphoma. Talk to your doctor about your individual risk.
Before using Protopic
You should not use Protopic if you are allergic to tacrolimus.
To make sure you can safely use Protopic, tell your doctor if you have any of these other conditions:
•skin cancer or a skin infection (including herpes or chickenpox);
•any genetic skin disorder (such as Netherton's syndrome);
•a weak immune system (caused by disease or by using certain medicines);
•kidney disease; or
•swelling, redness, or irritation of large areas of your skin.
Protopic can lower the blood cells that help your body fight infections. This can make it easier for you to get sick from a virus such as chicken pox or herpes (cold sores or shingles). Tell your doctor if you have been exposed to any illness.
Some people have developed skin cancer or lymphoma after using Protopic or pimecrolimus (Elidel). However, it is not known if either of these medicines causes skin cancer or lymphoma. Talk to your doctor about your individual risk.
FDA pregnancy category C. It is not known whether Protopic will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. Tacrolimus 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. Do not use Protopic on a child younger than 2 years old.
How should I use Protopic?
Use Protopic exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
If you are using Protopic on a child younger than 16 years old, use only the 0.03% ointment. The 0.1% ointment is for adults and children who are at least 16 years old, but is too strong to use on younger children.
Wash your hands before and after using Protopic, unless you are using the medication to treat a hand condition.
Apply the medicine in a thin layer, only to skin areas affected by eczema. Do not cover the treated skin with a bandage.
Do not bathe, shower, or swim right after applying Protopic. Water may wash off the medicine.
You may need to use a moisturizing cream or lotion to keep your skin from getting too dry. Ask your doctor about which moisturizer to use.
Protopic is not for long-term use. Stop using the medicine once your symptoms have cleared up, unless your doctor has told you otherwise.
Call your doctor if your symptoms do not improve after 6 weeks of treatment, or if they get worse while using Protopic.
Store Protopic at room temperature. Do not freeze. Keep ointment tube tightly closed when not in use.
What happens if I miss a dose?
Apply the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.
What happens if I overdose?
An overdose of Protopic is not expected to be dangerous. Seek emergency medical attention or call the Poison Help line at 1-800-222-1222 if anyone has accidentally swallowed the medication.
What should I avoid?
Avoid using other medications on the areas you treat with Protopic unless your doctor tells you to.
Avoid exposure to sunlight or tanning beds, and phototherapy treatments with UVA or UVB light. If you must be outdoors, wear loose clothing over the skin areas treated with Protopic. Do not use sunscreen on treated skin unless your doctor has told you to. Drinking alcohol while you are using Protopic may cause your skin or face to feel hot and become flushed or red.
Protopic side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Protopic: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Stop using Protopic and call your doctor at once if you have a serious side effect such as:
•severe stinging, burning, itching, or soreness where the medicine is applied;
•swollen glands;
•redness or crusting around your hair follicles; or
•signs of a skin infection (redness, swelling, itching, oozing).
Less serious Protopic side effects may include:
•mild burning, stinging, or itching;
•skin redness;
•acne;
•cold or flu symptoms such as stuffy nose, sneezing, sore throat;
•headache; or
•feeling more sensitive to hot or cold temperatures.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.