IMMUNE SUPPRESSANTS 免疫抑制剂 T- and B-Cell Suppressors T和B细胞抑制剂
Several T- and B-cell immune suppressors are available for use.
目前所用的T和B细胞抑制剂有几种。
Therapeutic Actions and Indications 治疗作用和适应症
The exact mechanism of action of the T- and B-cell suppressors is not clearly understood. It has been shown that they block antibody production by B cells, inhibit suppressor and helper T cells, and modify the release of interleukins and of T-cell growth factor.
The T- and B-cell suppressors are indicated for the prevention and treatment of specific transplant rejections.
预防和治疗特定移植排斥需要T和B细胞抑制剂。
Pharmacokinetics 药代动力学
Cyclosporine is well absorbed from the GI tract, reaching peak levels in 1 to 2 hours. It is extensively metabolized in the liver by the cytochrome P450 system and is primarily excreted in the bile. The half-life of the drug is about 19 hours for Sandimmune and 8.4 hours for Neoral. It is available as an oral solution that can be mixed with milk, chocolate milk, or orange juice for ease of administration.
Abatacept must be given as a 30-minute infusion every 2 to 4 weeks, depending on the patient’s response. Peak levels are reached at the end of the infusion. Abatacept has a half-life of 12 to 23 days and usually reaches a steady state by 60 days of treatment. The drug is cleared from the body by the kidneys.
Alefacept is rapidly absorbed and can be given IM or IV. It reaches peak levels in 4 to 6 hours and has a half-life of 270 hours.
阿来西普吸收快，可IM或IV给药；4-6小时后达峰，半衰期270小时。
Azathioprine is rapidly absorbed from the GI tract, reaching peak levels in 1 to 2 hours. This drug is catabolized in the liver and red blood cells.
硫唑嘌呤GI吸收快，1-2小时达峰，经肝和红血细胞代谢。
Little is known about the pharmacokinetics of glatiramer. Some of it is immediately hydrolyzed on injection, some enters the lymph system, and some may actually reach the systemic circulation.
Mycophenolate is readily absorbed and immediately metabolized to its active metabolite. Most of the metabolized drug is then excreted in the urine.
麦考酚酯吸收快，即时代谢为活性代谢物。多数代谢后药物经尿排出。
Sirolimus is rapidly absorbed from the GI tract, reaching peak levels in 1 hour. It is extensively metabolized in the liver, partly by the cytochrome P450 system. The drug is then excreted primarily in the feces.
Tacrolimus is rapidly absorbed from the GI tract, reaching peak levels in 1.5 to 3.5 hours. It is extensively metabolized in the liver by the cytochrome P450 system and is excreted in the urine.
他克莫司胃肠道吸收快，1.5 – 3.5小时后达峰，在肝经细胞色素P450广泛代谢，经尿排出。
Contraindications and Cautions 禁忌症与注意事项
The use of T- and B-cell suppressors is contraindicated in the presence of any known allergy to the drug or its components and during pregnancy and lactation because of the potential serious adverse effects on the fetus or neonate. Caution should be used with renal or hepatic impairment, which could interfere with the metabolism or excretion of the drug, and in the presence of known neoplasms, which potentially could spread with immune system suppression.
Adverse Effects 不良效应
Patients receiving these drugs are at increased risk for infection and for the development of neoplasms due to their blocking effect on the immune system. Other potentially dangerous adverse effects include hepatotoxicity, renal toxicity, renal dysfunction, and pulmonary edema. Patients may experience headache, tremors, secondary infections such as acne, GI upset, diarrhea, and hypertension.
suppressant – n. 抑制剂
suppressor – n.抑制剂
cyclosporine – n. 环孢菌素
abatacept – n. 阿巴西普
Orencia – n. 奥伦西亚
alefacept – n. 阿来西普
Amevive – n. 阿来西普商标名
azathioprine – n. 硫唑嘌呤
Imuran – n. 依木兰
Sandimmune – n. 山地明
Neoral – n. 新体睦
glatiramer – n. 格拉替雷
Copaxone – n. 考帕松
mycophenolate – n. 麦考酚酯
CellCept – n. 骁悉
pimecrolimus – n. 吡美莫司
Elidel – n. 爱宁达
sirolimus – n. 西罗莫司
Rapamune – n. 雷帕鸣
tacrolimus – n. 他克莫司
Prograf – n. 普乐可复
cytochrome – n. 细胞色素
P450 – n. 细胞色素P450
1. A nurse is doing an assessment data while completing an admission for a patient with a history of liver transplant who is receiving cyclosporine (Sandimmune), Prednisone (Orasone), and Azathioprine (Imuran). Which of the following information will give the nurse the most attention?
A. The client has a soft non-tender lump in the shoulder.
B. An increase cholesterol level.
C. Grade 1+ pitting edema in the feet.
D. Swollen and pinkish gums noted.
2. A client with an acute exacerbation of rheumatoid arthritis is admitted to the hospital for treatment. Which drug, used to treat clients with rheumatoid arthritis, has both an anti-inflammatory and immunosuppressive effect?
A. Gold sodium thiomalate (Myochrysine)
B. Azathioprine (Imuran)
C. Prednisone (Deltasone)
D. Naproxen (Naprosyn)
1. A. The client has a soft non-tender lump in the shoulder. Rationale: A client taking immunosuppressive medications are at risk for development of cancer. A soft non-tender lump will indicate that the patient has lymphoma. Options B, C, and D are common side effects of the immunosuppressive medications. 2. C. Prednisone (Deltasone) Rationale: Gold sodium thiomalate is usually used in combination with aspirin and nonsteroidal anti-inflammatory drugs to relieve pain. Gold has an immunosuppressive affect. Azathioprine is used for clients with life-threatening rheumatoid arthritis for its immunosuppressive effects. Prednisone is used to treat persons with acute exacerbations of rheumatoid arthritis. This medication is given for its anti-inflammatory and immunosuppressive effects. Naproxen is a nonsteroidal anti-inflammatory drug. Immunosuppression does not occur.
当前位置：
