An interleukin-receptor antagonist works to block the activity of the interleukins that are released in an inflammatory or immune response. The only available interleukin receptor antagonist is anakinra (Kineret). See Table 17.2 for additional information about this drug.
Therapeutic Actions and Indications 治疗作用和适应症
Anakinra specifically antagonizes human interleukin-1 receptors, blocking the activity of interleukin-1. Interleukin-1 levels are elevated in response to inflammation or immune reactions and are thought to be responsible for the degradation of cartilage that occurs in rheumatoid arthritis. Anakinra is used to reduce the signs and symptoms of moderately to severely active rheumatoid arthritis in patients 18 years of age and older who have not responded to the traditional antirheumatic drugs.
Pharmacokinetics 药代动力学
The recommended dosage is 100 mg/d by subcutaneous injection. Anakinra is administered by subcutaneous injection and is absorbed slowly, reaching peak effects in 3 to 7 hours. It is metabolized in the tissues with a 4- to 6-hour half-life and is excreted in the urine.
Contraindications and Cautions 禁忌症与注意事项
Anakinra is contraindicated with any known allergy to E. coli–produced products or to anakinra itself. It should be used with caution during pregnancy and lactation because the drug may cross the placenta and enter breast milk. It also is used cautiously in patients with renal impairment, immunosuppression, or any active infection because these could be exacerbated by the effects of the drug. There is an increased risk of infection whenever this drug is used, and the patient needs to be protected from exposure to infections and monitored closely after any invasive procedures. Immunizations cannot be given while the patient is on this drug.
Adverse Effects 不良效应
Headache, sinusitis, nausea, diarrhea, upper respiratory and other infections, and injection-site reactions are among the most common adverse effects.
头痛、鼻窦炎、恶心、腹泻、上呼吸道和其他感染；注射部位反应是最常见的不良效应。
Clinically Important Drug–Drug Interactions 临床重要的药药相互作用
Patients who are also receiving etanercept (Enbrel) must be monitored very closely because severe and even life-threatening infections have occurred. Anakinra should not be combined with abatacept because of the potential for serious infections.
anakinra – n. 阿那白滞素
Kineret – n. 阿那白滞素商品名
antagonize – v. 对抗，反对
degradation – n. 分解，降解，衰变
cartilage – n. 软骨
sinusitis – n. 鼻窦炎
etanercept – n. 依那西普
Enbrel – n. 恩利
Proleukin – n. 普留净
gold sodium thiomalate – 硫代苹果酸金钠
Myochrysine – n. 硫代苹果酸金钠注射液
prednisone – n. 泼尼松
Deltasone – n. 去氢可的松
naproxen – n. 萘普生
Naprosyn – n. 萘普生商标名
1. A patient who is receiving interleukin-2 (IL-2) therapy (Proleukin) complains to the nurse about all of these symptoms. Which one is most important to report to the health care provider?
A. Generalized aches
B. Dyspnea
C. Decreased appetite
D. Insomnia
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. B. Dyspnea Rationale: Dyspnea may indicate capillary leak syndrome and pulmonary edema, which requires rapid treatment. The other symptoms are common with IL-2 therapy, and the nurse should teach the patient that these are common adverse effects that will resolve at the end of the therapy. 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.
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