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    《ISPN学习》总第506期
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    《ISPN学习》总第667期
    日期:2020-08-12 14:11:00    
     
    《ISPN学习》2020年08月12日总第667期
     
     
    ISPN/RN Review
     
    Prototype Summary 原型药小结

    1. Baclofen 巴氯芬

    Indications: Alleviation of signs and symptoms of spasticity, may be of use in spinal cord injuries or spinal cord diseases.

    适应症:缓解痉挛状态症状体征;对脊髓损伤或脊髓病可能有用

    Actions: Gamma-aminobutyric acid analogue, exact mechanism of action is not understood, inhibits monosynaptic and polysynaptic spinal reflexes, CNS depressant.

    作用:γ-氨基丁酸类似物,确切作用机制未知;抑制单突触和多突触脊髓反射;充当CNS抑制剂

    Pharmacokinetics: 药代动力学

    Route             Onset            Peak      Duration
    Oral                1 h                 2 h          4 – 8 h
    Intrathecal     30 – 60 min    4 h           4 – 8 h

    T1/2: 3 to 4 hours; not metabolized, excreted in the urine.
    半衰期:3 – 4小时;不代谢,经尿排出

    Adverse Effects: Transient drowsiness, dizziness, weakness, fatigue, constipation, headache, insomnia, hypotension, nausea, urinary frequency.

    不良效应:暂时性瞌睡、头晕、无力、疲劳、便秘、头痛、失眠、低血压、恶心、尿频

    2. Dantrolene 丹曲林

    Indications: Control of clinical spasticity resulting from upper motor neuron disorders, preoperatively to prevent or attenuate the development of malignant hyperthermia in susceptible patients, IV for management of fulminant malignant hyperthermia.

    适应症:控制上运动神经元障碍引起的临床痉挛状态,术前防止或降低易感患者恶性体温过高机会,IV管理暴发性恶性体温过高

    Actions: Interferes with the release of calcium from the sarcoplasmic reticulum within skeletal muscles, preventing muscle contraction; does not interfere with neuromuscular transmission.

    作用:干扰骨骼肌肌质网的钙释放,防止肌收缩;不影响神经肌肉传递

    Pharmacokinetics: 药代动力学

    Route         Onset         Peak         Duration
    Oral            Slow            4 – 6 h      8 – 10 h
    IV                Rapid          5 h             6 – 8 h

    T1/2: 9 hours (oral), 4 to 8 hours (IV); excreted in the urine.
    半衰期:9小时(口服);4-8小时(IV)。经尿排出

    Adverse Effects: Drowsiness, dizziness, weakness, fatigue, diarrhea, hepatitis, myalgia, tachycardia, transient blood pressure changes, rash, urinary frequency.

    不良效应:瞌睡、头晕、无力、疲劳、腹泻、肝炎、肌痛、心动过速、一过性血压变化、皮疹、尿频。

     
    Vocabulary 
     
    prototype – n. 原型(药)
    Baclofen – n. 巴氯芬
    alleviation – n. 缓解,减轻
    Gamma-aminobutyric acid – γ-氨基丁酸
    analogue – n. 类似物,同型物
    aminobutyric – a. 氨基丁酸的
    monosynaptic – a. 单突触的
    polysynaptic – a. 多突触的
    spinal reflex -- 脊髓反射
    transient – a. 暂时的,瞬时的
    Dantrolene – n. 丹曲林
    attenuate – v. 使变薄,解毒,减弱
    malignant hyperthermia – 恶性体温过高
    fulminant – a. 暴发的
    sarcoplasmic reticulum –骨骼肌肌质网
    sarcoplasmic – a. 肌质的,肌浆的
    myalgia – n. 肌痛

     
     
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      Video
     
    Muscle Relaxants
     
    Test
     
    1. What is the centrally acting muscle relaxant of choice for children with tetanus?
    A. Botulinum toxin type B
    B. Dantrium
    C. Baclofen
    D. Methocarbamol
    2. A patient with severe spasticity sees his physician. The physician orders dantrolene. In what circumstances is the drug dantrolene contraindicated?
    A. Spasticity that contributes to upright position
    B. Spasticity that involves both legs
    C. Spasticity that involves the arm and the leg on the same side
    D. Spasticity that contributes to mobility

     
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    答案 Answers
     
    1. D. Methocarbamol
    Rationale: Both botulinum toxin type B and Dantrium are direct-acting skeletal muscle relaxants. Baclofen is indicated for relief of spasticity in children with cerebral palsy.
    2. A. Spasticity that contributes to upright position
    Rationale: Dantrolene is contraindicated in the presence of any known allergy to the drug. It is also contraindicated in the following conditions: spasticity that contributes to locomotion, upright position, or increased function, which would be lost if that spasticity was blocked; active hepatic disease, which might interfere with metabolism of the drug and because of known liver toxicity; and lactation because the drug may cross into breast milk and cause adverse effects in the infant. The other options would not contraindicate the medication.

     
     

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