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
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.
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
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.