环苯扎林 (Amrix, Fexmid, Flexeril)

概览

Cyclobenzaprine is a skeletal muscle relaxant that works on the brainstem to treat muscle spasms of local origin.

作用机制

The exact mechanism of action of cyclobenzaprine has not been fully elucidated in humans, and much of the information available regarding its mechanism has been ascertained from early animal studies. There is some evidence that cyclobenzaprine exerts its effects at the supraspinal level, specifically within the locus coeruleus of the brainstem, with little-to-no action at neuromuscular junctions or directly on skeletal musculature. Action on the brainstem is thought to result in diminished activity of efferent alpha and gamma motor neurons, likely mediated by inhibition of coeruleus-spinal or reticulospinal pathways, and ultimately depressed spinal cord interneuron activity. More recently it has been suggested that inhibition of descending serotonergic pathways in the spinal cord via action on 5-HT2 receptors may contribute to cyclobenzaprine’s observed effects.

适应症

用于缓解与急性疼痛的肌肉骨骼疾病相关的肌肉痉挛（作为休息和物理治疗的辅助药）。但环苯扎林对脑、脊髓疾病或儿童脑性瘫痪引起的痉挛无效。

• Muscle Spasms