Fendrich Z
Katedra farmakologie a toxikologie FaF UK, Hradec Králové.
Cas Lek Cesk. 2000 Jul 19;139(14):440-4.
Metamizol is an effective, non-opioid analgesics which was originally introduced to the therapy in the year 1922. However, with the reference to the side effects of other related pyrazolone derivatives its administration, similarly as the usage of other pyrazolones, was significantly limited. Later, metamizol has been used, usually mixed, with spasmolytic agents and quite recently it has been introduced as a mono-component medicament. Metamizol proved to be a very effective analgesic. When administered in equipotent doses, it had its effects comparable to various opioid analgesics, such as tramadol, pentazocine and pethidine. Beside the strong analgesic effect, it produces also significant antipyretic and splasmolytic effects without the adverse, unpleasant anticholinergic impact. Its spasmolytic effect on the smooth muscle of the sphincter Oddi, urinary tract, and the gal bladder is comparable to the effects of buthylscopolamine. Unlike aspirin and other nonsteroidal antiinflammatory drugs it has, however, no antiinflammatory activity when administered in clinical doses. Similarly, metamizol has no effect on the CNS, cardiovascular system, renal and metabolic functions. On the other hand, metamizol, like aspirin, has got a significant effect on the aggregation of platelets. Metamizol is basically a prodrug. The parent substance is not effective before its conversion into two active metabolites (4-methylaninoantipyrine and 4-aminoantipyrine) in the body. Metamizol is well absorbed from the small intestine but only two above mentioned active metabolites and no parent drug can be detected in the blood. The active metabolites are consequently metabolised to ineffective metabolites including the relevant acetylderivatives, in which the acetylation phenotypes can be distinguished. In the therapy, metamizol can be used, as an analgesic, at post-surgical pain, patient's controlled analgesia (PCA), at the cancer's pain and in the pains of different origin (post-traumatic pain, the pain at myocardial infarction, craniocerebral trauma, and the invasive diagnostic interventions), as well as at he pain of neuromuscular origin, headache and migraine. Its spasmolytic effect in connection with a strong analgesic activity is very useful at various colic attacks. Further, metamizol is a useful antipyretic both in the adults and children. Its adverse effects are not pronounced and drug interactions are minimal. Only when metamizol is administered together with cyclosporine, the blood levels of the last substance should be regularly checked.
安乃近是一种有效的非阿片类镇痛药，于1922年首次用于治疗。然而，鉴于其他相关吡唑啉酮衍生物的副作用，其给药方式与其他吡唑啉酮的使用一样，受到显著限制。后来，安乃近通常与解痉药混合使用，最近它已作为一种单组分药物推出。事实证明安乃近是一种非常有效的镇痛药。当以等效剂量给药时，其效果与各种阿片类镇痛药相当，如曲马多、喷他佐辛和哌替啶。除了强大的镇痛作用外，它还具有显著的解热和解痉作用，且没有不良的、令人不适的抗胆碱能影响。它对Oddi括约肌、泌尿道和胆囊平滑肌的解痉作用与丁基东莨菪碱的作用相当。然而，与阿司匹林和其他非甾体抗炎药不同，临床剂量给药时它没有抗炎活性。同样，安乃近对中枢神经系统、心血管系统、肾脏和代谢功能也没有影响。另一方面，安乃近与阿司匹林一样，对血小板聚集有显著影响。安乃近基本上是一种前体药物。母体物质在体内转化为两种活性代谢物（4-甲基氨基安替比林和4-氨基安替比林）之前没有效果。安乃近从小肠吸收良好，但血液中只能检测到上述两种活性代谢物，而没有母体药物。活性代谢物随后被代谢为无效代谢物，包括相关的乙酰衍生物，其中可以区分乙酰化表型。在治疗中，安乃近可用作镇痛药，用于术后疼痛、患者自控镇痛（PCA）、癌症疼痛以及不同来源的疼痛（创伤后疼痛、心肌梗死疼痛、颅脑创伤和侵入性诊断干预引起的疼痛），以及神经肌肉源性疼痛、头痛和偏头痛。其解痉作用与强大的镇痛活性相结合，在各种绞痛发作时非常有用。此外，安乃近对成人和儿童都是一种有用的解热药。其副作用不明显，药物相互作用最小。只有当安乃近与环孢素一起给药时，才应定期检查环孢素的血药浓度。
