Vogelzang Jolanda M J, Luinstra Marianne, Rutgers A Wijnand F
Department of Clinical Pharmacy and Toxicology, Martini Hospital, Groningen, The Netherlands.
Department of Neurology and Clinical Neurophysiology, Martini Hospital, Groningen, The Netherlands.
Case Rep Neurol. 2015 Oct 21;7(3):209-12. doi: 10.1159/000441489. eCollection 2015 Sep-Dec.
The aim of this report is to discuss whether or not rectal levodopa administration is useful in some situations.
In situations where oral intake of levodopa formulations is not possible, the treatment options of Parkinson's disease patients are limited. The literature describes no or low rectal absorption of levodopa.
A patient with an ileus was unable to take oral medication. After consulting the neurologist and pharmacist, the surgeon decided to describe a rectal formulation of levodopa/carbidopa (100/25 mg) once daily. On day 3 of the therapy, 1 h after administration of the rectal formulation of levodopa/carbidopa, a blood sample was drawn. The patient was unable to take his other Parkinson medication; therefore the dose of the rectal levodopa/carbidopa was increased to 5 times a day.
Full control of the symptoms was not achieved, but alleviation of the most severe tremor and rigidity was seen, which was confirmed by the neurologist, nurses and patient. The levodopa concentration detected was 17 nmol/l. Compared to levodopa concentrations described in the literature (1,400-12,000 nmol/l), the concentration is very low. There are some possible explanations for the low concentration detected. The presence of a specific amino acid transport system in the rectum is not known, which could lead to no or reduced absorption. The poor rectal absorption of carbidopa leads to a higher conversion of levodopa to dopamine peripherally.
In situations where patients are unable to take oral medication, rectal administration of levodopa/carbidopa is worth considering.
本报告旨在探讨直肠给予左旋多巴在某些情况下是否有用。
在无法口服左旋多巴制剂的情况下，帕金森病患者的治疗选择有限。文献表明左旋多巴经直肠吸收不良或吸收程度低。
一名肠梗阻患者无法口服药物。在咨询神经科医生和药剂师后，外科医生决定每天给予一次直肠用左旋多巴/卡比多巴制剂（100/25毫克）。在治疗的第3天，给予直肠用左旋多巴/卡比多巴制剂1小时后采集血样。该患者无法服用其他帕金森病药物；因此，直肠用左旋多巴/卡比多巴的剂量增加至每日5次。
症状未完全得到控制，但最严重的震颤和强直有所缓解，神经科医生、护士及患者均予以证实。检测到的左旋多巴浓度为17纳摩尔/升。与文献中描述的左旋多巴浓度（1400 - 12000纳摩尔/升）相比，该浓度非常低。对于检测到的低浓度有一些可能的解释。直肠中是否存在特定的氨基酸转运系统尚不清楚，这可能导致吸收不良或吸收减少。卡比多巴经直肠吸收不良导致左旋多巴在外周更多地转化为多巴胺。
在患者无法口服药物的情况下，直肠给予左旋多巴/卡比多巴值得考虑。
