Kuchay Mohammad Shafi, Mithal Ambrish
Division of Endocrinology and Diabetes, Medanta - The Medicity, Gurgaon, Haryana, India.
Indian J Endocrinol Metab. 2017 Mar-Apr;21(2):355-358. doi: 10.4103/ijem.IJEM_555_16.
Levosulpiride is the levorotatory enantiomer of sulpiride used in dyspeptic syndromes of various etiologies. The prokinetic effect of levosulpiride is mediated through the blockade of enteric inhibitory dopaminergic type 2 (D2) receptors. The antagonism of central D2 receptors leads to both therapeutic (e.g. antiemetic effect due to D2 receptor blockade in the chemoreceptor trigger zone) and adverse (including hyperprolactinemia) effects. Dopamine is the main endogenous inhibitor of prolactin synthesis and secretion in the anterior pituitary. Levosulpiride causes significant elevation of serum prolactin levels in significant number of patients. The resultant hyperprolactinemia often manifests as distressing menstrual abnormalities and galactorrhoea in females. A significant number of patients who use levosulpiride develop serum prolactin levels of > 200 ng/mL that goes against the classical textbook teaching where pituitary tumor is supposed to be the mostly likely cause. Careful drug history in patients presenting with high serum prolactin levels will be of great help in reaching the exact diagnosis and avoiding unnecessary brain imaging.
左舒必利是用于治疗各种病因引起的消化不良综合征的舒必利的左旋对映体。左舒必利的促动力作用是通过阻断肠道抑制性多巴胺能2型(D2)受体介导的。中枢D2受体的拮抗作用会导致治疗作用(例如由于化学感受器触发区的D2受体阻断而产生的止吐作用)和不良反应(包括高泌乳素血症)。多巴胺是垂体前叶催乳素合成和分泌的主要内源性抑制剂。左舒必利会使相当数量的患者血清催乳素水平显著升高。由此产生的高泌乳素血症在女性中常表现为令人苦恼的月经异常和溢乳。大量使用左舒必利的患者血清催乳素水平会超过200 ng/mL,这与传统教科书所讲的垂体瘤被认为是最可能的病因相悖。对于血清催乳素水平高的患者,详细的用药史对于准确诊断和避免不必要的脑部影像学检查有很大帮助。