Wiseman L R, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1995 Jan;49(1):143-55. doi: 10.2165/00003495-199549010-00010.
Pilocarpine is a cholinergic agonist which stimulates salivary secretion both in individuals with normal salivary gland function and in those with impaired salivary flow (xerostomia or oral dryness). A rapid increase in salivary flow rate is observed following oral pilocarpine administration and peak levels are maintained for at least 1 to 2 hours. Mean salivary flow rates after administration of pilocarpine are 2- to 10-fold higher than after placebo, and no evidence of tolerance to the pharmacological effects of the drug has been observed during prolonged administration for up to 5 months. The clinical efficacy of oral pilocarpine in relieving symptoms of xerostomia (resulting from radiation therapy to the head and neck region or salivary gland dysfunction), including oral dryness and difficulty in chewing, swallowing and speaking, has been demonstrated in double-blind placebo-controlled clinical trials. In these studies, pilocarpine 5 to 10mg 3 times daily increased salivary flow and improved symptoms of xerostomia in a significantly higher percentage of patients than did placebo (54 versus 25% in one study). Preliminary findings indicate that administration of pilocarpine during radiation therapy may reduce the severity of xerostomia; however, this requires further investigation. The majority of patients receiving oral pilocarpine therapy for xerostomia experience adverse events (most commonly sweating); however, these are generally mild and tolerable in nature. Thus, pilocarpine is an effective agent for the treatment of xerostomia, increasing salivary flow and reducing symptom severity to a significantly greater extent than placebo. Further clinical trials should evaluate the potential beneficial effects of pilocarpine on the incidence of dental caries and oral candidiasis during prolonged therapy, its prophylactic efficacy during radiation therapy and its efficacy relative to that of other salivary stimulants.
毛果芸香碱是一种胆碱能激动剂，它能刺激唾液分泌，无论是唾液腺功能正常的个体还是唾液分泌减少（口干症或口腔干燥）的个体。口服毛果芸香碱后，唾液流速会迅速增加，且峰值水平会维持至少1至2小时。服用毛果芸香碱后的平均唾液流速比服用安慰剂后高2至10倍，在长达5个月的长期给药过程中，未观察到对该药物药理作用产生耐受性的证据。在双盲安慰剂对照临床试验中，已证实口服毛果芸香碱在缓解口干症（由头颈部放疗或唾液腺功能障碍引起）症状方面的临床疗效，这些症状包括口腔干燥以及咀嚼、吞咽和说话困难。在这些研究中，与安慰剂相比，每日3次服用5至10毫克毛果芸香碱能使更多患者的唾液分泌增加并改善口干症状（一项研究中分别为54%和25%）。初步研究结果表明，在放疗期间服用毛果芸香碱可能会减轻口干症的严重程度；然而，这需要进一步研究。大多数接受口服毛果芸香碱治疗口干症的患者会出现不良事件（最常见的是出汗）；不过，这些不良事件通常性质轻微且可耐受。因此，毛果芸香碱是治疗口干症的有效药物，与安慰剂相比，它能显著增加唾液分泌并减轻症状严重程度。进一步的临床试验应评估毛果芸香碱在长期治疗期间对龋齿和口腔念珠菌病发病率的潜在有益作用、其在放疗期间的预防效果以及相对于其他唾液刺激剂的疗效。
