Kwekkeboom D J, Lamberts S W, Blom J H, Schroeder F H, De Jong F H
Department of Medicine, Erasmus University Rotterdam, The Netherlands.
Clin Endocrinol (Oxf). 1990 Apr;32(4):443-51. doi: 10.1111/j.1365-2265.1990.tb00884.x.
Seven patients with metastatic prostatic cancer were treated with biodegradable implants of the GnRH analogue buserelin and six were treated with buserelin intranasally. After 4-24 weeks of treatment mean serum testosterone concentrations were significantly lower in the patients treated with implants than in those treated intranasally (0.7 vs 1.7 nmol/l respectively; P less than 0.01). Also, serum LH concentrations were significantly lower in the group treated with implants. Serum alpha-subunit concentrations were significantly higher than pretreatment values during buserelin treatment. However, the sum of the concentrations of alpha-subunit present either as free alpha-subunit or as a part of LH did not differ significantly from pre-treatment values after 8 weeks or more of buserelin treatment. During buserelin treatment serum LH concentrations measured by radioimmunoassay (RIA) were higher than those measured by immunoradiometric assay (IRMA). Cross-reactivity of alpha-subunit in the LH RIA accounted for many, but not all, of the observed discrepancies. We conclude that: (1) the principal long-term effect of prolonged buserelin administration on the pituitary gonadotroph is the suppression of LH beta production, while alpha-subunit production is not affected; (2) the serum concentrations of bioactive LH are better reflected by LH concentrations measured by IRMA than by those measured by RIA. (3) Subcutaneous application of biodegradable buserelin implants is more effective in suppressing serum LH and testosterone concentrations than intranasal buserelin application.
7例转移性前列腺癌患者接受了促性腺激素释放激素(GnRH)类似物布舍瑞林的可生物降解植入物治疗,6例患者接受了布舍瑞林鼻内给药治疗。治疗4 - 24周后,接受植入物治疗的患者平均血清睾酮浓度显著低于鼻内给药治疗的患者(分别为0.7与1.7 nmol/L;P<0.01)。此外,接受植入物治疗的组血清促黄体生成素(LH)浓度也显著更低。在布舍瑞林治疗期间,血清α亚基浓度显著高于治疗前值。然而,在布舍瑞林治疗8周或更长时间后,游离α亚基或作为LH一部分存在的α亚基浓度总和与治疗前值相比无显著差异。在布舍瑞林治疗期间,通过放射免疫测定法(RIA)测得的血清LH浓度高于通过免疫放射测定法(IRMA)测得的浓度。LH RIA中α亚基的交叉反应解释了许多但并非所有观察到的差异。我们得出结论:(1)长期给予布舍瑞林对垂体促性腺细胞的主要长期影响是抑制LHβ的产生,而α亚基的产生不受影响;(2)通过IRMA测得的LH浓度比通过RIA测得的浓度能更好地反映生物活性LH的血清浓度。(3)皮下应用可生物降解的布舍瑞林植入物在抑制血清LH和睾酮浓度方面比鼻内应用布舍瑞林更有效。