Malec D
Department of Pharmacodynamics, Medical Academy, Lublin, Poland.
Pol J Pharmacol Pharm. 1987 May-Jun;39(3):229-35.
The influence of some antagonists of histamine receptors on morphine-, fentanyl-, and pentazocine-induced analgesia was studied in rats and mice. H1-receptor antagonists (benzhydramine mepyramine) potentiated analgesic action of morphine and fentanyl. Given alone in high doses they also induced a naloxone non-reversible analgesia. Analgesic effects of pentazocine were not changed by benzhydramine and mepyramine. H2-receptor antagonist-cimetidine enhanced also analgesia induced by morphine and fentanyl in rats, but it either increased (after icv injection of 50 micrograms) or decreased (after icv injection of 100 micrograms) the action of pentazocine. Thus, H1 and H2 antagonists potentiate the antinociceptive effects of morphine and fentanyl but the action of pentazocine is not changed by H1 antagonists and is affected in an inconsistent manner by a H2 antagonist cimetidine. It seems that the potentiating effect of H-antagonists is related to the opioid mu receptors.
研究了某些组胺受体拮抗剂对大鼠和小鼠吗啡、芬太尼及喷他佐辛所致镇痛作用的影响。H1受体拮抗剂(苯海拉明、美吡拉敏)增强了吗啡和芬太尼的镇痛作用。高剂量单独给予时,它们也诱导出纳洛酮不可逆性镇痛。苯海拉明和美吡拉敏未改变喷他佐辛的镇痛效果。H2受体拮抗剂西咪替丁也增强了大鼠吗啡和芬太尼诱导的镇痛作用,但它对喷他佐辛的作用要么增强(脑室内注射50微克后),要么减弱(脑室内注射100微克后)。因此,H1和H2拮抗剂增强了吗啡和芬太尼的抗伤害感受作用,但H1拮抗剂未改变喷他佐辛的作用,H2拮抗剂西咪替丁对其作用的影响不一致。H拮抗剂的增强作用似乎与阿片μ受体有关。