Jasinski D R, Preston K L
Drug Alcohol Depend. 1986 Nov;18(3):273-92. doi: 10.1016/0376-8716(86)90059-1.
Tilidine is an opioid analgesic that has been abused predominantly by the oral route. Studies of parenterally administered tilidine in animals did not clearly indicate a dependence potential of the morphine type. In this study we examined the abuse potential of orally and parenterally administered tilidine in humans. Both orally and intramuscularly given tilidine produced miosis and morphine-like subjective effects in non-dependent subjects. Oral tilidine was 1/8-1/10 as potent and intramuscular tilidine was 1/22 as potent as parenteral morphine in producing morphine-like subjective and miotic effects. Intramuscular tilidine suppressed and did not precipitate signs of abstinence in morphine-dependent subjects. However, intramuscularly given tilidine produced toxic effects not seen with morphine. Meperidine, codeine and d-propoxyphene produced morphine-like subjective and miotic effects, but also produced toxic effects at the highest doses tested. The results suggest that tilidine has a potential to be abused, that this potential is less than that of parenteral morphine and that tilidine is more likely to be abused orally than by the intramuscular route.
替利定是一种阿片类镇痛药,主要通过口服途径被滥用。对动物进行的替利定注射给药研究并未明确显示出吗啡类的成瘾潜力。在本研究中,我们考察了替利定口服和注射给药在人体中的滥用潜力。口服和肌肉注射替利定都能使非成瘾受试者产生瞳孔缩小及类似吗啡的主观效应。在产生类似吗啡的主观和缩瞳效应方面,口服替利定的效力仅为注射吗啡的1/8至1/10,肌肉注射替利定的效力仅为注射吗啡的1/22。肌肉注射替利定可抑制吗啡成瘾受试者的戒断症状,而不会引发戒断体征。然而,肌肉注射替利定会产生吗啡未出现的毒性作用。哌替啶、可待因和右丙氧芬能产生类似吗啡的主观和缩瞳效应,但在测试的最高剂量下也会产生毒性作用。结果表明,替利定有被滥用的潜力,但其潜力小于注射吗啡,且替利定经口服途径比肌肉注射途径更易被滥用。