Pharmacological and endocrinological studies on anabolic agents.

F Neumann
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Abstract

When used in connection with animal production the term "anabolic agents" covers a wide range. Ther steroidal male and female sex hormones are included in this list, as are the nonsteroidal estrogens. For the clinician and for the endocrinologist, anabolics are only steroids chemically related to testosterone and 19-nortestosterone. Estrogens, though possessing anabolic properties, too, do not belong to this class. This paper will deal with anabolic agents in in the stricter sense of which mainly trenbolone acetate combined with hexestrol has been recommended for bull and heifer fattening. To consider possible consumer injury from ingestion of meat from anabolic agent treated animals, it is necessary to know the pharmacological properties of the agents, the doses producing certain effects or might produce, and the levels of residues in the meat. Trenbolone acetate will be compared with the following anabolic agents: methenolone acetate, methandrostenolone, nandrone, androstanazole, and 19-nortestosterone. The activity spectrum of trenbolone acetate is similar to that of 19-nortestosterone or those anabolics that are derived from 19-nortestosterone. The compound has about three times stronger androgenic effect than testosterone propionate. Its index of dissociation between anabolic/androgenic activity is 2--3. This index is 3--10 for the other anabolic agents. As regards the virilizing potency, trenbolone acetate is also on the top of the list. It seems that androgenicity and degree of virilization run paralle. The antigonadotropic activity (inhibition of ovulation and testicular growth) of trenbolone acetate exceeds that of testosterone propionate by the factor 3. The compound is not estrogenic and seemingly not or only weakly progestationally active. In principle, the androgenic activity (symptoms of virilization) as well as the antigonadotropic effect (disturbances of the menstrual cycle in women, inhibition of spermiogenesis in men) of trenbolone acetate might be noted. This risk, however, can be excluded by mere calculation. In rats, 0.1 mg/kg trenbolone acetate have an antigonadotropic effect. This corresponds to a daily dose of 5--7 mg in humans. By the same extrapolation, a daily human dose of 100 mg can be calculated for androgenic activity. Such factors of conversion are, of course, not precise because rats are much less sensitive to androgens and anabolics than humans. Thus, testosterone propionate is active only in daily doses of 10--20 mg. If in humans trenbolone acetate also has three times the activity of testosterone propionate, effects in man had to be counted with not less than a daily intake of 3--5 mg trenbolone acetate. The dose which is recommended for livestock fattening is 300 mg. IT can, therefore, be excluded almost with certainty that the meat would contain such large amounts of hormone residues.

合成代谢剂的药理学和内分泌学研究。
当与动物生产有关时,术语“合成代谢剂”涵盖范围很广。他们的雄性和雌性甾体性激素包括在这个列表中,以及非甾体雌激素。对于临床医生和内分泌学家来说,合成代谢只是与睾酮和去甲睾酮化学相关的类固醇。雌激素虽然也具有合成代谢的特性,但不属于这一类。本文将从严格意义上讨论合成代谢剂,其中主要推荐醋酸trenbolone与己甾醇联合用于公牛和母牛的育肥。为了考虑食用经合成代谢剂处理过的动物的肉可能对消费者造成的伤害,有必要了解这些制剂的药理学性质、产生或可能产生某种效果的剂量以及肉中的残留物水平。将醋酸Trenbolone与以下合成代谢药物进行比较:醋酸美诺酮、美雄甾酮、奈雄酮、雄甾唑和去甲睾酮。醋酸trenbolone的活性谱与19-去甲睾酮或由19-去甲睾酮衍生的合成代谢产物相似。这种化合物的雄激素效应比丙酸睾酮强三倍。其合成代谢/雄激素活性分离指数为2- 3。其他合成代谢剂的指数为3- 10。至于阳刚功效,醋酸trenbolone也名列榜首。似乎雄激素性和男性化程度是并行的。醋酸trenbolone的抗促性腺活性(抑制排卵和睾丸生长)超过丙酸睾酮的因子3。该化合物不是雌激素,似乎没有或只有弱孕活性。原则上,可以注意到醋酸trenbolone的雄激素活性(男性化症状)以及抗促性腺激素作用(女性月经周期紊乱,男性精子生成抑制)。然而,仅仅通过计算就可以排除这种风险。在大鼠中,0.1 mg/kg醋酸trenbolone具有抗促性腺激素作用。这相当于人体每日5- 7毫克的剂量。通过同样的外推法,可以计算出人体每日剂量为100毫克的雄激素活性。当然,这种转化因素并不精确,因为老鼠对雄激素和合成代谢的敏感性远低于人类。因此,丙酸睾酮只有在每日剂量为10- 20mg时才有活性。如果在人体内醋酸trenbolone的活性是丙酸睾酮的三倍,那么在人体内的作用必须以每天摄入不少于3- 5mg醋酸trenbolone来计算。牲畜增肥的推荐剂量是300毫克。因此,几乎可以肯定地排除肉中含有如此大量的激素残留物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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