Mello N K, Mendelson J H, Drieze J, Kelly M
Alcohol and Drug Abuse Research Center, Harvard Medical School, McLean Hospital, Belmont, Massachusetts.
J Pharmacol Exp Ther. 1990 Sep;254(3):815-23.
The acute effects of i.v. cocaine on basal levels of prolactin (PRL), luteinizing hormone (LH) and follicle-stimulating hormone were examined in nine female rhesus monkeys during the early follicular phase of the menstrual cycle (days 4-7). Integrated plasma samples were collected at 10-min intervals for 40 min before and 110 min after administration of cocaine (0.4 and 0.8 mg/kg i.v.). Cocaine plasma levels averaged 105 +/- 19 and 157 +/- 23 ng/ml after low- and high-dose administration. PRL decreased significantly (P less than .01) after cocaine administration and reached a nadir within 60 to 70 min. Inasmuch as cocaine blocks dopamine reuptake, PRL suppression is consistent with dopaminergic inhibitory control of PRL release from the pituitary. However, cocaine's effects on PRL were biphasic in 10 of 18 studies. PRL increased within 90 to 110 min post-cocaine and sometimes exceeded base-line levels by over 100%. The duration of PRL suppression (80 min) and the time of onset of the subsequent rebound PRL increase corresponds to the estimated half-life of i.v. cocaine in monkey plasma. PRL suppression followed by a rebound elevation also is consistent with clinical reports of hyperprolactinemia in chronic cocaine abusers. LH increased significantly (P less than .01) within 20 min after cocaine administration and remained above base-line for 40 to 50 min. Follicle-stimulating hormone did not change significantly after cocaine administration. Cocaine's stimulation of LH is consistent with cocaine's alleged enhancement of sexual arousal.(ABSTRACT TRUNCATED AT 250 WORDS)
在月经周期卵泡期早期(第4 - 7天),对9只雌性恒河猴静脉注射可卡因,检测其对催乳素(PRL)、促黄体生成素(LH)和促卵泡激素基础水平的急性影响。在静脉注射可卡因(0.4和0.8mg/kg)前40分钟和给药后110分钟,每隔10分钟采集一次血浆样本。低剂量和高剂量给药后,可卡因血浆水平平均分别为105±19和157±23ng/ml。注射可卡因后PRL显著降低(P<0.01),并在60至70分钟内降至最低点。由于可卡因可阻断多巴胺再摄取,PRL的抑制与垂体释放PRL的多巴胺能抑制控制一致。然而,在18项研究中的10项中,可卡因对PRL的影响呈双相性。注射可卡因后90至110分钟内PRL升高,有时超过基线水平100%以上。PRL抑制的持续时间(80分钟)和随后PRL反弹升高的起始时间与静脉注射可卡因在猴血浆中的估计半衰期相对应。PRL先抑制后反弹升高也与慢性可卡因滥用者高催乳素血症的临床报告一致。注射可卡因后20分钟内LH显著升高(P<0.01),并在40至50分钟内保持高于基线水平。注射可卡因后促卵泡激素无显著变化。可卡因对LH的刺激与可卡因据称增强性唤起作用一致。(摘要截短至250字)