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THE HUMAN PHARMACOLOGY AND ABUSE POTENTIAL OF N-ALLYLNOROXYMORPHONE (NALOXONE)
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1967
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The study examined whether naloxone elicits behavioral effects, induces physical dependence, or substitutes for morphine in morphine‑dependent individuals. In a cross‑over study, naloxone showed minimal activity compared to placebo, while other antagonists produced pupil constriction and psychotomimetic effects; naloxone also antagonized morphine when given 1–4 h before a test dose. Naloxone was seven times more potent than nalorphine at precipitating abstinence, did not produce behavioral or physiological changes during chronic administration, and lacks abuse potential, distinguishing it from other narcotic antagonists.
The narcotic antagonist naloxone was studied in man to determine if it produced behavioral effects and physical dependence and if it substituted for morphine in morphine-dependent subjects. When compared to placebo in 12 subjects in a cross-over design, no or little activity was demonstrated for naloxone while, in contrast, the narcotic antagonists, nalorphine and levallorphan, constricted pupils, produced responses on the subject9s and observer9s single-dose opiate questionnaires and produced psychotomimetic and sedative-like responses in a drug effect questionnaire. In 10 subjects, naloxone administered 1, 2 and 4 hr before a test dose of morphine antagonized the effects of morphine. In morphine-dependent subjects, naloxone was 7 times as potent as nalorphine in precipiting abstinence. In three subjects, no behavioral or physiologic changes were observed during chronic administration and withdrawal of naloxone; however, the ability of naioxone to antagonize the effects of a test dose of morphine persisted. It is concluded that naloxone does not have abuse potential of the morphine type since it does not produce subjective effects or physical dependence and precipitates abstinence in morphine-dependent subjects. Further, naloxone is distinguished from the narcotic antagonists, nalorphine, levallorphan and cyclazocine, in that it does not constrict pupils or produce subjective effects, physical dependence or tolerance.