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Pentamorphone (14β-pentylaminomorphinone) was developed as a potent opiate with a rapid onset and short duration of action, similar to that of fentanyl, which was reported to produce analgesia with limited depression of ventilation [ ]. However, it proved to be ineffective in the treatment of acute pain after major abdominal or orthopedic surgery in a double-blind, randomized, placebo-controlled study of 72 patients who were given 0.08, 0.16, or 0.24 micrograms/kg of pentamorphone intravenously in the recovery room. Only those who received 0.24 micrograms/kg experienced reduced pain intensity and increased sedation, and the effects were transient and the total amounts of supplementary morphine required within the first hour were not different between the treatments [ ].
Subjective symptoms in 23 male volunteers who received pentamorphone were pain on injection, headache, tiredness, euphoria, dizziness, visual disturbances, and nausea [ ].
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