MorphiDex pharmacokinetic studies and single-dose analgesic efficacy studies in patients with postoperative pain.
MorphiDex (MS:DM), a 1:1 (weight:weight) ratio of morphine sulfate (MS) to dextromethorphan hydrobromide (DM), is under clinical development for the treatment of moderate to severe pain. The enhancement of MS analgesia by DM is due to a pharmacodynamic interaction, not an effect on MS blood levels or a pharmacokinetic interaction between MS and DM, or their metabolites. Peak blood levels were achieved at approximately 1 hour, similar to MS in solution, resulting in a rapid onset of effect. As the dose was increased, dose-proportionality was linear. Food reduced the peak concentration in blood (Cmax) but not the extent of the absorption. Single-dose, double-blind, placebo-controlled studies in patients suffering from moderate to severe postoperative pain after third-molar oral surgery or orthopedic surgery demonstrated a significantly greater analgesic effect for MS:DM over MS alone with an 8-hour duration of effect. MS:DM is an effective treatment of moderate to severe pain.
Caruso
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Algos Pharmaceutical Corporation, Neptune, New Jersey 07753, USA.
D000700:Analgesics / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D003915:Dextromethorphan / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D004334:Drug Administration Schedule; D004338:Drug Combinations; D018691:Excitatory Amino Acid Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D006801:Humans; D009020:Morphine / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D010149:Postoperative Pain / Q000188:drug therapy* / Q000378:metabolism*; D016032:Randomized Controlled Trials as Topic
D000700:Analgesics; D000701:Analgesics, Opioid; D004338:Drug Combinations; D018691:Excitatory Amino Acid Antagonists; D003915:Dextromethorphan; D009020:Morphine