Drug Interactions between ConZip and naloxone

MONITOR: Concomitant use of pure opioid antagonists, such as naloxone and naltrexone may reduce the therapeutic effects and/or precipitate withdrawal symptoms in patients treated with tramadol or tapentadol. The partial analgesic activity of tramadol or tapentadol due to mu-opioid receptor agonist activity can be antagonized by the mu-opioid receptor antagonists naloxone and naltrexone. It should be noted that tramadol and tapentadol have low affinity binding for the mu-opioid receptor compared with other opiates. For example, tapentadol has 18 times less binding affinity than morphine to the mu-opioid receptor. However, these opioid antagonists may still precipitate withdrawal symptoms in patients who are physically dependent on tramadol or tapentadol. Furthermore, the opioid antagonist naloxone has been recommended for clinically significant respiratory or circulatory depression secondary to tramadol or tapentadol overdose. However, the risk of seizures may be increased when naloxone is used to treat a tramadol overdose.

MANAGEMENT: Caution and clinical monitoring are recommended when pure opioid antagonists, such as naloxone and naltrexone are used concomitantly with tramadol or tapentadol. A non-opioid therapeutic alternative or a dosage adjustment for tramadol or tapentadol may be considered if concomitant use of an opioid antagonist is unavoidable. Patients with a suspected tramadol overdose should be closely monitored for seizure activity if an opioid antagonist is used to treat the overdose.

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