Drug intelligence / Profile preview

2-chloroprocaine + morphine

Development stage
Unknown
Lead developer
Sintetica
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Epidural
01

Overview

The combination of 2-chloroprocaine and morphine is used in epidural anesthesia, particularly following cesarean sections. However, there is a significant interaction between these two drugs that affects their clinical efficacy. 2-Chloroprocaine is an ester local anesthetic agent. When administered epidurally before morphine, it has been shown to diminish the efficacy and duration of epidural morphine analgesia compared to when morphine is administered after other local anesthetics like lidocaine. Even small doses of 2-chloroprocaine administered remotely from the time of morphine injection can interfere with the duration of epidural morphine analgesia. For example, in one study, patients who received 2-chloroprocaine for epidural catheter testing experienced a significantly shorter duration of morphine analgesia (median 16 hours) compared to those who received lidocaine (median 24 hours). ## Mechanism of Interaction The exact mechanism of the interaction between 2-chloroprocaine and morphine is unknown. Several possible explanations have been proposed, including differences in latency/duration of action, chemical interactions, or physiological effects. ## Clinical Implications This interaction is clinically significant as it can substantially reduce the pain relief duration provided by epidural morphine when 2-chloroprocaine is used prior to morphine administration. When planning epidural anesthesia followed by epidural morphine for postoperative pain management, clinicians should consider this interaction. Using alternative local anesthetics such as lidocaine or bupivacaine for epidural catheter testing or anesthesia may be preferable when epidural morphine will be administered for postoperative analgesia. While 2-chloroprocaine reduces the duration of morphine analgesia, it does not appear to alter the incidence of morphine-related side effects.

02

Targets

KOR (Kappa opioid receptor)NaV (Voltage-gated sodium channels)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)

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