Drug intelligence / Profile preview

mepivacaine + tramadol

Development stage
Phase 4
Modality
Small Molecules
Administration
Perineural
01

Overview

Mepivacaine + tramadol is a combination of two active ingredients used in anesthesia and pain management. This combination has been studied for its efficacy in dental procedures, particularly for inferior alveolar nerve blocks in cases of symptomatic irreversible pulpitis, and in axillary brachial plexus anesthesia. Mepivacaine is a local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine. It works by blocking nerve signals in the body. Tramadol is a centrally-acting opioid agonist and serotonin/norepinephrine reuptake inhibitor (SNRI). It exists as a racemic mixture with two pharmacologically active enantiomers that contribute to its analgesic properties through different mechanisms: (+)-tramadol and its metabolite (+)-O-desmethyl-tramadol act as μ opioid receptor agonists, while (+)-tramadol inhibits serotonin reuptake and (-)-tramadol inhibits norepinephrine reuptake. When combined, tramadol appears to enhance the duration and quality of anesthesia provided by mepivacaine, potentially offering improved postoperative analgesia with acceptable side effects.

02

Targets

MOR (Mu opioid receptor)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)NaV (Voltage-gated sodium channels)

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