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Bupivacaine hydrochloride monohydrate is a local anaesthetic medicine belonging to the aminoacyl amide group of local anaesthetics. It is chemically related to lidocaine and mepivacaine.[3] The substance is a white, odourless, crystalline powder that is soluble in water and freely soluble in 95 percent ethanol.[3] It is classified as a local injectable anaesthetic with the ATC code N01BB01.[1] Bupivacaine is already authorised as a medicine; one authorisation record is IE PA 2299/035/001, held by Baxter Holding B.V.[1] Other names for the substance include bupivacaine hydrochloride, bupivacaine HCl, and DL-bupivacaine.[4]
Bupivacaine blocks the generation and conduction of nerve impulses. It increases the threshold for electrical excitation in the nerve, slows the propagation of the nerve impulse, and reduces the rate of rise of the action potential.[3] Clinically, loss of nerve function follows a predictable order: first pain, then temperature, touch, proprioception, and finally skeletal muscle tone.[3] At normal therapeutic doses, effects on cardiac conduction and peripheral vascular resistance are minimal; however, toxic blood concentrations can depress cardiac conduction and excitability, potentially leading to atrioventricular block, ventricular arrhythmias, and cardiac arrest.[3]
Bupivacaine is a widely used local anaesthetic agent.[4] In the two trials covered here, it is being studied for:
Bupivacaine is available as a solution for injection for local infiltration, peripheral nerve block, and caudal and lumbar epidural blocks.[3] In the trials described here, two forms are used: a solution for injection given by intradermal use (into the skin) for scar pain, and a lozenge given by oromucosal use (in the mouth) under the name BupiZenge for oral mucositis.[1][2]
Two Phase 3 clinical trials are registered for bupivacaine hydrochloride monohydrate. Both are interventional studies measuring pain reduction.
The first trial (2024-518954-18-01) tests whether botulinum toxin injection is better than corticosteroid injection for persistent post-surgical scar pain. Bupivacaine 2.5 mg/ml solution for injection is used as an auxiliary medicine in this trial, which plans to enrol 60 participants. The primary outcome is the numerical rating scale of pain (NRS). The trial is currently suspended.[1]
The second trial (2025-524386-24-00) is a randomised, open-label Phase 3 trial comparing BupiZenge with lidocaine for pain associated with oral mucositis in head and neck cancer. BupiZenge is the test medicine in this trial, which plans to enrol 150 participants. The primary outcome is total pain reduction from baseline expressed as area under the curve (AUC) of patient-reported oral cavity pain intensity from pre-dose to 3 hours post-dose, measured by the NRS at the last day of radiotherapy. The trial is currently authorised.[2]
The scar pain trial enrols people with persistent post-surgical scar pain.[1] The oral mucositis trial enrols people with head and neck cancer who have oral mucositis during radiotherapy.[2] Detailed eligibility criteria are available in the registry records for each trial.
At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block, ventricular arrhythmias, and cardiac arrest.[3] Systemic absorption of local anaesthetics produces effects on the cardiovascular and central nervous systems.[3]
Bupivacaine is known to interact with 141 drugs, according to an interaction checker. Of these, 23 are major interactions, 113 are moderate, and 5 are minor. There are also 3 disease interactions, involving cardiovascular disease, liver disease, and renal impairment.[5] Major interactions are those where the risk of the interaction outweighs the benefit and the combination is usually avoided.[5]
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