Comparative Clinical Pharmacology of Local Anesthetic Agents

Comparison of the chronotropic responses to local anesthetics (procaine, lidocaine, prilocaine, mepivacaine and bupivacaine) of the canine sinus node in situ.

“…The results in the current study showed that selective administration of the 5 local anesthetics into the sinus node artery of the dog heart caused a dose-dependent decrease in heart rate which was associated with pacemaker shift at higher doses. The relative potencies which caused the negative chronotropic responses were approximately proportional to the anesthetic potencies of the agents (10)(11)(12). The negative response to procaine was not affected by treatment of the sinus node with atropine which completely blocked the effect of acetyl choline to induce a sinus bradycardia or a sinus arrest.…”

Liposome bupivacaine in peripheral nerve blocks and epidural injections to manage postoperative pain

“…Today, local or regional administration of anesthetics is integral to prevention of perioperative pain [3][4][5][6][7][8]. Ropivacaine, chloroprocaine, lidocaine, mepivacaine and bupivacaine are administered perioperatively via infiltration, peripheral or epidural (i.e., neuraxial) nerve block [9,10]. Of these, bupivacaine is one of the most widely studied and extensively used [3,10].…”

“…Ropivacaine, chloroprocaine, lidocaine, mepivacaine and bupivacaine are administered perioperatively via infiltration, peripheral or epidural (i.e., neuraxial) nerve block [9,10]. Of these, bupivacaine is one of the most widely studied and extensively used [3,10]. Favorable attributes of bupivacaine include high lipid solubility (which increases potency) and extensive protein-binding (which increases duration of action) [9,10].…”

“…Of these, bupivacaine is one of the most widely studied and extensively used [3,10]. Favorable attributes of bupivacaine include high lipid solubility (which increases potency) and extensive protein-binding (which increases duration of action) [9,10]. Unfortunately, even bupivacaine --one of the longest-acting local anesthetics available --provides a duration of action (typically < 24 h) insufficient to provide adequate postoperative analgesia following a single-dose administration.…”

“…Relatively poor or variable results have been reported for strategies such as adding dextran, carbonating the anesthetic or combining faster-acting with longer-acting anesthetics (e.g., chloroprocaine with bupivacaine). Currently, the most commonly used technique is the addition of additives such as epinephrine [10] and clonidine [13]. However, at present, there is no approved strategy to reliably extend the duration of action associated with single-injection peripheral or epidural nerve block to > 24 h. Therefore, the current gold standard for extending the duration of postsurgical analgesia with local anesthetics involves use of continuous peripheral or epidural nerve blocks in which a catheter is inserted percutaneously, adjacent to a target nerve or in the epidural space, and local anesthetic is subsequently infused for multiple days [14,15].…”