​Pharmacology - Bupivacaine

​Pharmacology - Bupivacaine 
Bupivacaine blocks the conduction of action potentials in nerves. At lower concentrations, it blocks pain fibers with smaller diameters.

Action Mechanism The blocking of intracellular voltage-gated Na+ channels occurs in a dose-dependent manner. Transports itself across cell membranes in its uncharged, lipid-soluble state. Weakly basic local anesthetics (LAs) are more effective at ionizing in tissues with inflammation because of the lower pH.

 
The P450 system in the liver converts these amides into glucuronides. These LAs have a longer half-life compared to others. Bupivacaine has a half-life of two to three hours.

Application in Clinical Practice 
In ltration, nerve block, epidural, and spinal anaesthesia. Reserved for situations that call for a more substantial response time.
Maybe mixed with adrenaline to make the effects last longer, or with fentanyl for an epidural injection.

Negative Impacts
Adverse effects are minimal at typical dosages. Cardiotoxic to a greater extent than alternative LAs. (Ropivacaine and levobupivacaine are less harmful to the heart.)