Indication: For the production of local or regional anesthesia or analgesia for surgery.
Pharmacology: Bupivacaine, a local amino amide-type anesthetic agent, is indicated for the production of local or regional anesthesia or analgesia for surgery, for oral surgery procedures, for diagnostic and therapeutic procedures, and for obstetrical procedures. Bupivacaine blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination and conduction velocity of affected nerve fibers.
Mechanism Of Action: Local anesthetics produce anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. Bupivicaine reversibly binds to and inactivates sodium channels (Voltage-gated sodium channel alpha subunit Nav1.8). Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. When a nerve loses depolarization and capacity to propagate an impulse, the individual loses sensation in the area supplied by the nerve. The analgesic effects of Bupivicaine are thought to be due to its binding to the prostaglandin E2 receptors, subtype EP1 (PGE2EP1), which inhibits the production of prostaglandins, thereby reducing fever, inflammation, and hyperalgesia
Drug Category: Anesthetics; Local Anesthetics; ATC:N01BB01; ATC:N01BB10
Interactions:
DrugBank: Interactions for Bupivacaine
Interactions for Bupivacaine:
The administration of local anesthetic solutions containing epinephrine or norepinephrine to patients receiving
monoamine oxidase inhibitors or tricyclic antidepressants may produce severe, prolonged hypertension. Concurrent use
of these agents should generally be avoided. In situations in which concurrent therapy is necessary, careful patient
monitoring is essential.
Concurrent administration of vasopressor drugs and of ergot-type oxytocic drugs may cause severe, persistent
hypertension or cerebrovascular accidents.
Phenothiazines and butyrophenones may reduce or reverse the pressor effect of epinephrine.
Chemical IUPAC Name: 1-butyl-N-(2,6-dimethylphenyl)-piperidine-2-carboxamide
