Bupivacaine is only found in individuals that have used or taken this drug. It is a widely used local anesthetic agent. [PubChem]Bupivacaine blocks the generation and the conduction of nerve impulses, pravdepodobne zvýšením prahu pre elektrickú excitáciu v nerve, spomalením šírenia nervového vzruchu, a znížením rýchlosti nárastu akčného potenciálu. Bupivacaine binds to the intracellular portion of sodium channels and blocks sodium influx into nerve cells, which prevents depolarization. Vo všeobecnosti, progresia anestézie súvisí s priemerom, myelinizácia a rýchlosť vedenia postihnutých nervových vlákien. Klinicky, poradie straty nervovej funkcie je nasledovné: bolesť, teplota, dotyk, propriocepcia, a tonusom kostrového svalstva. The analgesic effects of Bupivicaine are thought to potentially be due to its binding to the prostaglandin E2 receptors, subtype EP1 (PGE2EP1), which inhibits the production of prostaglandins, thereby reducing fever, zápal, and hyperalgesia.
Bupivacaine is indicated for local infiltration, blokáda periférnych nervov, sympathetic nerve block, and epidural and caudal blocks. It is sometimes used in combination with epinephrine to prevent systemic absorption and extend the duration of action. The 0.75% (most concentrated) formulation is used in retrobulbar block. It is the most commonly used local anesthetic in epidural anesthesia during labor, as well as in postoperative pain management.Liposomal formulations of buipivacaine are no more effective than plain solutions of bupivacaine.
Bupivacaine is contraindicated in patients with known hypersensitivity reactions to bupivacaine or amino-amide anesthetics. It is also contraindicated in obstetrical paracervical blocks and intravenous regional anaesthesia (Bier block) because of potential risk of tourniquet failure and systemic absorption of the drug and subsequent cardiac arrest. The 0.75% formulation is contraindicated in epidural anesthesia during labor because of the association with refractory cardiac arrest.
