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Pharmacotherapeutic group (ATC code): N01B B51.
Pharmacology: Pharmacodynamics: Bupivacaine is a potent amide local anaesthetic with a prolonged duration of action. It affects sensory nerves more than motor nerves and is ideal for producing analgesia without motor blockade.
Pharmacokinetics: In adults, the terminal half-life of bupivacaine is 3.5 hours. The maximum blood concentration varies with the site of injection and is highest after intercostal nerve blockade.
Total dose, rather than concentration, is an important determinant of peak blood levels.
Bupivacaine is biodegraded in the liver and only 6% is excreted unchanged in the urine.
In adults, adrenaline decreases peak plasma concentrations by up to 50% in brachial plexus block and by 5-25% in epidural block.
In children, the pharmacokinetics are similar to that in adults.
Toxicology: Preclinical safety data: Bupivacaine hydrochloride and adrenaline tartrate are well established active ingredients.
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