Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2012 Publisher: Antigen International Limited Roscrea Co. Tipperary Ireland
Pharmacotherapeutic Group (ATC code): N01B B51
Bupivacaine Hydrochloride is a long acting local anaesthetic of the amide type. It prevents the generation and conduction of the nerve impulse by decreasing the permeability of the nerve cell membrane to sodium ions. As well as blocking conduction in nerve axons in the peripheral nervous system, local anaesthetics interfere with the function of all organs in which conduction or transmission of impulses occur.
At high doses it produces surgical anaesthesia, while at lower doses it produces sensory block (analgesia) with less pronounced motor block.
Following absorption, bupivacaine may cause stimulation of the CNS followed by depression and in the cardiovascular system it acts primarily on the myocardium where it may decrease electrical excitability, conduction rate, force of contraction and eventually cardiac arrest.
Like other local anaesthetics, the rate of systemic absorption of bupivacaine is dependent upon the total dose and concentration administered, the route of administration and the vascularity of the tissue locally. Bupivacaine is about 95% bound to plasma proteins, mainly to alpha-1-acid glycoprotein at low concentrations and to albumin at high concentrations.
In adults, the terminal half-life of Bupivacaine is 2.7 hours. The maximum blood concentration varies with the site of injection. Foetal concentrations are lower than maternal concentrations because only the free, unbound drug is available for placental transfer.
Local anaesthetics are distributed to some extent to all body tissues, with higher concentrations found in highly perfused organs such as liver, heart and brain. Bupivacaine is metabolised in the liver and is excreted in the urine mainly as metabolites, with only 5 to 6% as unchanged drug.
No further relevant information other than that which is included in other parts of the Summary of Product Characteristics.
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