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Pharmacological particulars
Pharmacotherapeutic group: local anaesthetics, amides
ATCvet code: QN01BB03
Pharmacodynamic properties
Mepivacaine hydrochloride is a potent local anaesthetic, with a rapid onset of action. Since it does not cause vasodilation it does not require adrenaline to prolong its effect.
The mechanism of action of mepivacaine is to prevent the generation and conduction of the nerve impulse. Conduction is blocked by decreasing or preventing the large transient increase in the permeability of excitable membranes to Na+ that is produced by a slight depolarisation. This action is due to a direct effect with voltage-sensitive Na+ channels. Mepivacaine exists in both charged and uncharged forms at physiological pH while the intracellular environment favours formation of the active, charged molecule. The onset of action of mepivacaine is, therefore, rapid (2-4 minutes) with an intermediate duration of action (about 1 hour).
Pharmacokinetic particulars
Peak venous levels of mepivacaine have been measured in mares following caudal epidural anaesthesia or caudal subarachnoid anaesthesia. The maximum venous concentrations were similar (0.05 µg/ml) and were reached in 51-55 minutes. In a separate study, mepivacaine or its metabolites appeared in the urine within 15 minutes of subcutaneous injection and reached peak levels within 2-6 hours. It was largely cleared from the urine within 24 hours. The major metabolite in horse urine is 3-hydroxymepivacaine.