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Product Name:Levobupivacaine hydrochloride
Levobupivacaine is a local anaesthetic drug belonging to the amino amide group.
It is the S-enantiomer of bupivacaine,it is a reversible neuronal sodium
channel inhibitor, used as a long-acting local anesthetic.
Levobupivacaine hydrochloride is commonly marketed by Abbott under the trade
Compared to bupivacaine, levobupivacaine is associated with less vasodilation
and has a longer duration of action. It is approximately 13 percent less potent
(by molarity) than racemic bupivacaine and has a longer motor block onset time.
Levobupivacaine is an amide-type local anaesthetic. Levobupivacaine acts via
blockade of voltage-sensitive ion channels in neuronal membranes, preventing
transmission of nerve impulses. Localised and reversible anaesthesia is
produced by interference with the opening of the sodium channel, which inhibits
conduction of the action potential in nerves involved in sensory and motor
activity and sympathetic activity. Levobupivacaine displaces 3H-BTX from sodium
channels of rat brain synaptosomes with IC50 of 2.9 μM and Hill coefficients
of 1.2. When cell membrane is held at -80 mV, -70 mV, -60 mV or -100 mV,
Levobupivacaine shows tonic inhibition of sodium channel in GH3 cells with
IC50s of 132.1, 37.6, 21.6 and 264 μM, respectively. Levobupivacaine depresses
action potential of isolated axon in vitro. Levobupivacaine (1mM) depresses
action potential amplitude and maximal rate of rise of action potential
(dV/dtmax) in the crayfish giant axons with value of 88 and 81 respectively,
after perfusion for 15 min.  Levobupivacaine also displays activity on
cardiac ion channels. In isolated ventricular myocytes, the apparent affinity
for inactivated state of the sodium channel is 4.8 μM for Levobupivacaine,
with a calculated KD of 39μM. On inhibition of cardiac delayed rectifier
potassium channels (hKv1.5), the steady-state block for Levobupivacaine (20
μM) is 31%, with a calculated KD of 27.3 μM. Levobupivacaine may also inhibit
cardiac calcium channels. 10 μM Levobupivacaine produces a 50% decrease in
contractile force of guinea-pig papillary muscles.
Levobupivacaine has similar nerve blocking potency with bupivacaine.
Levobupivacaine at a dose of 0.125%, inhibits motor and nocifensive pinch
responses with maximum %MPE of 99 and 68 respectively, and inhibits the
duration of deficits of motor and nocifensive pinch responses (60 and 30 ,
respectively) after sciatic nerve block.
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