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Chirocaine

Clinical Pharmacology
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CLINICAL PHARMACOLOGY

Chirocaine

Mechanism of Action

Chirocaine® is a member of the amino amide class of local anesthetics. Local anesthetics block the generation and the conduction of nerve impulses by increasing the threshold for electrical excitation in the nerve, by slowing propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: 1) pain, 2) temperature, 3) touch, 4) proprioception, and 5) skeletal muscle tone.

Pharmacokinetics

 

Table 1. Pharmacokinetic parameter values of levobupivacaine after the administration of 40 mg levobupivacaine, and those of racemic bupivacaine, R(+)- and S(-)- enantiomers after the administration of 40 mg of bupivacaine intravenously in healthy volunteers (mean ± SD).
  Parameter
  Levobupivacaine   Bupivacaine
 Racemate 		  R(+)-
 bupivacaine 		  S(-)-
 bupivacaine
  C max , µg/mL
 1.445 ± 0.237  1.421 ± 0.224  0.629 ± 0.100  0.794 ± 0.131
  AUC 0-(infinity) , µg hour/mL
 1.153 ± 0.447  1.166 ± 0.400  0.478 ± 0.166  0.715 ± 0.261
  t 1/2 , hour
 1.27 ± 0.37  1.15 ± 0.41  1.08 ± 0.17  1.34 ± 0.44
  V d , Liter
 66.91 ± 18.23  59.97 ± 17.65  68.58 ± 21.02  56.73 ± 15.14
  CI, Liter/hour
 39.06 ± 13.29  38.12 ± 12.64  46.72 ± 16.07  46.72 ± 16.07

After IV infusion of equivalent doses of levobupivacaine and bupivacaine, the mean clearance, volume of distribution, and terminal half-life values of levobupivacaine and bupivacaine were similar. No detectable levels of R (+)-bupivacaine were found after the administration of levobupivacaine.

A comparison of the estimates for plasma AUC and C max between Chirocaine and bupivacaine in two Phase III clinical trials involving short duration administration of either agent found that neither total plasma exposure or C max differed between the two drugs when compared within studies. Between study values differed somewhat, likely due to differences in the injection sites, volume, and total dose administered in each of the studies. These data suggest that Chirocaine and bupivacaine have a similar pharmacokinetic profile. Pharmacokinetic data from two Phase III studies are presented below:

 

Table 2. Pharmacokinetic parameter values of levobupivacaine and bupivacaine in patients administered the respective drugs epidurally and for brachial plexus block.
Route
Epidural Brachial Plexus Block
 
 Levobupivacaine Bupivacaine Levobupivacaine Bupivacaine
Concentration (%)
0.50 0.75 0.50 0.25 0.50 0.50
Dose received
75mg 112.5mg 75mg 1 mg/kg 2 mg/kg 2 mg/kg
n
9 9 8 10 10 9
C max (µ/mL)
0.582 0.811 0.414 0.474 0.961 1.029
T max (h)
0.52 0.44 0.36 0.50 0.71 0.68
AUC (0-t) (µg.h/mL)
3.561 4.930 2.044 2.999 5.311 6.832

Brand Name: Chirocaine
Generic Name: Levobupivacaine

Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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