| Indication |
Used in obstetric anesthesia and regional anesthesia for surgery. |
| Pharmacodynamics |
Ropivacaine, a local anesthetic agent, is indicated for the
production of local or regional anesthesia or analgesia for surgery, for
oral surgery procedures, for diagnostic and therapeutic procedures, and
for obstetrical procedures. |
| Mechanism of action |
Local anesthetics such as Ropivacaine block the generation and the
conduction of nerve impulses, presumably by increasing the threshold
for electrical excitation in the nerve, by slowing the propagation of
the nerve impulse, and by reducing the rate of rise of the action
potential. Specifically, they block the sodium-channel and decrease
chances of depolarization and consequent action potentials. In general,
the progression of anesthesia is related to the diameter, myelination
and conduction velocity of affected nerve fibers. |
| Absorption |
Bioavailability is 87%–98% following epidural administration. |
| Volume of distribution |
Not Available |
| Protein binding |
94%, mainly to a1-acid glycoprotein |
| Metabolism |
Hepatic |
| Route of elimination |
Ropivacaine is extensively metabolized in the liver, predominantly
by aromatic hydroxylation mediated by cytochrome P4501A to 3-hydroxy
ropivacaine. After a single IV dose approximately 37% of the total dose
is excreted in the urine as both free and conjugated 3-hydroxy
ropivacaine. In total, 86% of the ropivacaine dose is excreted in the
urine after intravenous administration of which only 1% relates to
unchanged drug. |
| Half life |
Approximately 4.2 hours. |
| Clearance |
- 387 +/- 107 mL/min
- unbound plasma clearance=7.2 +/- 1.6 L/min
|
| Toxicity |
Systemic exposure to excessive quantities of ropivacaine mainly
result in central nervous system (CNS) and cardiovascular effects – CNS
effects usually occur at lower blood plasma concentrations and
additional cardiovascular effects present at higher concentrations,
though cardiovascular collapse may also occur with low concentrations.
CNS effects may include CNS excitation (nervousness, tingling around the
mouth, tinnitus, tremor, dizziness, blurred vision, seizures) followed
by depression (drowsiness, loss of consciousness, respiratory depression
and apnea). Cardiovascular effects include hypotension, bradycardia,
arrhythmias, and/or cardiac arrest – some of which may be due to
hypoxemia secondary to respiratory depression. |
