2. INTRODUCTION:
Long acting amide local anesthetic with both
anesthetic and analgesic effects.
Similar to bupivacaine & etidocaine in duration of
activity.
Structurally similar to mapivacaine & bupivacaine.
Decreased cardiotoxicity
Used for regional nerve block.
At high doses it produces surgical anesthesia and
at lower doses it produces analgesia (sensory
block) with limited motor block..
3. STRUCTURE:
belongs to the group of local
anaesthetics, the
pipecoloxylidides and has a
propyl group on the
piperidine nitrogen atom
(compared to bupivacaine,
which has a butyl group)
Enantiomer of propivacaine (S
stereoisomer)
4. PHARMACOKINETICS
Onset time : 15 mins
Duration :2-6 hrs
Bioavailability:87%–98% (epidural)
Metabolism: Hepatic (CYP1A2-mediated)
Biological half-life:1.6–6 hours (varies with
administration route)
Excretion: Renal 86%
less lipophilic than bupivacaine less likely to
penetrate large myelinated motor fibres selective
action on the pain-transmitting A β and C nerves rather
than Aβ fibres, which are involved in motor function.
bound to plasma proteins to an extent of 94%, mainly to
α1-acid glycoprotein.
5. MODE OF ACTION
reversible inhibition of sodium ion influx, and
thereby blocks impulse conduction in nerve fibre.
potentiated by dose-dependent inhibition of
potassium channels.
9. CLINICAL SIDE EFFECTS
CNS toxicity:usually occur at lower blood plasma
concentrations
CNS excitation,(nervousness, tingling around the
mouth, tinnitus,tremor, dizziness, blurred vision,
seizures) followed by depression(drowsiness, loss
of consciousness), respiratory depression and
apnea).
CVS toxicity:
hypotension, bradycardia, arrhythmias, and/or
cardiac arrest
10. INTERACTIONS WITH OTHER DRUGS
Anti-arrhythmics: increased myocardial
depresssion
Antidepressants:meabolism of ropivacaine
inhibited by fluvoxamine(strong inhibitors of
cytochrome P4501A2).
other local anaesthetics or agents : (structurally
related to amide-type local anaesthetics)toxic
effects of these drugs are additive.
11. TREATMENT OF OVERDOSE:
Celepid, a commonly available intravenouslipid
emulsion, can be effective in treating severe
cardiotoxicity.