Ropivacaine

274.4

274.40

617-525-1

7IO5LYA57N

DTXSID4040187|DTXSID2048379

N01BB09|N - Nervous system

2933399090

32.3

3

1

1.0±0.1 g/cm3

144-146 °C

410.2±45.0 °C at 760 mmHg

201.9±28.7 °C

1.552

2.53e-01 g/L

D25 -82.0° (c = 2 in methanol)

8.07None

8.07

3

R36/37/38:Irritating to eyes, respiratory system and skin .

36/37/39-26

LK8650000

Xi

P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, P501

H302

|Warning|H302 (92.31%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, and P501|Aggregated GHS information provided by 13 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, and P501|Aggregated GHS information provided by 3 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

High systemic doses of ropivacaine can result in central nervous system (CNS) and cardiovascular effects, with the CNS effects usually occurring at lower blood plasma concentrations and additional cardiovascular effects occurring at higher concentrations. However, cardiovascular collapse may bee seen at low concentrations. CNS effects include CNS excitation involving nervousness, tingling around the mouth, tinnitus, tremor, dizziness, blurred vision, seizures. CNS depressant effects may follow, associated with drowsiness, loss of consciousness, respiratory depression and apnea. Cardiovascular events may be caused by hypoxemia secondary to respiratory depression and include hypotension, bradycardia, arrhythmias, and/or cardiac arrest.

In clinical trials with the amide local anesthetics, serum aminotransferase and alkaline phosphatase elevations were rarely reported and were generally no more common than with placebo or comparator injections. Despite widespread use for many decades, the local amide anesthetics, when given as single or limited injections or infusions, have not been convincingly linked to instances of clinically apparent liver injury, and liver toxicity is not mentioned in product labels. Nevertheless, there have been several case series of jaundice arising a few days to as long as a month after use of bupivacaine given over several days as a constant infusion or as repeated injections into a localized area of pain. Some reports mentioned concurrent administration of an antibiotic such as cefazolin during the perioperative period, which might have accounted for the liver injury. However, in other reports, only bupivacaine was given. The liver injury was mixed or cholestatic and mild-to-moderate in severity, resolving within 1 to 2 months of onset without residual evidence of liver injury. In many instances, there was an accompanying low grade fever, rash or eosinophilia, suggesting a hypersensitivity reaction.

94%, mainly to a1-acid glycoprotein

Used in obstetric anesthesia and regional anesthesia for surgery.|FDA Label

The amide local anesthetics including lidocaine, bupivacaine and ropivacaine are commonly used for pain control during minor surgery or invasive procedures such as biopsies, small excisions or dental work. These local anesthetics have not been linked to serum enzyme elevations, but when given as constant infusions or repeated injections have been occasionally mentioned as possible causes of clinically apparent liver injury.

Anesthetics, Local

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.

Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)

Bioavailability is 87%–98% following epidural administration.|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.|387 +/- 107 mL/min

Hepatic|Ropivacaine has known human metabolites that include 3-hydroxy-ropivacaine and PPX.

Approximately 4.2 hours.

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.

1 Propyl 2',6' pipecoloxylidide

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients