Medication Guide App

Ropivacaine

Pronunciation: roe-PIV-a-kane
Class: Local anesthetic

Trade Names

Naropin
- Injection, solution 2 mg/mL (0.2%)
- Injection, solution 5 mg/mL (0.5%)
- Injection, solution 7.5 mg/mL (0.75%)
- Injection, solution 10 mg/mL (1%)

Pharmacology

Blocks 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.

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Pharmacokinetics

Absorption

C max is approximately 2.4 to 2.8 mg/L (epidural infusion), 1.1 to 1.6 mg/L (epidural block), 2.3 mg/L (plexus block), and 1.2 mg/L (IV infusion). T max is approximately 34 to 43 min (epidural block) and 54 min (plexus block).

Distribution

Vd at steady state is 41 ± 7 L. Ropivacaine is 94% protein bound, mainly to alpha-1 acid glycoprotein, and readily crosses the placenta.

Metabolism

Extensively metabolized in the liver, predominately by aromatic hydroxylation mediated by CYP4501A to 3-hydroxy ropivacaine and 4-hydroxy ropivacaine.

Elimination

Mainly (86%) excreted by the kidney. Half-life is approximately 5 to 6 h (epidural infusion), 5.7 to 7.1 h (epidural block), 6.8 h (plexus block), and 1.9 h (IV infusion).

Special Populations

Renal Function Impairment

No data available.

Hepatic Function Impairment

No data available.

Indications and Usage

For the management of acute pain (eg, postoperative, labor); for the production of local or regional anesthesia for surgery.

Contraindications

Known hypersensitivity to ropivacaine or to any local anesthetic agent of the amide type.

Dosage and Administration

Debilitated/Acutely Ill/Elderly Patients
Adults

IV Give reduced doses.

Labor Pain
Adults Lumbar epidural

IV 10 to 20 mL of a 0.2% solution (20 to 40 mg) as an initial dose, followed by 6 to 14 mL/h of a 0.2% solution (12 to 28 mg/h) as a continuous infusion or by incremental injections of 10 to 15 mL/h (20 to 30 mg/h) of 0.2% solution.

Postoperative Pain
Adults Epidural Infusion

IV If regional anesthesia was not used intraoperatively, an initial epidural block of 5 to 7 mL is induced via epidural catheter. Maintain analgesia with an infusion of 2 mg/mL (0.2%). Infusion rates of 6 to 14 mL (12 to 28 mg/h) provide adequate analgesia with nonprogressive motor block. Use epidural infusions up to 72 h.

Infiltration/Minor nerve block

IV 1 to 100 mL of a 0.2% solution (2 to 200 mg) or 1 to 40 mL of a 0.5% solution (5 to 200 mg)

Lumbar or thoracic epidural

IV 6 to 14 mL/h of a 0.2% solution (12 to 28 mg/h) as a continuous infusion.

Surgical Anesthesia
Adults Field block (eg, minor nerve blocks and infiltration)

IV 1 to 40 mL (5 to 200 mg) of a 0.5% solution.

Lumbar epidural

IV 15 to 30 mL (75 to 150 mg) of a 0.5% solution, 15 to 25 mL (113 to 188 mg) of a 0.75% solution, or 15 to 20 mL (150 to 200 mg) of a 1% solution.

Lumbar epidural for cesarean section

IV 20 to 30 mL (100 to 150 mg) of a 0.5% solution, 15 to 20 mL (113 to 150 mg) of a 0.75% solution.

Major nerve block

IV 35 to 50 mL (175 to 250 mg) of a 0.5% solution, or 10 to 40 mL (75 to 300 mg) of a 0.75% solution. Adjust the dose according to site of administration and patient status.

Thoracic epidural

IV 5 to 15 mL (25 to 75 mg) of a 0.5% solution, or 5 to 15 mL (38 to 113 mg) of a 0.75% solution.

Test Dose
Adults

IV During administration of epidural anesthesia, it is recommended that a test dose be administered initially. Use an adequate test dose (3 to 5 mL of a short-acting local anesthetic containing epinephrine) prior to induction of complete block. Repeat this test dose if patient movement potentiates epidural catheter displacement. Allow adequate time for onset of anesthesia following administration of each test dose.

General Advice

  • Use the lowest dosage that results in effective anesthesia to avoid high plasma levels and serious adverse reactions.
  • Inject the drug slowly and incrementally, with frequent aspirations before and during the injection to avoid intravascular injection
  • It is essential that aspiration for blood, or cerebrospinal fluid (where applicable), be done prior to injecting any local anesthetic (both the original dose and all subsequent doses) to avoid intravascular or subarachnoid injection.
  • Exercise caution when administering for prolonged periods of time (eg, more than 70 h in debilitated patients).
  • Supraclavicular brachial plexus blocks may be associated with a higher frequency of serious adverse reactions.
  • A test dose is recommended prior to administration during epidural anesthesia.
  • Do not use solutions of ropivacaine for the production of obstetrical paracervical block anesthesia, retrobulbar block, or spinal anesthesia (subarachnoid block), to perform intra-articular infusions, or to perform IV regional anesthesia (bier block).
  • Disinfecting agents containing heavy metals, which cause release of respective ions (eg, mercury, zinc, copper) should not be used for skin or mucous membrane disinfection because they have been related to incidents of swelling and edema.
  • Solubility is limited at pH above 6; therefore, care must be taken because precipitation may occur if ropivacaine is mixed with alkaline solutions.
  • Inspect parenteral drug products for particulate matter and discoloration prior to administration; discard solutions that are discolored or that contain particulate matter.

Storage/Stability

Store between 68° and 77°F. Any solution remaining from an opened container should be discarded promptly. Continuous infusion bottles should not be left in place for more than 24 h.

Drug Interactions

Class III antiarrhythmic drugs (eg, amiodarone)

Caution is advised during coadministration. Keep patients treated with class III antiarrhythmic drugs under close surveillance and consider ECG monitoring because cardiac effects may be additive.

CYP1A2 inhibitors (eg, fluvoxamine, quinolones [eg, ciprofloxacin, norfloxacin])

Plasma Cl of ropivacaine may be reduced, increasing ropivacaine plasma concentrations and the risk of adverse reactions. Exercise caution when CYP1A2 inhibitors are coadministered.

CYP1A2 substrates (eg, imipramine, theophylline)

Possible interactions with drugs known to be metabolized by CYP1A2 via competitive inhibition may occur. Plasma concentrations of these CYP1A2 substrates may be elevated. Use with caution and consider the possibility of an interaction.

CYP3A4 inhibitors (eg, ketoconazole)

Coadministration may reduce ropivacaine Cl, increasing ropivacaine plasma concentrations and the risk of adverse reactions. Monitor the clinical response of the patient. If an interaction is suspected, adjust treatment as needed.

Local anesthetics (eg, prilocaine)

Use with caution because the toxic effects of these drugs are additive.

Adverse Reactions

Cardiovascular

Hypotension (69%); bradycardia (20%); hypertension, tachycardia (1% to 5%); cardiac arrest; depressed myocardium; ventricular arrhythmias, including ventricular fibrillation and ventricular tachycardia.

CNS

Headache (8%); paresthesia (6%); anxiety, dizziness, hypoesthesia, rigors (1% to 5%); convulsions, excitation and/or depression, restlessness, tremors, unconsciousness.

Dermatologic

Pruritus (5%).

EENT

Blurred vision, constriction of pupils, tinnitus.

GI

Nausea (29%); vomiting (15%); fecal incontinence, loss of bowel control.

Genitourinary

Urinary retention (5%); oliguria, UTI (1% to 5%); breast disorder (breast-feeding) (1%); loss of bladder control, urinary incontinence; loss of perineal sensation and sexual function.

Hypersensitivity

Allergic-type reactions, such as urticaria, pruritus, erythema, angioneurotic edema, including laryngeal edema, tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and anaphylactoid symptomatology, including severe hypotension.

Respiratory

Dyspnea (1% to 5%); rhinitis (1%); respiratory arrest, respiratory paralysis, underventilation or apnea.

Miscellaneous

Back pain (16%); fever (9%); pain (8%); postoperative complications (7%); anemia (6%); chest pain, cramps, hypokalemia (1% to 5%); chills (4%); progression of labor poor/failed (1%).

Precautions

Monitor

Perform constant monitoring of CV and respiratory vital signs (adequacy of ventilation) and the patient's state of consciousness after each local anesthetic injection. During the administration of epidural anesthesia, it is recommended that a test dose be administered initially and the effects monitored before the full dose is given. Following the test dose, monitor the heart continuously for heart rate increases. Constantly observe patients receiving head and neck blocks; monitor their circulation and respiration. Keep resuscitative equipment and personnel for treating adverse reactions immediately available.


Pregnancy

Category B . Amounts measured in the maternal circulation are very low and do not appear to represent a significant embryofetal risk.

Lactation

Undetermined. There appears to be no risk to a breast-feeding infant.

Children

Safety and efficacy not established.

Elderly

Start at the low end of the dosage range; it may be useful to monitor renal function.

Renal Function

Risk of toxic reactions may be greater in patients with impaired renal function.

Hepatic Function

Use caution, especially with repeat doses. Patients with severe hepatic disease are at greater risk for developing toxic plasma concentrations.

Special Risk Patients

Use with caution in patients with hypotension or hypovolemia.

Cardiovascular effects

Use with caution in patients with heart block or impaired CV function. Unintended IV injection is possible and may result in cardiac arrhythmia or cardiac arrest.

Chrondrolysis

Has been reported when administered as intra-articular infusion following arthroscopic and other surgical procedures; the majority of the reported cases have involved the shoulder joint. Intra-articular infusion is an unapproved use.

CNS toxicity

Restlessness, anxiety, incoherent speech, light-headedness, metallic taste, numbness and tingling of the mouth and lips, tinnitus, dizziness, blurred vision, tremors, twitching, depression, or drowsiness may be early warning signs of CNS toxicity.

Emergency situations

Not recommended for emergency situations where a fast onset of surgical anesthesia is necessary.

Intravascular or subarachnoid injection

It is essential that aspiration for blood, or cerebrospinal fluid (where applicable), be done prior to injecting any local anesthetic (both the original dose and all subsequent doses) to avoid intravascular or subarachnoid injection

Malignant hyperthermia

Has been reported with amide local anesthetics.

Ophthalmic surgery

Use for retrobulbar block is not recommended.

Overdosage

Symptoms

Acidosis, apnea, cardiac arrest, convulsions, hypoxia, hypercarbia, muscle twitching.

Patient Information

  • Explain to patient that adverse reactions related to the CNS (eg, anxiety, blurred vision, incoherent speech, metallic taste, restlessness, twitching) can occur and may be a result of CNS toxicity.
  • Advise patients in advance that they may experience temporary loss of sensation and motor activity in the anesthetized part of the body following administration of lumbar epidural anesthesia.

Copyright © 2009 Wolters Kluwer Health.

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