Ropivacaine (Local) (Monograph)

Brand name: Naropin
Drug class: Local Anesthetics

Medically reviewed by Drugs.com on Jun 10, 2024. Written by ASHP.

Introduction

Long-acting local anesthetic (amide type).^{1 3 14}

Uses for Ropivacaine (Local)

Local or Regional Anesthesia and Analgesia

Local or regional anesthesia for surgery (including cesarean section) and management of acute pain (e.g., postoperative pain, labor pain).^{1 8 9 10 12 13 14 15}

Used as a component of multimodal analgesia (i.e., simultaneous use of a combination of analgesic drugs and techniques that target different mechanisms) in the management of postoperative pain.²²⁰

Compared with bupivacaine, generally has a similar onset and duration of sensory block, but a lower intensity and shorter duration of motor block.^{1 3 8 9 10 12 13 14 15} Appears to have a lower potential for CNS and cardiovascular toxicity than bupivacaine.^{3 8 9 10 11 12 14 15}

Not recommended for obstetrical paracervical block, retrobulbar block for ophthalmic surgery, spinal anesthesia (subarachnoid block), or IV regional anesthesia (Bier block) because of lack of clinical experience and/or risk of toxicity.¹

Ropivacaine (Local) Dosage and Administration

General

Dispensing and Administration Precautions

• Administer only by clinicians experienced in the diagnosis and management of toxicities and other complications associated with local anesthetics.¹

• Ensure that resuscitative equipment, oxygen, drugs, and personnel required for treatment of adverse reactions are immediately available.¹

• Administer slowly in incremental doses to reduce risk of adverse effects (e.g., local anesthetic systemic toxicity).^{1 7}

• Perform frequent aspirations for blood or CSF (when applicable) to avoid intravascular administration and inadvertent subarachnoid injection.¹

• Ensure a functioning IV line in patients receiving a major regional nerve block.¹

• Injections into the head and neck area require particular care; serious adverse effects reported due to complications from the anesthetic technique.¹

• Carefully and constantly monitor patients for possible cardiovascular, respiratory, or CNS complications during and after administration.¹

Administration

Injection

Administer by epidural block, peripheral nerve block (e.g., brachial plexus block), or local infiltration.^{1 6}

Do not use for obstetrical paracervical block, retrobulbar block, IV regional anesthesia (Bier block), or spinal anesthesia (subarachnoid block).¹

Has been administered by continuous intra-articular infusion^{† [off-label]} (e.g., for control of postoperative pain); however, such use associated with chondrolysis.^{5 200 201 202 203 204 205 206 207 208 209} (See Risk of Chondrolysis Associated with Intra-articular Infusions of Local Anesthetics under Cautions.)

Consult specialized references for specific techniques and procedures for administering local anesthetics.¹

During epidural administration, administer in incremental doses of 3–5 mL with sufficient time between doses to detect toxic manifestations of unintentional injection.¹

For chemical disinfection of container surface, moisten cotton or gauze with isopropyl (rubbing) alcohol (91%) or ethyl alcohol (70%) and wipe ampul or vial stopper thoroughly just prior to use.¹

Standardize 4 Safety

Standardized concentrations for ropivacaine have been established through Standardize 4 Safety (S4S), a national patient safety initiative to reduce medication errors, especially during transitions of care.²⁵¹ Because recommendations from the S4S panels may differ from the manufacturer’s prescribing information, caution is advised when using concentrations that differ from labeling, particularly when using rate information from the label.²⁵¹ For additional information on S4S (including updates that may be available), see [Web].²⁵¹

Dosage

Available as ropivacaine hydrochloride.^{1 6} Dosage expressed in terms of ropivacaine hydrochloride.¹

Individualize dosage based on anesthetic procedure, degree of anesthesia required, surgical site, and patient response.¹ Manufacturer's dosage recommendations are based on the expected average dosage range necessary to produce a successful block in adults; use as a general guideline.¹

Use smallest dose and concentration required to produce the desired effect.^{1 7}

To prevent intravascular or subarachnoid injection of a large epidural dose, inject a test dose (e.g., 3–5 mL of a short-acting local anesthetic solution containing epinephrine) prior to administering the total dose.¹ When clinical conditions permit, use a test dose containing epinephrine to detect inadvertent intravascular injection.¹ Repeat test dose if epidural catheter is displaced.¹ Allow adequate time for onset of anesthesia following administration of each test dose.¹

Adults

Surgical Anesthesia

Lumbar Epidural Block

For general surgery: 15–30 mL of a 0.5% solution (75–150 mg), 15–25 mL of a 0.75% solution (113–188 mg), or 15–20 mL of a 1% solution (150–200 mg).¹ Onset of anesthesia approximately 10–30 minutes and duration approximately 2–6 hours depending on the dose administered.¹

For cesarean section: 20–30 mL of a 0.5% solution (100–150 mg) or 15–20 mL of a 0.75% solution (113–150 mg).¹ Onset of anesthesia approximately 10–25 minutes and duration approximately 2–5 hours depending on the dose administered.¹

Thoracic Epidural Block

For general surgery: 5–15 mL of a 0.5 or 0.75% solution (25–113 mg).¹ Onset of anesthesia approximately 10–20 minutes depending on the dose administered.¹

Major Nerve Block (e.g., Brachial Plexus Block)

35–50 mL of a 0.5% solution (175–250 mg) or 10–40 mL of a 0.75% solution (75–300 mg).¹ Onset of anesthesia approximately 10–30 minutes and duration approximately 5–10 hours depending on the dose administered.¹

Doses given for major nerve blocks must be adjusted based on the site of administration and patient status.¹ A dose of 300 mg for brachial plexus block may approach the threshold for CNS toxicity; use with caution.^{1 4}

Field Block (e.g., Minor Nerve Blocks, Infiltration)

1–40 mL of a 0.5% solution (5–200 mg).¹ Onset of anesthesia approximately 1–15 minutes and duration approximately 2–6 hours depending on the dose administered.¹

Labor Pain Management

Lumbar Epidural Block

Initially, 20–40 mg (10–20 mL of a 0.2% solution), followed by a continuous epidural infusion of 12–28 mg/hour (6–14 mL/hour of a 0.2% solution) or incremental epidural injections (top-ups) of 20–30 mg/hour (10–15 mL/hour of a 0.2% solution).¹

Following administration of initial dose, onset of anesthesia approximately 10–15 minutes and duration approximately 0.5–1.5 hours.¹

Postoperative Pain Management

Lumbar or Thoracic Epidural Block

12–28 mg/hour (6–14 mL/hour of a 0.2% solution) as a continuous lumbar or thoracic epidural infusion.¹ In clinical studies, epidural infusions were administered for up to 72 hours.¹

Local Infiltration (e.g., Minor Nerve Block)

1–100 mL of a 0.2% solution (2–200 mg) or 1–40 mL of a 0.5% solution (5–200 mg).¹ Onset of analgesia approximately 1–5 minutes and duration approximately 2–6 hours depending on the dose administered.¹

Special Populations

Hepatic Impairment

Consider possibility of increased toxicity and adjust dosage accordingly.¹

Renal Impairment

Consider possibility of increased toxicity and adjust dosage accordingly.¹

Geriatric Patients

Generally reduce usual dosages.¹ (See Geriatric Use under Cautions.)

Other Populations

Reduce dosage in debilitated or acutely ill patients.¹ Use caution when administering for prolonged periods (>70 hours) in debilitated patients.¹

Cautions for Ropivacaine (Local)

Contraindications

• Known hypersensitivity to ropivacaine hydrochloride or other local anesthetics of the amide type.¹

Warnings/Precautions

Warnings

Administration Precautions

Because of the potential for serious adverse effects, take special precautions during administration.^{1 7} (See General under Dosage and Administration.) Ensure that oxygen, resuscitative equipment, drugs, and personnel required for treatment of adverse reactions are immediately available.¹

Delay in proper management of dose-related toxicities may result in acidosis, cardiac arrest, and possibly death.¹

Risk of Chondrolysis Associated with Intra-articular Infusions of Local Anesthetics

Chondrolysis (necrosis and destruction of articular cartilage) reported in patients receiving continuous intra-articular infusions of local anesthetics, administered for 48–72 hours via elastomeric infusion devices, for treatment of postoperative pain.^{1 200 201 202 203 204 205 206 207 208 209} Primarily observed in the shoulder joint following arthroscopic or other shoulder surgery.^{1 200} Time of onset of symptoms, including joint pain, stiffness, and loss of motion can be variable, but may begin ≥2 months after surgery.¹ May result in long-term disability; often requires intervention (e.g., shoulder replacement, arthroplasty).^{1 200 202 203 204 205 206 209} Not known whether the drug, infusion device, and/or other factors contributed to the development of chondrolysis.^{200 201} Neither local anesthetics nor elastomeric infusion devices are approved for use for continuous intra-articular infusion therapy.^{1 200 201}

Accidental Injection

Accidental intravascular or subarachnoid injection may cause cardiac and CNS toxicity.¹ (See CNS Effects and also see Cardiovascular Effects under Cautions.)

Aspirate prior to administration to guard against intravascular or subarachnoid injection; however, a negative aspiration does not ensure against an intravascular or subarachnoid injection.¹

Sensitivity Reactions

Hypersensitivity Reactions and Cross-hypersensitivity

Allergic-type reactions (e.g., urticaria, pruritus, erythema, angioedema, tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, anaphylactoid symptoms) have occurred rarely.¹

Possible cross-hypersensitivity between amide-type local anesthetics.¹ (See Contraindications under Cautions.)

General Precautions

CNS Effects

Possible adverse CNS effects (e.g., restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, twitching, depression, drowsiness) if absorbed systemically.^{1 3 4 7}

Dose of 300 mg used for brachial plexus block may approach threshold for CNS toxicity.¹ Prolonged blocks can increase risk of toxic plasma concentrations or induce local neural injury.¹

Carefully monitor patients for possible CNS toxicity after administration.¹

Cardiovascular Effects

Possible adverse cardiovascular effects (e.g., decreased cardiac output, arrhythmias, reduced myocardial contractility and conductivity) if absorbed systemically.^{1 7 14}

Carefully monitor patients for possible cardiovascular toxicity and monitor vital signs after administration.¹

Use with caution in patients with impaired cardiovascular function, hypotension, hypovolemia, or heart block.¹

If cardiac arrest occurs, prolonged resuscitative efforts may be required.¹

Familial Malignant Hyperthermia

Many drugs used during the conduct of anesthesia may trigger familial malignant hyperthermia; not known whether amide-type local anesthetics trigger this reaction.¹ Ensure standard protocol for management is available.¹

Specific Populations

Pregnancy

Category B.¹

No adequate and well-controlled studies in pregnant women.¹ No evidence of teratogenic effects or adverse developmental effects in animals; however, maternal toxicity observed.¹ Use during pregnancy only if benefits outweigh risks.¹

Labor and Delivery

Maternal hypotension reported.¹ To prevent decreases in BP, elevate patient’s legs and position patient on her left side.¹ Monitor fetal heart rate continuously; electronic fetal monitoring highly advisable.¹

Epidural anesthesia may prolong second stage of labor (by removing parturient’s reflex urge to bear down or by interfering with motor function).¹

Lactation

Distributed into milk in rats; not known if drug or its metabolites distribute into human milk.¹ Use with caution.¹

Pediatric Use

Manufacturer states safety and efficacy not established in pediatric patients;¹ however, has been used in pediatric patients for postoperative analgesia.^{14 15}

Geriatric Use

Differences in various pharmacodynamic measures observed with increasing age; in one clinical study, upper level of analgesia increased with age, maximum decrease of mean arterial pressure declined with age for the first hour following epidural administration, and intensity of motor blockade increased with age.¹

Because ropivacaine and its metabolites are substantially excreted by the kidneys, risk of toxic reactions may be greater in patients with renal impairment.¹ Select dosage with caution in geriatric patients, usually starting at the lower end of dosage range, since such patients are more likely to have decreased hepatic, renal, and/or cardiac function as well as concomitant illnesses.¹ Monitoring renal function in geriatric patients may be helpful.¹

Hepatic Impairment

Extensively metabolized in liver.¹ Possible increased risk of toxicity, particularly in patients with severe hepatic impairment.¹ Use with caution.¹

Renal Impairment

Eliminated by the kidneys.¹ Possible increased risk of toxicity in patients with renal impairment.¹

Common Adverse Effects

Hypotension, nausea, vomiting, bradycardia, fever, pain, postoperative complications, anemia, paresthesia, headache, pruritus, back pain.¹

Drug Interactions

No formal drug interaction studies performed to date.¹

Drugs Affecting or Affected by Hepatic Microsomal Enzymes

Metabolized by CYP1A2.¹

Potent inhibitors of CYP1A2 can increase plasma ropivacaine concentrations.¹ Caution is advised when ropivacaine is used concomitantly with CYP1A2 inhibitors.¹

There is also a possible interaction with drugs known to be metabolized by CYP1A2 via competitive inhibition.¹

Specific Drugs

Ropivacaine (Local) Pharmacokinetics

Absorption

Bioavailability

Systemic absorption is dependent on total dose and concentration of drug, route of administration, patient's hemodynamic/circulatory condition, and vascularity of administration site.¹

Peak plasma concentrations achieved approximately 34–54 minutes following epidural or brachial plexus nerve block.¹

Following epidural administration, complete and biphasic absorption is observed.^{1 6}

Onset

Approximately 10–30 minutes following lumbar epidural administration in recommended doses for general surgery.¹

Approximately 10–25 minutes following lumbar epidural administration in recommended doses for cesarean section.¹

Approximately 10–20 minutes following thoracic epidural administration in recommended doses for general surgery.¹

Approximately 10–30 minutes following major nerve block (e.g., brachial plexus block) in recommended doses.¹

Approximately 1–15 minutes following field block (e.g., minor nerve blocks, infiltration) in recommended doses for surgical anesthesia.¹

Approximately 10–15 minutes following lumbar epidural administration in recommended doses for labor pain management.¹

Approximately 1–5 minutes following local infiltration in recommended doses for postoperative pain management.¹

Duration

Approximately 2–6 hours following lumbar epidural administration in recommended doses for general surgery.¹ Higher doses produce a more profound block with a longer duration of effect.¹

Approximately 2–5 hours following lumbar epidural administration in recommended doses for cesarean section.¹

Approximately 5–10 hours following major nerve block (e.g., brachial plexus block) in recommended doses.¹

Approximately 2–6 hours following field block (e.g., minor nerve blocks, infiltration) in recommended doses for surgical anesthesia.¹

Approximately 0.5–1.5 hours following lumbar epidural administration in recommended doses for labor pain management.¹

Approximately 2–6 hours following local infiltration in recommended doses for postoperative pain management.¹

Distribution

Extent

Crosses the placenta.¹

Distributes into milk in rats; not known whether drug or metabolites distribute into human milk.¹

Plasma Protein Binding

94%, mainly to α₁-acid glycoprotein.¹

Elimination

Metabolism

Extensively metabolized in the liver, principally by CYP1A, to 3-hydroxyropivacaine.¹

Elimination Route

86% excreted in urine following IV administration (only 1% as unchanged drug).¹

Half-life

Half-life longer after epidural than IV administration.¹ Approximately 1.9 hours following 20-minute IV infusion; approximately 5–7 hours following epidural administration.¹

Approximately 6.8 hours following brachial plexus block.¹

Terminal half-life may be increased to >30 hours when doses >300 mg are used for local infiltration.¹

Stability

Storage

Parenteral

Injection

20–25°C.¹ Do not leave continuous infusion bottles in place for >24 hours.¹

Compatibility

Parenteral

Drug Compatibility

Do not use disinfecting agents containing heavy metals (e.g., mercury, zinc, copper) for skin or mucous membrane disinfection; swelling and edema have occurred.¹ For chemical disinfection of the container surface, isopropyl alcohol (91%) or ethyl alcohol (70%) recommended.¹

Actions

• Local anesthetics block the generation and conduction of nerve impulses possibly by increasing the threshold for electrical excitation, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.¹

• Progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers.¹

• Structurally related to bupivacaine, but differs in stereoselectivity (ropivacaine is a pure S-enantiomer while bupivacaine is a racemic mixture).^{1 14}

• Ropivacaine is less lipophilic and less likely to penetrate large myelinated nerve fibers than bupivacaine.^{14 15}

• Physiochemical and stereoselective differences are thought to contribute to lower cardiac and CNS toxicity of ropivacaine compared with bupivacaine.^{11 14 15}

• Epinephrine has no substantial effect on time of onset or duration of ropivacaine anesthesia.^{1 3}

Advice to Patients

• Importance of advising patients of the possibility of temporary loss of sensation and motor activity following lumbar epidural anesthesia.¹

• Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease).¹

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

• Importance of informing patients of other important precautionary information.¹ (See Cautions.)

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

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Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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