chloroprocaine (Rx)

Brand and Other Names:Nesacaine, Clorotekal
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

solution, injection for nerve block

  • 1% (Nesacaine)
  • 2% (Nesacaine, Nesacaine MPF [preservative free])
  • 3% (Nesacaine MPF)

solution, intrathecal injection

  • 10mg/mL (Clorotekal)
  • Supplied as 50mg/5mL chloroprocaine HCl (equivalent to 44.05mg/5mL [8.81mg/mL] chloroprocaine)

Subarachnoid Block

Clorotekal: Indicated for subarachnoid block (spinal anesthesia) in adults undergoing surgical procedures that are suitable for the product’s short duration of action

For intrathecal use only

To obtain an effective block to the T 10 level with 1 single administration in an adult of average height and weight (~70 kg), the recommended dose is 50 mg

Doses >50 mg have not been adequately tested for efficacy and safety

Extent and degree of spinal anesthesia depends upon several factors including dosage, specific gravity of the anesthetic solution, volume of solution used, force of injection, level of puncture, and position of the patient during and immediately after injection

Central Nerve Block

Nesacaine-MPF 2% and 3% injection in single-dose vials without a preservative indicated for production of local anesthesia by central nerve block, including lumbar and caudal epidural blocks

Caudal block, 2-3% solution: 15-25 mL initially; repeat doses may be given at 40-60 min intervals

Lumbar epidural, 2-3% solution: 2-2.5 mL per segment; usual total volume is 15-25 mL; repeat doses of 2-6 mL less than the original dose may be given at 40-50 min intervals

Infiltration & Peripheral Nerve Block

Nesacaine 1% and 2% injection in multidose vials with preservatives indicated for production of local anesthesia by infiltration and peripheral nerve block; not to be used for lumbar or caudal epidural anesthesia

Nesacaine-MPF 2% injection in a single-dose vial without a preservative indicated for production of local anesthesia by infiltration and peripheral nerve block

Nesacaine, Nesacaine-MPF: Not for subarachnoid administration

Nesacaine or Nesacaine-MPF 1%-2% total doses

  • Mandibular (2% solution): 40-60 mg (2-3 mL)
  • Infraorbital (2% solution): 10-20 mg (0.5-1 mL)
  • Brachial plexus (2% solution): 600-800 mg (30-40 mL)
  • Digital, without epinephrine (1% solution): 30-40 mg (3-4 mL)
  • Pudendal (2% solution): 400 mg (10 mL on each side)
  • Paracervical (1% solution): up to 120 mg (3 mL per each of 4 sites)
  • Single doses should not exceed 800 mg; single dose with epinephrine should not exceed 1000 mg
  • Cervical/thoracic region: 30-60 mg for each segment to be anesthetized

Dosage Forms & Strengths

solution, injection for nerve block

  • 1% (Nesacaine)
  • 2% (Nesacaine, Nesacaine MPF [preservative free])
  • 3% (Nesacaine MPF)

Infiltration

<3 years

  • Safety and efficacy not established

≥3 years

  • 0.5-1% concentration recommended; not to exceed 11 mg/kg

Nerve Block

<3 years

  • Safety and efficacy not established

≥3 years

  • 1-1.5% concentration recommended; not to exceed 11 mg/kg
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Interactions

Interaction Checker

and chloroprocaine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (1)

            • bupivacaine liposome

              chloroprocaine increases toxicity of bupivacaine liposome by Other (see comment). Contraindicated. Comment: Do not admix with other local nonbupivacaine-based local anesthetics; admixing results in a rapid increase in free (unencapsulated) bupivacaine.

            Serious - Use Alternative (1)

            • bupivacaine implant

              chloroprocaine, bupivacaine implant. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid additional local anesthetic administration within 96 hr following bupivacaine implantation. If use of additional local anesthetics is unavoidable based on clinical need, monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity.

              chloroprocaine, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.

            Monitor Closely (5)

            • hyaluronidase

              hyaluronidase, chloroprocaine. Other (see comment). Use Caution/Monitor. Comment: Hyaluronidase hastens the onset of local analgesia and reduces swelling, but increases systemic absorption of anesthetic. This decreases the duration of action and increases incidence of systemic reaction.

            • nadolol

              nadolol, chloroprocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).

            • pindolol

              pindolol, chloroprocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).

            • propranolol

              propranolol, chloroprocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).

            • timolol

              timolol, chloroprocaine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Increased effects of epinephrine in anesthetic; risk of hypertension and bradycardia. Do NOT D/C chronic beta blocker Tx prior to anesthetic administration. Consider selective beta 1 blocker (e.g., metoprolol).

            Minor (0)

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              Adverse Effects

              >10% (Intrathecal Administration, Clorotekal)

              Procedural pain (16%)

              1-10% (Intrathecal Administration, Clorotekal)

              Hypotension (4.9%)

              Injection site pain (3.7%)

              Frequency Not Defined

              Common

              • Anxiety
              • Dizziness
              • Restlessness
              • Tremor
              • Tinnitus
              • Blurred vision

              Rare (serious)

              • Bradyarrhythmia
              • Cardiac arrest
              • Hypotension
              • Excitation
              • Depression
              • Seizure
              • Anaphylaxis
              • Respiratory arrest

              Postmarketing Reports

              Immune system disorders: Hypersensitivity (including urticaria, pruritus, erythema multiforme, angioedema with possible airway obstruction), anaphylaxis

              Injury, poisoning, and procedural complications: Urinary retention postoperative, delayed recovery from anesthesia, anesthetic complication

              General disorders and administration site conditions: Feeling hot, malaise

              Musculoskeletal and connective tissue disorders: Back pain, groin pain, pain in extremity

              Nervous system disorders: Restlessness, paresthesia, dizziness, tremor, seizure, oral paresthesia, oral hypoesthesia, hearing disability, visual disorders, blurred vision, tinnitus, speech disorders, loss of consciousness, peripheral neuropathy, somnolence, unintentional total spinal block, urinary and anal incontinence, perineal disorder and sexual dysfunction, arachnoiditis, akathisia, presyncope, burning sensation, spinal cord injury, cauda equina syndrome, hypoesthesia, dysesthesia, motor dysfunction, myoclonus, phantom pain, headache

              Eye disorders: Diplopia, photophobia

              Cardiac disorders: Bradycardia, tachycardia, arrhythmia, myocardial depression, cardiac arrest

              Psychiatric disorders: Anxiety

              Vascular disorders: Hypertension, hypotension

              Respiratory, thoracic, and mediastinal disorders: Respiratory depression, dyspnea, respiratory arrest

              Gastrointestinal disorders: Nausea, vomiting

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              Warnings

              Contraindications

              Hypersensitivity to para-aminobenzoic acid (PABA) or parabens

              Lumbar and caudal epidural anesthesia should be used with extreme caution in persons with the following conditions: Existing neurological disease, spinal deformities, septicemia, and severe hypertension

              General and specific contraindications to spinal anesthesia regardless of the local anesthetic use, should be taken into account (eg, decompensated cardiac insufficiency, hypovolemic shock, coagulopathy)

              IV regional anesthesia (the anesthetic agent is introduced into the limb and allowed to set in while tourniquets retain the agent within the desired area)

              Serious problems with cardiac conduction

              Local infection at the site of proposed lumbar puncture

              Septicemia

              Cautions

              Local anesthetics should only be administered by clinicians who are well versed in diagnosis and management of dose-related toxicity and other acute emergencies which might arise from the block to be employed, and then only after insuring the immediate availability of oxygen, other resuscitative drugs, cardiopulmonary resuscitative equipment, and the personnel resources needed for proper management of toxic reactions and related emergencies

              Hypotension and bradycardia are well known side effects of all local anesthetics

              Neurological damage may occur after spinal anesthesia, manifesting as paresthesia, loss of sensitivity, motor weakness, paralysis, cauda equina syndrome; occasionally these symptoms persist and can be permanent

              Use extreme caution with lumbar and caudal epidural anesthesia in person with existing neurological disease, spinal deformities, septicemia, severe hypertension, heart block, high grade cardiac decompensation, advanced liver or kidney impairment, elderly patients and patients in poor general condition, genetic cholinesterase deficiency, severe anemia, congenital or acquired bleeding disorder, and patients taking anticoagulants

              Use preservative free preparations for spinal or epidural anesthesia

              DO NOT use solutions with epinephrine in distal areas of body (eg, digit, nose, ear)

              Addition of vasoconstrictor, epinephrine, will promote local hemostasis, decrease systemic absorption, and increase duration of action

              Monitor patient's state of consciousness following the injection; anxiety, dizziness, restlessness, tremors, depression, or blurred vision may be signs of CNS toxicity

              Chondrolysis associated with intra-articular infusions following arthroscopic and other surgical procedures (off-label use)

              Hypersensitivity reactions reported; cross-reactivity among ester-type local anesthetics may occur (see Contraindications)

              Respiratory arrest reported with local anesthetics

              Methemoglobinemia

              • Use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly; patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition
              • Advise patients or caregivers to seek immediate medical attention if patient experiences the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue; discontinue Bicillin C-R and any other oxidizing agents; depending on severity of signs and symptoms, patients may respond to supportive care, including oxygen therapy and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen
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              Pregnancy & Lactation

              Pregnancy

              Data are limited regarding use in pregnant women

              Labor or delivery

              • Local anesthetics appear to cross the placenta by passive diffusion; however, the rate and degree of diffusion varies considerably among the different drugs as governed by: (1) the degree of plasma protein binding, (2) the degree of ionization, and (3) the degree of lipid solubility
              • Fetal/maternal ratios of local anesthetics appear to be inversely related to the degree of plasma protein binding, since only the free, unbound drug is available for placental transfer
              • Spinal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts
              • Sinal anesthesia has also been reported to prolong the second stage of labor by removing the parturient’s reflex urge to bear down or by interfering with motor function
              • Obstetrical anesthesia may increase the need for forceps assistance
              • Maternal hypotension has resulted from regional anesthesia; local anesthetics produce vasodilation by blocking sympathetic nerves
              • Fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable

              Lactation

              Data are not available on the presence of chloroprocaine in human milk, the effects on the breastfed infant, or the effects on milk production

              The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child or from the underlying maternal condition

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Local anesthetics block the generation and conduction of nerve impulses by reducing sodium permeability and increasing action potential threshold

              Pharmacokinetics

              Duration: 30-60 min; the greater the degree of vasodilation produced by the local anesthetic, the faster the rate of absorption & shorter the duration of action

              Protein bound: highly

              Vd: Depends on route of administration

              Onset of action: 6-12 min

              Metabolism: Plasma cholinesterases

              Metabolites: Ester- & amide-type local anesthetics

              Excretion: Urine (principally)

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              Administration

              Preparation

              Clorotekal

              • Ampule should be visually inspected before use; solution that is discolored or contains particulate matter should not be administered
              • Do not heat before use
              • Do not autoclave
              • The medicinal product has to be used immediately after first opening
              • Discard any unused portion in an appropriate manner

              Administration

              Avoid the rapid injection of a large volume of local anesthetic injection through the catheter

              Consider fractional doses, when feasible

              Nesacaine

              • For local anesthesia by infiltration and peripheral nerve blocks
              • Not for subarachnoid administration
              • Not for lumbar and caudal epidural blocks

              Nesacaine MPF

              • For local anesthesia by infiltration, peripheral, and central nerve blocks, including lumbar and caudal epidural blocks
              • Not for subarachnoid administration

              Clorotekal

              • For intrathecal administration for subarachnoid block (spinal anesthesia)
              • Not for epidural use

              Storage

              Store in carton at 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)

              Protect from light

              Do not refrigerate or freeze

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Nesacaine injection
              -
              20 mg/mL (2 %) vial

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              chloroprocaine injection

              NO MONOGRAPH AVAILABLE AT THIS TIME

              USES: Consult your pharmacist.

              HOW TO USE: Consult your pharmacist.

              SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Consult your pharmacist.

              DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: No monograph available at this time.

              MISSED DOSE: Consult your pharmacist.

              STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

              Information last revised July 2016. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

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              • Access your plan list on any device – mobile or desktop.

              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.