Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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)
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
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
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.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)
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
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Nesacaine injection - | 20 mg/mL (2 %) vial |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
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) 2023 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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