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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Nesacaine
Generic Name
Chloroprocaine Hydrochloride
Active Ingredient
ChloroprocaineCategory
Other
Salt Form
Hydrochloride
Variants
4
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Nesacaine, you must consult a qualified healthcare professional.
| 63323-478 |
| 20 mg/mL | INJECTION, SOLUTION | INFILTRATION, PERINEURAL | 63323-476 |
Detailed information about Nesacaine
Chloroprocaine is a short-acting ester-type local anesthetic used for infiltration, nerve blocks, and epidural anesthesia. It is known for its rapid onset and low systemic toxicity profile.
The dosage of chloroprocaine varies significantly based on the anesthetic procedure, the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked, and the individual patient's tolerance. Healthcare providers aim to use the lowest dosage required to achieve the desired effect.
Chloroprocaine is not frequently used in pediatric patients, and its safety and effectiveness in children have not been extensively established through large-scale clinical trials. When used, dosages must be meticulously calculated based on the child's weight and physical condition. Most clinicians prefer amide-type anesthetics for pediatric regional blocks due to more robust clinical data. For infiltration in children, a maximum dose of 11 mg/kg is generally suggested as a guideline, but this must be individualized by a pediatric anesthesiologist.
While chloroprocaine is metabolized in the plasma, its metabolites are excreted by the kidneys. In patients with severe renal disease or end-stage renal failure, there is a theoretical risk of metabolite accumulation (specifically PABA). However, because the parent drug is cleared so rapidly, significant dose adjustments are rarely required for single-dose procedures. Caution is advised in patients with uremia.
Since chloroprocaine metabolism is independent of liver function (occurring via plasma cholinesterase), it is often considered a safer alternative to lidocaine for patients with liver cirrhosis or hepatic failure. No specific dose adjustment is typically required, though the patient's overall clinical status (such as protein levels and coagulation) must be considered.
Geriatric patients may have reduced physiological reserves and a higher prevalence of cardiovascular disease. While the metabolism of chloroprocaine remains rapid, elderly patients may be more sensitive to the hypotensive effects of epidural anesthesia. Lower volumes and slower administration rates are often recommended to prevent sudden changes in blood pressure.
Chloroprocaine is administered exclusively by healthcare professionals (anesthesiologists, CRNAs, or surgeons) in a clinical or hospital setting. It is not for self-administration.
As chloroprocaine is administered by a healthcare provider for a specific procedure, the concept of a 'missed dose' in the traditional sense does not apply. If the anesthesia wears off before the procedure is finished, the provider may administer additional doses based on clinical need.
An overdose of chloroprocaine can lead to Local Anesthetic Systemic Toxicity (LAST). This usually occurs due to accidental injection into a blood vessel rather than an excessive total dose.
> Important: Follow your healthcare provider's dosing instructions. Do not attempt to adjust or request specific doses without a thorough medical consultation regarding your surgical needs.
Side effects of chloroprocaine are often related to the technique of administration rather than the drug itself. When used for epidural anesthesia, the most common side effects include:
Chloroprocaine is a potent medication that must only be administered by clinicians trained in the management of local anesthetic toxicity and regional anesthesia techniques. The primary safety concern is the prevention of accidental intravascular injection, which can lead to rapid systemic toxicity. Facilities where chloroprocaine is used must have immediate access to resuscitative equipment, including oxygen, IV fluids, anticonvulsants, and lipid emulsion therapy.
There are no FDA black box warnings for Chloroprocaine. However, it is critical to distinguish between Nesacaine (containing preservatives) and Nesacaine-MPF (Methylparaben Free). Using the wrong formulation for spinal or epidural blocks can result in permanent neurological injury.
Chloroprocaine must NEVER be used in the following circumstances:
Chloroprocaine is classified as FDA Pregnancy Category C. This means that animal reproduction studies have not been conducted, and it is not known whether chloroprocaine can cause fetal harm when administered to a pregnant woman. However, chloroprocaine is widely used in clinical practice for obstetric anesthesia (epidurals for labor or C-sections). Its primary advantage in pregnancy is its rapid metabolism; it is broken down so quickly in the mother's blood that very little of the drug reaches the fetus. This makes it one of the safest options for the baby when a rapid anesthetic block is needed. It is not known to affect fertility.
It is not known whether chloroprocaine is excreted in human milk. However, because the drug has an extremely short half-life (seconds to minutes) and is rapidly hydrolyzed into inactive metabolites, it is highly unlikely that any significant amount of the drug would reach the nursing infant through breast milk. Most clinicians consider it safe to resume breastfeeding once the mother has recovered from the effects of anesthesia and is feeling well enough to hold the baby.
Safety and effectiveness in pediatric patients below the age of 12 have not been established. While it may be used off-label by pediatric anesthesiologists for specific procedures, it is not the standard of care for most pediatric regional blocks. The risk of systemic toxicity is a primary concern in smaller children, and weight-based dosing must be strictly followed.
Chloroprocaine is an ester-type local anesthetic. Its primary mechanism of action involves the reversible blockade of sodium channels on the internal surface of nerve cell membranes. By binding to these channels, chloroprocaine prevents the influx of sodium ions ($Na^+$) into the cell, which is the essential step for the generation and propagation of an action potential. When the action potential is inhibited, the nerve cannot transmit sensory information (pain, touch, temperature) or motor commands. The addition of a chlorine atom to the benzene ring of the procaine molecule increases its lipid solubility and enhances its potency compared to the parent compound.
Common questions about Nesacaine
Chloroprocaine is a short-acting local anesthetic used primarily to provide numbing for surgical procedures. It is commonly used for local infiltration to numb a small area of skin, for peripheral nerve blocks to numb a limb, and for epidural anesthesia, especially in obstetrics. Because it works very quickly and wears off fast, it is ideal for short surgeries or for procedures where the doctor needs the patient to regain feeling quickly. It is often used for emergency C-sections when rapid anesthesia is required for the safety of the mother and baby. Your doctor will choose the concentration and volume based on the specific type of surgery you are having.
The most common side effects of chloroprocaine, particularly when given as an epidural, include a drop in blood pressure (hypotension), nausea, and vomiting. Some patients may also experience a mild backache or soreness at the site of the injection. Because it is a short-acting drug, these effects usually resolve quickly as the medication is metabolized by the body. In some cases, patients might feel a temporary 'pins and needles' sensation as the numbness wears off. Most side effects are manageable with IV fluids or minor medications provided by your medical team during the procedure.
You should not drink alcohol for at least 24 hours after receiving chloroprocaine. While chloroprocaine itself leaves your system very quickly, it is almost always used during a surgical procedure where other medications, such as sedatives or pain relievers, may also be given. Alcohol can interact with these other drugs, leading to excessive drowsiness, dizziness, or a dangerous drop in blood pressure. Additionally, alcohol can interfere with your recovery from surgery and may cause dehydration. Always follow the specific post-operative instructions provided by your surgeon or anesthesiologist regarding diet and alcohol consumption.
Chloroprocaine is frequently used during pregnancy and is considered one of the safer local anesthetics for obstetric use. Its main advantage is that it is broken down by enzymes in the mother's blood so rapidly that very little of the drug ever reaches the baby. This reduces the risk of the baby experiencing any drug-related side effects after birth. It is commonly used for epidurals during labor and for both elective and emergency cesarean sections. However, like all medications during pregnancy, it should only be used when clearly needed. Your anesthesiologist will discuss the risks and benefits with you based on your specific clinical situation.
Chloroprocaine is known for its exceptionally fast onset of action. Depending on the type of block and the concentration used, it typically begins to work within 6 to 12 minutes. For local skin infiltration, the numbing effect is almost immediate. This rapid onset makes it a preferred choice in emergency situations, such as an urgent C-section, where every minute counts. The full effect of the anesthesia usually lasts between 30 and 60 minutes, which is shorter than many other local anesthetics like lidocaine or bupivacaine. This allows for a faster recovery time once the procedure is finished.
Chloroprocaine is not a medication that you 'take' on a regular schedule; it is a one-time injection administered by a healthcare professional for a specific procedure. Therefore, there is no need to worry about stopping it suddenly or experiencing withdrawal symptoms. The medication is naturally and very rapidly cleared from your body by enzymes in your blood. The numbing effect will naturally wear off within about an hour of the last dose. If you are concerned about the return of pain after the anesthetic wears off, your doctor will provide a plan for post-operative pain management using other types of medications.
Since chloroprocaine is only administered by healthcare professionals in a hospital or clinic setting for a procedure, you cannot miss a dose in the way you might miss a daily pill. The anesthesiologist or surgeon will determine the exact timing and amount of the drug you need during your surgery. If the procedure lasts longer than expected and the numbing begins to wear off, the medical team will simply administer more of the drug or switch to a different type of anesthesia. You do not need to keep track of the dosing yourself; your medical team will monitor your comfort level throughout the process.
No, chloroprocaine does not cause weight gain. It is a short-acting anesthetic used for a single procedure and is cleared from the body within minutes. Weight gain is typically a side effect associated with medications taken over a long period, such as certain steroids, antidepressants, or hormonal treatments. Since chloroprocaine does not affect your metabolism, appetite, or water retention in the long term, it has no impact on your body weight. Any temporary swelling you might notice after surgery is likely due to IV fluids or the surgical procedure itself, not the chloroprocaine.
Chloroprocaine can interact with certain other medications, so it is vital to give your doctor a full list of what you take. It can interfere with the effectiveness of 'sulfa' antibiotics (sulfonamides) because of how it is broken down in the body. It may also have increased risks if you are taking medications for myasthenia gravis or certain heart rhythm drugs. However, it is very commonly and safely used alongside other surgical medications like IV sedatives, oxygen, and post-operative pain killers. Your anesthesiologist is trained to manage these interactions and will adjust your care plan to ensure your safety during the procedure.
Yes, chloroprocaine hydrochloride is available as a generic injectable solution. It has been available for many decades, and several manufacturers produce it. It is also sold under brand names such as Nesacaine and Nesacaine-MPF. The 'MPF' stands for Methylparaben Free, which is the version used for epidural and spinal injections to ensure safety. Because it is a generic medication, it is generally cost-effective for hospitals and surgical centers to use. Regardless of whether the brand name or generic version is used, the active ingredient and its numbing effects remain the same.
Other drugs with the same active ingredient (Chloroprocaine)
> Warning: Inform your medical team immediately if you experience any of the following during or shortly after receiving chloroprocaine.
Chloroprocaine is designed for short-term use, and long-term side effects are extremely rare. Historically, there were concerns regarding 'Cauda Equina Syndrome' (permanent nerve damage) when large volumes of chloroprocaine with preservatives (sodium bisulfite) were accidentally injected into the spinal space. Modern preservative-free (MPF) formulations have largely eliminated this risk. Most patients recover full sensation and motor function within 60 to 90 minutes of the drug's administration.
No FDA black box warnings currently exist for Chloroprocaine. However, the FDA requires strict labeling regarding the use of preservative-free vs. preservative-containing vials. Vials containing preservatives (like methylparaben) MUST NOT be used for epidural or spinal anesthesia, as these additives are neurotoxic when placed in the space surrounding the spinal cord.
Report any unusual symptoms to your healthcare provider. Even minor symptoms like a persistent headache or localized tingling should be discussed with your anesthesiologist during your post-operative follow-up.
During the administration of chloroprocaine, the following monitoring is mandatory:
Patients should not drive or operate heavy machinery for at least 24 hours after receiving chloroprocaine. Even though the drug wears off quickly, the residual effects of the procedure, other surgical medications, and the stress of surgery can impair coordination and judgment. Always ensure you have a responsible adult to drive you home after an outpatient procedure.
Alcohol should be avoided for at least 24 hours following the administration of chloroprocaine. Alcohol can enhance the sedative effects of any other medications given during surgery and can contribute to dehydration and low blood pressure, complicating the recovery from anesthesia.
As chloroprocaine is a single-use anesthetic for a procedure, there is no tapering requirement. However, patients should be monitored until full sensation and motor function return to the affected area. If numbness persists significantly longer than 2 hours, the healthcare provider should be notified.
> Important: Discuss all your medical conditions, especially any history of 'bad reactions' to numbing medicine or a family history of enzyme deficiencies, with your healthcare provider before starting Chloroprocaine.
There are no known direct interactions between chloroprocaine and specific foods. However, patients undergoing surgery are typically required to fast (NPO status) for several hours prior to the procedure to prevent aspiration. Following the procedure, a light meal is usually recommended once the patient is fully awake and nausea has subsided.
Chloroprocaine does not typically interfere with standard blood chemistry or hematology tests. However, its metabolite PABA can interfere with certain specialized tests for pancreatic function (the bentiromide test). Patients should inform their doctor if they have had anesthesia within 24 hours of such a test.
For each major interaction, the management strategy involves:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter pain relievers and vitamins.
In these situations, the healthcare provider will perform a careful risk-benefit analysis:
Patients should be aware that cross-sensitivity is common among ester-type anesthetics. However, there is generally NO cross-sensitivity between ester anesthetics (like chloroprocaine) and amide anesthetics (like lidocaine or ropivacaine). If you are allergic to one class, the other class is usually a safe alternative, provided the allergy is confirmed by a specialist.
> Important: Your healthcare provider will evaluate your complete medical history, including any previous reactions to dental numbing or surgical anesthesia, before prescribing Chloroprocaine.
Clinical studies of chloroprocaine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range. This reflects the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Elderly patients may be more prone to the blood-pressure-lowering effects of the drug.
Metabolites of chloroprocaine are excreted by the kidneys. While the parent drug is cleared by the blood, patients with severe renal impairment (GFR < 30 mL/min) should be monitored for signs of metabolite toxicity, although this is rarely clinically significant for one-time procedures. No specific dose adjustment is usually required for a single dose.
Chloroprocaine is a preferred anesthetic for patients with liver disease because its metabolism does not rely on the liver. Unlike lidocaine, which can accumulate in patients with cirrhosis, chloroprocaine is cleared just as quickly in patients with liver failure as it is in healthy individuals, provided their plasma cholinesterase levels are within a reasonable range.
> Important: Special populations require individualized medical assessment. Always inform your anesthesiologist if you are pregnant, nursing, or have any chronic kidney or liver conditions.
| Parameter | Value |
|---|---|
| Bioavailability | N/A (Administered locally/regionally) |
| Protein Binding | Low (<10%) |
| Half-life | 20 - 25 seconds (Adults); ~45 seconds (Neonates) |
| Tmax | 1 - 5 minutes (depending on site) |
| Metabolism | Rapid hydrolysis by plasma pseudocholinesterase |
| Excretion | Renal (as metabolites PABA and diethylaminoethanol) |
Chloroprocaine belongs to the Ester Local Anesthetic class. It is grouped with other esters such as procaine (Novocain), tetracaine (Pontocaine), and benzocaine. It is distinct from the Amide Local Anesthetic class, which includes lidocaine, bupivacaine, and ropivacaine. The primary difference between these classes is the chemical linkage and the site of metabolism (plasma for esters vs. liver for amides).