mepivacaine

Action and Spectrum

Actions and spectrum: 

mepivacaine is a local anesthetic that belongs to the amide group of anesthetics. It is used for infiltration, nerve block, and epidural anesthesia. mepivacaine works by blocking sodium channels, thereby preventing nerve impulses from transmitting pain signals to the brain.

It has a fast onset of action and a moderate duration of action, making it suitable for short to intermediate duration procedures. mepivacaine is effective for both sensory and motor nerve blockade and has a lower cardiotoxicity compared to other local anesthetics like bupivacaine.

It is often used in dental procedures, obstetrics, and for postoperative pain relief. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Systemic dose-related toxicity 

• Hypotension 
• Systemic diseases 
• apnea 
• Acidosis 
• Urticaria 
• erythema 
• pruritus 
• excessive sweating 
• Nausea 
• Backache 
• vomiting 
• Urinary retention 
• Sneezing 
• fecal/urinary incontinence 
• respiratory paralysis 
• Loss of perineal sensation 
• Anaphylactoid symptoms 
• Slowing of labor 
• Angioneurotic edema   
• depression of the myocardium 
• heart block 
• Bradycardia 
• possibly cardiac arrest 
• Syncope 
• decreased cardiac output 
• Hypotension 
• ventricular arrhythmias 
• Excitation or depression 
• Anxiety 
• Tinnitus 
• Tremors 
• constriction of the pupils 
• paralysis of consciousness 
• paresthesia 
• septic meningitis 
• cranial nerve palsies 
• Restlessness 
• Dizziness 
• blurred vision 
• Chills 
• elevated temperature 
• persistent anesthesia 
• Weakness 
• Headache 
• meningismus 

Black Box Warning

Black Box Warning:  

There are no black box warnings associated with the use of mepivacaine. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity to mepivacaine or any of its components 
• Severe shock or heart block 
• Known sensitivity to other amide-type local anesthetics 
• Intravenous regional anesthesia (Bier block anesthesia)

Caution: 

• Allergy: Patients who are allergic to amide-type local anesthetics should not use mepivacaine. 
• Cardiovascular disease: mepivacaine can cause adverse cardiovascular effects, including hypotension and cardiac arrest. It should be used under caution in patients having cardiovascular disease or those who are hemodynamically unstable. 
• Hepatic or renal impairment: mepivacaine is metabolized in the liver and excreted by the kidneys. Patients with severe hepatic or renal impairment may have difficulty metabolizing and eliminating mepivacaine, which may increase the risk of toxicity. 
• Pregnancy and breastfeeding: mepivacaine should be used with caution in pregnant and breastfeeding women, as its effects on the fetus or infant are not well understood. 
• Neurological disorders: mepivacaine should be used with caution in patients with neurological disorders, as it can cause neurotoxicity, including nerve damage and seizures. 
• Elderly patients: Elderly patients may be more sensitive to the effects of mepivacaine and may require lower doses or more frequent monitoring. 
• Drug interactions: mepivacaine can interact with other medications, including beta-blockers, calcium channel blockers, and other local anesthetics. Patients taking these medications may require dosage adjustments or more frequent monitoring.

Comorbidities: 

mepivacaine is a local anesthetic medication that is safe and well-tolerated. However, caution should be exercised when administering the drug to patients with certain medical conditions. 

Patients with severe liver or kidney disease may be at an increased risk of developing toxic levels of mepivacaine in their blood, and the dosage of the drug may need to be adjusted accordingly. Additionally, patients with a history of drug allergies or hypersensitivity should be closely monitored during treatment with mepivacaine. 

Patients with cardiac disease or a history of heart rhythm problems, including long QT syndrome, may also be at an increased risk of adverse reactions to mepivacaine, including arrhythmias. The drug should be used under caution in these patients and only under close medical supervision. 

Finally, patients with a history of seizures or epilepsy should be closely monitored during treatment with mepivacaine, as the drug can lower the seizure threshold and potentially trigger seizures. 

Pregnancy / Lactation

Pregnancy consideration: Pregnancy Category C 

Lactation: safety and efficacy not established  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

mepivacaine is a local anesthetic with a short to intermediate duration of action. It works by blocking sodium channels in nerve fibers, preventing the initiation and transmission of nerve impulses, leading to a temporary loss of sensation in the affected area. mepivacaine is an aminoamide type of local anesthetic and is similar in structure and action to lidocaine. 

mepivacaine has a pKa of 7.6 and is mostly in the ionized form at physiologic pH, which allows it to remain in the extracellular fluid and not readily penetrate cell membranes. This characteristic results in a slower onset of action compared to lidocaine. mepivacaine is metabolized in the liver by hydrolysis of the amide linkage, and the metabolites are excreted in the urine.  

Pharmacodynamics: 

mepivacaine is a local anesthetic that blocks the generation and conduction of nerve impulses by reducing the permeability of sodium ions through the cell membrane. This action is achieved by binding to specific receptors on the sodium channels in nerve membranes, which leads to the inhibition of the sodium influx necessary for the initiation and conduction of impulses. mepivacaine is a type of amide local anesthetic, and it has a rapid onset and intermediate duration of action. Its potency is like that of lidocaine, but it has a longer duration of action.  

Pharmacokinetics: 

Absorption 

mepivacaine is rapidly absorbed from injection sites, with peak plasma concentrations occurring within 30-45 minutes after injection. The rate of absorption depends on the dose, route of administration, and vascularity of the injection site. 

Distribution 

mepivacaine is rapidly distributed to tissues, with a large volume of distribution. It is highly protein-bound, primarily to alpha-1 acid glycoprotein. 

Metabolism 

mepivacaine undergoes hepatic metabolism via the cytochrome P450 system. It is primarily metabolized to pipecolylxylidide, which is then further metabolized to 2,6-xylidine. 

Elimination and excretion 

mepivacaine and its metabolites are primarily excreted in the urine, with a half-life of approximately 1.9 hours. The clearance of mepivacaine is dependent on liver function, and the drug may accumulate in patients with hepatic impairment. 

Adminstartion

Administration: 

mepivacaine is administered as a local anesthetic through injection. The specific dosage and administration technique will vary depending on the intended use and the patient’s individual needs. In general, mepivacaine is administered slowly and carefully to ensure that the anesthetic effect is achieved without causing any unnecessary discomfort or complications.

The injection is typically given directly into the area where the anesthetic is needed, such as the gums, mouth, or skin. The dose and frequency of administration will be determined by the healthcare provider based on the patient’s medical history, current health status, and other factors.

It is important to follow the healthcare provider’s instructions carefully when using mepivacaine to minimize the risk of adverse effects. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: mepivacaine 

Pronounced: [ me-PIV-a-kane ]  

Why do we use mepivacaine? 

mepivacaine is a local anesthetic that is primarily used for regional anesthesia, including epidural and nerve block anesthesia, for surgery and acute pain management. It is also used for local infiltration anesthesia for minor surgical procedures and dental procedures.

mepivacaine is often preferred for dental procedures due to its rapid onset and intermediate duration of action. It may also be used for the treatment of certain types of chronic pain, such as neuropathic pain, although its use for chronic pain is less common.