articaine/epinephrine

Action and Spectrum

Actions and Spectrum: 

articaine with epinephrine is a commonly used local anesthetic combination in dentistry and specific medical procedures. Here’s an overview of the action and spectrum of articaine and epinephrine: 

• articaine: articaine is a type of amide local anesthetic. It blocks nerve signals in a specific body area, temporarily losing sensation and relieving pain. articaine is unique among local anesthetics because it contains an ester and an amide group in its chemical structure. This allows it to be rapidly metabolized by both plasma esterases and liver amidases, enhancing its effectiveness and providing a relatively short duration of action. 
• epinephrine: epinephrine is a vasoconstrictor and a sympathomimetic agent. When combined with articaine, it serves multiple purposes: 
• Prolongs duration of action: epinephrine is added to the articaine to extend its effect by constricting the blood vessels around the injection site. This reduces blood flow in the area, thereby slowing down the removal of the anesthetic from the site and prolonging its duration of action. 
• Reduces bleeding: epinephrine’s vasoconstrictive properties also help reduce bleeding during dental or surgical procedures by constricting blood vessels, thereby improving the visibility of the surgical field. 
• Enhances anesthesia: epinephrine can enhance the local anesthetic effect of articaine by aiding in the distribution and absorption of the anesthetic, leading to a more profound and longer-lasting numbing effect. 
• Reduces systemic toxicity: epinephrine also helps reduce the systemic absorption of articaine, minimizing the risk of toxic levels of the anesthetic reaching the bloodstream. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Headache 

Pain 

Vomiting 

Gingivitis 

Nausea 

Paresthesia 

Facial edema 

Sleepiness 

Infection 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

The contraindications for using articaine with epinephrine can vary depending on individual factors and medical history. It is key to consult with a healthcare professional or dentist for specific contraindications based on your unique circumstances. However, here are some general contraindications associated with the use of articaine with epinephrine: 

• Hypersensitivity or allergy: Individuals with known hypersensitivity or allergy to articaine, epinephrine, or other local anesthetics should avoid using articaine with epinephrine. 
• Uncontrolled cardiovascular disease: The vasoconstrictive properties of epinephrine can have cardiovascular effects. articaine with epinephrine should be used cautiously or avoided in individuals with severe cardiovascular diseases, such as uncontrolled hypertension (high blood pressure), significant cardiac arrhythmias, or recent myocardial infarction (heart attack). 
• Certain medical conditions: articaine with epinephrine should be used cautiously, or it may be contraindicated in individuals with hyperthyroidism, sulfite sensitivity, severe liver disease, and uncontrolled diabetes. 
• Certain medications: There may be potential drug interactions with medications such as non-selective beta-blockers (e.g., propranolol) or monoamine oxidase inhibitors (MAOIs). These interactions can potentiate the cardiovascular effects of epinephrine, leading to significant changes in heart rate and blood pressure. 
• Pediatric patients: The safety and efficacy of articaine with epinephrine in pediatric patients may vary depending on the specific age group. The dosage and administration should be carefully determined based on the child’s age, weight, and individual needs. 

Caution 

There are essential cautions that should be considered when using this combination. These cautions include: 

• Cardiovascular disease: People with a history of cardiovascular disease, such as angina, congestive heart failure, or arrhythmias, should be closely monitored when receiving articaine with epinephrine. The vasoconstrictive effects of epinephrine can potentially exacerbate these conditions and should be used with caution. 
• Hypertension: Patients with uncontrolled or severe hypertension (high blood pressure) should be carefully monitored when administering articaine with epinephrine. The vasoconstrictive properties of epinephrine can increase blood pressure, and appropriate measures should be taken to manage this effect. 
• Hyperthyroidism: Individuals with hyperthyroidism, a condition characterized by an overactive thyroid gland, might be more sensitive to the cardiovascular effects of epinephrine. Close monitoring is necessary to ensure the patient’s safety. 
• Diabetes: Patients with uncontrolled diabetes should be cautious when receiving articaine with epinephrine due to the potential effects on glucose metabolism. epinephrine can increase blood glucose levels, and adjustments in diabetes management may be necessary. 
• Pregnancy and breastfeeding: The use of articaine with epinephrine during pregnancy and breastfeeding should be carefully evaluated, as there is limited data on the safety of this combination in these populations. The potential risks, benefits should be discussed with a healthcare professional. 
• Elderly population: Elderly individuals may be more susceptible to the cardiovascular effects of epinephrine. Close monitoring and appropriate dose adjustments should be considered in this population. 
• Drug interactions: articaine with epinephrine may interact with certain medications, such as beta-blockers, tricyclic antidepressants, and MAOIs. These interactions can potentiate or diminish the effects of epinephrine or other medications, and caution should be exercised when using these drugs concomitantly. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C 

Lactation:   

Excreted into human milk: No 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

articaine and epinephrine have distinct pharmacological properties contributing to their effects when used together. Here’s an overview of the pharmacology of articaine and epinephrine: 

articaine: 

• articaine is a local anesthetic that works by reversibly inhibiting nerve conduction. It blocks sodium channels in the neuronal membrane, preventing the propagation of action potentials and producing a local anesthetic effect. 
• Onset and duration of action: articaine has a rapid onset of action, typically within a few minutes after administration. It provides a relatively long duration of action due to its metabolism by both plasma esterases and liver amidases. The duration of action can range from 1 to 4 hours, depending on the formulation and dose used. 
• Metabolism and elimination: articaine is metabolized primarily in the liver by amidases, forming articainic acid and other metabolites. These metabolites are then excreted mainly through the kidneys. 

epinephrine (Adrenaline): 

• epinephrine is a sympathomimetic agent that acts on adrenergic receptors. It stimulates both α-adrenergic and β-adrenergic receptors. Activating α1-adrenergic receptors causes vasoconstriction, reducing blood flow and prolonged local anesthesia. Activating β1-adrenergic receptors increases the strength and rate of heart contractions. 
• Vasoconstrictive effects: when combined with local anesthetics like articaine, epinephrine constricts blood vessels in the injection area. This reduces blood flow, delays systemic absorption of the anesthetic, and prolongs the duration of local anesthesia. 
• Reduction of bleeding: epinephrine’s vasoconstrictive properties also help to reduce bleeding during dental or surgical procedures by constricting blood vessels, thereby improving the visibility of the surgical field. 
• Systemic effects: epinephrine can have systemic effects, such as increased heart rate, elevated blood pressure, and stimulation of the central nervous system. These effects are more likely to occur with higher doses or if the drug is inadvertently injected into a blood vessel. 

Pharmacodynamics: 

Mechanism of action: articaine and epinephrine have distinct mechanisms contributing to their effects when used together. Here’s an overview of their mechanisms of action: 

articaine: articaine is a local anesthetic that inhibits nerve conduction, leading to temporary loss of sensation in the targeted area. Its mechanism of action involves blocking sodium channels in neuronal membranes, preventing the propagation of action potentials along nerve fibers. This blockade occurs by binding to specific receptors on the inside of sodium channels, resulting in a decrease in sodium ion influx and the prevention of depolarization necessary for transmitting pain signals. 

articaine has a unique property compared to other local anesthetics because it contains an ester group and an amide group in its structure. Plasma esterases metabolize the ester group, while the amide group undergoes biotransformation in the liver by amidases. This dual metabolism contributes to articaine’s more prolonged duration of action compared to more local anesthetics. 

epinephrine (Adrenaline): epinephrine is a naturally occurring hormone and neurotransmitter that acts as a sympathomimetic agent. Its mechanism of action involves binding to and activating adrenergic receptors throughout the body. epinephrine has both alpha-adrenergic and beta-adrenergic receptor agonist activity. 

• Alpha-adrenergic receptor activation: epinephrine activates alpha-1 adrenergic receptors on smooth muscle cells of blood vessels. This leads to vasoconstriction, which reduces blood flow in the immediate area. The vasoconstrictive effect helps prolong the local anesthetic’s duration by reducing systemic absorption of the drug, decreasing bleeding at the injection site, and enhancing anesthesia. 
• Beta-adrenergic receptor activation: epinephrine also activates beta-1 adrenergic receptors in the heart, leading to increased heart rate (positive chronotropic effect) and increased force of contraction (positive inotropic effect). These effects can affect cardiovascular function and should be considered in patients with cardiovascular disease. 

Additionally, the systemic effects of epinephrine, such as increased heart rate, bronchodilation, and metabolic changes, are mediated through beta-2 adrenergic receptor activation in various tissues. 

When used together, the combination of articaine with epinephrine provides adequate local anesthesia with prolonged duration, reduced bleeding, and enhanced anesthesia due to the vasoconstrictive effects of epinephrine.  

Pharmacokinetics: 

Absorption 

Various routes can administer articaine, including subcutaneous injection, infiltration, and nerve block. After injection, articaine is readily absorbed into the systemic circulation. The rate, extent of absorption depend on factors such as the area’s dose, injection site, and vascularity. 

Various routes, including subcutaneous injection, infiltration, and nerve block can administer epinephrine. When co-administered with articaine, epinephrine is readily absorbed into the systemic circulation. 

Distribution 

articaine is distributed throughout the body after absorption. It has a moderate protein binding (approximately 95%) to plasma proteins such as albumin. The drug can cross the blood-brain barrier, allowing it to exert its local anesthetic effects in the central nervous system. 

epinephrine is distributed widely throughout the body. It can act on α-adrenergic and β-adrenergic receptors in various tissues and organs, including blood vessels, the heart, and the central nervous system. 

Metabolism 

articaine undergoes metabolism primarily in the liver by amidases, forming articainic acid and other metabolites. These metabolites are less potent than articaine itself and are pharmacologically inactive. 

epinephrine undergoes extensive metabolism, mainly in the liver, where it is metabolized by enzymes such as catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). The metabolites of epinephrine include metanephrine and normetanephrine. 

Elimination and Excretion 

The metabolites of articaine, including articainic acid, are primarily excreted through the kidneys. A small amount of unchanged articaine is also excreted in the urine. The elimination half-life of articaine is relatively short, ranging from about 20 to 120 minutes, depending on the dose and formulation. 

The metabolites of epinephrine are primarily excreted through the urine. A small portion may be excreted in the feces. 

Adminstartion

Administration: 

Intraoral submucosal administration 

The administration of articaine with epinephrine should be performed by a trained healthcare professional or dentist familiar with the appropriate techniques and safety considerations. Here are some general guidelines for the administration of articaine with epinephrine: 

• Patient assessment: Before administering articaine with epinephrine, the healthcare professional should conduct a thorough patient assessment, including medical history, allergies, and any contraindications to the medication. Particular attention should be given to cardiovascular health, history of allergic reactions, and medications the patient takes. 
• Proper dosage calculation: The appropriate dosage of articaine and epinephrine should be calculated based on the patient’s age, weight, and the specific procedure being performed. Ensuring the dosage falls within the recommended limits is vital to avoid potential systemic toxicity. 
• Anesthetic technique: The choice of anesthetic technique will depend on the specific procedure and the patient’s needs. articaine with epinephrine can be administered via infiltration (injection near the treatment site) or nerve block (injection near a primary nerve trunk). The healthcare professional should be skilled in the chosen technique and follow proper aseptic measures. 
• Aspiration: Before injecting the solution, it is crucial to perform an aspiration test to ensure that the needle is not intravascular. Aspiration involves pulling back on the syringe plunger to check for the presence of blood. If blood is aspirated, it indicates that the needle is within a blood vessel, and the injection should be repositioned. 
• Slow injection: The articaine with epinephrine solution should be injected slowly to minimize discomfort and potential complications. The injection rate should be controlled, and the healthcare professional should be attentive to the patient’s response. 
• Monitoring and post-administration care: The patient should be monitored for adverse reactions or complications after administering an articaine with epinephrine. Vital signs, such as heart rate, BP, and oxygen saturation, may need to be monitored during and after the procedure. Appropriate post-administration care should be provided, including patient education on post-procedure instructions and potential side effects. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: articaine/epinephrine 

Pronounced: [ AR-ti-kane-and-EP-i-NEF-rin ] 

Why do we use articaine/epinephrine? 

articaine with epinephrine is a local anesthetic combination commonly used in dental and oral surgical procedures. Certain common uses of articaine with epinephrine: 

• Dental procedures: articaine with epinephrine is widely used in dental procedures to provide local anesthesia and numbness in the oral cavity. It is commonly used for dental fillings, extractions, root canals, periodontal treatments, and implant placement. 
• Oral surgery: articaine with epinephrine is also used in oral surgical procedures, including tooth extractions (simple and surgical), wisdom tooth removal, and biopsy of oral tissues. The combination of articaine and epinephrine helps to provide profound anesthesia and minimize bleeding during these procedures. 
• Endodontic procedures: Endodontic treatments, such as root canal therapy, often involve using articaine with epinephrine. The local anesthetic helps to numb the affected tooth and the surrounding tissues, allowing the dentist to perform the procedure comfortably and painlessly. 
• Periodontal procedures: In periodontal treatments, which involve the treatment of gum diseases, articaine with epinephrine may be used to provide anesthesia for deep cleanings (scaling and root planing), periodontal surgery, or gum grafting procedures. 
• Maxillofacial procedures: articaine with epinephrine can also be used in specific maxillofacial procedures, such as jaw surgery, facial trauma repair, or the placement of dental implants.