Local Anesthetic
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Local anesthetics are indispensable tools in dental and medical practice for managing pain during procedures. Their primary mechanism is to block sodium channels in nerve membranes, thereby inhibiting the propagation of pain signals. For the INBDE, understanding the classification, metabolism, and clinical significance of local anesthetics is crucial.
AMIDES AND ESTERS
Local anesthetics are broadly classified into two categories based on their molecular structure and metabolism: amides and esters. The distinction between these two groups is critical for understanding their pharmacokinetics, clinical application, and potential for adverse effects.
Amides are metabolized in the liver by hepatic enzymes (cytochrome P450) and are generally associated with lower allergenic potential. Amides are less allergenic and more stable in solution, which makes them the go-to choice for most dental procedures. Amide toxicity risks increase in patients with liver dysfunction. Examples include:
- Lidocaine (Xylocaine)
- Bupivacaine (Marcaine)
- Mepivacaine (Carbocaine)
- Articaine (Septocaine)
- Prilocaine (Citanest)
Esters are metabolized in the blood plasma by an enzyme called pseudocholinesterase. Though effective, they are less commonly used due to their allergenic potential (due to a byproduct called para-aminobenzoic acid (PABA)) and shorter duration of action. Esters are rapidly metabolized in plasma. Toxicity is often related to pseudocholinesterase deficiencies or allergic reactions.
Examples include:
- Procaine (Novocaine)
- Cocaine
- Tetracaine
- Benzocaine (commonly used as a topical anesthetic)
Articaine is unique because it has both amide and ester characteristics, allowing it to be metabolized in both the liver and plasma. A simple way to differentiate amides from esters is by their names. Amides contain an “i” before “-caine” (e.g., lidocaine, bupivacaine).Esters: Do not contain an “i” before “-caine” (e.g., procaine, tetracaine).
PROPERTIES OF LOCAL ANESTHETICS
Local anesthetics are critical for pain management during dental and medical procedures. Their effectiveness depends on their ability to block sodium channels in nerve cells, which prevents the transmission of pain signals. Local anesthetics block voltage-gated sodium channels in nerve membranes. Sodium channels are essential for nerve depolarization, a process that allows the transmission of pain signals to the brain.
By preventing sodium influx, local anesthetics halt the propagation of the nerve impulse, effectively numbing the area. Local anesthetics bind to sodium channels from inside the nerve cell membrane.
This means the drug must penetrate the nerve membrane to reach its target. Local anesthetics exist in two forms: ionized (charged) and non-ionized (uncharged). The non-ionized form is lipid-soluble, enabling it to cross the fatty nerve membrane. Once inside the nerve, the drug changes to its ionized form, which binds to the sodium channel and blocks it. The pKa of a drug determines the proportion of the non-ionized form available. Drugs with a lower pKa have a faster onset of action because more of the drug is in the non-ionized form at physiological pH.
The environment’s pH affects the drug’s ability to penetrate the nerve membrane. In inflamed or infected tissue, which is acidic, there are fewer non-ionized molecules available to cross the membrane. As a result, local anesthetics are less effective in inflamed or infected tissue.If local anesthetics are ineffective in inflamed areas, alternative strategies such as nerve blocks may be necessary.
For full anesthesia to occur, local anesthetics must block at least three consecutive Nodes of Ranvier along a nerve. The more of the nerve length exposed to the anesthetic, the better the chance of achieving profound anesthesia.
Local anesthetics are absorbed into tissues and must cross the nerve membrane to take effect. Absorption depends on tissue vascularity and the drug’s lipid solubility. Increased blood flow at the injection site reduces the duration of the anesthetic, as the drug is carried away faster. Vasoconstrictors, such as epinephrine, are added to local anesthetic solutions to prolong their duration by reducing blood flow. Higher lipid solubility enhances potency and duration of action because the drug penetrates the nerve membrane more easily. Drugs with higher protein-binding capacity remain attached to receptors longer, increasing the duration of action.
Common vasoconstrictor ratios include 1:100,000 epinephrine, which prolongs anesthesia and reduces systemic toxicity. The choice of anesthetic depends on the required duration, potency, and the patient’s medical history.
INJECTION TECHNIQUES
Administering local anesthetics effectively is a critical skill in dentistry, as it ensures patient comfort and procedural success. The goal of any injection is to deliver the anesthetic to the appropriate nerve or tissue while minimizing discomfort and maximizing efficacy.
Infiltration injections are used to anesthetize a small, localized area, typically a single tooth and its surrounding soft tissue. This technique is most effective in the maxilla due to the thin cortical bone, which allows the anesthetic to diffuse easily to the nerve endings. For example, a local infiltration near the apex of a maxillary central incisor can provide profound anesthesia for restorative work on that tooth.
Nerve blocks target larger areas by anesthetizing the main nerve trunk before it branches into smaller nerves. These injections are commonly used in the mandible, where the dense cortical bone makes infiltration less effective. Examples include the inferior alveolar nerve block (IAN block), which anesthetizes all mandibular teeth in one quadrant, and the posterior superior alveolar (PSA) block, which anesthetizes the maxillary molars.
Successful administration of local anesthetics requires a thorough understanding of anatomical landmarks. Below are some of the most commonly used injections and their associated landmarks.
Inferior Alveolar Nerve (IAN) Block is used to anesthetize all mandibular teeth in one quadrant, as well as the buccal soft tissue anterior to the molars.
- Landmarks:
- The coronoid notch, the deepest concavity on the anterior border of the mandibular ramus.
- The pterygomandibular raphe, a fibrous band of tissue that serves as a guide for needle insertion.
- The mandibular occlusal plane, which helps determine the height of the injection.
- Technique:
- The needle is inserted approximately 1.5 cm above the occlusal plane, lateral to the pterygomandibular raphe.
- Advance the needle until bone is contacted (usually 20-25 mm deep), withdraw slightly, aspirate to ensure the needle is not in a blood vessel, and inject slowly.
Posterior Superior Alveolar (PSA) Block is used to anesthetize the maxillary molars, except for the mesiobuccal root of the first molar in some cases.
- Landmarks:
- The zygomatic process of the maxilla.
- The mucobuccal fold above the maxillary second molar.
- Technique:
- The needle is inserted at a 45-degree angle to the occlusal plane and advanced approximately 16 mm into the tissue.
- Aspiration is critical to avoid injecting into the pterygoid venous plexus, which can lead to a hematoma.
Mental Nerve Block is used to anesthetize the buccal soft tissue from the mandibular premolars to the midline.
- Landmarks:
- The mental foramen, located near the apices of the mandibular premolars.
- Technique:
- Palpate the mental foramen and insert the needle anterior to it. Aspirate and inject slowly.
Greater Palatine Nerve Block is used to anesthetize the posterior hard palate from the maxillary third molar to the first premolar.
- Landmarks:
- The greater palatine foramen, located near the junction of the maxillary alveolar process and the hard palate, typically opposite the second molar.
- Technique:
- Apply pressure with a cotton tip applicator to the foramen before injecting to minimize discomfort.
Nasopalatine Nerve Block is used to anesthetize the anterior hard palate from canine to canine.
- Landmarks:
- The incisive papilla, located at the midline of the palate behind the maxillary central incisors.
- Technique:
- Insert the needle at the base of the incisive papilla and inject slowly.
Canine (Infraorbital) Block is used to anesthetize the maxillary central and lateral incisors, canines, and sometimes the premolars, along with their associated buccal soft tissues.
- Landmarks:
- The infraorbital foramen, located below the orbit and above the maxillary first premolar.
- The mucobuccal fold at the level of the first premolar.
- Technique:
- Palpate the infraorbital foramen to locate its position.
- Insert the needle into the mucobuccal fold over the maxillary first premolar. Angle the needle toward the infraorbital foramen and advance it approximately 16 mm.
- Aspirate and inject slowly.
Gow-Gates nerve block is used to anesthetize the mandibular nerve and its branches, providing profound and widespread anesthesia to the mandibular quadrant. Unlike the inferior alveolar nerve (IAN) block, which is limited in scope and has a higher failure rate, the Gow-Gates technique is designed to deliver anesthesia to a larger area, including the inferior alveolar nerve, lingual nerve, buccal nerve, mylohyoid nerve, auriculotemporal nerve, and mental nerve.
- Landmarks
- Tragus of the Ear: Serves as a reference for the posterior positioning of the condyle.
- Corner of the Mouth: The syringe is aligned from the contralateral corner of the mouth for proper angulation.
- Neck of the Mandibular Condyle: The target area, where the mandibular nerve exits the foramen ovale after branching from the trigeminal nerve (V3).
- Intertragic Notch: Used for vertical alignment of the syringe.
- Technique
- Patients must open their mouths wide to fully translate the mandibular condyle forward. This movement creates better access to the target area.
- The injection is administered at the height of the mesiolingual cusp of the maxillary second molar. The needle passes through the buccal mucosa and soft tissues to reach the neck of the condyle.
- Insert the needle at the height of the mesiolingual cusp of the maxillary second molar, directing it toward the neck of the condyle.
- The syringe should be aligned parallel to an imaginary line between the corner of the patient’s mouth and the intertragic notch of the ear.
- Advance the needle slowly until it contacts bone at the condylar neck (approximately 25 mm deep for most patients).
- Once bone is contacted, withdraw the needle slightly (1-2 mm) to avoid injecting into the periosteum.
- Aspiration is crucial to avoid intravascular injection, as the pterygoid venous plexus is in close proximity.
Even with proper technique, complications can arise during or after the administration of local anesthetics. These may include
- Pain During Injection – caused by rapid injection, poor technique, or failure to use a topical anesthetic. Always inject slowly (1 cartridge per minute) and use a topical anesthetic to numb the surface tissue before needle insertion.
- Hematoma Formation – caused by accidental puncture of a blood vessel, particularly during PSA or IAN blocks. Apply pressure and ice to the area immediately. Avoid further injections in the same site until the hematoma resolves.
- Trismus – caused by trauma to the muscles of mastication or the temporomandibular joint during injection. Advise the patient to apply warm compresses and perform gentle jaw exercises.
- Paresthesia – caused by trauma to the nerve during injection or contamination of the anesthetic solution. Reassure the patient that most cases resolve spontaneously within a few weeks. If symptoms persist, refer to a specialist.
- Inadequate Anesthesia – caused by incorrect needle placement, insufficient anesthetic volume, or anatomical variations. Reassess landmarks and technique, and consider using a supplemental injection, such as a periodontal ligament (PDL) injection.