Pharmacology of Local Anesthetics PDF
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Faculty of Medicine and Health Sciences, Department of Dentistry and Dental Surgery
2023
Dr. Thikrayat Yahya
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Summary
This document provides a lecture outline on the pharmacology of local anesthetics, focusing on their use in dentistry. It covers definitions, indications, properties, classifications, mechanisms of action, pharmacokinetics, and dosage calculations. Key topics include the different types of local anesthetics, their properties, and how they work in blocking nerve conduction.
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& :ja ** Pharmacology of Local Anesthestics Faculty Of Medicine and Health Sciences Department Of Dentistry and Dental Surgery Dr. Thikrayat Yahya g...
& :ja ** Pharmacology of Local Anesthestics Faculty Of Medicine and Health Sciences Department Of Dentistry and Dental Surgery Dr. Thikrayat Yahya g DDS, ID MSc. First Semester 2023-2024 [ "122 = + +4) 4 Pharmacology of Local Anesthetics Lecture Outline Definition of anesthesia and local anesthetics. Indications of local anesthesia Properties of an ideal local anesthetic Classification of local anesthetics Physiochemical properties of local anesthetic molecules Mode of action of local anesthetic drugs Theories of local anesthetics mode of action Pharmacokinetics of local anesthetics Components of local anesthetic cartridge Dosage calculation of local anesthesia in dentistry Systemic Actions of Local Anesthetics Contraindications of local anesthesia Advantages of L.A over G.A in dentistry Preparations and dosage of Some local anesthetics Intended Lecture Outcomes After completing this lecture on the pharmacology of local anesthesia, students are expected to: Have a comprehensive understanding of different local anesthetic agents commonly used in dentistry. Be familiar with the pharmacokinetics of local anesthetics Be able to explain how local anesthetic agents work at the cellular level, particularly their role in blocking nerve conduction and preventing pain sensation Explain theories of anesthetic agents mechanism of action. Have a strong grasp of safe dosage ranges for local anesthetic agents and understand how to calculate and administer appropriate doses based on the patient's age, weight, and medical history. Be aware of potential adverse effects and complications associated with local anesthesia ? 98 Anesthesia - V in * E" /&1 jjj D Types of Anesthesia jey s is ASA defines the following types of anesthesia: major surgeries( is op5 juji 3 General Regional & -; 8% T i anesthesia anesthesia is is block is S 245555551 : & deep sleep51 : sedation Monitored Local > - - 1 /15 85 5 Jij I sedation anesthesia je ⑤ minimally invasive procedure (+ (1155- Local Anesthetics &"Y 1 sli nerve conduction &zoilagents / Sis Local Anesthetics : (N gi Defined as : Agents that reversibly block nerve conduction when applied to a circumscribed area of the body. Ap inhibition nociceptive N S fibers )4 : 5 dg1 CNS & Pain impulse /11992% Wils /12 Y (15) 1 - : Note * &"X10 Indications of Local Anesthesia: Injectable anesthesia indications: Elimination of pain during various dental procedures :Conservative dentistry, periodontal, endodontic, prosthodontic, pediatric procedures… etc. Oral surgical procedures (extractions, biopsies, oral surgeries…..) 10 % 9 5115) Diagnostic purposes 6) 9/15519SLA/ > - njj9 -j1 LA BJ Injection /10 Topical) 1 m : Topical anesthesia indications: 12Sis yes er mucosal tissues is Pentration /Is Before local anesthesia injections. To relieve pain of conditions like: ulcers, teething, sores. - ↓ s If y To reduce gag reflex. JENLA/Is Teething/Id … etc. j X1j95 % local anesthetic & * solution) PROPERTIES OF IDEAL ANESTHETIC AGENT - : "Isel" S action Bis5 ① Reversible action -j bes jo-I reversible s is Non irritant (/319yjij..... %10 - 1 non-irritant No allergic reaction =1) non-allergic 5% -is Low systemic toxicity * , jso i. I Syd d systemic toxicity : G. Rapid onset Sja y toxicity 6) pay "I i Sufficient duration of action & & 5& /jeisb Wri Sufficient potency S 31. % 19psl Y pentrating properties jigs i & newve conducting I block / /& & jip S , Sufficient penetrating properties & join--stable jgpiy ⑧ Stable in solution and undergo biotransformation in body ·li, javj2/i@ Not interfere with healing of local tissues &-jis Have vasoconstrictor action or compatible with V.C surgery /18159 51 healing /125 Do % V ) solution 591 constrictor action : Vase ⑪. Not expensive 55 8,01;54 Methods of Local anesthesia Classification of local anesthetics according to mode of application: 1. Injectable anesthetics Infiltration anesthesia Field blook anesthesia Nerve block anesthesia 2. Surface anesthetics (Topical) · Infiltration anesthesia D Syl5551 small newe endings n blocks i - : Field block anesthesia larger nerve branch block 1 > - nerve block anesthesia or alveolar nerve block : 51g, " [inter ] jo newve is a , is block a - Es mandibles mandibular branch of trigiminal newe / Structure-Activity Relationships jac lipophilic "amphipathic SjosS$1 31 molecule" = hydrophilic * The typical local anesthetic molecule can be divided into three parts: (1) an aromatic group (Benzene ring), (2) an intermediate chain, and I (3) an amino terminus. properties ester-i lipophilic amide a hydrophilic properties &1) molecule /11/1 400 mg) result from its metabolic breakdown to o-toluidine, an inducer of methemoglobinemia. Prilocaine has also been associated with a greater incidence of nerve damage after inferior alveolar nerve block injections than seen with lidocaine or mepivacaine. Preparations And Dosage of Some Local Anesthetics Bupivacaine Bupivacaine is approximately four times as potent and as toxic as mepivacaine; it also has a slightly higher pKa and a slower onset of action. For dentistry, 0.5% bupivacaine hydrochloride is available with 1:200,000 epinephrine. Preparations And Dosage of Some Local Anesthetics Articaine It is unique among the amides, it’s a hybrid molecule containing both ester and amide components, and undergoes metabolism in both the blood and the liver. Found in a 4% concentration with 1:100,000 or 1:200,000 epinephrine, articaine has become a popular agent for routine use in dentistry. L A/I Preparations And Dosage of Some Local Anesthetics. N / lidocaine JI Xyle :. Caine &3 Articaine & 9/251 5 stable I V )/ 1. : It is unique among the amides, it’s a hybrid molecule containing 100000 0, 9 -both ester and amide components, and undergoes metabolism in Ig 100000mL : both the blood and the liver. Found in a 4% concentration with 1:100,000 or 1:200,000 epinephrine, articaine Cartridge(1 >has become a , 29 popular agent for routine.use in dentistry. om , L Alis lidocaine. U C &s 000;j. 1: USP = United States Pharmacopeia References Local anesthetics, Pharmacology and Therapeutics for Dentistry, 6th edition. Angelo Mariotti, Bart Johnson and Frank J. Dowd. Pharmacology of Local Anesthetics, Handbook of Local Anesthesia, Stanley Malamed, Elsevier, 7th Edition 2020 9jet! Firas. Q Dentist-122