Articaine Overview: Properties and Metabolism
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Questions and Answers

What is a distinguishing feature of articaine compared to other amide local anesthetics?

  • Is exclusively metabolized in the liver
  • Contains a diethyl group
  • Is less potent than lidocaine
  • Has a thiophene group enhancing lipid solubility (correct)
  • Which of the following local anesthetics has a maximum recommended dose of 7.0 mg/kg body weight?

  • Lidocaine
  • Procaine
  • Articaine (correct)
  • Bupivacaine
  • What is the onset of action for infiltration anesthesia using articaine?

  • 1 to 2 minutes (correct)
  • 1 minute
  • 2 to 3 minutes
  • 5 minutes
  • What potential side effect is associated with articaine usage?

    <p>Methemoglobinemia</p> Signup and view all the answers

    Which group of patients should avoid using articaine due to methemoglobinemia risks?

    <p>Patients with idiopathic or congenital methemoglobinemia</p> Signup and view all the answers

    What is the classification of Bupivacaine?

    <p>Amide</p> Signup and view all the answers

    Which patient group should avoid the use of Bupivacaine?

    <p>Physically &amp; mentally disabled children</p> Signup and view all the answers

    What structure does articaine possess that allows for dual biotransformation?

    <p>An ester group</p> Signup and view all the answers

    Which ASA classes identify patients with significant cardiovascular disease?

    <p>ASA class 3 and 4</p> Signup and view all the answers

    Which of the following local anesthetics is available in a plain form without vasoconstrictors?

    <p>Mepivacaine</p> Signup and view all the answers

    What is the main reason why topical anesthetics are only effective on surface tissues?

    <p>Intact skin forms a barrier</p> Signup and view all the answers

    What is the maximum number of carpules for 2% Mepivacaine with Epi for a patient weighing 70 kg?

    <p>8 carpules</p> Signup and view all the answers

    What concentration of lidocaine is commonly used in topical anesthetics?

    <p>5% or 10%</p> Signup and view all the answers

    What is the duration of pulpal anesthesia using articaine with 1:100,000 epinephrine?

    <p>60-75 minutes</p> Signup and view all the answers

    What should EMLA cream be applied for?

    <p>1 hour prior to a procedure</p> Signup and view all the answers

    How much Mepivacaine is contained in one carpule of 3% Mepivacaine without Epi?

    <p>54 mg</p> Signup and view all the answers

    What effect do MAO inhibitors have in relation to Epinephrine?

    <p>Prevent breakdown of Epinephrine</p> Signup and view all the answers

    Which of the following is a contraindication for using EMLA cream?

    <p>Methemoglobinemia</p> Signup and view all the answers

    What is the potency comparison of Bupivacaine to Lidocaine?

    <p>4 times more potent</p> Signup and view all the answers

    What is the maximum amount of carpules that can be administered for 4% Articaine with Epi based on body weight?

    <p>72 mg/cartridge</p> Signup and view all the answers

    What is a potential factor in selecting a local anesthetic for a patient?

    <p>Length of time pain control is necessary</p> Signup and view all the answers

    What is the primary action of adrenergic vasoconstrictors in local anesthesia?

    <p>Decrease bleeding and improve hemostasis</p> Signup and view all the answers

    Which of the following is classified as a non-catecholamine vasoconstrictor?

    <p>Phenylephrine</p> Signup and view all the answers

    Which receptor type mediates vasoconstriction when stimulated by catecholamines?

    <p>Alpha (α) receptors</p> Signup and view all the answers

    What is a clinical application of epinephrine?

    <p>Management of cardiac arrest</p> Signup and view all the answers

    In what manner do indirectly acting vasoconstrictors function?

    <p>Increase the release of catecholamines</p> Signup and view all the answers

    Which effect is NOT associated with the action of epinephrine?

    <p>Bronchoconstriction</p> Signup and view all the answers

    What is the role of alpha (α) adrenergic receptors in the cardiovascular system?

    <p>Cause vasoconstriction</p> Signup and view all the answers

    Which condition is NOT typically treated with vasoconstrictors?

    <p>Chronic pain management</p> Signup and view all the answers

    What is the maximum dosage of epinephrine for a normal healthy patient (ASA I) per appointment?

    <p>0.2 mg</p> Signup and view all the answers

    What is the primary mode of action of levonordefrin?

    <p>Direct α-receptor stimulation</p> Signup and view all the answers

    Which side effects are commonly associated with levonordefrin overdose?

    <p>Hypertension and anginal episodes</p> Signup and view all the answers

    How does the potency of levonordefrin as a vasopressor compare to epinephrine?

    <p>Levonordefrin is 15% as potent</p> Signup and view all the answers

    What is the maximum dosage of levonordefrin per appointment for all patients?

    <p>1 mg</p> Signup and view all the answers

    Which factor is NOT considered when selecting a vasoconstrictor for a dental procedure?

    <p>Patient's insurance coverage</p> Signup and view all the answers

    What is the maximum number of cartridges of epinephrine a patient with clinically significant cardiovascular disease (ASA III or IV) can receive per appointment?

    <p>1 cartridge</p> Signup and view all the answers

    Why might the benefits of using vasoconstrictors be weighed against the use of plain anesthetic solutions?

    <p>To minimize potential side effects</p> Signup and view all the answers

    Study Notes

    Articaine

    • Hybrid molecule, classified as an amide, but with ester characteristics
    • 1.5 times more potent than lidocaine
    • Toxicity similar to lidocaine and procaine
    • Metabolism:
      • Only amide local anesthetic with a thiophene group (enhances lipid solubility and tissue penertration)
      • Biotransformation occurs in plasma via hydrolysis by plasma esterase and in liver via hepatic microsomal enzymes
    • Excretion:
      • Via the kidneys; 5% to 10% unchanged, 90% metabolites
    • Vasodilating Properties:
      • Vasodilating effect equal to that of lidocaine
    • Effective dental concentration: 4%
    • Onset of action:
      • Infiltration: 1 to 2 minutes
      • Block: 2 to 3 minutes
    • Pulpal anesthesia:
      • 1:100,000 epinephrine: 60 – 75 minutes
      • 1:200,000 epinephrine: 45– 60 minutes
    • Soft tissue anesthesia:
      • 1:100,000 epinephrine: 180 -360 minutes (3-6 hours)
      • 1:200,000 epinephrine: 120-300 minutes (2-5 hours)
    • Maximum recommended dose: 7.0 mg/kg body weight
    • Pregnancy classification: C (not safe)
    • Side effect: Methemoglobinemia
    • Contraindications:
      • Idiopathic or congenital methemoglobinemia
      • Cardiac & respiratory failure
      • Allergy to sulfite - containing drugs

    Bupivacaine

    • Classification: Amide
    • Long acting local anesthetic drug
    • Bupivacaine HCl 0.5% + epinephrine 1:100,000 or 1:200,000
    • Potency: 4 times that of Lidocaine
    • Pregnancy classification: C (not safe)
    • Indications:
      • Lengthy dental procedures (Oral Surgery, implant surgery, periodontal procedures)
      • Management of postoperative pain
    • Contraindications:
      • Physically & mentally disabled children
      • Patients with cardiovascular issues

    Topical Anesthetics

    • Intact skin is a barrier to diffusion of local anesthetics
    • Mucous membranes and injured skin lack this barrier which allows for penetration
    • Topical anesthesia is effective only on surface tissues (2 to 3mm)
    • To increase efficacy, a more concentrated form is used (5% or 10% lidocaine)
    • Commonly used topical local anesthetics: benzocaine, dyclonine hydrochloride, EMLA, lidocaine
    • Benzocaine 20%:
      • Ester local anesthetic
      • Poorly soluble in water, remains at the site of application longer, providing a prolonged duration of action
      • Not suitable for injection
    • Dyclonine Hydrochloride:
      • Ketone derivative without an ester or amide linkage
      • Can be used in patients that are allergic to common anesthetics
    • EMLA (Eutectic Mixture of Local Anesthetics):
      • 2.5% Lidocaine + 2.5% Prilocaine
      • Emulsion of lidocaine and prilocaine in a 1:1 ratio by weight
      • Works on intact skin
      • Applied 1 hour prior to procedure
      • Contraindications:
        • Congenital or idiopathic methemoglobinemia (Prilocaine)
        • Infants younger than 12 months receiving treatment with methemoglobin inducing agents
        • Known sensitivity to amide type local anesthetics

    Selection of Local Anesthetic for a Patient

    • Length of time pain control is necessary
    • Potential need for post treatment pain control
    • Possibility of self-mutilation (self harm) in the post operative period
    • Requirement for hemostasis
    • Presence of any contraindications (Medical History, Allergies, Pregnancy)

    Vasoconstrictors

    • Classification:
      • Based on chemical structure:
        • Catecholamines: Epinephrine, Norepinephrine, Levonordefrin, Isoproterenol, Dopamine
        • Noncatecholamines: Amphetamine, Methamphetamine, Ephedrine, Hydroxyamphetamine, Metaraminol, Methoxamine, Phenylephrine
      • Based on mode of action:
        • Directly Acting: Epinephrine, Norepinephrine, Levonordefrin, Isoproterenol, Dopamine, Methoxamine, Phenylephrine
        • Indirectly Acting: Amphetamine, Methamphetamine, Hydroxyamphetamine, Tyramine
        • Mixed Acting: Metaraminol, Ephedrine

    Action of Vasoconstrictors

    • Decrease blood flow
    • Decreased rate of absorption of LA into CVS, lower anesthetic blood levels
    • Decrease the risk of toxicity
    • Increases duration of action
    • Decrease bleeding (hemostasis)

    Adrenergic Receptors

    • Special proteins found on the surface of cells, act as docking stations for catecholamines (Epinephrine)
    • Two types of receptors:
      • Alpha (α) - vasoconstriction
      • Beta (β) - vasodilation, bronchodilation, cardiac stimulation

    Epinephrine

    • Mode of action: Acts directly on alpha (α) and beta (β) adrenergic receptors
    • Systemic Effects:
      • Myocardium: ↑ heart rate & cardiac output
      • Blood Pressure: ↑ systolic pressure
      • Vasculature: vasoconstriction of smaller arterioles
      • Respiratory: Bronchodilator
      • CNS: Not a potent CNS stimulant
      • Metabolism:
        • Increase oxygen consumption
        • Glycogenolysis - ↑ blood sugar
    • Clinical applications:
      • Management of acute allergic reactions (anaphylaxis)
      • Management of refractory bronchospasm (status asthmaticus)
      • Management of cardiac arrest
      • As a vasoconstrictor in local anesthetics
      • To produce mydriasis (dilatation of the pupil)
    • Normal healthy patient (ASA I):
      • 1:50000 (36): 5.5 cartridges
      • 1:100000 (18): 11 cartridges
      • 1:200000 (9): 22 cartridges
    • Patient with clinically significant CVS disease (ASA III or IV):
      • 1:50000 (36): 1 cartridges

      • 1:100000 (18): 2 cartridges

      • 1:200000 (9): 4 cartridges

      • Maximum epinephrine dose of 0.2 mg (200 µg) per appointment for normal healthy patients (11 cartridges)

      • Maximum epinephrine dose of 0.04 mg (40 µg) per appointment for ASA III or ASA IV (2 cartridges)

    Levonordefrin

    • Mode of Action:
      • Direct α-receptor stimulation (75%), with some β activity (25%)
      • 15% as potent a vasopressor as epinephrine
    • Systemic Actions:
      • Produces less cardiac and CNS stimulation than epinephrine
    • Side Effects and Overdose:
      • The same as with epinephrine but to a lesser extent
      • Higher doses can cause: hypertension, ventricular tachycardia, and anginal episodes in patients with coronary artery insufficiency
    • Clinical Applications:
      • Used as a vasoconstrictor in local anesthetics
      • Combined with Mepivacaine in a 1:20,000 dilution
    • Maximum Doses:
      • 1 mg per appointment for all patients of a 1:20,000 dilution (11 cartridges)
      • Volume is limited by local anesthetic dose

    Selection of Vasoconstrictors

    • Length of the dental procedure
    • Need for hemostasis
    • Requirement for postoperative pain control
    • Medical status of the patient

    Contraindications of Vasoconstrictors

    • Benefits and risks of including the vasopressor must be weighed against using a plain solution
    • Groups of patients with contraindications include:
      • Patients with more significant cardiovascular disease (ASA class 3 and 4)
      • Patients with certain non-cardiovascular diseases (e.g., thyroid dysfunction, diabetes, sulfite sensitivity)
      • Patients receiving MAO inhibitors (monoamine oxidase inhibitors)

    How to calculate the maximum number of carpules (cartridges) per appointment

    • 2% Mepivacaine with Epi 1:100,000 (red color):
      • (Body weight X 6.6mg/kg) / 36 mg/cartridge = maximum number of carpules/visit
      • 36mg came from 2% which is 20 mg of mepivacaine/ml
    • 3% Mepivacaine without Epi (green color):
      • (Body weight X 6.6mg/kg) / 54 mg/cartridge = maximum number of carpules/visit
      • 54mg came from 3% which is 30 mg of mepivacaine/ml
    • 4% Articaine with Epi (blue color):
      • (Body weight X 7 mg/kg) / 72 mg/cartridge = maximum number of carpules/visit

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    Description

    This quiz covers the key characteristics and pharmacology of Articaine, including its potency compared to other local anesthetics, metabolic pathways, and clinical application in dental procedures. Test your understanding of its properties, efficacy, and safety parameters.

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