WWA#3; Ch. 5: Local Anesthetic Agents – Flashcards
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cartridge contents
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local anesthetic drug, vasoconstritor, vaso preservative/sodium bisulfite, buffer/sodium hydroxide or sodium chloride, methylparraben/bacteriostatic agent and preservative (before 1984 only)
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1.8 mL or 1.7 ml?
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most cartridges contain 1.8 mL but FDA requires it be labeled as 1.7 mL if manufacturer cannot guarantee due to slight machine variations
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2 classifications of LAs
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esters metabolized in plasma by cholinesterase; and amides metabolized in liver, except articaine which is metabolized in blood --all for dentistry are amides because of possibility of hypersensitivity
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5 generic classificaitons of amide LAs available for use in dentistry
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lidocaine mepivacaine prilocaine articaine bupivacaine
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selection of LA determined on patient-by-patient basis with consideration of
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efficacy, safety, individual patient assessment, consultations and dental or dental hygiene care plan
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DH must consider
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--duration of pain control based on length of procedure --need for post-treatment pain control --patient's health assessment and currents meds --allergy to sodium bisulfite, metabisulfite or local anesthetic --need for homeostasis
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duration of action and operative pain control
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--lower pKa = more anions in base for better penetration, more rapid onset of action -- lipid solubility and protein-binding capacity related to duration of action -- lipid solubility determines potency
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bupivacaine has highest perctnage of protein binding and is most lipid-soluble; so therefore has
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longest duration and is most potent --it also has hightest pKa, so slowest onset of action
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mepivacaine and prilocaine have least vasodilating effects, allowing
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anesthetic to remain in area of deposition longer --therefore effective without a vasocinstrictor --good alternatives if vasoconstrictor contraindicated
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duration of LA has 3 categories, influenced by presence or absence of a vasoconstrictor
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1. short acting: 30 min of pulpal anesthesia, no vasoconstrictor 2. intermediate acting: 60 min of poulpal anesthesia with a vasoconstrictor 3. long acting: 90+ minutes with a vasoconstrictor; only Bupivacaine
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duration of anesthesia varies among patients depending on
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--individual response to anesthetic --accuracy of anesthetic administration --vascularity of tissue --variation of anatomic structure --injection technique
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individual response, using Lidocaine 2%, 1:100,000 as an example
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normal responders, 70% hyper-responders, 15% hypo-responders, 15% --note in chart if hypo or hyper, or any modifications made to achieve appropriate duration
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accuracy of anesthetic administration
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--most difficult when giving nerve block --least difficult when giving supraperiosteal
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vascularity of tissue
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--onset of action and duration more predictable in healthy tissue --inflamed tissue has increased vascularity, so slower onset and decreased duration because of rapid absorption
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variation of anatomic tissue
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difficult to predict, often decrease duration;
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decreased duration and effectiveness in maxillae due to
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--density of bone --flaring of palatal roots --lower than normal zygomatic arch, esp in children
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decreased duration and effectiveness in mandible due to
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--height of mandibular foramen --width of mandible --width and length of ramus --volume of musculature and adipose tissue --injection technique
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posttreatment pain control if posttreatment discomfort expected
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--most procedures performed by DH fall within intermediate range --avoid longer-acting LA for children and special needs patients b/c of possibility of self-mutilation
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patient health assessment and current meds
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evaluate at each appointment, then determine MRD
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relative contraindication
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administration of offending drug may be used judiciously
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absolute contraindicaiton
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offending drug should not be administered under any circumstances
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maximum recommended dose/MRD
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maximum quantity of drug a patient can safely tolerate during an appointment based on physical status
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local anesthetic, sodium bisulfite and metabisulfite allergy
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may include respiratory reactions in asthmatic patients --individuals allergic to sulfites should not be given LA with vasoconstrictor --if allergy to anesthetic, give one in different class
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need for homeostasis
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--no difference in pain control b/c of epinephrine, but there is a difference in bleeding control --1:50,000 has most homeostasis --epinephrine better bleeding control than levonordefrin
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lidocaine --a xylidine derivitive
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--first amide available for dentistry --most common --rarely used without a vasoconstrictor b/c of duration of pulpal anesthesia (60 min with, 5-10 min. without) --anticonvulsant properties; used to terminate seizures --only topical anesthetic available --avail in 3 formulations
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mepivacaine --a xylidine derivitive
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similar to lidocaine in onset of action, duration, potency, toxicity and no reported allergic reactions --less vasodilation than lidocaine, so effective without a vasoconstrictor (3% formulation) --2% with levonordefrin used in US --but not same degree of homeostasis --not effective as topical
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prilocaine --a toluidine derivative
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equal potency to lidocaine and mepivacaine --least toxic anesthetic available --good when need slightly longer duration of action --metabolized more easily by the liver --contraindicated for patients at risk of methemoglobinemia, or patients with oxygenation difficulties --topical uses combination with lidocaine
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methemoglobinemia
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limiting factor for clinical use of prilocaine --presence of a higher than normal level of methemoglobin in blood that does not bind to oxygen --clinical cyanosis of the lips and mucous membranes can be observed
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articaine, --thiophene derivative, which is an ester linkagae, so better lipid solubility --hydrolyzed by esterase and in liver
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--safer drug to readminister later during dental visit if more anesthesia needed --concern over increased incidence of paresthesia --good alternative for patients with increased risk of CV disease, or for those taking medications that enhance effect of epinephrine
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bupivacaine
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--most potent and toxic --only one with long duration of action, but has slower onset --pulpal anesthesia for 1.5 to 3 hours, soft tissue 4-9 --good alternative when profound anesthesia hard to attain --not recommended for children or special needs
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procaine/Novacain --an ester, still available for use in medicine --not used in dentistry
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--less potent and toxic than amides --used as an antiarrhythmic --greatest vasodilating properties, no pulpal anesthesia --was first injectable LA
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buffering
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may improve patient comfort by eliminating the sting, may reduce tissue injury and may reduce anesthetic latency, may provide more effective anesthesia in area of infection
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1. most important advantage of amide over ester local anesthetics
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less allergenicity
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2. which local anesthetic is longest acting? --lidocaine, procaine, bupivacaine with epi, prilocaine with epi, articaine with epe
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bupivacaine with epinephrine
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3. Which local anesthetic has the least vasodilatory effect when used without epinephrine? --mepivacaine, lidocaine, cocaine, procaine
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Mepivacaine --Mepivacaine has the least vasodilatory properties second only to prilocaine.
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4. Which local anesthetic has the greatest vasodilatory effect when used without epinephrine? --mepvicaine, lidocaine, articaine, procaine
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procaine --Procaine has the greatest vasodilatory properties of all ester and amide local anesthetics.
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5. One cartridge of anesthetic contains how much solution?
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1.8 mL
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6. Factors in selection of local anesthetic for a patient include all of the following
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--length of time pain control is necessary --presence of any contraindication, absolute or relative --requirements for homeostasis --not influenced by vitamin intake
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7. Which is false? --Esters of para-aminobenzoic acid are not commercially available. --Procaine is an ester. --Topical benzocaine is an amide. --Prilocaine is an amide.
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--Topical benzocaine is an amide. FALSE! --Benzocaine is an ester topical anesthetic. Lidocaine is the only topical anesthetic.
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8. Which of the following LAs is metabolized in the plasma and liver?
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articaine
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9. Which of of the following is an advantage of having a LA metabolized in the plasma and liver? --increased duration of action --shorter half-life of drug --decreased vasoactiviy of drug --easy excretion of metabolites
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shorter half-life --Articaine is metabolized predominately in the plasma, and has a half-life of 45 minutes compared to lidocaine's half-life of 90 minutes.
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10. Which of the following LA is metabolized in the lungs and liver? --mepivacaine, bupivacaine, prilocaine or articaine
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prilocaine --It is metabolized easier by the liver than lidocaine and mepivacaine because much of the drug is already metabolized by alternate sites in the lungs and kidneys before it reaches the liver.
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11. Methylparaben
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bacteriostatic agent that is no longer added to dental cartridges due to high incidence of allergic reactions
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12. How is 3% mepivacaine formulated?
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3% plain --3% mepivacaine is only formulated without a vasoconstrictor.
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13. Which of the following is a concern when selecting bupivacaine? --patient self-mutilation, decreased risk of toxicity, concentration of anesthetic, ease of biotransformation
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patient self-mutilation, because of longer duration
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14. Best option for readministration of anesthetic to provide a lessened likelihood of blood concentration buildup? --lidocaine, mepivacaine, prilocaine, articaine or bupivacaine
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articaine --Because of articaine's rapid metabolism and its inactive metabolites, it may be a safer drug to re-administer later during a dental visit if more anesthetic is necessary.
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15. The lower the pKa of a drug, the more cations are present, which decreases the onset of action.
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false; The lower the pKa, the more anions are present in base form for better penetration through the lipid rich nerve, which provides a more rapid onset of action.
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16. Which is not a factor in the duration of a LA? --individual response, anatomic structure, patient health assessment, injection technique
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patient health assessment Duration of anesthesia varies among patients depending on individual response to anesthetic, accuracy of anesthetic administration, vascularity of tissue, variation of anatomic structure, and injection technique.
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17. Which LA is used when a vasoconstrictor provides intermediate duration of action when administering a block injection? --lidocaine, mepivacaine, prilocaine or bupivacaine
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prilocaine --4% Prilocaine when administered as a block injection increases its duration from short to intermediate action providing pulpal anesthesia for approximately 40-60 minutes and soft tissue anesthesia for approximately 2 to 4 hours.
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18. Which is the best reason for choosing a local anesthetic that provides a long duration? --need for postopertive pain control, medical status of patient, dense bone in area of administration, infection in the area
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need for postopertive pain control
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19. When is lidocaine 1:50,000 epinephrine most effective?
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when homeostasis is needed
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20. Where is procaine metabolized? --in liver, lungs, plasma or plasma and liver
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plasma --Procaine is an ester, and is metabolized via plasma cholinesterase to PABA, which is the major metabolic by-product responsible for allergic reactions.