Dental Local anesthetic drugs: Chapter 5 – Flashcards
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Was the first amide local anesthetic drug, developed by Lofgren 1943?
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Lidocaine
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What type of LA drug remains the gold standard against which local anesthetic drugs are compared?
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Lidocaine
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It has a long and impressive record of reliability, with a rapid onset, rare reposrts of hypersensitivity, typical pulpal durations of 60 min. or more, and soft tissue durations of up to 5 hours?
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Lidocaine
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What type of LA drug has been described as a Versatile drug due to its nearly universal applicability in all areas of health care delivery?
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Lidocaine
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What is another name for Lidocaine?
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Xylocaine
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What type of LA drug has been noted to have anticonvulsant properties and in large doses has been used to terminate seizures or decrease their durations?
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Lidocaine
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What type of LA drug acts to prevent or terminate seizures by depressing the excitability of cortical neurons thus raising seizure thresholds?
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Lidocaine
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Lidocaine is provided in the following formulations:
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- 2% lidocaine plain - 2% lidocaine with 1:100,000 epi. - 2% lidocaine with 1:50,000 epi.
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What is a vasoconstrictor added to increase the safety and duration of local anesthetic drugs?
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Epinephrine
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A ________ pulpal duration in dentistry typically lasts from approximately 20 to 40 minutes.
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Short
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A ________ pulpal duration in dentistry typically lats up to 70 minutes.
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Intermediate
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A ________ pulpal duration in dentistry typically lats up to 8 hours depending on the injection technique.
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Long
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_____________ durations are usually much greater even when no vasoconstrictors are used.
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Soft tissue
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What are the Key considerations in its duration of action in LA drugs?
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The receptor binding strength and its vasoactivity
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What prolongs local anesthetic durations by constricting local vasculature?
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Vasoconstrictors
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A long acting amide no longer packaged for dentistry and formaerly marketed as Duranest?
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Etidocaine
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What is the MRD for Lidocaine 2%?
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2.0 mg/lb
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What does MRD (Maximum recommended does) of a local anesthetic drug stand for?
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Represents the maximum quantity of drug that can be SAFELY administered during an appointment in most situations.
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What is the absolute MRD for lidocaine per appointment?
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300 mg per appointment (8 cartrages)
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What type of LA drug is metabolized by hepatic enzymes also known as oxidases and amidases?
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Lidocaine
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T/F Hydrolysis accounts for about one-third of lidocaine elimination.
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True
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What retains most of the pharmacological activity of lidocaine?
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MEGX (monoethylglycinexylidide)
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Less than __% of lidocaine is excreted unchanged by the kidneys.
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10
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What is the pKa of lidocaine?
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7.7
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What is the range for the most useful pKa for injectable anesthetics fall between?
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7.6 and 8.1
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Drugs with pKa values in what range provide more rapid onsets of anesthesia?
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7.6 and 8.1
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When a vasoconstrictor is added, the pH of local anesthetic drugs is ____________. A. Decreased B. Increased C. Stay nuetral
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Decreased (acidic)
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Solutions containing ______________ are more acidic in order to preserve the _____________, which would otherwise oxidize, shortening shelf life considerably.
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Vasoconstrictors; Vasoconstrictors
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What happens when LA drugs expire?
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Decrease the pH and can cause increased buring sensations upon administration.
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Lidocaine is available with epinephrine in dilutions of?
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- 1:50,000 - 1:100,000
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Lidocaine with a 1:50,000 dilution of epinephrine contains how many times more quantity of vasoconstrictor drug as a 1:100,000 dilution?
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2 times
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What is the elimination half life of lidocaine?
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1.6 hours (96 minutes)
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T/F Lidocaine is effective as a topical anesthetic.
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True
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T/F Lidocaine enters breast milk in small amounts.
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True
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What type of LA drug was introduced in Sweden (1957) as an alternative to lidocaine by A.F. Eckenstam?
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Mepivacaine
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What is another name for Mepivacaine?
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- Carbocaine - Polocaine
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Which of the following is a weak vasodilator and is effective for short durations without a vasoconstrictor? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Mepivacaine
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In individuals for whom vasoconstrictors are contraindicated, what type of LA drug are particularly useful?
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3% Mepivacaine
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Mepivacaine is provided in the following formulations:
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- 3% Mepivacaine plain - 3% Mepivacaine with 1:20,000 Levonordefrin
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As with lidocaine what type of LA drug has been noted to have anticonvulsant properties and has been used to terminate seizures or decrease their durations? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Mepivacaine
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What is the MRD of Mepivacaine as in mg/lb?
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2.0 mg/lb
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What is the MRD of Mepivacaine as in mg absolute maximum recommended dose per appointment?
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300 mg absolute maximum recommended dose per appointment
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What type of LA drug is metabolized in the liver, amidase activity is insignificant its elimination half life of 1.9 hours reflects its less efficient metabolic pathways?
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Mepivacaine
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Excreation is variable with anywhere from virtually none to up to 16% excreted unchanged?
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Mepivacaine
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It is the weakest vasodilator of the five injectable drugs available in dental cartridge form and provides useful short term durations in both infiltrations and nerve blocks in plain?
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Mepivacaine
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Mepivacaine is available in what type of vasoconstrictor dilutions?
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- 3% none plain - 2% Levonordefrin 1:20,000
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T/F It is not known whether mepivacaine is excreted in human milk. caution is recommended.
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True
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What type of LA drug was first prepared by Lofgren and Tegner in 1953 and approved by the FDA in 1965?
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Prilocaine
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What type of LA drug is very similar to mepivacaine?
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Prilocaine
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What are onther names for Prilocaine ?
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- Citanest - Citanest Forte
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What type of LA drug can reduce the bloob's oxygen-carrying capacity, which may lead to a specific anemia known as Methemoglobinemia?
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Prilocaine
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Prilocaine is provided in the following formulations:
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- 4% prilocaine plain - 4% prilocaine with 1:200,000 epi
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Which of the following LA drugs aromatic ring is linked to a secondary amine, unlike the other LA drugs which all are linked to tertiarty amines?
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Prilocaine
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What is the MRD in mg/lb for Prilocaine?
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2.7 mg/lb
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What is the MRD mg absolute maximum recommended dose per appointment for Prilocaine?
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400 mg (5 cartridges) absolute maximum recommended dose per appointment.
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What is in Prilocaine that some individuals are at increased risk of developing a potentially life threatening anemia known as methemoglobinemia?
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Metabolite orthotoluidine (o-toluidine)
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What type of Pt would be contraindicated when using Prilocaine?
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Patients at risk for methemoglobinemia as well as patients with - oxygenation difficulties, especially those taking - medications that are independently capable of inducing methemoglobinemia.
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What type of LA drug has a simpler fepatic metabolism, and is cleared before it is able to reach the liver; The lungs and kidneys are alternate sites of metabolism when the liver is not utilized?
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Prilocaine
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T/F Prilocaine is a weak vasodilator, making it effective without the addition of vasoconstrictors, although prilocaine is a stronger vasodilator compared with mepivacaine.
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True
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Prilocaine is available with epinephrine in dilutions of?
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- 1:200,000 epi.
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LA drugs with what type of epinephrine dilutions can be beneficial when it is necessary to limit vasoconstrictor doses; such as cardiovascular compromised pt, tricyclic antidepressant use, and insulin resistant diabetes with underlying cardiovascular disease?
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-1:200,000 epi.
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What type of LA drug was synthesized in 1969 by H. Rusching, is the most Recent FDA approved injectable local anesthetic drug?
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Articane
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What is another name for Articaine?
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Septocaine
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Which of the following LA drugs has a distinctly different aromatic ring structure with an ester component attached? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Articaine
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What is present in Articaine that makes it highly lipophilic, easing the passage through neural membranes?
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Sulfur atom within the ring structure
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What type of LA drug has a controversial association with a higher than typical incidence of post operative nerve damage paresthesia? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Articaine
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Articaine is provided in the following formulations:
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- 4% articaine with 1:100,000 epi. - 4% articaine with 1:200,000 epi.
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What is the MRD in mg/lb for Articaine?
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3.2 mg/lb
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What is the MRD in mg absolute maximum recommended dose per appointment for Articaine?
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500 mg (7 cartridges)
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What is defined as a nerve injury that may be a prolonged temporary or permanent, partial or complete loss or alteration of sensation?
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Paresthesia
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Which of the following LA drugs metabolism is unique, five to ten percent is metabolized via hepatic p450 enzymes? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Articaine
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If the patient has liver issues which of the following LA drugs is the best choice? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Articaine
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Which of the following LA drugs the majority of removal is accomplished by rapid plasma cholinesterase metabolism to articainic acid, its inactive primary metabolite, prior to reaching the liver? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Articaine
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Articaine is available with epinephrine in dilutions of:
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- 1:100,000 - 1:200,000
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Due to its long durations, what type of LA drug may not be appropriate in many clinical situations, but does have several important clinical indications?
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Bupivacaine
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What type of LA drug might be helpful when extended postoperative pain control is needed?
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Bupivacaine
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What type of situation would it be best to use Bupivacaine?
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In situations where profound and durable anesthesia have proven to be difficult if not impossible to achieve with all the other available drugs.
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What type of LA drug would you use for extended procedures requiring longer than 60 to 90 minuts durations?
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Bupivacaine
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Bupivacaine is provided in the following formulation:
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0.5% bupivacaine with 1:200,00 epi.
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T/F The strength of bupivacaines receptor site binding does NOT allow for lower concentrations of epi to be used.
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False
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What type of LA drug has a long duration up to 12 hours; pulpal and sogt tissue?
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Bupivacaine
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What type of LA drug is frequently administered for pain management when significant postoperative pain is anticipated?
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Bupivacaine
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What is the MRD mg/lb for Bupiviacaine?
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0.6 mg/lb
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What is the MRD absolute maximum recommended dose per appointment with Bupivacaine?
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90 mg
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What type of LA drug will NOT be metabolized or cleared as quickly in the presence of a compromised cardiovascular system?
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Bupivacaine
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What are the two main factors that contribute to the increased risk versus other drugs regarding Bupivacaine?
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1. Lengthy half life 2. Early CVS involvement
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What type of LA drug metabolism is refered as complex, The liver provides the major amidase metabolic pathway?
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Bupivacaine
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What type of LA drug biotransformation is much SLOWER compared with the other local anesthetic drugs?
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Bupivacaine
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Which of the following LA drugs is a more aggressive vasodilator? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Bupivacaine
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Out of the two which one is the Most potent vasodilator? A. Bupivacaine B. Procaine
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Procaine
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Which of the following LA drugs has the slowest onset of all the injectable drugs in dentistry and is up to five to ten times slower than mepivacaine and articaine in some situations? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Bupivacaine
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Bupivacain is available with epinephrine in dilutions of:
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1:200,000
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Which of the following has the longest half-life of all dental injectable local anesthetics? A. Articaine B. Lidocaine C. Mepivacaine D. Bupivacaine
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Bupivacaine
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Which of the following is not currently available in dental cartridges, and can be obtained in medical vials in the following formulations? A. Articaine B. Procaine C. Mepivacaine D. Bupivacaine
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Procaine
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Was introduced by Alfred Einhorn in the early 1900s as an alternative to cocaine due to the desire to eliminate addictive tendencies when using local anesthetic drugs as well as the systemic toxicity and local tissue injusry that too often accompanied cocaine's use?
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Procaine
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Its rapid metablolism and complete avoidance of liver metablolism make it the safest drug of the six?
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Procaine
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What is thought to be responsible for procaine's relatively high rate of allergenicity?
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PABA Para-aminobenzoic
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The definition of the maximum recommended dose (MRD) of a drug best fits which one of the following definitions?
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A safe guideline when administering local anesthetic drugs
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Which one of the following best describes articaine's metabolism?
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Articaine is metabolized primarily via plasma cholinesterase
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You are treating a patient with significant cardiovascular compromise who suffers from significant liver damage. Which one of the following drugs would anesthetizing the maxillary right Quadrant?
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4% articaine, 1:200,000 epi.
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A periodontist requires hemostasis on palatal tissues in the maxillary left quadrant prior to elevating a surgical flap. Which one of the following drugs would furnish the most vigorous hemostasis?
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2% lidocain, 1:50,000 epi.
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Which characteristic of a local anesthetic drug determines how well it works without a vasoconstrictor?
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Vasoactivity
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If a patient is taking a tricyclic antidepressant and a beta blocker, which one of the following drugs would be most appropriate to administer?
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3% Mepivacaine plain
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Methemoglobinemia is a life threatening condition that may be precipitated by which one of the following drugs?
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Prilocaine
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Arrange the injectable local anesthetic drugs in descending order of overall CNS and CVS toxicity:
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Bupivacaine, Mepivacaine, Lidocaine, Articaine, Prilocaine
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The maximum recommended dose for epinephrine in a healthy patient is?
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0.2 mg
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What is the maximum recommended dose for epi. in a patient with ischemic heart disease?
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0.04 mg/ 2 cartridges
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Relevant information and mathematical operations required to calculate drug doses for LA and vasoconstrictors include all but which one of the following? A. Dilution percentages B. Standard cartridge volumes C. Defined MRD for each drug D. Hieght and weight
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Height and weight
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Which of the following is NOT related to the MRD for 2% lidocaine, 1:00,000 epinephrine? A. 8 cartridges B. 11 cartridges C. 2 mg/lb for a 150 individual D. 300 mg for a 150 lb individual
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11 cartridges
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What is the MRD for vasoconstrictors when administering 2% lidocaine, 1:100,000 epi. to a healthy individual?
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0.2 mg
