Pharmacology- Local anesthesia – Flashcards
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Ideal local anesthetic properties
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•Potent local anesthesia •Reversible local anesthesia •Absence of local reactions •Absence of systemic reactions •Absence of allergic reactions •Rapid onset •Satisfactory duration •Adequate tissue penetration •Low cost •Long shelf Life •Sterilization by autoclave •Ease of metabolism and excretion
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Local anesthetics are drugs that produce
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loss of sensation in localized area of body
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Primary use of LA
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prevention and alleviation of pain
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Chemical structure of LA
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â—¦Esters â—¦Amides â—¦Other
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Site of action of LA
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nerve membrane that is responsible for conducting nerve action potential
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Mechanism of action of LA
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â—¦Interfere with functions of neurons by reduce transient increase in sodium flow into nerve membrane â—¦rate of depolarization decreased, increases the threshold for excitability, and prevents the propagation of action potential â—¦May reduce permeability by competing with calcium by preventing onset of nerve conduction
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Ester
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â—¦Cocaine â—¦Ethylaminobenzoate (Benzocaine) has great quality â—¦Tetracaine (Pontocaine) â—¦Procaine (Novocaine) â—¦Propoxycaine (in Ravocaine)
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Amides
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â—¦Lidocaine (Xylocaine) â—¦Mepivacaine (Carbocaine) â—¦Bupivacaine (Marcaine) â—¦Prilocaine ( Citanest) â—¦Articaine (Septocaine)
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Use commonly in dental office
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Amide
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How LA absorption?
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Systemic absorption greater, especially with inflammation •Topical application on denuded mucous membranes - absorption can approximate IV injection
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Purpose of vasoconstrictor
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•Reduces blood supply •Limits systemic absorption •Reduces systemic toxicity
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Factors affect vascularity:
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degree of inflammation, vasodilation, warmth and massage
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Why to Decreased systemic absorption
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reduces chance of systemic toxicity
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To reduce absorption
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vasoconstrictor added
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Where LA distribution
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â—¦throughout body â—¦Highest concentrations in highly vascular organs
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Metabolism of LA
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â—¦esters by plasma pseudocholinesterases â—¦amides primarily by liver
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Use amides carefully patients with
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Liver failure
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LA excretion
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â—¦esters and amides excreted by kidney â—¦use carefully in patients with kidney failure
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Primary clinical effect of local anesthetics is to
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reversibly block peripheral nerve conduction
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Order
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â—¦autonomic, cold, warmth, pain, touch, pressure, vibration, proprioception, and motor response â—¦order may variety in patients â—¦returns in reverse order
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Adverse reaction
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•Adverse reactions and toxicity of local anesthetics directly related to plasma level of drug •Considering widespread use, potential for danger must be minimal •Deaths from local anesthetics difficult to document, but dental related mortality even rarer •Low incidence of ADR's (esters >amides)
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Adverse reactions and toxicity of local anesthetics directly related to
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Plasma level of drug
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Toxicity drug factor
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•Drug •Concentration •Route of administration •Rate of injection •Vascularity •Patient's weight •Rate of metabolism and excretion
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Who are debilitating patients more likely to experience ADR?
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-Children and elderly -2 main systems affect by ADR - local - (Malignant hyperthermia not related to amides)
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Two main system affect by ADR
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•CNS stimulation may precede CNS depression •restlessness, tremors, seizures, then CNS depression ◦CV •myocardial depression, cardiac arrest with peripheral vasodilation
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What about local give ADV
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â—¦injection technique - most common is injection of excessive volume too quickly
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Maglinant hyperthermia
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â—¦Inherited disease resulting in acute rise in calcium with symptoms of muscular rigidity, metabolic acidosis and extremely high fever â—¦Mortality 50% â—¦Most commonly associated with halothane, the inhalation anesthetic, and succinylcholine, the neuromuscular blocking agent â—¦Treatment - supportive measures and administration of dantrolene â—¦Patients with family history can receive amide LA's
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Elective dental treatment should be rendered before pregnancy
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True
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If needed, which may be administered to pregnant women
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Lidocaine
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Which has been reported with larger doses are administered to mother near term
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Fetal bradycardia
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FDA pregnancy category B
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Lidocaine and prilocaine
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pregnancy category C
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Mepivacaine, articaine, and bupivacaine
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Usual doses given to nursing mothers DO NOT affect health of normal nursing infant
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True
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Allergy to LA
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•Range from rash to anaphylactic shock •Elicit allergy history before local chosen •Esters greater allergic potential •Locals with vasoconstrictors also have sulfites
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No allergy to amide
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True
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Antioxidant
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â—¦Sodium metabisulfite, sodium bisulfite, or acetone sodium sulfite â—¦Prolong shelf life â—¦Can precipitate symptoms of wheezing or chest tightness in asthmatic patients
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Composition of LA solution
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•Vasoconstrictor •Antioxidant Sodium Chloride (Makes injectable solution isotonic) Sodium hydroxide(Adjusts ph) •Methylparaben and propylparaben
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Methylparaben and propylparaben
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â—¦Preservatives â—¦Not used in single dose cartridges
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Amide
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•Amides are only class of anesthetics used parenterally. -lower hypersensitivity reaction rate, longer shelf life, more efficacious, and action suitable for most dental procedures. -No cross allergenicity between the amide lidocaine, other available amides, or esters has been documented.
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Good for almost all dentistry
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Lidocaine â—¦No cross allergenicity between other amides or esters â—¦Some patients experience sedation â—¦In toxicity reactions, likely to see CNS depression rather than CNS stimulation
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â—¦In dentistry, lidocaine 2% with a:100,000 epi used for
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infiltration and block anesthesia
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Lidocaine ADR
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hypotension, positional headache, shivering
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Used for topical anesthesia as
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5% ointment, 10% spray, 2% viscous solution Topical onset rapid (2-3 minutes
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Lidocaine with Epi 1:100,000 provides
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1-1.5 hrs duration of pulpal anesthesia with soft tissue anesthesia maintained for 3-4 hours)
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Bupivacaine-prolonged duration
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â—¦Amide similar to lidocaine and mepivacaine â—¦More potent and less toxic than other amides â—¦Major advantage is greatly prolonged duration of action â—¦Ideal for lengthy dental procedures when pulpal anesthesia of greater than 1.5 hrs expected or when postop pain anticipated (endo, perio, or oral surgery) â—¦Similar to mepivacaine, but slower onset and longer duration â—¦Should not be used in patients prone to self mutilation (mental patients or children younger than 12 years) â—¦Pregnancy rating C-use only if others not an option
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To avoid vasoconstrictor
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Mepivacaine plain
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Usual dose form of Mepivacaine
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2% with 1:20,000 levonordefrin as vasoconstrictor
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Use for short procedures when a vasoconstrictor is contraindicated (not often)
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Mepivacaine
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What caution when using Mepivacaine
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should be exercised when using increased concentrations of la's without vasoconstrictor because systemic toxicity more likely
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Except in unusual cases, benefit of shorter duration does not warrant
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eliminating vasoconstrictor, especially when concentration is increased
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How long for procedure of Mepivacain without vasoconstrictor
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<30 minutes only (short procedu
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Mepivacaine
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Rate of onset, duration, potency, toxicity similar to lidocaine with vasoconstrictor, procedure 30-90 minutes
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Prilocaine
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â—¦Related chemically and pharmacologically to lidocaine and mepivacaine â—¦Less potent and less toxic than lidocaine and has slightly longer action â—¦Niche is situations when desired duration is somewhat longer than mepivacaine (without and with vasoconstrictor)
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Related chemically and pharmacologically to lidocaine and mepivacaine
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Prilocaine
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Less potent Less toxic than lidocaine Has slightly longer action
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Prilocaine
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Which LA is similar to lidocaine and Mepivacaine
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Bupivacaine
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Which LA is MORE potent LESS toxic than other amides?
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Bupivacaine
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Major advantage of Bupivacaine
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greatly prolonged duration of action
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Bupivacaine should not used in which patient
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Patients prone to self mutilation (mental patients or children younger than 12 years) â—¦Pregnancy rating C-use only if others not an option
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When using Bupivacaine, fatalities in obstetrics occurs during
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its early use in anesthesiology when much higher doses than those used in dentistry were used
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-Newest amide approved in US by FDA in 2000 -Has become the most widely used LA
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Articaine
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Articaine
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-Different derivation allows for greater lipid solubility and ability to cross lipid barriers such as nerve membranes -Enhanced action compared with other LA
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Time life if Articaine
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T ½ 20 minutes compared to 90 minutes with lidocaine, so may be safer for reinjection during a dental visit
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Average patient can tolerate Articaine
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2X as much lidocaine as articaine before max dose reached
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Very high dose of Articaine can cause
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methemoglobin, but no cases reported in dental patients
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Rarely causes paresthesia following mandibular block when 4% used
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True
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Which LA More desirable in patients who may need reinjection, lowering risk for toxicity
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Articaine
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Although clinical trials have not shown that articaine is better than other LA, many trials show that articaine slightly outperformed other LA that it was compared to
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TRUE
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most commonly used (adrenergic agonists or sympathomimetics)
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Epinephrine and levonordefrin
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What happend when LA dose not contain vasoconstrictor
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anesthetic drug more quickly removed from injection site and distributed into systemic circulation than if contained vasoconstrictor
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How is duration for plain anesthetic (without vasoconstrictor)
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exhibit shorter duration of action and result in more rapid buildup of systemic blood level
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any anesthetic given without vasoconstrictor more likely to be
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toxic than those given with vasoconstrictor
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Must be weighed against possible systemic effect of vasoconstrictor
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True
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Reasons for Use of Vasoconstricting Agents in Local Anesthetics
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-Prolong duration action -Increase depth of anesthesia -Delay systemic absorption of LA -Reduce toxic effect in systemic circulation -Reduce bleeding in area of injection and improve visibility of surgical site
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In past, felt vasoconstrictors should not be used in patients with
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cardiovascular disease
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Stemmed from fear that vasoconstrictor would
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elevate blood pressure too much
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patient produces endogenous epi far in excess of that administered in dentistry in
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presence of inadequate anesthesia which sometimes occurs when vasoconstrictors are avoided
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If controlled hypertension or angina can receive LA with
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epi
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Administer in lowest possible dose using techniques that minimize
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systemic absorption
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Do not use vasoconstrictor if
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uncontrolled hypertension, hyperthyroidism, unstable angina, MI or stroke in past 6 months should make appointment after controlled
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For MI or CVA, when can use vasoconstrictor
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after 6 months
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Patients with cardiovascular disease who are able to withstand dental treatment should/should not receive administration of epinephrine-containing la's
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should
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Maximum safe dose of epinephrine in healthy patient
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0.2 mg
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Maximum safe dose of epinephrine in appropriate cardiac patient is
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0.04 mg
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Dental Practitioner should become familiar with
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at least 2 agents, or short, an intermediate, and a long acting agent
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Short Duration (Pulpal = 30 minutes)
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-Lidocaine plain (without) -Mepivacaine plain (without) -Prilocaine plain (infiltration)
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Intermediate Duration (Pulpal 30-60 minutes)
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-Mepivacaine with vasoconstritor -Prilocaine plain (block) (without) -Prilocaine with (60-90 minutes) -Articaine with (60-90 minutes)
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Long Duration (Pulpal > 90 minutes)
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Bupivacaine with
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Duration of lidocaine with vasodilation in pupal
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60 min
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Duration of lidocaine with vasodilation in soft tissue
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3-5 hrs
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Mepivacaine without (plain) in pupal
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40 min
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Mepivacaine without (plain) with infilatration in pupal
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20 min
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Mepivacaine without (plain) in soft tissue
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2-3 hrs
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Mepivacaine with in pupal Mepivacaine with in soft tissue
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60-90 min 3-5 hrs
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Prilocaine without (plain) in soft tissue Prilocaine with infiltration in soft tissue
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2-4 hrs 1.5-2 hrs
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Prilocaine without (plain) in pupal Prilocaine without (plain) in pupal with infiltration
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60 mintues 10 min
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Prilocaine with in pupal Prilocaine with infiltration in pupal
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60-90 min 45-60 min
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Prilocaine with in soft tissue Prilocaine with 1:200,000 epinephrine
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3-8 hrs 2-4 hrs
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Bupivacaine with in pupal Bupivacaine with in soft tissue
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90-180 min 4-9 (12)
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Articaine with in pupal Articaine with in soft tissue
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60-90 min 3-4 hrs
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Dental Concerns LA
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-Detailed medication/health history -Use maximum safe dose of LA and vasoconstrictor based on physical health and medication history -Record local anesthetic concentration, vasoconstrictor concentration, and number cartridges used -Check BP -Consultation with MD may be advised
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Instructions for Patients Receiving LA
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-Advise patients to tell dental practitioner if feeling anxious, nervous, or if having heart palpitations -Most of these symptoms can be avoided by lowering dose or switching to another la -Some LA can cause sedation (lidocaine) -Use caution if opioid analgesic or antianxiety drug also prescribed -Avoid driving or doing anything that requires concentration -Avoid eating or drinking very hot or cold foods or drinks
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Which can more likely to be absorbed and cause systemic toxicity
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Hydrochloride salt
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When topical Lidocaine - base preferred
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large areas of mucosal surfaces are ulcerated, abraded, denuded, or erythematous
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What form of topical anesthesic base available
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jelly, oral topical solution Hydrochloride available as ointment, oral topical, oral aerosol
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poorly absorbed and lacks significant systemic toxicity, but can cause hypersensitivity reactions
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topical bezocaine
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Dental Hygiene ConsiderationsTopical Anesthetic Agents
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-Limit area of application -Select topical based on patients medication/health history -Avoid using spray formulations
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Dental Concerns for topical anesthesia
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-Inform patients of ADR potential -Educate patient to relate any ADR -Sedation with lidocaine and need to be accompanied -Refrain from eating and drinking heat or cold
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Topical anesthetic include
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Benzocaine Lidocaine
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Used of topical anesthetic
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-Applied to mucous membranes -Limit area of application -Use smallest volume of least toxic topical -All can be absorbed systemically