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Metabolism: by the hepatic microsomal enzyme system Safest local anesthetic to use in pediatrics is 2%
in liver and excreted primarily in the urine. lidocaine with 1:100,000 epinephrine.
The most abundant urinary metabolite of For pregnant women, lidocaine and prilocaine have
lidocaine is 4-hydroxyxylidine. the best FDA ranking. Lidocaine may be preferable
Metabolism mechanism of amide type LAs: because it has a low-concentration formulation,
Dealkylation, Hydrolysis and Hydroxylation. which makes it easier to minimize the total dose. For
Hepatic function does not affect the topical preparations, lidocaine also has the safest
duration of action of local anesthesia, rating.
which is determined by redistribution and
not biotransformation. Therefore, a patient
with liver disease needs the standard
amount of local anesthetic at each site.
When treating a patient with significant
liver disease, it is prudent to treat one
quadrant at a time, thereby minimizing
total dose. Use of an ester may not offer
any advantage, because
pseudocholinesterase is also synthesized in
the liver.
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PHARMACOLOGY FOR CANADIAN DENTISTS (BY Dr Mehdi Adibrad)
Important: A dental carpule contaios 1.8 ml solution. formed. If a patient has an allergy to PABA, all
ester-type LA agents are contraindicated.
Note: 1.8 ml of 2% solution of Lidocaine with PABA can decrease the effectiveness of
1:100,000 epinephrine contains 36 mg of
sulfonamides (antibiotics).
Lidocaine and 0.018 mg epinephrine.
Important: All local anesthetics except cocaine are
vasodilators; however, mepivacaine has less of a
vasodilator effect compared to the others and,
Agents: Procaine (Novocaine®), Propoxycaine, therefore, is the drug chosen when a vasoconstrictor
Benzocaine, Tetracaine, Cocaine. is not used with the local anesthetic.
Note: Ester-type LAs are no longer available as Cocaine causes significant euphoria (due to its
dental anesthetic injectable preparations because of
blockade of reuptake of catecholamines and
their relatively high incidence of allergy. They are
mainly available as topical anesthetics (like dopamine in the brain), and its abuse can lead to a
benzocaine). physical dependence. Cocaine increases the
Metabolism: by the plasma pseudocholinesterase (a pressor activity of other sympathomimetic amines
plasma enzyme). and can increase the risk of developing cardiac
o When procaine is metabolized, a highly allergic arrhythmias and hypertension.
compound called para aminobenzoic acid (PABA) is Avoid epinephrine altogether in patients who
have ingested cocaine within the previous 24
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PHARMACOLOGY FOR CANADIAN DENTISTS (BY Dr Mehdi Adibrad)
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PHARMACOLOGY FOR CANADIAN DENTISTS (BY Dr Mehdi Adibrad)
use of another amide. Allergy to epinephrine is Clinical signs: cyanosis, decreased pulse
impossible. oximetry, “chocolate-colored”blood
Treatment: IV methylene blue (1–2 mg/kg of
“Sodium metabisulfite” prevents the oxidation of 1% solution over 5 minutes).
the epinephrine in dental cartridges. It may cause
allergy in patients with a history of asthma and
hypersensitivity to sulfites. It may be best to avoid a Paresthesia:
vasoconstrictor if there is a true documented allergy Articaine and prilocaine were reported as more
to sulfites, as metabisulfite is added as an likely than other anesthetics to be associated
antioxidant whenever vasoconstrictor is present. with paresthesia. Such reactions have most
Vasoconstrictor can be used in patients with an commonly affected the lingual nerve.
allergy to the sulfonamide antibacterials, commonly
called sulfa, as there is no cross-allergenicity with
sulfites.
Methemoglobinemia:
Hemoglobin is oxidized to methemoglobin which cannot
bind and carry oxygen. It is caused by excessive doses of
benzocaine, prilocaine, or rarely lidocaine.
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PHARMACOLOGY FOR CANADIAN DENTISTS (BY Dr Mehdi Adibrad)
Functions:
prolongs the duration of action and increases its
depth,
increases depth of anesthesia,
permits smaller volumes of LA to be administered,
reduces risk of systemic toxicity,
reduces the rate of vascular absorption,
provides a hemostatic effect.
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PHARMACOLOGY FOR CANADIAN DENTISTS (BY Dr Mehdi Adibrad)
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o f t h e a u t h o r ( w w w . c o n f i d e n t i s t . c a )