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Chapter 8
Local Anesthetics
96
Pharmacology
Professional
03/20/2013

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Term
What are some desirable effects of local anesthetics?
Definition
-potent
-rapid onset
-good duration
-reversible
-good penetration of tissues
-easily metabolized and excreted
-no localized, systemic, or allergic reaction
-low cost
-stable solution
-can be steralized
Term
Why do we want a potent local anesthetic?
Definition
because an increased potency requires a lower dose
Term
Why do we want local anesthetics to be reversible?
Definition
because we do not want the person to loose sensation to the area permanently
Term
Why do we want a local anesthetic that penetrates the skin really well?
Definition
so that it can get to the nerves
Term
Which local anesthetic is more potent: 2% or 5%?
Definition
2% is more potent
Term
What are the two chemical structures of local anesthetics?
Definition
esters and amides
Term
What is a bad thing about esters?
Definition
they have a higher allergen potential than amides
Term
What are some examples of ester anesthetics?
Definition
1.procaine
2.benzocaine
3.tetracaine
4.cocaine
Term
Which of these esters is the only one still on the market?
Definition
benzocaine
Term
What is procain(Novacain)?
Definition
an ester anesthetic no longer on the market
Term
WHat are some examples of amide anesthetics? (5)
Definition
1.lidocaine
2.prilocaine
3.mepivscaine
4.articaine
5.bupivacaine
Term
What is the mechanism of action of local anesthetics?
Definition
block voltage-gated Na+ channels in peripheral nerves
Term
What does this cause?
Definition
the membrane to not be able to easily depolarize and this prevents transmission of pain signals to the CNS
Term
Are smaller or larger fibers affected by local anesthetics first?
Definition
smaller
Term
All local anesthetics are...
Definition
weak bases, lipophilic
Term
Are local anesthetics ionized at the normal oral pH?
Definition
no, they are nonionized at normal pH
Term
Is this a good thing? (that local anesthetics are nonionized at oral pH)
Definition
yes because this allows them to cross tissue membrane to get to the nerve (allows them to penetrate tissue)
Term
What is the absorption of local anesthetics?
Definition
depends on the tissue at the site of application(works well at neutral or basic pH, works bad at acidic pH)
Term
What is the distribution of local anesthetics?
Definition
lipophilic so throughout the body, can easily cross membranes
Term
What is the metabolism of local anesthetics(esters and amides)?
Definition
esters-metabolized by the plasma and liver
amides-metabolized by liver
Term
What is the excretion of local anesthetics?
Definition
renal
Term
What happens to local anesthetics given to someone with an infection?
Definition
drug is more ionized, so it cannot cross tissues to get to the nerves
Term
What is the best thing to do when someone with an infection needs a local anesthetic?
Definition
treat the infection first and then go get the work done that needs the anesthetics or use higher dose
Term
What do infections do to the body's overall pH?
Definition
lower it
Term
What do lower doses of local anesthetics effect?
Definition
fewer/smaller nerves
Term
What are some common CNS adverse effects of local anesthetics?
Definition
-Stimulation(tremors)
-depression(respiratory, cardiovascular)
Term
What are some adverse cardiovascular effects of local anesthetics?
Definition
arrhythmia
Term
What are some adverse local effects of local anesthetics?
Definition
hematoma(bruising), increased systemic effects
Term
What are some adverse effects associated with pregnancy and local anesthetics?
Definition
fetal heart effects
Term
What are some allergic reactions that can occur with local anesthetics?
Definition
full range from rash to anaphalaxis
Term
What is in local anesthetics that used for in dentistry?
Definition
1.the local anesthetic itself
2.as a vasoconstrictor
3.as an antioxidant
4.sodium hydroxide
5.sodium chloride
Term
How does the vascoconstritor effect of local anesthetics help in dentistry?
Definition
helps decrease systemic absoprtion, prolongs duration
Term
How does a local anesthetic being an antioxidant help in dentistry?
Definition
it prolongs the shelf life of the anesthetic
Term
How does a local anesthetic having sodium hydroxde help in dentistry?
Definition
helps adjust pH appropriately, makes local anesthetic have a basic pH so it can cross membranes
Term
How does a local anesthetic having sodium chloride help in dentistry?
Definition
to make sodium isotonic to tissues
Term
What lidocaine?
Definition
a common dental amide anesthetic, almost always paired with epinephrine
Term
What are some brand names of lidocaine?
Definition
-Xylocaine
-Octocaine
Term
What is the % solution for injections of lidocaine?
Definition
2%, varies for other formulations
Term
Who is lidocaine preferred for?
Definition
pregnant patients, cat B
Term
What is the onset like with lidocaine? What about the duration?
Definition
-rapid onset
-medium duration(60-90 mins after injection)
Term
Does lidocaine work well? WHat are some adverse effects?
Definition
-good anesthetic effect
-hypotension
-sedation
-positional headache
-shivering
-CNS depression
-cardiovascular effects
Term
What is the % lidocaine with epinephrine for injections?
Definition
2% w/epinephrine, for infiltration and blocks
Term
What is the % lidocaine with topical use? What is the onset like?
Definition
-5% ointment
-rapid onset
Term
What is the % lidocaine with topical(viscious)?
Definition
2% gel
Term
What is the % lidocaine with spray?
Definition
8-10% oral spray
Term
What is the % lidocaine with a patch? How long does it take to work?
Definition
-5% onset of ~10 mins
Term
What is mepivacaine?
Definition
another common dental amide anesthetic
Term
What are some brand names of mepivacaine?
Definition
-Carboncaine
-Isocaine
Term
Is Carbocaine paired with a vascoconstritor? Why does it have side effects?
Definition
no, it has side effects because it is a 3% drug
Term
What is Isocaine paired with? What % is it?
Definition
paired with levondefrin as a vascoconstrictor at 2%
Term
What is mepivacaine similar to? Is it as effective for topical use?
Definition
similar to lidocaine, but not effective for topical use
Term
What are the benefits of a plain solution of mepivacaine rather than having it paired with a vascoconstrictor?
Definition
-shorter duration of action
-more likely to cause systemic effects
Term
What is prilocaine?
Definition
another common amide anesthetic used in dental offices
Term
What are the brand names of prilocaine?
Definition
-Citanest
-Citanest-Forte
Term
Is Cinanest paired wih epinephrine? What % is it?
Definition
-no epinephrine, 4%
Term
Is Citanest-Forte paired with epinephrine? What % is it?
Definition
yes, 4%, 1:200,000 epinephrine
Term
How does prilocaine compare to lidocaine? (3)
Definition
-less potent
-longer duration of action
-fewer cardiac effects
Term
What can prilocaine cause at high doses?
Definition
methemoglobinema
Term
What is articaine?
Definition
a local amide anesthetic
Term
What is the brand name for articaine? Is it paired with epinephrine?
Definition
-Septocaine
-4% solution, 1:100,000 epinephrne
Term
What is articaine like compared to other amide anesthetics?
Definition
more lipophilic, good anesthetisa effect
Term
What is the 1/2 life of articaine? Where is it primarily metabolized?
Definition
~20 mins
-primarily metabolized in the blood
Term
Is there a high risk of toxicity seen with articaine when reinjected?
Definition
no, there is a low risk of toxicity when reinjected
Term
What is bupivacaine?
Definition
another common dental amide anesthetic
Term
What are the brand names of bupivacaine? (2) Are these paired with epinephrine?
Definition
-Marcaine
-Vivacaine
**both paired with epinephrine**
Term
What is the potency of the brand names of bupivacaine?
Definition
-Marcaine(0.5%, 1:200,000 epinephrine)
-Vivacaine(0.5%, 1:200,000 epinephrine)
Term
What is the duration of action like with bupivacaine?
Definition
long duration of action seen with low toxicity, effects seen long after surgery
Term
What type of procedures is bupivacaine good for?
Definition
long procedures like:
-full mouth reconstruction
-implants
-extensive periodontal treatments
Term
How do local anesthetics work? What will an increase in local anesthetic do?
Definition
-block neurons from sending pain signals, so there is no pain felt
-block voltage gated Na+ channels
-increase in anesthetic will diffuse away from area quickly
Term
What do vascoconstrictors do when paired with anesthetics? (4)
Definition
-increase duration of action at injection site
-decrease systemic distribution
-reduces bleeding
-may allow for lower dose of local anesthetic
Term
What are two types of vascoconstrictors?
Definition
-epinephrine
-levonodefirin
Term
What do both of these bascoconstrictors do? What type of drug are they?
Definition
-both agonists
-both stimulate sympathetic system effectors
Term
What causes vascoconstriction with epinephrine?
Definition
Beta2 stimultion at low doses
Term
What causes vascoconstriction of smooth muscle at high doses with epinephrine?
Definition
Alpha1 stimulation
Term
What is epinephrine used at?
Definition
-1:50,000
-1:100,000
-1:200,000
Term
What does epinephrine used at 1:50,000 cause?
Definition
hemostasis(stops bleeding)
Term
What does Levonordefrin cause?
Definition
-alpha 1 stimulation that produces vascoconstriction
-increased blood pressure(this is why is it not used as much)
Term
What is Levonordefrin used at?
Definition
1:20,000, it is a lower potency so it is given in higher doses
Term
What dose of vascoconstrictors should a cardiac patient stay under?`
Definition
0.04 mg vascoconstrictor, this is 2 cartridges of local+1:100,000 epinephrine
Term
Which conditions should we wait to get under better control before undergoing elective procedures?
Definition
-severe cardiovascular disease
-uncontrolled high blood pressure
-MI or stroke within 6 months
Term
What are some medical conditions that contridict the use of vascoconstrictors or local anesthetics?
Definition
-recent MI(<1 month)
-high risk arrhythmia
-severe or uncontrolled hypertension
-unstable angina
-pts taking digoxin
-uncontrolled diabetes
-uncontrolled hyperthyroidism
-mod-severe asthma
-allergy
-phenochromocytoma
-drug abuse
Term
What are some antidepressant drugs that interact with epinephrine? (2) Why?
Definition
-tricyclic antidepressants
-MAOI antidepressants
**can cause increased blood pressure**
Term
What are some tricyclic antidepressants that react with epinpehrine?
Definition
-Amitriptyline(Elavil)
-Imipramine(Tonfranil)
Term
What are some tricyclic antidepressants that react with epinpehrine?
Definition
-Amitriptyline(Elavil)
-Imipramine(Tonfranil)
Term
What are some MAOI antidepressants that interact with epinpehrine?
Definition
-phenelzine(Nardil)
-isocarboxazid(Marplan)
Term
What is an example of a Beta blocker that reacts with epinephrine? What does it cause?
Definition
-propranolol (Inderal)
**causes increased blood pressure and bradycardia**
Term
What are two examples of a antidiabetic medication that reacts with epinephrine? What does it cause?
Definition
-metformin(Glucophage)
-sulfonylureas
**caused increased blood glucose**
Term
Do topical anesthetics usually cause allergic reactions?
Definition
no
Term
What are three topical anesthetics?
Definition
1.Benzocaine
2.Lidocaine
3.Lidocaine+prilocaine
Term
What are some brand names of benzocaine? (4)
Definition
-Hurricaine
-Obabase-B
-Orajel
-Anbesol
Term
What is the onset/duration of benzocaine products?
Definition
-onset is ~1 min
-duration is 15-45 mins
Term
What are some brand of lidocaine? What is the onset and duration like? What is the concentration like compared to benzocaine?
Definition
-Xylocaine
-onset 2-5 mins
-duration 15-45 mins
-lower concentration than benzocaine
Term
What is the brand of lidocaine+prilocaine?
Definition
Oraqix
Term
What is the onset and duration of Oraquix?
Definition
-onset is ~30 seconds
-duration 15-30 mins
Term
What type is anesthesia id Oraquix used for?
Definition
intrapocket anesthesia, best for those who perceive scaling as painful
Term
**see math for calculations of anesthetic doses**
Definition
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