Pharmacology chapter 6 & 7 – Flashcards

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question
What are the five general routes for the application of local anesthetic agents?
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a) Topical, by creams, patches, sprays, or lozenges b) Infiltration, by direct intradermal or subcutaneous injection into the tissue near the area of operation. c) Nerve block, by injection near a bundle of nerves (a "sensory nerve trunk"), to induce anesthetic and relieve pain or spasms along several nerve pathways e) Spinal, by direct injection into the subarachnoid space cerebral spinal fluid (CSF) in the lumbar area, to induce anesthesia in the nerve roots of the body's complete lower trunk. The density of the solution and the position of the patient affect the diffusion of the anesthetic. f) Epidural, by injection into the epidural space of the spinal column, primarily for anesthesia for labor and delivery; takes a relatively large amount of anesthetic to diffuse across the localized area.
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What is the mechanism of action for local anesthetics? Which electrolyte is involved?
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Local anesthetics bind to receptors near the sodium channel on the nerve membrane. As the amount of the local anesthetic accumulates, the sodium channels become obstructed. Impulses along the nerve slowed, the strength and propagation of the action potential are diminished, and communication along the fiber is blocked.
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What is the numeric value of physiological pH? Is it basic acidic or neutral?
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7.4; Basic
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Why is a local anesthetic less effective in the presence of inflammation?
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An oral infection with the accompanying inflammation can therefore, create a reduction in pH, which in turn can cause a local anesthetic to develop a charge, become polarized, and have diminished tissue penetration.
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What is the purpose of adding epinephrine to a local anesthetic?
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The addition of epinephrine not only minimizes the vasodilation caused by the local anesthetic agent, but causes vasoconstriction of the blood vessels in the area surrounding the injection. The vasoconstriction decreases perfusion of blood to the region, and the local anesthetic is not carried away.
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Which local anesthetic causes vasoconstriction without the addition of epinephrine? What is its historical significance?
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Novocaine; Historically, the esters represent the first collection of local anesthetic agents. They are more prone to cause allergic reactions among patients.
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Which patient population is most prone to problems when sulfites are used as preservatives?
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Patients with asthma are susceptible to sulfites known to cause bronchospasm.
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Which patient population is more likely to have excessive capillary constriction and tissue damage when epinephrine is used?
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Diabetes patients
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How many milligrams of epinephrine are contained in a 1.8mL cartridge when the stated dilution of epinephrine is 1:200,000?
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0.009mg
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How many milligrams of lidocaine are contained in a 1.8mL cartridge when the stated concentration is 2%.
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36mg.
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What are the two general categories of local anesthetics? Do cross-over allergies between these categories exist? Which category is more prone to allergic reactions?
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1- Esters 2- Amides these two categories do not have any cross-over effect between them; however, esters have a cross-over effect within the ester category. For example: A patient having an allergy to one ester-type anesthetic will probably have a cross-over allergy to other states.
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Which category is based on PABA? How are local anesthetics in this category metabolized?
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With the exception of cocaine, the local anesthetics of the ester class are all derivatives of para- aminobenzoic acid (PABA). The ester linkage is primarily hydrolyzed by plasma cholinesterase before going through further metabolism by the liver. The esters are excreted by the kidneys, nearly all as metabolites.
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The sulfonamide class of antibiotic's can have a drug interaction with which category of local anesthetics?
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Ester-type anesthetics
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A red flag should fly up when a patient states he is allergic "to Novocain" Why?
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Because patients often confuse panic reactions with allergies. When the patient describes his allergy as "palpitations," "cold perspirations," or even (fainting," chances are it's a panic reaction.
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Lidocaine is a prototype drug in which local anesthetics category?
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Amide class
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What drug allergy is a specific contraindication to the use of articaine?
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Patients with allergy to sulfur drugs.
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What is the name of a "natural" analgesic and anesthetics?
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Eugenol (oil of cloves) is use for topical application of clove oil depresses the function of sensory receptors by a powerful inhibition of prostaglandin biosynthesis. When applied topically, it causes local anesthetics and analgesia to the oral mucosa and in post-extraction alveolitis (dry socket).
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What is the name of an alternative anesthetic when a patient is allergic to drugs in the primary two categories?
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Anesthesia can be used by using diphenhydramine (Benadryl) injection.
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Which reflex may be blocked by the use of lidocaine as a topical anesthetic? Why is this a concern?
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The "gag reflex" can be blocked. This is a concern because if lidocaine is gargled, the body's natural reflex is to prevent inhaling, or aspiration, fluids and mucous into the lungs can be hindered.
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What is the best way to store local anesthetics agents?
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(1) Place the date of the first entry into the bottle (2) Note the number of times the viral has been used (3) Place a time limit on using the multiple-dose vial. (6-9 mths can be a guide)
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The (an) in anesthesia means what?
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without
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Esthesia in anesthesia means what?
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sensation
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1853: He was the first to permit the injection of small, measured volumes.
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Alexander Wood's
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1856: He proposed use of coco leaves as an anesthetic
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Samuel Percy
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What was the antiseptic used clinically?
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Lidocaine, 1948
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What are the uses of Local anesthetics in dentistry
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extractions, apical surgery, cyst removal, restorations, simple incise and drain
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What are the five routes of administration for using local anesthetics
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Topical, Infiltration, nerve block, spinal, epidural
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Topical anesthetic includes
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creams, patches, sprays, lozenges
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Infiltration anesthetic is what
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Subcutaneous or intradermal injection near area of operation, usually maxilla, in areas of infection, occasionally in mandibule.
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Nerve block anesthetic is what
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injection near a sensory trunk, serveral nerve pathways such as alveolar nerve, long buccal nerve, mental nerve
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spinal anesthetic is what
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into the sub arachnoid space of spinal column
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epidural does what as an anesthetic
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into the epidural space of the spinal column (labor and delivery)
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When impulses are generated by changes in the nerve's membrane permeability Sodium ions inflow across the nerve membrane causing what reaction?
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Action potential
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Action potential does what
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relays information along the nerve so there is communication between the Peripheral Nervous System and the CNS
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What happens to make anesthesia occur
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When the action potential is restricted the communication is blocked and if enough nerve is affected that is the anesthesia occurs.
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In its simplest terms where does local anesthetics bind?
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binds to receptors near the sodium channel on the nerve membrane
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As the amount of the local anesthetic accumulates, the sodium channels become obstructed the what happens
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Impulses along the nerve are slowed, the strength and propagation of the action potential are diminished and communication along the fiber is blocked.
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pH is a measure of what
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acid, base
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what is the pH that neutral
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7
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pH over 7 is what
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basic
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pH under 7 is what
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acidic
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Physiological pH is what and what does it mean
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7.4, meaning the body is slightly basic
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nonpolar charge are these with
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a negative charge
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non polar drugs have no charge this means that they are more
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lipophilic
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non polar drugs are those that do not have a charge, they are more readily
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absorbed by tissues
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If the environment into which a drug is deposited is altered, the drug may develop a
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charge
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Most local anesthetics are _______bases.
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weak
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The mechanism of action of local anesthetics is to
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block nerve conduction by preventing nerve depolarization
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Local anesthetics produce their primary effects by
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blocking nerve conduction
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Local anesthetics exert their action by
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interfering with the flow of sodium across neural membranes
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An infection in an area can prevent the accumulation of effective concentrations of local anesthetic solution because of
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low tissue pH.
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Patches anesthetics work best when the are applied
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on dried areas to soft tissues and to regaines that are not thickened by repeated use
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spray anesthetic have several limitations because
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difficult to control on small area, sufficient amounts could be inhaled to cause a toxic reactions
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Absorption across a mucous membrane is hampered due to the poor buffering nature of the tissue, meaning
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the mucosa environment can possess a pH as low as 5.5
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What are the best ways to prevent a toxic reaction from the administration of a local anesthetic is to
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being safe with family history, aspirate the syringe (draw back to make sure the capsule is fully engaged,
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What is a couple of reasons that local anesthetics help people
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It is very safe, fear is lessened
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What are some challenges in using local anesthetics
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Allergies to specific agents may emerge, vials contain preservatives known as (methylparaben, sulfites). Novacain which needs to be distinguished between allergies and anic reactions, syncope, side effects, etc.
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What are the best ways to prevent a toxic reaction from the administration of a local anesthetic
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through medical history, aspiration (make sure the syringe is fully engaged), use the least amount needed to reduce potential sensitivities or allergies, inject slowly, repeated injection in the same can cause vasoconstriction with epi., wait for the anes. to work, avoid infection/inflamed areas
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what causes an increased perfusion of blood to the injected area
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vasodilation
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what happens when vasodilation happens in ansthetics
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(1) the drug is being carried away (less effective), (2) anesthetic reaches the cardiac muscle with the potential for undesired myocardial effects.
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What is used in medical emergencies to decrease ventricular arrhythmias
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Lidocaine
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Patients with ____are predisposed to problems with capillary circulation. They may experience an increase in tissue damage.
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diabetes
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what is add is added to anesthetics in order to maintain effective concentrations of at the injection site
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epinephrine
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The ______decreases perfusion of blood to the region, and the local anesthetic is not carried away.
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vasoconstriction
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Epinephrine added to local anesthetics is expressed in terms of dilution, what are the dilution examples
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1:100,000 and 1:200,000, 1 gram per 100,000 or 1 gram per 200,000 1000mg/100,000ml 1mg/100ml so in 1.8ml of solution of local anesthetic there are .018mg of epinephine
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What is the oldest in the classification of anesthetics
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Esters
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what is the generic of Procaine: gets confusing when patients say they are allergic, hasn't been used in years
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Novacaine
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What is the action of epinephrine when combined with local anesthetic is to
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increase the duration of anesthetic
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What are the two classes of local anesthetics
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Esters and Amides
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A patient having an allergy to one of the ester-type anesthetics will probably have
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a cross-over allergy to other esters.
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What are the drugs in the Ester class
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Procaine (novocaine) short half-life, Chloroprocaine (Nesacaine) short half-life, Propoxycaine, Tetracaine, Benzocaine
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Despite its greater notoriety as a drug of abuse____is an excellent topical local anesthetic and can be legally prescribed
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cocaine
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What are local anesthetics
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Procaine- (Novacaine) short-half-life Chloroprocaine (Nesacaine) Propoxycaine- potent and toxic Tetracaine- topical Benzocaine- can sensitize pt's to all esters
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What NS does cocaine stimulate that others anesthetics does not.
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sympathetic
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The amide class of local anesthetics agents are metabolized where?
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in liver & excreted by the kidneys
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Why does cocaine work (by what addition)
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addition caused by dopamine accumulation which affects brain pleasure centers by cocaine blocking uptake of dopamine.
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Where are the Amides local anesthetics derived from?
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the dye aniline
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What are the routes for anesthetics
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topical: creams, patches, sprays infiltration: direct intradermal or subcutaeous nerve block: injection near bundle of nerves spinal: direct into cerebral spinal fluid (CSF) epidural: epidural space of spine: delveries
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What is the pH above and below 7
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7 is netrual, below is acidic and above is basic
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When a drug develops electrical charge, its considered___this makes it become less____.
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polarized, lipophilic
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What type of activity gives physiological pH the ability to have adequate penentration?
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lipophilic
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Epinephrine added to local anesthetics is expressed in what terms
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1:100,000 ml= .018mg of epinephrine
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What is the oldest classification of local anesthetics
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Esters
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The prototype agent in the Amides class is
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lidocaine
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An acidic environment is
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7 or below
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What are the ways that you can prevent toxic reactions from local anesthetics
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1- through medical hx 2-aspiration- make sure that the carpule is fully engaged. 3- Use least amount: reduce potential sensitivities or allergies 4- Inject slowly 5-Repeated injection in same area causes vasoconstriction 6- wait for anesthetic to work 7- avoid repeated injunction in same area/ inflamed area.
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What are the topical anes. forms
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patches-best used dry sprays- difficult to control
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The action potential relays information along the nerve so there is communication between the PNS and ____
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CNS. Action potentials are diminished and communication between the PNS and the CNS is blocked causing the anesthetic to work.
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Sodium ions inflow across the nerve membrane causing an ______.
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action potential.
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What are the toxicity/challenges in using local anesthetics
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-Very safe -people fear injections -allergies (methylparaben, sulfides)
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Local anesthetics should easily
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bn
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