Part 2-PharmacoKinetics

Question 1

What is the MOST potent vasodilator?

Answer 1

PRO-caine

Question 2

What is the ONLY LA that produces vasoconstriction?

Answer 2

Co-caine

Question 3

Co-caine: Prohibits uptake of _________ (especially ______) into tissue binding sites

Answer 3

catecholaimes (esp NOR EPI)

Question 4

LA- _____ route = poorly absorbed from GI tract (except for cocaine) Also significant _____ effect

Answer 4

ORAL…first-pass

Question 5

LA- Topical route = different rates of absorption on

mucous membranes Ineffective on intact skin (barrier) Need _________ or damaged tissue

Answer 5

mucous membrane

Question 6

Which route are we as dentists going to use most? (general name and sub-category pleeeeease)

Answer 6

Par-enteral Route….SUB-CUTANEOUS injection

Question 7

Highly ______ organs obtain higher blood levels of LA

Answer 7

perfused

Question 8

________ contains greatest percentage of LA (largest mass of tissue in body) even though not as highly perfused!!!

Answer 8

Skeletal muscle

Question 9

LA READILY crosses the _______ and the _______

Answer 9

blood brain barrier and the placenta

Question 10

Healthier people can redistribute the drug more quickly, leading to ______ blood levels

Answer 10

lower

Question 11

What order kinetics do LA’s follow? How many .5 lives?

Answer 11

1st Order Kinetics…..4 to 5 half lives

Question 12

SO, Esters are metabolized in the blood by pseudocholinesterase, what is the SOMETIMES allergenic metabolite? how is it excreted?

Answer 12

PABA…excreted in urine

Question 13

Atypical pseudocholinesterase is an INHERITED disorder where a person cannot hydrolyze the ester LA….is this a relative or absolute contraindication?

Answer 13

relative contra

Question 14

What are two examples of Pts that are going to have a hard time metabolizing amide LAs c/o less hepatic blood flow….?

Answer 14

Hypotension and Congestive Heart Failure

Question 15

Is significant live dysfunction or heart failure an absolute or relative contraindication to amide LA use?

Answer 15

Relative contra

Question 16

Rates of biotransformation of amides are relatively ______

Answer 16

SIMILAR!!

Question 17

WHAT is the crazy amide LA that undergoes metabolism in the liver AND some in the LUNG??

Answer 17

PRI-LO-caine

Question 18

What can happen with inefficient metabolism of prilocaine? (the metabolite-orthotoluidine goes free)

Answer 18

Leads to Pt turning BLUE!!! Methemoglobinemia!!

Question 19

What can happen with inefficient metabolism of Lidocaine?

Answer 19

Metabolites cause SEDATION!!!

Question 20

What organ excretes LA and its metabolites?

Answer 20

KIDNEYS

Question 21

_____: type of LA appear in very small concentrations in urine

Answer 21

ester

Question 22

______: type of LA are present in urine as a parent compound in greater percentage than esters (but still small amount)

Answer 22

amide

Question 23

Is kidney disease (and therefore DIABETES) a relative or absolute contraindication to LA?

Answer 23

RELATIVE!!

Question 24

Systemic actions of LAs are related to ______/_____ level

Answer 24

blood/plasma

Question 25

What is the pharmacological action of LA once it crosses the BBB?

Answer 25

CNS depression

Question 26

Although toxicity of LA can cause CNS depression, what is the main manifestation of O.D. in the CNS (immediate) and why!!!??

Answer 26

generalized tonic-clonic SEIZURES....becuase LA INHIBITS inhibition in CNS!!

Question 27

Some LA have _________ properties... Blood level is lower than that which produces seizures􏰀 Used to treat epilepsy

Answer 27

anticonvulsant

Question 28

What is the pharmacological action of LA on the heart? Which LA is used as an anti-arrhythmic med?

Answer 28

Myocardial depression...LIDOcaine!!

Question 29

What basic CVS effect can LAs exhibit?

Answer 29

hypotension

Question 30

More in depth-CVS effects of LA-Non-overdose levels = slight increase or no change in _____ due to increased CO and HR

Answer 30

BP

Question 31

More in depth-CVS effects of LA- Approaching overdose levels, but still below = mild ________

Answer 31

hypotension

Question 32

More in depth-CVS effects of LA- At overdose levels = profound ________ caused by decreased myocardial contractility, decreased CO and decreased peripheral resistance (SHOCK)

Answer 32

hypotension

Question 33

At lethal levels = cardiovascular collapse; massive peripheral ________,

Answer 33

vasodilation

Question 34

Which LA may produce fatal ventricular fibrillation at overdose levels

Answer 34

BU-piv-acaine

Question 35

_________ more sensitive to irritating properties of LA than other tissues....Localized damage...DONT worry! its reversible after __ weeks!!

Answer 35

Skeletal muscle...2 weeks

Question 36

LA respiratory effect: At non-overdose levels = direct _______ action on bronchial smooth muscle

Answer 36

RELAXANT

Question 37

LA respiratory effect: At overdose levels = respiratory arrest due to generalized CNS ________

Answer 37

depression

Question 38

Malignant _________ = genetic variant that increases an individual’s susceptibility to this disorder in response to certain drugs

Answer 38

hyperthermia