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FreakinLOCALanesthesia!!! > Part 2-PharmacoKinetics > Flashcards

Part 2-PharmacoKinetics Flashcards

1
Q

What is the MOST potent vasodilator?

A

PRO-caine

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2
Q

What is the ONLY LA that produces vasoconstriction?

A

Co-caine

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3
Q

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

A

catecholaimes (esp NOR EPI)

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4
Q

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

A

ORAL…first-pass

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5
Q

LA- Topical route = different rates of absorption on

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

A

mucous membrane

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6
Q

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

A

Par-enteral Route….SUB-CUTANEOUS injection

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7
Q

Highly ______ organs obtain higher blood levels of LA

A

perfused

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8
Q

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

A

Skeletal muscle

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9
Q

LA READILY crosses the _______ and the _______

A

blood brain barrier and the placenta

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10
Q

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

A

lower

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11
Q

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

A

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

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12
Q

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

A

PABA…excreted in urine

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13
Q

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

A

relative contra

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14
Q

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

A

Hypotension and Congestive Heart Failure

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15
Q

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

A

Relative contra

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16
Q

Rates of biotransformation of amides are relatively ______

A

SIMILAR!!

17
Q

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

A

PRI-LO-caine

18
Q

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

A

Leads to Pt turning BLUE!!! Methemoglobinemia!!

19
Q

What can happen with inefficient metabolism of Lidocaine?

A

Metabolites cause SEDATION!!!

20
Q

What organ excretes LA and its metabolites?

A

KIDNEYS

21
Q

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

A

ester

22
Q

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

A

amide

23
Q

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

A

RELATIVE!!

24
Q

Systemic actions of LAs are related to ______/_____ level

A

blood/plasma

25
Q

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

A

CNS depression

26
Q

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

A

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

27
Q

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

A

anticonvulsant

28
Q

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

A

Myocardial depression…LIDOcaine!!

29
Q

What basic CVS effect can LAs exhibit?

A

hypotension

30
Q

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

A

BP

31
Q

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

A

hypotension

32
Q

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

A

hypotension

33
Q

At lethal levels = cardiovascular collapse; massive peripheral ________,

A

vasodilation

34
Q

Which LA may produce fatal ventricular fibrillation at overdose levels

A

BU-piv-acaine

35
Q

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

A

Skeletal muscle…2 weeks

36
Q

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

A

RELAXANT

37
Q

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

A

depression

38
Q

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

A

hyperthermia

FreakinLOCALanesthesia!!! (11 decks)

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