Lec 2 Flashcards

(44 cards)

1
Q

Pharmacokinetics of LA is

A

Uptake
Distribution
Metabolism(biotransformation)
Excretion

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2
Q

All la possess some degree of

A

All la possess some degree of
Vasoactivity

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3
Q

Ester local anesthetics are potent ___ drugs

A

Vasodilating

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4
Q

The most potent vasodilator

A

Procaine

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5
Q

The only anesthetic that consistently produce vasoconstriction

A

Cocaine

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6
Q

Vasodilation leads to increase in ?

A

Increase rate of absorption of la in blood
Decreasing duration and depth of anesthesia
Increase chance of overdose

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7
Q

Routes for administration of la

A

Oral route
Topical route
Injection

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8
Q

Reason for all la absorbed properly?

A

High first pass metabolism

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9
Q

When you apply topical route on intact skin it’s produces

A

When you apply topical route on intact skin it’s produces
No anesthetic action

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10
Q

Emla is

A

Mixture of local anesthetics lidocaine and prilocaine capable of providing surface anesthetics of intact skin

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11
Q

Commonly used route for administration of LA

A

Injection

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12
Q

Uptake of la after parenteral administration depends on

A

Vascularity of injection site
Vasoactivity of drug

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13
Q

Iv time (min)

A

1

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14
Q

Topical time

A

5

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15
Q

Intrammandar-me

A

5-10

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16
Q

Subcutaneous time

A

30 - 90

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17
Q

Brain head liver lungs kidney and spleen have hugh levels of LA due to their

A

High level of perfusion

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18
Q

____ has the highest level bcos it has the largest mass of tissue in body

A

Skeletal muscle

19
Q

Blood level of LA is influenced by

A

Rate at which drug is absorbed into CVS
Rate of distribution from the vascular compartment to the tissues
Elimination of drug through metabolic or excretory pathways

20
Q

Elimination half life is the

A

Rate at which local anesthetic is removed from the blood the time neceassary for 50% reduction in the blood level

21
Q

All las can cross the

A

Blood brain barrier and placenta( cannot give prilocaine)

22
Q

Metabolism is the mechanism by which

A

Metabolism is the mechanism by which
The body biologically transforms the active drug into one that is pharmacologically inactive

23
Q

The overall toxicity of a drug depends on a balance between its

A

Rate of absorption into the blood stream at site of injection and its
Rate of removal from the blood through the processes of tissue uptake and metabolism

24
Q

Ester metabolized in

25
Amides metabolized in
Liver
26
Esters la hydrolyzed in plasma by enzyme
Esters la hydrolyzed in plasma by enzyme Pseudocholinesterase
27
Slow hydrolysis means
High toxicity
28
Rate of hydrolysis related to
Rate of hydrolysis related to degree of Toxicity
29
Which is hydrolyzed slowest
Which is hydrolyzed slowest Tetracaine
30
Chloroprocaine rate of hydrolysis
4.7
31
Procaine rate of hydrolysis
1.1
32
Tetracaine rate of hydrolysis
0.3
33
Ester broken into
Paraaminobenzoic acid and Dimethyl amino alcohol
34
Primary site of metabolusm of amide la is
Liver
35
Prilocaine is metabolized in
Liver and lung its a secondary amine
36
Rate of metabolism is greatly affected by
Liver function Hepatic perfusion
37
Relative contraindication to use of amide La
Significant liver dysfunction or heart failure
38
Why does articaine has a shorter half life
A portion of its metablusm occurs in ththe blood by plasma cholinesterase
39
Whats a relative contraindication
Drug in question maybe given to the patient after carefully weighing risks and benefits
40
Whats an absolute contraindication
Under no circumstance shoulf this drug be administered
41
Major excretory organs for both LA
Kidneys
42
Do esters appear in urine
In v small concentrations this is bcos they are almsot hydrolyzed in plasma
43
Procaine(novocaine) appears in urine as
90% paba and 2% unchanged
44
10% of cocaine is found unchanged in urine undergoing dialysis bcos
10% of cocaine is found unchanged in urine undergoing dialysis bcos Unavle to excrete unchanged poryion ot esters or amides Thus increasing toxicity