Lec 2 Flashcards

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

A

Plasma

25
Q

Amides metabolized in

A

Liver

26
Q

Esters la hydrolyzed in plasma by enzyme

A

Esters la hydrolyzed in plasma by enzyme
Pseudocholinesterase

27
Q

Slow hydrolysis means

A

High toxicity

28
Q

Rate of hydrolysis related to

A

Rate of hydrolysis related to degree of
Toxicity

29
Q

Which is hydrolyzed slowest

A

Which is hydrolyzed slowest
Tetracaine

30
Q

Chloroprocaine rate of hydrolysis

A

4.7

31
Q

Procaine rate of hydrolysis

A

1.1

32
Q

Tetracaine rate of hydrolysis

A

0.3

33
Q

Ester broken into

A

Paraaminobenzoic acid and
Dimethyl amino alcohol

34
Q

Primary site of metabolusm of amide la is

A

Liver

35
Q

Prilocaine is metabolized in

A

Liver and lung its a secondary amine

36
Q

Rate of metabolism is greatly affected by

A

Liver function
Hepatic perfusion

37
Q

Relative contraindication to use of amide La

A

Significant liver dysfunction or heart failure

38
Q

Why does articaine has a shorter half life

A

A portion of its metablusm occurs in ththe blood by plasma cholinesterase

39
Q

Whats a relative contraindication

A

Drug in question maybe given to the patient after carefully weighing risks and benefits

40
Q

Whats an absolute contraindication

A

Under no circumstance shoulf this drug be administered

41
Q

Major excretory organs for both LA

A

Kidneys

42
Q

Do esters appear in urine

A

In v small concentrations this is bcos they are almsot hydrolyzed in plasma

43
Q

Procaine(novocaine) appears in urine as

A

90% paba and 2% unchanged

44
Q

10% of cocaine is found unchanged in urine undergoing dialysis bcos

A

10% of cocaine is found unchanged in urine undergoing dialysis bcos
Unavle to excrete unchanged poryion ot esters or amides
Thus increasing toxicity