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CC 2 LEC FINALS > TDM PART 1 > Flashcards

TDM PART 1 Flashcards

1
Q

Delivery of drug is through the rectum

A

Suppository

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2
Q

Pharmacological Parameters that determine Serum Drug
Concentration

A

LIBERATION
ABSORPTION
DISTRIBUTION
METABOLISM
EXCRETION

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3
Q

Passive diffusion requires the drug to be ___
in state

A

hydrophobic

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4
Q

If branded medicines, the ___is different
from the generic ones.

A

formulation

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5
Q

Drugs absorbed from the intestine enter the ____

A

portal hepatic
system

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6
Q

DRUG DISTRIBUTION
TABLETS AND CAPSULES

A

DISSOLUTION

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7
Q

DRUG DISTRIBUTION
LIQUID

A

RAPID ABSORPTION

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8
Q

DRUG DISTRIBUTION
WEAK ACIDS

A

STOMACH

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9
Q

DRUG DISTRIBUTION
WEAK BASE

A

SMALL INTESTINE

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10
Q

FACTORS AFFECTING ABSORPTION RATE

A

IPIFAPPO

Intestinal motility
pH
Inflammation
Food intake
Age
Pregnancy
Pathologic conditions
Other drug

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11
Q

An index used to describe the distribution characteristics
of a drug

A

VOLUME DISTRIBUTION

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12
Q

🔊D is the ___
➔ Either in mg or grams

A

Injected Dose

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13
Q

FORMULA

A

Vd = D/C

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14
Q

C is the ____
➔ Expressed either mg/L or g/L

A

concentration of drug in the Plasma

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15
Q

Unit for Vd =

A

Liter

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16
Q

○ Capable of entering biochemical pathway

A

Xenobiotics:

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17
Q

Except for the ____, all substances absorbed from the intestine
enter the hepatic portal system, which means that all medications
absorbed from the GIT must first pass via the liver before reaching
the bloodstream.

A

rectum

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18
Q

🔊Biochemical Pathway that is important for drug to be metabolized

A

MFO (Mixed Function Oxidase) System

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19
Q

In the liver, it is converted into___

A

water soluble
substances

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20
Q

MFO (Mixed Function Oxidase) System

A

-Takes hydrophobic substances
-Conversion of substance into a water soluble substances
-Transported into the bile or released into the general
circulation for elimination

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21
Q

🔊Elimination is through ___

A

renal filtration

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22
Q

🔊Two functional Phases of the MFO system

A

A mechanism for transforming hydrophobic compounds into
water-soluble ones. The end products of this process are either
delivered to the bile or discharged into the bloodstream.

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23
Q

Generates reactive intermediates

A

PHASE 1 REACTION

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24
Q

Combine functional groups to these reactive sites

A

PHASE2 REACTION

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25
Q

Most common substrate:

A

xenobiotics

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26
Q

Faster elimination, the ____of the drug

A

shorter half-life

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27
Q

Slow elimination, the___of the drug.

A

longer half-life

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28
Q

Elimination rate of free drug is ____ to GFR

A

directly
proportional

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29
Q

not bound to protein

A

Free drug

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30
Q

Metabolism of drugs occurs in the___

A

liver

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31
Q

Serum constituents:

A

Protein

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32
Q

What is the role of proteins in the binding of drugs? Why does the
drug need to bind with proteins?

A

Proteins act as carriers or transporters of drug to the
target site

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33
Q

What will happen if GFR is elevated, what will be the elimination
rate?

A

Increased elimination rate

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34
Q

Decreased GFR, decreased elimination rate, what happens to the
half life of a drug? Will it be prolonged or shortened?

A

Half life is Prolonged.

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35
Q

Capable of interacting with the site of action to elicit
biologic response
● Best correlates with both the therapeutic and toxic effects
of a drug (active fraction)

A

UNBOUND DRUG FRACTIONS

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36
Q

When will those toxic effects happen in the patient?

A

-Experienced if there is HIGH FREE DRUG FRACTION.
-Drug is not seen as effective even if it is in the therapeutic
range

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37
Q

🔊 One of the major factor that can affect on the amount of free
fractions of drug:

A

Concentration of Serum Proteins

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38
Q

CAUSES OF DRUG TOXICITY

A

● Increased concentration of free drug

● Presence of active drug metabolites

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39
Q

🔊Part of drug dose that reaches circulation

A

● Bioavailable Fraction

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40
Q

Dilution of drug after it has been distributed in the body

A

Drug Vd

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41
Q

Drugs pass through liver which loses a fraction of its
bioavailability before reaches the bloodstream

A

First- Pass Hepatic Metabolism

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42
Q

Half Life is also known as

A

Elimination Constant

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43
Q

Relationship between the concentration of a drug at the
site of action (target site) and response of tissue

A

Pharmacodynamic

44
Q

Study of genes which contribute to performance of drug
in an individual

A

Pharmacogenomics

45
Q

🔊Relationship of drug dose and level of drug in the
circulation

A

Pharmacokinetics

46
Q

Ratio between minimum toxic and maximum
therapeutic serum concentration

A

Therapeutic index

47
Q

Difference between the highest and lowest effective
dosages of the drug

A

Therapeutic range

48
Q

🔊Lowest drug concentration obtained in the dosing
interval

A

Trough concentration

49
Q

Drug activity in the body that is affected by 4 factors

A

bsorption, Distribution, Metabolism, &
Excretion

50
Q

Simultaneous____ can only happen in a dosing
interval

A

distribution, elimination, &
absorption

51
Q

Increased serum drug concentration if

A

Absorption rate > distribution and elimination

52
Q

Can only determine oscillating action or
movement from maximum to minimum and back
to maximum drug concentration if there is a

A

dosing interval or Dosage Plan:

53
Q

Decreased serum drug concentration decreases

A

Elimination and distribution rate > absorption

54
Q

STEADY STATE OSCILLATION: 🔊

A

We cannot measure peak concentration if it’s only a
single dose.

55
Q

Needs about ____before we reach steady
state oscillation

A

5-7 doses

56
Q

In general, peak concentration is ___ after the
administration

A

an hour

57
Q

🔊Benefit from the drug & achieve the therapeutic benefit
of the drug

A

Responders

58
Q

Patients who fail to experience the benefits and
therapeutic effect of drug

A

Non-responders 🔊

59
Q

🔊Effectiveness of drugs is dependent on the ____
of a patient.

A

genetic characteristics

60
Q

🔊Drugs needed to improve the function of the heart

A

CARDIOACTIVE DRUGS

61
Q

Only have ___ that needs to be
monitored

A

Cardiac Glycoside and
Antiarrhythmic drugs

62
Q

CARDIOACTIVE DRUGS

A

3D2PQ

  1. Digoxin
  2. Digitoxin
  3. Propranolol
  4. Quinidine
  5. Procainamide
  6. Disopyramide
63
Q

DIGOXIN

A

2 hrs

64
Q

DIGITOXIN

A

4-6 hrs

65
Q

PROPRANOLOL

A

3 hrs

66
Q

PROCAINAMIDE

A

3-5 hours

67
Q

QUINIDINE

A

5-12 hours

68
Q

LIDOCAINE

A

2 hours

69
Q

Cardiac glycoside for CHF (Congestive Heart Failure)
treatment

A

DIGOXIN

70
Q

DIGOXIN Suppresses

A

intracellular potassium K+

71
Q

DIGOXIN Increased in ___

A

intracellular Calcium in the cardiac
myocytes

72
Q

_____to proteins are delivered to
the muscles or cardiac myocytes to elicit its
function

A

Digoxin not bound

73
Q

DIGOXIN
PEAK LEVEL EVALUATION:

A

8-10 hours after an oral
dose

74
Q

PROPRANOLOL
TOXIC LEVEL

A

Toxic Level: > 100 ng/mL

75
Q

DIGITOXIN
TOXIC LEVEL

A

Toxic level: >25 ng/mL

76
Q

2 MOST COMMON FORMULATION
QUINIDINE

A

Quinidine sulfate
Quinidine gluconate

77
Q

Peak Serum Concentrations
Quinidine sulfate
Quinidine gluconate

A

Quinidine sulfate: 2-hours after an or oral dose 🔊 In its evaluation, we have to wait 2 hours after an oral
dose
● Quinidine gluconate: 4-5 hours after an oral dose 🔊In its evaluation, we have to wait 4-5 hours after an
oral dose

78
Q

Cont. Quinidine
Therapeutic range
Toxic level:

A

Therapeutic range
○ 2.3 - 5 ng/mL
● Toxic level:
○ >5 ng/mL

79
Q

Cont. Quinidine
Metabolism happens in the liver through ___

A

acetylation

80
Q

After metabolism of quinidine , the product is
____

A

n-acetylprocainamide

81
Q

PROCAINAMIDE
● Toxic level:

A

○ >12 ng/mL

82
Q

Used as a substitute for quinidine

A

DISOPYRAMIDE

83
Q

➔ Prolonged half life leads to ___

A

increased serum concentration
◆ Increase concentration leads to adverse effects
of the drug

84
Q

🔊Undergoes metabolism in the liver through dealkylation.

A

LIDOCAINE

85
Q

We have 2 forms of antibiotics that requires TDM or that their
concentrations be monitored

A

Aminoglycosides
Vancomycin

86
Q

Treatment of infections caused by gram negative bacteria

A

○ Gentamicin
○ Tobramycin
○ Amikacin
○ Kanamycin

87
Q

● Ototoxicity

A

○ Hearing and balance impairment

88
Q

○ Electrolyte imbalance and proteinuria

A

Nephrotoxicity

89
Q

Treatment of gram positive cocci and bacilli infection

A

VANCOMYCIN

90
Q

VANCOMYCINToxic effects:

A

○ Red man syndrome
○ Nephrotoxicity
○ Ototoxicity

91
Q

Anticonvulsants

A

: Anti epileptic drugs or AED

92
Q

Anti epileptic drugs or AED
Specimen:

A

Trough serum concentration

93
Q

Stabilizes the neuronal membranes

A

PHENOBARBITAL

94
Q

PHENOBARBITAL

A

Half life: 70-100 hours
Therapeutic range: 15-40 ug/mL
Toxic level: >40 ug/mL
Peak concentration
○ 10 hours after an oral dose
Administration: oral
Elimination: hepatic metabolism or Liver
Dosing interval: 10-15 days

95
Q

Block Na and Ca influx into neurons

A

PHENYTOIN

96
Q

DIFFERENCE OF CALCIUM WHEN ENTERS
DIGOXIN
PHENYTOIN

A

Digoxin inhibits ATPase enzyme
◆ Lower concentration of potassium inside the cell
particularly the cardiac myocytes
➔ Results to more room for calcium to enter
➔ Once calcium enters cardiac myocytes and increases its
concentration, there will be decreased excitability
🔊For Phenytoin, it is the opposite of Digoxin.
➔ Inhibits the entry of sodium and calcium into the neurons
◆ Results to decreased excitability of the neurons
◆ Prevents the convulsions and epilepsy

97
Q

PHENYTOIN

A

Half life: 12-36 hours
● Therapeutic range: 10-20 ug/mL
● Toxic level: >20 ug/mL
Elimination: hepatic metabolism
Administration route: oral /intravenous

98
Q

PHENYTOIN OTHER NAME

A

“Dilantin” 🔊 Other name

99
Q

injectable form of phenytoin

A

Fosphenytoin:

100
Q

🔊Majority of phenytoin is bound to protein
➔ About____ bound to protein

A

87 - 97%

101
Q

What happens to the level of the active or unbound portion of
phenytoin?

A

➢ Increase of unbound fraction and serum concentration

102
Q

VALPROIC ACID
● Enhances

A

GABA-mediated inhibitory system

103
Q

VALPROIC ACID

A

Half-Life: 8-15 hours
● Therapeutic Range: 50-100 ug/mL
● Toxic Level: >100 ug/mL
🔊 Valproic Acid is administered orally
● Rapid and complete absorption in the GIT

➔ 7% not bound to protein
● Elimination: Hepatic metabolism

104
Q

OTHER NAME OF VALPROIC ACID

A

● “Depakene” 🔊Other name

105
Q

Indications: treatment of petit mal or absence seizure
condition

A

VALPROIC ACID

106
Q

🔊 Majority of valproic acid is bound to protein, about____

A

93%

CC 2 LEC FINALS (8 decks)

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