TDM PART 1 Flashcards
1
Q
Delivery of drug is through the rectum
A
Suppository
2
Q
Pharmacological Parameters that determine Serum Drug
Concentration
A
LIBERATION
ABSORPTION
DISTRIBUTION
METABOLISM
EXCRETION
3
Q
Passive diffusion requires the drug to be ___
in state
A
hydrophobic
4
Q
If branded medicines, the ___is different
from the generic ones.
A
formulation
5
Q
Drugs absorbed from the intestine enter the ____
A
portal hepatic
system
6
Q
DRUG DISTRIBUTION
TABLETS AND CAPSULES
A
DISSOLUTION
7
Q
DRUG DISTRIBUTION
LIQUID
A
RAPID ABSORPTION
8
Q
DRUG DISTRIBUTION
WEAK ACIDS
A
STOMACH
9
Q
DRUG DISTRIBUTION
WEAK BASE
A
SMALL INTESTINE
10
Q
FACTORS AFFECTING ABSORPTION RATE
A
IPIFAPPO
Intestinal motility
pH
Inflammation
Food intake
Age
Pregnancy
Pathologic conditions
Other drug
11
Q
An index used to describe the distribution characteristics
of a drug
A
VOLUME DISTRIBUTION
12
Q
🔊D is the ___
➔ Either in mg or grams
A
Injected Dose
13
Q
FORMULA
A
Vd = D/C
14
Q
C is the ____
➔ Expressed either mg/L or g/L
A
concentration of drug in the Plasma
15
Q
Unit for Vd =
A
Liter
16
Q
○ Capable of entering biochemical pathway
A
Xenobiotics:
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
18
Q
🔊Biochemical Pathway that is important for drug to be metabolized
A
MFO (Mixed Function Oxidase) System
19
Q
In the liver, it is converted into___
A
water soluble
substances
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
21
Q
🔊Elimination is through ___
A
renal filtration
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.
23
Q
Generates reactive intermediates
A
PHASE 1 REACTION
24
Q
Combine functional groups to these reactive sites
A
PHASE2 REACTION
25
Most common substrate:
xenobiotics
26
Faster elimination, the ____of the drug
shorter half-life
27
Slow elimination, the___of the drug.
longer half-life
28
Elimination rate of free drug is ____ to GFR
directly
proportional
29
not bound to protein
Free drug
30
Metabolism of drugs occurs in the___
liver
31
Serum constituents:
Protein
32
What is the role of proteins in the binding of drugs? Why does the
drug need to bind with proteins?
Proteins act as carriers or transporters of drug to the
target site
33
What will happen if GFR is elevated, what will be the elimination
rate?
Increased elimination rate
34
Decreased GFR, decreased elimination rate, what happens to the
half life of a drug? Will it be prolonged or shortened?
Half life is Prolonged.
35
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)
UNBOUND DRUG FRACTIONS
36
When will those toxic effects happen in the patient?
-Experienced if there is HIGH FREE DRUG FRACTION.
-Drug is not seen as effective even if it is in the therapeutic
range
37
🔊 One of the major factor that can affect on the amount of free
fractions of drug:
Concentration of Serum Proteins
38
CAUSES OF DRUG TOXICITY
● Increased concentration of free drug
● Presence of active drug metabolites
39
🔊Part of drug dose that reaches circulation
● Bioavailable Fraction
40
Dilution of drug after it has been distributed in the body
Drug Vd
41
Drugs pass through liver which loses a fraction of its
bioavailability before reaches the bloodstream
First- Pass Hepatic Metabolism
42
Half Life is also known as
Elimination Constant
43
Relationship between the concentration of a drug at the
site of action (target site) and response of tissue
Pharmacodynamic
44
Study of genes which contribute to performance of drug
in an individual
Pharmacogenomics
45
🔊Relationship of drug dose and level of drug in the
circulation
Pharmacokinetics
46
Ratio between minimum toxic and maximum
therapeutic serum concentration
Therapeutic index
47
Difference between the highest and lowest effective
dosages of the drug
Therapeutic range
48
🔊Lowest drug concentration obtained in the dosing
interval
Trough concentration
49
Drug activity in the body that is affected by 4 factors
bsorption, Distribution, Metabolism, &
Excretion
50
Simultaneous____ can only happen in a dosing
interval
distribution, elimination, &
absorption
51
Increased serum drug concentration if
Absorption rate > distribution and elimination
52
Can only determine oscillating action or
movement from maximum to minimum and back
to maximum drug concentration if there is a
dosing interval or Dosage Plan:
53
Decreased serum drug concentration decreases
Elimination and distribution rate > absorption
54
STEADY STATE OSCILLATION: 🔊
We cannot measure peak concentration if it’s only a
single dose.
55
Needs about ____before we reach steady
state oscillation
5-7 doses
56
In general, peak concentration is ___ after the
administration
an hour
57
🔊Benefit from the drug & achieve the therapeutic benefit
of the drug
Responders
58
Patients who fail to experience the benefits and
therapeutic effect of drug
Non-responders 🔊
59
🔊Effectiveness of drugs is dependent on the ____
of a patient.
genetic characteristics
60
🔊Drugs needed to improve the function of the heart
CARDIOACTIVE DRUGS
61
Only have ___ that needs to be
monitored
Cardiac Glycoside and
Antiarrhythmic drugs
62
CARDIOACTIVE DRUGS
3D2PQ
1. Digoxin
2. Digitoxin
3. Propranolol
4. Quinidine
5. Procainamide
6. Disopyramide
63
DIGOXIN
2 hrs
64
DIGITOXIN
4-6 hrs
65
PROPRANOLOL
3 hrs
66
PROCAINAMIDE
3-5 hours
67
QUINIDINE
5-12 hours
68
LIDOCAINE
2 hours
69
Cardiac glycoside for CHF (Congestive Heart Failure)
treatment
DIGOXIN
70
DIGOXIN Suppresses
intracellular potassium K+
71
DIGOXIN Increased in ___
intracellular Calcium in the cardiac
myocytes
72
_____to proteins are delivered to
the muscles or cardiac myocytes to elicit its
function
Digoxin not bound
73
DIGOXIN
PEAK LEVEL EVALUATION:
8-10 hours after an oral
dose
74
PROPRANOLOL
TOXIC LEVEL
Toxic Level: > 100 ng/mL
75
DIGITOXIN
TOXIC LEVEL
Toxic level: >25 ng/mL
76
2 MOST COMMON FORMULATION
QUINIDINE
Quinidine sulfate
Quinidine gluconate
77
Peak Serum Concentrations
Quinidine sulfate
Quinidine gluconate
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
Cont. Quinidine
Therapeutic range
Toxic level:
Therapeutic range
○ 2.3 - 5 ng/mL
● Toxic level:
○ >5 ng/mL
79
Cont. Quinidine
Metabolism happens in the liver through ___
acetylation
80
After metabolism of quinidine , the product is
____
n-acetylprocainamide
81
PROCAINAMIDE
● Toxic level:
○ >12 ng/mL
82
Used as a substitute for quinidine
DISOPYRAMIDE
83
➔ Prolonged half life leads to ___
increased serum concentration
◆ Increase concentration leads to adverse effects
of the drug
84
🔊Undergoes metabolism in the liver through dealkylation.
LIDOCAINE
85
We have 2 forms of antibiotics that requires TDM or that their
concentrations be monitored
Aminoglycosides
Vancomycin
86
Treatment of infections caused by gram negative bacteria
○ Gentamicin
○ Tobramycin
○ Amikacin
○ Kanamycin
87
● Ototoxicity
○ Hearing and balance impairment
88
○ Electrolyte imbalance and proteinuria
Nephrotoxicity
89
Treatment of gram positive cocci and bacilli infection
VANCOMYCIN
90
VANCOMYCINToxic effects:
○ Red man syndrome
○ Nephrotoxicity
○ Ototoxicity
91
Anticonvulsants
: Anti epileptic drugs or AED
92
Anti epileptic drugs or AED
Specimen:
Trough serum concentration
93
Stabilizes the neuronal membranes
PHENOBARBITAL
94
PHENOBARBITAL
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
Block Na and Ca influx into neurons
PHENYTOIN
96
DIFFERENCE OF CALCIUM WHEN ENTERS
DIGOXIN
PHENYTOIN
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
PHENYTOIN
Half life: 12-36 hours
● Therapeutic range: 10-20 ug/mL
● Toxic level: >20 ug/mL
Elimination: hepatic metabolism
Administration route: oral /intravenous
98
PHENYTOIN OTHER NAME
“Dilantin” 🔊 Other name
99
injectable form of phenytoin
Fosphenytoin:
100
🔊Majority of phenytoin is bound to protein
➔ About____ bound to protein
87 - 97%
101
What happens to the level of the active or unbound portion of
phenytoin?
➢ Increase of unbound fraction and serum concentration
102
VALPROIC ACID
● Enhances
GABA-mediated inhibitory system
103
VALPROIC ACID
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
OTHER NAME OF VALPROIC ACID
● “Depakene” 🔊Other name
105
Indications: treatment of petit mal or absence seizure
condition
VALPROIC ACID
106
🔊 Majority of valproic acid is bound to protein, about____
93%
