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Flashcards in Pharmacokinetics Deck (29):
0

Narrow therapeutic drugs

CD FLP ST VW

1

Mass spectrometry

Gold standard of chromatography

2

PK info

Prescribing information

Clinical pharmacology of package insert

3

Goal of TDM

Better relationship between Cp and response than dose and response

Goal: optimize patients clinical outcomes by managing their medication regimen with measured drug concentrations

4

Pharmacodynamic markers

BP, cholesterol, coagulation time

5

High performance liquid chromatography

Lipophilic, stationary, long retention time

Hydrophilic, mobile, short retention time

6

Robustness

Rapid turnaround time

7

Specificity

Lack cross reactivity

8

Sensitivity

Detection of units nanograms

9

Concentration interpretation

Interpret after considering

Clinical response
Demographic and clinical status
Dosage regimen
PK characteristics of the drug

10

Transplant

Eye, blood easy

Lung difficult

11

Isograft

Genetically identical

12

Autograft

Same individual

13

Allograft

Same species

14

Cyclosporine ADME

Variable oral bioavailability
Highly bound to plasma lipoproteins
3A4 metabolism
Bile elimination

Monitor trough concentration for dose individualization

AE nephrotoxicity

No clear relationship between concentration and the risk of rejection

15

Tacrolimus

Incomplete and variable absorption
Food decreases absorption
Highly bound
Bile elimination

3A4 and 3A5 metabolism

AE: nephrotoxicity, neurotoxicity

Increased with PPI

16

3A5 metabolism

African American have more functional 3A5 and can metabolize tacrolimus better

17

Mycophenolic acid

MMF prodrug, teratogen

18

Sirolimus

mTOR inhibitor

Linear dose PK proportionality

3A4 metabolism, pgp efflux
Long half life, needs loading dose

19

3A4 inhibitors increase concentration

Erythro macrolides
CCB diltiazem verapamil
Azole antifungal
Grapefruit juice

20

3A4 inducers decrease concentration

Anticonvulsant pheny, pheno, carbamazepine

Glucocorticoids, rifampin, SJW

21

Theophylline

Antiinflammatory, steroid sparing
Half life shorter in children (higher clearance) higher Vd

Activates HDAC gene repression

Absorption is variable, not influenced by food
Binds to albumin
1A2 metabolism
Smoking increases clearance

22

Kidney metabolism

Water soluble molecules

GFR iohexol iothalamate gold standard

MDRD for staging CKD

Renal adjustment for drugs that are 30% renally eliminated

Renal dysfunction decreases 3A4

23

Liver metabolism

Metabolize lipophilic to more water soluble forms then renally eliminated

Child Pugh liver severity ABC
Hepatic encephalopathy
Ascites, albumin
Bilirubin, INR

24

Bile elimination

Non water soluble molecules

25

LogP

Positive lipophilic

Negative hydrophilic

26

Hemodialysis

Removes molecules <500D
Water soluble
Low Vd, unbound drugs

27

Continuous renal replacement

Up to 5000D

Can't remove large Vd drugs

Sieving coefficient closer to 1 has better passage across filter

28

Immunoassay

Enzyme linked