Final - Pharmacokinetics

Question 1

Time to steady state

Answer 1

3-5 half lives

Question 2

Bioavailability of IV drugs

Answer 2

100%

Question 3

Context Sensitive Half Time

Answer 3

50% decrement time

Time reqd to reach 50% of concentration after infusion stopped

Question 4

Time delay between change in plasma concentration and drug effect

Answer 4

Hysteresis

Question 5

Volume of distribution

Answer 5

Vd=dose/concentration

Question 6

Who has larger Vd: 100kg male or 70kg female?

Answer 6

Larger person = larger Vd

Question 7

In critically ill, AAG leads to _____ fraction unbound drug, _____ Vd

Answer 7

Decreased

Decreased

Question 8

In critically ill, Albumin levels lead to ______ fraction unbound drug, _____ Vd

Answer 8

Increased

Increased

Question 9

Highly albumin bound Drugs

Answer 9

Propofol
Morphine
Propranolol
Verapamil

Question 10

Medium albumin bound Rx

Answer 10

Aspirin
Carvedilol
Omeprazole
Midazolam

Question 11

Low Albumin bound Rx

Answer 11

Carbamazepine
Ceftriaxone
Dexamethasone
Diazepam
Itraconazole
Phenytoin
Valproic Acid
Warfarin
Diltiazem

Question 12

Which drug form causes a clinical effect?

Answer 12

Unbound, free drugs

Question 13

AAG bound Rx - High

Answer 13

Lidocaine
Fentanyl
Propranolol
Verapamil

Question 14

AAG bound Rx - Medium

Answer 14

Midazolam

Question 15

AAG bound Rx - Low

Answer 15

Carbamazepine

Diltiazem

Question 16

After large IVF administration, how will Vd effect hypophilic + lipophilic Rxs?

Answer 16

Hydrophilic —>increased Vd (dec serum concentration)

Lipophilic —> no change

Question 17

Hepatic Clearance

Answer 17

CLh=E x Qh

Hepatic clearance = Hepatic blood flow x extraction ratio

Question 18

Hepatic blood flow increases d/t

Answer 18

Increased CO

Hyperdynamic phase of sepsis

Question 19

Hepatic blood flow decreases d/t

Answer 19

Hypovolemic/Hemorrhagic/Cardiogenic shock
Hypodynamic phase of sepsis
MI/Acute HF exacerbation 
Increased Intrathoracic pressure
Spinal anesthesia

Question 20

Which phase of biotransformation is most often outside liver/no CYP involvement?

Answer 20

Hydrolysis - Remifent, Succs, esmolol, ester local anesthetics

Question 21

CYP inducer = _____ serum concentrations

Answer 21

Decreased

Question 22

CYP inhibitor = ______ serum concentrations

Answer 22

Increased

Question 23

Pt is hypothermic, how will intrinsic clearance change?

Answer 23

Decreased metabolism thru CYP —> enzyme activity decreases

Increased serum concentrations

Question 24

Renal injury will effect intrinsic clearance how?

Answer 24

Decreased metabolism via CYP - increased concentration

Question 25

Goal of Phase I biotransformation

Answer 25

Make Rx more polar/water soluble (hydrophilic) —> allow elimination via phase II

Question 26

Hepatic extraction ratio

Answer 26

Fraction of Rx removed during 1 pass thru liver | Range: 0-1

Question 27

Hepatic extraction ratio: 0

Answer 27

Liver does not metabolize drug

Question 28

Hepatic Extraction Ratio: 1

Answer 28

Hepatic metabolism entirely dependent on blood flow

Question 29

Hepatic Extraction Ratio: High

Answer 29

> 0.7 Propofol, Bupivacaine, Diltiazem, Fentanyl, Ketamine, Lidocaine, Meperidine, Metoprolol, Morphine, Naloxone, Nifedipine, Propranolol, Sufentanil

Question 30

Hepatic Extraction Ratio: Intermediate

Answer 30

0.3-0.7 Alfentanil, methohexital, midazolam, Vecuronium Metabolism dependent on hepatic blood flow, intrinsic clearance, fraction unbound drug

Question 31

Hepatic Extraction Ratio: Low

Answer 31

<0.3 Diazepam, Lorazepam, methadone, phenytoin, rocuronium, theophylline, thiopental Clearance is independent of hepatic blood flow; varies with changes in hepatic enzyme activity

Question 32

CYP inducers

Answer 32

``` St. John’s wart Rifampin Phenytoin Carbamazepine Phenobarbital *increase metabolism ```

Question 33

CYP inhibitors

Answer 33

Amino, cimetidine, clarithromycin, diltiazem, erythromycin, grapefruit juice, fluconazole, isoniazid, ritonavir, verapamil *decrease metabolism

Question 34

Drugs that undergo significant renal clearance in anesthesia

Answer 34

Aminoglycosides, carbapenems, cephalosporins, PCNs, quinolones pancuronium/rocuronium/Suggamadex Neostigmine, Pyridostigmine Atenolol, nadolol, procainamide, digoxin

Question 35

Drugs excreted via pulmonary system

Answer 35

Volatile anesthetics

Question 36

Generally speaking - fungals cleared thru

Answer 36

Liver

Question 37

Generally speaking - antbx cleared thru

Answer 37

Kidney

Question 38

Potency

Answer 38

Amount of drug needed to cause an effect

Question 39

Large range between MED/MTD

Answer 39

Large therapeutic window

Question 40

Argatroban and Bivalirudin are dosed on what pharmacodynamic parameter

Answer 40

aPTT

Question 41

LMWH is dosed on what lab value

Answer 41

Anti-Xa