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Pharm Fall 2019 > Final - Pharmacokinetics > Flashcards

Final - Pharmacokinetics Flashcards

1
Q

Time to steady state

A

3-5 half lives

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2
Q

Bioavailability of IV drugs

A

100%

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3
Q

Context Sensitive Half Time

A

50% decrement time

Time reqd to reach 50% of concentration after infusion stopped

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4
Q

Time delay between change in plasma concentration and drug effect

A

Hysteresis

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5
Q

Volume of distribution

A

Vd=dose/concentration

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6
Q

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

A

Larger person = larger Vd

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7
Q

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

A

Decreased

Decreased

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8
Q

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

A

Increased

Increased

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9
Q

Highly albumin bound Drugs

A

Propofol
Morphine
Propranolol
Verapamil

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10
Q

Medium albumin bound Rx

A

Aspirin
Carvedilol
Omeprazole
Midazolam

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11
Q

Low Albumin bound Rx

A 
Carbamazepine
Ceftriaxone
Dexamethasone
Diazepam
Itraconazole
Phenytoin
Valproic Acid
Warfarin
Diltiazem
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12
Q

Which drug form causes a clinical effect?

A

Unbound, free drugs

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13
Q

AAG bound Rx - High

A

Lidocaine
Fentanyl
Propranolol
Verapamil

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14
Q

AAG bound Rx - Medium

A

Midazolam

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15
Q

AAG bound Rx - Low

A

Carbamazepine

Diltiazem

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16
Q

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

A

Hydrophilic —>increased Vd (dec serum concentration)

Lipophilic —> no change

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17
Q

Hepatic Clearance

A

CLh=E x Qh

Hepatic clearance = Hepatic blood flow x extraction ratio

18
Q

Hepatic blood flow increases d/t

A

Increased CO

Hyperdynamic phase of sepsis

19
Q

Hepatic blood flow decreases d/t

A 
Hypovolemic/Hemorrhagic/Cardiogenic shock
Hypodynamic phase of sepsis
MI/Acute HF exacerbation 
Increased Intrathoracic pressure
Spinal anesthesia
20
Q

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

A

Hydrolysis - Remifent, Succs, esmolol, ester local anesthetics

21
Q

CYP inducer = _____ serum concentrations

A

Decreased

22
Q

CYP inhibitor = ______ serum concentrations

A

Increased

23
Q

Pt is hypothermic, how will intrinsic clearance change?

A

Decreased metabolism thru CYP —> enzyme activity decreases

Increased serum concentrations

24
Q

Renal injury will effect intrinsic clearance how?

A

Decreased metabolism via CYP - increased concentration

25
Q

Goal of Phase I biotransformation

A

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

26
Q

Hepatic extraction ratio

A

Fraction of Rx removed during 1 pass thru liver

Range: 0-1

27
Q

Hepatic extraction ratio: 0

A

Liver does not metabolize drug

28
Q

Hepatic Extraction Ratio: 1

A

Hepatic metabolism entirely dependent on blood flow

29
Q

Hepatic Extraction Ratio: High

A

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

30
Q

Hepatic Extraction Ratio: Intermediate

A

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

31
Q

Hepatic Extraction Ratio: Low

A

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

32
Q

CYP inducers

A 
St. John’s wart
Rifampin
Phenytoin
Carbamazepine
Phenobarbital
*increase metabolism
33
Q

CYP inhibitors

A

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

34
Q

Drugs that undergo significant renal clearance in anesthesia

A

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

35
Q

Drugs excreted via pulmonary system

A

Volatile anesthetics

36
Q

Generally speaking - fungals cleared thru

A

Liver

37
Q

Generally speaking - antbx cleared thru

A

Kidney

38
Q

Potency

A

Amount of drug needed to cause an effect

39
Q

Large range between MED/MTD

A

Large therapeutic window

40
Q

Argatroban and Bivalirudin are dosed on what pharmacodynamic parameter

A

aPTT

41
Q

LMWH is dosed on what lab value

A

Anti-Xa

Pharm Fall 2019 (33 decks)

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