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Pharm Fall 2019 > Exam 1 - Pharmacokinetics > Flashcards

Exam 1 - Pharmacokinetics Flashcards

(79 cards)

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1
Q

Steady State Concentration

A

Constant serum concentration that is achieved when rate of drug administration = rate of drug metabolism/excretion

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2
Q

What is steady state concentration used for?

A

Assess patient response, make new decisions

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3
Q

Linear pharmacokinetics

A

Steady state concentrations increase/decrease proportionally according to dose. Example: Vancomycin, procainamide

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4
Q

Linear pharmacokinetics - not applicable when?

A

Patient has renal failure, organ failure, etc.

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5
Q

Non-linear pharmacokinetics

A

Steady state concentrations change in disproportionate fashion after dose is changed

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6
Q

Valproic acid, carbamazepine, phenytoin have what type of pharmacokinetics?

A

Non-linear

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7
Q

Saturable or Michaelis-Menten Pharmacokinetics

A

Steady state concentration increases more than expected after dose increase. Number of drug molecules overwhelms enzymes ability to metabolize drug

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8
Q

Half life

A

Time required for serum concentrations to decrease 50% during elimination phase after absorption/distribution are complete

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9
Q

How long does it take to reach steady-state concentrations during continuous dosing?

A

3-5 half lives

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10
Q

A faster clearance will cause a _____ half life

A

Shorter (if kidney function picks up, half life will be shorter)

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11
Q

Larger volume of distribution will result in ____ half life

A

Longer (amiodarone) or shorter (propofol)

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12
Q

Bioavailability

A

Fraction of administered drug that is delivered to systemic circulation

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13
Q

Bioavailability of IV drugs

A

100%

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14
Q

Central compartment

A

Plasma

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15
Q

Peripheral compartment

A

Tissues

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16
Q

Multi compartment model

A

Body is central compartment where drug is administered, peripheral compartment is where drug is distributed - curvature will be non linear.

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17
Q

Back end kinetics

A

Describes how plasma drug concentrations decrease once a continuous infusion is terminated

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18
Q

Decrement time

A

Predicts the time required to reach a certain plasma concentration once infusion is terminated

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19
Q

If decrement time is 50%, what is another name?

A

Context sensitive half time

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20
Q

Longer infusion will result in ______ decrement time

A

Prolonged — due to increased accumulation

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21
Q

Effect site

A

Biophase - drugs exert their biological effect at this site

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22
Q

Biophase

A

Body compartment in which receptor sites reside

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23
Q

Pharmacokinetics

A

Relationship between the drug administration and drug concentration at the site of action. Movement of drug throughout the body

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24
Q

Pharmacokinetics principles

A

ADME - Absorption, distribution metabolism, excretion/elimination

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25
Magnitude of drug effect and duration of action is affected by?
Absorption
26
Percent of drug that reaches systemic circulation
Bioavailability
27
Volume of distribution equation
Dose divided by concentration
28
A larger person will have a _______ volume of distribution
Larger
29
A smaller person will have a _______ volume of distribution
Smaller
30
When does volume of distribution increase?
When drugs move from blood to tissues
31
As volume of distribution increases due to drugs moving from blood to tissues, what will happen to blood concentration?
Decreases
32
Redistribution
Drug will distribute from organ back to blood once concentration in organ exceeds blood. Once in the blood, the drug will redistribute to other tissues that are still up taking the drug
33
Highly lipophilic drugs leads to ________ in brain concentration and redistribution to muscle
Decrease
34
Critically ill patient has _____ albumin, which causes fraction unbound drug to _______, leading to _________ volume of distribution
Decreased, increased, increased
35
Unbound drug can or cannot cause a clinical effect?
Can
36
If fraction of unbound drug decreases, what will happen to volume of distribution?
Decrease
37
Drugs highly bound to albumin - part 1
Propofol Morphine Propranolol Verapamil
38
Drugs highly bound to albumin - part 2
Aspirin Carvedilol Omeprazole Midazolam
39
Drugs highly bound to albumin - part 3
``` Carbamazepine Ceftriaxone Dexamethasone Diazepam Itraconazole Phenytoin Valproic acid Warfarin Diltiazem ```
40
AAG increases, fraction of unbound drug ______, volume of distribution _______
Decreases, decreases
41
Drugs highly bound to AAG - part 1
Lidocaine Fentanyl Propranolol Verapamil
42
Drugs highly bound to AAG - part 2
Midazolam
43
Drugs highly bound to AAG - part 3
Carbamazepine | Diltiazem
44
Increase in total body water due to IVF will increase volume of distribution for what type of drugs?
Hydrophilic - decreased serum concentration
45
Intrinsic clearance is expressed as?
Volume per unit of time (mL/hour)
46
Drugs excreted unchanged in urine/stool are ______philic
Hydrophilic
47
Drugs that are not very _______philic are converted into more _____philic compounds for excretion
Hydrophilic, hydrophilic
48
Phase I metabolism reactions are catalyze by what?
CYP450
49
High concentrations of CYP enzymes are found in
Smooth endoplasmic reticulum of hepatocytes | Membranes of upper intestinal enterocytes
50
Lower concentrations of CYP enzymes are found
Lungs Kidneys Skin
51
Inhibitors or inducers of CYP3A4 will cause what to occur
Inhibition of metabolism or induction (causing) of metabolism
52
Most common CYP450 enzyme
CYP3A4
53
CYP3A4 accounts for ______% of all CYP mediated drug metabolism
40-45
54
CYP inducers result in _____ metabolism
Increased
55
CYP inhibitors result in ________ metabolism
Decrease
56
CYP inducers
St. John’s wort, rifampin, phenytoin, carbamazepine, phenobarbital
57
CYP inhibitors that decrease metabolism
``` Amiodarone Cimetidine Clarithromycin Diltiazem Erythromycin Grapefruit juice Fluconazole Isoniazid Ritonavir Verapamil ```
58
Hydrolysis occurs in which drugs?
Remifentanyl, succinylcholine, esmolol, ester local anesthetics
59
Type of reaction that does not involve CYP system and metabolizes drugs
Hydrolysis
60
Phase II of biotransformation
Transforms hydrophobic molecules into water soluble molecules thru addition of polar groups; form glucuronides, acetates, or sulfates
61
Drugs that undergo phase II conjugation
Propofol, morphine, midazolam
62
Hypermetabolism may occur in which patients?
Febrile, traumatic brain injury
63
Hypo-metabolism will occur in which patients?
Hepatic failure, kidney injury, hypothermic,
64
Hepatic clearance equation
Hepatic clearance (CLh) = Extraction ratio * Hepatic Blood Flow
65
Hepatic extraction ratio
Fraction of drug removed during one pass through liver
66
Hepatic extraction ratio - Low
0 - 0.3
67
Hepatic extraction ratio = 0
Liver does not metabolize the drug
68
Hepatic extraction ratio - intermediate
0.3-0.7
69
Hepatic extraction ratio - high
> 0.7
70
Hepatic extraction ratio = 1
Hepatic metabolism entirely dependent on blood flow
71
Pharmacodynamics
Relationship between drug concentration and biochemical/physiologic effect on body
72
What type of drug is Narcan?
Competitive antagonist
73
Up regulation
Number of receptors increases
74
Down regulation
Number of receptors decrease
75
Tachyphylaxis
Tolerance - decreased response to same amount of agonists
76
Agonist-antagonist
Partial agonists that have antagonist activity
77
ED50
Potency
78
ED50
Dose required for desired effect in 50% of population exposed to it
79
Therapeutic drug monitoring is a measure of pharmaco_______
Pharmacodynamics

Pharm Fall 2019 (33 decks)

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