Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Anesthesia Pharm Spring '25 > Test 1: PK/PD > Flashcards

Test 1: PK/PD Flashcards

(91 cards)

Start Studying
1
Q

In order to know what interventions are creating desired change we need to _________

A

deliberately change 1 variable at a time if possible to determine the effectiveness of our interventions.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Drug receptors are usually a

A

protein

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

When bound, a receptor undergoes a _____

A

conformational change

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

The effect of a drug relates to _______

A

the number of bound receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

The more receptors you have bound the _______ the effect of the drug

A

greater

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is an agonist

A

It is a drug that is capable of binding to, and activating, a receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Agonist and antagonists bind by what 3 interactions that are reversible?

A

1- Ion (electrocovalent)
2- Hydrogen bonding
3- van der Waals interaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Agonists and antagonist can bind by _______. This is irreversible

A

covalent bonds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what is an antagonist

A

They block the action of an agonist getting to the receptor to elicit a response, therefore no response is made
“musical chairs”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the difference between a competitive antagonist and a non-competitive antagonist?

A

Competitive antagonists can be outnumbered and outcompeted as a larger and larger dose of the agonist is given.
non-competitive antagonists cannot be overcome by increasing doses of agonists. (No matter the dose of the agonists you will not see the full effect of the agonist)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is a partial agonist?

A

A drug that binds to its receptor but produces a smaller effect at full dosage than a full agonist.

In the presence of an agonist a partial agonist acts as an antagonist.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is an inverse agonist

A

Agonist that binds to the same site as an agonist however produces an opposite response. They move the receptor into the inactive form.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is tolerance?

A

the diminishing effect with regular use of the same dose of a drug, requiring the user to take larger and larger doses before experiencing the drug’s effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is tachyphylaxis?

A

Increased tolerance to a drug that is administered repeatedly. This process is usually rapid.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What mixed beta agonist used in the OR commonly exhibits tachypylaxis?

A

ephedrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Receptor types are classified by ______

A

location

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is the most common receptor type?

A

lipid bilayer receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Receptors for insulin, steroids, and milrinone are all _______

A

intracellular receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Anticoagulants, such as warfarin, bind to what type of receptor?

A

Circulating (plasma) proteins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What 5 drug classes listed in lecture bind to receptors that are in the lipid bilayer?

A

1- Opioids
2- Benzodiazepines
3- Beta-Blockers
4- Catecholamines
5- Neuromuscular Blocking Drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What term is used to describe what effects the body has on the drug?

A

pharmacokinetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the 4 principles of pharmacokinetics?

A

Adsorption
Distribution
Metabolism
Excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the 1 compartment model

A

instantaneous distribution of drug throughout the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

If a drug has a low volume of distribution that means the majority of the drug is likely located ________

A

in the plasma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
10% of your body mass is considered the vessel rich group, it receives _______% of cardiac output and is made up of what 5 organs according to lecture?
75% 1- Heart 2- Lungs 3- Liver 4- Kidneys 5- Brain
26
If a drug has a large volume of distribution that means _________
The drug leaves the plasma at higher rates
27
Drugs that are fat soluble and preferentially move to the fat have a ______ volume of distribution
high
28
What is the 2 compartment model of volume distribution?
The 2 compartment model recognizes that the drug can be present in the plasma or the periphery, it is not always present in the blood.
29
Acidic drugs primarily bind to
albumin
30
Alkalotic/Basic drugs primarily bind to
A-1 acid glycoprotein
31
only drug that is ________ or ________ can determine concentration available to receptor
free or unbound
32
What types of things mentioned in lecture would cause an abnormal decrease in plasma protein concentration
1- Age 2- Nutrition 3- hepatic disease 4- renal failure 5- pregnancy 6- burns
33
The following 2 medications listed in lecture have poor protein binding and are lipophilic
1- Thiopental 2- Diazepam
34
If there is a lower than normal circulating blood volume then we would expect _________ volume of distributions
lower/smaller
35
If there is an increase in blood volume, then we would expect ______ volume of distribution
higher/larger
36
4 drugs from lecture with active metabolites
1- Diazepam / Valium 2- Propranolol / Inderal 3- Morphine (2 active metabolites) 4- Codeine (a prodrug)
37
The process of metabolism converts active, lipid soluble drugs to _________
(usually) inactive water soluble metabolites
38
3 primary ways drugs are metabolized
1- in the liver via microsomal enzymes (think CYP) 2- In the kidneys 3- In the plasma
39
What is Hoffman elimination?
Spontaneous elimination of a drug in the plasma
40
What is ester hydrolysis?
when an ester reacts with water, the ester breaks to form an alcohol and carboxylic acid. Is a hydrolysis reaction.
41
3 examples of phase 1 reactions
Oxidation, reduction, hydrolysis
42
Phase 1 reactions increase
polarity / water solubility
43
Phase 2 reactions AKA __________
conjugation
44
What is added during a phase 2 reaction
We attach a highly polar molecule to cause higher water solubility to prepare / mark for elimination
45
CYP450 enzymes have a large family consisting of _____ isoforms
10
46
CYP450 enzymes catalyze
oxidation / reduction reactions
47
The CYP that has the most targets for metabolism (>50% of drugs) is ______
CYP3A4
48
Define homologous
Any shared traits or features inherited from a common ancestor.
49
The longer the name of a CYP enzyme the _______
more closely related/alike they are
50
CYP inducers have what effect?
They increase the amount/activity of the CYP enzyme.
51
CYP Inducers (PS PORCS)
P-Phenytoin S-Smoking P-phenobarbital O-oxcarbazepine R-Rifampin C-Carbamazepine S-St.johns wort (this info was not given in lecture)
52
CYP inhibitors have what effect?
They decrease the activity of the enzymes
53
CYP Inhibitors (G PACMAN)
G-grapefruit P- protease inhibitors A-azoles C-cyclosporine/cimetidine M-macrolides A-amiodarone N-Non-dihydropyridine(diltiazem and verapamil) / CCB (not all given in lecture)
54
For most anesthetic drugs clearance is constant meaning they are in _______ elimination
first order
55
What is flow limited hepatic clearance?
When the clearance rate is proportional to concentration and is only effected by the amount of blood flow through the liver or "Q"
56
What is capacity limited hepatic clearance?
This is when the livers ability to metabolize and clear the substance is the limiting fact, adding more blood flow will not result in more clearance (parallels zero order elimination from last semester)
57
Renal clearance is determined by the amounts of what 3 processes?
1- Filtration 2- Reabsorption 3- Secretion
58
In reference to renal clearance _______ is almost zero for water soluble drugs
Reabsorption (these drugs are excreted in the urine)
59
In terms of renal clearance, what drug class experiences active tubular secretion?
penicillins
60
Define elimination half-time
The time it takes for 50% of drug to be removed from plasma during elimination phase
61
Define elimination half-life
Elimination half life = the time it takes for 50% of the drug to be removed from body after rapid IV injection
62
Redosing a medication prior to allowing time for adequate elimination to occur can result in __________
Accumulation of higher concentrations in the plasma
63
What is context sensitive half-time?
increased duration of drug effect with increased drug infusion time Meaning elimination / half time takes longer for the longer we have an infusion going.
64
Context sensitive half-time is related to __________ Elimination half time is related to _________
IV infusions / drips Bolus administrations
65
When the pK and the pH are identical, 50% of the drug exists in
the ionized form and 50% of the drug exists in the non-ionized form
66
Local anesthetics and opioids are weak ________
bases
67
barbiturates are weak ___
acids
68
If pH is less than pKa
a majority of the species will be protenated
69
A weak acid that is protonated is considered ionized or unionized?
unionized
70
A weak base that is protonated is considered ionized or unionized?
ionized
71
Typically a drug is most effective when it is in it's ________ form
non-ionized
72
Given a pH and a pK value of a weak acid we can use this formula to determine if a drug is going to be ionized or nonionized
pH - pK
73
given a pH and a pK value of a weak base we can use this formula to determine if a drug is going to be ionized or nonionized
pK - pH
74
Nicely Negative Numbers are _____
non-ionized Meaning the formulas to determine ionization will give you a positive number if the drug is likely to be positive and a negative number if a drug is likely to be nonionized.
75
To have effective drugs we want them to be _________ in the pH of the intended area
nonionized
76
What is pharmacodynamics
what drug does to body
77
What is pharmacodynamics
potent ; efficacious
78
More potent drugs require _______ doses to reach their intended effect
lower
79
The plasma is not the site of effect for anesthetic drugs, this means we may see a ____ time between administration and effect.
lag
80
How do you calculate the therapeutic index?
TI = LD50/ED50
81
What is a chiral compound?
Molecules with asymmetric centers
82
What is an enantiomer?
each of a pair of molecules that are mirror images of each other.
83
Labeling enantiomers by the way they reflect light, L represents ________ and R represents _________
Levorotatory (Left rotation) Dextrorotatory (right rotation)
84
Labeling L and R enantiomers related to their molecule sequence, R represents _______ and L represents _______
Recuts (clockwise) Sinister (counter-clockwise)
85
Enantiomers can have different effects on the body because they undergo the principles of pharmacokinetics differently, those principles are _______
Enantiomers can have different effects on the body because they undergo the principles of pharmacokinetics differently, those principles are _______
86
Which enantiomer of ketamine is more potent while also offering less delirium?
S Ketamine
87
Which bupivacaine enantiomer is 3-4 times less cardiotoxic?
L-Bupivacaine
88
This isomer of atracurium lacks the histamine effects associated with atricurium ________
cisatricurium (nimbex)
89
What is the isomer of albuterol that is associated with less side effects such as tachycardia?
Xopenex
90
Define pharmacogenomics
the study of how genes affect a person's response to drugs
91

Anesthesia Pharm Spring '25 (2 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions