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Anes Pharm (Spring 2025) Grayson Mixed > Pharmacokinetics/Pharmacodynamics (Exam I) > Flashcards

Pharmacokinetics/Pharmacodynamics (Exam I) Flashcards

1
Q

What does TTE mean in regards to pharmacodynamics/kinetics?

A
  • Titrated to effect
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2
Q

Receptors are usually __________.

A
  • Proteins
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3
Q

Almost all drugs are reversible except for drugs that are ________ ______.

A
  • Covalently bonded
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4
Q

Regarding the graph below: What type of drug would you expect looking at the orange line? (agonist, antagonist, partial, inverse, etc.)

A

Orange = Full Agonist

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5
Q

Regarding the graph below: What type of drug would you expect looking at the blue line? (agonist, antagonist, partial, inverse, etc.)

A

Blue = Strong partial agonist

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6
Q

Regarding the graph below: What type of drug would you expect looking at the yellow line? (agonist, antagonist, partial, inverse, etc.)

A

Yellow = Weak partial agonist

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7
Q

Regarding the graph below: What type of drug would you expect looking at the black line? (agonist, antagonist, partial, inverse, etc.)

A

Black = Antagonist

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8
Q

Regarding the graph below: What type of drug would you expect looking at the green line? (agonist, antagonist, partial, inverse, etc.)

A

Green = Inverse agonist

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9
Q

What two mechanisms can occur with receptors that will increase or decrease their expressed quantity?

A
  • Downregulation & Upregulation
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10
Q

What is tachyphylaxis and what drug was given as an example in lecture?

A
  • Tachyphylaxis = rapid tolerance development
  • Ex. Ephedrine
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11
Q

What sort of expression of β receptors would expect to see in a patient dealing with a chronic pheochromocytoma?

A
  • Downregulation of β receptors in response to the increase in catecholamines
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12
Q

What three receptor locations were discussed in lecture?

A
  • Lipid Bilayer
  • Intracellular
  • Circulating in plasma
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13
Q

What type of drugs interact with intracellular receptors?

A
  • Insulin, steroids & milrinone
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14
Q

What type of drugs interact with circulating protein receptors?

A
  • Anticoagulants
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15
Q

What type of drugs interact with membrane bound receptors?

A
  • Opioids, benzos, β-blockers, NMBs
  • Most common (especially for anesthetics)
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16
Q

Acidic drugs bind primarily to ________.

A
  • Albumin
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17
Q

Basic/Alkalotic drugs bind primarily to _______.

A
  • α1-acid glycoprotein
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18
Q

How much bound drug crosses protein membranes?

A
  • 0% (only “free” unbound drugs cross membranes)
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19
Q

What degree of volume of distribution (VD) would be seen with drugs that are poorly protein bound and lipophilic?
What examples were given in lecture?

A
  • ↑ ↑ ↑ VD
  • Thiopental & Diazepam
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20
Q

What degree of volume of distribution (VD) would be seen with drugs that are highly protein bound and/or hydrophilic?
What example(s) were given in lecture?

A
  • ↓ ↓ ↓ VD
  • Warfarin
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21
Q

What drug examples were given in lecture as having active metabolites?

A
  • Diazepam
  • Propanolol (Inderal)
  • Morphine (2 metabolites)
  • Codeine (& other prodrugs)
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22
Q

What does metabolism convert active drugs into?

A
  • H₂O soluble & inactive metabolite forms
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23
Q

What is the most common way that drugs are metabolized?
What other ways exist?

A
  • Hepatic CYP450’s
  • Hoffman Elimination, Ester hydrolysis, Kidneys, & Tissue Esterases (GI tract & placenta)
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24
Q

What is the purpose of Phase I reactions?
What chemical processes occur during these reactions?

A
  • Increase polarity & prepare for phase II
  • Oxidation/Reduction & Hydrolysis
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25
What occurs during Phase II reactions? By what chemical process does this occur?
- Covalent bond with polar molecule = H₂O-soluble - Conjugation
26
What is the most common CYP450 enzyme? How many drugs are estimated to be metabolized by this enzyme?
- CYP3A4 - >50% (opioids, benzos, LA, antihistamines, etc)
27
What is CYP450 induction? Give an example.
- Drug **induces** enzyme to increase enzyme activity. - Phenobarbitol induces enzymes & metabolism of other drugs is increased.
28
What is CYP450 Inhibition? Give an example.
- Drug **inhibits** enzyme & decreases enzyme activity. - Ex. Grapefruit juice inhibits CYP activity and some drugs become more toxic.
29
What is the formula for Rate of Drug Metabolism?
- R = Q ( C-inflow - C-outflow) or - R = Q (ΔC)
30
What is flow-limited hepatic clearance?
- When Q limits metabolic rate
31
What is capacity-limited hepatic clearance?
- Liver CYP450's ability to metabolize is the limiting factor
32
What are the three components of Renal Clearance discussed in lecture?
- Glomerular filtration - Active tubular secretion - Passive tubular reabsorption
33
What two factors determine glomerular filtration of drugs?
- GFR - Amount of drug that is protein-bound
34
What drug example was given in lecture that is subject to active tubular secretion?
- Penicillins
35
What increases the tubular reabsorption of certain drugs? What decreases the tubular reabsorption of drugs?
- Lipophillic = reabsorbed - Hydrophillic = **no reabsorption**; excreted in urine.
36
Differentiate Elimination Half-Time & Elimination Half-Life.
- Half-Time = time to elimination of 50% of drug from the **plasma**. - Half-Life = time to elimination of 50% of drug from all tissues.
37
80mg of a drug is given with the E 1/2 time known to be 5 minutes. What will the plasma concentration of the drug be in 20 minutes immediately after giving a second 80mg dose?
- 85mg (5mg from original dose, 80mg from second dose)
38
What is the context-sensitive half-time? Give an example of a drug with a low context-sensitive half-time vs a high context-sensitive half-time.
- Time to a 50% decrease after an infusion is discontinued. (essentially measures increasing tissue accumulation affecting how long it takes for a drug to leave the body) - Fentanyl = higher context half-time - Propofol = lower context half-time
39
What drug class is comprised of weak acids?
- Barbiturates
40
What drug class is comprised of weak bases?
- Local Anesthetics & Opioids
41
Ionization numbers that are ________ cross lipid bilayers very well.
- negative
42
If the drug is a weak acid then PK ______ pH.
After
43
If the drug is a weak base then PK ______ pH
Before
44
Aspirin (weak acid; PK = 7.7) travels to blood with a pH of 7.4. Will this aspirin work well?
- 7.4 - 7.7 = -0.3 - Yes; ionization is negative therefore non-ionized & crosses barriers.
45
Morphine (PK = 8.0) is injected into blood with a pH of 7.2. What will occur with this morphine?
- 8.0 - 7.2 = +0.8 - Ionization is + so drug **will not** cross membranes well and thus not work well.
46
What is the process of ion trapping?
- When a drug is ionized and thus accumulates somewhere without being "used up" (mother-fetus example).
47
What factors affect pharmacodynamics in elderly patients?
- ↓CO (affects brain & liver) - ↓ protein binding - ↑ body fat
48
Differentiate acute vs chronic alcohol ingestion effects on pharmacodynamics.
- Acute: EtOH using all CYPs (drugs will "stick around" longer) - Chronic: less of an effect, body has usually compensated.
49
What is an example of a genetic phenotype correlating with increased anesthetic needs?
- Redheads
50
In the graph below, which line would in indicate the most efficacious drug?
- Red
51
In the graph below, which line would in indicate the most potent drug?
- Blue
52
What is relative potency (time to drug effect)?
- Lag time between administration & effects (fent vs alifentanil)
53
How is Therapeutic Index calculated? What would a narrow TI indicate?
- LD50/ED50 - Narrow TI = more "dangerous" drug requiring careful monitoring.
54
Differentiate LD50 and ED50.
- LD50 = dose at which 50% of patients die. - ED50 = dose at which 50% of patients experience drug effect.
55
What are chiral compounds?
- Molecules with asymmetric centers
56
What are the characteristics of enantiomers?
- Chemically identical - Mirror images - Non-superimposable
57
What term(s) would indicate a rightward rotation light in an optical isomer?
- Dextrorotary (D) or Rectus
58
What term(s) would indicate a leftward rotation light in an optical isomer?
- Levoorotary (L) or Sinister
59
What is a 50/50 mixture of optical isomers called? Why does it matter?
- Racemic - These compounds will have differing characteristics, effects, & ADME
60
Which isomer of Ketamine is more potent and results in less delirium?
- S-Ketamine
61
Which isomer of bupivicaine exhibits less cardiotoxicity?
- L-Bupivicaine
62
Why would one want Cisatracurium over atracurium?
- Atracurium causes massive histamine release. Cisatracurium does not.

Anes Pharm (Spring 2025) Grayson Mixed (21 decks)

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