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KM (Spring 2024) Anesthesia Pharm ** > 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
Q

What occurs during Phase II reactions?
By what chemical process does this occur?

A
  • Covalent bond with polar molecule = H₂O-soluble
  • Conjugation
26
Q

What is the most common CYP450 enzyme?
How many drugs are estimated to be metabolized by this enzyme?

A
  • CYP3A4
  • > 50% (opioids, benzos, LA, antihistamines, etc)
27
Q

What is CYP450 induction?
Give an example.

A
  • Drug induces enzyme to increase enzyme activity.
  • Phenobarbitol induces enzymes & metabolism of other drugs is increased.
28
Q

What is CYP450 Inhibition?
Give an example.

A
  • Drug inhibits enzyme & decreases enzyme activity.
  • Ex. Grapefruit juice inhibits CYP activity and some drugs become more toxic.
29
Q

What is the formula for Rate of Drug Metabolism?

A
  • R = Q ( C-inflow - C-outflow)

or

  • R = Q (ΔC)
30
Q

What is flow-limited hepatic clearance?

A
  • When Q limits metabolic rate
31
Q

What is capacity-limited hepatic clearance?

A
  • Liver CYP450’s ability to metabolize is the limiting factor
32
Q

What are the three components of Renal Clearance discussed in lecture?

A
  • Glomerular filtration
  • Active tubular secretion
  • Passive tubular reabsorption
33
Q

What two factors determine glomerular filtration of drugs?

A
  • GFR
  • Amount of drug that is protein-bound
34
Q

What drug example was given in lecture that is subject to active tubular secretion?

A
  • Penicillins
35
Q

What increases the tubular reabsorption of certain drugs?
What decreases the tubular reabsorption of drugs?

A
  • Lipophillic = reabsorbed
  • Hydrophillic = no reabsorption; excreted in urine.
36
Q

Differentiate Elimination Half-Time & Elimination Half-Life.

A
  • 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
Q

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?

A
  • 85mg

(5mg from original dose, 80mg from second dose)

38
Q

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.

A
  • 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
Q

What drug class is comprised of weak acids?

A
  • Barbiturates
40
Q

What drug class is comprised of weak bases?

A
  • Local Anesthetics & Opioids
41
Q

Ionization numbers that are ________ cross lipid bilayers very well.

A
  • negative
42
Q

If the drug is a weak acid then PK ______ pH.

A

After

43
Q

If the drug is a weak base then PK ______ pH

A

Before

44
Q

Aspirin (weak acid; PK = 7.7) travels to blood with a pH of 7.4. Will this aspirin work well?

A
  • 7.4 - 7.7 = -0.3
  • Yes; ionization is negative therefore non-ionized & crosses barriers.
45
Q

Morphine (PK = 8.0) is injected into blood with a pH of 7.2. What will occur with this morphine?

A
  • 8.0 - 7.2 = +0.8
  • Ionization is + so drug will not cross membranes well and thus not work well.
46
Q

What is the process of ion trapping?

A
  • When a drug is ionized and thus accumulates somewhere without being “used up” (mother-fetus example).
47
Q

What factors affect pharmacodynamics in elderly patients?

A
  • ↓CO (affects brain & liver)
  • ↓ protein binding
  • ↑ body fat
48
Q

Differentiate acute vs chronic alcohol ingestion effects on pharmacodynamics.

A
  • Acute: EtOH using all CYPs (drugs will “stick around” longer)
  • Chronic: less of an effect, body has usually compensated.
49
Q

What is an example of a genetic phenotype correlating with increased anesthetic needs?

A
  • Redheads
50
Q

In the graph below, which line would in indicate the most efficacious drug?

A
  • Red
51
Q

In the graph below, which line would in indicate the most potent drug?

A
  • Blue
52
Q

What is relative potency (time to drug effect)?

A
  • Lag time between administration & effects (fent vs alifentanil)
53
Q

How is Therapeutic Index calculated?
What would a narrow TI indicate?

A
  • LD50/ED50
  • Narrow TI = more “dangerous” drug requiring careful monitoring.
54
Q

Differentiate LD50 and ED50.

A
  • LD50 = dose at which 50% of patients die.
  • ED50 = dose at which 50% of patients experience drug effect.
55
Q

What are chiral compounds?

A
  • Molecules with asymmetric centers
56
Q

What are the characteristics of enantiomers?

A
  • Chemically identical
  • Mirror images
  • Non-superimposable
57
Q

What term(s) would indicate a rightward rotation light in an optical isomer?

A
  • Dextrorotary (D) or Rectus
58
Q

What term(s) would indicate a leftward rotation light in an optical isomer?

A
  • Levoorotary (L) or Sinister
59
Q

What is a 50/50 mixture of optical isomers called?
Why does it matter?

A
  • Racemic
  • These compounds will have differing characteristics, effects, & ADME
60
Q

Which isomer of Ketamine is more potent and results in less delirium?

A
  • S-Ketamine
61
Q

Which isomer of bupivicaine exhibits less cardiotoxicity?

A
  • L-Bupivicaine
62
Q

Why would one want Cisatracurium over atracurium?

A
  • Atracurium causes massive histamine release. Cisatracurium does not.

KM (Spring 2024) Anesthesia Pharm ** (101 decks)

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