[7] Pharmacokinetics in Special Conditions Flashcards

1
Q

Are most active drugs Basic or Acidic?

A

Basic

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2
Q

Assessment of Renal Function (3)

A
  1. Hourly urine output
  2. Amount of circulating Urea and Nitrogen Concentration
  3. Creatine clearance and GFR
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3
Q

Average Hourly Urine Output?

A

60mL

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4
Q

Limitation of Creatinine Clearance

A

Less muscle bulk or in elderly patients would give a lower than average creatinine clearance value

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5
Q

Formula: Dose Adjustment Factor

A

1 / F (kf -1) +1

F: Fraction of Drug Excreted Unchanged
Kf: Relative Kidney function calculated by dividing actual creatinine clearance with 120 mL/min

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6
Q

Example:

Digoxin F = 0.75
If the oral digoxin dose is 0.25mg orally, what is the DAF for a patient with creatinine clearance of 60 mL/minute?

A

DAF = 1/0.75 (60/120 - 1) + 1
= 1.6

Adjusted dose is 0.25 / 1.6 or 1.6mg daily

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7
Q

Conditions for Validity of DAF

A

o Only for first order kinetic (one compartment) in the therapeutic concentration range →What you excrete is proportionate to what’s in your body
o Metabolites of the drug are not active and non-toxic; otherwise, it would follow a 2 compartment model
o No difference in the absorption, metabolism and distribution of the drug between normal and uremic patients
o No alterations in drug sensitivity in uremic patients
o A direct relationship is assumed between ClCr and the renal elimination of the drug
o Stable kidney function

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8
Q

Reduction in Drug Dosage Depends on? (3)

A
  1. Therapeutic Index of Drug
  2. Proportion of Renal Clearance of Total Clearance
  3. Severity of Renal Impairment
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9
Q

How does renal damage affect drugs in terms of protein bound forms?

A

With less albumin present, the drugs that are unbound are in their active form and as such would be stronger than usual

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10
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Amoxicillin

A

Slight decrease

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11
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Bilirubin

A

Decrease

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12
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Cefazolin

A

Decrease

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13
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Furosemide

A

Decrease

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14
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Indomethacin

A

Normal

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15
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Cefoxitin

A

Decrease

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16
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Clofibrate

A

Decrease

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17
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Diazoxide

A

Decrease

18
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Phenobarbital

A

Decrease

19
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Phenytoin

A

Decrease

20
Q

[Binding to Plasma Proteins in Patients with Poor Renal Function]

Salicyclate

A

Decrease

21
Q

How do you achieve diuresis in patients with renal disease?

A

Loop Diuretics

22
Q

What can you never give pregnant women at any stage?

A

ACE Inhibitors, they would cause renal damage

23
Q

Most important drug you cannot give to patients with renal failure

A

Potassium, since only kidneys excrete K

Highly cardiotoxic

24
Q

Most Common of Pathway of Biotransformation in the Liver?

A. Conjugation
B. Oxidation
C. Sulfuridation
D. Glucorination

A

A

25
Q

Filipinos are rapid acetylators

A

Hi! This is a note card! Give yourself a 5. Unless you just read this now, maybe give yourself a 3. Then a 5!

26
Q

2 Examples of Hetapic Derangement that can Affect Drug Fate and Action

A
  1. Hepatocellular loss with absolute decrease in quantity of Drug Metabolizing Enzymes
  2. Effect of Altered Perfusion
27
Q

Which drug will give more adverse reactions with cirrhosis?

Lidocaine ER: 0.9
Antipyrine ER: 0.1

A

Lidocaine, because of the high extraction ratio

28
Q

Large volume of distribution indicates high affinity of drug to tissues or plasma?

A

Tissues

29
Q

Define: Extraction Ratio

A

Extent to which a drug is cleared in one passage in the liver

30
Q

What are the drugs that can have prolonged or unchanged Half-Life?

A

Pentobarbital
Phenytoin
Prednisone
Tolbutamide

TP3

31
Q

Liver problems cause losses of which vitamin?

A

Vitamin K

32
Q

Examples of Drugs Extensively Metabolized by the Liver

A

Benzodiazepines
NSAIDs
Opiods

33
Q

Plasma Volume increases by how much during pregnancy?

A

40-50%

34
Q

Effect on:

Plasma Albumin Levels
Plasma Total Protein
A1 Acid Glycoprotein

A

PA: Decreases
PTP: The Same
A1AG: The Same

35
Q

Example of a drug that would increase in concentration during pregnancy?

A

Probenicin

Drug with high protein binding affinity

36
Q

What causes the delay in gastric emptying time in pregnant women?

A

Progesterone, increased during pregnancy

37
Q

[Pregnancy]

What happens to acid secretion during the 1st, 2nd, and 3rd trimester?

A

1st: Decreased
2nd: Decreased
3rd: Increased

38
Q

Effect of Smoking on Babies in Utero

A

Low Birth Weight

39
Q

Effect of Drugs on Fetus Before 20th Day

A

All-or-Nothing Effect

40
Q

Effect of Drugs on Fetus 3rd to 8th Week (3)

A
  1. No Measurable Effect/Abortion
  2. Permanent Subtle Metabolic/Functional Defect
  3. Sublethal Gross Anatomic Defect
41
Q

Effect of Drugs on Fetus 2nd and 3rd Trimester

A

Altered growth and function of normally formed organ and tissues

42
Q

Most delicate organ that can be affected at any point of growth in utero and onward

A

Reproductive System

The Brain is also counted