Pharmacy 8260

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Contents

Fall 2014

Wednesday, October 8th

Class Notes

Monday, October 13th

Class Notes

Calculations

Review

Wednesday, October 15th

Assignments and Tests

Take-home (50%100% of grade)

In-class test (50%0% of grade)

  • The in-class test will be a significantly shorter version of your homework question (above) with a different drug.
  • New.jpg as of 11/17/14: No in-class test.

In-class (Not Graded)

Other

References

  1. Introduction to Drug Metabolism 3rd Ed. Published 2001.
  2. Drug Metabolism: Chemical and Enzymatic Aspects 1st Ed. Published 2007.
  3. Concepts in Clinical Pharmacokinetics Published 2014
    • Fairly easy book on pharmacokinetics.

Recommended Textbooks for the Class

  1. Physiologically-Based Pharmacokinetic (PBPK) Modeling and Simulations: Principles, Methods, and Applications in the Pharmaceutical Industry
  2. Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization

Useful Approximations

Flow Rate Approximations

  • Liver and Renal Blood Flow: QH=QR=1L/(kg*hr)
  • Glomerular filtration rate (GFR): GFR=0.1*QR=0.1L/(kg*hr)
  • Urine flow rate (UFR): UFR=0.01*GFR=0.001L/(kg*hr)

Mass Approximations

Organism

  • Adult Human: 70 kg (154 lbs.)
  • Adult Dog (Beagle): 10 kg [1]
  • Adult Rabbit: 4 kg [2]
  • Adult Guinea Pig (Dunkin Hartley): 1 kg [3]
  • Adult Rat: 0.3 kg [4]
  • Adult Mouse: 0.03 kg [5]

Organs/Suborgans

  • Brain: 20g/kg body weight [6]
  • Kidney: 2g/kg body weight [6]
  • Liver: 20g/kg body weight [7]
  • Lung: 8g/kg body weight [6]
  • Spleen: 2g/kg body weight [6]

References and Notes

  1. (Males 10 – 11 kg; Females 9 – 10 kg)
  2. (Male 3-5 kg,Female 3-5 kg.)
  3. (Male 1,000-1,200 grams,Female 900-1,000 grams.)
  4. (Male 250 – 300 g, Female 180-220 g)
  5. (Male 25-40 grams. Female 20-35 grams.)
  6. 6.0 6.1 6.2 6.3 Approximated from http://www.ncbi.nlm.nih.gov/pubmed/22182984
  7. 7.0 7.1 http://dmd.aspetjournals.org/content/27/11/1350.full.pdf+html
  8. Another reference with 40mg/g Liver http://www.bdbiosciences.com/documents/webinar_2009_12_metabolic_stability.pdf
  9. PharmPK Discussion List Archive
  10. Another reference with 40mg/g Liver http://www.bdbiosciences.com/documents/webinar_2009_12_metabolic_stability.pdf
  11. PharmPK Discussion List Archive