Pharmacology Exam Ib

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Anonymous
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32272
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Pharmacology Exam Ib
Updated:
2010-09-01 16:11:12
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Pharmacology
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Pharmacology
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  1. Factors controlling extent and speed of distribution of drugs
    • Blood profusion of various organs
    • Binding of drug to proteins in blood
    • The nature of capillaries
    • Mechanisms of drug transport with in the target organ
  2. Organs with high blood profusion
    • Brain
    • Kidney
    • Liver
    • Lungs
  3. Organs with poor blood profusion
    • Skeleton
    • Fat
  4. Organs with mid-level profusion
    Skeletal muscle
  5. Proteins in plasma that bind drugs
    • Albumin
    • Alpha 1 acid glycoproteins
  6. Albumin
    • 50% of proteins in plasma
    • affinity to bind weak acid drugs
  7. Alpha 1 acid glycoproteins
    • Affinity for weak base drugs
    • much less abundant than albumin
  8. Organs with Leaky capillaries
    • better drug delivery
    • kidney
    • liver
  9. Organs with tight capillaries
    • Poor drug delivery
    • Brain
  10. Intersticial Transport Mechanisms
    • Conductive = drug travels well
    • Non-conductive = drug will not travel well
  11. Free drug in blood reflects
    • free drug in organs
    • Free drug in circulation is in equillibrium with drug in organs
  12. Malnutrition
    • Lowered proteins in the body
    • Lower binding of weak acid drugs to albumin
    • Increased free drug concentration in circulation
    • More drug distribution
  13. Fasting for a long period of time
    lowered proteins
  14. Free Fatty Acids from diet
    • Bind albumin
    • Compete with weak acid drug for binding
    • May result in a higher free drug concentration if fatty acid has a higher affinity for albumin than drug
  15. Effects of aging on distribution of drugs
    • Decreased plasma albumin
    • Increased Alpha 1 Acid Glycoproteins
    • Decreased body water
    • Decreased lean body mass
  16. Decrease in albumin
    more weak acid drug distribution
  17. Increased alpha 1 acid glycoproteins
    lower distribution of weak base drugs
  18. Decreased body water
    less opportunity for drug to disperse resulting in higher drug concentrations in the body.
  19. Decreased lean body mass
    • increased fat
    • lipid soluble drugs hide in fat
  20. Drug Metabolism
    • Alteration in chemical structure of a drug
    • Enzymatic or non-enzymatic
  21. Purpose of drug metabolism
    • Make the drug less lipid soluble and more water soluble
    • Promote excretion
  22. What happens to a drug when it is metabolized
    • Pharmacological activation
    • Pharmacological inactivation
    • Toxification
    • Detoxification
    • A combination of any of the above
  23. Pharmacological activation
    • Prodrug -> Drug
    • Not the most common
  24. Pharmacological inactivation
    Most drugs are rendered inactive when they are metabolized.
  25. Toxification
    body changes a harmless entity into a harmful entity
  26. detoxification
    most common
  27. Liver
    Major organ of metabolism
  28. Hepatocytes
    • Major cells of metabolism in the liver
    • Nucleus
    • Mitochondria
    • Endoplasmic Reticulum
    • Cytosol
  29. Microsomes
    Endoplasmic Reticulum
  30. Phase 1 Metabolic Reactions
    • First wave of reactions to which the drug is subject
    • Drugs may bypass phase 1 and go directly to phase 2
    • Reduction
    • Hydrolysis
    • Dehalogenation
    • Oxidation
  31. Microsomal Oxidation Reactions
    • Side chain hydroxylation
    • Aromatic hydroxylation
    • O-Dealkylation
    • N-Dealkylation
    • S-Dealkylation
    • Sulfoxidation
  32. Non-microsomal oxidation reactions
    Enzymes present in every other cell compartment
  33. Phase 2 Metabolic Reactions
    • Further metabolism
    • Increase solubility
    • Decrease lipid solubility
    • Synthetic Reactions
    • Conjugation Reactions

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