Pharm- Drug Elimination.txt

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Mawad
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300806
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Pharm- Drug Elimination.txt
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2015-04-14 16:49:18
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vetmed pharm elimination
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vetmed, pharm drug elimination
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  1. The sum of chemical reactions in which an endogenous or exogenous substrate is converted into a larger molecule or a smaller molecule.
    Metabolism
  2. Metabolism plays an important role in the ________ and ________ of drugs.
    inactivation; elimination
  3. Kidneys provide a concentration gradient which favors...
    passive resorption of lipid-soluble molecules back into the blood.
  4. The development of metabolic pathways renders lipid-soluble materials that would normally be resorbed back into the blood at the kidneys...
    less lipid soluble and less likely to be resorbed, thus eliminated more quickly.
  5. The primary site for drug metabolism.
    the liver
  6. The system of enzymes located on the smooth endoplasmic reticulum that is the primary site for drug metabolism and endogenous steroid metabolism.
    hepatic microsomal system
  7. A hyperbolic curve that provides estimates of maximal reaction velocity (Vmax) and the apparent Km.
    Michaelis-Menten metaboilsm
  8. What is phase I of drug metabolism?
    oxidations, reduction, hydrolysis, deaminations
  9. Phase of drug metabolism that transforms the molecule to a more polar product which then may be excreted.
    Phase I
  10. What are phase II reactions of drug metabolism?
    conjugated of glucronic acid, glycine, etc. are added
  11. The phase of drug metabolism in which the addition of a conjugate increased the polarity of the drug molecule and the size, making is much less likely to be resorbed at the kidney.
    Phase II
  12. Phase ___ products sometimes retain biological activity, but Phase ___ products are rarely active.
    I; II
  13. The primary phase I reactions, _________ and __________, are carrier out by the __________, which requires... (3)
    oxidation and reduction; electron transport system; molecular oxygen, reduced NADPH, and cytochrome P450
  14. The phase II reactions are _______ in nature; they can be limited in their rate or capacity by... (2)
    synthetic; limited amounts of transferase enzyme, limited amounts of conjugate substrate
  15. Metabolic transformation can result in... (3)
    inactivation of an active drug, activation of an inactive drug (prodrug), and conversion of one form of an active drug to another active form.
  16. Acetominophenis a(n) ________ that is metabolized to a(n) ____________, which leads to ____________.
    active drug; reactive intermediate; hepatic necrosis
  17. Benzo[a]pyrene is a(n) ___________ that is metabolized to a(n) ____________, which is ___________.
    active drug; reactive intermediate; carcinogenic
  18. Two important properties of drug metabolism are...
    enzyme induction and enzyme inhibition.
  19. When one drug stimulates or induces enzymes for its own metabolism and the metabolism of the other.
    enzyme induction
  20. With enzyme induction, the dosage of the second drug will need ____________.
    to be adjusted
  21. When one drug competitively or non-competitively inhibits the metabolism of another drug.
    enzyme inhibition
  22. The u=inhibited drug may require that its dosage rate be __________ to __________.
    lowered; avoid toxicity
  23. With enzyme induction, when an active drug is metabolized to an inactive molecule, you need ________ drug.
    more
  24. With enzyme inhibition, when an active drug is metabolized to an inactive molecule, you need ________ drug.
    less
  25. With enzyme induction, when an inactive drug is metabolized to an active molecule, you need ________ drug.
    less
  26. With enzyme inhibition, when an inactive drug is metabolized to an active molecule, you need ________ drug.
    more
  27. The ________ is principally responsible for drug excretion.
    kidney
  28. Many polar drugs depend on excretion of the ________, __________ form of the drug as the main means of elimination.
    active, unmetabolized
  29. There is significant _____________ in herbivores.
    salivary excretion
  30. There is significant __________ in the lactating female.
    mammary excretion
  31. The kidney functions ___________ to maintain body fluid composition and balance.
    homeostatically
  32. What are the steps of filtration in the kidney? (5)
    systemic circulation--> glomerular filtration --> active tubular secretion <--> passive and active tubular resorption --> excretion
  33. The glomerular membrane acts as a filter, allowing _________ and _________ of the plasma to enter the nephron, while excluding ________ and ________.
    water; solutes; blood solutes; large proteins
  34. Filtration through the glomerulus is driven by _____________.
    hydrostatic pressure
  35. The processes of _________ and ________ modify the tubular fluid in the tubule.
    reabsorption; secretion
  36. Active transport mechanisms occur primarily in the _________ of the kidney.
    proximal tubule
  37. Most ________ solutes diffuse passively from higher concentration within the tubular fluid back to the blood via peritubular capillaries.
    lipid-soluble
  38. Drugs that are _____________ are not filtered at the glomerulus but are secreted by active transport.b
    bound to protein
  39. __________ accounts for the retention of many lipid-soluble substances, but substances that do not easily diffuse across membranes can be resorbed by _____________.
    Passive reabsorption; active reabsorption
  40. The rate of renal excretion of a substance is summarized by what 3 processes?
    filtration, secretion, and reabsorption
  41. The volume of blood which would be required to contain the amount drug which is removed per unit of time; the rate of removal from thhe total body or from a specific organ.
    clearance
  42. Changes in ___________ or _____________ will affect a drug dosage schedule.
    elimination rate; volume of distribution
  43. Two clearance mechanisms that are related to renal drug elimination.
    GFR and effective renal plasma flow (ERPF)
  44. A substance which is almost completely removed in one passage through the kidney can be used to measure ________.
    ERPF
  45. As clearance increases, half-life _______.
    decreases
  46. As volume of distribution increases, half-life ________.
    increases
  47. Inulin is only cleared by _________.
    filtration
  48. If clearance ratio is <1, _________ has taken place.
    reabsorption
  49. If clearance ratio = 1, then ___________.
    filtration removes the drug or filtration= secretion
  50. If clearance ratio > 1, __________ has taken place.
    secretion
  51. Drugs that are weak acids or bases will ____________ from the ___________ to the __________.
    passively diffuse; tubular fluid; blood (based on their degree of ionization)
  52. If the concentration of drug exceeds the capacity of the transport system, then __________ occurs and the rate of _________ becomes limited.
    saturation; secretion or reabsorption
  53. If a drug is excreted by filtration but not secretion, then only ___________ is available for filtration and excretion. If a second drug competes with the first for protein binding so that more drug is _______________, the rate of excretion of the first drug will _________.
    free, unbound drug; free to be filtered; increase
  54. If a drug is protein bound and also actively secreted so that not only free drug but also bound drug become cleared as it passes through the kidney, if you cause less drug to be bound, excretion can be ________.
    slowed
  55. Diuretic drugs __________ drug excretion by.... (2)
    increase; decreasing the conc gradient that drives passive reabsorption and by decreasing contact time resorption in the tubules by increased flow.
  56. Drugs which are extensively and rapidly removed by the liver following oral administration undergo ____________.
    first-pass effect
  57. Drugs enter the bile by a ____________.
    active transport secretory mechanism
  58. The proportion of drug in the bile compared to the urine increases as ____________ increases.
    molecular size
  59. Dogs, rats, and chickens are classified as _______ excreters; cats and sheep are ___________ excreters; rabbits, guinea pigs, and primates are ________ excreters.
    good; moderate; poor
  60. Unmetabolized drug secreted in the bile to the intestine ill undergo reabsorption according to its ______________; drug that are __________ at the pH of the intestine will not be reabsorbed; ___________ drugs will largely be reabsorbed back into circulation.
    lipid-solubility; polar/mostly ionized; less polar/more unionized
  61. The major difference b/w renal and hepatic excretion is that...
    intestinal contents, unlike urine, are capable of altering/degrading the drug molecule through chemical or enzymatic processes.
  62. Extraction ratio (E) > 0.7 refers to those drugs which are __________ (i.e most drugs undergoing ____________); E <0.3 refers to drugs with ___________.
    highly extracted significant first-pass effect; low extraction [BY THE LIVER]
  63. Drugs with low extraction ratios are referred to as ____________ and depend on the _______________.
    capacity-limited; liver's intrinsic metabolic capability
  64. Drugs with low extraction ratios are cleared independently of _____________ but are sensitive to ____________ because clearance is limited to ____________.
    blood flow; protein-binding; free fraction of the drug
  65. Drugs with high extraction ratios are capable of ___________; they have _________-limited clearance and are not sensitive to ______________.
    high metabolic capacity; blood flow; changes in protein binding
  66. Drug elimination by milk, saliva, and perspiration are all primarily dependent on ____________ and _____________.
    passive diffusion; lipid-solubility of the drug
  67. With systemic treatment for mastitis, ___________ tend to concentrate in the mammary gland more than ________.
    basic drugs; acidic drugs

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