pharm 1

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  1. pharmacotherapeutics?


    desired outcome of admin of a drug

    indication, therapeutics
  2. 3 therapeutic effects of drugs?
    Tx s/s, cure, prevent
  3. How are pharmacotherapeutics of a drug determined?
    clinical drug trials are sent to the FDA
  4. Off label use of a drug?
    using a drug in a way that is not therapeutically OK'd for by the FDA
  5. Should the nurse question off label uses of meds?

    When is this OK?
    yes, but it is OK if the literature supports use of the drug for other things or the doctor can explain why they are using it
  6. Pharmacokinetics?
    movement of drug particles in the body and the processes that occur during this movement

    the effect of the body on the drug
  7. 4 phases of pharmacokinetics?
    • 1. absorption
    • 2. distribution
    • 3. metabolism
    • 4. excretion
  8. Absorption?
    the movement of the drug from the site of admin to the bloodstream
  9. Distribution?
    movement from blood -> tissues -> cells
  10. Metabolism?
    drug is converted into another substance or substances
  11. Excretion?
    removal of the drug or drug substance after metabolism
  12. What must occur for drugs to move through the body?
    must pass cell membranes
  13. 3 ways that drugs pass through cell membranes?
    1. pass b/t spaces of channels b/t molecules in the membrane if the drug molecules are very small

    2. use transport system that may not require use of enery

    3. penetrate the membrane directly - if soluble in lipids
  14. What method of entering cell membranes is the most commonly used by drugs?
    direct penetration
  15. Describe a polar molecule.

    Can polar molecules penetrate the cell membrane?
    There is a neutral overall charge but one end is positive and the other end is negative

    no, they are hydrophilic
  16. What are ions?
    molecules with a net charge
  17. Ionization?
    `process of inducing a molecule to carry a charge
  18. What will happen to acids in a basic environment?

    Bases in an acidic environment?
    acids give up a positive charge in a basic env and bases accept a positive charge in an acidic env
  19. What will happen to most molecules if they become ionized?
    they will not be able to pass through the cell membrane....very small ions can pass through channels but most cannot pass at all
  20. What will occur if the pH on either side of the cell membrane differs?

    What is this process called?
    the molecules tend to go to the side where they will ionize.  Once they get there, they cannot pass back through

    ion trapping or pH portioning
  21. How may the movement of drug molecules be altered?
    altering the pH on one side of the membrane
  22. What is the completeness of absorption?
    the portiuon of the drug that is absorbed
  23. 2 factors that affect the rate of absorption?
    1. route of admin

    2. rate of absorption / rate of dissolution
  24. Route rate of absorption in order?
    • 1. oral
    • 2. SQ
    • 3. IM
    • 4. IV
  25. Large surface area increases/decreases the rate of absorption?
  26. How does blood flow affect rate of drug absorption?

    Implications for patients with impaired circulation?
    increased blood volume = increased rate of absorption

    they do not absorb drugs as quickly as others do
  27. thins that affect the rate of absorption?
    • 1. surface area
    • 2. blood flow volume
    • 3. lipid solubility
    • 4. pH differences b/t site of admin and plasma
    • 5. physiological condition of the pt
  28. How does pH b/t site of admin and plasma affect drug absorption?
    will be absorbed faster if if pH diff. favor the molecules being ionized in the plasma
  29. 3 factors that affect the distribution of a drug throughout the body?
    • 1. blood flow to the tissues
    • 2. drug's ability to leave the blood
    • 3. drug's ability to enter cells
  30. 2 types of pathophysiologic conditions that are mostly avascular?
    1. abscesses - pus-filled pockets surr. by normal tissues

    2. solid tumors
  31. Where does the drug leave the vascular space?
    in the capillary bed b/t the widely spaced cells here
  32. How do proteins affect the distribution of drugs?
    drugs form reversible bonds with proteins/albumin

    drug molecules attached to albumin/protein cannot pass through cap walls and will have no effect - drugs that are highly protein bound will require higher doses to have an effect

    the bonds are reversible and will eventually dissolve and leave the drug free to act
  33. How does protein-binding of a drug affect its dosing?

    What may occur if a person has abnormal protein levels?
    drug dosages are calculated based on drug protein-binding ability and normal protein in the body

    if protein levels are abnormally low then there will be an abnormal amount of free drug in the body and may overdose
  34. Displacement in relationship to protein binding?
    if 2 drugs are given and 1 has more affinity for albumin the other drug will be displaced from the albumin and will be more highly distributed than normal - will need to reduce it's dose
  35. 2 ways drugs may cross the BBB?
    • 1. lipophilic
    • 2. have a transport system
  36. The placental membrane separates ___ from ___. 

    How does it differ from other membranes in the body in relation to drug molecules passing?
    separates maternal and fetal circulation

    any molecule that can pass through a membrane can pass through the placenta
  37. In order to pass through the placenta a molecule must be ____, _____, and not ____ ____.
    • 1. lipophilic
    • 2. non-ionized
    • 3. protein-bound
  38. How may hepatic dysfunction affect drug distributuion?
    causes less albumin = increased drug free in body
  39. Consideration when giving infants meds that work on brain?
    BBB is not fully dev. and drugs may have increased affect
  40. How can malnutrition affect the distribution of drugs?
    albumin will be decreased = increased free drug
  41. How may alcohol affect the distribution of drugs?
    affects the liver - lower albumin
  42. How may obesity affect the distribution of drugs?
    if drugs are highly lipophilic they will go to adipose cells and circulating levels will be decreased
  43. Where does drug metabolism occur?
    mostly in the liver

    also in the sm int, lungs, kidney, brain, olfactory mucosa, and skin
  44. Pt who have decreased drug metabolism?

    What effect does this have?
    neonates, children, and older adults

    can decrease metabolism and increase adverse effects from the drug
  45. How may malnutrition affect the metabolism of drugs?
    may prolong drug effects r/t poor hepatic metabolism
  46. How may obesity affect the metabolism of drugs?
    can increase the rate of transformations = need higher drug doses
  47. Biotransformation?
    another term for the metabolism of a drug into other forms
  48. What usually occurs when a drug is metabolized?

    drug will be changed from lipophilic to hydrophilic so it can be excreted in the renal system
  49. Metabolite?
    products of metabolism
  50. Prodrugs?
    drugs that are incative until metabolized into an active form
  51. Most drugs are metabolized into active/inactive form?
  52. What does it mean if a drug is highly metabolized?
    every time it passes through the liver in circulation a large number of drug molecules are metabolized
  53. First-pass effect?
    drugs that are taken orally go -> portal vein -> liver where most of the drug will be metabolized and not a lot will circulate

    may need higher doses to get therapeutic effect or give by another route so it doesn't go strait to liver
  54. Describe how drug is metabolized in liver based on percetage and number of drug molecules metabolized with each pass?
    same percentage of drug molecules will be metabolized with each pass but there will be less number of molecules metabolized with each pass b/c the drug number in body will be decreasing
  55. Cytocrome P-450 system?
    enzyme system that predominantly carries out metabolism
  56. Where is most of the P450 system located?
    in the liver
  57. How may drugs affect the p450 system?

    How will this affect other drugs?
    drugs can stim or repress enzyme p450 enzyme synth

    this can alter the met. of other drugs/substrates for that enzyme

    if the enzyme is increased the drug will be met. faster and their will be less drug circulating
  58. What will occur if 2 or more drugs are met. by the same enzyme?
    they will compete for the enzyme and at least one of them will have altered met.
  59. Why does each individual met. drugs differently?
    genetic differences is isoenzymes
  60. If a person poorly metabolizes a drug how will this affect the amount of circulating levels of the drug?

    What may occur?
    the circulating level will be higher than expected

    more therapeutic affect and more side effects
  61. What will drug levels be like if a person is a rapid metabolizer?

    What may need to be done?
    lower than normal circulating levels

    increase dosage
  62. How can grapefruit affect the p450 system?

    How does this affect drug metabolism?
    decreases isoform 3A in the intestines but does not affect the liver amnt

    drugs that rely on 3A for met. will have higher levels
  63. What is St John's Wart?

    How may it affect the p450 system?
    herb for depression

    • opposite effect from grapefruit
    • (increases 3A)
  64. How may inflammation affect the p450 system?
    can increase enzymes and metabolism of drugs

    the drugs will be ineffective without higher doses
  65. How may body temp affect the p450 system?
    hypothermia can decrease met. of drugs and their effectiveness and can increase adverse affects
  66. Most common route for drug excretion?

    Other routes?

    GI, sweat, lungs, saliva, breast milk
  67. Major pathophysiologic change that can affect drug excretion? - 3 things that may cause this?

    What other body system can decrease excretion if damaged?
    • decreased renal functioning: 
    • 1. decreased CO = decreased perfusion
    • 2. elderly
    • 3. renal drug toxicity

  68. 3 processes involved in renal excretion?
    • 1. glomerular filtration
    • 2. tubular reabsorption
    • 3. active tubular secretion
  69. How does drug get from bloodstream into renal system?
    drug enters the glomerulus through caps around it unless they are bound to proteins which are too big to pass through
  70. What occurs during tubular reabsorption of a drug?

    When will this not occur?
    the conc. gradient of the drug causes it to go from the renal tubule back into the blood stream so that only some of the blood is excreted

    this will not occur unless the drug is lipophilic - if the met. of the drug makes it hydrophilic all of the drug will be excreted
  71. What occurs during active tubular secretion of a drug?
    active transport systems in the renal tubule move some drugs from the blood into the urine
  72. What 2 types of drug metabolites are hydrophilic and cannot undergo tubular reabsorption?
    ions and polar compounds
  73. How can the renal excretion of a drug be encouraged?

    How can this be useful?
    if the pH of the urine causes the drug to ionize then the drug will be excreted b/c it will not be able to be reabsorbed

    urine is acidic and if the drug is basic = ionization and if the urine is made more basic by a drug then it can be made to ionize a toxic acid to encourage its excretion
  74. What may occur is 2 drugs are taken together that both use the active transport system?

    How can this be used to advantage?
    the drugs will compete for the active transport and be in the system longer than normal

    2 drugs may be given together in order to deliberately slow their rate of excretion
  75. Factor that affects excretion of durgs through bile?

    How does this occur?
    enterohepatic recirculation

    some of the bile that leaves the liver -> intestine is reabsorbed into the portalk circulation and returned to general circulation = drug molecules are reabsorbed
  76. Half-life?

    How is it expressed?
    amount of time that is required to remove half of the blood conc of a drug\

    will always be a percentage
  77. What will happen to the half life a drug if the pt has renal or liver problems?
    the half life may be longer
  78. Steady state?

    How long does it take for this to be achieved?
    the amount of drug coming in matches the amount being excreted

    4 to 5 half lives
  79. Can steady state be achieved faster by increasing the dose of the medicine?
    no, it is achieved based on the amnt of time required for 4 to 5 half lives to occur
  80. When can the full pharmacotherapeutic response of a drug be measured?

    What implications does this have?
    once the drug has reached steady state

    before adjusting a dose must allow steady state to occur to measure effects of the drug
  81. What may be done if therapeutic effect of a drug is needed quickly and can't wait for steady state?
    loading dose = high level of the drug so get therapeutic effect
  82. Clearance?
    rate in which the drug is cleared from the circulation
  83. 2 major modes of clearance?
    renal excretion and hepatic metabolism
  84. Pharmacodynamics?
    biological, chem, and physiologic actions of a drug withing the body and study of how these actions occur
  85. How do drugs cause therapeutic responses?
    they turn on/off, promote, or block the body's already existing functions - they cannot make the body do a new function
  86. How do most drugs create their effects in the body?
    they attach to cell receptors and stim the cell to act or block other molecules from attaching to the receptor
  87. How do drugs attach to body cell receptors?
    using hormones, NT, etc
  88. Agonist drugs?
    drugs that attach to a receptor and stim cell to act
  89. Antagonist drugs?
    drugs that attach to receptors in order to block other stimulatory molecules from attaching
  90. Intrinsic activity of a drug?
    drug's ability to stimulate its receptor
  91. How may receptors change?

    Why does this occur?
    they may be become less sensitive or their numbers can be changed

    in response to stim. or inhibition
  92. What can occur if an agonist drug is cont. given?
    the receptors are cont stimulated and may become less sensitive
  93. What can occur is an antagonist is cont. given?
    stim of the receptor is cont blocked and it may become hypersensitive
  94. How do nonreceptor drugs work?
    they interact chem with substances in the body
  95. MEC?
    minimum effect concentration - min. amnt of a drug required to have an effect at all
  96. What will occur with additional dosing after MEC is reached?
    response to drug increases as more drug is given until a plateau is reached and increasing the dose will have no effect
  97. Potency?

    What is the potency of the drug r/t?
    the amnt of drug that must be given in order to produce a particular response - it pharmacologic activity

    r/t to its affinity for receptors
  98. Efficacy of a drug?

    What is this r/t?
    how well a drug prod. its desired effect

    r/t its intrinsic activity
  99. ED50?
    dose that is required to produce the therapeutic response in 50% of the population  

    is used as the standard starting dose
  100. Maintenance dose?
    dose that is admin consistently over time
  101. LD50?
    dose that would be fatal in 50% of the population
  102. Therapeutic index?

    relationship of the ED50 to the LD50

  103. Narrow therapeutic index?

    The closer the therapeutic index is to ___ the more risk of OD.
    the LD50 and ED50 do not differ by much

  104. Therapeutic range?

    How is the measured?
    dose that reaches MEC but below the level at which adverse effects occur

    measure blood levels of the drug
  105. What must be noted if a blood sample is order for drug blood levels?
    must note when the last dose was given
Card Set:
pharm 1
2013-05-28 22:49:30

pharmacology test 1
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