1. To what class of drugs does nifedipine belong?
  2. What are the indications for nifedipine?
    • HTN
    • Stable or vasospastic angina
  3. Is nifedipine a DHP or Non-DHP CCB?
  4. Target MOA: which type of calcium channels does nifedipine block?
    L-type (cardiac, vascular smooth muscle).
  5. Target MOA: which type of vascular smooth muscle contains L-type calcium channels?
    • Coronary arteries
    • Systemic arteries
  6. Target MOA: true or false?

    Venous smooth muscle is more sensitive to clacium usage than arteriolar smooth muscle.
    False. CCBs therefore exert more effects on arteriolar smooth muscle.
  7. Target MOA: when nifedipine causes blood vessels to dilate, what happens to TPR? What overall effect does this have?
    TPR decreases, which utlimately decreases BP.
  8. Target MOA: what is the effect of the vasodilation of coronary arteries?
    Increased oxygen is delivered to myocardial tissue.
  9. Target MOA: true or false?

    Nifedipine's action to decrease BP is not immediate, and therefore sustained release formulations are common.
    • False.
    • Onset occurs rapidly, and sustained release formulations are often used.
  10. Target MOA: why does decreased intracellular Ca++ lead to smooth muscle relaxation?
    The activity of myosin light chain kinase (which activates myosin light chain) is dependent on calcium for activation.
  11. What are some adverse effects associated with nifedipine?
    • Flushing (from cutaenous vascular relaxation)
    • Gingeval hyperplasia (dilation of vessels in gums causes swelling)
  12. True or false?

    CCBs like nifedipine are targeted at the extracellular site of calcium channels.
  13. To which of the three conformations of caclium channels does nifedipine bind/inhibit?
    DHP CCBs bind during calcium channel depolarization and stabilize the channel's "inactive" state. Therefore the channel must be open before the drug can bind --> "use dependent" binding.
  14. True or false?

    Nifedipine's action may be termed "frequency dependent."
    • True.
    • Nifedipine binds and unbinds rapidly over and over again over time.
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