Cardiovascular Mindmap

  • Created by: Mohsin
  • Created on: 08-04-18 12:50
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  • Cardio Therapeutics
    • Calcium Channel Antagonists
      • Bind to calcium channel protein
      • Vasodilators
      • Found: Skeletal, cardiac and SM muscle contraction
        • Ischaemic cells tend to have longer action potentials than healthy cells
          • Ca channel is open longer -  VASOCONSTRICTION
            • If a drug is too water soluble it will undergo first pass metabolism and transferred to the kidneys - no systemic effect
      • 1st Gen:  Verapamil (Phenylalkylamines) - OPEN channel state
        • 1st Gen: Nifedipine (1,4-Dihydropyrines) - OPEN /CLOSED channel state
          • 1st Gen: Diltiazem (Benzothiazepine) - OPEN channel state
          • 2nd Gen: Felodipine, Isradipine, NIcardipine, Nimodipine
          • MOA: Through the phospholipid bilayer, acts on the closed ion channel
        • 2nd Gen: Anipamil, Bepirdil
        • MOA: hydrophilic pathway through the ion channel
          • 1st Gen: Diltiazem (Benzothiazepine) - OPEN channel state
      • 2nd Gen: more selective for vascular SM.
    • Henderson-Hasselbalch Equation
      • Acidic centres: 100/ (1+antilog (pka - pH)
      • Basic centres: 100/ (1+antilog (pH - pka)
      • If the ionisation is HIGH the drug will pass the open channel and vice versa
    • ACE (angiotensin covering enzyme)
      • Ace cleaves the amide bond between PHE and HIS
      • For ACE binding site: charged ZN and ARG (to hold in place)
      • ACE Inhibitors
        • Captopril
          • Thiol group will interact with the Zn and then carboxylic acid group will interact will ARG
          • Functional group side effects: rash and loss of sensation
            • stop therapy
          • Pro-drug
        • Enalapril and Ramipril
          • Pro-drugs
            • Centres very ionised = very water soluble
          • Require hydrolysis if ester to create the active di-carboxylic acid


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