Pharm 3:HTN drugs

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  1. Renin
  2. Angiotensinogen
  3. Angiotensin I (inactive)
  4. Angiotensin II (active)
    Powerful vasoconstrictor
  5. ACE
    • Enzyme which converts Angiotensin I to Angiotensin II
    • Found in all blood vessels. There is a lot of ACE present in the capillary rich lungs
  6. RAAS System
  7. ACE Inhibitors: Uses
    • Blocks conversion of Angiotensin I to Angiotensin II
    • Mild to moderate HTN
    • Treatment for heart disease (vasodilator)
    • May be used with a diuretic
    • Diabetic prophylatic against renal failure
    • Reverse damage in coronary vessel and kidney
    • Prevent coronary remodeling
  8. captopril
    • Capoten
    • ACE inhibitor
  9. lisonopril
    • Prinivil
    • Zestril
    • ACE inhibitor
  10. ACE inhibitors: ADRs
    • Dry hacking cough (chief reason for discontinuation)
    • First dose effect: significant drop in BP
    • Hyperkalemia if also taking K+ products
    • Severe renal insufficiency if only 1 kidney or bilateral renal stenosis
    • Fetal harm
    • Angioedema: discontinue if large wheals on tongue, pharynx, or glottis
  11. Angiotensin II Antagonists (ARBs)
    • Angiotensin II Receptor blockers
    • Block action (vasoconstriction and aldosterone production) of Angiotensin II
    • Block binding of Angiotensin II to angiotensin receptors
    • Uses: HTN, HF, Diabetic nephropathy, MI,and stroke prevention
  12. ¬ólosartan
    • Cozaar
    • Angiotensin II Antagonist
    • Newer than ACE inhibitor
    • No cough
  13. Angiotensin II Antagonist: ADRs
    • angioedema
    • renal failure
    • teratogenic
  14. Direct Renin Inhibitor
    • Prevents conversion of angiotensinogen to angiotensin I: blocks the entire RAAS system
    • Low absorption especially with a fatty meal
    • Works in top of renal system (proximal tubules?)
    • Affected by CYP3A4 enzyme system
    • ADR: tetrogenic, diarrhea, less cough, and less angioedema
  15. aliskiren
    • Tekturna
    • Direct Renin Inhibitor
  16. Aldosterone antagonist
    • Blocks aldosterone receptors in kidneys
    • Results in excretion of Na+ and water and retention of K+
    • Effective for HTN and HF
    • Caution: hyperkalemia
  17. Eplerenone
    • Inspra
    • Aldosterone antagonist
  18. Calcium channel blockers (action)
    • Block slow Ca channels which prevents Ca from entering cell - decrease smooth muscle contractions resulting in vasodilation and decreased PVR
    • Do not act on veins
  19. Diltiazem
    • Ca channel blocker
    • Acts on heart and vascular smooth muscle
  20. Ca channel blockers (uses)
    • HTN
    • Cardiac arrhythmias (slows ventricular HR)
    • Angina pectoris (causes vasodilation)
  21. Ca channel blockers: ADRs
    • Constipation (blocks smooth muscle in intestines)
    • Dizziness, facial flushing, headache, edema in ankles and feet
    • cardiac: bradycardia in susceptible pts.
  22. nifedipine
    • Procardia
    • Ca channel blocker
    • Acts on vascular smooth muscle only
  23. verapamil
    • Calan, Isoptin
    • Ca channel blocker
    • Acts on heart and vascular smooth muscle
    • opposes reflexive tachycardia
  24. Beta-adrenergic blockers: Actions
    • Compete with epinephrine for beta receptors
    • Block beta1 receptors (heart): decreased HR, decreased contractility, decreased CO
    • Block beta2 receptors (lungs): bronchospasms
    • uses: HF, post MI, HTN
  25. Atenolol
    • Tenormin
    • Selective beta blocker (blocks only beta1 sites)
  26. Metoprolol
    • Lopressor
    • Selective beta blocker (blocks only beta1 sites)
  27. carvedilol
    • Coreg
    • Nonselective beta blocker
    • Do not give to asmatics or people with respiratory distress
  28. propranolol
    • Inderal
    • Nonselective beta blocker
    • Do not give to asmatics or people with respiratory distress
  29. Beta blockers: Properties
    • relief of anxiety
    • little volume retention
    • antianginal
    • post MI protection
    • reverse left ventricular hypertrophy
  30. Beta blockers: ADRs
    • Bronchospasm (don't give to asmatics)
    • mask hypoglycemia (caution with DM)
    • Fld retention to HF
    • impotence
    • cold extremities
    • increased triglycerides
    • decreased HDL
    • exercise intolerance
  31. Vasodilators: uses
    • HTN
    • angina
    • HF
    • MI
  32. hydralazine
    • Apresoline
    • vasodilator: arterioles
    • decreases peripheral resistance
    • uses: HTN, HTN crisis (parenterally), HF
    • ADR: reflexive tachycardia, salt and H20 retention, heart failure, drug-induced lupus
  33. minoxidil
    • Loniten or Rogaine
    • Similar to hydralazine but more intense
    • ADRs more intense too
    • uses: severe HTN, unresponsive to other drugs
    • ADR: hypertrichosis (Rogaine)
  34. sodium nitroprusside
    • Nipride
    • Acts directly on both arteries and veins
    • Quick reduction of BP of pt in HTN crisis
    • metabolized to cyanide; measure thiocyanate levels
    • caution: prolonged use
  35. clonidine
    • Catapres
    • centrally acting sympathetic nervous system inhibitors
    • block sympathetic nervous system
    • PO and transdermal
    • Other uses: migraine, pain, opioid withdrawal
  36. Centrally acting sympathetic nervous system inhibitors
    • action: decreases sympathetic tone = peripheral vasodilation
    • uses: mild to moderate HTN (not first line, better drugs available)
  37. prazosin
    • Minipress
    • Sympatholytic
    • Action: decrease PVR and CO
    • Uses: mild to moderate HTN
    • ADRs: orthostatic hypotension (give at bedtime), resistance/tolerance, Na+ & fluid retention
  38. Drugs for HF
    • beta blockers (decrease LV fx, decrease HR, survival)
    • diuretics (esp thiazide and loop: decrease fld vol excess, edema, workload)
    • Renin inhibitors (ACE and ARBs): increase renal flow, decrease HTN, decrease cardiac remodeling
  39. digoxin
    • Lanoxin
    • cardiac glycoside
    • increase contraction, decrease HR
    • rapid onset, short duration
    • digitalis - foxglove (native plant in N. America)
  40. digoxin: uses
    • congestive HF: systolic (inability to pump)
    • dysrhythmias (atrial fib, atrial flutter, surpraventricular tachycardia)
    • slows conduction through AV node (dromotropic)
    • inotropic: increase contraction
    • chronotropic: decrease HR
    • does not prolong life (2nd line drug)
  41. digoxin assessment
    • apical pulse: ADR = decr HR (<60 adult, <70 child, <90 infant)
    • monitor serum electrolytes: hypokalemia can cause digoxin toxicity
  42. dopamine
    • Intropin
    • Positive inotropic
    • Given for shock: increase BP, increase CO, increase urine output
    • low dose: increase urine output
    • med dose: increase urine output, increases CO
    • high dose: renal vasoconstriction = decrease urine output and increase BP (DO NOT WANT THIS)
  43. inamrinone
    • Inocor
    • inotropic agent
    • increases contraction, promotes vasodilation
    • Use: if not responding to other drugs; usually short term in hospital
  44. Class Ia antiarrythmics
    • Blocks Na+ channels: slows
    • Slows conduction velocity in atria, ventricles
    • Delays time for heart to repolarize for another impulse
  45. quinidine
    • sulfate, gluconate
    • Class Ia antiarrhythmics
    • uses: AF (atrial fibrillation), PVC (premature ventricular contraction), VT (ventricular tachycardia)
  46. procainamide
    • Pronestyl
    • Class Ia antiarrhythmics
    • uses: AF (atrial fibrillation), PVC (premature ventricular contraction), VT (ventricular tachycardia)
  47. quinidine: ADRs
    • diarrhea (may become severe)
    • cinchonism- tinnitus, vertigo, visual disturbances, hearing loss, confusion
    • cardiac toxicity
    • used in sustained VT, atrial fib, and atrial flutter
  48. procainamide
    • measure CBC with 1st therapy as leukocytes, neutrophils, and platelets may drop
    • if antinuclear antibody elevated for prolong use may lead to lupus
    • useful for terminating VT and VF
  49. Class 1b antiarrhythmics
    • Blocks sodium influx: slows conduction
    • accelerate the repolarization phase
  50. lidocaine
    • Xylocaine
    • Uses: ventricular dysrhythmias (PVC, VT)
    • treats both acute and chronic conditions
  51. lidocaine
    • loading dose - IV push (50 mg/min)
    • continuous infusion: 1-4 mg/min
    • ADRs: (parasthesia, numbness, agitation, disorientation)
    • Do NOT give lidocaine with preservative
  52. Class Ic antiarrhythmics
    • Action: blocks sodium channels: slows
    • depresses sinus node automaticity
    • prolonged conduction in the atria,, AV node, ventricle,
    • uses: life-threatening arrhythmias refractory to other antiarrhythmics
  53. propofanone
    • Rythmol
    • Class Ic antiarrhythmic
    • may make VT worse
    • May decrease myocardial contractility, exacerbating HF
Card Set
Pharm 3:HTN drugs
ACE inhibitors, Ca Channel blockers, beta blockers
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