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ANTI- ANGINAL DRUGS




           Prashiddha
                     Dhakal
            MBBS (KUSMS, 11th)
What Is Angina?

   Central chest discomfort or pain due to
    transient ishemia of the myocardium

   Pain may radiate to one arm OR to both arms
    OR to neck OR to jaw OR to the epigastrium

   Duration- Less than 20min
Types Of Angina

   Classical/Typical/Stable/Exertional Angina
   Due to fixed and stable plaque

   Prinzmetal/Variant Angina
   Due to spasm of coronary artery

   Unstable Angina
   Due to unstable plaque (賊 thrombus)
Pharmacological Goals &
            Drugs Classification
    Preload (Venodilation)
   Nitrates, Potassium Channel Openers
    Afterload (Arteriolodilation)
    Calcium Channel Blockers, Potassium
    Channel Openers
    Heart Rate
    Beta Blockers, Calcium Channel Blockers
   Dilate Coronary Artery
   Dipyridamole
NITRATES
 Nitroglycerine, Isosorbide Dinitrate, Isosorbide Mononitrate



 Release Nitric Oxide in smooth muscles of Veins(mainly) & Arterioles



                 Stimulate Guanylyl Cyclase & cGMP


                       Stimulate Protein Kinase G



               Dephosphorylation & inactivation of MLCK



                 Relaxation of vascular smooth muscle
NITRATES
   Venodilation   Venous Return  Preload

   Venodilation  intraventricular pressure 
    less compression on vessels supplying
    subendocardial myocardium   Perfusion

   Arteriolodilation   TPR   Afterload

   Dilates collateral pathways & provides blood
    to ischemic area
NITRATES
BETA BLOCKERS

  Non-selective - Propanolol
  Cardioselective (硫1) - Atenolol, Metoprolol
 Have following actions :

 -ve Chronotropy (SA Node)
 -ve Dromotropy (AV Node)
 -ve Inotropy (Contractile myocardium)
 -ve Clinotropy (Velocity of contraction &
   relaxation)
BETA BLOCKERS
   Adverse Effects
   Fatigue (Blockade of 硫2 receptors in blood
    vessels supplying skeletal muscles)
   Bradycardia (Blockade of 硫1 receptors in
    heart)

   Precaution
   Abrupt withdrawal can heart rate,
    contractility & cause arrythmia & even MI.
    (Upregulation of receptors)
BETA BLOCKERS
   Contraindications

   Prinzmetal Angina
   COPD, Asthma,Bronchiectesias (硫2 in lungs)
   Diabetes Mellitus(硫2 in liver & pancreas)
   Raynauds Disease(硫2 in peripheral blood
    vessels)
   Bradyarrythmias (硫1 in heart)
   Depression
CALCIUM CHANNEL BLOCKERS

   Phenyl Alkylamines- Verapamil
    Benzothiazepines- Diltiazem
    Dihydropyridines- Nifedipine, Amlodipine,
    Felodipine

   Blocks voltage gated L-type Ca channels
    present in cardiac & vascular smooth
    muscles
CALCIUM CHANNEL BLOCKERS

   Depending upon their types, they can have
    following actions :
    -ve Chronotropy (SA Node)
    -ve Dromotropy (AV Node)
    -ve Inotropy (Contractile myocardium)
    -ve Clinotropy (Velocity of contraction &
    relaxation)
    Afterload (Arteriolodilatation)
CALCIUM CHANNEL BLOCKERS
                    HEART            ARTERIOLES
 Verapamil          ++++             +
 Diltiazem          ++               ++
 Dihydropyridines   -                ++++


Adverse Effects

Verapamil- similar to Beta Blockers
Dihydropyridines- similar to Nitrates
Diltiazem- common to above two
POTASSIUM CHANNEL
OPENERS

   Nicorandil, Pinacidil
   Opens Potassium channels in vascular
    smooth muscles & causes K efflux resulting
    into the hyperpolarization of the cell.
     Venodilation- Preload
     Arteriolodilation- Afterload
PHARMACOTHERAPY FOR
            ANGINA
   Stable Angina
    Acute attack- NTG 0.5mg S/L
    Prophylaxis-
    Nitrates- Isosorbide Mononitrate, Transdermal
    NTG
    硫 Blockers- Propanolol, Atenolol, Metoprolol
    CCB-Amlodipine, Verapamil SR & Diltiazem SR
PHARMACOTHERAPY FOR
          ANGINA
 Variant Angina
  Acute- NTG S/L or I/V
  Prophylaxis-
  Nitrates- Isosorbide Mononitrate
  CCB-Amlodipine, Diltiazem SR
  Potassium Channel Openers- Nicorandil,
  Pinacidil
硫 BLOCKERS ARE CONTRAINDICATED
PHARMACOTHERAPY FOR
            ANGINA
   Unstable Angina
    NTG S/L
    Antiplatelets agent- Aspirin, Clopidogrel
    硫 Blockers- Atenolol, Metoprolol
    CCB- Amlodipine or Nifedipine SR
    LMW Heparin
Anti  anginal drugs

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Anti anginal drugs

  • 1. ANTI- ANGINAL DRUGS Prashiddha Dhakal MBBS (KUSMS, 11th)
  • 2. What Is Angina? Central chest discomfort or pain due to transient ishemia of the myocardium Pain may radiate to one arm OR to both arms OR to neck OR to jaw OR to the epigastrium Duration- Less than 20min
  • 3. Types Of Angina Classical/Typical/Stable/Exertional Angina Due to fixed and stable plaque Prinzmetal/Variant Angina Due to spasm of coronary artery Unstable Angina Due to unstable plaque (賊 thrombus)
  • 4. Pharmacological Goals & Drugs Classification Preload (Venodilation) Nitrates, Potassium Channel Openers Afterload (Arteriolodilation) Calcium Channel Blockers, Potassium Channel Openers Heart Rate Beta Blockers, Calcium Channel Blockers Dilate Coronary Artery Dipyridamole
  • 5. NITRATES Nitroglycerine, Isosorbide Dinitrate, Isosorbide Mononitrate Release Nitric Oxide in smooth muscles of Veins(mainly) & Arterioles Stimulate Guanylyl Cyclase & cGMP Stimulate Protein Kinase G Dephosphorylation & inactivation of MLCK Relaxation of vascular smooth muscle
  • 6. NITRATES Venodilation Venous Return Preload Venodilation intraventricular pressure less compression on vessels supplying subendocardial myocardium Perfusion Arteriolodilation TPR Afterload Dilates collateral pathways & provides blood to ischemic area
  • 8. BETA BLOCKERS Non-selective - Propanolol Cardioselective (硫1) - Atenolol, Metoprolol Have following actions : -ve Chronotropy (SA Node) -ve Dromotropy (AV Node) -ve Inotropy (Contractile myocardium) -ve Clinotropy (Velocity of contraction & relaxation)
  • 9. BETA BLOCKERS Adverse Effects Fatigue (Blockade of 硫2 receptors in blood vessels supplying skeletal muscles) Bradycardia (Blockade of 硫1 receptors in heart) Precaution Abrupt withdrawal can heart rate, contractility & cause arrythmia & even MI. (Upregulation of receptors)
  • 10. BETA BLOCKERS Contraindications Prinzmetal Angina COPD, Asthma,Bronchiectesias (硫2 in lungs) Diabetes Mellitus(硫2 in liver & pancreas) Raynauds Disease(硫2 in peripheral blood vessels) Bradyarrythmias (硫1 in heart) Depression
  • 11. CALCIUM CHANNEL BLOCKERS Phenyl Alkylamines- Verapamil Benzothiazepines- Diltiazem Dihydropyridines- Nifedipine, Amlodipine, Felodipine Blocks voltage gated L-type Ca channels present in cardiac & vascular smooth muscles
  • 12. CALCIUM CHANNEL BLOCKERS Depending upon their types, they can have following actions : -ve Chronotropy (SA Node) -ve Dromotropy (AV Node) -ve Inotropy (Contractile myocardium) -ve Clinotropy (Velocity of contraction & relaxation) Afterload (Arteriolodilatation)
  • 13. CALCIUM CHANNEL BLOCKERS HEART ARTERIOLES Verapamil ++++ + Diltiazem ++ ++ Dihydropyridines - ++++ Adverse Effects Verapamil- similar to Beta Blockers Dihydropyridines- similar to Nitrates Diltiazem- common to above two
  • 14. POTASSIUM CHANNEL OPENERS Nicorandil, Pinacidil Opens Potassium channels in vascular smooth muscles & causes K efflux resulting into the hyperpolarization of the cell. Venodilation- Preload Arteriolodilation- Afterload
  • 15. PHARMACOTHERAPY FOR ANGINA Stable Angina Acute attack- NTG 0.5mg S/L Prophylaxis- Nitrates- Isosorbide Mononitrate, Transdermal NTG 硫 Blockers- Propanolol, Atenolol, Metoprolol CCB-Amlodipine, Verapamil SR & Diltiazem SR
  • 16. PHARMACOTHERAPY FOR ANGINA Variant Angina Acute- NTG S/L or I/V Prophylaxis- Nitrates- Isosorbide Mononitrate CCB-Amlodipine, Diltiazem SR Potassium Channel Openers- Nicorandil, Pinacidil 硫 BLOCKERS ARE CONTRAINDICATED
  • 17. PHARMACOTHERAPY FOR ANGINA Unstable Angina NTG S/L Antiplatelets agent- Aspirin, Clopidogrel 硫 Blockers- Atenolol, Metoprolol CCB- Amlodipine or Nifedipine SR LMW Heparin