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Antianginal Drugs Claro M. Isidro M.D.
Definition of terms ,[object Object],[object Object],[object Object]
Types of Angina ,[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
ANTIANGINAL DRUGS ,[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Nitrates ,[object Object],[object Object],[object Object],[object Object],[object Object]
Nitrates ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Nitrates ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Effects ,[object Object],[object Object],[object Object]
[object Object],Beneficial effects Results Decrease Ventricular vol. Decrease myocardial oxygen requirement Decrease arterial pressure Decrease ejection time Venodilatation of epicardial coronary art. Relief of coranary artery spasm Increase collateral flow due to venodilatation Increase perfusion to ischemic myocardium Decrease left ventricular pressure   > decrease preload due to dilatation of the vein > decrease after load due to dilatation of the arteries Improved subendocardial perfusion
Potential Deleterious Effects Deleterious Effects   Results Reflex tachycardia Increase myocardial oxygen requirement   Reflex increase in contractility   Decrease diastolic perfusion   Decrease myocardial perfusion
ROUTES OF ADMINISTRATION 1. Sublingual route  – rational and effective for the treatment of acute attacks of angina pectoris. Half-life depend only on the rate at which they are delivered to the liver. 2. Oral route  – to provide convenient and prolonged prophylaxis against attacks of angina 3. Intravenous Route  – useful in the treatment of coronary vasospasm and acute ischemic syndrome. 4. Topical route  – used to provide gradual absorption of the drug for prolonged prophylactic purpose .
Drug Usual single dose Route of administration Duration of action Short acting Nitroglycerin 0.15-1.2 mg sublingual 10 - 30 min Isosorbide dinitrate 2.5-5 mg sublingual 10 – 60 min Amyl nitrite 0.18 – 3 ml  inhalation 3 – 5 min Long acting Nitroglycerin sustained action 6.5 – 13 mg q 6-8 hrs oral 6 – 8 hrs Nitroglycerin 2% ointment 1 – 1.5 inches q hr topical 3 – 6 hrs Niroglycerin slow released 1 –2 mg per 4 hrs Buccal mucosa 3 – 6 hrs Nitroglycerin slow released   10 – 25 mg /24hrs (one patch/day}   transdermal   8 –10 hrs   Isosorbide dinitrate   2.5 – 10 mg per 2 hrs sublingual   1.5 – 2 hrs   Isosorbide dinitrate 10 –60 mg per 4-6 hrs   oral   4 – 6 hrs   Isosorbide dinitrate chewable   5 – 10 mg per 2-4 hrs oral   2 – 3 hrs   Isosorbide mononitrate   20 mg per 12 hrs   oral   6 –10 hrs
Adverse Effects ,[object Object],[object Object],[object Object],[object Object]
Contraindication ,[object Object],[object Object],[object Object]
B-Blockers ,[object Object],[object Object],[object Object]
B-Blockers ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Contraindication ,[object Object],[object Object],[object Object]
Ca - Channel Blockers ,[object Object],[object Object],[object Object]
Ca Channel Blockers ,[object Object],[object Object],[object Object],[object Object],[object Object]
Ca channel Blockers ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],Drugs Onset of action Peak of action Half-life Nifedipine 20 minutes   1 hour   3-4 hours   Verafamil   1-2 hours   5 hours   8-10 hours Diltiazem   15 minutes   30 minutes   3-4 hours   Nicardifine   20 minutes   45 minutes   2-4 hours   Felodipine   2-5 hours   6-7 hours   11-16 hour
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
Type of Angina Other Names Description Drug Therapy STABLE Classic Exertional Fixed Atherosclerotic Obstruction coronary artery Nitrates CCB B-blockers VARIANT Prinzmetal’s Vasospasmic Vasospasm at any time Nitrates CCB UNSTABLE Crescendo Combined effect Pre= MI Nitrates  CCB

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Antianginal Drugs

  • 1. Antianginal Drugs Claro M. Isidro M.D.
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  • 17. Potential Deleterious Effects Deleterious Effects Results Reflex tachycardia Increase myocardial oxygen requirement Reflex increase in contractility Decrease diastolic perfusion Decrease myocardial perfusion
  • 18. ROUTES OF ADMINISTRATION 1. Sublingual route – rational and effective for the treatment of acute attacks of angina pectoris. Half-life depend only on the rate at which they are delivered to the liver. 2. Oral route – to provide convenient and prolonged prophylaxis against attacks of angina 3. Intravenous Route – useful in the treatment of coronary vasospasm and acute ischemic syndrome. 4. Topical route – used to provide gradual absorption of the drug for prolonged prophylactic purpose .
  • 19. Drug Usual single dose Route of administration Duration of action Short acting Nitroglycerin 0.15-1.2 mg sublingual 10 - 30 min Isosorbide dinitrate 2.5-5 mg sublingual 10 – 60 min Amyl nitrite 0.18 – 3 ml inhalation 3 – 5 min Long acting Nitroglycerin sustained action 6.5 – 13 mg q 6-8 hrs oral 6 – 8 hrs Nitroglycerin 2% ointment 1 – 1.5 inches q hr topical 3 – 6 hrs Niroglycerin slow released 1 –2 mg per 4 hrs Buccal mucosa 3 – 6 hrs Nitroglycerin slow released 10 – 25 mg /24hrs (one patch/day} transdermal 8 –10 hrs Isosorbide dinitrate 2.5 – 10 mg per 2 hrs sublingual 1.5 – 2 hrs Isosorbide dinitrate 10 –60 mg per 4-6 hrs oral 4 – 6 hrs Isosorbide dinitrate chewable 5 – 10 mg per 2-4 hrs oral 2 – 3 hrs Isosorbide mononitrate 20 mg per 12 hrs oral 6 –10 hrs
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  • 34. Type of Angina Other Names Description Drug Therapy STABLE Classic Exertional Fixed Atherosclerotic Obstruction coronary artery Nitrates CCB B-blockers VARIANT Prinzmetal’s Vasospasmic Vasospasm at any time Nitrates CCB UNSTABLE Crescendo Combined effect Pre= MI Nitrates CCB