this presentation about introduction, mechanism of action, drugs available and their structures, mechanisms and use will be provide

1. ANTI-ANGINA DRUGS
PRESENTED BY:
Arun Agarwal
BPHARM (2011-2015)
Inveris institute of pharmcay,
Invetis university,
Bareilly

2. CONTENTS
• Introduction of angina
• Types of angina
• Causes of angina
• Introduction of anti-angina drugs
• Classification of anti-angina drugs
• Mechanism of action all classes of drugs
• Introduction of Isosorbide mononitrate
• Synthesis
• Mechanism of action
• Structure activity relationship
• Side effects
• uses

3. Angina

4. Introduction of angina
• Angina is chest pain or discomfort that occurs if an area of your
heart muscle doesn't get enough oxygen-rich blood.
• Angina may feel like pressure or squeezing in your chest. The pain
also can occur in your shoulders, arms, neck, jaw, or back. Angina
pain may even feel like indigestion.
• Angina isn't a disease; it's a symptom of an underlying heart
problem. Angina usually is a symptom of coronary heart
disease (CHD).
• CHD is the most common type of heart disease in adults. It occurs if
a waxy substance called plaque builds up on the inner walls of your
coronary arteries. These arteries carry oxygen-rich blood to your
heart.

5. Plaque Buildup in an Artery
• Figure A normal artery with normal blood flow. The inset
image shows a cross-section of a normal artery. Figure B
shows an artery with plaque buildup. The inset image shows a
cross-section of an artery with plaque buildup.

6. Types of Angina
• There are four types of angina
• Stable angina
• Unstable angina
• Variant angina (Prinzmetal's)
• Micro vascular angina

7. Stable angina
• Stable angina is the most common type
of angina. It occurs when the heart is
working harder than usual. Stable angina
has a regular pattern. (“Pattern” refers to
how often the angina occurs, how severe
it is, and what factors trigger it.)
• Stable angina isn't a heart attack, but it
suggests that a heart attack is more likely
to happen in the future.

8. Unstable angina
• Unstable angina doesn't follow a
pattern. It may occur more often and
be more severe than stable angina.
• Unstable angina also can occur with
or without physical exertion, and rest
or medicine may not relieve the pain.
• Unstable angina is very dangerous
and requires emergency treatment.
This type of angina is a sign that a
heart attack may happen soon.

9. Variant(Prinzmetal's) angina
• Variant angina is rare. A spasm in a
coronary artery causes this type of
angina. Variant angina usually occurs
while you're at rest, and the pain can
be severe.
• It usually happens between midnight
and early morning. Medicine can
relieve this type of angina.

10. Micro vascular angina
• Angina also can be a symptom of coronary
microvascular disease (MVD). This is heart
disease that affects the heart’s smallest
coronary arteries. In coronary MVD, plaque
doesn't create blockages in the arteries like it
does in CHD.
• Studies have shown that coronary MVD is
more likely to affect women than men.
Coronary MVD also is called cardiac
syndrome X and nonobstructive CHD.
• Microvascular angina can be more severe
and last longer than other types of angina.
Medicine may not relieve this type of angina.

11. Causes of angina
conditions also can cause chest pain, such as:
• Pulmonary embolism (a blockage in a lung
artery)
• A lung infection
• Aortic dissection (tearing of a major artery)
• Aortic stenosis (narrowing of the heart’s
aortic valve)
• Hypertrophic cardiomyopathy (heart
muscle disease)
• Pericarditis (inflammation in the tissues
that surround the heart)
• A panic attack

12. ANTI-ANGINA DRUGS

13. Anti-angina Drugs
• The term angina derived from
Greek verb meaning to choke
and is used to describe the
pain or discomfort.
• An anti-anginal is
any drug used in the
treatment of angina pectoris,
a symptom of ischaemic heart
disease.

14. Classification Of Anti-Angina Drugs

15. classification
1) Nitrates and nitrites
• a) Nitrates:
e.g. Nitroglycerin, Erythritol tetranitrate, Trolnitrate phosphate,
Isosorbide dinitrate, Pentaerythritol tetranitrate, Mannitol
hexanitrate.
• b) Nitrites:
e.g. Amyl nitrite , Sodium nitrite . Nitroprusside sodium

16. 2) Calcium Channel Blockers
a) Aryl alkyl amine derivative:
e.g. Verapamil
b) Benzothiazepine:
e.g. Diltiazem
c) Dihydropyridine derivative:
e.g. Nifedipine , Nimodipine , Nitrendipine ,
Nicardipine, Amlodipine , Felodipine , Isradipine
d) Newer second generation alkyl amine
derivative:
e.g. Bepridil

17. 3) β-Adrenergic Antagonist:
e.g. Propranolol (antihypertensives)
4) Miscellaneous Coronary Vasodilators:
e.g. Dipyridamol 1, Cyclandelate , Papaverine

18. 1(a) nitrates
Nitroglycerine
Erythritol tetranitrate
Trolnitrate Phosphate Isosorbide dinitrate
Pentaerythritol
tetranitrate
Mannitol
hexanitrate

19. 1(b) Nitrites
Amyl nitrite
Sodium Nitrite
Nitroprusside sodium

20. 2(a) Aryl alkyl amine derivative
Verapamil

21. 2(b)Benzothiazepine
Diltiazem

22. 3(c) Dihydropyridine derivative
Nifedipine Nimodipine Nitrendipine Nicardipine
Amlodipine Felodipine Isradipine

23. 2(d) Newer second generation alkyl
amine derivative
Bepridil

24. 3) β-Adrenergic Antagonist
Propranolol

25. 4) Miscellaneous Coronary Vasodilators
Dypyridamole
Cyclandelate
Papaverine

26. Mechanism Of All Classes Of Drugs

27. Machenism of action of Organic
Nitrates and Nitrites
Administrated nitrates
 Nitrites
 Nitric oxide (NO)
 cGMP
 Dephosphorylation of myosin light chain
Vascular smooth muscle relaxation

28. Mechanism of action of calcium
channel blockers
Inhibit the influx of Calcium into CARDIAC & VASCULAR cells
MUSCLE TONE

29. Mechanism of action of β-Adrenergic
Antagonist
 Adrenergic
blocker
Inotropic
chronotropic
domotropic
Renin  Ag  peripheral BP 
resistance
aldosteron
 Sodium, water
retention
BP 
 O2 demand

30. Introduction of Isosorbide mononitrate

31. ISOSORBIDE MONONITRATE
8-nitroxy2,6-dioxabicyclo[3,3,0]octan-4-ol

32. Synthesis of Isosorbide Mononitrate

33. Mechanism of action
• Nitric oxide formed in smooth muscle from nitro
vasodilators or from endothelial cells.
• It activates guanylate cyclase (GC*).
• Guanylate cyclase (GC*) activates cGMP dependent
protein kinesis that phosphorylate myosin light-
chain kinesis.
• Causing its inactivation and subsequent muscle
relaxation.

34. Structure Activity Relationship
• The basic moiety isosorbide a important for
activity.
• Varying the chemical structure of the organic
nitrates yields differences in speed of onset,
duration of action, and potency.
• The number of nitrate esters groups may vary
from one to six or more.

35. Cont…
• It appears that the higher the oil/water partition
coefficient of the drug, the greater the potency.
• The orientation of the groups within the
molecule of also may affect potency.
• Lipophillicity of the nitrogen-oxide containing
compound produces a much longer response of
vasodilatory action.

36. Side Effects
• Fullness in head
• Throbbing headache
• Flushing
• Weakness
• Sweating
• Palpitation
• Dizziness
• fainting

37. Uses
• Treatment or prophylaxis of acute angina attack
• CHF
• Myocardiac infarction
• Percutaneous coronary angioplasty, thrombolytic
therapy of acute myocardiac infarction.
• Cyanide poisoning

38. Thank you !!