anti anginal drugs · microsoft powerpoint - anti anginal drugs [compatibility mode] author:...
TRANSCRIPT
![Page 1: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/1.jpg)
ANTIANGINAL DRUGS
Dr. BINOY VARGHESE
CHERIYAN
Professor
Department of Pharmaceutical
Chemistry
![Page 2: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/2.jpg)
Angina pectoris
• Disease affecting the coronary arteries
which supply oxygenated blood from left
ventricle to heart tissues
• The lumen of artery become restricted
and it becomes less efficient in supplying
the blood and oxygen to heart called as
ischemia
![Page 3: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/3.jpg)
Definition of Angina
![Page 4: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/4.jpg)
GOALS OF TREATMENT• Therapy of angina is mainly directed to
minimize the Anginal attacks
• By restoring the balance between oxygen
supply/oxygen demand to cardiac muscles or
dilating coronary vessels
• Reversing and preventing myocardial ischemia
SUPPLY AND DEMAND.
• Improve the quality of life.
![Page 5: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/5.jpg)
TYPES OF ANGINA
• Stable or classical
• Unstable angina or acute coronary syndrome
• Prinzmetal or variant angina
![Page 6: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/6.jpg)
• What antianginal drugs do ?
• Decrease the demand of oxygen or
increase the supply of oxygen
• Dilates coronary arteries
• Decrease the after load
![Page 7: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/7.jpg)
CLASSIFICATION 1) NITRATES:
a) Short acting: Glyceryl trinitrate (GTN)
b) Long acting: Isosorbide dinitrate, Isosorbide mononitrate, Erythrityl tetranitrate, Pentaerythrityl tetranitrate
_______________________________________________
2) Β blockers: Metoprolol, Atenolol, Bisoprolol, Celiprolol
______________________________________________
3) Calcium Channel Blockers:
a) Verapamil, Diltiazem
b) Dihydropyridine ---Nifedipine, Amlodipine, Nitrendipine, Nimodipine
________________________________________________
4) Potassium Channel opener: Nicorandil, Pinacidil, Cromakalim, Minoxidil, Diazoxide
________________________________________________
5) Cytoprotective drugs: Trimetazidine, Ranolazine.
![Page 8: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/8.jpg)
Organic Nitrates
These are esters of simple organic alcohols or polyols with nitric acid
Glyceryl trinitrate (GTN)
Amyl nitrate
Isosorbide mononitrate,
Erythrityl tetranitrate,
Pentaerythrityl tetranitrate
![Page 9: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/9.jpg)
CLASSIFICATION 1) NITRATES:
a) Short acting: Glyceryl trinitrate (GTN)
b) Long acting: Isosorbide dinitrate, Isosorbide mononitrate, Erythrityl tetranitrate, Pentaerythrityl tetranitrate
_______________________________________________
2) Β blockers: Metoprolol, Atenolol, Bisoprolol, Celiprolol
______________________________________________
3) Calcium Channel Blockers:
a) Verapamil, Diltiazem
b) Nifedipine, Amlodipine, Nitrendipine, Nimodipine
________________________________________________
4) Potassium Channel opener: Nicorandil, Pinacidil, Cromakalim, Minoxidil, Diazoxide
________________________________________________
5) Cytoprotective drugs: Trimetazidine, Ranolazine.
![Page 10: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/10.jpg)
Nitrates/nitrites
1)NITRATES
Mechanism of action:
![Page 11: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/11.jpg)
Synthesis of nitrates
![Page 12: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/12.jpg)
Synthesis of nitrates
Erythrityl Tetranitrate Pentaerythritol tetranitrate
![Page 13: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/13.jpg)
Nitrates
uses
• Stable angina
• Unstable angina
• Cyanide poisining
Adverse effects
• Head ache
• Palpitation
• Tolerance
![Page 14: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/14.jpg)
Calcium channel blockers
• The contraction of the cardiac and
vascular smooth muscle is dependent on
extracellular calcium concentration
• Transport of calcium into cardiac and
vascular smooth muscle is regulated
voltage gated channel
![Page 15: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/15.jpg)
• Calcium channel blockers interacts L type
channels and reduces the calcium flux
through the channels
• This reduces the availability of intracellular
calcium and leads to
• Relaxation of arteriolar smooth muscle
• Depress myocardial contractility
![Page 16: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/16.jpg)
Calcium channel blockers
![Page 17: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/17.jpg)
Calcium channel blockers
![Page 18: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/18.jpg)
Calcium channel blockers
![Page 19: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/19.jpg)
Synthesis of Nifedipine
Hantczsh
![Page 20: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/20.jpg)
Synthesis of Verapamil
![Page 21: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/21.jpg)
Verapamil contd
![Page 22: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/22.jpg)
Calcium channel blockers
• Uses
• Hypertension
• Vasospastic angina
• Migraine
• Preterm labour
•
• Adverse effects
• Constipation
• Bradycardia
• Heart block
• Gum hyperplasia
![Page 23: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/23.jpg)
Beta Blockers
• Drugs that block the action of
cathecholamines through beta receptors
• Non selective - Propranalol, nadolol
• Cardioselective – Metoprolol, atenolol
esmolol
• With additional alpha blocking - labetalol
![Page 24: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/24.jpg)
BETA BLOCKERS
![Page 25: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/25.jpg)
METAPROLOL
![Page 26: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/26.jpg)
Potassium channel opener
• Nicorandil
• These drug opens the ATP – sensitive K
channels
• Opening of this leads to hyper polarisation
• Followed by closing of calcium channels
• Less intracellular calcium -- muscle
relaxation
![Page 27: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/27.jpg)
Nicorandil
![Page 28: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/28.jpg)
Trimetazidine
• Calcium Channel Blocker
• Protective effect on ischemic myocardium &
left ventricular function
• used in Exertional angina
![Page 29: anti anginal drugs · Microsoft PowerPoint - anti anginal drugs [Compatibility Mode] Author: venkatesan Created Date: 1/27/2020 11:15:06 AM](https://reader034.vdocument.in/reader034/viewer/2022042709/5f3de8de62847b2a0c1b25eb/html5/thumbnails/29.jpg)
Thank you