too much introduction about angina and the medicinal chemistry view of antianginal drugs

1. Submitted by:
Ahmad al-jifri

2. Definition
symptoms
Causes
Types
Risk factors & Complications
Diagnosis & Treatment strategy
Mechanism of the drug
Structure ( SAR )
Uses
Adverse effect

8. Type of Angina
Pectoris
typical Stable
Angina
↓ coronary flow
,Occurs on physical
Exertion
(five minutes or less)
Unstable angina
Epicardial coronary
spasm & formation of
non-occlusive thrombi
Can Occurs at rest Heart
attack
(emergency)
Variant ,
vasospastic or
prinzmetal angina
..
Reversible coronary
spasm .. Occurs
at rest
2%

17. Classification of drugs
Organic
nitrates
(2)Nitroglyc
erin,
Glyceryl
Trinitrate:
Calcium
channel
blockers
Dihydropyri
dines:
Nifedipine
Benzothiaze
pines
Diltiazem
Phenylalkyla
mines:
1-Verapamil
Beta-
blockers
(a)Non-
selective
Beta Blocker
Propranolol
(Inderal)
(b)Beta1-
Selective
Blockers
Atenolol

20. Organic nitrates interact with tissue thiols and
release Nitric Oxide which stimulates the guanyl
cycles which increase the intracellular concentration
of cGMP which cause vasodilatation in large veins,
resulting in pooling of the blood in the vines and
decreased venous return to the heart (which means
decreased preload) also they dilate the arteries
resulting in decrease in the resistance of the
peripheral tissues (which means decreased after
load) that’s results in general decrease in cardiac
work.

21.  It has been used to treat angina and heart failure since at least 1870 .
 it can be prepared
 as rapid acting preparation as sublingual tablets or spray of glyceryl
trinitrate for treatment of acute attacks
 or can be as long acting preparation (sustained released) as transdermal
patches and buccal tablets and ointments of glyceryl trinitate
 If the first dose does not work, a second dose can be taken after five
minutes, and a third dose after a further five minutes. If no effect
seems to appear after the third dose, the patient must be hospitalized
.
 for prevention therapy one dose of glyceryl trinitrate usually eases the
pain within 2-3 minutes.
:

24. :
Influx of Ca ions through these channels leads to membrane
depolarization and initiates or strengthens muscle contraction.
CCBs block the inward movement of Ca2+ by binding to the L-
type Ca channels. This causes muscle relaxation and suppresses
cardiac or blood vessels activity.
In normal tissue an ion channel will most likely be in this state. The channel
blocker cannot reach its receptor site.
Ca2+ can pass; also the blocker now has access to its binding site.
This is refractory to further depolarization. Ca2+ cannot pass through the
channel, nor will the drug. Depending on the lipid solubility of the drug, it
can still have access to its binding site through the phospholipids bilayer.

27. :
--

36. References:
University of Alexandria, Faculty of pharmacy,
Pharmaceutical chemistry department.

37. Thank you