INTRODUCTION

DECREASE INCREASE
OXYGEN OXYGEN
DELIVERY
ISCHEMIA HEART
REQUIREMENT

ANGINAL PAIN
 Type of Angina Pectoris
• Classic angina/Atherosclerotic angina/Angina Of
Effort (associated with atheromatous plaque)

• Variant angina/Vasospastic angina/Rest angina or

Prinzmetal’s angina (reversible coronary spasm)

• Unstable angina/Acute Coronary Syndrome (it is a

combination between atherosclerotic plaque,
platelet aggregation and vasospasm)
 THERAPEUTIC STRATEGIES

INCREASE OXYGEN DECREASE OXYGEN

DELIVERY REQUIREMENT

VASODILATOR CARDIAC DEPRESSANT

NITRATE Ca BLOCKER β BLOCKER

LONG ACTING ( trandermal nitroglycerin)

INTERMEDIATE ACTING
(oral nitroglyserin or sustained release)

SHORT ACTING
(sublingual nitroglyserin or ISDN )

VERY SHORT ACTING

( inhale amyl nitrite )
 Drugs that increase oxygen delivery

• Nitrates (Nitroglycerin, Isosorbid dinitrate)

< very short acting (inhale Amyl Nitrate)
< short acting (sublingual Nitroglycerin or ISDN)
< intermediate acting (oral Nitroglycerin or ISDN)
< long acting (transdermal Nitroglycerin)

• Ca antagonist (Nifedipine, Felodipine)

 NITRATE

NITRIC OXIDE
(NO)

GUANYLYL CYCLASE

GTP cGMP GMP

PDE5

SMOOTH MUSCLE
RELAXATION

VASODILATATION
 NITROGLYSERIN
( GLYSERIL TRINITRATE)
DENITRATED IN THE LIVER

GLYSERIL DINITRATE
(ACTIVE METABOLITE)
DENITRATED IN THE LIVER

GLYSERIL MONONITRATE
(LESS ACTIVE METABOLITE)
 Clinical use of Nitrate
• Nitroglycerin and ISDN are drug of first
choice or standard therapy for Acute Anginal
Pain
• Transdermal formulation (ointment or patch)
maintain blood level for up to 24 hours
• Tolerance can develop after 8-10 hours
 Side effect of Nitrate
• Orthostatic hypotension (venodilatation)
• Tachycardia (baroseptor reflex)
• Throbing headache (dilatation of meningeal
artery)
• Tolerance
• Interact with Sildenafil (dangerous
hypotension)
 NITRATE

NITRIC OXIDE
(NO)

GUANYLYL CYCLASE

GTP cGMP GMP

PDE5

SMOOTH MUSCLE
RELAXATION

ERECTILE BLOOD VESSEL

TISSUE
 Drug that depress cardiac work
(decrease oxygen requirement)
• Ca antagonist (Verapamil, Diltiazem)

• β blocker (Propranolol, Bisoprolol, Nadolol)

 Ca blocker (Ca antagonist)

Dihydropyridine Non Dihydropyridine

(Nifedipine, Felodipine) (Diltiazem, Verapamil)

• Greater vasodilatation <Cardiac depressant

• Symphatetic reflex <Reduce heart rate
• Increase heart rate <Reduce contractility
 Clinical use of Ca antagonist
• Effective as prophylactic for:
< angina of effort
< vasospastic angina
• Nifedipine has also been used to abort
Acute Anginal Attack
• In atherosclerotic angina it’s better
combine with nitrate
 Side effect of Ca antagonist
• Constipation
• Pretibial edema
• Nausea
• Dizziness
• Serious cardiac depression (cardiac arrest,
bradycardia, heart failure)
• AV block
 β blocker
• Decrease heart rate
• Decrease cardiac contractility
• Decrease blood pressure
 Clinical use of β blocker
• Effective as prophylactic for atheroslerotic angina
• Combination with nitrate has a useful effect
 Conclusion
• The basic cause of Angina pectoris is Ischemia of
the Heart (decrease oxygen delivery or increase
oxygen requirement)
• Therapeutic strategies: increase oxygen delivery
(nitrate, Ca blocker) or decrease oxygen
requirement (Ca blocker, β blocker)
• Nitrate is the drug of first choice of Acute Anginal
attack
• For prophylactic/maintenance therapy :
transdermal nitrate, Ca blocker and β blocker