Vasodilators and The Treatment of Angina Pectoris

Vasodilators and the By:
Agila
Agaloos
Reyes
Sacliwan
Treatment of Aluan
Andres
Azarcon
Salvador
Santos
Soriano
Angina Pectoris Bassig

Butacan
Cardona
Tamayo
Torio
Udan
Corpuz Vite
Raju
Case Study
A 74-year-old man presents with a history of anterior chest
pressure whenever he walks more than one block. The
chest discomfort is diffuse, and he cannot localize it;
sometimes it radiates to his lower jaw. The discomfort is
more severe when he walks after meals but is relieved
within 5–10 minutes when he stops walking.
Assuming that a diagnosis of stable effort angina
is correct, what medical treatments should be implemented
to reduce the acute pain of an
attack and to prevent future attacks?
Angina Pectoris
• Denotes chest pain caused by accumulation of metabolites resulting
from myocardial ischemia.
• Primary cause: an imbalance between the oxygen requirement of the
heart and the oxygen supplied to it via the coronary vessels
• Insufficient blood supply and oxygen of the heart  ANGINA
3 Types of Angina
Atherosclerotic Plaque Spasm
Stable/Classic/Effort Angina  Vasospastic or Variant
• Inadequate blood flow in the presence of
Coronary Artery disease
angina/Prinzmetal angina
• Triggered by exercise, stress, and excitement • Transient spasm of coronary
• Promptly relieved by rest or nitroglycerin vessels
 Unstable angina • Responds promptly to coronary
• small platelet clots occurring in the vicinity vasodilators (Nitroglycerin,
of an atherosclerotic plaque. Calcium channel blockers)
• Chest pain occurs at rest; it occurs with
increased SEVERITY, FREQUENCY, AND
DURATION
• Acute coronary syndrome: may lead to M.I.
***Insert video clip showing 3 types of angina
Treatment
• Help balance the cardiac oxygen supply and demand  affecting
heart rate, contractility, arterial blood pressure or ventricular volume
Calcium Channel
Beta blockers
Blockers
Sodium channel
Organic Nitrates blocking drug
(Ranolazine)
Organic Nitrates
Mechanism of action
• >nitrates decrease coronary
vasoconstriction and increase perfusion
of myocardium by RELAXING coronary
arteries.
• >they also relax veins, decreasing preload

and myocardial oxygen consumption.
Mechanisms of Clinical uses of nitrates
• Nitrate Effects in Angina of Effort

• ↓ venous return to heart & the resulting ↓ of intracardiac volume are important beneficial
effects of nitrates → ↓ arterial pressure
• Reduction in oxygen demand is the major mechanism for the relief of effort angina
• Nitrate Effects in Variant Angina
• Nitrates benefits patients with variant angina by relaxing the smooth muscle of the
epicardial coronary arteries → relieving coronary artery spasm
• Nitrate Effects in Unstable Angina
• The precise mechanism for the beneficial of nitrates in unstable angina is not clear
Beneficial and deleterious effects of nitrates in treatment of angina
Adverse Effects Throbbing headache (most common)
Orthostatic hypotension,tachycardia
CI Increased intracranial pressure

External defibrillators
CONS Development of tolerance

Except: Nitroprusside retains activity over long periods of
time
Calcium channel blockers
Toxic effects
Extension of therapeutic action
Weakened cardiac contraction and automaticity

—> bradycardia, atrioventricular block, cardiac arrest, and heart failure
Other nitro-vasodilator
NICORANDIL
• nitrate derivative of nicotinamide
• can be used for the prevention and long-term treatment of angina in
combination with either a beta-blocker or CCB
MOA: dilates epicardial coronary arteries and stimulates adenosine
triphosphate-sensitive potassium channels in vascular smooth muscle
CI: Cardiogenic shock, CHF/Low blood pressure
SE: Headache, dizziness, flushing of skin, nausea, vomiting, weakness,
palpitation
BETA-ADRENERGIC BLOCKING
DRUGS
• beta-blockers antagonize or reverse the effects of sympathetic
activation caused by exercise and other physical or mental exertions
• decrease heart rate and force of contractions
• Beta-blockers are indicated for the long-term (chronic) management
of angina pectoris
• Includes:
• propranolol is usually the preferred beta-blockers for the treatment of angina
and CAD
• Atenolol, metoprolol, others: b1-Selective blockers, less risk of bronchospasm,
but still significant
Newer antianginal drugs
• Ranolazine act by reducing a late sodium current (INa) that facilitates calcium entry via the sodium-calcium
exchanger approved for use in angina in the US

• Certain metabolic modulators (eg, trimetazidine) known as pFOX inhibitors because they partially inhibit the fatty
acid oxidation pathway in myocardium. not approved for use in the USA.

• Perhexiline this drug may shift myocardial metabolism from fatty acid oxidation to more efficient glucose
oxidation (compared with trimetazidine).
• So-called bradycardic drugs, relatively selective If sodium channel blockers (eg, ivabradine) reduce cardiac rate
by inhibiting the hyperpolarization-activated sodium channel in the sinoatrial node.
• Fasudil, inhibitor of smooth muscle Rho kinase and reduces coronary vasospasm in experimental animals
investigational in angina.
• Allopurinol, inhibits xanthine oxidase, an enzyme that contributes to oxidative stress and endothelial dysfunction in
addition to reducing uric acid synthesis, its mechanism of action in gout. not currently approved for use in angina.
Clinical pharmacology of drugs used to treat
angina
• First-line therapy of CAD depends on modification risk factors:
Smoking, HPN, hyperlipedemia, obesity, and clinical depression.
Addition of anti platelet drugs are very important.
• Specific pharmacologic therapy to prevent MI and death:

Antiplatelet agents (Aspirin, ADP receptor blockers), lipid lowering agents esp. statins,
and ACE Inhibitors
• Aggressive therapy in pts with Unstable angina and non-ST-segment

elevation MI
Coronary stenting, Antilipid drugs, Heparin, and Anti platelet agent is recommended.
Angina of Effort
• For maintenance therapy of chronic stable angina:
Long acting nitrates, CCB agents, or B blockers may be chosen; DOC depends on individual
patient’s response
• For hypertensive pt’s, monotherapy:
Eeither slow release or long-acting CCB or B blockers may be adequate
• For normotensive pts:
Long acting nitrates may be suitable
Combination of a B blocker with CCB (propanolol with nifedipine)

Or 2 CCB (nifedipine and verapamil) has shown to be more effective than individual drugs used alone
• Primary methods for promptly restoring coronary blood floow:

Surgical revascularization (CABG) and catheter-based revascularization (PCI)
Vasospastic Angina
• Nitrates and CCB are effective drugs for relieving and preventing
ischemic episodes.
• 70% angina attacks are abolished
• 20% marked reduction of frequency of anginal episodes
• Surgical revascularization and angioplasty not indicated.
Unstable Angina and ACS
• Aggressive antiplatelet therapy with aspirin and clopidogrel is
indicated.
• IV heparin or SQ low-molecular-weight heparin is also indicated
in most pts.
• If percutaneous coronary intervention with stenting is required:
Glycoprotein Iib/IIIa inhibitors (abciximab) should be added
Nitroglycerin and B blocker should be considered
CCB should be added in refractory cases
Primary lipid lowering and ACE-I therapy should be initiated
Treatment of peripheral artery disease (PAD)
& Intermittent claudication
• Claudication/Pain occurs in skeletal muscles esp legs, during exercise and
disappears with rest.
• It results from obstruction of blood flow by atheromas in large and medium
arteries.
Tx:
• Control of hyperlipidemia, HPN, Obesity, cessation of smoking, and control of DM if present.
• Physical therapy and exercise training is of proven benefit.
• Conventional vasodilators areof no benefit
• Antiplatelet (aspirin and clopidogrel) are often used to prevent clotting
• Pentoxyfylline, xantine derivative, reducing viscosity of blood
• Cilostazol, phosphodiesterase type 3 PDE3 inhibitor, poorly understood, but may have
selective antiplatelet and vasodilating effects
Percutaneous Angioplasty with stenting often effective in pts with medically intractable s/sx of
schemia
Thank you!
• References: Katzung – Basic and Clinical Pharmacology

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Vasodilators and the By:

Angina Pectoris Bassig

• >they also relax veins, decreasing preload

• Nitrate Effects in Angina of Effort

CI Increased intracranial pressure

CONS Development of tolerance

Weakened cardiac contraction and automaticity

• Specific pharmacologic therapy to prevent MI and death:

• Aggressive therapy in pts with Unstable angina and non-ST-segment

Combination of a B blocker with CCB (propanolol with nifedipine)

• Primary methods for promptly restoring coronary blood floow:

• References: Katzung – Basic and Clinical Pharmacology

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