ANTI- ANGINAL DRUGS

Prashiddha
Dhakal
MBBS (KUSMS, 11th)
What Is Angina?

 Central chest discomfort or pain due to

transient ishemia of the myocardium

 Pain may radiate to one arm OR to both arms

OR to neck OR to jaw OR to the epigastrium

 Duration- Less than 20min

Types Of Angina

 Classical/Typical/Stable/Exertional Angina
• Due to fixed and stable plaque

 Prinzmetal/Variant Angina
• Due to spasm of coronary artery

 Unstable Angina
• Due to unstable plaque (± thrombus)
 Pharmacological Goals &
Drugs Classification
 ↓ Preload (Venodilation)
• Nitrates, Potassium Channel Openers
 ↓ Afterload (Arteriolodilation)
• Calcium Channel Blockers, Potassium
Channel Openers
 ↓ Heart Rate
• Beta Blockers, Calcium Channel Blockers
 Dilate Coronary Artery
• Dipyridamole
NITRATES
Nitroglycerine, Isosorbide Dinitrate, Isosorbide Mononitrate

Release Nitric Oxide in smooth muscles of Veins(mainly) & Arterioles

Stimulate Guanylyl Cyclase & ↑cGMP

Stimulate Protein Kinase G

Dephosphorylation & inactivation of MLCK

Relaxation of vascular smooth muscle

NITRATES
 Venodilation → ↓ Venous Return → ↓Preload

 Venodilation → ↓intraventricular pressure →

less compression on vessels supplying
subendocardial myocardium → ↑ Perfusion

 Arteriolodilation → ↓ TPR → ↓ Afterload

 Dilates collateral pathways & provides blood

to ischemic area
NITRATES
BETA BLOCKERS

 Non-selective - Propanolol
Cardioselective (β1) - Atenolol, Metoprolol
 Have following actions :

-ve Chronotropy (SA Node)

-ve Dromotropy (AV Node)
-ve Inotropy (Contractile myocardium)
-ve Clinotropy (Velocity of contraction &
relaxation)
BETA BLOCKERS
 Adverse Effects
 Fatigue (Blockade of β2 receptors in blood
vessels supplying skeletal muscles)
 Bradycardia (Blockade of β1 receptors in
heart)

 Precaution
 Abrupt withdrawal can ↑heart rate,
↑contractility & cause arrythmia & even MI.
(Upregulation of receptors)
BETA BLOCKERS
 Contraindications

 Prinzmetal Angina
 COPD, Asthma,Bronchiectesias (β2 in lungs)
 Diabetes Mellitus(β2 in liver & pancreas)
 Raynaud’s Disease(β2 in peripheral blood
vessels)
 Bradyarrythmias (β1 in heart)
 Depression
CALCIUM CHANNEL BLOCKERS

 Phenyl Alkylamines- Verapamil

Benzothiazepines- Diltiazem
Dihydropyridines- Nifedipine, Amlodipine,
Felodipine

 Blocks voltage gated L-type Ca channels

present in cardiac & vascular smooth
muscles
CALCIUM CHANNEL BLOCKERS

 Depending upon their types, they can have

following actions :
-ve Chronotropy (SA Node)
-ve Dromotropy (AV Node)
-ve Inotropy (Contractile myocardium)
-ve Clinotropy (Velocity of contraction &
relaxation)
↓Afterload (Arteriolodilatation)
 CALCIUM CHANNEL BLOCKERS
HEART ARTERIOLES
Verapamil ++++ +
Diltiazem ++ ++
Dihydropyridines - ++++

Adverse Effects

•Verapamil- similar to Beta Blockers

•Dihydropyridines- similar to Nitrates
•Diltiazem- common to above two
POTASSIUM CHANNEL
OPENERS

 Nicorandil, Pinacidil
 Opens Potassium channels in vascular
smooth muscles & causes K efflux resulting
into the hyperpolarization of the cell.
Venodilation- ↓Preload
Arteriolodilation- ↓Afterload
 PHARMACOTHERAPY FOR
ANGINA
 Stable Angina
Acute attack- NTG 0.5mg S/L
Prophylaxis-
Nitrates- Isosorbide Mononitrate, Transdermal
NTG
β Blockers- Propanolol, Atenolol, Metoprolol
CCB-Amlodipine, Verapamil SR & Diltiazem SR
 PHARMACOTHERAPY FOR
ANGINA
 Variant Angina
Acute- NTG S/L or I/V
Prophylaxis-
Nitrates- Isosorbide Mononitrate
CCB-Amlodipine, Diltiazem SR
Potassium Channel Openers- Nicorandil,
Pinacidil
β BLOCKERS ARE CONTRAINDICATED
 PHARMACOTHERAPY FOR
ANGINA
 Unstable Angina
NTG S/L
Antiplatelets agent- Aspirin, Clopidogrel
β Blockers- Atenolol, Metoprolol
CCB- Amlodipine or Nifedipine SR
LMW Heparin