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CVS & IBL - Pharmacology 💊 > L2: Antianginal drugs > Flashcards

L2: Antianginal drugs Flashcards

1
Q

What are ischemic heart diseases?

A
  • Chronic stable angina (Classic exertional angina) “effort”
  • Acute coronary syndromes (ACS): “rest and effort”
    A. Unstable angina
    B. Myocardial infarction “result from unstable angina”
  • Prinzmetal’s angina “rest and effort”
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2
Q

What causes chronic stable angina (Classic exertional angina)?

A
  • It is due to atheromatous narrowing of the coronary artery.
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3
Q

What are the symptoms of chronic stable angina?

A
  • Pain is induced by effort and disappears with rest.
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4
Q

What causes unstable angina? And what causes myocardial infarction?

A
  • It is due to rupture of atheromatous plaque and formation of thrombus.
  • An intraluminal thrombus completely occludes the epicardial coronary artery at the site of plaque rupture leading to irreversible coagulative necrosis.
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5
Q

What are the symptoms of unstable angina?

A
  • The patient experiences acceleration in the frequency or severity of chest pain, or new-onset angina pain.
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6
Q

What are other names for Prinzmetal’s angina?

A
  • Variant angina; angina of rest; α-mediated angina
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7
Q

What is the cause of Prinzmetal angina?

A
  • The coronary artery undergoes severe spasm due to overactivity of α1 receptors.
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8
Q

What are the symptoms of Prinzmetal angina?

A
  • The patient develops pain at rest.
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9
Q

How is stable angina managed?

A
  • Non-drug therapy = life style modification
  • Pharmacological therapy
  • Surgical treatment (myocardial revascularization)
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10
Q

What is the non-drug therapy for stable angina?

A
  • Alteration of lifestyle
  • Correct obesity and reduce fat intake
  • Treatment of predisposing factors
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11
Q

What is the pharmacological therapy for stable angina?

A
  • Immediate treatment of acute chest pain:
    ✓ Glyceryl trinitrate (GTN): sublingual or spray.
    ✓ Refer the patient to hospital if an ACS is suspected.
  • Long-term therapy:
    ✓ Beta-blockers: the first-line agents for chronic stable (exertional) angina.

✓ CCBs: the second-line agents for chronic stable angina

✓ Long and intermediate acting nitrates.

✓ Newer drugs: nicorandil , trimetazidine , Ivabradine, ranolazine

✓ Lipid lowering drugs: statins

✓ Antiplatelet drugs: e.g. aspirin, clopidogrel (see pharmacology of blood).

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12
Q

What is the classification of organic nitrates and nitrites?

A

Glyceryl trinitrate (GTN)

Isosorbide dinitrate

Isosorbide mononitrate

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13
Q

What is the onset of Glyceryl trinitrate (GTN), Isosorbide dinitrate and Isosorbide mononitrate Respictively?

A

Short - medium - long

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14
Q

What is the route of adminstration of Glyceryl trinitrate (GTN), Isosorbide dinitrate and Isosorbide mononitrate Respictively?

A

SL/TD - SL/Oral - Oral

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15
Q

What is the status of first pass metabolism of Glyceryl trinitrate (GTN), Isosorbide dinitrate and Isosorbide mononitrate Respictively?

A

Present - present - absent

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16
Q

What is the onset of GTN?

A

1 – 5 min

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17
Q

What is the duration of transdermal patches for treatment of angina?

A

10 hrs. duration

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18
Q

When are GTN mainly used?

A
  • Relief of acute angina attack.
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19
Q

When are isosorbide mononitrates mainly used?

A
  • Prophylaxis to prevent attacks
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20
Q

What is the pharmacokinetics of organic nitrates and nitrites?

A
  • Absorption:
    ✓ Nitrates are rapidly absorbed from all sites of administration.
  • Metabolism: in the liver:
    ✓ If given oral → extensive first-pass metabolism (oral
    bioavailability <10%)
    ✓ If given sublingual → no first-pass metabolism → high
    bioavailability.
    ✓ Mononitrate: Has no hepatic metabolism → long duration of action.
  • Excretion:
    ✓ via the kidney.
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21
Q

What is the mechanism of action of organic nitrates and nitrites?

A
  • Nitrates cause formation of the free radical nitric oxide (NO) which is identical to the endothelial derived relaxing factor (EDRF) → ↑ cGMP → VD (more on veins than arteries).
  • They also ↑ formation of vasodilator PGE2 and PGI2.
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22
Q

What are the pharmacological effects of organic nitrates and nitrites?

“By two ways”

A

CVS: Blood vessels:
✓ VD of the venous (and to lesser extent the arterial) side leading to ↓ preload and ↓ afterload → ↓ cardiac work.
✓ VD of coronary arteries leading to increased coronary blood flow.
✓ VD of arteries in the face and neck leading to flushing of the face.
✓ VD of meningeal arteries leading to throbbing headache.

  • Heart: Reflex tachycardia (in high dose) 2ry to ↓ BP.
  • BP: High doses cause ↓↓ in both systolic and diastolic BP.
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23
Q

What are the therapeutic uses of organic nitrates and nitrites?

A
  • Angina pectoris
  • Myocardial infarction: to ↓ the area of myocardial damage. “Just dec, no full treatment”
  • Acute heart failure: to ↓ preload and afterload.
24
Q

How do organic nitrates and nitrites treat angina pectoris?

A

✓ Nitrates are used for treatment of all types of angina both for relieving the acute attack and for prophylaxis.

✓ Decrease cardiac work & myocardial O2 demand through:
▪ Venodilatation → ↓ venous return (preload = ↓ end-diastolic pressure).
▪ Arteriolodilatation → ↓ peripheral resistance (afterload).

✓ Enhancement of coronary blood flow (perfusion) through:
▪ Coronary VD.
▪ Redistribution of blood from large epicordial vessels to
ischemic subendocardial vessels.

25
Q

What are the side effects of organic nitrates and nitrites?

A
  • Throbbing headache
  • Flushing of face
  • Orthostatic hypotension
  • Reflex tachycardia
  • Tolerance
26
Q

What causes tolerance to organic nitrates and nitrites?

A
  • Inactivation of mitochondrial enzyme
27
Q

How is tolerance to organic nitrates and nitrites managed?

A
  • Nitrate free period.
28
Q

What are the precautions that should be followed while nitrate therapy?

A
  • Check the expiry date (active tablets have burning taste).
  • Use the smallest effective dose to avoid hypotension and reflex tachycardia.
  • The patient should expel the SL tablet after pain relief.
  • The patient should consult his doctor if anginal pain does not improve after taking 3 SL tablets of NG during 15 min (the pain may be due to ACS)
  • Nitrates are contraindicated with sildenafil severe hypotension
29
Q

What are examples of beta blockers used in treatment of angina?

A
  • Nonselective (β1- & β2) ✓ e.g. propranolol
  • Cardioselective β1-blocker ✓ e.g. atenolol
  • β-blocker With α-blocking activity ✓ e.g., (β-blocker with VD effect) carvedilol
30
Q

What is a mechanism of action of beta blockers in treatment of angina?

A
  • Competitive inhibitors of catecholamine at β-adrenoceptors
  • Inhibit sympathetic stimulation of heart (β1) HR & contractility cardiac work & O2 requirement at rest and during exercise
31
Q

What is the clinical use of beta blockers in treatment of angina?

A
  • BB is the 1st choice in exertional angina
  • Absolutely CI in variant angina (because they block the β2- mediated coronary dilatation leaving the α1 receptors unopposed → ↑ coronary spasm).
32
Q

What are the side effects of beta blockers in treatment of angina?

A
  • Beta-1 effects:
    ✓ Bradycardia, heart block, heart failure
  • Beta-2 effects:
    ✓ bronchospasm, worsening PVD (peripheral vascular disease)
  • Others:
    ✓ Fatigue, depression, nightmares, impotence
33
Q

When are beta blockers contraindicated?

A
  • Variant angina (CI)
  • Asthma (CI)
  • Verapamil (CCB) and beta blockers are CI as both are myocardial depressants (inhibit conduction & contraction)
  • Avoid abrupt withdrawal
34
Q

What are examples of calcium channel blockers used in treatment of angina?

A
  • Verapamil
    ✓ Relatively cardioselective
    ✓ - ve chronotropic and inotropic
  • Nifedipine , amlodipine
    ✓ Smooth muscle selective
    ✓ Potent arterial dilator
  • Diltiazem
    ✓ Intermediate properties
35
Q

What is the mechanism of action of calcium channel blockers?

A
  • Block cardiac and smooth muscle voltage-gated L-type Ca++ channels
36
Q

What are the pharmacological effects of calcium channel blockers in treatment of angina?

A
  • Cardio-selective CCBs (verapamil & diltiazem):
    ✓ ↓↓ myocardial contractility and myocardial O2 demand.
    ✓ Produce coronary VD and ↑ coronary blood flow.
    ✓ ↓ Ca2+- mediated myocyte cell necrosis.
  • Nifedipine, amlodipine CCBs
    ✓ Vasodilator effect on resistance vessels → ↓↓ afterload
    ✓ Produce coronary VD and ↑ coronary blood flow.
37
Q

What is the Clinical use of calcium channel blockers in treatment of angina?

A
  • CCB is the 1st choice in variant angina

- Alternative to Betablockers (BB) instable angina if BB is contraindicated

38
Q

What are the advantages of combination of beta blockers with nitrates?

A
  • Combination of BBs and nitrates ↑ their efficiency & ↓ their side effects

“Check the table”

39
Q

Why shouldn’t nitrates be combined with nifedipine?

A
  • As it would cause severe hypotension and reflex tachycardia
40
Q

Why you shouldn’t beta blockers be combined with verapmil?

A
  • As it would cause heart block and Bradycardia
41
Q

What is additional therapy in treatment of stable angina?

A
  • Potassium-channel activators:(Nicorandil)

- Metabolic modulators (Cytoprotective)

42
Q

What is the mechanism of action of nicorandil?

A

✓ It combines activation, of the potassium k, channel with nitro- vasodilator (NO donor) actions.

✓ It is both an arterial and a venous dilator,

43
Q

What are the uses of nicorandil?

A

✓ It is used for patients who remain symptomatic despite optimal management with other drugs, often while they await surgery or angioplasty.

44
Q

What are the adverse effects of nicorandil?

A

✓ headache, flushing and dizziness.

“FHD”

45
Q

What are metabolic modulators (cytoprotective)?

A
  1. Na Channel blocker: Ranolazine
  2. Trimetazidine
  3. Ivabradine
46
Q

What is the mechanism of action of Na channel blocker (Ranolazine)?

“Dec intacellular Na which dec intracellular Ca”

A
  • It inhibits the late phase of the Na current →↓ intracellular Na →↓ intracellular Ca (↓ Ca overload that causes ischemia & death).
  • It has no effect on hemodynamic circulation.
47
Q

What are the uses of Ranolazine?

A
  • In chronic angina when other antianginal therapies fail
48
Q

What is the mechanism of action of trimetazidine?

“Enhances glocuse oxidation instead of fatty acids oxidation”

A
  • Inhibits beta-oxidation of fatty acids pathway in myocardium, which enhances glucose oxidation.
  • In an ischemic cell, energy obtained during glucose oxidation requires less oxygen consumption than in the beta-oxidation process.
49
Q

What is the use of trimetazidine?

A

Unstable angina, orally

50
Q

What is a mechanism of action of ivabradine? “Dec HR”

A
  • Selectively inhibits the pacemaker current leading to decrease cardiac pacemaker activity
  • Slowing the heart rate and allowing more time for blood to flow to the myocardium.
51
Q

What are other drugs used in management of angina?

A
  • Anti-platelets:
    Aspirin & clopidogrel
  • Other drugs
    1. Lipid-lowering therapy (statins): inhibit cholesterol synthesis in the liver
  1. ACE inhibitors: Reduction in preload and afterload, Reduction in left ventricular mass & inhibit pathological remodelling
52
Q

What is the most preferred and least preferred drugs in treatment of Angina with bronchial asthma?

A
  • Nitrates, CCBs

- Beta-Blockers

53
Q

What is the most preferred and least preferred drugs in treatment of Angina with heart failure?

A
  • Amlodipine

- Beta-Blockers

54
Q

What is the most preferred and least preferred drugs in treatment of Angina with hypertension?

A
  • Beta-Blockers, CCBs

- Nitrates

55
Q

What is the most preferred and least preferred drugs in treatment of Angina with DM?

A
  • Nitrates, Nifedipine

- Beta-Blockers, Verapamil

56
Q

How are acute coronary syndromes managed?

“‏مسكن + ‏أكسجين + ‏تذويب الجلطة + Nitrate or BB’

A

Hospitalization in CCU “MONA” + “T”

  • Morphine or Diamorphine
    ▪ Analgesia ▪ Afterload and Preload
  • Oxygen
  • Nitrates &/or Beta-blocker(Limit infraction size)
  • Aspirin &/or Clopidogrel
  • Anticoagulant &/or Thrombolytics

CVS & IBL - Pharmacology 💊 (6 decks)

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