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CVS & IBL - Pharmacology πŸ’Š > L2: Antianginal drugs > Flashcards

L2: Antianginal drugs Flashcards

1
Q

What are ischemic heart diseases?

A
  • Chronic stable angina (Classic exertional angina) β€œeffort”
  • Acute coronary syndromes (ACS): β€œrest and effort”
    A. Unstable angina
    B. Myocardial infarction β€œresult from unstable angina”
  • Prinzmetal’s angina β€œrest 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; Ξ±-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 Ξ±1 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:
    βœ“ Glyceryl trinitrate (GTN): sublingual or spray.
    βœ“ Refer the patient to hospital if an ACS is suspected.
  • Long-term therapy:
    βœ“ Beta-blockers: the first-line agents for chronic stable (exertional) angina.

βœ“ CCBs: the second-line agents for chronic stable angina

βœ“ Long and intermediate acting nitrates.

βœ“ Newer drugs: nicorandil , trimetazidine , Ivabradine, ranolazine

βœ“ Lipid lowering drugs: statins

βœ“ 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:
    βœ“ Nitrates are rapidly absorbed from all sites of administration.
  • Metabolism: in the liver:
    βœ“ If given oral β†’ extensive first-pass metabolism (oral
    bioavailability <10%)
    βœ“ If given sublingual β†’ no first-pass metabolism β†’ high
    bioavailability.
    βœ“ Mononitrate: Has no hepatic metabolism β†’ long duration of action.
  • Excretion:
    βœ“ 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) β†’ ↑ cGMP β†’ 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?

β€œBy two ways”

A

CVS: Blood vessels:
βœ“ VD of the venous (and to lesser extent the arterial) side leading to ↓ preload and ↓ afterload β†’ ↓ cardiac work.
βœ“ VD of coronary arteries leading to increased coronary blood flow.
βœ“ VD of arteries in the face and neck leading to flushing of the face.
βœ“ 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. β€œJust dec, no full treatment”
  • Acute heart failure: to ↓ preload and afterload.
24
Q

How do organic nitrates and nitrites treat angina pectoris?

A

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

βœ“ Decrease cardiac work & myocardial O2 demand through:
β–ͺ Venodilatation β†’ ↓ venous return (preload = ↓ end-diastolic pressure).
β–ͺ Arteriolodilatation β†’ ↓ peripheral resistance (afterload).

βœ“ Enhancement of coronary blood flow (perfusion) through:
β–ͺ Coronary VD.
β–ͺ 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 (Ξ²1- & Ξ²2) βœ“ e.g. propranolol
  • Cardioselective Ξ²1-blocker βœ“ e.g. atenolol
  • Ξ²-blocker With Ξ±-blocking activity βœ“ e.g., (Ξ²-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 Ξ²-adrenoceptors
  • Inhibit sympathetic stimulation of heart (Ξ²1) 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 Ξ²2- mediated coronary dilatation leaving the Ξ±1 receptors unopposed β†’ ↑ coronary spasm).
32
Q

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

A
  • Beta-1 effects:
    βœ“ Bradycardia, heart block, heart failure
  • Beta-2 effects:
    βœ“ bronchospasm, worsening PVD (peripheral vascular disease)
  • Others:
    βœ“ 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
    βœ“ Relatively cardioselective
    βœ“ - ve chronotropic and inotropic
  • Nifedipine , amlodipine
    βœ“ Smooth muscle selective
    βœ“ Potent arterial dilator
  • Diltiazem
    βœ“ 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):
    βœ“ ↓↓ myocardial contractility and myocardial O2 demand.
    βœ“ Produce coronary VD and ↑ coronary blood flow.
    βœ“ ↓ Ca2+- mediated myocyte cell necrosis.
  • Nifedipine, amlodipine CCBs
    βœ“ Vasodilator effect on resistance vessels β†’ ↓↓ afterload
    βœ“ 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

β€œCheck 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

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

βœ“ It is both an arterial and a venous dilator,

43
Q

What are the uses of nicorandil?

A

βœ“ 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

βœ“ headache, flushing and dizziness.

β€œFHD”

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)?

β€œDec 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?

β€œEnhances 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? β€œDec 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?

β€œβ€Ω…Ψ³ΩƒΩ† + β€Ψ£ΩƒΨ³Ψ¬ΩŠΩ† + ‏Ψͺذويب Ψ§Ω„Ψ¬Ω„Ψ·Ψ© + Nitrate or BB’

A

Hospitalization in CCU β€œMONA” + β€œT”

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

CVS & IBL - Pharmacology πŸ’Š (6 decks)

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