Angina drugs Flashcards

1
Q

First line treatment of angina

A

nitrates
CCBs
beta blockers

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2
Q

nitrates- examples

A

nitroglycerin

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3
Q

nitrate MOA

A
  • dilation of veins
  • dilation of large arteries
  • dilation of coronary collateral
  • prevent vasospasm (variant angina)

nitrate can be converted into nitric oxide

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4
Q

nitrate- pharmacokinetics

A
  • low oral bioavailability due to fast metabolism by the liver, use sublingual route instead
  • rapid onset, short duration of action, excreted by kidneys
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5
Q

nitrate- complications

A

tachyphylaxis- 8-12 hours of nitrate free period, usually at night
dependence- arterial and digital vasospasm if withdraw suddenly, have to be careful when without with chronic patients

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6
Q

nitrate- drug cautions

A
  • do not take with PDE5 inhibitors (slidenafil) because it causes hypotension then reflex tachycardia
  • and soluble guanylate cyclase stimulators such as riociguat
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7
Q

nitrate- contraindications and side effects

A
  • orthostatic hypotension, tachycardia, headache

contraindicated in increased intracranial pressure patients

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8
Q

nitrate- route of administration

A
  • sublingual: immediate relieve
  • oral: need high dose or sustained release formulation for prophylaxis
  • subcutaneous: prophylaxis for nocturnal angina
  • buccal or transmucosal: above the incisor under the upper lip, prophylaxis for a short time
  • IV: coronary spasm
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9
Q

CCBs

A
  • artery and arterioles vasodilation
  • reduce force of contraction of the heart
  • reduce coronary spasm (variant angina)
  • vascular selective one may cause hypotension (reduce coronary blood flow) and tachycardia (worsen)
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10
Q

beta blockers

A
  • reduce force and rate of contraction of the heart
  • increasing the diastole duration, coronary blood flow duration and perfusion to the myocardium
  • causes vasospasm (contraindicated in variant angina)
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11
Q

nicorandil- MOA

A
  • similar to nitrate: stimulate the guanylate cyclase activity
  • activate the ATP-sensitive K channels in VSCM: hyperpolarization of smooth muscle and vasodilation
  • reduce coronary spasm (variant angina)
  • act on both artery and venous
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12
Q

nicorandil- side effects

A

hypotension, tachycardia, headache

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13
Q

trimetazidine- MOA

A
  • inhibit the 3-KAT
  • inhibit the fatty acid oxidation, have to switch to glucose oxidation for more efficient utilization of cardiac oxygen
  • usable in low heart rate and bp patients
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14
Q

trimetazidine- side effects

A

parkinson syndrome

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15
Q

ranolazine- MOA

A
  • inhibit the late Na current (usually seen in ischemia)
  • reduce the Na influx and therefore reduce the influx of Ca by Na Ca exchanger
  • reduce intracellular Ca overload and contractility
  • reduce the cardiac workload
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16
Q

ranolazine- contraindications and side effects

A
  • do not use with CYP3A4 inhibitors

- inhibit the potassium current -> don’t use in long QT syndrome patients and prolong the duration of action potential

17
Q

Ivabradine- MOA

A
  • inhibit the HCN channels of SA node to reduce the funny current, reducing the heart rate
  • reduce the cardiac workload
  • increase coronary perfusion
18
Q

ivabradine- side effects

A
  • bradycardia

- atrial fibrillation (take over by the AV node)

19
Q

ivabradine- use

A

alternative for patients not responding to beta blockers

20
Q

ivabradine- cautions and contraindications

A
  • do not use with CYP3A4 inhibitors
  • do not use with CCBs, hypokalemia inducing drug e.g. loop and thiazide, long QT inducing drugs e.g. sotalol and quinidine
  • must have 70 bpm, chronic stable angina with normal sinus rhythm
  • do not use in hypotension patients
  • do not use in pregnant or possibly will be pregnant patients
21
Q

Combination therapy

A

vascular + cardiac
CCBs + nitrate
dihydropyridine + beta blockers
beta blockers + nitrate