Drugs used to Treat Angina (ch 46)

angina

Pain in response to lack of oxygen in the heart muscle

stable angina

• No damage to heart muscle.

• Basic reflexes surrounding the pain restore blood flow

unstable angina

Episodes of ischemia occur even when at rest

prinzmetal angina

Seems to be caused by spasm of the blood vessels, not just by vessel narrowing

acute myocardial infarction

• Coronary vessel becomes completely occluded and is unable to

deliver blood to the cardiac muscle.

• Area of muscle that depends on that vessel for oxygen becomes

ischemic and then necrotic.

• Pain can be excruciating.

• Nausea and severe sympathetic stress reaction may be present.

• Serious danger: arrhythmias can develop in nearby ischemic,

irritable tissue.

• Most deaths caused by MI are result of fatal arrhythmias.

antianginal agents

• Help restore appropriate supply-and-demand ratio in oxygen

delivery to the myocardium.

• Improve blood delivery to the heart muscle in one of two ways:

• By dilating blood vessels

• By decreasing the work of the heart

• All are effective.

• May be used in combination.

• Drug choice is determined by tolerance of adverse effects and

response to drug

beta blockers are not indicated for the treatment of?

Prinzmetal angina because they could cause peripheral ischemia and may

exacerbate vasospasm due to blocking of beta-receptor sites.

beta blockers

• Decrease in the excitability of the heart, a decrease in cardiac

output, a decrease in cardiac oxygen consumption, and a lowering

of blood pressure.

• They are indicated for the long-term management of angina

pectoris caused by atherosclerosis.

• These drugs are sometimes used in combination with nitrates to

increase exercise tolerance.

calcium channel blocker

indicated for the treatment of Prinzmetal angina, chronic angina, effort-associated angina, and

hypertension

in prinzmetal angina, calcium channel blockers relieve?

coronary artery vasospasm, increasing blood flow to the muscle cells

what is the prototype for the classification nitrates

nitroglycerin

what is the classification for the prototype nitroglycerin

nitrates

nitroglycerin therapeutic actions

Enter the bloodstream

• They are converted to nitric oxide (NO) inside vascular smooth

muscle.

• Nitric oxide activates an enzyme (guanylate cyclase).

• This increases cyclic GMP (cGMP).

• ↑ cGMP causes smooth muscle relaxation.

• Blood vessels dilate (vasodilation)

nitroglycerin therapeutic use

Treatment and prophylaxis of angina pectoris

nitroglycerin admin

• Rapid-acting forms (only transmucosal tablets, translingual spray

and Sublingual tablets treat an angina attack)

• Longer acting forms such as regular tablets, immediate release or

sustained release tablets/capsules are used to prevent attacks

from occurring

• IV nitroglycerin is used for severe unstable angina attacks and to

control blood pressure perioperatively and to treat heart failure

after acute MI

rapid-acting forms of nitroglycerin( transmucosal/ sublingual tablets + sprays) treat?

angina attacks

longer acting forms of nitroglycerin (regular tablets, immediate release/ sustained release) do what?

prevent attacks

IV introglycerin

severe unstable angina attacks and to

control blood pressure perioperatively and to treat heart failure

after acute MI

nitroglycerin adverse reactions

• Headache (severe at first, reduced with treatment)

• Orthostatic hypotension

• Tachycardia

• Tolerance develops quickly to all forms (decreased effectiveness)

nitroglycerin contraindications

• Allergy or tolerance to nitroglycerin or isosorbide

• Pregnancy, lactation

• Increased intracranial pressure

• Severe anemia

• Uncorrected hypovolemia- why ??????

nitroglycerin precautions

• Head trauma

• Glaucoma

• Cardiomyopathy

• Severe liver disease

• Conditions that cause dry mouth (sublingual and transmucosal forms)

nitroglycerin drug-drug interactions

Phosphodiesterase-5 (PDE5) inhibitors, such

as sildenafil may cause hypotension

• antihypertensive meds/ alcohol

• anti-cholinergic meds

nitroglycerin sublingual tablet instructions

place under tongue to dissolve when chest pain starts; if not relieved in 5

minutes, call 911, take a second tablet; take a third tablet 5 minutes later if no relief

nitroglycerin admin instructions

sublingual tablets, sustained-release capsules or tablets, a translingual

spray or transmucosal tablets, transdermal ointment or patch, and IV form

• Place sublingual tablets under tongue to dissolve when chest pain starts; if not relieved in 5

minutes, call 911, take a second tablet; take a third tablet 5 minutes later if no relief

• Sublingual sprays: Dose equals 1 or 2 sprays; as for sublingual tablets, no more than 3 doses in a

15-minute period

• Client should not swallow transmucosal tablets; may need to moisten mouth to help tablet

dissolve

• Transdermal patches are for prevention only; apply to a hairless area and rotate sites.

• Remove patches for 10–12 hours daily to prevent tolerance; apply patch in morning, remove at

night.

• When discontinuing long-acting forms, taper doses to prevent increased chest pain (vasospasm)

• IV form is infused continuously in a glass bottle with special tubing only

nitroglycerin interventions

• Monitor length and severity of client

headache – suggest mild analgesics PRN

• Monitor baseline BP and pulse; check again

when nitrate form reaches its peak effect

(e.g. ½ to 1 hr for transdermal forms)

• Monitor heart rate in clients taking nitrates

• Give beta blocker or calcium channel

blocker, if prescribed, to suppress

tachycardia

• Monitor for medication tolerance

nitroglycerin client instructions

• Take over-the-counter analgesic for unrelieved

headaches (most subside spontaneously within

20 minutes)

• Report dizziness, syncope to provider

• Move slowly from lying down to sitting or standing

to prevent injury

• Do not perform hazardous activity, such as driving,

if dizziness occurs

• Take pulse and report tachycardia above

prescribed parameters

• Remove transdermal forms for part of each day

• Take only as many sublingual tablets as needed

what is the classification for the prototype ranolazine

antianginal agent

what is the prototype for the classification antianginal agent

ranolazine

ranolazine therapeutic actions

• It blocks the late sodium (Na⁺) current in cardiac cells.

• ↓ Sodium inside the cell

• This leads to ↓ calcium inside the cell

• ↓ Calcium reduces tension in the heart muscle during diastole

• The heart muscle relaxes better

• Oxygen demand decreases

ranolazine therapeutic use

• Chronic stable angina.

• Used in combination with other antianginals (nitrates, beta blockers, and calcium channel

blockers).

• Does not affect HR, BP, or vascular resistance.

ranolazine adverse effects

• Common (Usually Mild)

• Dizziness

• Headache

• Constipation

• Nausea

• Serious (Monitor Closely)

• QT interval prolongation

• Palpitations

• Syncope

• Arrhythmias (risk for torsades de pointes) – can be lethal

ranolazine contraindications

• See drug to drug interactions

• Liver cirrhosis due to increased risk

of QT prolonging

ranolazine precautions

• Heart conditions that increase the

risk of prolonging the QT interval

• History of renal failure.

• Metformin ( concurrent use can

increase concentration of

metformin)

ranolazine drug-drug interactions

grapefruit juice, HIV protease inhibitors, macrolide

antibiotics, azole antifungals, and some calcium channel blocker

medications

ranolazine admin

• Administer orally twice a day with

or without food.

• Avoid giving grapefruit juice.

ranolazine interventions

• Assess and report adverse

effects.

• Monitor electrolytes and heart

rhythm for bradycardia,

arrhythmias, and prolonging of

QT interval.

• Monitor kidney function tests,

creatinine, BUN, and urine output

for with moderate or severe

kidney impairments.

ranolazine client instructions

• Do not crush, break, or chew.

• Do not eat grapefruit or drink grapefruit juice.

• Avoid drinking alcohol.

• Drive with caution or operating machinery and move slowly from

lying to standing position