Pharmacology - Ischemic Heart Disease (IHD) Flashcards by amanda kastel

angina pectoris meaning

how can it be divided?

chest pain bc of accumulation of metabolites due to ischemia of the heart

classic/effort
unstable/ACS
vasospastic/prinzmetal

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acute coronary syndrome (ACS) can also be called ___ angina

unstable angina (pain at rest)

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what is preload and afterload

preload - the left ventricular end diastolic volume (how much blood in left ventricle after filling)

afterload - systemic vascular resistance

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if O2 demand is greater than O2 supply, what condition is this?

ischemia

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name 4 factors contributing to O2 demand

heart rate
contractility
preload
afterload

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name 2 factors contributing to O2 supply

the coronary blood flow and regional myocardial blood flow

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name drug agents that decrease oxygen demand

name 2 that work on decreasing HR and contractility and 2 others

beta blockers and SOME calcium channel blockers (verapamil and diltiazem) work on the HR and contractility

others are organic nitrates and calcium channel blockers (dihydropyridines)

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name 3 agents that increase oxygen supply and improve coronary flow

vasodilators (esp ca channel blockers)

statins
antithrombotics

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non-medication option for CAD (coronary artery disease)

bypass surger/angioplasty/stent

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name 4 classes of drugs that can be used for CAD (ischemic heart disease)

antianginals
antiplatelets
statins
antihypertensives

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can diet and smoking cessation help with CAD/IHD

yes

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name 3 particular kinds of antihypertensives that can be used to treat CAD/IHD

ace inhibitors/ARBS
beta blockers

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name 2 new drugs (not part of a class) that can sometimes be used for CAD

ranolazine
ivabradine

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name 4 nitrate/nitrite drugs that can be used for CAD

amyl nitrite
isosorbide dinitrate
isosorbide mononitrate
nitroglycerin

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explain the MOA of anti anginals in CAD/IHD

they decrease the myocardial oxygen requirement by decreasing the major determinants of O2 demand (ie - heart size/HR/BP/contractility)

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in some patients, nitrates and calcium channel blockers have what additional benefit

they not only decrease the O2 demand, but in some pts they cause a redistribution of coronary flow and increase O2 DELIVERY to ischemic tissue

ALSO they can be used in variant angina to increase O2 delivery by reversing coronary artery spasm!

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name the 2 types of drugs that can be used in variant angina by increasing myocardial O2 delivery by reversing coronary artery spasm

nitrates and calcium channel blockers

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3 MOLECULAR mechanisms of antianginals

increased cAMP
decreased intracellular calcium
stabilize/prevent depolarization of smooth muscle membrane

NOTE - ONLY WORK ON SMOOTH MUSCLE !! NOT HEART

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How are nitrates stored

in tightly closed glass containers

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TRUE OR FALSE

all nitrates are prodrugs

true!!!

they all must be metabolized (reduced) to produce gaseous NO

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which 2 nitrates have very high first pass metabolism and thus their oral bioavailability is low

nitroglycerin and isosorbide dinitrate

bc the liver inactivates the drug with its high-capacity organic nitrate reductase

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true or false

nitroglycerin given sublingually bypasses its extensive first pass metabolism

TRUE

will go to heart before the liver

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true or false

nitroglycerin is not available in an ointment

false - it is

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true or false

sublingual nitroglycerin has a long peak plasma time and a short half life

FALSE – has a very fast peak plasma time of 5 mins and a short hald life of 3 mins

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true or false sublingual nitroglycerin has very fast action, but the effects do not last long

true

is the metabolite of nitroglycerin active

yes - but not nearly as active as original molecule

which is only used for prevention and why - isosorbide mononitrate or isosorbide dinitrate

isosorbide mononitrate has too slow of an onset to be used acutely.

true or false isosorbide mononitrate has no significant first pass metabolism and has a pretty long half life

TRUE 5-6 hour half life

true or false isosorbide dinitrate takes a long time to work

FALSE - only takes 6 mins metabolites give sustained action

true or false isosorbide dinitrate has high first pass metabolism

true

why is amyl nitrite not really used

smalls bad - and its vapor form to sniff it in also, short duration of action

how is amyl nitrite excreted

glucuronidation

explain the molecular MOA of nitrates

produced from arginine. through endothelial NO synthase enzyme NO is a gas and easily diffuses through the endothelial membrane and into SMOOTH MUSCLE CELLS (NOT CARDIAC) NO activates guanylyl cyclase. guanylyl cyclase makes cGMP cGMP is a secondary messenger which activates protein kinase G protein kinase G DEPHOSPHORYLATES myosin-light chain the dephosphorylated myosin light chain allows for RELAXATION OF SMOOTH MUSCLE CELLS

explain why PDE inhibitors cannot be taken with nitrates

both of them increase cGMP which relaxes smooth muscle WAY TOO MUCH --- hypotension liability

true or false phosphorylated myosin light chain causes smooth muscle contraction

TRUE

what enzyme converts nitroglycerin into nitrate + NO gas

aldehyde dehydrogenase

true or false nitrates ACTIVATE myosin light chain phosphatase

true - causes smooth muscle relaxation

true or false nitrates have NO EFFECT on cardiac and skeletal muscles

TRUE - ONLY SMOOTH

true or false nitrates relax the ENTIRE vascular system - both arteries and veins

true but have less effect on arterioles and precapillary sphincters

do nitrates have any effect on the heart?

they dont act directly on the heart, but they decrease preload by relaxing veins and increasing capacitance (ability to hold blood without increasing BP)

how do nitrates help ischemic regions

they redistribute coronary flow to ischemic regions

name the NEGATIVE EFFECTS of nitrates

the body's reflex responses are not very good cause reflex tachycardia and increased heart contraction -- also salt and water retention - to account for the decreased blood pressure

effect of nitrates at TOXIC doses what is the cure

methemoglobinemia methylene blue -- replaces cyanide from hemoglobin - can reverse

effect of nitrates on platelets is this good or bad

the increase in cGMP decreases platelet aggregation this is good in ischemic heart disease patients!

how are nitrates beneficial in each type of angina

classic - reduced oxygen demand reliefs symptoms unstable - decreased oxygen demand and dilates the coronary arteries prinzmetal/variant - relieves coronary artery spasm and relaxes coronary arteries

true or false nitrates can only be used in classic angina

false - all types

which form of nitroglycerin has the fastest onset, but lowest duration

sublingual nitroglycerin

name some side effects of nitroglycerin

headache hypotension--potential syncope reflex tachycardia tolerance!! "monday disease"

which dosage form of nitroglycerin has the slowest onset

transdermal

true or false nitroglycerin has high first pass metabolism

true

true or false isosorbide dinitrate has the same MOA as nitroglycerin

true

true or false the metabolite of isosorbide dinitrate is inactive

FALSE - active!! 1 of the metabolites is the mononitrate

true or false isosorbide dinitrate is rarely used today

true - except for sublingual dosage form. bc high tolerance

rank the following according to their tolerance isosorbide dinitrate isosorbide mononitrate nitroglycerin

highest tolerance - nitroglycerin isosorbide dinitrate lowest tolerance - isosorbide mononitrate

true or false isosorbide dinitrate has longer sublingual coverage than nitroglycerin

true

true or false isosorbide mononitrate has high tolerance liability

FALSE - low tolerance liability bypasses 1st pass metabolism

true or false isosorbide mononitrate bypasses 1st pass metabolism

true

___ is a metabolite of ___

isosorbide mononitrate is a metabolite of isosorbide dinitrate

is isosorbide mononitrate used acutely?

NO as a prophylactic - not during an angina attack

**caution for all nitrates

do not use with sildenafil!!!!!! (or others in category) can cause severe hypotension, fantining, or myocardial ischemia too much vasodilation!!!

some SE of isosorbide mononitrate

similar to nitroglycerin - flushing, reflex tachycardia, fainting also some respiratory effects like bronchitis, pneumonia

true or false sublingual nitroglycerin is for acute attack and prevention ONLY

true

which dosage forms of nitroglycerin are used prophylactically

long acting dosage forms - ie - po, patch

when should nitrates be discarded after opening

6 months

what is the phenylalkyl amine calcium channel blocker? what is the benzothiazepine calcium channel blocker?

phenylalkyl amine - verapamil benzothiazepine - diltiazem

Explain the MOA of calcium channel blockers

NORMALLY - calcium gets into the cell through a channel. calcium forms a complex with calmodulin. myosin light chain kinase is activated myosin light chain is phosphorylated this allows for contraction CALCIUM CHANNEL BLOCKERS BLOCK THIS PROCESS BY PREVENTING CALCIUM FROM GETTING INTO THE CELL THROUGH THE CHANNEL

which has more effect on decreasing cardiac contractility and decreasing SA and AV node conduction - verapamil or diltiazem

verapamil BOTH have much more effect on the heart than dihydropyridines

true or false nondihydropyridines increase cardiac contractility

FALSE - decrease

true or false nondihydropyridines AND dihydropyridines all cause vasodilation

TRUE - dihydropyridines just cause the most

are calcium channel blockers indicated for angina

yes

what type of calcium channels do CCB's block in which muscle are they found

L-type voltage gated found in cardiac, skeletal, and smooth muscle (DHP only act on smooth muscle and non DHP act on cardiac and smooth)

true or false calcium is a trigger for contraction in BOTH cardiac and smooth muscle

true

true or false calcium channel blockers inhibit calcium influx

true

calcium channel blockers have negative ____ effects on the heart

inotropic

***what region of the calcium channel do calcium channel blockers bind at

a1 subunit

***explain HOW calcium channel blockers bind to the channel

block FROM THE INSIDE, and only in OPEN and INACTIVATED states does NOT block when the channel is closed or gated

effect of calcium channel blockers (in general) on: -smooth muscle -the heart

smooth muscle - long-lasting relaxation heart - negative chronotropic, ionotropic, and dromotropic effects

which is more sensitive to relaxation by calcium channel blockers - arterioles or veins

arterioles are more sensitive - relax more

**true or false dihydropyridines have greater vascular effects than cardiac

true

**true or false verapamil/diltiazem have a similar effect on both vessels AND the heart

true action on heart is major tho

true or false dihydropyridines directly inhibit SNS activation of the heart

false - nondihydropyridines

true or false both dihydropyridines and nondihydropyridines increase cardiac output

true

Pharmacology - Ischemic Heart Disease (IHD) Flashcards

(83 cards)