Angina - Pharm Q1 Test 3

Front 1

short acting nitrates (3)

Back 1

1. amyl nitrite (inhalant)
2. nitroglycerin (sublingual
3. isosorbide dinitrate (sublingual)

**all minutes

Front 2

long acting nitrates (2)

Back 2

1. nitroglycerin (oral, ointment, sublingual, transdermal)
2. isosorbide dinitrate (oral and chewable)

Front 3

Nitrates mechanism of action for vasodilation

Back 3

nitrite ion --> metab to NO --> activates GC --> increases cGMP --> relaxes vascular smooth muscle

**all VSM are relaxed, but VD is uneven

Front 4

Uneven VD in nitrates

Back 4

- large veins are dilated --> increased venous capacitance and decrease preload = dec heart WL

- arterioles and precap sphincters dilated less, but still decrease after load

**veins > arteries
venodilation most

Front 5

DOC for acute angina attack

Back 5

nitrates

Front 6

Good and bad effects of nitrates

Back 6

GOOD
- decreased pre/after load = decreased cardiac workload

BAD
- can increase cardiac workload
- decrease BP --> increase symp activity (baroreflex) --> increase HR and contractility

**this reflex tachycardia will shorten the time for diastolic perfusion

Front 7

Two mechanisms for anginal relief with nitrate therapy

Back 7

1. Predominant relief mechanism:
**decrease 02 requirement
- lg vein dilation = decreased preload and cardiac work

2. Secondary relief mechanism:
- redistribute coronary blood flow from normal to ischemic areas (even though total flow remains the same)

Front 8

Other uses for nitrates (3)

Back 8

1. relax other smooth muscles (bronchi, GI, GU)
2. methemoglobin formation for reversing cyanide poisoning
3. viagra

Front 9

Routes of administration of nitrates and key points

Back 9

1. Oral
- rapidly metabolized (high first pass)

2. Sublingual
- preferred for rapid absorption
* avoids hepatic destruction
(nitroglycerin and isosorbide dinitrate)
*nitroglycerin = rapid onset and short duration

3. Inhalation
*fastest acting

4. Transdermal

Front 10

Adverse effects of nitrates (2)

Back 10

1. Acute toxicity
- high VD leading to orthostatic hypotension, tachycardia, and *throbbing headaches*

2. Tolerance
- **NOT GOOD FOR LONG TERM TX**

Front 11

Calcium Channel Blocker drugs and specificity

Back 11

Dihydropyridines (dipines)
**vascular specific (VD = baroreflex)**
1. Nifedipine
2. Nimodipine
3. Nicardipine
4. Amlodipine

Others
**Heart specific
1. Diltiazem
2. Verapamil

Front 12

What vessels and muscles do CCB effect?

Back 12

- relax ALL Ca-dependent smooth muscles

- arterioles > veins

Front 13

Major cardiac effects of CCB (3)

Back 13

1. negative ionotropic effect (b/c decreased contractility)
2. reduced SA node impulse
3. slowed AV conduction

Front 14

Which CCB have the
1) strongest VD effects
2) strongest cardiac effects

Back 14

1. strongest VD effects = nifedipine
2. strongest cardiac effects = verapamil

*diltiazem is in between

Front 15

What kind of treatment are CCB good for?

Back 15

CHRONIC (no tolerance)

- not good with acute/rapid

Front 16

Nifedipine and other dihydropyridines (CCB) beneficial and harmful effects

Back 16

Beneficial
- angina relief
- coronary VD = relaxes vasospasms and some increase O2 supply
- systemic arterial VD = decreased after load

Harmful:
- enhanced dev of MI
- rapid hypoTN --> reflex symp activation --> increase cardiac WL (reflex tachycardia)

Front 17

Verapamil and diltiazem (CCB) beneficial and harmful effects

Back 17

Beneficial:
- anginal relief
- decreased contractility = decreased cardiac WL
- decreased SA automaticity and AV node --> bradycardia --> decreased cardiac WL

Harmful:
- too slow = cardiac depression, ending in:
- cardiac arrest
- AV block
- CHF

**less likely to cause tachycardia b/c weak VD and directly depresses SA/AV nodes

Front 18

Beta blockers drugs in angina (4)

Back 18

1. Propranolol
2. Metoprolol
3. Nebivolol
4. Acebutolol

Front 19

BB CV effects at three organs:

Back 19

1. Heart - reduce CO
2. Kidneys - reduce renin secretion
- dec blood volume = dec diastole = dec pre/postload
3. CNS - reduce symp vasomotor tone

Front 20

Benificial anginal relief effects of BB

Back 20

dec symp activation --> dec cardiac activity and dec VC --> hypoTN and bradycardia --> dec cardiac WL --> dec O2 demand

**bradycardia will also inc perfusion time

Front 21

Are BB effective in producing coronary VD? And why?

Back 21

NO
BB do not directly cause VD

Front 22

BB contraindications in "diseased" patients (for angina tx) (7)

Back 22

1. acute MI
2. cardiomegaly
3. compensated heart failure
**all above can induce/worsen CHF
4. diabetics
5. pts with high lipid levels
6. pts with variant angina (BB don't directly cause VD = not help vasospasm)
7. ASTHMA!! (BRONCHOCONSTRICTION)

Front 23

Adverse effects of BB in angina patients (6)

Back 23

1. ***BRONCHOCONSTRICTION
2. plasma TC increased
3. delayed recovery from hypoglycemia
4. CNS side effects
- fatigue, depression, sleep probe
5. worsen CHF (with preexisting conditions)
6. harmful in variant angina pts
- slow HR and inc ejection time --> inc left ventricular EDV --> increase O2 needs (so opposite effect)

Front 24

Angina treatment for variant/angiospastic angina

Back 24

Nitrates and CCB (more effective than BB)
- want direct VD <-- BB doesn't

for CCB: want dipines, not verapamil b/c it has no VD effects

Front 25

Most effective drug combo for angina

Back 25

BB and a VD (nifedipine or nitrate)

Front 26

Angina pt with asthma: preferred and least preferred drugs

Back 26

Preferred:
- CCB
- nitrate/nitrite

Least:
- BB

Front 27

Angina pt with DM: preferred and least preferred drugs

Back 27

Preferred:
- CCB
- nitrate/nitrite

Least:
- BB

Front 28

Angina pt with heart failure: preferred and least preferred drugs

Back 28

Preferred:
- nitrate/nitrite

Least:
- BB
- diltiazem (CCB)
- verpamil (CCB)

Front 29

Angina pt with HTN: preferred and least preferred drugs

Back 29

Preferred:
- BB
- CCB

Least:
- nitrate/nitrite

Front 30

Angina pt with peptic ulcer: preferred and least preferred drugs

Back 30

Preferred:
- BB
- nitrate/nitrite

Least:
- CCB

Front 31

PDE5 inhibitor drugs for "angina" (3)

Back 31

1. Sildenafil (viagra)
2. Vardenafil
3. Tadalafil

Front 32

Indications for sildenafil (2)

Back 32

- ED
- pulmonary HTN

Front 33

Pharmacokinetics of sildenafil:
1) Administration
2) Absorption
3) Plasma concentrations
4) Half-life
5) Metabolized

Back 33

1) Administration = oral
2) Absorption = rapid (40% bioavailability)
3) Plasma concentrations (max at 30 min-2 hrs)
4) Half-life = 4 hours
5) Metabolized = by CYP3A4 = lots of ixns

Front 34

Adverse effects of sildenafil (2)

Back 34

1. VISUAL IMPAIRMENT = BLUE TINGE

2. general transient mild/mod
- headache, flushing, nasal conges, UTI, dyspepsia

Front 35

Sildenafil contraindications (other drugs) (2)

Back 35

nitrates/nitrites
alpha blockers

= severe hypoTN

Front 36

Vardenafil and Tadalafil drugs

Back 36

*both similar to sildenafil
* pre selective for PDE5 than PDE6 (less visual effects)

Vardenafil
- max conc sooner than sil or tad

Tadalafil
- longer duration = more spontaneity