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89 Cards in this Set

  • Front
  • Back
Describe the etiology and tx of Classic "Angina of effort"
Obstruction, esp with exercise

Drugs or surgery
Describe the etiology and tx of Variable/Prinzmetal's Angina
Spasm or VC

Reversed by nitrates or CCBs
O2 demand depends on (3):

Wall tension changed by (2):
Cardiac workload = HR, contractility, and wall tension

Pressure and volume
Coronary blood flow is proportional to (2):
Perfusion pressure and duration of diastole
How do antianginal drugs work (2)?

Why is increasing 02 supply inefficient for tx of angina?
Increase 02 supply

Decrease 02 demand

"Coronary steal" phenomenon
Which drug classes improve the regional flow distribution to the heart (02 supply)? {3 classes}
Nitrates, CCBs, BBs
Which drug classes improve coronary blood flow (02 supply)? {2 classes}
Nitrates, CCBs
Which drug classes decrease HR & contractility (02 demand)? {2 classes}
Some CCBs, BBs
Which drug classes decrease preload (02 demand)? {1 class}
Nitrates
Which drug classes decrease afterload (02 demand)? {1 class}
CCBs
Which are the 3 fastest acting nitrates?
Inhaled amyl nitrite
IV nitroprusside (risk of cyanide poisoning)
Sublingual nitroglycerin (bypasses first pass metab)
Nitroglycerin & Isosorbide dinitrate

Biochem Mech
Causes VD by releasing nitrite ion, which is metab to NO, which activates GC, which increases cGMP
VD by nitrates is uneven. Describe how.
Large veins are markedly dilated and decrease preload.

Small arterioles are less dilated and decrease afterload.

Either way, you still get decreased 02 demand.
What are the two general relief mechanisms of nitro tx?

Does total coronary blood flow change?
Predominant relief mech: decrease 02 demand

Secondary relief mech: redistribution of coronary bloff flow

No
What other parts of the body will nitro affect (3)?
Any smooth mm: bronchi, GI, GU.
What does sodium nitrite have to do with cyanide?
Sodium nitrite is used to induce methemoglobin formation for tx of cyanide poisoning.
Nitro drugs

Adverse Effects (3)
Acute toxicity = marked hypotension, HA, tachycardia

Can result in tolerance

Can result in Monday disease.
What is Monday Disease?
Refers to workers who are chronically exposed to high nitrate levels. Their tolerance drops over the weekend, and they experience toxicity sxs on Monday back at work.
Name the 6 important CCBs for angina tx.
Verapamil
Diltiazem
"- dipines"/dihydropyridines
- Nifedipine
- Nimodipine
- Isradipine
- Amlodipine/Norvasc
What is the mech of CCBs?

What are the two effects relating to the tx of angina?
Bind L-type CCs on sm mm.

Decreases cardiac contractility, automaticity, conduction and also causes long-term vasc VD.
What two roles does IC Ca play?
Triggers muscle contraction in myocardium & vasc sm mm

Required for pacemaker activity (SA & AV node)

Will also relax other sm mm to lesser extent.
In heart and vasc sm mm, what opens Ca channels?

Then, what drug closes them?
Beta rec stim opens them.

CCBs (duh)
Which blood vessels are most sensitive to CCB VD?

Which drug has the greatest impact on arteriolar VD?

Which drug has the greatest impact on venous VD?
Arterioles

CCBs

Nitrites
Which drugs don't affect venous dilation at all, but have some effect on arteriolar VD?
Hydralazine and Minoxidil
What are the three prototypes for CCBs? Compare them.
Verapamil - strongest cardiac effects (Depress automaticity)

Nifedipine - strongest VD & reflex tachycardia inducer. Also, diff type: dihydropyridine.

diltiazem - inbetween.
nifedipine

Drug Class:

How can it cause MI?

General Adverse Effect of CCBs:
CCB

Causes rapid hypotension, reflex tachycardia.

Hyperglycemia & decreased platelet aggregation
Verapamil, Diltiazem

Drug Class:

Main Adverse Effect:

General Adverse Effect of CCBs:

Contraindications:
CCB

Might cause serious cardiac depression through SA/AV node effects

Hyperglycemia & decreased platelet aggregation

GF inhibits P450 = verapamil toxicity
What do Beta Blockers do for angina (2)?

What do Beta Blockers NOT do, ever?
Decrease SNS = less 02 demand.

Resulting bradycardia increases coronary perfusion time

They never produce coronary VD!
Beta Blockers

Adverse Effects (4):

Which angina do you NOT use Beta Blockers for?
Bronchoconstriction
Hyperlipidemia
Mask hypoglycemia
CNS effects

Do NOT use them for Variant/Prinzmetal's angina: slows HR, prolongs ejection time, increases LV end-diastolic volume = increased O2 demand.
List the 3 PDE5 inhibitors
sildenafil
vardenefil
taladaifil
What were PDE5I's first developed for?

What else do they treat, besides ED?
Tx of angina

Tx of pulmonary HTN
Sildenafil

Drug Class:

Mech:

Why might someone have vision troubles using sildenafil?
PDE5I

Selective inhibition of cGMP specific PDE, increasing NO release.

Somewhat selective for retina-specific PDE6
Sildenafil

PHKs:

Interactions:

Contraindications:
Oral: well abs, rapid action
t1/2: 4 hrs
P450 3A4 metab

Do NOT use with nitro tx, alpha blockers, or 3A4 inhibitors = severe
hypotension.

NOT for use in children or pregnant women.
Vardenifil

Drug Class:

How is it different from sildenafil (2)?
PDE5I

More selective for PDE5, so less visual side effects.

Also achieves maximum plasma concentration sooner. Gets the pt into the action faster.
Tadalafil (Hey, honey! Ta-da!!!)

Drug Class:

How is it different from sildenafil (3)?
PDE5I

Longer duration: 24-36 hrs
Allows for more sexual sponteneity
Zero visual disturbances
Ranolazine

Drug Class:

Mechs (3):

Use:
None mentioned

PFox inhibitor
Inhibits late inward Na current
Decreases LV stiffness

Tx of chronic, stable angina as a last resort
Ranolazine

PHKs (3):

May cause:
Oral: 73% bioavail
RExc
P450 metab - so lots of interactions expected

TdP
Bosentan

Drug Class:

Mech:

Use:

Adverse Effects:
Endothelin rec antagonist

Competitive antagonist for both Type A & B recs

Orally, and only for severe pulm HTN

P450 rxns, teratogenic
What are the two tx goals for angina?
Increase exercise tolerance

Decrease frequency of attacks
List three common drug combos for the tx of angina
BBs & CCBs

2 CCBs

Nitrates & BB or CCBs to decrease reflex tachycardia.
What are endothelins?

So, then, what is an example of an endothelin rec inhibitor?
Peptides that counter NO = VC

Bosentan = VD
If your patient has X, tx with ?:

Asthma:
DM:
HF:
HTN:
Ulcer:
Asthma: CCB, NO
DM: CCB, NO
HF: NO
HTN: BB, CCB
Ulcer: BB, NO
Which anti-HTNs work at the VMC (2)?
Clonodine
Methyldopa
Which anti-HTNs work at the SNS nerves (2)?
Reserpine
guanethidine
Which anti-HTNs work at the a-recs in blood vessels (1)?
The "-sins"
Which anti-HTNs work at the beta-recs in the heart (1)?
The Beta Blockers - "-olols"
Which anti-HTNs work at the vasc sm mm and/or cause VD (8)?
VDs: hydralazine, minoxidil, diazoxide, nitroprusside (VD both arteries & veins)

CCBs: verapamil, diltiazem, "-dipines"

D1 rec agonist: fenoldopam
Which anti-HTNs work at the kidneys (1)?
Diuretics
What does the poly pill consist of (6 drugs)? [tx of FATBAS-tards]
Folic acid, Aspirin, Thiazides, BBs, ACEIs, Statins
If your pt is over 65 and has HTN, what do you treat with?

What do you NOT treat with?
Diuretics, ACEIs, CCBs

(Central acting a-agonist)
If your pt is African American and has HTN, what do you treat with?

What do you NOT treat with?
Diuretics, CCBs

(BBs)
If your pt is pregnant and has HTN, what do you treat with?

What do you NOT treat with?
Methyldopa, labetalol

(ACEI, ARB)
If your pt has angina pectoris and has HTN, what do you treat with?

What do you NOT treat with?
BBs, CCBs

(Central acting a-agonist)
If your pt has had an MI and has HTN, what do you treat with?
BB, ACEI, aldosterone antagonist
If your pt has CHF and has HTN, what do you treat with?
Diuretic, ACEI, ARB, BB
If your pt has asthma and has HTN, what do you treat with?

What do you NOT treat with?
CCB, ACEI

(Never BB)
How do diuretics tx HTN (2)?

Which thiazide is a VD?
Acutely, they reduce body Na stores, reducing blood volume.

After 6-8 wks, they activate K channels, causing a decrease in periph resistance.

Indapamide
Thiazides are most effective in what population?

Which diuretic is the 1st choice for HTN tx?
Old, black men.

Thiazides
List the 6 subtypes of sympatholytics used in HTN.
Central agonists
Ganglion Blockers
Neuron Blockers
a1 Blockers
BBs
Combined a & Beta Blockers
Clonodine & Methyldopa

Drug Class:

Mech (2):

Contraindications (2):
Central a-agonists

Act on a2 recs in brain medulla to decrease SNS tone.
Also results in decreased renin.

Do NOT use with TCAs or yohimbine
Clonodine and Methyldopa both have a risk of severe side effects. What are they?

Which one is a prodrug?
Clonodine: sudden w/d causes severe hypotension

Methyldopa: may cause hemolytic anemia with + Coomb's test. Prodrug.
How can clonodine be administered?
Orally or transdermally. Don't sit in a hot tub with a clonodine patch on - will pass out.
Mecamylamine

Drug Class:

Class action:

Used for:
Only Ganglion Blocker we need to know.

Complete blockade of PNS & SNS. Bad juju.

Not used much due to bad side effects, but this one is being used for tx of Tourette's (Fuck! ASS! Get me a beer!)
Guanethidine

Drug Class:

Mech:

Adverse Effect with IV admin:
Adrenergic Neuron Blocker

Replaces NE in the vesicles, inhibiting NE release.

HTN crisis, esp in pheochromocytoma.
What does guanethidine have to do with sex?
May cause retrograde ejaculation. (along with postural hypotension, diarrhea, fluid retention)
Reserpine/AKA:

Drug Class:

Mech:

Contraindications (1):
Reserpine = the "Dirty Drug"

Adrenergic Neuron Blocker

Called "dirty" because it eliminates SNS tone via inhibition of NE transport into vesicle.

Serious rx with MAOIs because released NE needs to be metab by MAO.
Prazosin (terazosin, doxazosin)

Drug Class:

Mech:

Huge benefit:
a1 Blockers

a1 block reduces NE - causes VD of BOTH arteries & veins

a1 selection means less reflex tachycardia
Prazosin

Adverse Effects (2):

Lack of adverse effect (1):
First-dose phenomenon: hypotension, syncope

Increased renin (& Na & H2O retention)

NO hyperlipidemia, though.
BBS and HTN

Mechs (3):

BBs are more effective for tx of HTN in:
Heart: reduce CO
Kidney: reduce renin
CNS: reduce SNS tone

Young white people.
Why would you add other HTN drugs to BB tx (2)?
Reduce reflex tachycardia from extreme VD
Counteract increase in renin
Nebivolol

Drug Class:

Other Mech:
BB

Increases prod of NO = periph VD
BB

Adverse Effects (3)
Hyperlipidemia + low HDL = atherosclerosis

Mask hypoglycemia

Increase exercise tol for angina pts but decrease for CHF pts
BB

Contraindicated conditions (4)

Preferred for (3)
DM
CHF
Cardiac Blocks
Asthma

angina, p MI, migraines
Labetalol & Carvedilol

Drug Class:

Other details (3):
Combined a & Beta Blockers = lowered BP

Labetolol is OK in pregnancy but is usually only used in emergencies.
They can be hepatotoxic.
May cause bronchospasm.
Hydralazine

Drug Class:

Administration:

Mechs (2):

Adverse Effects (2):
VD

Oral

Selectively dilates arteries
Also increases NO prod

SLE in slow acetylators
May cause angina due to reflex tachycardia
Minoxidil

Drug Class:

Administration:

Mech:

Adverse Effects:

Is also a:
VD

Oral

Selectively dilates arteries

Hypertrichosis
May cause angina due to reflex tachycardia

K channel blocker
Name two HTN drugs that also act through NO
Hydralazine
Sodium Nitroprusside
What combo HTN tx is incredibly effective in the African American population?
Hydralazine & isosorbide dinitrate
Sodium nitroprusside

Drug Class:

Administration:

Adverse Effects (2):

Mech:
VD

IV

Like NO, rapid.

Cyanide accum. & metab acidosis
Diazoxide

Drug Class:

Administration:

Mech:

Is also a:

Also causes:
VD

IV

Activates ATP K channels

Non-diuretic thiazide with long duration of action 24-36 hrs

Excessive hair growth
Fenoldopam

Drug Classes:

Administration:

Mech:
VD, D1 rec agonist

IV

Stims relax of sm smm. t1/2 = 5 mins
What drugs cause gingival hyperplasia (3)?
"-dipines" (CCBs)
phenytoin
cyclosporine
What is the most common adverse effect of verapamil?
Constipation
How do you tx long term HTN with VDs?

Acute?
Oral VDs

IV VDs
Captopril & Enalapril

Drug Class:

Mech:
ACEI

ACE converts AngI to AngII. When blocked = VD. Also destroys bradykinin, so inhibit = enough bradykinin.
Why would you use ACEIs for HTN?

Most effective for who?
Fewer side effects: no cardiac, CNS, or renal compromise.

Young white people.
ACEIs

More benefits (2):

Adverse Effects (3):
Well abs/excreted.
Enhances anti-HTN efficacy of other drugs.

Severe hypotension in hypovolemic pts
Acute renal failure in stenosis
Bad for 2nd & 3rd trimester of preg
May cause coughing & angioedema
Losartan

Drug Class:

Selective for:

Better because (2):
Angiotensin rec Blocker

AT1 recs

Reduce mortality better than atenolol
No coughing or angioedema like ACEIs
Aliskren

Drug Class:

Blocks:

Contraindicated in:
Renin inhibitor

Formation of AngI

Pregnancy