Cardiovascular Drugs for Pharmacology Final
Name
Class/MOA
Clinical Use
-methyldopa
Prodrug, →-methylNE, an 2
agonist that↓’s CNS symp.
outflow
Treat HTN (second line)
Amiodarone
K+ channel blocker; also blocks
Na+ channels and β receptors.
Amlodipine
L-type Ca++-channel blocker;
Strong arteriolar vasodilation is
main effect.
β-blocker
HMG-CoA reductase inhibitor;
inhibits rate-limiting step in
cholesterol synthesis, up-regulates
hepatic LDL receptors, so↓LDL
ACE inhibitor; active drug,
competitive;↓angiotensin II and
aldosterone, so↓PVR and inhibits
AT-mediated hypertrophy;
Class III antiarrhythmic drug. DOC
to terminate A-fib, 2nd
choice for prevention.
DOC to suppress or
prevent V-tach.
A DOC for prophylaxis
of variant angina
Atenolol
Atorvastatin
(Lipitor®)
Captopril
Carvedilol
Cholestyramine
Clofibrate
Clonidine
Treat HTN, angina
Treat hyperlipidemia
(first-line for lowering
LDL)
1st line treatment of
CHF and HTN
Also beneficial effects on
serum lipids.
1, β1 and β2 blocker; (racemic
mixture);↓PVR,↑regulates β
receptors in heart. Also↓LVH.
Bile acid sequestrant (resin);
moderately lowers LDL cholesterol
Treat mild-to-moderate
CHF, HTN, ischemic
heart disease.
Fibrate – ligand for nuclear
receptor controlling FA
metabolism; effective in reducing
TG levels (↓40%)
2 agonist that↓’s CNS symp.
outflow (“sympatholytic”)
Treat hyperlipidemia
Treat hyperlipidemia
Treat HTN (second line)
Toxicity/Contraindications
Other
Don’t give i.v., or will cause ↑BP due to action
on vascular 2R’s. CNS effects: sedation,
fatigue, dry mouth, sexual dysfunction.
Hemolytic anemia.
NO drug-induced proarrhythmia!
Variable effects on thyroid function because it
is iodinated; some pulmonary toxicity.
↑levels of warfarin and digoxin with
amiodarone – often used in same patients!
Not widely used anymore
due to CNS side effects.
Contraindicated if already significant
hypotension; Don’t mix w/other vasodilators.
Reflex tachycardia (serious), headache, edema.
This one not really covered…
Contraindicated in active or chronic liver
disease, pregnancy.
Myopathy,↑liver transaminases.
Strongest vascular
effects of the Ca++
blockers (w/nifedipine).
Persistent cough, angioedema.
May↓renal fxn, so don’t use if renal artery
stenosis.
Kidney response to
lowered BP is blocked, so
diuretics not required
with ACE inhibitors.
Little effect on heart rate (no reflex tachycardia).
Same side effects as propranolol.
Short-term i.v., or longterm oral treatment.
Prolongs Q-T interval.
Good for pts. w/ CHF or
post-infarct.
Reduces risk for acute
coronary syndromes and
stroke.
Positive effects on lipid
profiles
Little systemic availability, so low toxicity.
Contraindicated if TG > 400 mg/dL (may↑
more)
Risk of gallstones.
Risk of myopathy when comb. w/statin.
Contraindicated w/ hepatic or renal insufficiency.
Often combined w/other
lipid-lowering drugs.
Sedation, fatigue, dry mouth, sexual dysfunction.
Apraclonidine = ocular
form,↓aqueous humor
Digoxin
Cardiac glycoside, inhibits
myocardial Na+-K+ ATPase
(competitive inh. of K+), causes↑
intracell. Na+, inhibiting exchange
of Na+ (in) for Ca++ (out), so ↑
intracellular Ca++ (positive
inotropism) Slows SA and AV nodal
conduction.
Digitoxin
Diltiazem
Dipyridamole
Treat CHF,
Anti-arrhythmic
(for supraventricular
tachyarrhythmias)
Limited therapeutic
index.
N/V, visual disturbances, various arrhythmias.
Renal disease ↓’s clearance, may lead to toxic
buildup. Amiodarone, quinidine and verapamil
↓renal clearance of digoxin. Cholestyramine
↓’s bioavailability. Hypokalemia ↑’s likelihood
of toxicity (beware diuretics!). Hypoxia also ↑’s
toxicity. Elderly more sensitive!
Same as digoxin, except: 90-100% GI absorption; Hepatic metabolism, renal excretion.; t½ = 4-6 days
L-type Ca++-channel blocker;
A DOC for prophylaxis
See others
of variant angina
moderate↓in cardiac contraction,
slowed conduction @ SA and AV
nodes, moderate vasodilation (art.)
Phosphodiesterase (PDE)
Prevents clot formation;
Therarpy for MI, angina;
inhibitor; ↑cAMP, inhibits
platelet activation, promotes arterial
Variable GI absorption.
Excreted unchanged by
kidney.
t½ = 36-48h
Treat toxicity w/
phenytoin, lidocaine, K+,
Fab fragments to digoxin.
Intermediate cardiac &
vascular effects (compare
other Ca++ blockers.)
Adjunct for
anticoagulation therapy.
relaxation
β1 & β2 agonist,↑force of
myocardial contraction.
ACE inhibitor; prodrug,
metabolized to active enalaprilat.
Na+ channel blocker (strongest!)
Treat cardiogenic shock,
CHF
Same as captopril…
Long term use can cause downregulation &
desensitization of receptors. Give i.v. only.
Racemic mixture, is 1
agonist & antagonist, too.
Class IC
anti-arrhythmic drug –
a DOC for prophylaxis
of A-fib.
Significantly widens QRS
Furosemide
Loop diuretic (sulfonamide):
inhibits Na/K/2Cl transporter in
TALH cells, ↑ GFR
Treat HTN
Relatively high incidence of proarrhythmia –
contraindicated with structural heart disease
(ischemic damage or hypertrophy). Also avoid
with depressed ventricular fxn (↓ejection
fraction).
Alkalosis, hypokalemia (beware
digoxin/digitoxin!), hypovolemia, dehydration,
shock. CN VIII damage (deafness).
Gemfibrozil
Guanethidine
Fibrate – see clofibrate
Sympatholytic, inhibits Ca++dependent release of NE in
periphery
Arterial selective vasodilator;
↑’s smooth muscle levels of cGMP;
result is ↓PVR,↓cardiac
afterload, ↑ cardiac output.
Thiazide diuretic, ↓s plasma
volume and↓s PVR long-term.
Treat HTN
Hypotension, bradycardia.
Not widely prescribed –
“historical interest”.
Treat CHF and HTN
Lupus-like symptoms, headache, reflex
tachycardia (blocked by co-administered βblockers), water and salt retention (co-administer
diuretics).
Hypokalemia, may cause ventricular
arrhythmias (not a major impediment to
therapeutic use).
Use is decreasing due to
safer, more effective drugs
(ACE inhibitors and AT-R
antagonists)
Especially effective in
African Americans and
the elderly.
Dobutamine
Enalapril
Flecainide
Hydralazine
Hydrochlorothiazide
Treat HTN, often in
combination w/other
antihypertensives.
In CHF, even before
diuresis, eases breathing,
↓pulmonary resistance
and pulmonary artery BP.
Inamrinone
(previously amrinone)
PDE inhibitor (cardiac/vascular
isoform); effectively ↑’s cAMP
levels,↑cardiac output,↓PVR;
Isoproterenol
β1 & β2 agonist
(more affinity than Epi or NE)
Organic nitrate, slow onset,
medium duration↓’s preload on
heart due to vasodilation of large
veins.
1, β1 and β2 blocker
Na+ channel blocker
(weakest, safest).
Competitive angiotensin II (AT1)
receptor antagonist; inhibits
vasoconstriction, aldosterone
release and hypertrophic growth.
HMG-CoA reductase inhibitor
Selective β1 blocker
PDE inhibitor
Primarily an arterial vasodilator
by↑cGMP, stim. outward K+
channels, hyperpolarizes vascular
sm. muscle.
β-blocker
Decreases fatty acid mobilization
from adipose to liver.↓plasma
TG,↓VLDL and LDL and ↑
HDL.
L-type Ca++-channel blocker;
Strong arteriolar vasodilation is
main effect.
Isosorbide dinitrate
Labetalol
Lidocaine
Losartan
Lovastatin
Metoprolol
Milrinone
Minoxidil
Nadolol
Nicotinic acid (niacin)
Nifedipine
Nitroglycerin
Nitroprusside
(sodium nitroprusside)
Organic nitrate, ↓’s preload on
heart due to vasodilation of large
veins.
Balanced vasodilator; ↑’s smooth
muscle levels of cGMP; result is
↓ cardiac preload and afterload,
↑ cardiac output, ↓ pulmonary
congestion.
Short-term treatment of
CHF. (Positive inotropic
agent).
Potential to induce arrhythmias,
thrombocytopenia, nausea/vomiting.
Reserved for patients who don’t respond to
vasodilators or other positive inotropic agents.
NOT effective in reducing
morbidity and mortality
a/w heart failure
VERY low affinity for 
receptors (“pure β-ag”)
2nd choice for angina
prophylaxis
Treat HTN
Class IB
anti-arrhythmic drug.
1st line treatment of CHF
and HTN
Headache, hypotension, reflex tachycardia.
Nitrate tolerance with continuous exposure.
Don’t combine w/sildenafil (Viagra®)!
Some risk of proarrhythmia
(less than other Na+ blockers).
Fewer side effects than ACE inhibitors.
See atorvastatin
Like propranolol, but without β2-mediated side effects.
Like inamrinone, but with less toxicity.
Reserved for treatment of Headache, hypotension, reflex tachycardia
(counter w/β-blockers), edema (counter
moderate to severe
HTN.
w/diuretics). Reflexes may blunt effect of ↓
PVR.
Treat HTN, angina
This one not really covered…
Treat hyperlipidemia;
Glucose intolerance (avoid high doses w/type 2
Most effective at raising
DM), hepatotoxicity, hyperuricemia:
HDL levels.
contraindicated w/severe liver disease or gout.
A DOC for prophylaxis
of variant angina
Sublingual = DOC to
terminate anginal
episode (stable or
variant)
Patch = 2nd choide for
angina prophylaxis
Acute management of
CHF.
Useful in hypertensive
emergencies (diastolic BP
> 120 w/ end-organ
Contraindicated if already significant
hypotension; Don’t mix w/other vasodilators.
Reflex tachycardia (serious), headache, edema.
Use extended release formulation.
Headache, hypotension, reflex tachycardia.
Nitrate tolerance with continuous exposure (i.e.,
with patch).
Minimal effect on ECG.
Parenteral use only.
Diuretics not required.
Also causes hair growth
(marketed as Rogaine®)
Strongest vascular
effects of the Ca++
blockers (w/amlodipine).
Don’t combine w/sildenafil (Viagra®)!
Translingual spray or
sublingual tab = rapid
onset, short DOA;
Patch = slow onset, long
DOA
Hypotension, risk of cyanide poisoning w/high
concentrations (it is metabolized to cyanide).
Unstable in solution, ultrashort DOA
damage).
Phenylephrine
Prototype 1 agonist, causes
vasoconstriction
Pindolol
β-blocker with intrinsic
sympathomimetic activity (ISA)
(partial agonist)
Selective 1 antagonist
(competitive),↓TPR & venous
return
Non-selective β-blocker (β1 & β2);
↓’s HR and force of contraction,
so ↓’s O2 demand of heart.
Slows conduction @ AV node.
Prazosin
Propranolol
Quinidine
Blocks Na+ and delayed rectifying
K+ channels. Slows conduction
through ventricles and prolongs
ventricular action potential.
Reserpine
Sympatholytic, depletes NE from
nerve endings in CNS & periphery.
K+ channel blocker; also blocks
β1 and β2- receptors.
Sotalol
Streptokinase
Sulfinpyrazone
Verapamil
Hemorrhage control,
treatment of
hypotension.
Treat HTN
Treat HTN
DOC for prophylaxis of
stable angina and
ischemia relief during
acute coronary
syndromes; also for
HTN. Class II antiarrhythmic drug (DOC
for ventricle rate
control w/A-fib).
Class IA
anti-arrhythmic drug.
Treat HTN
Class III (and II) antiarrhythmic drug. DOC
for prophylaxis of Afib.
Binds, activates plasminogen
Clot buster for acute MI,
DVT, multiple PE
(without cleavage)→fibrinolysis.
Uricosuric agent: why is it on the cardiovascular drug list???
A DOC for prophylaxis
L-type Ca++-channel blocker;
Strong inhibition of cardiac
of variant angina.
contractility and conduction
Class IV antiacross SA and AV nodes.
arrhythmic drug.
DOC for ventricular
rate control in A-fib.
Masks hypoglycemic emergency (prevents
tachycardia) in diabetics, exacerbates AV node
block.
Renal reflex may → fluid retention, so give
diuretic too. Orthostatic hypotension and 1st
dose syncope.
Contraindicated (due to β2 block) in patients with
COPD (asthma) or peripheral vascular
disease.
Also masks hypoglycemic emergency (prevents
tachycardia) in diabetics, exacerbates AV node
block (due to β1-block). “Withdrawal
syndrome” possible, →tachycardia… so↓dose
gradually.
Risk of drug-induced arrhythmias (torsades de
pointe), cinchonism (tinnitus, visual disturbances
and anticholinergic effects), negative inotropic
effect.
↑digoxin levels and ↓elimination of same –
can be life-threatening!
Hypotension (↓PVR and CO), insomnia,
sedation, depression
Significant risk of drug-induced arrhythmias
(torsades de pointe) – incidence 2-4%.
Beware β2 effects with asthma, etc.
Could aggravate CHF (β1-block, negative
inotropism).
Bleeding!
Don’t combine w/other drugs that ↓cardiac fxn!
(β-blockers, digoxin). Avoid w/CHF, SA or AV
node block, or hypotension. Side effects include
hypotension, bradycardia, AV node block.
Less potent than Epi or
NE, but orally active and
longer t½
Blocking effect
predominates over ISA as
endog. NE is released.
↓BP does NOT cause
reflex tachycardia.
A DOC for
supraventricular
tachyarrhythmias (A-fib.),
but secondary choice for
V-tach.
Widens QRS complex
(Na+ block) and lengthens
Q-T interval (K+ block)
Not widely prescribed –
“historical interest”.
Prolongs Q-T interval.
Good for patients
w/ischemic heart disease
due to β-block.
Aprotinin may be used as
antidote for excess bleed.
Strongest cardiac effects
of the Ca++ blockers.
Prolongs P-R interval.