DRUGS AFFECTING THE CARDIOVASCULAR SYSTEM

DRUGS USED TO TREAT HYPERLIPIDEMIAS

 Atherosclerosis is the leading cause of death in the Western world. Drugs must
prevent the sequelae of atherosclerosis (heart attacks, angina, peripheral arterial
disease, ischemic stroke) and decrease mortality in patients with a history of
cardiovascular disease and hyperlipidemia.
 Although the drugs are generally safe and effective, they can cause problems,
including drug-drug interactions and toxic reactions in skeletal muscle and the liver.
 The strongest risk factors for CVD include elevated low-density lipoprotein
cholesterol (LDL-C or “bad” cholesterol), decreased high-density lipoprotein
cholesterol (HDL-C or “good” cholesterol), high blood pressure, diabetes (type 1 or
2), cigarette smoking, and obesity. 
 Some of these risk factors may be present at young ages, and research has shown
that they should be addressed early.Children and adolescents are becoming
increasingly overweight and obese.
 A recent study reported that the prevalence of overweight 12- to 19-year olds is
15.5%. The childhood obesity epidemic has increased the need for pediatric health
care professionals to become more knowledgeable about the risk factors for CVD
and to begin implementing lifestyle changes in patients.

DRUGS USED TO TREAT HYPERTENSION

 High blood pressure (hypertension) is diagnosed if the blood pressure reading is
equal to or greater than 130/80 mm Hg. A diagnosis of high blood pressure is usually
based on the average of two or more readings taken on separate occasions.
 Blood pressure is grouped according to how high it is. This is called staging. Staging
helps guide treatment.

 Stage 1 hypertension. The top number is between 130 and 139 mm Hg or the bottom
number is between 80 and 89 mm Hg.
  Stage 2 hypertension. The top number is 140 mm Hg or higher or the bottom number is
90 mm Hg or higher.
 Sometimes the bottom blood pressure reading is normal (less than 80 mm Hg) but
the top number is high. This is called isolated systolic hypertension. It's a common
type of high blood pressure in people older than 65.

Treatment

 Eating a heart-healthy diet with less salt

 Getting regular physical activity
 Maintaining a healthy weight or losing weight
 Limiting alcohol
 Not smoking
 Getting 7 to 9 hours of sleep daily

Medications
Medicines used to treat high blood pressure include:
 Water pills (diuretics). 
 These drugs help remove sodium and water from the body. They are often the first
medicines used to treat high blood pressure.
 There are different classes of diuretics, including thiazide, loop and potassium
sparing depending on blood pressure measurements and other health conditions,
such as kidney disease or heart failure.
 Diuretics commonly used to treat blood pressure include chlorthalidone,
hydrochlorothiazide (Microzide) and others.
 A common side effect of diuretics is increased urination. Urinating a lot can reduce
potassium levels. A good balance of potassium is necessary to help the heart beat
correctly.

 Angiotensin-converting enzyme (ACE) inhibitors

 These drugs help relax blood vessels. They block the formation of a natural chemical
that narrows blood vessels.
 Examples include lisinopril (Prinivil, Zestril), benazepril (Lotensin), captopril and
others.

 Angiotensin II receptor blockers (ARBs). 

 These drugs also relax blood vessels. They block the action, not the formation, of a
natural chemical that narrows blood vessels. 
 ARBs include candesartan (Atacand), losartan (Cozaar) and others.
 Calcium channel blockers
 These drugs help relax the muscles of the blood vessels. Some slow heart rate.
 They include amlodipine (Norvasc), diltiazem (Cardizem, Tiazac, others) and others.
  Don't eat or drink grapefruit products when taking calcium channel blockers.
Grapefruit increases blood levels of certain calcium channel blockers, which can be
dangerous.

Other medicines sometimes used to treat high blood pressure

 Alpha blockers

 These medicines reduce nerve signals to blood vessels. They help lower the effects
of natural chemicals that narrow blood vessels.
 Alpha blockers include doxazosin (Cardura), prazosin (Minipress) and others.

 Alpha-beta blockers

 Alpha-beta blockers block nerve signals to blood vessels and slow the heartbeat.
They reduce the amount of blood that must be pumped through the vessels.
 Alpha-beta blockers include carvedilol (Coreg) and labetalol (Trandate).

 Beta blockers
 These medicines reduce the workload on the heart and widen the blood vessels. This
helps the heart beat slower and with less force.
 Beta blockers include atenolol (Tenormin), metoprolol (Lopressor, Toprol-XL,
Kapspargo sprinkle) and others.
 Beta blockers aren't usually recommended as the only medicine prescribed. They
may work best when combined with other blood pressure drugs.

 Aldosterone antagonists

 These drugs may be used to treat resistant hypertension. They block the effect of a
natural chemical that can lead to salt and fluid buildup in the body.
 Examples are spironolactone (Aldactone) and eplerenone (Inspra).

 Renin inhibitors
 Aliskiren (Tekturna) slows the production of renin, an enzyme produced by the
kidneys that starts a chain of chemical steps that increases blood pressure.
 Due to a risk of serious complications, including stroke, taking aliskiren
with ACE inhibitors or ARBs should not be done.

 Vasodilators

 These medicines stop the muscles in the artery walls from tightening. This prevents
the arteries from narrowing. Examples include hydralazine and minoxidil.

 Central-acting agents

 These medicines prevent the brain from telling the nervous system to increase the
heart rate and narrow the blood vessels.
  Examples include clonidine (Catapres, Kapvay), guanfacine (Intuniv) and
methyldopa.

Note: Always take blood pressure medicines as prescribed. Never skip a dose or abruptly stop
taking blood pressure medicines. Suddenly stopping certain ones, such as beta blockers, can
cause a sharp increase in blood pressure called rebound hypertension.

DRUGS USED TO TREAT HEART FAILURE

Table 1
Oral Therapies for the Treatment of Heart Failure
Medication Initial Dose Target Dose* Adverse Effects Contraindications
Angiotensin-Converting Enzyme Inhibitors
Captopril 6.25–25 mg 50 mg TID Hypotension Hypersensitivity
TID SCr/BUN increase Previous
Hyperkalemia angioedema due
Enalapril 2.5 mg BID 20 mg BID Cough to any ACE
Fosinopril 5–10 mg 40 mg daily inhibitor
daily
Lisinopril 2.5–5 mg 40 mg daily
daily
Perindopril 2 mg daily 16 mg daily
Quinapril 5 mg BID 20 mg BID
Ramipril 1.25–2.5 mg 10 mg daily
daily
Trandolapril 1 mg daily 4 mg daily
Angiotensin Receptor Blockers
Medication Initial Dose Target Dose* Adverse Effects Contraindications
Candesartan 4–8 mg daily 32 mg daily Hypotension Hypersensitivity
SCr/BUN increase Concomitant use
Losartan 25–50 mg 150 mg daily
Hyperkalemia with aliskiren in
daily patients with
Valsartan 20–40 mg 160 mg BID diabetes
BID
Beta Blockers
Bisoprolol 1.25 mg daily 10 mg daily
Hypotension Severe
First-degree heart bradycardia
Carvedilol 3.125 mg BID 50 mg BID
block Second- or third-
Carvedilol CR 10 mg daily 80 mg daily Edema degree heart
Dizziness block in the
Metoprolol 12.5–25 mg 200 mg daily
Abdominal absence of a
succinate daily pain/diarrhea pacemaker
Cardiogenic shock
Decompensated
HFrEF
Sick sinus
syndrome
Loop Diuretics
Bumetanide 0.5–1.0 mg 10 mg daily Hypotension/dizziness Hypersensitivity
daily or BID Fluid loss Anuria
Hypokalemia,
Furosemide 20–40 mg 600 mg daily hypocalcemia,
daily or BID hypomagnesemia,
Torsemide 10–20 mg 200 mg daily hyponatremia,
hypochloremia
daily
Hyperuricemia
Ethacrynic acid 25–50 mg 100 mg BID Cramping/diarrhea
daily Nephrotoxicity/
ototoxicity
Thiazide Diuretics Used in Combination With Loop Diuretics
Metolazone 2.5–10 mg NA Hypotension Hypersensitivity
daily + loop Dizziness Anuria
diuretic Gout attacks Hydrochlorothiazi
Hypercalcemia de: CrCl ≤ 10
Hydrochlorothiaz 25–100 mg NA BUN increase mL/min
ide daily or BID +
loop diuretic
Aldosterone Antagonists
CrCl < CrCl CrCl < CrCl Hyperkalemia Spironolactone:
50 > 50 50 > 50 Diarrhea acute renal
Impaired renal insufficiency,
Spironolactone 12.5 12.5 12– 25 function anuria, or
mg –25 25 mg Dizziness significant renal
daily mg mg daily Fatigue dysfunction
or daily daily or Spironolactone: Eplerenone:
Medication Initial Dose Target Dose* Adverse Effects Contraindications
every BID
other
day
Eplerenone 25 25 25 50
mg mg mg mg gynecomastia serum potassium >
every daily daily daily 5.5 mEq/L at
other or initiation, CrCl < 30
ml/min,
day BID
concomitant use of
Vasodilators
Hydralazine 25–50 mg 300 mg daily Hypotension Allergy to nitrates
TID–QID in divided Headache PDE5 inhibitors
doses Dizziness (avanafil,
Asthenia sildenafil,
Isosorbide 20–30 mg 120 mg daily Nausea tadalafil,
dinitrate TID–QID in divided vardenafil)
doses Riociguat
Fixed-dose 37.5 mg 75 mg
combination hydralazine/ hydralazine/
20 mg 40 mg
isosorbide isosorbide
dinitrate TID dinitrate TID
Digoxin
Digoxin 0.125–0.25 0.25 mg daily Arrhythmias Hypersensitivity
mg daily (may be Heart block Ventricular
lower in Nausea/vomiting fibrillation
Diarrhea
patients
Anorexia
older than
Visual changes
70 years of Headache
age or Gynecomastia (long-
patients with term use)
renal Confusion
dysfunction
to maintain
serum
concentratio
n between
0.5–0.9
ng/mL)
I(f) Inhibitor
Ivabradine 5 mg BID 7.5 mg BID Bradycardia Acute
Atrial fibrillation decompensated
Phosphenes (transient HFrEF
enhanced brightness BP < 90/50 mm
in restricted area of Hg
Medication Initial Dose Target Dose* Adverse Effects Contraindications
visual field) Sick sinus
Blurred vision syndrome,
sinoatrial block,
or third-degree
AV block without
functioning
demand
pacemaker
Resting HR < 60
bpm prior to
treatment
Severe hepatic
impairment
Pacemaker
dependence
Concomitant use
with strong
CYP3A4 inhibitors
Angiotensin Receptor-Neprilysin Inhibitor
Sacubitril/ 49 mg/51 mg 97 mg/103 Hypotension Previous
valsartan BID mg BID Hyperkalemia angioedema due
SCr increase to any ACE
Dizziness inhibitor or ARB
Cough Concomitant use
of ACE inhibitors
or use within the
previous 36 hours
Concomitant use
of aliskiren in
diabetic patients