DRUGS AFFECTING THE
CARDIOVASCULAR
SYSTEM
• ANTIHYPERTENSIVES
–ACE inhibitors
– vasodilators
– Angiotensin II receptor blocker
– Calcium Channel Blocker
– Sympatholytics
• DIURETICS
–Thiazide
– osmotic
– Loop
– Potassium- Sparing
Brief Review Ana/ Physio
• Determinants of BP
– Cardiac output
– Peripheral vascular resistance
• Baroreceptors (pressure receptors)
specialized cells in the arch of the aorta
• Renin- Angiotensin Aldosterone system
– Compensatory mechanism when blood
pressure within the kidneys fall
Baroreceptors
BLOOD ( VENTRICLES)
AORTA & CAROTID ARTERIES
SUFFICIENT INSUFFICIENT
PRESSURE PRESSURE
BARORECEPTORES
SEND INFO TO BRAIN
Renin- Angiotensin System
Dec BP/Oxygen
Juxtaglomerular cell (kidney)
Renin
Angiotensinogen (liver)
Angiotensin I
ACE
Angiotensin II
A B
A
Intense vasoconstriction
> Increase peripheral resistance
> Increase BP, restore blood flow
Increase – kidney
Decrease renin
B
Adrenal Cortex
aldosterone
nephrons
Na & water retention
increase BP Na rich blood
hypothalamus
osmoreceptors
anti diuretic hormone
further increase blood volume
hypertension
• “ silent killer” • Stepped Care
• When a person’s Approach
blood pressure is 1. Lifestyle
above the normal modification
limits for a 1. Wt reduction
sustained period 2. Dec sodium intake
• TYPES: 3. Moderate alcohol
– Primary intake
– secondary 4. Smoking cessation
5. Increase physical
exercise
2. + drug
Health Teachings
P- ressure (blood) monitor
R- ise slowly
E- ating must be considered
S- tay on medication
S- kipping or abrupt stopping is NO- NO
U- ndesirable responses
R- emind to exercise, decrease alcohol
E- liminate smoking
Angiotensin- Converting
Enzyme Inhibitors (“pril’)
• MOA: blocks the conversion of angiotensin I to
angiotensin II
• Uses: hypertension, MI
• Eg:
– benazepril (Lotesin) moexipril (Univasc)
– captopril (capoten) perindopril (Aceon)
– enalapril maleate (Vasotec) lisinopril
– quinapril (Accupril) ramipril
– fosinopril (Prinivil) trandorapril
• SE: cough, hypotension, HA, dysgeusia (any
perversion of taste perception), insomia, N/V, diarrhea
• AE: reflex tachycardia, chest pain, angina, CHF,
cardiac arrythmias, ulcers, liver & renal problem
,photosensitivity, hyperkalemia, neutropenia,
angioedema
• DI: + probenecid = decrease elimination
+ potassium supplement & diuretics =
hyperkalemia
+ NSAIDS = decrease hypotensive effect
+ Antacids = decrease absorption
+ tetracycline = decrease absorption of tetra
• CI: renal disease, severe Na depletion, CHF,
pregnant and lactating women
Considerations
• Encourage implement lifestyle changes
• Administer on an empty stomach
• Alert if patient is for surgery/ dialysis /
situations which may drop the fluid volume
• Parenteral form only if oral form is not
available
• Adjust dose if with renal failure
• Do not give if BP is below 90/70, monitor BP
esp for 2 hours after the first dose
(hypotension)
• Avoid ambulation (dizziness)
• Report cough / angioedema
• Report dysgeusia if more than 1 month
Angiotensin II Receptor
Antagonist (“sartan”)
• Selectively bind the angiotensin II receptors
in the blood vessels and adrenal cortex.
• Eg: telmisartan ( Micardis)
losartan ( Diovan)
irbesartan ( Aprovel)
candesartan ( Blopress)
valsartan ( Cozaar)
eprosartan ( Teveten)
• USES: when ACE inhibitors are not
tolerated
• SE: HA, diarrhea, dyspepsia, cramps
• AE: angioedema, hyperkalemia
• CI: nephro dysfunction, CHF,
pregnancy
• CONSIDERATIONS:
• +++ ensure female patient not pregnant
• Take without regard to food
Calcium Channel Blockers
• MOA: prevents movement of calcium ions in the
myocardium and vascular smooth muscles.
• Normally: Ca inc muscle contractility, peripheral
resistance and BP
• EG: amlodipine ( Norvasc) nimodipine
(Nimotopp)
diltiazem (Cardizem) felondipine (Plendil)
nicardipine ( Cardene)
nifedipine (Procardia) potent
verapamil ( Calan)
USES: Angina, hypertension, atrial fibrillation
• SE/AD: HA, dizziness, hypotension, syncope,
reflex tachycardia, constipation, AV block,
bradycardia, peripheral edema
• CONSIDERATIONS
– Monitor ECG, CR, BP
– Have “E” cart available with IV administration
– Position to decrease peripheral edema
– Protect drug from light and moisture
– Increase OFI and fiber in the diet
– Avoid overexertion when anginal pain is
relieved
– May give paracetamol if with HA
– Take with meals or milk
– No not chew or crush sustained released
Vasodilators
• MOA: relaxes smooth muscles of blood
vessels esp the arteries; promotes
increase blood flow to the brain & kidney
• EG: hydralazine ( Apresoline)
minoxidil (Loniten)
diazoxide ( Hyperstat) POTENT
nitroprusside ( Nitropress)
USES: severe hypertension, emergencies
• SE/ AE:
– hydralazine: tachycardia (beta blockers),
palpitations, edema (diuretics), HA, dizziness,
GI bleed, lupus like and neurologic symptoms
– minoxidil: similar effects, excess hair growth,
precipitates angina
– Nitroprusside & diazoxide (hyperglycemia) :
similar
• CI: allergy, pregnancy, lactation, cerebral
insufficiency
• DI: + other antihypertensive drugs =
additive effect
CONSIDERATIONS:
D – irectly acts on vascular smooth muscle
I – ncrease renal and cerebral blood flow
L – upus like reaction ( fever, facial rash,
muscle and joint pain, spleenomegaly)
A - ssess peripheral edema
T – ake with food
O – ther side effects (headache, dizziness,
anorexia, Inc. Cardiac, Dec. Blood pressure)
R – eview BP (orthostatic hypotension), blood
glucose,
SYMPATHOLYTIC DRUGS
BETA- BLOCKERS
“OLOL”
• beta-adrenergic blocking
agents,
• beta-adrenergic antagonists,
• beta antagonists.
BETA- ADRENERGIC
BLOCKERS
• MOA: block beta 1 (Cardiac) and / or
beta 2 (lungs) adrenergic receptor
sites; decrease the effects of the
SNS by blocking the release of
catecholamines, thereby decreasing
the HR and BP
Beta-one receptors
• are found in the heart and kidneys.
• When stimulated, they increase
heart rate, AV conduction, &
automaticity.
Beta1-blockers
• reduce heart rate, blood pressure,
myocardial contractility, and
myocardial oxygen consumption.
Beta-two receptors
• mainly in the lungs, gastrointestinal
tract, liver, uterus, vascular smooth
muscle, and skeletal muscle.
• serve to dilate bronchial & vascular
smooth muscle.
Beta2-receptor blockade
• inhibits relaxation of smooth muscle
in blood vessels, bronchi, the
gastrointestinal system, and the
genitourinary tract.
• USES: hypertension, dysrhythmias,
angina pectoris
• AE: rebound hypertension
Main contraindications (ABCDE)
• A-sthma
• B-lock (heart block)
• C-OPD
• D-iabetes Mellitus
• E-lectrolyte Imbalance
• DI:
– + antacids = delayed drug absorption
– + lidocaine = increase plasma level of
lidocaine
– + insulin/ OHA= hypo/ hyperglycemia
– + cardiac glycosides= additive
bradycardia
– + calcium channel blockers= increase
pharmacologic and toxic effects
of both
– + cimetidine= decrease metabolism of
beta blockers
• EG:
– Nonselective Beta Blockers
• Carvedilol ( Coreg)
• Nadolol ( Corgard)
• Propranolol ( Inderal)
• Timolol ( Blocadren)
• Pindolol ( Visken)
– Cadioselective Beta Blockers (B1)
• acebutolol (Sectral)
• atenolol ( Tenormin)
• betaxolol ( Kerlone)
• bisoprolol (Zebeta)
• esmolol (Brevibloc)
• metoprolol (Betaloc, Cardiostat)
• CONSIDERATIONS:
– Lifestyle modification; Compliance (
rebound hypertension)
– Monitor blood sugar with diabetics
– Monitor triglycerides and cholesterol
level (LDL)
– Monitor BP & pulse before and after
– Withhold if pulse is < 60 or SBP < 90
– Monitor any change in the rhythm or
signs of CHF
Blocker
B- radycardia
L- ipidemia increases
- libido decreases
br O - nchospasm
C - HF
- onduction abnormalities
K - onstriction peripheral
vascular
E - xhaustion
- motional depression
R - educes recognition of hypoglycemia
“BLOCKER” outlines undesirable effects of
Beta Blockers.