This document summarizes several classes of antihypertensive drugs. It discusses diuretics, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, beta blockers, alpha blockers, direct vasodilators, and their mechanisms of action, indications, side effects and monitoring. The document provides tables with examples of drugs within each class and details regarding administration and patient education.
4. β ADRENERGIC BLOCKING DRUGS
CLASSIFICATION
• Nonselective (β1 and β2)
a. Without intrinsic sympathomimetic activity Propranolol, Sotalol,
Timolol.
b. With intrinsic sympathomimetic activity Pindolol
c. With additional α blocking property Labetalol, Carvedilol
• Cardioselective (β1) Metoprolol, Atenolol, Acebutolol, Bisoprolol,
Esmolol, Betaxolol, Celiprolol, Nebivolol
5. Beta blockers, also known as beta-adrenergic blocking agents, are drugs that block
norepinephrine and epinephrine (adrenaline) from binding to beta receptors on
nerves. Norepinephrine and epinephrine are produced by nerves throughout the
body as well as by the adrenal gland. They serve as neuro-transmitters (chemicals
that nerves use to communicate with one another) that may be active locally where
they are produced, or elsewhere in the body, when they are released into the blood.
There are both alpha and beta receptors in the body. There are three types of beta
receptors, and they control several different functions based on their location in the
body.
1. beta-1 (β1) receptors are located in the heart, eye, and kidneys.
2. beta (β2) receptors are found in the lungs, gastrointestinal tract, liver, uterus,
blood vessels, and skeletal muscle.
3. beta (β3) receptors are located in fat cells.
Beta blockers primarily block β1 and β2 receptors and thereby the effects of
norepinephrine and epinephrine. By blocking the effects of norepinephrine and
epinephrine, beta blockers reduce heart rate; reduce blood pressure by dilating blood
vessels; and may constrict air passages by stimulating the muscles that surround the
air passages to contract considered an adverse side effect).
6.
7.
8. BETA-ADRENERGIC BLOCKERS
DRUG NAME nadolol, propranolol, pindolol, sotalol atenolol, metoprolol, carvedilol, nebivolol
CLASS Nonselective β-blockers Selective β-blockers
MECHANISM
OF ACTION
Block β receptors → prevent catecholamines (norepinephrine and epinephrine) from binding and activating them
→ decrease cardiac contractility, decrease conduction velocity through AV node, decrease heart rate, cardiac
output, and blood pressure
INDICATIONS
•Hypertension
•Coronary artery disease; angina pectoris, myocardial infarction
•Arrhythmias
•Heart failure
•Essential tremor
•Glaucoma
•Migraine prophylaxis
ROA
•PO
•IV
•Opth
SIDE
EFFECTS
•Bradycardia
•Hypotension
•Fatigue, Dizziness
•Bronchospasm and dyspnea
•Headache, Depression, Hallucination, Insomnia and nightmares
•Erectile dysfunction, Decreased libido
•Hyperglycemia, Hypertriglyceridemia, Hyperkalemia.
9. CONTRAINDICATIONS
AND CAUTIONS
•Bradycardia, Hypotension
•Decompensated heart failure
•Asthma, COPD
•Diabetes
•Raynaud phenomenon
•Severe hepatic or renal disease
ASSESSMENT AND
MONITORING
•Baseline assessment
• Vital signs
• Orthostatic hypotension
• Frequency and duration of angina attacks
• Weight, lung sounds; presence of edema, dyspnea
•Laboratory test results: renal and hepatic function tests, electrolytes, glucose, lipid panel.
•Monitor - Heart rate, blood pressure, ECG
• Evaluate therapeutic response; e.g., normalized blood pressure, decreased anginal pain,
absence of heart failure symptoms
CLIENT EDUCATION
•Change positions slowly
•Do not abruptly discontinue medication
•Self-monitoring of pulse, blood pressure
•Lifestyle modifications
• Dietary modifications; e.g., low sodium diet
• Weight control and Regular activity as tolerated
• Alcohol and Smoking cessation
•Clients with diabetes: recognize signs of hypoglycemia; e.g., fatigue, hunger and difficulty
concentrating
•Report symptoms such as bradycardia, hypotension, hypertension, dyspnea, edema
10. Calcium Channel Blockers
Calcium influx occurs during the contraction of cardiac and smooth muscle
cells.
Calcium channels types
1. Voltage gated channels
1. L- type: Long lasting channel – cardiac, smooth muscle and neurons
2. T- type: Fast channel – neurons and endocrine cells
3. N- type: neural channel – neurons
2. Receptor operated channels
3. Stretch operated channels
4. Sodium calcium exchange channels
11. CCBs
Block L type Ca++ channels
Decreased frequency of Ca++ channel opening
Decreased Ca current and Ca++ entry into
cardiac and smooth muscle cells
1. Decreased cardiac contractility, heart rate
2. Vascular smooth muscle relaxation
• Benzothiazepines (diltiazem);
• Phenylalkylamines (verapamil);
• Dihydropyridines
o Amlodipine
o Felodipine
o Isradipine
o Nicardipine
o Nifedipine
o Nimodipine
o Nisoldipine
Classification
12.
13.
14. CALCIUM-CHANNEL BLOCKERS
DRUG NAME
Dihydropyridines: nifedipine, amlodipine, nicardipine, felodipine, nimodipine
Non-dihydropyridines: diltiazem, verapamil.
CLASS Calcium Channel Blockers (CCB)
MECHANISM OF
ACTION
•Block the entry of calcium into the cells
•Reduce the contraction of vascular smooth muscle and cardiac muscle
• Dilate arterioles, and reduce blood pressure and peripheral vascular resistance
• Dilate coronary vessels and increase oxygen supply to the heart
• Reduce force of contraction of cardiac muscles and reduce oxygen demand of the
heart
•Reduce the firing and conduction of impulse through the SA and AV nodes in the heart
INDICATIONS
•Cardiac arrhythmia, hypertension, angina pectoris, tocolysis in preterm labor, Raynaud’s
phenomenon, migraine prophylaxis; Nimodipine: subarachnoid hemorrhage
ROA PO, IV
SIDE EFFECTS
•General: headache, dizziness, flushing of the skin, peripheral edema, hypotension
•Dihydropyridines: reflex tachycardia, gingival hyperplasia
•Non-dihydropyridines: bradycardia, constipation and hyperprolactinemia
CONTRAINDICATIONS
AND CAUTIONS
•Pre-existing bradycardia
•Heart block and Heart failure
•Use with caution: hepatic and renal disease
•Interactions: digoxin, grapefruit
15. CALCIUM-CHANNEL BLOCKERS
ASSESSMENT AND
MONITORING
•Vital signs, CBC, sodium, potassium, creatinine, BUN, liver function tests, and
urinalysis, ECG
•For angina: frequency and severity of symptoms
•Monitor for side effects and therapeutic response
CLIENT EDUCATION
•Purpose of medication
•Self-administration
• Take exactly as prescribed, do not stop abruptly
• Swallow whole; do not divide, crush, or chew
• Avoid grapefruit juice and limit caffeine
•Side effects
• Hypotension and reflex tachycardia: change positions slowly
• Peripheral edema: elevate legs
• Constipation: increase fiber and fluids
• Gingival hyperplasia: good dental hygiene
•Lifestyle modifications for cardiovascular health
•Heart rate and blood pressure self-monitoring
•Report persistent side effects, hypotension, bradycardia; seek medical attention
if angina not relieved by rest or medication
18. ACE INHIBITORS
DRUG TABLE
-pril: e.g., lisinopril; captopril; ramipril; enalapril;
enalaprilat
CLASS ACE inhibitors
MECHANISM OF ACTION
Block angiotensin-converting enzyme (ACE), preventing it from converting angiotensin I
to its active form angiotensin II; decrease aldosterone secretion
INDICATIONS
•Hypertension
•Heart failure
•Post-myocardial infarction
ROA
•PO
•IV (enaaprilat)
SIDE EFFECTS
•Headache
•Dizziness
•Fatigue
•Constant, dry, irritating cough
•Angioedema
•Hypotension
•Tachycardia
•Hyperkalemia
CONTRAINDICATIONS
AND CAUTIONS
•Concurrent use of potassium-sparing diuretics
•Hyperkalemia
•Boxed warning: pregnancy
19. ASSESSMENT
AND
MONITORING
CLIENT
EDUCATION
Vital signs, ECG, CBC, urinalysis, sodium, potassium, creatinine,
and BUN, negative pregnancy test
For heart failure: weight, edema, lung sounds, dyspnea
Monitor for side effects; have 1:1000 epinephrine available for
angioedema
Purpose of medication
Side effects
• Change position slowly to avoid orthostatic hypotension
• Avoid potassium supplements, salt substitutes, NSAIDs
• Cough
• Angioedema
Do not stop abruptly
Lifestyle modifications
Blood pressure self-monitoring
22. ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs)
DRUG NAME -sartan: i.e., Telmisartan; valsartan; losartan; candesartan; irbesartan
CLASS Angiotensin II receptor blockers (ARBs)
MECHANISM OF ACTION
Prevent angiotensin II from binding to angiotensin II receptors on blood
vessels and adrenal glands; decrease aldosterone secretion
INDICATIONS
•Hypertension
•Heart failure
ROA PO
SIDE EFFECTS
•Headache
•Dizziness
•Drowsiness
•Angioedema
•Hypotension
•Hypoglycemia
•Hyperkalemia
CONTRAINDICATIONS AND
CAUTIONS
•Boxed warning: pregnancy
•Hypotension
•Hypovolemia
•Hyperkalemia
•Renal or hepatic disease
23. ASSESSMENT
AND
MONITORING
CLIENT
EDUCATION
Vital signs, ECG, CBC, urinalysis, sodium, potassium, creatinine, and BUN,
negative pregnancy test
•For heart failure: weight, edema, lung sounds, dyspnea
•Monitor for side effects; have 1:1000 epinephrine available for angioedema
Purpose of medication
•Side effects
• Change position slowly to avoid orthostatic hypotension
• Avoid potassium supplements, salt substitutes, NSAIDs
• Angioedema
•Do not stop abruptly
•Lifestyle modifications
•Blood pressure self-monitoring
26. DIRECT-ACTING VASODILATORS
DRUG NAME hydralazine, minoxidil, sodium nitroprusside
CLASS Direct-acting vasodilators
MECHANISM OF ACTION
Prevent the increase of intracellular calcium concentration within vascular smooth muscle cells →
vasodilation → reduced total peripheral resistance and blood pressure
INDICATIONS
•Severe refractory hypertension
•Malignant hypertension
•Hypertensive emergencies
ROUTE(S) OF
ADMINISTRATION
•Hydralazine: PO, IV, IM
•Minoxidil: PO
•Sodium nitroprusside: IV
SIDE EFFECTS
•Hypotension
•Dizziness, Headache
•Reflex tachycardia
•Palpitations
•Edema
•Nausea, Vomiting, GI distress
•Minoxidil: pericardial effusion (boxed warning), cardiac tamponade
•Nitroprusside: Cyanide poisoning (boxed warning), hypothyroidism
CONTRAINDICATIONS
AND CAUTIONS
•Cerebrovascular insufficiency
•Peripheral vascular disease, Coronary artery disease, Heart failure, Mitral valve disease
•Pregnancy and breastfeeding
•Septic shock
27. DIRECT-ACTING VASODILATORS
ASSESSMENT AND
MONITORING
•Baseline assessment
Vital signs, ECG, heart and lung sounds, weight, CBC, electrolytes, hepatic and renal function
Hydralazine IV
Frequent vital signs; signs of fluid overload - edema, pulmonary crackles, orthopnea
Nitroprusside IV
Continuous cardiorespiratory monitoring
•Automatic blood pressure monitoring
•Patent IV access
•Emergency equipment and sodium thiosulfate readily available
•Double-check infusion pump settings with a second nurse
•Monitor for extravasation
•Assess for signs of toxicity: altered mental status, agitation, tremor
•For suspected toxicity, stop the infusion and notify the physician immediately; prepare to administer
antidote
CLIENT EDUCATION
•Concurrent use of beta-blocker and diuretic
•Report signs of water retention, shortness of breath, fast heartbeat (reflex tachycardia), chest pain
Hydralazine
Take with meals
•Report side effects: symptoms of lupus-like syndrome: muscle aches, joint pain, fever
Minoxidil
Take without regard to meals
Can cause reversible increase in hair growth
Nitroprusside
Report burning or stinging at IV site, tinnitus
30. ALPHA-1 BLOCKERS
DRUG NAME prazosin (Minipress), terazosin, doxazosin (Cardura)
CLASS
Peripheral adrenergic antagonists
α1 selective adrenergic blockers
MECHANISM of ACTION
Block peripheral α1-adrenergic receptors → dilates peripheral blood vessels → lowers
peripheral resistance → reduces blood pressure
INDICATIONS
Hypertension
Benign prostate hyperplasia (to decrease urine outflow obstruction)
ROA •PO
SIDE EFFECTS
•Dizziness, headache, and drowsiness
•Anxiety, CNS depression
•Palpitations, orthostatic hypotension, reflex tachycardia, and edema
•Blurred vision
•Dry mouth
•Nausea, diarrhea, and constipation
•Urinary frequency, incontinence, impotence, and priapism
•Doxazosin: arrhythmias and hepatitis
CONTRAINDICATIONS
& CAUTIONS
•Pregnancy and breastfeeding
•Children and elderly clients
•Prazosin and Terazosin: prostate cancer
•Doxazosin: hepatic disease
•Drug interactions: vasodilators, beta blockers, and PDE5 inhibitors
31. ASSESSMENT AND
MONITORING
CLIENT EDUCATION
Assessment - Weight, vital signs, orthostatic blood pressure
Monitoring- Side effects
•Evaluate for the therapeutic response: blood pressure control
Purpose of medication: blood pressure control
•Take with or without food
• Take consistently; do not abruptly stop medication to avoid rebound
hypertension
•Take first dose at bedtime to avoid severe orthostatic hypotension and
syncope
•Continue to make position changes slowly, sit down if dizziness occur
• Contact healthcare provider if hypotension and dizziness persist
•Avoid alcohol
•Check with healthcare provider before taking over-the-counter medications
•Blood pressure self-monitoring technique
• Desired blood pressure; readings that require medical attention
•Lifestyle modifications: maintaining a healthy weight, smoking cessation,
reducing their intake of sodium, increasing physical activity as tolerated
33. ALPHA-2 ADRENERGIC AGONISTS
DRUG NAME Clonidine, Methyldopa
CLASS α2 selective adrenergic agonists
MECHANISM of ACTION
Stimulate presynaptic α2-adrenergic receptors in the CNS → dilates peripheral blood vessels → lowers
peripheral resistance → reduces blood pressure
INDICATIONS
•Hypertension
Clonidine:- Pain management (epidural)
•Attention-deficit / hyperactivity disorder (ADHD)
Methyldopa:-Hypertensive crisis
ROA
•Clonidine: PO, TD, Epidural
•Guanfacine: PO
•Methyldopa: PO, IV
SIDE EFFECTS
•Nausea, vomiting, constipation, dry mouth
•Bradycardia
•Clonidine: rebound hypertension when stopped abruptly, CNS depression
•Methyldopa: granulocytopenia, thrombocytopenia, hemolytic anemia, hepatotoxicity, hepatic necrosis
CONTRAINDICATIONS &
CAUTIONS
•Pregnancy and breastfeeding
•Children and elderly clients
•Cardiovascular, cerebrovascular, or renal disease
•Clonidine: epidural use for obstetrical, postpartum, or perioperative pain management not
recommended (boxed warning)
•Methyldopa: active hepatic disease, MAO inhibitors
Drug interactions:
Clonidine: verapamil, diltiazem, beta-blockers
•Methyldopa: lithium, MAO inhibitors, levodopa
34. ALPHA-2 ADRENERGIC AGONISTS
ASSESSMENT &
MONITORING
Assess:- Vital signs, especially blood pressure and heart rate
•Laboratory test results; renal function
Monitor:- Side effects
•Evaluate therapeutic response: blood pressure within a normal range
CLIENT EDUCATION
•Transdermal patch
• Apply every seven days at a consistent time each week
• Apply to a clean, dry, intact and hairless skin
• Chest or upper arm preferred, Rotate the application site
• Proper disposal of a used patch
•Do not discontinue abruptly
• Notify healthcare provider for symptoms of hypertension: sweating, flushing, nervousness,
severe headache, blurred vision
•Side effects: Nausea, vomiting, constipation
• Management: consuming smaller, more frequent meals; increasing fluids, fiber-rich
foods
• Dry mouth, suggest - Use sugar-free hard candy or gum; frequent sips of water
• Drowsiness
• Avoid alcohol or other CNS depressants
• Avoid activities that require alertness
• Dizziness, bradycardia and hypotension - Make position changes slowly; use caution when
going up and down stairs
•Lifestyle modifications for blood pressure management
• Weight loss, smoking cessation, increased physical activity as tolerated, low sodium diet