INTRODUCTION
Antihypertensive drugs are medications used to lower high blood pressure
(hypertension) and keep it within a healthy, normal range.
• High blood pressure, if left untreated, can damage the heart, kidneys, brain,
and blood vessels over time.
• These drugs work through different mechanisms: some relax blood vessels,
some remove excess fluid from the body, and some block hormones that raise
blood pressure.
• The main classes include Diuretics, Calcium Channel Blockers (CCBs),
Angiotensin II Receptor Blockers (ARBs), ACE Inhibitors, and Beta-Blockers.
• Today's lecture will focus on two important classes: Calcium Channel Blockers
(CCBs) and Angiotensin II Receptor Blockers (ARBs).
Learning Objectives
At the end of this presentation, students should be able to:
• Define Calcium Channel Blockers (CCBs)
• Explain the mechanism of action of CCBs
• State the indications, examples, adverse effects, contraindications, and nursing
responsibilities of CCBs
• Define Angiotensin II Receptor Blockers (ARBs)
• Explain the mechanism of action of ARBs
• Discuss the indications, adverse effects, contraindications, and nursing
responsibilities of ARBs
CALCIUM CHANNEL BLOCKERS (CCBs)
Definition
Calcium Channel Blockers (CCBs) are antihypertensive drugs that block the entry
of calcium ions into the smooth muscle cells of blood vessels and the heart. This
causes the muscles to relax, widening the blood vessels and lowering blood
pressure.
CLASSIFICATION OF CALCIUM CHANNEL BLOCKERS
A. Dihydropyridines (Mainly act on blood vessels)
Examples:
* Amlodipine
* Nifedipine
* Felodipine
* Nicardipine
* Isradipine
Uses:
* Hypertension
* Angina
* Vasospastic angina
B. Non-Dihydropyridines (Act on the heart and blood vessels)
Examples:
Phenylalkylamine
* Verapamil
Benzothiazepine
* Diltiazem
Uses:
* Hypertension
* Supraventricular arrhythmias
* Angina
MECHANISM OF ACTION
Calcium channel blockers:
• Normally, calcium ions enter smooth muscle and cardiac cells and trigger the muscle to
contract.
• CCBs block the entry of calcium into these cells.
• With less calcium available, the muscle fibers relax instead of contracting.
• Blood vessels widen (vasodilation), blood pressure falls, and the heart's workload is reduced.
PHARMACOKINETICS
Absorption
* Well absorbed orally.
* First-pass metabolism occurs in the liver.
Distribution
* Widely distributed.
* Highly protein bound.
Metabolism
* Mainly metabolized in the liver by CYP3A4 enzymes.
Excretion
* Eliminated through urine and feces.
Examples
Amlodipine
* Onset: 6–12 hours
* Duration: about 24–48 hours
Nifedipine
* Rapid onset
* Duration: 6–12 hours
Verapamil
* Duration: 6–8 hours
INDICATIONS
Calcium channel blockers are indicated for:
* Hypertension
* Stable angina
* Vasospastic (Prinzmetal) angina
* Supraventricular tachycardia
* Atrial fibrillation (Verapamil and Diltiazem)
* Hypertrophic cardiomyopathy
EXAMPLES AND DOSAGE
(Dose depends on patient’s condition and physician’s prescription.)
Amlodipine
* 5–10 mg once daily
Nifedipine (Extended Release)
* 30–90 mg once daily
Verapamil
* 80–120 mg three times daily
Diltiazem
* 120–360 mg daily
Adverse Effects
• Peripheral / ankle edema
• Headache and facial flushing
• Dizziness and hypotension
• Reflex tachycardia (DHPs)
• Bradycardia and AV block (non-DHPs)
• Constipation (especially verapamil)
• Gingival hyperplasia (gum overgrowth)
CONTRAINDICATIONS
• Severe hypotension
• Heart failure with reduced ejection fraction
• Severe aortic stenosis
• AV block (for non-dihydropyridines)
• Known hypersensitivity to the drug
Nursing Responsibilities — CCBs
• Assess: Check baseline blood pressure and heart rate before administration. Hold
the dose and notify the physician if systolic BP is below 90 mmHg or heart rate is
below 60 bpm.
• Monitor: Watch for edema, dizziness, and signs of hypotension throughout
therapy.
• Educate: Teach patients to avoid grapefruit juice (it alters drug metabolism) and to
rise slowly from sitting or lying to prevent orthostatic hypotension.
• Safety: Never stop the drug abruptly — this can cause rebound hypertension.
Encourage good oral hygiene to prevent gum overgrowth.
DRUG INTERACTIONS
* Beta-blockers increase risk of bradycardia.
* Digoxin increases risk of heart block.
* Grapefruit juice increases blood concentration.
Angiotensin II Receptor Blockers
Definition
Angiotensin II Receptor Blockers (ARBs) are a class of antihypertensive drugs that lower blood
pressure by selectively blocking the action of Angiotensin II at the AT₁ (Angiotensin II Type 1)
receptors. This prevents vasoconstriction and reduces the release of aldosterone, resulting in
vasodilation and decreased blood pressure.
Mechanism of Action
To understand how ARBs work, we need to understand the Renin–Angiotensin–Aldosterone
System (RAAS).
When blood pressure falls, the kidneys release renin.
Renin converts angiotensinogen (produced by the liver) into angiotensin I.
Angiotensin I is converted by Angiotensin-Converting Enzyme (ACE) into Angiotensin II.
Angiotensin II has two major effects:
* It causes vasoconstriction (narrowing of blood vessels), which increases blood pressure.
* It stimulates the adrenal glands to release aldosterone, causing the kidneys to retain sodium
and water, further increasing blood pressure.
ARBs block the AT₁ receptors, preventing angiotensin II from exerting these effects.
MOA
Normally, angiotensin II is produced in the body and binds to AT1 receptors on blood vessels.
• This binding causes blood vessels to constrict and stimulates aldosterone release, which
increases sodium and water retention.
• ARBs block the AT1 receptor directly, preventing angiotensin II from attaching.
• As a result, blood vessels relax, sodium and water retention decreases, and blood pressure
falls.
RAAS FLOWCHART
Decrease in Blood Pressure
↓
Decreased Blood Flow to Kidney
↓
Kidney (Juxtaglomerular Cells)
Releases RENIN
↓
Renin converts
Angiotensinogen (from Liver)
↓
Angiotensin I
↓
Angiotensin-Converting Enzyme (ACE)
(found mainly in the lungs)
↓
Angiotensin II
↓
• Vasoconstriction
• Stimulates Aldosterone secretion
• Sodium and Water retention
• Increased Blood Volume
• Increased Blood Pressure
Classification of Angiotensin II Receptor Blockers
Examples include:
* Losartan
* Valsartan
* Candesartan
* Irbesartan
* Telmisartan
* Olmesartan
* Eprosartan
PHARMACOKINETICS
Absorption
* Well absorbed orally.
* Food has minimal effect on most ARBs.
Distribution
* Highly protein bound.
* Widely distributed throughout body tissues.
Metabolism
* Mainly metabolized in the liver.
* Losartan has an active metabolite.
Excretion
* Eliminated through urine and bile.
Examples
Losartan
* Onset: about 1 hour
* Duration: about 24 hours
Valsartan
* Duration: about 24 hours
Telmisartan
* Long half-life (about 24 hours)
EXAMPLES AND DOSAGE
(Dose depends on the patient’s condition and physician’s prescription.)
* Losartan: 50–100 mg once daily
* Valsartan: 80–320 mg once daily
* Telmisartan: 40–80 mg once daily
* Irbesartan: 150–300 mg once daily
* Candesartan: 8–32 mg once daily
Indications for ARBs
• Hypertension — first-line treatment, effective alone or combined with other
antihypertensive agents.
• Heart Failure — reduces the workload on the heart, especially when ACE
inhibitors are not tolerated.
• Diabetic Nephropathy — protects kidney function in patients with diabetes.
• ACE Inhibitor Intolerance — used as an alternative when patients develop a
persistent dry cough on ACE inhibitors.
ARB Adverse Effects & Contraindications
Adverse Effects
• Dizziness and hypotension
• Hyperkalemia (raised potassium)
• Headache
• Fatigue
• Renal impairment (in some patients)
• Rarely, angioedema
Contraindications
• Pregnancy (can harm the fetus)
• Bilateral renal artery stenosis
• Severe hepatic impairment
• Known hypersensitivity
• Concurrent use with ACE inhibitors (increases risk of hyperkalemia and renal injury)
Nursing Responsibilities — ARBs
• Assess: Check baseline blood pressure and renal function (urea and creatinine)
before starting therapy.
• Monitor: Watch serum potassium levels regularly, as there is a risk of
hyperkalemia.
• Educate: Advise female patients of childbearing age to use reliable contraception,
since ARBs are contraindicated in pregnancy.
• Safety: Instruct the patient to report swelling of the face or lips (angioedema)
immediately, and to rise slowly to prevent dizziness from low blood pressure.
DRUG INTERACTIONS
* Potassium supplements increase hyperkalemia.
* Potassium-sparing diuretics increase hyperkalemia.
* NSAIDs reduce antihypertensive effects.
* Lithium toxicity may increase.
* Other antihypertensive drugs increase hypotension.
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