Cardiovascular and Renal Pharmacology: Drug Mechanisms and Side Effects

What is the mechanism of action of calcium channel blockers?

They inhibit the influx of calcium ions into cardiac and smooth muscle cells, leading to decreased contractility and vasodilation.

What do cardiac glycosides do?

They increase the force of heart contractions and slow down the heart rate by inhibiting the sodium-potassium ATPase.

What is the primary action of antianginals?

They relieve angina by decreasing myocardial oxygen demand or increasing oxygen supply.

Name a major adverse effect of verapamil.

Constipation

What is a common adverse effect of digoxin?

Nausea and vomiting

What class of drug is amlodipine?

Calcium channel blocker

What is the mechanism of action of angiotensin II receptor blockers (ARBs)?

They block the action of angiotensin II, leading to vasodilation and decreased blood pressure.

What is the primary use of diuretics?

To promote the excretion of water and electrolytes, reducing blood volume and blood pressure.

What class does lisinopril belong to?

Angiotensin converting enzyme (ACE) inhibitor

What is a major adverse effect of furosemide?

Electrolyte imbalances, particularly hypokalemia

What is the mechanism of action of adrenergic drugs?

They stimulate adrenergic receptors, leading to effects such as increased heart rate and vasoconstriction.

What drug class does clopidogrel belong to?

Antiplatelet agent

What are the main classes of antihypertensive drugs covered in Module 2?

Diuretics, antianginal drugs, heart failure drugs, coagulation modifiers, antilipidemic drugs, adrenergic drugs, vasodilators, SA node modulators, and Angiotensin Receptor-Neprilysin Inhibitors (ARNi).

What is the formula for blood pressure?

Blood pressure = cardiac output × systemic vascular resistance.

What do ACE inhibitors (ACEIs) prevent?

They prevent the conversion of angiotensin I into angiotensin II.

How do ACE inhibitors lower blood pressure?

By decreasing the concentration of angiotensin II, leading to vasodilation and improved renal function.

What is a major side effect of ACE inhibitors?

Cough, hypotension, and angioedema (rare but serious).

What do Angiotensin Receptor Blockers (ARBs) do?

They block the action of angiotensin II, preventing blood vessel constriction.

Name an example of an Angiotensin Receptor Blocker.

Irbesartan (Avapro), Losartan (Cozaar), or Valsartan (Diovan).

What are the common side effects of ARBs?

Dizziness, headache, fatigue, diarrhea, and high potassium levels.

What is the mechanism of action of beta-blockers?

They bind to beta-adrenergic receptors, preventing adrenaline and noradrenaline from activating them.

What effects do beta-blockers have on the heart?

They decrease heart rate, force of contractions, and blood pressure.

What are the two main types of beta-adrenergic receptors?

β1-ARs (primarily in the heart) and β2-ARs (primarily in the lungs and blood vessels).

What is a common side effect of beta-blockers?

Bradycardia, hypotension, dizziness, fatigue, and cold hands and feet.

What do calcium channel blockers (CCBs) inhibit?

The influx of calcium ions into cells in the heart and blood vessels.

How do CCBs lower blood pressure?

By relaxing blood vessels and reducing heart rate.

What are the three classes of calcium channel blockers?

Dihydropyridines, phenylalkylamines, and benzothiazepines.

What is a common side effect of CCBs?

Constipation, peripheral edema, and slow heart rate.

What do alpha-1 adrenergic receptor antagonists treat?

High blood pressure and benign prostatic hyperplasia (BPH).

Name an example of a selective alpha-1 antagonist.

Doxazosin (Cardura), prazosin (Minipress), or tamsulosin (Flomax).

What are common side effects of selective alpha-1 antagonists?

Hypotension, orthostatic hypotension, and sexual dysfunction.

What is a selective aldosterone receptor antagonist (SARA)?

A drug that blocks the aldosterone receptor, used to treat hypertension and heart failure.

Name a commonly known selective aldosterone blocker.

Eplerenone (Inspra).

What are common side effects of eplerenone?

Dizziness, insomnia, headaches, coughing, and nausea/vomiting.

What are sinoatrial (SA) node modulators?

Factors that change the activity of the SA node, controlling heart rate and rhythm.

What is an example of an SA node modulator?

Ivabradine (Lancora).

What major side effects can SA node modulators cause?

Bradycardia and hypotension.

What is the role of bradykinin in relation to ACE inhibitors?

ACE inhibitors increase bradykinin levels, contributing to vasodilation.

How do CCBs alleviate angina?

By improving blood flow to the heart and reducing oxygen deprivation.

What is the 'first-dose effect' associated with alpha blockers?

A significant drop in blood pressure after the first dose, leading to fainting or dizziness.

What are ACEIs and ARBs used for?

They support cardiac function by decreasing afterload and reducing the work of the failing heart.

What is the mechanism of action of digoxin?

Digoxin increases myocardial force (positive inotropic effect) and augments cholinergic stimulation from the parasympathetic nervous system.

What are the side effects of digoxin?

Bradycardia, hypokalemia, cardiac arrhythmias, and cardiac arrest can occur with toxicity.

What is the purpose of vasodilators like hydralazine/isosorbide dinitrate?

They relax blood vessels, increasing blood flow and oxygen to the heart while reducing its workload.

What is a significant characteristic of hydralazine/isosorbide dinitrate?

It was the first drug approved specifically for the Black population.

What class of drugs do Angiotensin receptor/Neprilysin inhibitors (ARNIs) belong to?

They are a combination of an angiotensin receptor blocker (ARB) and a Neprilysin inhibitor.

What is the first drug in the ARNI class?

Valsartan/Sacubitril (Entresto).

What does Sacubitril do?

It inhibits neprilysin, leading to increased levels of natriuretic peptides.

What is a black box warning associated with Valsartan/Sacubitril?

It is contraindicated in pregnancy (category D) and in patients with a history of angioedema related to ACE inhibitors or ARBs.

What are the five types of diuretics?

Carbonic anhydrase inhibitors, osmotic diuretics, loop diuretics, thiazide and thiazide-like diuretics, and potassium-sparing diuretics.

How do loop diuretics work?

They reduce sodium chloride reabsorption in the thick ascending limb of the loop of Henle.

What are major side effects of loop diuretics?

Hypokalemia, hyponatremia, hypochloremia, hypomagnesemia, dehydration, orthostatic hypotension, dizziness, and fatigue.

What is an example of a loop diuretic?

Furosemide (Lasix) or bumetanide (Bumex).

What do thiazide diuretics primarily inhibit?

They inhibit the reabsorption of sodium chloride in the distal convoluted tubule.

What is a common thiazide diuretic?

Hydrochlorothiazide (HCTZ).

What are side effects of thiazide diuretics?

Hypokalemia, hyponatremia, metabolic alkalosis, hypercalcemia, hyperglycemia, and hyperuricemia.

How do potassium-sparing diuretics work?

They prevent the kidneys from excreting potassium while promoting sodium excretion.

What is an example of a potassium-sparing diuretic?

Spironolactone (Aldactone).

What are the side effects of potassium-sparing diuretics?

Hyperkalemia, which can cause palpitations, muscle pain, arrhythmias, muscle weakness, or numbness.

What are nitrates used for?

They relieve chest pain by dilating blood vessels and reducing myocardial oxygen demand.

What is the mechanism of action of nitrates?

They produce nitric oxide (NO), which activates enzymes leading to relaxation of blood vessel smooth muscle.

What are common side effects of nitrates?

Headache, flushing, and hypotension.

What are anticoagulant drugs used for?

They prevent blood clot formation, crucial for preventing strokes and pulmonary embolisms.

What is an example of a low molecular weight heparin?

Enoxaparin (Lovenox).

What do antiplatelet agents do?

They prevent platelets from sticking together, vital in preventing heart attacks and strokes.

What are thrombolytics used for?

They dissolve existing clots and are used in emergencies like acute myocardial infarction or ischemic stroke.

What is a major side effect of coagulation modifier drugs?

Bleeding.

What do statins do?

They lower LDL cholesterol by inhibiting its production in the liver.

What are common side effects of statins?

Muscle pain, liver damage, and digestive issues.

What can interfere with the metabolism of some statins?

Grapefruit.

What is the function of sodium in the body?

Fluid balance and nerve function.

What is the primary function of potassium?

Heart rhythm and muscle contraction.

What is calcium primarily responsible for?

Bone health and blood clotting.