Pharmacology of Blood Circulation

Question 1

Azilsartan medoxomil (EDARBI); Candesartan (ATACAND); Eprosartan (TEVETEN); Irbesartan (AVAPRO); Losartan (COZAAR); Olmesartan (BENICAR); Telmisartan (MICARDIS); Valsartan (DIOVAN);

Answer 1

Mechanism of action: angiotensin II receptor (AT1) blockers causing vasodilation and reduced aldosterone secretion lowering blood pressure by decreased salt and water retention;
Clinical indications: treats hypertension (antihypertensive);
Side-effects: same as ACE inhibitors (but no increased bradykinin so cough and angioedema risk is low), should not be given with ACE inhibitors as mechanism of action is similar, is also a teratogen and should be discontinued in pregnant individuals.

Question 2

Aliskiren (TEKTURNA)

Answer 2

Mechanism of action: renin inhibitors so acts early on within the RAAS system;
Clinical indications: treats hypertension (antihypertensive);
Side-effects: should not be given with ACE inhibitors or ARBs, diarrhea, cough, angioedema, tetratogenic.

Question 3

Benazepril (LOTENSIN); Captopril (CAPOTEN); Enalapril (VASOTEC); Fosinopril (MONOPRIL); Lisinopril (PRINIVOL, ZESTRIL); Moexipril (UNIVASC); Quinapril (ACCUPRIL); Perindopril (ACEON); Ramipril (ALTACE); Trandolapril (MAVIK);

Answer 3

Mechanism of action: ace inhibitor and breaks down bradykinin leading to vasodilation of arterioles and veins and decrease aldosterone secretion decreasing sodium and water retention reducing preload and after load - so reduce peripheral vascular resistance without reflexively increasing CO, heart rate and contractility;
Clinical indications: treats hypertension first line treatment for those at high risk of CAD, DM, stroke, heart failure MI and chronic kidney disease (antihypertensive);
Side effects: dry cough, rash, fever, altered taste, hypotension and hyperkalemia, angioedema, fetal malformations and alters potassium levels.

Question 4

Amiloride (MIDAMOR); Bumetanide (BUMEX); Chlorthalidone (HYGROTON); Eplerenone (INSPRA); Ethacrynic acid (EDECRIN); Furosemide (LASIX); Hydrochlorothiazide (MICROZIDE); Indapamide (LOZOL); Metolazone (MYKROX, ZAROXOLYN); Spironolactone (ALDACTONE); Triamterene (DYRENIUM); Torsemide (DEMADEX);

Answer 4

Mechanism of action: diuretics;

Clinical indications: treats hypertension (antihypertensive).

Question 5

Acebutolol (SECTRAL); /”Atenolol (TENORMIN)”\; Betaxolol (KERLONE); “Bisoprolol (ZEBETA)”; /Esmolol (BREVIBLOC)\; /”Metoprolol (LORPRESSOR)”\; Nadolol (CARGARD); Nebivolol (BYSTOLIC); Penbutolol (LEVATOL); Pindolol (VISKEN); “Propranolol (INDERAL LA)”; Timolol (BLOCADREN);

Answer 5

Mechanism of action: β - blockers decrease cardiac output and by decreasing sympathetic NS stimulation inhibits renin release, selective beta 1 agonists decrease vascular resistance (by NO release) by acting as a vasodilator;
Clinical indication: treats hypertension (antihypertensive), drugs in quotation marks are also used as anti-anginals those in obliques are also class II antiarrhythmics;
Side effects and contraindications: non-selective beta agonists are contraindicated in asthma patients, may cause bradycardia, hypotension, fatigue, lethargy, insomnia, erectile dysfunction (non-selective beta blockers may also cause disturbances to lipid metabolism increasing TGs) withdrawal side-effects include angina, MI, SD.

Question 6

“Amlodipine (NORVASC)”; Clevidipine (CLEVIPREX); “Felodipine (PLENDIL)”; Isradipine (DYNACIRC); Nicardipine (CARDENE); “Nifedipine (ADALAT)”; Nisoldipine (SULAR);

Answer 6

Mechanism of action: calcium channel blocker (dihydropyridines) blocks movement of calcium through L-type calcium ion channels reducing vascular smooth tone in myocardium and arteries/arterioles;
Clinical indication: treats hypertension (antihypertensive), drugs in quotation marks are also anti-anginal drugs and cna be used in patients with asthma and DM;
Side effects: I degree AV block, constipation, dizziness, fatigue, headache, peripheral edema and gingival hyperplasia.

Question 7

Doxazosin (CARDURA); Prazosin (MINIPRESS); Terazosin (HYTRIN);

Answer 7

Mechanism of action: α - competitive blockers decreasing peripheral resistance lowering ABP; however, salt and water retention occur so reflex tachycardia can occur so slow titration of drug is required at onset of treatment;
Clinical indication: treats hypertension (antihypertensive).

Question 8

Fenoldopam (CORLOPAM);

Answer 8

Mechanism of action: peripheral D1 agonist (rapid vasodilation);
Clinical indication: treats hypertension (antihypertensive).

Question 9

Clonidine (CATAPRES); Methyldopa (ALDOMET);

Answer 9

Mechanism of action: centrally acting adrenergic α2 agonist inhibiting sympathetic vasomotor centres decreasing sympathetic outflow in the periphery;
Clinical indication: treats hypertension (antihypertensive);
Extra information: Clonidine does not effect renal blood flow - can be used if pt has renal dysfunction; Methyldopa has to be converted to methylnorepinephrine and needs multiple daily dosing (but is safe to use in pregnancy);
Side effect: rebound hypertension with abrupt withdrawal, sedation, dry mouth, constipation.

Question 10

Hydralazine (APRESOLINE); Minoxidil (LONITEN);

Answer 10

Mechanism of action: vasodilators (direct acting smooth muscle relaxants) of arteries and arterioles;
Clinical indications: treats hypertension (antihypertensive) hydralazine is safe to use during pregnancy, minoxidil can be sed to treat male pattern baldness;
Extra information: reduce peripheral resistance but stimulate reflex tachycardia and angina pectoris, also increase plasma renin concentration leading to increased sodium retention - therefore must be given with a β - blocker and a diuretic;

Question 11

Nitroprusside (NITROPRESS);

Answer 11

Mechanism of action: nitric oxide vasodilator decreasing peripheral resistance;
Clinical indications: Clinical indications: treats hypertension (antihypertensive).

Question 12

“Verapamil (CALAN)”; “Diltiazem (CARDIZEM)”;

Answer 12

Mechanism of action: calcium channel blockers (nondihydropyridines);
Clinical indications: treats hypertension (anti-hypertensives), drugs in quotation marks are also anti-anginal drugs.

Question 13

Nitroglycerin (NITRO-BID); Isosrbide dinitrate (ISORDIL); Isosorbide mononitrate (IMDUR);

Answer 13

Mechanism of action: nitrates;

Clinical indications: used to treat angina (anti-anginal drugs);

Question 14

Ranolazine (RANEXA)

Answer 14

Mechanism of action: sodium channel blocker;

Clinical indication: used to treat angina (anti-anginal drug).

Question 15

Atorvastatin (LIPITOR); Fluvastatin (LESCOL); Lovastatin (MEVACOR); Pitavastatin (LIVALO); Pravastatin (PRAVACHOL); Rosuvastatin (CRESTOR); Simvastatin (ZOCOR);

Answer 15

Mechanism of action: HMG CoA reductase competitive inhibitors (statins) which is the rate limiting step in cholesterol synthesis this also increases LDL catabolism;
Clinical indications: treats hyperlipidemia is pts who do not have familial hypercholesterolemia as they lack LDL receptors;

Question 16

Niacin (NIASPAN)

Answer 16

Mechanism of action: inhibits lypolysis in adipose tissue –> reducing free fatty acids –> reduced TG production in liver –> reducing VLDL production and LDL-C plasma concentration;
Clinical indications: treats hypercholesterolemia and familial hyperlipidemia.

Question 17

Fenofibrate (TRICOR); Gemfibrozil (LOPID);

Answer 17

Mechanism of action: fibrates decrease triglyceride concentrations by activating PP (peroxisome proliferator) AR binding to the PP response elements increasing lipoprotein lipase (decreasing triglycerides), decreasing apolipoprotein I and II concentration (increasing HDL);
Clinical indications: treats hypertriglyceridemia and type III hyperlipidemia.

Question 18

Ezetimibe (ZETIA)

Answer 18

Mechanism of action: cholesterol (dietary and biliary) absorption inhibitor in the small intestine reducing hepatic cholesterol stores and increasing blood cholesterol clearance;
Clinical indications: used to treat hypercholesterolemia.

Question 19

Colesevelam (WELCHOL); Colestipol (COLESTID); Cholestyramine (QUESTRAN);

Answer 19

Mechanism of action: bile acid sequestrants - anion exchange resins that bind to bile acids –> hepatocytes compensate by converting cholesterol into bile acids –> replace cholesterol by increasing uptake of LDL (via upregulation of cell surface LDL receptors);
Clinical indications: used to treat hyperlipidemia (but less effective in patients who lack functional LDL receptors).

Question 20

Docosahexaenoic and eicosapentaenoic acid (LOVAZA); Icosapent ethyl (VASCEPA);

Answer 20

Mechanism of action: Omega - 3 fatty acids inhibit VLDL and TG synthesis;
Clinical indications: used to treat hyperlipidemia.

Question 21

Disopyramide (NORPACE); Flecanide (TAMBOCOR); Lidocaine (XYLOCAINE); Mexiletine (MEXITIL); Procaineamide (PRONESTYL); Propafenone (RYTHMOL); Quindine (QUINDEX)

Answer 21

Mechanism of action: sodium channel blockers;
Clinical indication: class I antiarrhythmic.

Question 22

Amiodarone (CORDARONE); Dofetilide (TIKOSYN); Dronedarone (MULTAQ); Ibultilide (CORVERT); Sotalol (BETAPACE).

Answer 22

Mechanism of action: potassium ion channel blockers; 
Clinical indications: class III antiarrhytmics;

Question 23

Diltiazem (CARDIZEM); Verapamil (CALAN);

Answer 23

Mechanism of action: calcium ion channel blockers;
Clinical indications: class IV antiarrhythmics;

Question 24

Digoxin

Answer 24

Mechanism of action: inhibits sodium potassium ATPase pump shortening refractory period in atrial and ventricular cardiomyocytes but prolonging refractory period in the AV node;
Clinical indications: used to treat atrial fibrilation and flutter.

Question 25

Adenosine

Answer 25

Mechanism of action: nucleoside;

Clinical indications: when given IV treats acute supraventricular tachycardia.

Question 26

Magnesium sulfate

Answer 26

Mechanism of action: slows rate of SA node impulse formation and prolongs conduction in myocardial tissue;
Clinical indications: when given IV treats arrhythmias.

Question 27

Chlorothiazide (DIURIL); Chlorthalidone (THALITONE); Hydrochlorothiazide (MICROZIDE); Indapamide, Metolazone (ZAROXOLYN)

Answer 27

Mechanism of action: thiazide diuretics;

Clinical indications:

Question 28

Bumtanide, Ethacrynic acid (EDECRIN); Furosemide (LASIX); Torsemide (DEMADEX)

Answer 28

Mechanism of action: loop diuretics;

Clinical indications:

Question 29

Amiloride (MIDAMOR); Eplerenone (INSPRA); Spironolactone (ALDACTONE); Triamterene (DYRENIUM).

Answer 29

Mechanism of action: potassium-sparing diuretics;

Clinical indications:

Question 30

Acetazolamide (DIAMOX)

Answer 30

Mechanism of action: carbonic anhydrase inhibitors;

Clinical indications:

Question 31

Mannitol (OSMITROL); Urea

Answer 31

Mechanism of action: osmotic diuretics;

Clinical indications:

Question 32

In what order should drug classes be prescribed when treating hypertension?

Answer 32

For patients with no previous history of MI (first line of treatment beta blockers) or chronic renal disease (first line of treatment ACE inhibitors) the first line of treatment is to prescribe diuretics. In heart failure if diuretics are not sufficient a beta blocker should be added. The next line of treatment for all cases is to prescribe an ACE inhibitor. For diabetics, those with heart failure and those with chronic renal disease an ARB should be added. For diabetics and thoses at high risk of coronary artery disease.

Question 33

Hydrochlorothiazide, Chlorthalidone, Hydrochlorathiazide, Indapamide, Metolazone

Answer 33

Mechanism of action: thiazide diuretics that increase sodium and water excretion decreasing the extracellular volume and decreasing cardiac output and renal blood flow (but also decreases peripheral resistance [hypotension] so must be given in combination with beta blockers or ACE inhibitors;
Clinical indications: used as first line treatment for hypertension;
Side effects: induce hypokalemia, hyperuricemia and hyperglycemia.

Question 34

Furosemide, Toresemide, Bumetanide, Ethacrynic acid

Answer 34

Mechanism of action: loop diuretic blocking sodium and chloride reabsorption in kidneys (decrease renal vascular resistance and increase renal blood flow;
Clinical indications: Used to treat hypertension (have a hypotensive effect) and can manage symptoms of heart failure and edema;
Side effects: increase sodium in the urine.

Question 35

Amiloride, Triamterene

Answer 35

Mechanism of action: potassium-sparing diuretics (inhibit epithelial sodium transport at the late distal and collecting ducts);
Clinical indications: used to treat hypertension.

Question 36

Eplerenone, Spironolactone

Answer 36

Mechanism of action: potassium-sparing diuretics (aldosterone receptor antagonists);
Clinical indications: treat hypertension and diminish cardiac remodelling following heart failure and reduce potassium loss from other diuretics.

Question 37

Labetalol (TRANDATE); Carvedilol (COREG);

Answer 37

Mechanism of action: mixed alpha and beta receptor antagonist;
Clinical indications: antihypertensive but used mainly to reduce morbidity associated with heart failure.

Question 38

What is considered a hypertensive emergency? If a patient is experiencing a hypertensive emergency how should antihypertensives be administered?

Answer 38

A hypertensive emergency is when systolic BP is > 180 mmHg or diastolic pressure is > 120 mmHg. If a patient experiences a hypertensive emergency antihypertensives such as nitric oxide vasodilators, hydralazine, fenoldapam or calcium channel blockers should be administered intravenously.