Final Exam Review Flashcards
What is the MOA of Thiazide Diuretics?
MOA of Thiazide Diuretics: Inhibit sodium and chloride reabsorption in the thick ascending loop and early distal tubule. This loss of ions increases urine volume.
Can cause hypokalemia.
What is the MOA of ACE Inhibitors? What is the well-known side effect?
ACE Inhibitors –> Drugs causing reduction of cardiac workload
Angiotensin-converting enzyme (ACE) inhibitors: improve symptoms, slow progression of heart failure, and prolong survival. Also used in tx of hypertension.
MOA of ACE Inhibitors:
- block the synthesis of angiotensin II, a potent vasoconstrictor
- reduce aldosterone secretion from adrenal cortex resulting in net water loss
Side Effects of ACE Inhibitors:
- headaches, dizziness, abdominal pain, confusion, renal failure and impotence
- ACE Inhibitors can also cause dry, irritating cough
What is MOA of Loop Diuretics? What are the undesirable side effect of Loop Diuretics?
MOA of Loop Diuretics: inhibit chloride reabsorption in the ascending loop of Henle. They are used in th tx of pulmonary edema because of their potent and rapid action.
Undesirable effects of Loop Diuretics:
hyponatremia (level of sodium in blood too low)
hypokalemia (level of potassium in blood too low)
hypocalcemia (level of calcium in blood too low)
hypomagnesia (level of magnesium in blood too low)
hyperglycemia (high blood glucose)
hyperuricemia (high level of uric acid in blood)
ototoxicity (ear poisoning – drugs that damage the inner ear)
What is the MOA of cardiac glycosides? Example.
What are precautions when taking these drugs?
List their toxicities.
MOA of cardiac glycosides: They inhibit NA+-K+-ATPase. This causes an increase in the level of sodium ions in the myocytes, which leads to a rise in the level of intracellular calcium ions. This occurs because the sodium/calcium exchanger on the plasma membrane depends on a constant inward sodium gradient to pump out calcium. Digoxin decreases sodium concentration in myocardiocytes. Thus the force of myocardial contraction is increased.
Important to note: Cardiac Glycosides have a low therapeutic index which means that the plasma concentration that causes serious toxicity is only slightly higher than the therapeutic dose. Toxicity resulting from cardiac glycosides can be manifested by:
arrhythmias
anorexia
nausea and diarrhea
drowsiness and fatigue
visual disturbances
What is MOA of Class I Antirrhythmics? Give Examples.
MOA Class I Antiarrhythmic: (sodium channel blockers) They block sodium entry into the cell during depolarization. This decreases the rate of rise of Phase 0 of the action potential.
Class IA: useful in tx of atrial and ventricular arrhythmias (all-purpose) –> Procainamide (Pronestyl)
Class IB: used in tx of ventricular arrhythmias (ventricular tachycardia, ventricular fibrillation, and ventricular ectopy) –> Lidocaine (Xylocaine)
What is MOA of Class II antiarrhythmics? Give Example
MOA Class II Antiarrhythmic: (B-adrenoreceptor blockers) are potentially useful in the suppressing the tachyarrhythmias that result from increased sympathetic activity. They stabilize cardiac membrane, slow down conduction through SA and AV nodes, and increase the refractory period.
Propranolol (Inderal) –> most commonly used to tx arrhythmia patients
What is MOA of Class III Antiarrhythmics? Give examples.
MOA of Class III Antiarrhythmics: (K+ channel blockers) they prolong repolarization. Useful in treating intractable ventricular arrhythmias –> Amiodarone: effective in tx and prevention of ventricular fibrillation and ventricular tachycardia.
What is MOA of Class IV antiarrhythmics? Give examples.
MOA of Class IV antiarrhythmics: (Ca++ channel blockers) by slowing the inward calcium current, these drugs slow conduction and prolong the effective refractory period, especially in the AV node. They are the most effective against atrial than ventricular arrhythmias.
- Verapamil
- Diltiazem
What is MOA of organic nitrates in relieving angina? What is the drug of choice for acute coronary spasm? What are the routes of administration?
MOA of organic nitrates for angina:
- they dilate the large myocardial arteries to increase the blood supply of the heart.
- also reduce cardiac preload by reducing venous tone.
- Nitrates –> increase Nitrites –> increase Nitric Oxide –> cGMP
- -> Dephosphorylationof myosin light chain –> vascular smooth muscle relaxation
***drug of choice for acute coronary spasm –> nitroglycerine: useful in tx of all types of angina. Often administered sublingually for rapid onset of action (2 min), but it can be applied transdermally for a longer duration of action…
What is the MOA of Beta Blockers in relieving angina? What are contraindications? These drugs should be tapered off how and why?
MOA of Beta Blockers for angina:
- they decrease oxygen demand of the myocardium by lowering both thte rate and the force of contraction of the heart.
- the cardioselective beta blockers are preferred. they suppress the activation of the heart by blocking B1 receptors.
- they are particularly useful in the tx of patients with MI and have been shown to prolong survival.
Contraindications of Beta Blockers for angina: asthma, diabetes, severe bradycardia, peripheral vascular disease, or COPD.
Cautions of Beta Blockers for angina: do not discontinue Beta Blocker therapy abruptly. The dose should be gradually tapered off over 5-10 days to avoid rebound angina or hypotension.
List group of hypertensive drugs useful in tx of diabetes patients?
ACE Inhibitors do not affect glucose levels, so are useful for tx of diabetes patients with hypertension.
ACE Inhibitors are particularly useful in hypertension that is a result of increased renin levels.
***ACE Inhibitors may not be effective in lowering blood pressure in African American patients.
List group of hypertensive drugs useful in tx of African American patients?
African American patients respond well to treatment of hypertension with calcium blockers.
List group of hypertensive drugs useful in tx of patients with angina?
Beta Blockers are particularly useful for treatment of hypertension with patients with angina or those with migraines.
***Beta Blockers may not be affective in treatment of hypertension in African American patients.
List group of hypertensive drugs useful in tx of pregnant women.
Central acting adrenergic drugs specifically Methyldopa (Aldomet) is used to treat hypertension in pregnant women.
What antihypertensive drug can be used on patients with renal disease?
Central acting adrenergic drugs, specifically Clonidine (Catapress) is an A2 agonist that reduces central sympathetic outflow. It has no direct effect on the kidneys and can be used in patients with renal disease.
List important antiplatelet drugs. What is the MOA of aspirin and clopidegrol.
Antiplatelet drugs inhibit platelet aggregation.
***Aspirin –> MOA: Inhibits platelet aggregation by inhibiting thromboxane A2 synthesis in the platelets, and thus prolongs bleeding time. Reduces the risk of MI, and stroke.
***Clopidegrol (Plavix) –> MOA: Blocks platelet aggregation by irreversibly inhibiting the binding of ADP to its receptor on platelets and, thus inhibit the activation of GP IIb/IIIa receptors required for platelets to bind to fibrinogen; thus it blocks platelet aggregation
***Abciximab (Reopro)–> MOA: Prevent platelet aggregation by blocking and binding of fibrinogen to the glycoprotein IIb/IIIa receptor on the surface of the platelet.
What is the action of heparin? What is the important side effect? What drug is used to treat that side effect?
Heparin is an anticoagulant – they inhibit the development and enlargement of clots.
Heparin and LMWH class –>
MOA of Heparin:
-Interfere with the clotting factor activation in both the intrinsic and extrinsic pathways.
-The prinipal anticoagulant actions of heparin are a result of its binding to antithrombin III with the subsequent rapid inactivation of coagulation factors, especially thrombin and Xa.
- **Side effect of heparin: hemorrhage
- **Protamine is a specific heparin antagonist that can be used to treat heparin-induced hemorrhage.
What is the MOA of oral anticoagulants? Give an example.
MOA of oral anticoagulants: they antagonize Vitamin K, interfere with the synthesis of Vitamin K dependent clotting factors (II, VII, IX, X)
Warferin (Coumadin)
***Administration of Vitamin K can overcome anticoagulant effects of the oral anticoagulants, but the effect takes about 24 hours.
Define thrombolytic drugs. What is the MOA? Give an example.
Thrombolytic drugs are used to lyse already formed clots.
MOA of thrombolytic drugs: activate plasminogen to plasmin. Plasmin digests fibrin forming degradation products.
-Clot dissolution is more likely if therapy is initiated early after clot formation. Clots becomes more difficult to lyse as they age.
- **Streptokinase
- **Tissue plasminogen activator (t-PA)
List the drugs used to treat anemia in end-stage renal failure and megaloblastic anemia?
***Erythropoietin is synthesized in the kidney in response to hypoxia or anemia. It stimulates erythropoiesis. Used to treat end-stage renal failure.
***Epoetin alpha, darbepoetin alpha –> human recombinant erythropoietin effective in the treatment of anemia caused by end-stage renal disease.
***Cyanocobalamin (Vitamin B12) –> used to treat megaloblastic anemia
What is the mechanism of action of HMG-CoA reductase inhibitors? What are their side effects? List important drugs of this group.
MOA of HMG-CoA reductase inhibitors –>
- **first choice of for treatment of patients with hypercholesterolemia.
- They are structural similar to HMG-CoA reductase which is a precursor of cholesterol.
- They inhibit HMG-CoA reductase, the enzyme that controls the rate-limiting step in cholesterol synthesis.
- They decrease cholesterol, LDL, VDL and Triglycerides (TG) and increases HDL.
***Side Effects: Liver fx abnormalities, myopathy, rhabdomyolysis (disintegration of muscle) etc.
Grapefruit juice is prohibited.
Drugs:
Simvastatin (Zocor)
Atrovastatin (Lipitor) **most potent
Rosuvastatin (Crestor) **most potent
What are the mechanisms of actions of Niacin? What are the adverse effects of Niacin?
MOA of Niacin: strongly inhibits lipolysis in adipose tissue; decreases cholesterol, TG, LDL, VLDL, and increases HDL.
***Adverse effects of Niacin: flush and pruritus
What is the MOA of Ezetimibe (Zetia)?
MOA of Ezetimibe --> cholesterol absorption of dietary and biliary cholesterol --> they inhibit intestinal absorption of dietary and biliary cholesterol; they cause: -decrease in LDL, -increase in HDL, -decrease in Triglycerides
Captopril (Capoten)
**Drugs causing reduction of cardiac workload
Captopril (Capoten): ACE Inhibitors
(block the synthesis of angiotensin II, a potent vasoconstrictor;
reduce aldosterone secretion from adrenal cortex resulting in net water loss)
**infrequently causes agranulocytosis or neutropenia
What are the major side effects of ACE Inhibitors?
headache, dizziness, abdominal pain, confusion, renal failure, and impotence… can also cause a dry, irritating cough
Enalapril (Vasotec)
***Drugs causing reduction of cardiac workload
Enalapril (Vasotec): ACE Inhibitors
(block the synthesis of angiotensin II, a potent vasoconstrictor;
reduce aldosterone secretion from adrenal cortex resulting in net water loss)
Losartan (Cozaar)
***Drugs causing reduction of cardiac workload
Losartan (Cozaar): Angiotensin II Receptor Antagonists
(These drugs interfere with the binding of angiotensin II with its receptors. They do not produce cough. Also used in tx of hypertension).
Minoxidil (Loniten)
***Drugs causing reduction of cardiac workload
Minoxidil (Loniten): Direct vasodilator
(directly relaxes arterioles)
***side effect: unwanted hair growth; also marketed for topical tx of male pattern baldness.
Chlorthiazide (Diuril)
***Drugs causing control of excessive fluid: diuretics
Chlorthiazide (Diuril): Thiazide diuretic
(inhibit sodium and chloride reabsorption in the thick ascending loop and early distal tubule. This loss of ions increases urine volume. They can cause hypokalemia - low potassium)
***side effects: hyponatremia, hypokalemia, hyperglycemia, hyperuricemia, hypercalcemia
Furosemide (Lasix)
***Drugs causing control of excessive fluid: Diuretics
Furosemide (Lasix): Loop Diuretic
(inhibit chloride reabsorption in the ascending loop of Henle. They are used in the tx of pulmonary edema because of their potent and rapid action)
***side effects: hyponatremia, hypokalemia, hypocalcemia, hypomagnesia, hyperglycemia, hyperuricemia, ototoxicity
Ethacrynic Acid (Ethacrynate)
**Drugs causing Control of excessive fluid: diuretics
Ethacrynic Acid (Ethacrynate): Loop Diuretics
**most ototoxic
(inhibit chloride reabsorption in the ascending loop of Henle. They are used in the tx of pulmonary edema because of their potent and rapid action)
***side effects: hyponatremia, hypokalemia, hypocalcemia, hypomagnesia, hyperglycemia, hyperuricemia, ototoxicity
Spironolactone (Aldactone)
**Drugs causing control of excessive fluids: Diuretics
Spironolactone (Aldactone): Potassium Sparing Diuretics
**underdesirable effect: hyperkalemia
(they enhance sodium excretion and retain potassium by an action in the distal tubule. They are often used in combination with the other diuretics to help maintain the potassium balance).
Digoxin (Lanoxin)
**Drugs causing enhancement of contractility
Digoxin (Lanoxin): Cardiac glycoside
**cardiac glycosides have a low therapeutic index which means that the plasma concentration that causes serious toxicity is only slightly higher than the therapeutic dose. Toxicity resulting from cardiac glycosides can be manifested by arrythmias; anorexia; nausea; and diarrhea; drowsiness and fatigue; visual disturbances…
Dobutamine (Dobutrex)
***Drugs causing enhancement of contractility
Dobutamine (Dobutrex): Sympathomimetics
is a Beta1 agonist
***In patients with impaired renal function, the use of dopamine (instead of dobutamine) may preserve renal blood flow and, as a result, renal function.
Nitroglycerine
***Drugs to treat angina pectoris
Nitroglycerine: Organic Nitrate
useful in treating all forms of angina. It is the drug of choice for relieving acute coronary spasm. It is often administered sublingually for rapid onset (2 min), but i can be applied transdermally for a longer duration of action.
- **headache and postural hypotension are common side effects
- **drug interaction with Sildenafil (Viagra)
Isosorbide dinitrate (Isordil)
***Drugs to treat angina pectoris
Isosorbide dinitrate (Isordil): organic nitrates
used for prophylaxis of angina not for acute attack
Diltiazem (Cardizem)
***Drugs to treat angina pectoris
Diltiazem (Cardizem): Calcium Blocker
(block calcium influx into the smooth muscle cells of the arteries causing them to dilate)
***side effects: headache, dizziness, hypotension, etc.
Amlodipine (Norvasc)
***Drugs to treat angina pectoris
Amlopdipine (Norvasc): calcium blocker
(they block calcium influx into the smooth muscle cells of the arteries causing them to dilate)
***common side effects: headache, dizziness, hypotension, etc.
Atenolol (Tenormin)
***Drugs used to treat hypertension
Atenolol (Tenormin): beta blocker: B1 antagonist
(prevent sympathetic stimulation of the heart thereby causing decreased heart rate and cardiac output).
Metoprolol (Lopressor)
***Drugs used to treat hypertension
Metoprolol (Lopressor): beta blockers: B1 antagonist
(prevent sympathetic stimulation of the heart thereby causing decreased heart rate and cardiac output)
Methyldopa (Aldomet)
***Drugs to treat hypertension
Methyldopa (Aldomet): Central acting adrenergic drugs: A2 agonist that reduces central sympathetic outflow
- **it has no direct effect on the kidneys and can be used in patients with renal disease
- **used to treat hypertension in pregnant women
Minoxidil (Loniten)
***Drugs used to treat hypertension
Minoxidil (Loniten): direct vasodilators
***side effect: unwanted hair growth; also marketed for topical treatment of mail pattern baldness
Sodium nitroprusside
***Drugs used in hypertensive crisis
Sodium nitroprusside
(given IV; causes prompt vasodilation; capable of reducing BP in all patients regardless of the cause of hypertension)
***poisonous if given orally because of its hydrolysis to cyanide, antidote is sodium thiosulfate
Procainamide (Pronestyl)
***antiarrhythmic drugs
Procainamide (Pronestyl): Class 1a
useful in the treatment of atrial and ventricular arrhythmias – all purpose
Lidocaine (Xylocaine)
***anti-arrhythmic drugs
Lidocaine (Xylocaine): Class 1b
(ventricular fibrillation and ventricular ectopy)
