PBL Pharm- Trachte

Question 1

Digoxin

Answer 1

Inhibits Na/K ATPase Positive Inotrope (increases contractility= positive inotrope)

• Inhibits Na/K ATPase
• Increased intracellular Na
• Reduces NCX activity because of high Na levels
• Decreased expulsion of Ca from cell because don’t want MORE Na brought in
• Increased intracellular Ca
• Increased contraction of cardiac sarcomere

NOTE* Ca+ overload can lead to delayed after-depolarizaiton = arrhythmia (why this isn’t first choice!!)

Also a negative chronotrope (decreases SA nodal rate –> HR)

Used in acute CHF management (wehn furosemide and enalapril are not controlling symptoms

Question 2

Metoprolol

Answer 2

Specific B1 blocker

Decrease heart rate and contractility thus decreasing myocardial oxygen demand

Decreases BP

Used for chronic management in CHF

(Contraindicated in acute CHF, need to perserve heart function and complete diuresis first)

Question 3

Propranolol

Answer 3

Non-specific B1 and B2 blocker

Decrease heart rate and contractility thus decreasing myocardial oxygen demand

Decreases BP

Used for chronic management in CHF

(Contraindicated in acute CHF, need to perserve heart function and complete diuresis first)

Question 4

Enalapril

Answer 4

ACE inhibitor

SUprresses RAAS system by inhibiting conversion of angiotensin 1 to angiotensin II

NET EFFECTS:

Decreased aldosterone release - decreased Na+ reabsorption -decreased fluid retention - decreases blood volume and preload

Decreased vasoconstriction - decreased afterload

USE FOR CHRONIC MANAGEMENT OF CHF

Question 5

Nitroglycerine

Answer 5

Converted to NO by aldehyde dehydrogenase on endothelium - binds smooth muscle g-protein coupled receptor - activates guanylyl cylcase - increased cGMP - decrease in intracellular Ca+ concentration - relaxes smooth muscles

Vasodilator of VEINS!

Acute CHF management

Question 6

Isosorbide Dinitrate

Answer 6

Same mechanism as nitroglycerine but longer half life (60-90 minutes)

Question 7

Lisinopril

Answer 7

ACE inhbitor

Question 8

Metoprolol

Answer 8

Specific B1 blocker

Main activity on heart is to decreased heart rate and contractility thus decreasing myocardial oxygen demand

Decreased BP

Used in MI to reduce ischemia

Chronic management of CHF (NOT ACUTE!)

Question 9

Eplerenone

Answer 9

Aldosterone receptor antagonists

Blockes aldosterone action

Net effects:

Decreases Na+ reabsorption in the kidney - decreases blood volume and preload

Question 10

Spirinolactone

Answer 10

Aldosterone receptor antagonists

Blockes aldosterone action

Net effects:

Decreases Na+ reabsorption in the kidney - decreases blood volume and preload

Question 11

Furosemide

Answer 11

Inhibits NKCC2

Decreases Na and Cl reabsorption

Increased Na and H20 excretion

Decreased blood volume

Decreased Preload

Question 12

Ceftriaxone

Answer 12

Binds penicillin binding protein (transpeptidase) and prevents peptidoglycan synthesis

Gram + and - bacteria

Less susceptible to penicillianases

Bactericidal

Question 13

Penicillin G

Answer 13

IV/IM

binds penicillin binding proteins (transpeptidase) and inhibts cross-linking of peptidoglyan

Gram + ONLY

Sensitive to B-lactamases (specifically penicillinases)

Bactericidal

Question 14

Vancomycin

Answer 14

froms H-bonds with D-ala-D-alanine and prevents the incorporation of NAM/NAG peptide subunits into peptidoglycan matrix (inhibits synthesis)

Broad spectrum for Gram + and -

Bactericidal

Question 15

Morphine

Answer 15

Analgesic

Works on mu receptor

Question 16

Nitroglycerin

Answer 16

• forms free radical NO
• Activates guanylyl cyclse
• Increases cGMP
• Dephosphorylation of myosin light chains
• Smooth muscle relaxation
• Vasodilation
• Affects veins more than arteries
• Decreases preload

Question 17

Aspirin

Answer 17

irreversibly inhibits COX1 & COX2

Inhibits TXA2 synthesis

Inhibits platelet aggregation

Question 18

Clopidogrel

Answer 18

• Irreversible ADP receptor antagonist that prevents activation of ADP receptor (lasts the lifetime of the platelet)
• Inactiavtion of ADP receptor prevents more GpIIbIIIa receptors from being exposed
• Decreases plateles adhesion

Question 19

Heparin

Answer 19

Enhances activity of antithrombin III in the degradation of thrombin and factor 10

Since thromin is inhibited fibrinogen is not converted to fibiring to form the clot

Question 20

Eptifibatide

Answer 20

• Fibrinogen analgogue that binds GpIIbIIIa receptor and prevents binding of adhesive glycoproteins such as fibrinogena nd vWF to activated platelets

Question 21

Alteplase (tPA)

Answer 21

• ACtivates plasminogen (preferentially that is bound to fibrin so you don’t get systemic activation)
• Dissolbes existing thrombi

Question 22

Hydrochlorothiazide

Answer 22

Diuretic

Blocks sodium ion transport across the renal epithelium

Blocks Chloride transport as well (via unknown mechanism)

Results in more NaCl and H20 excretetion

Used to treat = Hypertension and CHF

Question 23

Losartan

Answer 23

Angiotensin II Receptor Blocker

Reversibly and non-competitvely binds AT1, thus blocking directly the vasoconstriction of Angiotensin II and secondarily the actions of Aldosterone

***Decrease in systemic vascular resistance without and increase in HR

Used for HYPERTENSION

Question 24

Hyzaar

Answer 24

Combo durg of Losartan and Hydroclororthiazide

Small dose of diuretic greatly increases an ARBs efficacy

Losartan also reduced Potassium loss from HCTZ

Used for HYPERTENSION

Question 25

Amlodipine

Answer 25

Ca+ Channel Blocker Dihydropyridine Main action is on the arteriolar vasculature - vasodilates Blocks Ca+ influx thus decreasing basal contractility of coronary and systemic arteries Decreased coronary resistance and increased O2 delivery to myocardium NOTE\*\* decreased pressure and vasodilation may lead to an increase in caridac stimulation = reflex tachycardia.....can greatly increased myocaridal O2 demand. THUS NOT used for angina

Question 26

Fluticasone/ Salmerterol

Answer 26

Fluticasone - acts on intracellular receptors to alter transcription resulting in: * Decreased inflammatory allergen response by decreasing histamine, eosinophil chemotactic factor, PGs, bradykinins, & others * Also up-regulates B-receptors Salmeterol - B-2 agonist * B2 activation -\> Gs -\> adenylyl cyclase -\> increased cAMP -\> PKA -\> dephosphorylates MLCs -\> BRONCHODILATION USED FOR ASTHMA/ COPD

Question 27

STATINS

Answer 27

Inhibit cholesterol synthesis * HMG-CoA Reductase inhibitors = decreases mevalonic acid a precursor of cholesterol * Decreased de novo synthesis also increases LDL reuptake/clearance

Question 28

Cilstazol

Answer 28

Platelet aggregate inhibitor with vasodilator abilities * Blocks Phosphodiesterase * Increases intracellular cAMP * Decreased platelet activation by ADP, AA, collagen, etc. Used for intermitent claudication

Question 29

Niacin

Answer 29

Lipid-lowering Agent Inhibits lipolysis in adispose tissue, reduces hepatic VLDL synthesis Decreases LDL, and Triglycerides Increases HDL

Question 30

Bile Acid Resins (Cholestyramine Colestipol, Colesevelam)

Answer 30

Lipid-lowering agents Prevents intestinal reabsorption of bile acids Liver must used cholesterol to make more Decreases LDL Slightly increases HDL and Triglycerides

Question 31

Ezetimibe

Answer 31

(Cholesterol Absorbtion Blockers) Prevent cholesterol absorption at small intesting brush border Decrease LDL, no effect on HDL, Triglycerides

Question 32

Gemifbrozil (Fibrates)

Answer 32

Upregualtes lipoprotein lipase Increase TG clearance Activates PRAR-alpha to induce HDL synthesis Decrease LDL, Increase HDL, REALLY Decrease Tri

Question 33

Aliskiren

Answer 33

Direct Renin Inhibitor Binds to S3 binding site, decreases activity of enzyme. Less conversion of angiotensinogen to angiotensin I