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3 Pharm Unit > New Drugs test 3 > Flashcards

New Drugs test 3 Flashcards

1
Q

Drug Name

A

Drug Class
Mechanism
Special side effects
Use

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2
Q

esomeprazole

A
  • Proton Pump Inhibitors
  • Irreversible H/K ATPase inhibit
  • rebound hypergastrinemia, CYP enz->increase in warfarin levels & decreased clopidogrel levels,
  • All stomach acid things (GERD, gastric/duodenal ulcer, Zollinger-Ellison, erosive esophagitis, H. Pylori treatment, NSAID ulcers)
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3
Q

lansoprazole

A
  • Proton Pump Inhibitors
  • Irreversible H/K ATPase inhibit
  • rebound hypergastrinemia, CYP enz->increase in warfarin levels & decreased clopidogrel levels,
  • All stomach acid things (GERD, gastric/duodenal ulcer, Zollinger-Ellison, erosive esophagitis, H. Pylori treatment, NSAID ulcers)
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4
Q

omeprazole

A
  • Proton Pump Inhibitors
  • Irreversible H/K ATPase inhibit
  • rebound hypergastrinemia, CYP enz->increase in warfarin levels & decreased clopidogrel levels,
  • All stomach acid things (GERD, gastric/duodenal ulcer, Zollinger-Ellison, erosive esophagitis, H. Pylori treatment, NSAID ulcers)
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5
Q

cimetidine

A
  • H2 receptor antagonists
  • H2 block (from ECL cell)
  • long-term: down testosterone & estradiol (gynecomastia, impotence, galactorrhea), rarely CNS effects parenterally, tolerance in 3 days, rebound
  • Zollinger-Ellison, decrease nocturnal acid secretion (requires 4 wks)
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6
Q

famotidine

A
  • H2 receptor antagonists
  • H2 block (from ECL cell)
  • rarely CNS effects parenterally, tolerance in 3 days, rebound
  • Zollinger-Ellison, decrease nocturnal acid secretion (requires 4 wks)
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7
Q

ranitidine

A
  • H2 receptor antagonists
  • H2 block (from ECL cell)
  • rarely CNS effects parenterally, tolerance in 3 days, rebound
  • Zollinger-Ellison, decrease nocturnal acid secretion (requires 4 wks)
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8
Q

sucralfate

A
  • Misc. (coating)
  • sticky neutral pH coating
  • block absorption of other drugs (but requires acid activation)
  • stress ulcers (sticks to duodenum better)
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9
Q

aluminum hydroxide

A

-delays gastric emptying, slows motility, rebound
-slow-acting acid neut.

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10
Q

calcium carbonate

A

-rebound
-acid neut.

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11
Q

magnesium hydroxide

A

-stim gastric emptying, rebound
-fast-acting acid neut.

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12
Q

magnesium trisilicate

A

-stim gastric emptying, renal stones, rebound
-fast-acting acid neut.

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13
Q

misoprostol

A
  • prostaglandin analog
  • PGE1 analog
  • exacerbate inflam. bowel disease, abortion (uterine contract)
  • Prevent NSAID gastric injury (PPI’s better)
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14
Q

pirenzepine

A
  • M1 antagonists
  • stops signal from vagal nerve (down acid secretion)
  • anticholinergic effects
  • rarely used
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15
Q

bethanechol

A
  • cholinergic ag (prokinetic agent)
  • general constriction of whole intestine
  • anti-ACh effects
  • help urinate, prokinetic motility
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16
Q

erythromycin

A
  • antibiotic (prokinetic agent)
  • motilin agonist
  • fast painful dumps
  • counter an ileus
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17
Q

metoclopramide

A
  • DA antagonist (prokinetic agent)
  • block DA->increased coordinated ACh release
  • Parkinson’s-like, dyskinesia
  • antiemetic, up esophageal sphincter tone (GERD), up GI motility
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18
Q

neostigmine

A
  • AChE inhibitor (prokinetic agent)
  • general constriction of whole intestine
  • ACh effects
  • counter an ileus
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19
Q

tegaserod

A
  • 5-HT4 agonist
  • stim intestinal sensory neurons
  • fatal arrythmias
  • females w/ irritable bowel syndrome
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20
Q

cisapride

A
  • 5-HT4 agonist (prokinetic agent)
  • stim intestinal sensory neurons via 5-HT4 & adenylate cyclase
  • fatal arrythmias
  • GERD
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21
Q

heparin sulfate

A
  • anticoagulant- indirect thrombin inhibitor
  • binds antithrombin up flexibility catalyzes activity (blocks IIA,IXa,Xa)
  • Bleeding, allergy, thrombosis, osteoporosis. NEVER GIVE INTRAMUSC!
  • Acute Tx of DVT and PE. Sometime venous thrombosis and DIC
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22
Q

protamine sulfate

A
  • heparin antagonist
  • cationic peptide binds heparin and inhibits anticoagulant activity
  • allergies (fish)?
  • reverse heavy heparin after surgery
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23
Q

rivaroxaban

A

-anticoagulants
-Factor Xa inhibitor, liver/renal/faecal-biliary clearance
-
-

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24
Q

warfarin

A
  • anticoagulant
  • inh. Vit K metab–> disrupts gamma-carboxylation of II, VII, IX, X, C, S.
  • bleeding, skin necrosis, teratogen, thrombosis
  • prevent blood clots- 3 day warfarinization needs heparin start
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25
Q

menadione

A

-warfarin antidote- vit K
-
-
-

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26
Q

dalteparin

A
  • low molecular weight heparins- indirect thrombin inhibitor
    -enhances antithrombin action on factor X
    -
    -Tx=MI, angina, thrombophlebitis Prevent=clots etc.
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27
Q

enoxaparin

A

-low molecular weight heparins- indirect thrombin inhibiotor
-enhances antithrombin action on factor X
-
-Tx=MI, angina, thrombophlebitis Prevent=clots etc.

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28
Q

fondaparinux

A
  • Xa inhibitor- indirect thrombin inhibitor
  • pentasaccharide inhibits Xa, renal clearance
  • bleeding hemmorhage
  • SubQ for DVT, PE prevention following surg,
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29
Q

argatroban

A

-direct thrombin inhibitors
-inhibits thrombin, hepatic clearance
-
-parenteral in heparin contraindicated individuals

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30
Q

bivalirudin

A

-direct thrombin inhibitors
-inhibits thrombin, hepatic and renal clearance
-
-parenteral in heparin contraindicated individuals

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31
Q

lepirudin

A

-direct thrombin inhibitors
-inhibits thrombin, renal clearance
-
-parenteral in heparin contraindicated individuals

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32
Q

dabigatran

A
  • direct thrombin inhibitors
  • inhibits thrombin, 80% renal clearance
  • GI BLEEDS!
  • Oral
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33
Q

tissue plasminogen activator

A
  • thrombolytics
  • serine protease, plasminogen to plasmin
  • intracranial hemmorhage
  • massive venous thrombosis or PE, acute MI
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34
Q

streptokinase

A
  • thrombolytics
  • binds and activates plasminogen
  • allergic reactions, intracranial hemmorhage
  • massive venous thrombosis or PE, acute MI
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35
Q

urokinase

A
  • thrombolytics
  • promotes plasminogen to plasmin
  • intracranial hemmorhage
  • massive venous thrombosis or PE, acute MI
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36
Q

abciximab

A
  • antiplatelet drugs
  • chimeric monoclonal Ab targets platelet Iib/IIIa
  • bleeding/hemorrhage
  • parenteral, prevent blood clot during vessel procedure
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37
Q

aspirin

A
  • antiplatelet drugs
  • irrev. Acetylates cyclooxygenase inhibits TXA2 syn
  • excessive bleeding (aneurysm in brain)
  • prevention MI, TIA, stroke, restenosis (most common used)
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38
Q

clopidogrel

A
  • antiplatelet drugs
  • thienopyridine deriv–>irrev blocks P2Y receptor–>blocks plat. Agg.
  • less than ticlopidine, less dosing so preferred
  • coronary stent placement- also for patients non tolerant of aspirin
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39
Q

prasugrel

A

-antiplatelet drugs
-thienopyridine deriv–>irrev blocks P2Y receptor–>blocks plat. Agg
-
-prevent stroke MI, coronary intervention (more eff/rapid HYDROLYSIS not CYP)

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40
Q

ticlopidine

A
  • antiplatelet drugs
  • thienopyridine deriv–>irrev blocks P2Y receptor–>blocks plat. Agg
  • nausea, dyspepsia, diarrhea, hemorrhage LEUKOPENIA
  • coronary stent placement- also for patients non tolerant of aspirin
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41
Q

tirofiban

A
  • antiplatelet drugs
  • carboxy fibrinogen terminal targets platelet IIb/IIIa receptor
  • bleeding/hemorrhage
  • parenteral, prevent blood clot during vessel procedure
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42
Q

Chlorothiazide

A
  • Thiazide Diuretics
  • Block Na-Cl symporter in DCT
  • Hypokalemia, increased uric acid, sulfa crossreactivity
  • antihypertensive, heart failure
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43
Q

Chlorthalidone

A
  • Thiazide Diuretics
  • Block Na-Cl symporter in DCT
  • Hypokalemia, increased uric acid, sulfa crossreactivity
  • antihypertensive, heart failure
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44
Q

Hydrochlorothiazide

A
  • Thiazide Diuretics
  • Block Na-Cl symporter in DCT
  • Hypokalemia, increased uric acid, sulfa crossreactivity
  • antihypertensive, heart failure
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45
Q

Furosemide

A
  • Loop diuretic
  • Blocks Na-K-2Cl cotransporter in ascending loop of Henle
  • Hypokalemia, increased uric acid, deafness, sulfa cross reactivity
  • Hypertension, heart failure
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46
Q

Ethacrynic Acid

A
  • Loop diuretic
  • Blocks Na-K-2Cl cotransporter in ascending loop of Henle
  • Hypokalemia, increased uric acid, deafness (especially this drug)
  • Hypertension, heart failure
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47
Q

Bumetanide

A
  • Loop diuretic
  • Blocks Na-K-2Cl cotransporter in ascending loop of Henle
  • Hypokalemia, increased uric acid, deafness, sulfa cross reactivity
  • Hypertension, heart failure
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48
Q

Torsemide

A
  • Loop diuretic
  • Blocks Na-K-2Cl cotransporter in ascending loop of Henle
  • Hypokalemia, increased uric acid, deafness, sulfa cross reactivity
  • Hypertension, heart failure
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49
Q

Spironolactone

A
  • Aldosterone Receptor Blockers (mild diuretic)
  • Block sodium and water reabsorption in collecting ducts
  • Hyperkalemia
  • Resistant hypertension, congestive heart failure with hypertension
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50
Q

Eplerenone

A
  • Aldosterone Receptor Blockers (mild diuretic)
  • Block sodium and water reabsorption in collecting ducts
  • Hyperkalemia
  • Resistant hypertension, congestive heart failure with hypertension
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51
Q

Triamterene

A
  • Potassium sparing diuretic
  • Sodium channel blocker in DCT and collecting duct
  • Hyperkalemia
  • Diuresis, antihypertensive
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52
Q

Amiloride

A
  • Potassium sparing diuretic
  • Sodium channel blocker in DCT and collecting duct
  • Hyperkalemia
  • Diuresis, antihypertensive
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53
Q

Captopril

A
  • ACE inhibitors
  • Block conversion of Ang I to Ang II & bradykinin breakdown
  • Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
  • Mild/moderate hypertension, heart failure (1st line tx), for HF usually combo with B-blocker; prevent progression of heart failure after MI
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54
Q

Enalapril

A
  • ACE inhibitors
  • Block conversion of Ang I to Ang II & bradykinin breakdown
  • Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
  • Mild/moderate hypertension, heart failure (1st line tx), for HF usually combo with B-blocker; prevent progression of heart failure after MI
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55
Q

Lisinopril

A
  • ACE inhibitors
  • Block conversion of Ang I to Ang II & bradykinin breakdown
  • Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
  • Mild/moderate hypertension, heart failure (1st line tx) for HF usually combo with B-blocker; prevent progression of heart failure after MI
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56
Q

Fosinopril

A
  • ACE inhibitors
  • Block conversion of Ang I to Ang II & bradykinin breakdown
  • Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
  • Mild/moderate hypertension, heart failure
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57
Q

Conivaptan

A
  • Vasopressin Receptor Antagonist (intravenous)
  • Blocks V1 (reduces afterload) and V2 receptors (for hyponatremia)
  • Blood pressure can fall abruptly in patients with impared sympathetic nervous system (due to V1), increased osmolality
  • Hyponatremia associated with Syndrome of Inappropriate ADH (SIADH) and heart failure
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58
Q

Tolvaptan

A
  • Vasopressin Receptor Antagonist (oral)
  • Blocks V2 receptor selectively
  • increased plasma osmolality
  • Hyponatremia associated with heart failure, cirrhosis, and SIADH
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59
Q

Losartan

A
  • ARBs
  • Block AT1 receptor, block effects of Ang II
  • Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
  • Hypertension and heart failure
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60
Q

Valsartan

A
  • ARBs
  • Block AT1 receptor, block effects of Ang II
  • Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
  • Hypertension and heart failure
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61
Q

Candesartan

A
  • ARBs
  • Block AT1 receptor, block effects of Ang II
  • Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
  • Hypertension and heart failure
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62
Q

Irbesartan

A
  • ARBs
  • Block AT1 receptor, block effects of Ang II
  • Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs
  • Hypertension and heart failure
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63
Q

Aliskiren

A
  • Renin Inhibitor
  • Competitive inhibitor of renin
  • Hypotension, cough, hyperkalemia
  • Hypertension
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64
Q

Verapamil

A
  • Cardioselective calcium channel Blocker
  • Blocks L-type Calcium channels
  • Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
  • Hypertension and heart failure (negative ionotropic)
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65
Q

Diltiazem

A
  • Cardioselective calcium channel Blocker
  • Blocks L-type Calcium channels
  • Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
  • Hypertension and heart failure (negative ionotropic)
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66
Q

Nifedipine

A
  • Vascular smooth muscle selective calcium channel Blocker
  • Blocks L-type Calcium channels
  • Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
  • Hypertension and heart failure
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67
Q

Nicardipine

A
  • Vascular smooth muscle selective calcium channel Blocker
  • Blocks L-type Calcium channels
  • Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
  • Hypertension and heart failure
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68
Q

Amlodipine

A
  • Vascular smooth muscle selective calcium channel Blocker
  • Blocks L-type Calcium channels
  • Headache, don’t use in heart failure w/ edema (depressive A-V conductance and contractility
  • Hypertension and heart failure
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69
Q

Atenolol

A
  • Beta Blocker
  • Blocks Beta 1 receptors
  • Inability to elevate glucose, nausea, vomiting, confusion, dizziness, fatigue, sleep disorders
  • Hypertension
70
Q

Terazosin

A
  • Alpha blocker
  • Blocks alpha 1 receptors
  • Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence
  • Hypertension (pheochromocytoma)
71
Q

Prazosin

A
  • Alpha blocker
  • Blocks alpha 1 receptors
  • Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence
  • Hypertension (pheochromocytoma)
72
Q

Doxazosin

A
  • Alpha blocker
  • Blocks alpha 1 receptors
  • Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence
  • Hypertension (pheochromocytoma)
73
Q

Labetalol

A
  • Mixed Adrenergic Blocker
  • Blocks beta receptors and alpha 1 receptors
  • (none mentioned)
  • Chronic Hypertension, hypertensive emergencies
74
Q

Carvedilol

A
  • Mixed Adrenergic Blocker
  • Blocks beta receptors and alpha 1 receptors
  • (none mentioned)
  • CHypertension and heart failure
75
Q

Reserpine

A
  • Adrenergic Transmission Blockers
  • Depletes Norepinephrine from adrenergic nerve terminals, blocks its reuptake
  • Postural hypotension, sedation, dry mouth, night mares, sodium and water retention
  • Mild to moderate hypertension
76
Q

Clonidine

A
  • Centrally mediated agents
  • Alpha 2 agonists
  • Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
  • Resistant hypertension
77
Q

Alpha-methyldopa

A
  • Centrally mediated agents
  • Alpha 2 agonists
  • Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
  • Pregnancy Induced hypertension
78
Q

Guanabenz

A
  • Centrally mediated agents
  • Alpha 2 agonists
  • Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
  • Resistant hypertension
79
Q

Hydralazine

A
  • Vasodilators
  • Unknown mechanism (reduces intracell calcium in arterioles
  • Headache, anorexia, nausea, dizziness, sweating, reflex tachcardia (angina and ischemic arrhythmias, Lupus
  • Hypertension
80
Q

Minoxidil

A
  • Vasodilators
  • Activates Potassium channels preferentially In arterioles
  • Fluid retention, reflex tachycardia, abnormal hair growth, pericardial effusion and cadiac tamponande
  • Resistant hypertension
81
Q

Nitroprusside

A
  • Vasodilators
  • Generates nitric oxide, increases cGMP in veins and arteries
  • Rapid decrease in MAP, cyanide accumulation
  • Hypertensive crisis, cause hypotension during surgery
82
Q

Riociguat

A
  • Vasodilators
  • Direct stimulation of guanylyl cyclase, increases cGMP
  • Headaches, dizziness, nausea, diarrhea, hypotension, birth defects
  • Pulmonary hypertension, thromboembolic hypertension
83
Q

Nitroglycerin

A
  • Vasodilators
  • Generates nitric oxide, increases cGMP in veins
  • Headache
  • hypertensive crisis, cause hypotension during surgery
84
Q

Epoprostenol

A
  • Vasodilators
  • Direct vasodilation via cAMP (drug is prostacyclin, counters TXA2)
  • (none mentioned)
  • Pulmonary hypertension (continuous IV admin)
85
Q

Bosentan

A
  • Vasodilators
  • Non selective endothelin receptor blocker
  • Edema, headache, blocks spermatogenesis, resp. tract infection, decreased hematocrit, hepatic effects
  • Pulmonary hypertension
86
Q

Ambrisentan

A
  • Vasodilators
  • ET-A (endothelin A) receptor blocker
  • Edema, headache, blocks spermatogenesis, resp. tract infection, decreased hematocrit, hepatic effects
  • Pulmonary hypertension
87
Q

Rizatriptan

A
  • Serotonin Receptor Agonist
  • Activate prejunctional 5-HT1B/D receptors on sensory nerves, block trigemnovascular system, inhibit release of inflammatory peptides (CGRP) and 5-HT1D receptors promote vasoconstriction in cranial blood vessels
  • Coronary spasm in patients with CV disease. Contraindicated in liver failure.
  • Acute migraines, cluster headaches
88
Q

Sumatriptan

A
  • Serotonin Receptor Agonist
  • Activate prejunctional 5-HT1B/D receptors on sensory nerves, block trigemnovascular system, inhibit release of inflammatory peptides (CGRP) and 5-HT1D receptors promote vasoconstriction in cranial blood vessels
  • Coronary spasm in patients with CV disease. Contraindicated in liver failure.
  • Acute migraines, cluster headaches
89
Q

Zolmitriptan

A
  • Serotonin Receptor agonist (more lipophilic and longer half life than sumatriptan)
  • Activate prejunctional 5-HT1B/D receptors on sensory nerves, block trigemnovascular system, inhibit release of inflammatory peptides (CGRP) and 5-HT1D receptors promote vasoconstriction in cranial blood vessels
  • Coronary spasm in patients with CV disease. Contraindicated in liver failure.
  • Acute migraines, cluster headaches
90
Q

Cyproheptadine

A
  • Serotonin Receptor Antagonist
  • nonselective 5-HT1, 5-HT2 antagonist and H1 receptor antagonist
  • Drowsiness, GI disturbances, prolonged vasospasm
  • Treats symptoms resulting from carcinoid tumors
91
Q

Ketanserin

A
  • Serotonin Receptor Antagonist
  • Selective 5-HT2 (smooth muscle) receptor antagonist (5HT2A>5HT2C), blocks alpha1 adrenergic R too
  • none specified in lecture
  • Lowers arterial pressure in hypertensives (not approved in U.S.)
92
Q

Ergonovine

A
  • Serotonin Receptor Partial Agonist
  • 5HT2 R partial agonist, weak antagonist activity
  • Prolonged vasospasm, GI disturbances
  • Postpartum and postabortal hemorrhage, diagnostic tool for vasospastic angina
93
Q

Ergotamine

A
  • Serotonin Receptor Partial Agonist
  • Partial agonist at 5-HT1/2 R
  • Prolonged vasospasm, GI disturbances
  • Acute migraines, postpartum bleeding
94
Q

Methysergide

A
  • Serotonin Receptor Partial Agonist
  • Antagonist at 5-HT2 R and partial agonist at 5-HT1 R
  • Prolonged vasospasm, GI disturbances, CNS disturbances (hallucination)
  • Symptoms of carcinoid tumors
95
Q

Amlodipine

A
  • Vasoselective Ca channel blocker
  • Block L-type Ca channels (down cytosolic Ca)
  • gingival hyperplasia, arrhythmia, heart failure (but not as bad as the other 3 drugs)
  • Hypertension, chronic for coronary heart disease to vasodilate, prevent vasospasm post-stroke
96
Q

Nicardipine

A
  • Vasoselective Ca channel blocker
  • Block L-type Ca channels (down cytosolic Ca)
  • gingival hyperplasia, arrhythmia, heart failure
  • Hypertension, chronic for coronary heart disease to vasodilate, prevent vasospasm post-stroke
97
Q

Nifedipine

A
  • Vasoselective Ca channel blocker
  • Block L-type Ca channels (down cytosolic Ca)
  • gingival hyperplasia, arrhythmia, heart failure
  • (avoid post-MI!), Hypertension, chronic for coronary heart disease to vasodilate, prevent vasospasm post-stroke
98
Q

Nimodipine

A
  • Vasoselective Ca channel blocker
  • Block L-type Ca channels (down cytosolic Ca)
  • gingival hyperplasia, arrhythmia, heart failure
  • ONLY for post-subarachnoid hemorrhage prevention of vasospasm (cuz more lipophilic)
99
Q

Isosorbide Dinitrate

A

-Nitrovasodilators
-reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg.
-
-angina/CHD

100
Q

Isosorbide Mononitrate

A
  • Nitrovasodilators
  • reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg.
  • minimal first-pass metab!
  • angina/CHD (longer action)
101
Q

Nitroglycerin

A
  • Nitrovasodilators
  • reduce O2 demand, up O2 supply to heart (relaxes large arteries & veins!), inhibit platelet agg.
  • first-pass hepatic metab.
  • vasodilate distal to a stenosis (heart) for angina, CHD
102
Q

Nitroprusside Sodium

A

-Nitrovasodilators
-reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg.
-
-angina/CHD

103
Q

Aspirin

A

-
-Acute coronary syndrome, MI, stroke in combo w/ a P2Y12 inhibitor

104
Q

Clopidogrel

A
  • Miscellaneous vasoactive (anticoagulant)
  • Inhibit Platelet P2Y12 to reduce platelet activation, down ADP activation of GPIIb/IIIa
  • Neutropenia!, genetic variability
  • Acute coronary syndrome, MI, stroke in combo w/ aspirin
105
Q

Prasugrel

A
  • Miscellaneous (anticoagulant)
  • Inhibit Platelet P2Y12 to reduce platelet activation, down ADP activation of GPIIb/IIIa
  • Fewest drug interactions!
  • Acute coronary syndrome, MI, stroke in combo w/ aspirin
106
Q

Ranolazine

A
  • Miscellaneous vasoactive
  • down late Na current (reduce Na, Ca overload in ischemic myocytes), shift ATP production to glycolysis
  • NO negative chrono/ino effects, better exercise tolerance!
  • Angina
107
Q

Ticagrelor

A

-Miscellaneous vasoactive (anticoagulant)
-Inhibit Platelet P2Y12 to reduce platelet activation, down ADP activation of GPIIb/IIIa
-
-Acute coronary syndrome, MI, stroke in combo w/ aspirin

108
Q

cholestyramine

A
  • bile acid sequestrants
  • cationic binds bile acids prevent reabsorption, up LDL rec., up VLDL prod
  • dyspepsia and other GI, Malabsorp vit K, impaired absorption of drugs
  • lower cholesterol levels
109
Q

colesevelam HCl

A
  • bile acid sequestrants
  • cationic binds bile acids prevent reabsorption, up LDL rec., up VLDL prod
  • DOWN HYPERGLYCEMIA. dyspepsia and other GI, Malabsorp vit K, impair absorption of drugs
  • lower cholesterol
110
Q

atorvastatin

A
  • HMG CoA reductase inhibitors- CYP3A4
  • competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
  • liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
  • lower cholesterol and prevent cardiac disease
111
Q

fluvastatin

A
  • HMG CoA reductase inhibitors- CYP2C9
  • competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
  • liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
  • lower cholesterol and prevent cardiac disease
112
Q

lovastatin

A
  • HMG CoA reductase inhibitors- CYP3A4
  • competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
  • liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
  • lower cholesterol and prevent cardiac disease
113
Q

simvastatin

A
  • HMG CoA reductase inhibitors-CYP3A4
  • competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
  • liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
  • lower cholesterol and prevent cardiac disease
114
Q

pravastatin

A
  • HMG CoA reductase inhibitors-CYP3A4
  • competitive inhibit–> decrease chol. Syn, UP LDL rec. –> dec. LDL
  • liver tox, inc. Creat. Kinase–>myopathy/rhabdomyolysis
  • lower cholesterol and prevent cardiac disease
115
Q

clofibrate

A
  • fibric acids
  • PPAR ligand–>UP lipase, apo AI,II–>Clears chylomicrons and VLDL and raises HDL
  • Rashes, GI, arrhythmias (lowers potassium), myopthathy, galls stones
  • treat hypertriglyceridemias (VLDL)
116
Q

fenofibrate

A
  • fibric acids
  • PPAR ligand–>UP lipase, apo AI,II–>Clears chylomicrons and VLDL and raises HDL
  • Rashes, GI, arrhythmias (lowers potassium), myopthathy, galls stones
  • treat hypertriglyceridemias (VLDL)
117
Q

gemfibrozil

A
  • fibric acid (increase blood conc. statins)
  • PPAR ligand–>UP lipase, apo AI,II–>Clears chylomicrons and VLDL and raises HDL
  • Rashes, GI, arrhythmias (lowers potassium), myopthathy, galls stones -treat hypertriglyceridemias (VLDL)
118
Q

ezetimibe

A
  • misc. agents for atherosclerosis (not CYP substrate)
  • inhibits NPC1L1-impairs intestinal absorption of cholesterol
  • Non specific- headache diarrhea etc. (similar to others that lower chol.)
  • lowers cholesterol (not CYP substrate)
119
Q

nicotinic acid (niacin)

A
  • misc. agents for atherosclerosis
  • G prot. Down cAMP, prevents VLDL secretion and subseq. Decreases LDL production
  • cutaneous vasodilat, insulin resistance, hyperuricemia, liver tox.
  • lowers triglycerides>cholesterol
120
Q

quinapril

A
  • ACE inhibitors
  • Block conversion of Ang I to Ang II & bradykinin breakdown
  • Dry cough, hyperkalemia, angioedema, hypotension, rash, fetal renal damage
  • Mild/moderate hypertension, heart failure (1st line tx) for HF usually combo with B-blocker; prevent progression of heart failure after MI
121
Q

candesartan

A
  • ARB (AT1 Receptor antag)
  • competitive antagonist of AT1 recept (supress Ang2 & Ang 3 actions & incr Ang1-7 actions)
  • (none listed)
  • reasonable alternative to ACE inhib for HF (not in combo)
122
Q

losartan

A
  • ARB (AT1 Receptor antag)
  • competitive antagonist of AT1 recept (supress Ang2 & Ang 3 actions & incr Ang1-7 actions)
  • (none listed)
  • reasonable alternative to ACE inhib for HF (not in combo
123
Q

valsartan

A
  • ARB (AT1 Receptor antag)
  • competitive antagonist of AT1 recept (supress Ang2 & Ang 3 actions & incr Ang1-7 actions)
  • (none listed)
  • reasonable alternative to ACE inhib for HF (not in combo
124
Q

Loop diuretics

A
  • ## --preferred diuretic in most HF patients for management of fluid retention (symptomatic benefit); no mortality benefit in HF, should not be used alone in stage C HF patients
125
Q

thiazides

A
  • ## --preferred in hypertensive patients with HF for management of fluid retention (symptomatic benefit) & anti-hypertensive actions; no mortality benefit in HF, should not be used alone in stage C HF patients
126
Q

bisoprolol

A
  • beta R antagonists
  • selective beta-1 R antag (mechanism not fully known but likely impairs SNS-mediated incr in automaticity and hypoK, improves L ventricular structure and fx by preventing remodeling in HF, and improves abnormal Ca handling in HF by preventing hyperphosphorylation of RYR)
  • fluid retention, fatigue, bradycardia (heart block), hypotension; contraindications: bradycardia or reactive airway disease
  • all patients with stage C HF (reduce death)
127
Q

carvedilol

A
  • beta R antagonists
  • alpha-1, beta-1, & beta-2 R antag (mechanism not fully known but likely impairs SNS-mediated incr in automaticity and hypoK, improves L ventricular structure and fx by preventing remodeling in HF, and improves abnormal Ca handling in HF by preventing hyperphosphorylation of RYR)
  • fluid retention, fatigue, bradycardia (heart block), hypotension; contraindications: bradycardia or reactive airway disease
  • all patients with stage C HF (significantly reduce death compared to metoprolol)
128
Q

metoprolol

A
  • beta-1 R antagonists; class II anti-arrhythmic drug
  • selective beta-1 R antag; decr phase 4 slope (reduced automaticity)
  • fluid retention, fatigue, bradycardia (heart block), hypotension, Inability to elevate glucose, nausea, vomiting, confusion, dizziness, fatigue, sleep disorders; contraindications: bradycardia or reactive airway disease
  • all patients with stage CHF (reduce death); atrial arrhythmias, slow AV node conduction, prevent sudden cardiac death post-MI
129
Q

digoxin

A
  • cardiac glycosides
  • Cardiac tissue action: inhib Na/K ATPase (incr intracellular free Ca > incr CO > decr reflex SNS activity & incr renal perfusion); Non-cardiac action: sensitizes cardiac baroreceptors (sense P as higher), incr vagal tone and incr SA node sensitivity to ACh > decr SNS and incr PSNS activity; inhib Na-K ATPase in hidney > reduce reabsorption of Na > incr Na release to distal tubules > decr renin
  • electrical cardiac toxicity (arrhythmias, heart block), therapeutic range (2ng/mL) deleterious effects on heart with long-term use; toxicity treated with anti-digoxin immunotherapy
  • arrhythmias; no longer 1st line therapy for HF; tx patient with HF & atrial fibrillation or persistent, severe symptoms despite ACEI/ARB & B-blocker tx
130
Q

digitoxin

A

-cardiac glycosides
-No other info not specific to digoxin
-
-

131
Q

eplerenone

A

-
-addition to ACEI/ARBs in patient with moderately severe HF (class C/D) or with L ventricular dysfunction after MI

132
Q

spironolactone

A

-
-addition to ACEI/ARBs in patient with moderately severe HF (class C/D) or with L ventricular dysfunction after MI

133
Q

hydralazine

A

-vasodilators
-arterial vasodilator > reduced renal vasc resistance & incr renal blood flow
-
-used as combo with isosorbide dinitrate (incr survival but not as good as enalapril); used in patients who cannot tolerate ACEIs; may provide hemodynamic improvement in advanced HF already treated with ACEI, digoxin, & diuretics

134
Q

isosorbide dinitrate

A

-vasodilators
-short acting, venodilation > incr venous capacitance > reduce preload; also incr coronary artery flow
-
-used as combo with hydralazine

135
Q

nitroglycerine

A

-vasodilators
-sublingual quick acting; IV NO source selective for venous capacitance vessels
-
-L sided HF due to acute myocardial ischemia or when prompt reduct. of ventricular fillling P required

136
Q

dobutamine

A
  • beta agonists
  • Beta agonist; does not activate DA R; improve cardiac performance, facilitate diuresis, & promote clinical stability in SHORT TERM use
  • tolerance limits efficacy with longer term use; tachycardia & arrhythmias
  • systolic dysfuntion & congestion w/ HF; refractory HF (hospitalized frequently for clinical deterioration)
137
Q

dopamine

A
  • beta agonists
  • Beta agonist (low conc > stim cardiac contractility); alpha-agonist (high conc > periph arterial/venous constriction); improve cardiac performance, facilitate diuresis, & promote clinical stability in SHORT TERM use
  • tachycardia (can provoke ischemia in CAD); arterial vasoconstriction incr afterload, not helping HF
  • circulatory failure; refractory HF (hospitalized frequently for clinical deterioration)
138
Q

inamrinone

A
  • cAMP PDE inhib
  • prevent cAMP degradation > more active PKA > incr cytosolic Ca > stimulate myocardial contraction & accelerate relaxation; stimulate balanced arterial/venous dilation (reduce afterload & preload); longer half life & less selective
  • worse SE profile than milrinone
  • short term support of circulation in advanced HF (parenteral inotropic support)
139
Q

milrinone

A
  • cAMP PDE inhib
  • prevent cAMP degradation > more active PKA > incr cytosolic Ca > stimulate myocardial contraction & accelerate relaxation; stimulate balanced arterial/venous dilation (reduce afterload & preload); shorter half life & more selective for PDE3
  • more favorable SE profile, best PDE inhib
  • short term support of circulation in advanced HF (parenteral inotropic support)
140
Q

disopyramide

A
  • Na channel blocker, class IA anti-arrhythmic drug
  • block Na channels > incr threshold (prolong action potential), oral admin, dissociate from Na channels with medium kinetics
  • negative inotrope; contraindications: HF
  • ventricular arrhythmias, recurrent atrial arrhythmias
141
Q

procainamide

A
  • Na channel blocker, class IA anti-arrhythmic drug
  • block Na channels > incr threshold (prolong action potential), oral/IV admin, dissociate from Na channels with medium kinetics
  • lupus-like effect, nausea
  • ventricular arrhythmias & recurrent atrial arrhythmias
142
Q

quinidine

A
  • Na channel blocker, class IA anti-arrhythmic drug
  • block Na channels > incr threshold (prolong action potential), oral/IV admin, dissociate from Na channels with medium kinetics
  • diarrhea
  • ventricular arrhythmias & recurrent atrial arrhythmias
143
Q

lidocaine

A
  • Na channel blocker, class IB anti-arrhythmic drug
  • block Na channels > incr threshold (shorten action potential), IV admin, dissociate from Na channels with fast kinetics
  • CNS toxicity
  • Acute ventricular arrhythmias
144
Q

mexiletine

A
  • Na channel blocker, class IB anti-arrhythmic drug
  • block Na channels > incr threshold (shorten action potential), oral admin, dissociate from Na channels with fast kinetics
  • CNS toxicity
  • Chronic ventricular arrhythmias
145
Q

flecainide

A
  • Na channel blocker, class IC anti-arrhythmic drug
  • block Na channels > incr threshold (minimal effect on action potential duration), oral admin, dissociate from Na channels with slow kinetics
  • arrhythmogenic (avoid in patients with underlying structural heart disease or post-MI)
  • Recurrent atrial arrhythmias
146
Q

propafenone

A
  • Na channel blocker, class IC anti-arrhythmic drug
  • block Na channels > incr threshold (minimal effect on action potential duration), oral admin, dissociate from Na channels with slow kinetics
  • arrhythmogenic (avoid in patients with underlying structural heart disease or post-MI)
  • Recurrent atrial arrhythmias
147
Q

amiodarone

A
  • K channel blocker, class III anti-arrhythmic drug
  • incr action potential duration, oral/IV admin
  • bradycardia (beta blocking effects)
  • atrial and ventricular arrhythmias (less arrhythmogenic in patients with HF/post-MI)
148
Q

dofetilide

A
  • K channel blocker, class III anti-arrhythmic drug
  • incr action potential duration, oral admin
  • marked QT prolongation (torsades de pointes)
  • atrial arrhythmias
149
Q

dronedarone

A

-K channel blocker, class III anti-arrhythmic drug
-incr action potential duration
-
-

150
Q

ibutilide

A

-K channel blocker, class III anti-arrhythmic drug
-incr action potential duration
-
-

151
Q

sotalol

A

-K channel blocker, class III anti-arrhythmic drug
-incr action potential duration
-
-

152
Q

diltiazem

A

-
-decr phase 4 slope & incr threshold
-
-class IV anti-arrhythmic drug

153
Q

verapamil

A

-
-decr phase 4 slope & incr threshold
-
-class IV anti-arrhythmic drug

154
Q

atenolol

A
  • beta-R blocker, class II anti-arrhythmic drug
  • decr phase 4 slope (reduced automaticity), oral/IV admin
  • bradycardia, negative inotrope
  • atrial arrhythmias, slow AV node conduction, prevent sudden cardiac death post-M
155
Q

esmolol

A
  • beta-R blocker, class II anti-arrhythmic drug
  • decr phase 4 slope (reduced automaticity), IV admin, short half-life
  • bradycardia, negative inotrope
  • atrial arrhythmias, slow AV node conduction
156
Q

propranolol

A
  • beta-R blocker, class II anti-arrhythmic drug
  • block beta-1 & beta-2 receptors; decr phase 4 slope (reduced automaticity), oral/IV admin
  • bradycardia, negative inotrope, bronchospasm; Inability to elevate glucose, Nausea, vomiting, confusion, dizziness, fatigue, sleep disorders
  • hypertension; atrial arrhythmias, slow AV node conduction
157
Q

digoxin

A

-
-

158
Q

adenosine

A

-
-incr max diastolic potential
-
-

159
Q

acebutolol

A
  • Beta 1 antagonist (cardioselective)
  • inhibits SNS input to heart decreasing O2 demand
  • contraindicated: COPD, asthma, diabetes
160
Q

atenolol

A
  • Beta 1 antagonist (cardioselective)
  • inhibits SNS input to heart decreasing O2 demand
  • contraindicated: COPD, asthma, diabetes
161
Q

esmolol

A
  • Beta 1 antagonist (cardioselective)
  • inhibits SNS input to the heart decreasing O2 demand
  • Contraindicated: COPD, asthma, diabetes
162
Q

metoprolol

A
  • Beta 1 antagonist (cardioselective)
  • inhibits SNS input to the heart decreasing O2 demand
  • Contraindicated: COPD, asthma, diabetes
163
Q

nadolol

A
  • Beta antagonist (non selective)
  • B1 and B2 antagonist
  • Contraindicated: COPD, asthma, diabetes
164
Q

pindolol

A
  • Beta antagonist (non selective)
  • B1 and B2 antagonist, partial Beta agonist
  • Contraindicated: COPD, asthma, diabetes
165
Q

propranolol

A
  • Beta antagonist (non selective)
  • B1 and B2 antagonist
  • Contraindicated: COPD, asthma, diabetes
166
Q

timolol

A
  • Beta antagonist (non selective)
  • B1 and B2 antagonist
  • Contraindicated: COPD, asthma, diabetes
167
Q

avanafil

A
  • PDE5 inhibitor
  • increase levels of cGMP
  • Do not take with nitrates or alpha receptor blocker vision changes
168
Q

tadalafil

A
  • PDE5 inhibitor
  • increase levels of cGMP
  • Do not take with nitrates or alpha receptor blocker (17 Hr T1/2) vision changes
169
Q

sildenafil

A
  • PDE5 inhibitor
  • increase levels of cGMP
  • Do not take with nitrates or alpha receptor blocker. Vision changes
170
Q

vardenafil

A
  • PDE5 inhibitor
  • increase levels of cGMP
  • Do not take with nitrates or alpha receptor blocker. Vision changes
171
Q

verapamil

A
  • Ca+ channel blocker (cardioselective)
  • Block L type Ca+ channels in heart
  • Can cause heart failure, gingival inflammation
172
Q

diltiazem

A
  • Ca+ channel blocker (cardioselective)
  • Block L type Ca+ channels in heart
  • can cause bradycardia/heartblock

3 Pharm Unit (3 decks)

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