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3 Pharm Unit > New Drugs test 3 > Flashcards

New Drugs test 3 Flashcards

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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
menadione
-warfarin antidote- vit K - - -
26
dalteparin
- low molecular weight heparins- indirect thrombin inhibitor -enhances antithrombin action on factor X - -Tx=MI, angina, thrombophlebitis Prevent=clots etc.
27
enoxaparin
-low molecular weight heparins- indirect thrombin inhibiotor -enhances antithrombin action on factor X - -Tx=MI, angina, thrombophlebitis Prevent=clots etc.
28
fondaparinux
- Xa inhibitor- indirect thrombin inhibitor - pentasaccharide inhibits Xa, renal clearance - bleeding hemmorhage - SubQ for DVT, PE prevention following surg,
29
argatroban
-direct thrombin inhibitors -inhibits thrombin, hepatic clearance - -parenteral in heparin contraindicated individuals
30
bivalirudin
-direct thrombin inhibitors -inhibits thrombin, hepatic and renal clearance - -parenteral in heparin contraindicated individuals
31
lepirudin
-direct thrombin inhibitors -inhibits thrombin, renal clearance - -parenteral in heparin contraindicated individuals
32
dabigatran
- direct thrombin inhibitors - inhibits thrombin, 80% renal clearance - GI BLEEDS! - Oral
33
tissue plasminogen activator
- thrombolytics - serine protease, plasminogen to plasmin - intracranial hemmorhage - massive venous thrombosis or PE, acute MI
34
streptokinase
- thrombolytics - binds and activates plasminogen - allergic reactions, intracranial hemmorhage - massive venous thrombosis or PE, acute MI
35
urokinase
- thrombolytics - promotes plasminogen to plasmin - intracranial hemmorhage - massive venous thrombosis or PE, acute MI
36
abciximab
- antiplatelet drugs - chimeric monoclonal Ab targets platelet Iib/IIIa - bleeding/hemorrhage - parenteral, prevent blood clot during vessel procedure
37
aspirin
- antiplatelet drugs - irrev. Acetylates cyclooxygenase inhibits TXA2 syn - excessive bleeding (aneurysm in brain) - prevention MI, TIA, stroke, restenosis (most common used)
38
clopidogrel
- 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
39
prasugrel
-antiplatelet drugs -thienopyridine deriv-->irrev blocks P2Y receptor-->blocks plat. Agg - -prevent stroke MI, coronary intervention (more eff/rapid HYDROLYSIS not CYP)
40
ticlopidine
- 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
41
tirofiban
- antiplatelet drugs - carboxy fibrinogen terminal targets platelet IIb/IIIa receptor - bleeding/hemorrhage - parenteral, prevent blood clot during vessel procedure
42
Chlorothiazide
- Thiazide Diuretics - Block Na-Cl symporter in DCT - Hypokalemia, increased uric acid, sulfa crossreactivity - antihypertensive, heart failure
43
Chlorthalidone
- Thiazide Diuretics - Block Na-Cl symporter in DCT - Hypokalemia, increased uric acid, sulfa crossreactivity - antihypertensive, heart failure
44
Hydrochlorothiazide
- Thiazide Diuretics - Block Na-Cl symporter in DCT - Hypokalemia, increased uric acid, sulfa crossreactivity - antihypertensive, heart failure
45
Furosemide
- Loop diuretic - Blocks Na-K-2Cl cotransporter in ascending loop of Henle - Hypokalemia, increased uric acid, deafness, sulfa cross reactivity - Hypertension, heart failure
46
Ethacrynic Acid
- Loop diuretic - Blocks Na-K-2Cl cotransporter in ascending loop of Henle - Hypokalemia, increased uric acid, deafness (especially this drug) - Hypertension, heart failure
47
Bumetanide
- Loop diuretic - Blocks Na-K-2Cl cotransporter in ascending loop of Henle - Hypokalemia, increased uric acid, deafness, sulfa cross reactivity - Hypertension, heart failure
48
Torsemide
- Loop diuretic - Blocks Na-K-2Cl cotransporter in ascending loop of Henle - Hypokalemia, increased uric acid, deafness, sulfa cross reactivity - Hypertension, heart failure
49
Spironolactone
- Aldosterone Receptor Blockers (mild diuretic) - Block sodium and water reabsorption in collecting ducts - Hyperkalemia - Resistant hypertension, congestive heart failure with hypertension
50
Eplerenone
- Aldosterone Receptor Blockers (mild diuretic) - Block sodium and water reabsorption in collecting ducts - Hyperkalemia - Resistant hypertension, congestive heart failure with hypertension
51
Triamterene
- Potassium sparing diuretic - Sodium channel blocker in DCT and collecting duct - Hyperkalemia - Diuresis, antihypertensive
52
Amiloride
- Potassium sparing diuretic - Sodium channel blocker in DCT and collecting duct - Hyperkalemia - Diuresis, antihypertensive
53
Captopril
- 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
54
Enalapril
- 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
55
Lisinopril
- 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
56
Fosinopril
- 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
57
Conivaptan
- 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
58
Tolvaptan
- Vasopressin Receptor Antagonist (oral) - Blocks V2 receptor selectively - increased plasma osmolality - Hyponatremia associated with heart failure, cirrhosis, and SIADH
59
Losartan
- ARBs - Block AT1 receptor, block effects of Ang II - Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs - Hypertension and heart failure
60
Valsartan
- ARBs - Block AT1 receptor, block effects of Ang II - Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs - Hypertension and heart failure
61
Candesartan
- ARBs - Block AT1 receptor, block effects of Ang II - Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs - Hypertension and heart failure
62
Irbesartan
- ARBs - Block AT1 receptor, block effects of Ang II - Hypotension, hyperkalemia, fetal renal toxicity (angioedema and cough < ACEIs - Hypertension and heart failure
63
Aliskiren
- Renin Inhibitor - Competitive inhibitor of renin - Hypotension, cough, hyperkalemia - Hypertension
64
Verapamil
- 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)
65
Diltiazem
- 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)
66
Nifedipine
- 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
67
Nicardipine
- 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
68
Amlodipine
- 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
69
Atenolol
- Beta Blocker - Blocks Beta 1 receptors - Inability to elevate glucose, nausea, vomiting, confusion, dizziness, fatigue, sleep disorders - Hypertension
70
Terazosin
- Alpha blocker - Blocks alpha 1 receptors - Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence - Hypertension (pheochromocytoma)
71
Prazosin
- Alpha blocker - Blocks alpha 1 receptors - Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence - Hypertension (pheochromocytoma)
72
Doxazosin
- Alpha blocker - Blocks alpha 1 receptors - Reflex tachycardia, orthostatic hypotension, fluid retention, palpitations, tinnitus, GI upset, headaches, urinary incontinence - Hypertension (pheochromocytoma)
73
Labetalol
- Mixed Adrenergic Blocker - Blocks beta receptors and alpha 1 receptors - (none mentioned) - Chronic Hypertension, hypertensive emergencies
74
Carvedilol
- Mixed Adrenergic Blocker - Blocks beta receptors and alpha 1 receptors - (none mentioned) - CHypertension and heart failure
75
Reserpine
- 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
Clonidine
- Centrally mediated agents - Alpha 2 agonists - Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension - Resistant hypertension
77
Alpha-methyldopa
- 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
Guanabenz
- Centrally mediated agents - Alpha 2 agonists - Withdrawal syndrome - rebound hyertension, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension - Resistant hypertension
79
Hydralazine
- Vasodilators - Unknown mechanism (reduces intracell calcium in arterioles - Headache, anorexia, nausea, dizziness, sweating, reflex tachcardia (angina and ischemic arrhythmias, Lupus - Hypertension
80
Minoxidil
- Vasodilators - Activates Potassium channels preferentially In arterioles - Fluid retention, reflex tachycardia, abnormal hair growth, pericardial effusion and cadiac tamponande - Resistant hypertension
81
Nitroprusside
- Vasodilators - Generates nitric oxide, increases cGMP in veins and arteries - Rapid decrease in MAP, cyanide accumulation - Hypertensive crisis, cause hypotension during surgery
82
Riociguat
- Vasodilators - Direct stimulation of guanylyl cyclase, increases cGMP - Headaches, dizziness, nausea, diarrhea, hypotension, birth defects - Pulmonary hypertension, thromboembolic hypertension
83
Nitroglycerin
- Vasodilators - Generates nitric oxide, increases cGMP in veins - Headache - hypertensive crisis, cause hypotension during surgery
84
Epoprostenol
- Vasodilators - Direct vasodilation via cAMP (drug is prostacyclin, counters TXA2) - (none mentioned) - Pulmonary hypertension (continuous IV admin)
85
Bosentan
- Vasodilators - Non selective endothelin receptor blocker - Edema, headache, blocks spermatogenesis, resp. tract infection, decreased hematocrit, hepatic effects - Pulmonary hypertension
86
Ambrisentan
- Vasodilators - ET-A (endothelin A) receptor blocker - Edema, headache, blocks spermatogenesis, resp. tract infection, decreased hematocrit, hepatic effects - Pulmonary hypertension
87
Rizatriptan
- 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
Sumatriptan
- 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
Zolmitriptan
- 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
Cyproheptadine
- 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
Ketanserin
- 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
Ergonovine
- 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
Ergotamine
- Serotonin Receptor Partial Agonist - Partial agonist at 5-HT1/2 R - Prolonged vasospasm, GI disturbances - Acute migraines, postpartum bleeding
94
Methysergide
- 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
Amlodipine
- 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
Nicardipine
- 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
Nifedipine
- 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
Nimodipine
- 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
Isosorbide Dinitrate
-Nitrovasodilators -reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg. - -angina/CHD
100
Isosorbide Mononitrate
- Nitrovasodilators - reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg. - minimal first-pass metab! - angina/CHD (longer action)
101
Nitroglycerin
- 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
Nitroprusside Sodium
-Nitrovasodilators -reduce O2 demand, up O2 supply to heart (relaxes arteries & veins!), inhibit platelet agg. - -angina/CHD
103
Aspirin
-Miscellaneous (anticoagulant) - - -Acute coronary syndrome, MI, stroke in combo w/ a P2Y12 inhibitor
104
Clopidogrel
- 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
Prasugrel
- 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
Ranolazine
- 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
Ticagrelor
-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
cholestyramine
- 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
colesevelam HCl
- 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
atorvastatin
- 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
fluvastatin
- 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
lovastatin
- 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
simvastatin
- 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
pravastatin
- 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
clofibrate
- 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
fenofibrate
- 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
gemfibrozil
- 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
ezetimibe
- 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
nicotinic acid (niacin)
- 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
quinapril
- 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
candesartan
- 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
losartan
- 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
valsartan
- 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
Loop diuretics
- - - -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
thiazides
- - - -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
bisoprolol
- 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
carvedilol
- 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
metoprolol
- 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
digoxin
- 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
digitoxin
-cardiac glycosides -No other info not specific to digoxin - -
131
eplerenone
-aldosterone antag - - -addition to ACEI/ARBs in patient with moderately severe HF (class C/D) or with L ventricular dysfunction after MI
132
spironolactone
-aldosterone antag - - -addition to ACEI/ARBs in patient with moderately severe HF (class C/D) or with L ventricular dysfunction after MI
133
hydralazine
-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
isosorbide dinitrate
-vasodilators -short acting, venodilation > incr venous capacitance > reduce preload; also incr coronary artery flow - -used as combo with hydralazine
135
nitroglycerine
-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
dobutamine
- 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
dopamine
- 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
inamrinone
- 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
milrinone
- 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
disopyramide
- 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
procainamide
- 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
quinidine
- 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
lidocaine
- 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
mexiletine
- 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
flecainide
- 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
propafenone
- 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
amiodarone
- 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
dofetilide
- K channel blocker, class III anti-arrhythmic drug - incr action potential duration, oral admin - marked QT prolongation (torsades de pointes) - atrial arrhythmias
149
dronedarone
-K channel blocker, class III anti-arrhythmic drug -incr action potential duration - -
150
ibutilide
-K channel blocker, class III anti-arrhythmic drug -incr action potential duration - -
151
sotalol
-K channel blocker, class III anti-arrhythmic drug -incr action potential duration - -
152
diltiazem
- -decr phase 4 slope & incr threshold - -class IV anti-arrhythmic drug
153
verapamil
- -decr phase 4 slope & incr threshold - -class IV anti-arrhythmic drug
154
atenolol
- 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
esmolol
- 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
propranolol
- 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
digoxin
- - - -
158
adenosine
- -incr max diastolic potential - -
159
acebutolol
- Beta 1 antagonist (cardioselective) - inhibits SNS input to heart decreasing O2 demand - contraindicated: COPD, asthma, diabetes
160
atenolol
- Beta 1 antagonist (cardioselective) - inhibits SNS input to heart decreasing O2 demand - contraindicated: COPD, asthma, diabetes
161
esmolol
- Beta 1 antagonist (cardioselective) - inhibits SNS input to the heart decreasing O2 demand - Contraindicated: COPD, asthma, diabetes
162
metoprolol
- Beta 1 antagonist (cardioselective) - inhibits SNS input to the heart decreasing O2 demand - Contraindicated: COPD, asthma, diabetes
163
nadolol
- Beta antagonist (non selective) - B1 and B2 antagonist - Contraindicated: COPD, asthma, diabetes
164
pindolol
- Beta antagonist (non selective) - B1 and B2 antagonist, partial Beta agonist - Contraindicated: COPD, asthma, diabetes
165
propranolol
- Beta antagonist (non selective) - B1 and B2 antagonist - Contraindicated: COPD, asthma, diabetes
166
timolol
- Beta antagonist (non selective) - B1 and B2 antagonist - Contraindicated: COPD, asthma, diabetes
167
avanafil
- PDE5 inhibitor - increase levels of cGMP - Do not take with nitrates or alpha receptor blocker vision changes
168
tadalafil
- PDE5 inhibitor - increase levels of cGMP - Do not take with nitrates or alpha receptor blocker (17 Hr T1/2) vision changes
169
sildenafil
- PDE5 inhibitor - increase levels of cGMP - Do not take with nitrates or alpha receptor blocker. Vision changes
170
vardenafil
- PDE5 inhibitor - increase levels of cGMP - Do not take with nitrates or alpha receptor blocker. Vision changes
171
verapamil
- Ca+ channel blocker (cardioselective) - Block L type Ca+ channels in heart - Can cause heart failure, gingival inflammation
172
diltiazem
- Ca+ channel blocker (cardioselective) - Block L type Ca+ channels in heart - can cause bradycardia/heartblock

3 Pharm Unit (3 decks)

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