Drugs Flashcards

1
Q

Colesevelam

A
  • Bile Acid Binding Sequestrant (gel)
  • Lower LDL ~20%
  • Very safe, non-systemic, but cannot be used if triglycerides >250
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2
Q

Ticlopidine

A
  • Platelet aggregation inhibitor
  • ADP receptor blocking agent
  • Trade name: Ticlid, use is associated with increased incidence of Thrombotic Thrombocytopenic Purpura (TTP) in 1:2000-4000 patients
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3
Q

Nitroglycerin

A
  • IV Vasodilator
  • Primarily a venodilator
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4
Q

Mexiletine

A
  • Ib
  • Binds INa+ channel in active and inactive states, but not in the resting state. So it has little effect in normal tissue, but does exert effects in sick (ischemic) tissue.
  • Chronic suppression of ventricular arrhythmias (not first line, but sometimes)
  • Nausea, vomiting
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5
Q

Methyldopa

A
  • Centrally acting agent
  • Replaces norepinephrine in secretory vesicles in adrenergic neurons. Acts centrally on the brain to inhibit central adrenergic outflow.
  • Useful for hypertension in pregnancy, but many side effects
  • Sedation, dry mouth, fatigue, depression, liver toxicity
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6
Q

Aspirin

A
  • Platelet aggregation inhibitor
  • Acetylates cyclooxygenase, irreversibly inhibiting it. Prevents production of ThromboxaneA2 (platelet activator)
  • Function returns to normal after 7-10 days when new platelets appear in circulation.
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7
Q

Milrinone

A
  • Inotrope
  • Phsophodiesterase inhibitor
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8
Q

Digoxin

A
  • Inotrope
  • Complicated mechanism: direct membrane effects (mediated by blocking Na+/K+ ATPase), and indirect effects (vagomimetic). Slows conduction, mainly in the SA node, atria, and AV node.
  • Control of ventricular response in atrial fibrillation/flutter (usually with a β-blocker or Ca2+ channel blocker)
  • Yellow vision, anorexia, nausea, vomiting, disorientation, hallucination. Toxicity treated with anti-digoxin antibody fragments
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9
Q

Amiodarone

A
  • III
  • Blocks potassium channels, increases action potential duration and effective refractory period. Also blocks Na+ channels, β receptors, and Ca2+ channels (class I, II, and IV-like effects). Most effective, but has significant side effects.
  • Suppression of ventricular tachycardia (defibrillators more effective). Maintenance of sinus rhythm in atrial fibrillation/flutter. Acute conversion from atrial fibrillation to sinus rhythm.
  • Hyperthyroidism and hypothyroidism. Pulmonary fibrosis, liver toxicity, photodermatitis (grayish-blue skin discoloration). Dronedarone, a congener, has fewer side effects.
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10
Q

Propanolol

A
  • Beta blocker
  • Blocks the B1 and B2 receptors
  • Basically decrease CO. Decreasing HR, decreased contractility, and decreased renin release. Also causes vasoconstriction and a slight increase in PVR. Used in patients with CAD, and for hypertension (but not as the sole agent)
  • Bradycardia, hyperkalemia, fatigue, cold extremeties, bronchospasm.
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11
Q

Ibutilide

A
  • III
  • K+ channel blocker
  • Acute termination of atrial fibrillation and atrial flutter
  • Few extracardiac effects other than GI complaints
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12
Q

Torsemide

A
  • Loop Diuretic
  • Inhibit the Na-K-2Cl symporter in the thick ascending loop of Henle
  • Rapid diuresis, HTN in CKD
  • Hypokalemia, hypocalcemia, hypomagnesemia, increased LDL and triglycerides, hyperglycemia
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13
Q

Nifedipine

A
  • Calcium channel blocker (Dihydropyridine)
  • Block the L-type calcium channel (primarily in smooth muscle), relaxing smooth muscle
  • Hypertension, decreases cardiac output and PVR. Good in patients with diabetes, renal insufficiency, lipid problems, and asthma.
  • Peripheral edema, headaches, flushing, dizziness, GERD, constipation
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14
Q

Angiotensin receptor blocker (-artan)

A
  • Oral Vasodilator
  • Block the angiotensin II receptor (AT1), decreasing sympathetic activation, relaxing smooth muscles, and causing diuresis
  • Hyperkalemia, renal failure, teratogenic!
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15
Q

Apixiban

A
  • Direct Factor Xa Inhibitor
  • Small molecule inhibitor of factor Xa (free and bound)
  • Anticoagulant
  • Trade name: Eliquis, monitoring not required
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16
Q

Verapamil

A
  • Calcium channel blocker (phenylalkylamine)
  • Block the L-type calcium channel (mostly cardiac), relaxing smooth muscle
  • Hypertension, greatly reduces PVR. Good in patients with diabetes, renal insufficiency, lipid problems, and asthma.Constipation, dizziness, nausea, bradycardia
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17
Q

Atorvastatin

A
  • Statin
  • Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors
  • High intensity (40/80 mg/day), moderate intensity (10 mg/day)CYP3A4
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18
Q

Lidocaine

A
  • Ib
  • Binds INa+ channel in active and inactive states, but not in the resting state. So it has little effect in normal tissue, but does exert effects in sick (ischemic) tissue.
  • Ventricular arrhythmias, particular post-MI
  • CNS toxicity: confusion, delirium, paresthesias, grand mal seizures
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19
Q

Spironolactone

A
  • Potassium Sparing Diuretic
  • Antagonizes the mineralcorticoid (aldosterone) receptor on epithelial cells in the late distal tubule and cortical collecting duct
  • Diuretic, generally an add-on therapy with another diuretic class
  • Hyperkalemia, gynecomastia
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20
Q

Aliskiren

A

Inhibit renin

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21
Q

Ezetimibe

A
  • Cholesterol absorption inhibitor
  • Absorbed, glucuronidated, and then localizes to the intestinal villi, preventing absorption of cholesterol
  • Lower LDL ~20%
  • Useful in combination with a moderate intensity statin
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22
Q

Lovastatin

A
  • Statin
  • Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors
  • Moderate intensity
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23
Q

Niacin

A
  • Vitamin B3
  • Potent inhibitor of adipose tissue lipolysis by activating GPR109A (a GPCR). This decreases flux of free fatty acids to the liver for VLDL production
  • Lowers LDL and VLDL, raises HDL
  • No measurable benefit when added to a statin. Take aspirin before niacin to avoid cutaneous vasodilation and flushing.
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24
Q

PCSK9 Inhibitors

A
  • Disinhibit LDLR
  • Dec LDL
  • Myalgias, Delerium, Dementia
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25
Dobutamine
* Inotrope * Beta I and B2 agonist
26
Ethycrinic Acid
* Loop Diuretic * Inhibit the Na-K-2Cl symporter in the thick ascending loop of Henle * Rapid diuresis, HTN in CKD * Ototoxicity, hypokalemia, hypocalcemia, hypomagnesemia, increased LDL and triglycerides, hyperglycemia
27
Digoxin
* Unclassified * Complicated mechanism: direct membrane effects (mediated by blocking Na+/K+ ATPase), and indirect effects (vagomimetic). Slows conduction, mainly in the SA node, atria, and AV node. * Control of ventricular response in atrial fibrillation/flutter (usually with a β-blocker or Ca2+ channel blocker) * Yellow vision, anorexia, nausea, vomiting, disorientation, hallucination. Toxicity treated with anti-digoxin antibody fragments
28
Tenecteplase (TNK-tPa)
* Act plasminogen * Higher fibrin specificity * Direct plasminogen activation
29
Propafenone
* Ic * Sodium channel blocker, some β-blocking activity, negative inotropic effects * Acute conversion of atrial fibrillation to sinus rhythm. Maintenance of sinus rhythm in atrial fibrillation. Suppression of premature ventricular contractions (rarely used for this, raises mortality). * Can exacerbate bronchospasm (β-blocker...)
30
Minoxidil
* Peripheral vasodilator * Activates a potassium channel in vascular smooth muscle, causing K efflux. This hyperpolarizes the cell and relaxes it. * Lower blood pressure in difficult patients * Water and sodium retention, tachycardia/angina/heart failure, hypertrichosis, effusions
31
Hirudin
* Direct Thrombin Inhibitor * Binds both the active pocket site and fibrinogen binding exosite on thrombin. * Anticoagulant * Originally derived from leeches, now made with recombinant DNA technology
32
Nitroprusside
* IV Vasodilator * Metabolized by blood vessels to nitric oxide, causing vasodilation. * Lower blood pressure in difficult patients or emergencies. Mixed venous and arterial vasodilator * Hypotension, cyanide and thiocyanate toxicity. IV only
33
Heparin
* Heparin * Lower molecular weight inhibits Xa, higher molecular weight inhibits thrombin and binds platelets. All enhance antithrombin activity. * Anticoagulant * Can cause heparin induced thrombocytopenia, and osteoporosis (when used chronically), can be self administered.
34
Chlorthiazide, metolazone
* Thiazide Diuretic * Inhibit the Na-Cl symporter in the distal convoluted tubule * First line hypertension * Hypokalemia, hyponatremia, hypercalcemia, impotence, impaired glucose tolerance, increased cholesterol
35
Disopyramide
* Ia * Blocks INa and blocks IKr, slowing the action potential upstroke and prolonging the action potential duration. Also binds the M2 muscarinic receptor for vagolytic effects (stronger than quinidine) * Hypertrophic obstructive cardiomyopathy (but not commonly used) * Antimuscarinic side effects (urinary retention, constipation, blurred vision, dry mouth, closed-angle glaucoma)
36
Cholestryamine
* Bile Acid Binding Sequestrant (resin) * Binds bile acids in the gut, causing depletion of hepatic cholesterol pools and increased production of LDL receptors. Lower LDL ~20% * Very safe, non-systemic, but cannot be used if triglycerides \>250
37
Ticagrelor
* Platelet aggregation inhibitor * ADP receptor blocking agent, used in patients resistant to clopidogrel * Trade name: Brilinta
38
Sotalol
* III * Blocks K+ channels with some β-blocking activity * Maintenance of sinus rhythm in atrial fibrillation/flutter. Prevention of AVNRT, AVRT. Ventricular tachyarrhythmias. * Similar side effects to β-blockers: bronchospasm, depression, hypotension, cognitive impairment
39
Beta-blockers
* II * Decrease slope of phase 4 in the SA node, and decrease the upstroke velocity in the SA and AV node, slowing conduction * Slowing of ventricular response in atrial fibrillation. Disrupting reentrant arrhythmias. Suppressing premature ventricular contractions or atrial premature beats * Bronchospasm, depression, cognitive impairment, hypotension
40
Flecainide
* Ic * Sodium channel blocker, prolongs conduction time. Has negative inotropic effects * Acute conversion of atrial fibrillation to sinus rhythm. Maintenance of sinus rhythm in atrial fibrillation. Suppression of premature ventricular contractions (rarely used for this, raises mortality). * Confusion, irritabilityIcSodium channel blocker, prolongs conduction time. Has negative inotropic effects * Acute conversion of atrial fibrillation to sinus rhythm. Maintenance of sinus rhythm in atrial fibrillation. Suppression of premature ventricular contractions (rarely used for this, raises mortality).Confusion, irritability
41
Amlodipine
* Calcium channel blocker (Dihydropyridine) * Block the L-type calcium channel (primarily in smooth muscle), relaxing smooth muscle * Hypertension, decreases cardiac output and PVR. Good in patients with diabetes, renal insufficiency, lipid problems, and asthma. * Peripheral edema, headaches, flushing, dizziness, GERD, constipation
42
Pitavastatin
* Statin * Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors * Moderate intensity (2-4 mg/day)Longest half-life, tolerated in HIV patients, not well studied
43
Bivalirudin
* Direct Thrombin Inhibitor * Binds both the active pocket site and fibrinogen binding exosite on thrombin, but is a truncated version of hirudin * Anticoagulant * Need to test activated clotting time at 45 minutes, avoid in renal failure
44
Lepirudin
* Direct Thrombin Inhibitor * Binds only the active site pocket on thrombin * Anticoagulant * Need to test APTT at 2 hours, avoid in renal failure
45
Hydrochlorothiazide (HCTZ)
* Thiazide Diuretic * Inhibit the Na-Cl symporter in the distal convoluted tubule * First line hypertension * Hypokalemia, hyponatremia, hypercalcemia, impotence, impaired glucose tolerance, increased cholesterol
46
Clopidogrel
* Platelet aggregation inhibitor * P2Y12 ADP receptor blocking agent, can be used with aspirin. Needs to be activate, some people resistant. * Trade name: Plavix
47
Eplerenone
* Potassium Sparing Diuretic * Antagonizes the mineralcorticoid receptor (aldosterone) on epithelial cells in the late distal tubule and cortical collecting duct * Diuretic, generally an add-on therapy with another diuretic class
48
Argatroban
* Direct Thrombin Inhibitor * Binds only the active site pocket on thrombin * Anticoagulant * Need to test APTT at 2 hours, avoid in liver failure
49
Dipyridamole
* Platelet aggregation inhibitor * Inhibits adenosine uptake, acts on PLA2, causes increased platelet cAMP, leading to inhibition * Trade name: Persantine
50
Abciximab
* Platelet aggregation inhibitor * Humanized murine Fab monoclonal antibody binds to and inhibits GP IIb/IIIa function * Trade name: ReoPro
51
Stanol ester
* Plant Stanol/Sterol Ester * Inhibit micellar cholesterol absorption * Lower LDL 10-14%
52
Alteplase (tPa)
* Act plasminogenShort t1/2 * Higher fibrin specificity * Direct plasminogen activation
53
Atenolol
* Beta blocker * Cardioselective, blocks the B1 receptor * Basically, decrease CO. Decreasing HR, decreased contractility, and decreased renin release. Used in patients with CAD, and for hypertension (but not as the sole agent) * Bradycardia, hyperkalemia, fatigue, cold extremeties, bronchospasm.
54
Fondaparinux
* Synthetic heparin analog * Enhances ability of antithrombin to inhibit factor Xa, but no anti-thrombin activity. * Anticoagulant * Trade name: Arixtra. No thrombocytopenia, but cannot be used in patients in renal failure.
55
Diltiazem
* Calcium channel blocker (Benzothiazepine) * Block the L-type calcium channel (vascular and cardiac), relaxing smooth muscle * Hypertension, decreases cardiac output and PVR. Good in patients with diabetes, renal insufficiency, lipid problems, and asthma. * Edema, headache, nausea, dizziness, diarrhea, bradycardia
56
Quinidine
* Ia * Blocks INa and partially blocks IKr, slowing the action potential upstroke and prolonging the action potential duration. Also binds the M2 muscarinic receptor for vagolytic effects * Converts atrial fibrillation or flutter to sinus rhythm (rarely used for this). Maintain sinus rhythm in patients with atrial fibrillation (but can raise mortality) * Cinchonism (CNS toxicity: tinnitus, hearing loss, delirium, and psychosis). Nausea, vomiting, diarrhea
57
Dabigatran
* Direct Thrombin Inhibitor * Binds only the active site pocket on thrombin * Anticoagulant * Dabigatran etexilate (trade name: Pradaxa) is a prodrug that is converted to dabigatran in the gut, does not need to be monitored
58
Gemfibrozil
* Fibrate * Doubt we need, he cited a paper * Lowers LDL if LDL is high alone. LDL elevated if not high already. Increases HDL if baseline levels are low. * Can cause cholelithiasis and mild GI symptoms
59
Procainamide
* Ia * Blocks INa and partially blocks IKr, slowing the action potential upstroke and prolonging the action potential duration * Termination of sustained ventricular tachycardia (not first line). Ventricular tachycardia after MI (rarely used for this). * Drug-induced lupus, only during long term oral use (not available PO in USA). Fever. Agranulocytosis
60
Prasugrel
* Platelet aggregation inhibitor * ADP receptor blocking agent, used in patients resistant to clopidogrel * Trade name: Efient
61
Nesiritide
* IV Vasodilator * Primarily an arteriolar dilator
62
Ranolazine
* Inhibit late, inward Na current -\> less Na/Ca exchange in ischemic tissue -\> less Ca overload * Safe with other anti-ischemic drugs and if low HR/BP
63
Furosemide
* Loop Diuretic * Inhibit the Na-K-2Cl symporter in the thick ascending loop of Henle * Rapid diuresis, HTN in CKD * Hypokalemia, hypocalcemia, hypomagnesemia, increased LDL and triglycerides, hyperglycemia
64
Metoprolol
* Beta blocker * Cardioselective, blocks the B1 receptor * Basically, decrease CO. Decreasing HR, decreased contractility, and decreased renin release. Used in patients with CAD, and for hypertension (but not as the sole agent) * Bradycardia, hyperkalemia, fatigue, cold extremeties, bronchospasm.
65
Dofetilide
* III * Blocks K+ channels, and some Na+ channel blocking activity * Maintenance of sinus rhythm in atrial fibrillation/flutter * Headaches, GI complaints
66
Timolol
* Beta blocker * Blocks the B1 and B2 receptors * Basically decrease CO. Decreasing HR, decreased contractility, and decreased renin release. Also causes vasoconstriction and a slight increase in PVR. Used in patients with CAD, and for hypertension (but not as the sole agent) * Bradycardia, hyperkalemia, fatigue, cold extremeties, bronchospasm.
67
Warfarin
* Vitamin K Antagonist * Inhibits vitamin K epoxide reductase (VKORC1)Anticoagulant * Trade name: Coumadin
68
Low Molecular Weight Heparin
* Heparin * Enhanced inactivation of factor Xa relative to heparin * Anticoagulant * Reduced incidence of heparin induced thrombocytopenia, and reduced risk of osteoporosis. Can also be self-administered.
69
Omega 3 Fatty Acids
* Inhibit hepatic production and utilization of triglyceride rich particles * Lower TG in a dose-dependent fashion (up to 50% in pt with very high TG). Slightly increase HDL, do nothing for LDL. * No consistent evidence in RCT
70
Fenofibrate
* Fibrate * Doubt we need, he cited a paper * Lowers LDL if LDL is high alone. LDL elevated if not high already. Increases HDL if baseline levels are low. * Can cause cholelithiasis and mild GI symptoms
71
Adenosine
* Unclassified * Interacts directly with A1 adenosine receptors in the heart, activating K+ channel, indirectly decreasing L-type Ca2+ channel activity and the funny current, If. Causes marked hyperpolarization and transient elective heart block. * Diagnosis and termination of supraventricular tachycardias by producing transient heart block. Effective in terminating reentrant rhythms (acts as a reset button). * Transient flushing, chest pressure, and chest burning
72
Rosuvastatin
* Statin * Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors * High intensity (20/40 mg/day), moderate intensity (5/10 mg/day) * Minimally metabolized by CYP2C9
73
Verapamil
* IV * Ca2+ channel blockers, block L-type channels and prolong conduction time and refractory periods in the AV node * Heart rate control in atrial fibrillation/flutter. Can be used to terminate supraventricular tachycardias. * Constipation and peripheral edema (from smooth muscle interference in gut and vasodilation, respectively), hypotension
74
Nitrates
* Oral Vasodilator * Pure venodilator * Can cause reflex tachycardia
75
ACE inhibitors (-opril/-april/-epril/-ipril)
* Oral Vasodilator * Block conversion of angiotensin I to angiotensin II, decreasing sympathetic activation, relaxing smooth muscles, causing diuresis, and increasing bradykinin (vasodilation) * Cough, hyperkalemia, renal failure, angioedema, teratogenic!
76
Dopamine
* Inotrope * B1 agonist
77
Simvastatin
* Statin * Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors * Moderate intensity (40 mg/day)CYP3A4
78
a1 blockers (-zosin)
* a1 blocker * Blocks the a1 receptor (postsynaptic), causing vasodilation. * Hypertension, decreases total peripheral resistance and BP
79
Clonidine
* Centrally acting agent * Stimulates a2 receptors in the brain, decreasing PVR to lower BP * Used adjunctively due to side effects, has few interactions with other drugs * Sedation, dry mouth, sleepiness, bradycardia, fatigue, depression, liver toxicity. Can get withdrawal symptoms if stopped suddenly.
80
Fluvastatin
* Statin * Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors * Moderate intensity (40/80XL mg/day) * CYP2C9
81
Chlorthalidone
* Thiazide Diuretic * Inhibit the Na-Cl symporter in the distal convoluted tubule * First line hypertension * Hypokalemia, hyponatremia, hypercalcemia, impotence, impaired glucose tolerance, increased cholesterol
82
Norepinephrine
* Inotrope * B1 agonist
83
Streptokinase
* Act plasminogen * Antigenic
84
Colestipol
* Bile Acid Binding Sequestrant (resin) * Lower LDL ~20% * Very safe, non-systemic, but cannot be used if triglycerides \>250
85
NSAIDs
* Platelet aggregation inhibitor * Reversibly inhibits cyclooxygenase, function returns when drug concentration falls.
86
Trimterene
* Potassium Sparing Diuretic * Inhibits renal epithelial Na channels in the late distal tubule and collecting duct * Diuretic, generally an add-on therapy with another diuretic class * Hyperkalemia, nausea, vomiting
87
Pravastatin
* Statin * Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors * Moderate intensity (40 mg/day) * Not metabolized by CYPs
88
Hydralzaine
* Oral Vasodilator * Causes arteriolar smooth muscle to relax * Lower blood pressure in difficult patients or emergencies. Pure arterial vasodilator * Headache, nausea, flushing, dizziness, angina, edema. Can cause reflex tachycardia. Drug induced lupus. IV or oral
89
Amiloride
* Potassium Sparing Diuretic * Inhibits renal epithelial Na channels in the late distal tubule and collecting duct * Diuretic, generally an add-on therapy with another diuretic class * Hyperkalemia, nausea, vomiting
90
Rivaroxaban
* Direct Factor Xa Inhibitor * Small molecule inhibitor of factor Xa (free and bound) * Anticoagulant * Trade name: Xarelto, monitoring not required