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1

Colesevelam

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

2

Ticlopidine

  • 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

3

Nitroglycerin

  • IV Vasodilator 
  • Primarily a venodilator

4

Mexiletine

  • 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

5

Methyldopa

  • 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

6

Aspirin

  • 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.

7

Milrinone

  • Inotrope
  • Phsophodiesterase inhibitor

8

Digoxin

  • 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

9

Amiodarone

  • 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. 

10

Propanolol

  • 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.

11

Ibutilide

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

12

Torsemide

  • 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

13

Nifedipine

  • 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

14

Angiotensin receptor blocker (-artan)

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

15

Apixiban

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

16

Verapamil

  • 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

17

Atorvastatin

  • 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

18

Lidocaine

  • 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

19

Spironolactone

  • 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

20

Aliskiren

Inhibit renin

21

Ezetimibe

  • 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

22

Lovastatin

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

23

Niacin

  • 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.

24

PCSK9 Inhibitors

  • Disinhibit LDLR
  • Dec LDL
  • Myalgias, Delerium, Dementia

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