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
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
3
Q
Nitroglycerin
A
- IV Vasodilator
- Primarily a venodilator
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
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
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.
7
Q
Milrinone
A
- Inotrope
- Phsophodiesterase inhibitor
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
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.
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.
11
Q
Ibutilide
A
- III
- K+ channel blocker
- Acute termination of atrial fibrillation and atrial flutter
- Few extracardiac effects other than GI complaints
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
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
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!
15
Q
Apixiban
A
- Direct Factor Xa Inhibitor
- Small molecule inhibitor of factor Xa (free and bound)
- Anticoagulant
- Trade name: Eliquis, monitoring not required
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
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
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
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
20
Q
Aliskiren
A
Inhibit renin
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
22
Q
Lovastatin
A
- Statin
- Inhibits HMG CoA Reductase, decreasing cholesterol synthesis. Leads to increased LDL receptors
- Moderate intensity
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.
24
Q
PCSK9 Inhibitors
A
- 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