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Pharm- Cardo/Cancer
Exam 2
164
Pharmacology
Graduate
10/05/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Propranolol
Definition

Beta Antagonist

(beta blocker)

 

Nonselective sympathetic beta antagonist - decrease BP

Term
Atenolol
Definition

Beta-1 antagonist

 

Cardioselective (decrease BP)

Term
Clonidine
Definition

Alpha-2 agonist

 

Sympatholytic and indirect (stop NE release)

Term
Prazosin
Definition

Alpha-1 antagonist

 

(causes vasodilation)

Term
-osin
Definition

all alpha-1 antagonist

 

-these vasodilate (for tx of hypertension and BPH)

Term
Isoproteronol
Definition
Beta-1 and beta-2 agonist
Term
Dobutamine
Definition
Beta-1 selective agonist (increase HR)
Term
-olol
Definition

Beta blockers

 

(sympathetic antagonist for Beta-1 and Beta-2)

Term
Cocaine
Definition
Inhibits reuptake of sympathetic NE. This is an indirect agonist.
Term
Amphetamine
Definition
Causes vesicular release. This is an indirect sympathetic agonist.
Term
Ephedrine
Definition
Causes vesicle release (indirect) and is a nonselective direct agonist.
Term
Reserpine
Definition
Causes release of vesicle to be inhibited. This is indirect.
Term
Tyrosine Hydroxylase Inhibitor
Definition
Inhibits synthesis of NE. Indirect.
Term
Chlorthalidone
Definition

A thiazide. It works on the distal tubule.

-Blocks NaCl co-transporter, so salt stays in urine, and hence you pee more. 

 

Side effects: hypokalemia and hypouricemia

Term
Furosemide
Definition

Loop diuretic

-act on thick, ascending limb to prevent NaCl reabsorption, specifically from a Na/K/2Cl transporter. 

 

Side effects: hypokalemia and hyperuricemia

Term
Spironolactone
Definition

Potassium sparing diuretic.

 

-antagonist at the mineralocorticoid receptor. they block aldosterone from having an effect. normally aldosterone would increase Na/K ATPase, which promotes sodium reabsorption. Instead, we're blocking aldosterone from binding to MR receptor. so it's an MR antagonist.

Term
Amiloride
Definition

Potassium sparing diuretic

 

Blocks Na channels on the lumen. 

Term
Clonidine
Definition

alpha-2 agonist

 

-Works on solitary nucleus. It reduces sympathetic nervous system activity

Term
Reserpine
Definition
Inhibits the vesicular release of NE
Term
Propranolol
Definition

Nonselective beta blocker. decreases BP. 

-Direct acting

Term
Atenolol
Definition

Selective for Beta-1 antagonist. 

-Cardioselective beta-blocker

Term
Prazosin
Definition

Alpha-1 antagonist

-vasodilate

Term
Terazosin
Definition

Alpha-1 antagonist

-vasodilate

Term
Hydralazine
Definition

-oral drug. selective arterial dilator. 

-keeps potassium channels open

Term
Minoxidil
Definition

highly effective vasodilator. 

-used for severe hypertension

-lots of side effects: hypertrichosis

-keeps potassium channels open

Term
Sodium nitroprusside (a nitrate)
Definition

-used in emergency situations. and is too efficacious with too many side effects for outpatient use. 

-it's a IV nitrate drug.

-it's dinitrated to nitric oxide (a vasodilator) and acts to hyperpolarize the neuron by keeping K channels open. 

Term
Calcium channel blockers
Definition
Block voltage-gated dependent calcium channes, thereby preventing actin/myosin binding, so you can't get smooth muscle contraction
Term
Verapamil
Definition
Cardioactive. Will relax smooth muscle AND reduce cardiac output (decrease HR, AV conduction, and force of contraction)
Term
Dihydropyridines
Definition

Non-cardioactive and relax smooth muscles but have little effect on cardiac output

-all end in -dipine

Term
Amiodipine
Definition
longer-acting dihydropyridines (CCBs) at 30-50 hours
Term
Nifedipine
Definition

Shorter acting Dihydropyridines (CCBs) at 4 hours. 

-increased risk of MI

Term
ACE inhibitors
Definition

These are inhibiting the conversion of angiotesin I to angiotensin II at ACE.

-end in -pril

-Side effects: due to bradykinin (less metabolism with ACE inhibitors) such as dry cough, angioedema; also hyperkalemia, and reduced kidney function (good for diabetic)

Term
Captopril
Definition
ACE inhibitor with no metabolism necessary
Term
Enalapril
Definition
Pro-drug metabolized to active ACE inhibitor
Term
Angiotensin receptor blockers (ARBs)
Definition
These inhibit binding of angiotensin II to the AT1 receptor, but spare side effects of bradykinin increase (that you got with ACE inhibitors)
Term
losartan
Definition
angiotensin receptor blocker
Term
Valsartan
Definition
Angiotensin receptor blockers
Term
Aliskiren
Definition

Inhibits the conversion of angiotensinogen to angiotensin I by blocking the enzyme renin.

 

So they're a renin-inhibitor

Term
Heparin
Definition
indirectly inhibit thrombin via anti-thrombin III
Term
Enoxaparin
Definition

Low molecular weight heparin

-less efficacy

Term
Unfractionated Heparin
Definition
-better efficacy, but greater bleed risk
Term
Direct Thrombin Inhibitors (DTI's)
Definition
analogs of Hirudin (purified from medicinal leeches) they directly inhibit thrombin.
Term
Lepirudin
Definition
DTI
Term
Warfarin
Definition

Only oral anticoagulant

-It prevents the synthesis of clotting factors by inactivating Vitamin K epoxide reductase . 

-slower than heparin. 

Term
Tissue plasminogen activator
Definition
promotes the conversion of plasminogen to plasmin
Term
Anticoagulants?
Definition
Heparin, DTI, Warfarin
Term
Antiplatelet?
Definition
-aspirin, ADP receptor blockers, GP IIa/IIIb blockers
Term
Sterptokinase
Definition
TPA purified from bacteria
Term
Alteplase
Definition
recombinant TPA
Term
Aspirin
Definition
Inhibits COX-1 from making TXA2 (which would cause platelet aggregation)
Term
ADP receptor blockers
Definition
prevents ADP from binding to platelet purinergic receptors
Term
Clopidogrel
Definition
a pro-drug activated by CYP's for ADP receptor blockers
Term
Gp IIa/IIIb blockers
Definition
used for PCI patients - antiplatelet
Term
Abciximab
Definition
GP IIa/IIIb blockers. These are anti-GPIIb/IIIa antibody.  It binds directly to GP IIb/IIIa
Term
Tirofiban
Definition
Gb IIa/IIIb antagonist. binds directly to GP IIb/IIIa receptor
Term
Niacin (nicotinic acid)
Definition
increase HDL, decrease VLDL (by decreasing synthesis and increasing lipoprotein lipase) and decrease LDL (by decreasing VLDL)
Term
Fibric acid derivatives/fibrates
Definition
decrease VLDL only
Term
Gemfibrozil
Definition
Fibric acid derivative
Term
Bile acid binding resin
Definition

prevents bile acid reabsorption, so it gets eliminated!

-therefore you need to increase LDL receptors to get more LDL in the liver cells to make more cholesterol for bile!

Term
Colestipol
Definition
Bile acid binding resins
Term
Statins
Definition

inhibit HMG-CoA reductase

-ergo preventing cholesterol synthesis

Term
Atorvastatin
Definition
high efficacy statin
Term
Fluvastatin
Definition
Statin
Term
Lovastatin
Definition
Statin
Term
Pravastatin
Definition
low efficacy statin
Term
Rosuvastatin
Definition
high efficacy statin
Term
Simvastatin
Definition
Medium efficacy statin
Term
Ezetimibe (Zetia)
Definition
binds to protein on GI epithelial cells that promotes cholesterol absorption in the small intestine. So you're inhibiting absorption of dietary cholesterol
Term
Vytorin
Definition

Simvastatin/Ezetimibe

-combo drug

-it produced greater reductions in LDL than simvastatin alone, but no different in coronary atherosclerotic plaque.

Term
Organic Nitrates
Definition

These dilate veins (reduce preload and oxygen demand)  and dilate arteries (increase oxygen supply via coronary arteries) more than resistance arteries.

 

Note: high tolerance and toxic effects of headache, flushing/sweating and hypotension

Term
Nitroglycerin
Definition

Nitroglycerin is very effectively metabolized when given orally due to first pass effects. you can avoid this by giving nitroglycerine sublingually. This is because blood supply in mouth is different than hepatoportal system that shunts right to the liver. 

Note: there are also sprays &transdermal patches

Term
Isosorbide
Definition
organic nitrate that can be administered orally
Term
Di/mono- nitrate
Definition
These are organic nitrates that can be administered orally.
Term
Calcium Channel Blockers (CCBs)
Definition
These are especially useful for Variant Angina Pectoris. They can be used for classic, but only when others aren't an option. 
Term
When do you use cardioactive CCBs and when do you use noncardioactive CCBs?
Definition

-Use cardioactive CCBs when by themselves

-Use non-cardioactive when used with beta blockers.

 

Note: they should not be used when unstable or with people who have a history of acute MI.

Term
Amlodipine
Definition
Non-cardioactive CCB. They block channels in vascular smooth muscle without large effects on cardiac muscles. They're vasodilators only!!
Term
Dihydropyridine
Definition

Non-cardioactive CCB. They block channels in vascular smooth muscle without large effects on cardiac muscles. They're vasodilators only!!

 

AKA amlodipine!

Term
Verapamil
Definition
Cardioactive CCB. They block channels in vascular smooth muscle AND in the heart.  So they are a vasodilator AND cardiac inhibitor. 
Term
Beta Blockers
Definition

Best for classic angina. They decrease oxygen demand by decreasing heart rate and decreased contractile force. 

 

Note: may precipitate vasospasm in people with variant angina

Term
Propranolol
Definition
Non-selective beta blocker
Term
Atenolol
Definition
Cardioselective beta blocker
Term
Aspirin
Definition
An anti-platelet drug that protects against acute MI or during a heart attack prevents against re-occlusion against heart attack.
Term
Clopidogrel
Definition
An antiplatelet drug that is an ADP blocker. This is for higher-risk individuals. They can be used post-MI or post-PCI surgery. They block platelet aggregation.
Term
Abciximab
Definition
These are anti-platelet drugs that are glycoprotein IIa/IIIb blockers. Use them during PCI surgery. They prevent fibrinogen binding. 
Term
Tirofiban
Definition

These are anti-platelet drugs that are glycoprotein IIa/IIIb blockers. Use them during PCI surgery. They prevent fibrinogen binding. 

Term
t-PA
Definition
Tissue plasminogen activation. Breaks down fibrin components of clots to open vessels after coronary occlusion has already occurred.  They are effective at clearing clots 50% of the time. They're usually given IV or intra-arterially.
Term
Ateplase
Definition
recombinant tPA
Term
Streptokinase
Definition
Bacterial tPA
Term
Digoxin, Digitoxin
Definition
Increases cardiac output by increasing myocardial contractility as a result of effects on calcium. Used for congestive heart failure.
Term
Digitalis/Cardiac Glycosides
Definition
Used to be first-line treatment, but now only used in specific populations. You can't switch from digitalis glycosides to ACE inhibitors without deterioration of condition
Term
Digitalis Antibodies
Definition
How you treat overdose (since there's a very low margin of safety and you have a high risk of cardiac arrthmias)
Term
Captopril
Definition
An ACE inhibitor that blocks the conversion of angiotensin I to angiotensin II. The therapeutic effects are at AT1 receptors to relax arterial smooth muscle (and reduce afterload) and to reduce aldosterone production/release (and reduce sodium reabsorption and blood volume=reduce preload). also by unknown mechanisms they dilate veins (reduce venous return and preload) and reduce trophic changes in the myocardium (and prevent/reverse myocardial hypertrophy-remodeling)
Term
Enalopril
Definition
ACE inhibitor. Used for congestive heart failure.
Term
Losartan (ARB)
Definition
For unknown reasons, ACE inhibitors are more effective than angiotensin blockers. ARBs should only be used in patients who can't tolerate ACE inhibitors.
Term
Spironolactone 
Definition
Antagonist at aldosterone (mineralocorticoid receptors). They prevent effects of aldosterone on sodium/potassium exchange in the kidneys. Also prevents other non-renal effects of aldosterone, possibly in the heart (remodeling) and the lungs (reduced edema/congestion). Used for congestive heart failure.
Term
Chlorthalidone
Definition
A thiazide diuretic. It has moderate efficacy but produces hypokalemia. Used for congestive heart failure.
Term
Furosemide
Definition
A diuretic at the loop of henle. it has high efficacy but produces hypokalemia. Used for congestive heart failure.
Term
Hydralazine
Definition
An arterial dilator that decreases afterload. Good for treating patients with fatigue as a primary symptom. Used for congestive heart failure.
Term
Isosorbide Dinitrate
Definition
Venous dilator/nitrate that decreases preload. Good for treating patients with pulmonary edema as a primary symptom. Used for congestive heart failure.
Term
Carvedilol
Definition
Beta blocker with alpha-1 antagonist effect.  Therefore it will vasodilate and actually reduce CO, but appear to improve survival in some patients. Used for congestive heart failure.
Term
Bispropolol
Definition
Cardioselective beta blocker. selective at beta-1 receptors. Somehow it reduces heart rate which may restore synchonized filling and contraction of the heart.  Possibly reduced remodeling (cardiac hypertrophy) too. Used for congestive heart failure.
Term
Metoprolol
Definition

Cardioselective beta blocker. selective at beta-1 receptors. Somehow it reduces heart rate which may restore synchonized filling and contraction of the heart.  Possibly reduced remodeling (cardiac hypertrophy) too. Used for congestive heart failure.

Term
Milrinone
Definition
A phosphodiesterase 3 (PDE3) inhibitor.  Blocking PDE means you get an accumulation of cAMP with results in positive ionotropic effects. This accumulation allows you to increase the activity of heart cells. Used for acute heart failure.
Term
Dobutamine
Definition
Beta-1 adrenergic receptor agonists. It's a selective beta-1 agonist. Used for acute heart failure.
Term
Atrophine
Definition
An muscarinic antagonist that blocks effects of the ParaNS on heart. This allows you to have a greater activation of SympNS since you're removing parasympathetic inhibition. Used for acute heart failure.
Term
Organic Nitrates
Definition

These dilate veins (reduce preload and oxygen demand)  and dilate arteries (increase oxygen supply via coronary arteries) more than resistance arteries.

 

Note: high tolerance and toxic effects of headache, flushing/sweating and hypotension

Term
Nitroglycerin
Definition

Nitroglycerin is very effectively metabolized when given orally due to first pass effects. you can avoid this by giving nitroglycerine sublingually. This is because blood supply in mouth is different than hepatoportal system that shunts right to the liver. 

Note: there are also sprays &transdermal patches

Term
Isosorbide
Definition
organic nitrate that can be administered orally
Term
Di/mono- nitrate
Definition
These are organic nitrates that can be administered orally.
Term
Calcium Channel Blockers (CCBs)
Definition
These are especially useful for Variant Angina Pectoris. They can be used for classic, but only when others aren't an option.
Term
When do you use cardioactive CCBs and when do you use noncardioactive CCBs?
Definition

-Use cardioactive CCBs when by themselves

-Use non-cardioactive when used with beta blockers.

 

Note: they should not be used when unstable or with people who have a history of acute MI.

Term
Amlodipine
Definition
Non-cardioactive CCB. They block channels in vascular smooth muscle without large effects on cardiac muscles. They're vasodilators only!!
Term
Dihydropyridine
Definition

Non-cardioactive CCB. They block channels in vascular smooth muscle without large effects on cardiac muscles. They're vasodilators only!!

 

AKA amlodipine!

Term
Verapamil
Definition
Cardioactive CCB. They block channels in vascular smooth muscle AND in the heart.  So they are a vasodilator AND cardiac inhibitor.
Term
Beta Blockers
Definition

Best for classic angina. They decrease oxygen demand by decreasing heart rate and decreased contractile force. 

 

Note: may precipitate vasospasm in people with variant angina

Term
Aspirin
Definition
An anti-platelet drug that protects against acute MI or during a heart attack prevents against re-occlusion against heart attack.
Term
Clopidogrel
Definition
An antiplatelet drug that is an ADP blocker. This is for higher-risk individuals. They can be used post-MI or post-PCI surgery. They block platelet aggregation.
Term
Abciximab
Definition
These are anti-platelet drugs that are glycoprotein IIa/IIIb blockers. Use them during PCI surgery. They prevent fibrinogen binding.
Term
Tirofiban
Definition

These are anti-platelet drugs that are glycoprotein IIa/IIIb blockers. Use them during PCI surgery. They prevent fibrinogen binding. 

Term
t-PA
Definition
Tissue plasminogen activation. Breaks down fibrin components of clots to open vessels after coronary occlusion has already occurred.  They are effective at clearing clots 50% of the time. They're usually given IV or intra-arterially.
Term
Ateplase
Definition
recombinant tPA
Term
Streptokinase
Definition
Bacterial tPA
Term
Digoxin, Digitoxin
Definition
Increases cardiac output by increasing myocardial contractility as a result of effects on calcium. Used for congestive heart failure.
Term
Digitalis/Cardiac Glycosides
Definition
Used to be first-line treatment, but now only used in specific populations. You can't switch from digitalis glycosides to ACE inhibitors without deterioration of condition
Term
Digitalis Antibodies
Definition
How you treat overdose (since there's a very low margin of safety and you have a high risk of cardiac arrthmias)
Term
Captopril
Definition
An ACE inhibitor that blocks the conversion of angiotensin I to angiotensin II. The therapeutic effects are at AT1 receptors to relax arterial smooth muscle (and reduce afterload) and to reduce aldosterone production/release (and reduce sodium reabsorption and blood volume=reduce preload). also by unknown mechanisms they dilate veins (reduce venous return and preload) and reduce trophic changes in the myocardium (and prevent/reverse myocardial hypertrophy-remodeling)
Term
Losartan (ARB)
Definition
For unknown reasons, ACE inhibitors are more effective than angiotensin blockers. ARBs should only be used in patients who can't tolerate ACE inhibitors.
Term
Spironolactone
Definition
Antagonist at aldosterone (mineralocorticoid receptors). They prevent effects of aldosterone on sodium/potassium exchange in the kidneys. Also prevents other non-renal effects of aldosterone, possibly in the heart (remodeling) and the lungs (reduced edema/congestion). Used for congestive heart failure.
Term
Chlorthalidone
Definition
A thiazide diuretic. It has moderate efficacy but produces hypokalemia. Used for congestive heart failure.
Term
Furosemide
Definition
A diuretic at the loop of henle. it has high efficacy but produces hypokalemia. Used for congestive heart failure.
Term
Hydralazine
Definition
An arterial dilator that decreases afterload. Good for treating patients with fatigue as a primary symptom. Used for congestive heart failure.
Term
Isosorbide Dinitrate
Definition
Venous dilator/nitrate that decreases preload. Good for treating patients with pulmonary edema as a primary symptom. Used for congestive heart failure.
Term
Carvedilol
Definition
Beta blocker with alpha-1 antagonist effect.  Therefore it will vasodilate and actually reduce CO, but appear to improve survival in some patients. Used for congestive heart failure.
Term
Bispropolol
Definition
Cardioselective beta blocker. selective at beta-1 receptors. Somehow it reduces heart rate which may restore synchonized filling and contraction of the heart.  Possibly reduced remodeling (cardiac hypertrophy) too. Used for congestive heart failure.
Term
Metoprolol
Definition

Cardioselective beta blocker. selective at beta-1 receptors. Somehow it reduces heart rate which may restore synchonized filling and contraction of the heart.  Possibly reduced remodeling (cardiac hypertrophy) too. Used for congestive heart failure.

Term
Milrinone
Definition
A phosphodiesterase 3 (PDE3) inhibitor.  Blocking PDE means you get an accumulation of cAMP with results in positive ionotropic effects. This accumulation allows you to increase the activity of heart cells. Used for acute heart failure.
Term
Dobutamine
Definition
Beta-1 adrenergic receptor agonists. It's a selective beta-1 agonist. Used for acute heart failure.
Term
Atrophine
Definition
An muscarinic antagonist that blocks effects of the ParaNS on heart. This allows you to have a greater activation of SympNS since you're removing parasympathetic inhibition. Used for acute heart failure.
Term
Hydrochlorothiazide
Definition
Thiazide!
-inhibits sodium reabsorption from distal tubule!
-usually for long-term HTN management
Term
Ethacrynic Acid
Definition
High efficacy loop diuretic
-short-term HTN management
Term
Triamterine
Definition
Potassium Sparing Diuretic
Term
Nadolol
Definition
long-acting beta blocker
Term
Diazoxide
Definition
Vasodilator
Highly effective and long-acting
Parenteral - not a first choice drug.
Term
Diltiazem
Definition
Cardioactive CCB
Term
Nebivolol
Definition
Beta blocker that promotes nitric oxide (NO) production.
Term
Dabigatran Etexilate
Definition
Oral non-peptide DTI
Term
Prasugrel
Definition
ADP receptor Blocker.
-aka Effient
-A prodrug but metabolized by different CYP enzymes than Clopidogrel.
-More consistent effects
Term
Anti-fibrinolytics
Definition
Procoagulants
-Prevent plasmin formation - promote clotting
Term
Hemostatic Aids
Definition
Facilitate the natural hemostatic process.
-ie: vasoconstrictors, clotting factors, collagen/cellulose sheets
Term
Vitamin K
Definition
Reverses effects of Warfarin
Term
Protamine
Definition
Reverses effects of Heparin
Term
Colesevelam
Definition
Bile Acid Sequestrants
-reduce LDL and increase HDL
-best tolerated
Term
Cholestyramine
Definition
Bile Acid Sequestrants
-reduce LDL, increase HDL
Term
Pitavastatin
Definition
Medium efficacy statin
Term
What do Class I Antiarrythmics do?
Definition
Block fast voltage-dependent sodium channels
Term
What do Class II Antiarrythmics do?
Definition
Beta blockers
Term
What do Class III Antiarrythmics do?
Definition
Block potassium channels
Term
What do Class IV Antiarrhythmics do?
Definition
Cardioactive CCBs
Term
Class Ia drugs?
Definition
Quinidine and Procainamide
Term
Class Ib drugs?
Definition
lidocaine and mexilentine
Term
Class Ic drugs?
Definition
Flecainide
Term
Which beta blockers are used as anti-arrhythmics?
Definition
Esmolol and propranolol
Term
Which drugs are used as Class III antiarrhythmics?
Definition
Ibulitide, sotalol, amiodarone
Term
Which drugs are class IV antiarrhythmics?
Definition
Verapamil and diltiazem
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