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154 Cards in this Set
- Front
- Back
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Mannitol
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Osmotic Diuretic
Increases osmolarity of tubular fluid Reduces Na reabsorption Not often used |
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Acetazolamide
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Carbonic Anhydrase Inhibitor
Decreases NaHCO3 reabsorption Metabolic acidosis Tx for glaucoma |
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Loop Diuretics
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Inhibit Na-K-2 Cl pump (luminal)
Thick ascending loop Increased Ca2+ excretion Hypokalemia Metabolic Alkalosis Hyperuricemia Hyponatremia Ototoxicity |
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Furosemide
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Loop Diuretic
Sulfonamide Group May have vascular effect |
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Digitoxin
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Cardiac Glycoside
Inhibits Na/K pump Positive Iontrope Negative Chronotrope |
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Bumetanide
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Loop Diuretic
Sulfonamide Group |
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Torsemide
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Loop Diuretic
Sulfonamide Group |
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Ethacrynic Acid
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Loop Diuretic
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Proximal Tubule
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65% of filtered Na
Carbonic Anhydrase - HCO3 reabsorption |
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Thick Ascending Limb
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25% of filtered Na
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Mannitol
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Osmotic Diuretic
Increases osmolarity of tubular fluid Reduces Na reabsorption Not often used |
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Acetazolamide
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Carbonic Anhydrase Inhibitor
Decreases NaHCO3 reabsorption Metabolic acidosis Tx for glaucoma |
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Loop Diuretics
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Inhibit Na-K-2 Cl pump (luminal)
Thick ascending loop Increased Ca2+ excretion Hypokalemia Metabolic Alkalosis Hyperuricemia Hyponatremia Ototoxicity |
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Furosemide
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Loop Diuretic
Sulfonamide Group May have vascular effect |
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Digitoxin
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Cardiac Glycoside
Inhibits Na/K pump Increased Contractility Vagal Stimulation Decreased Sympathetic Nervous System Heart Block/Arrhythmia - toxic Nausea/Vomiting/Diarrhea CNS - blurred vision Hypokalemia - increases risk of toxicity |
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Bumetanide
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Loop Diuretic
Sulfonamide Group |
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Torsemide
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Loop Diuretic
Sulfonamide Group |
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Ethacrynic Acid
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Loop Diuretic
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Proximal Tubule
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65% of filtered Na
Carbonic Anhydrase - HCO3 reabsorption |
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Thick Ascending Limb
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25% of filtered Na
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Distal Convoluted Tubule
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10% filtered NaCl
4-8% filtered Na |
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Collecting Tubule
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2-5% Na reabsorbed
K/H Secretion Action of Aldosterone Water pores (ADH) |
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Thiazides
Where do they work? What do they block? Adverse Effects? |
Distal Convoluted Tubule
Inhibits NaCl reabsorption Decreased Vascular Resistance Decreased Ca2+ Excretion Hypokalemia Metabolic Alkalosis Hyperuricemia Hyperglycemia Hyperlipidemia |
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Hydrochlorothiazide
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Thiazide Diuretic
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Chlorthalidone
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Thiazide Diuretic
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Metolazone
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Thiazide Diuretic
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K-Sparing Diuretics
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Collecting Tubule
Used w/ Thiazides Sodium Channel Blockers Aldosterone Antagonist Hyperkalemia |
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K-Sparing Diuretics
Na Channel Bockers |
Inhibits Na Channel in luminal late distal/collecting duct
Decreases K/H excretion Hyperkalemia |
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K-Sparing Diuretics
Mineralcorticoid receptor antagonists |
Aldosterone Antagonist
Decreases Na reabsorption Decreases K/H excretion Used for diseases of increased aldosterone levels Gynecomastia in males Hyperkalemia |
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Triamterene
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K-Sparing Diuretics
Na Channel Bockers |
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Amiloride
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K-Sparing Diuretics
Na Channel Bockers Hyperkalemia |
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Spironolactone
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K-Sparing Diuretics
Aldosterone Antagonist Hyperkalemia Hyperaldosteronism Heart Failure Cirrhosis w/ ascites |
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Epelerone
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K-Sparing Diuretics
Aldosterone Antagonist More selective Hyperkalemia |
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Arginine Vasopressin
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ADH
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Desmopressin
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DDAVP
Increased antidiuretic to pressor activity |
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V2
V1 |
V2 - increased perm to H20
V1 - vasoconstriction/GI |
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ADH Agonist
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Increase permeability of collecting ducts to water
Vasoconstriction - vasc/GI Rx: Central Diabetes Insipidus |
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ADH Antagonist
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Rx for Hyponatremia
Can cause diabetes insipidus |
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Creates an Increased risk of Adverse Hyperkalemia
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K-Sparing Diuretics
NSAID ACE inhibitors |
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Conivaptan
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V1a and V2 (ADH) antagonist
Increases free water excretion Rx: hyponatremia IV admin |
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Why should you slowly correct serum Na concentration?
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Correcting to quickly can cause serious problems/death
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Tolvaptan
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Selective V2 (ADH) antagonist
Rx: hyponatremia heart failure cirrhosis SIADH Thirst/dry mouth GI bleed in cirrhosis |
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Clonidine
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a2 agonist
depresses CNS possible life threatening withdrawal orthostatic hypertension |
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Methyldopa
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central alpha agonist by active metabolite
positive coombs test (hemolytic anemia) hepatotoxicity |
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Exhibits first dose phenomenon
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Prazosin (-osin)
alpha 1 receptor blocker |
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Aliskiren
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Renin inhibitor
decreases plasma renin activity increases plasma renin concentration |
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Losartan
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Angiotensin II receptor blocker
Increase plasma renin activity hypotension hyperkalemia |
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Captopril
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ACE inhibitor - highest bioavailability
Increase plasma renin activity Increase Bradykinin *Cough *Angioedema *Hyperkalemia |
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Enalapril
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ACE inhibitor
Increase plasma renin activity Increase Bradykinin *Cough *Angioedema *Hyperkalemia |
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Lisinopril
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ACE inhibitor
Increase plasma renin activity Increase Bradykinin *Cough *Angioedema *Hyperkalemia |
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Fenoldopam
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Vasodilator
Dopamine-1 receptor agonist Hypertensive Emergencies (iv) increased intraocular pressure reflex bradycardia |
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Hydralazine
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Vasodilator - arterial smooth muscle
Used w/ beta blocker/diuretic Acetylated Drug induced lupus |
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Diazoxide
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Vasodilator (arterial)
Opens potassium channels reflex sympathetic stimulation hypotension fluid retention hyperglycemia can provoke angina |
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Minoxidil
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Vasodilator (highly efficacious)
Hyperpolarizes smooth muscle Reflex sympathetic stimulation Hypertrichosis pericardial effusion |
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Sodium Nitroprusside
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Arterial/Venous vasodilator
Hypertensive emergencies Stimulates Guanylyl Cyclase Increases cGMP Close monitoring required Cyanide poisoning hypotension |
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Ditiazem
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Ca Channel Blocker
L-type Ca Channels Vasospastic/Chronic Stable Angina Rx: Hypertension/Angina/Arrhythmias Decreased BP May decrease HR Decrease AV Conduction Decreased Contractility |
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Verapamil
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Ca Channel Blocker
L-type Ca Channels Vasospastic/Chronic Stable Angina Rx: Hypertension/Angina/Arrhythmias Decreased BP May decrease HR Decrease AV Conduction Decreased Contractility |
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Nifedipine
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Ca Channel Blocker
L-type Ca Channels Vasospastic/Chronic Stable Angina Rx: Hypertension/Angina/Arrhythmias Decrease BP Reflexive increase HR High Vascular Selectivity |
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Ca Channel Blockers
Effects on O2 Demand |
Decreased Peripheral Resistance
Decreased Contractility Decreased HR |
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Isosorbide Dintrate
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Venous Dilation
Decreased Ventricular Volume Decrease Arterial BP **Significant 1st pass effect** |
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Nitrates
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Release of NO -> stimulates cGMP release
Venous Dilation Decreases Ventricular Volume Decrease LV End Diastolic Pressure Rx: Angina/Vasospasms |
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Sildenafil (Viagra)
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Phosphodiesterase 5 Inhibitor
Causes increase in cGMP Blocks Breakdown of cGMP Contraindicated w/ Nitrates |
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Beta Blockers
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Decrease:
HR BP Contractility Increases: EDV Ejection Time Increased Diastollic Perfusion Time Prophylactic against MI Withdrawl can occur (taper) |
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Ranolazine
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Newer Drug for Angina
No known mechanism Little effect on HR and BP Increases QT intrerval |
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Dobutamine
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Increases CO with less reflex tachycardia
Arrhythmias |
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Milrinone
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Phosphodiesterase Inhibitor
Increases cAMP Increases Contractility Vasodilation Only I.V. for Acute Heart Failure |
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Nesiritide
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hBNP
Increases cGMP Smooth Muscle Relaxation |
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Increase Plasma Digoxin Toxicity?
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Thiazide/Loop Diuretics - hypokalemia
Quinidine - anti arrhthymia Verapamil/Amiodarone |
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Decreases Plasma Digoxin Toxicity?
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Antacids
Kaolin-Pectin Cholestyramine St. Johns Wort |
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Mechanisms of Arrhythmias
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Increased Automaticity
Afterdepolarizations Re-entry |
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Quinidine
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Class IA
Block Na and K channels Atrial Fibrillation Anti-vagal effects (increase av conductance) Can cause Ventricular Tachycardia alpha blockage Associated w/ cinchonism |
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Procainamide
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Class IA
Blocks Na and K channels Ventricular arrhythmias Acetylated - both active Drug induced lupus Agranulocytosis |
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Disopyramide
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Class IA
Blocks Na and K channels Anticholinergic Lengthens AP Negative Iontrope Constipation |
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Lidocaine
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Class 1B
Acute Tx for Vent Arrhythmia I.V. (large first pass) Can cause Cardiac Toxicity Neurotoxicity - tremor, lightheadedness, tremor |
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Mexiletine
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Class IB
Vent Arrhythmia Orally effective Tremor/Nausea |
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Flecainide
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Class IC
Maintenance of sinus Blocks Na and K channels Negative Ionotrope Blurred Vision Can cause arrhythmia |
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Propafenone
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Class IC
Afib Blocks Na channels B blocker effect Can exacerbate arrhythmias |
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B blcokers
Class 2 Drugs |
Anti-arrhythmic
Afib |
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Amiodarone
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Class III Drug
Serious Ventricular Arrhythmia Increases QT interval Blocks K channels Blocks Na channels Blocks Ca channels Long half life (weeks) Anti-adrenergic Decreases HR (AV Block) Thyroid (contains iodine) Bue-gray skin discoloration Decreases elimination of warfarin |
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Dronedarone
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Class III Drug
Afib/flutter Increase QT liver injury Fetal harm possible |
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Sotalol
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Class III Drug
Serious Vent Arrhythmia Maintain sinus in afib Blocks K channels Increases QT Decreases AV node |
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Adenosine
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Class IV
Paroxysmal Supravent Tachycardia Slows AV conduction Increases refractory period Hyperpolarizes the cell Very short half life |
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Dofetilide
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Class III drug
Maintain sinus w/ afib Increases QT |
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Ibutilide
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Class III Drug
Rapid conversion of a fib/flutter Increase AP Duration |
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Cholestyramine
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Bile Acid Sequestrant
+ charged anion Binds Bile Acids Decreases Cholesterol absorption Inceased HMG-CoA reductase Increased LDL receptors Contraindications: patient with high TAG Can impair warfarin/digoxin absorption |
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Colestipol
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Bile Acid Sequestrant
+ charged anion Binds Bile Acids Decreases Cholesterol absorption Inceased HMG-CoA reductase Increased LDL receptors Contraindications: patient with high TAG Can impair warfarin/digoxin absorption |
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Colesevelam
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Bile Acid Sequestrant
Gel - drug of choice Binds Bile Acids Decreases Cholesterol absorption Inceased HMG-CoA reductase Increased LDL receptors Contraindications: patient with high TAG Can impair warfarin/digoxin absorption |
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Atorvastatin
(statin drugs) |
HMG-CoA reductase inhibitors
Increase LDL receptors Decreased liver cholesterol synthesis Decreases CRP Decreases TG and LDL Increases HDL |
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When added to a statin increases risk of myopathy?
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fibrates (gemfibrozil)
nicotinic acid |
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Ezetimibe
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Blocks NPC1L1 on enterocyte
Reduces cholesterol absorbtion Upregulates LDL receptor Used for hypercholesterolemia Only medicine for Sitosterolemia Cation: Can increase risk of myopathy with statin Can cause elevated liver enzymes w/ statin Diarrhea |
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Vytorin
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simvaStatin + ezetimibe
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Nicotinic Acid (Niacin, B3)
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Prescription = 100x vitamin dose
Inhibits AC activity Reduces Lipolysis (FFA) Reduced TG/VLDL synthesis GPR109A Increased HDL Also reduces lipoprotein a (independent risk factor for heart disease) **Broad Spectrum Agent** Secondary MI prevention Flushing - can give aspirin Increased insulin resistance Hyperuricemia |
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Fibrates
Gemfibrozil Clofibrate Fenofibric Acid |
Increases FA B oxidation
Decreases LDL Small LDL to Big LDL Activates PPARa Decreases ApoB and VLDL Increases LPL Increases Apo AI/AII (HDL) Reduced CETP Increases Warfarin INR Clofibrate - gallstones |
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Fibrates Vs Statin
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Fibrates - more efficacious at lowering TG and raising HDL
Statins - more efficacious in lowering LDL both - additional lowering of TG both - no additional raise in HDL |
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Omega 3 PUFA
Lovaza |
Very Efficacious
Lower TG Decrease VLDL LDL may increase Small LDL to larger LDL Inhibit platelet aggregation |
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Orlistat (Alli)
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Gastric/pancreatic lipase inhibitor
Blocks absorbtion/breakdown of dietary TG Obesity management Gastrointestinal dysfunction Decreases plasma cyclosporine Decreases D,A,K,E Improved diabetes control Increased bleeding time in warfarin therapy |
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Activated Protein C
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Used for Septic Shock
Inhibits Factor V/VIII/IX |
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Unfractionated Heparin
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Binds to antithrombin
Inactivates factor Xa/IIa/9/11/12 Pentasacharide Sequence Monitor aPTT Enhances Tissue factor pathway inhibitor |
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Low Molecular Weight Heparin
(LMWH) |
fragments of of UFH
1/3 as big Inhibits Xa>IIa |
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Fondaparinux
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synthetic pentasaccharide sequence
(heparin) |
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Antithrombin
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Recombinant human antithrombin
Tx: hereditary antithrombin deficiency |
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Activated Protein C
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Used for Septic Shock
Inhibits Factor V/VIII/IX |
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Unfractionated Heparin
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Binds to antithrombin
Inactivates factor Xa/IIa/9/11/12 Pentasacharide Sequence Monitor aPTT Cleared by endothelial/macrophages Enhances Tissue factor pathway inhibitor |
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Low Molecular Weight Heparin
(LMWH) |
fragments of of UFH
1/3 as big Inhibits Xa>IIa |
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Fondaparinux
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synthetic pentasaccharide sequence
(heparin) |
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Antithrombin
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Recombinant human antithrombin
Tx: hereditary antithrombin deficiency |
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Longer Half-Life?
LMWH or UFH |
LMWH/Fondaparinux
LMWH - 3-6 hrs UFH - dose dep 30 min to 150 min |
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Prolonged heparin (over 1 month) side effect? (besides bleeding)
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osteoporosis
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Heparin Induced Thrombocytopenia
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Rapid drop in platelet count due to IgG antibodies against complexes of UFH and platelets
Can lead to: DVT PE DIC MI Ischemic leg/arm injury |
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Tx: for Overdose of Heparin
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Protamine (+)
binds with (-) UFH Does not reverse Fondaparinux |
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What do you give in place of heparin in cases of HIT?
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Direct Thrombin Inhibitors
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Leech anticoagulant?
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hirudin
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Lepirudin
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Direct Thrombin Inhibitor
IV administration t1/2 = 1.3 hours Can increase INR immunogenic - can lead to anaphylaxis No antidote |
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Argatroban
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Direct Thrombin Inhibitor
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Which drug is not indicated in cases of HIT?
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Warfarin (Coumadin)
Only give when Thrombocytopenia is corrected |
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Desirudin
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Direct Thrombin Inhibitor
Recombinant hirudin Tx: prophlaxis for DVT SubQ bid |
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Bivalirudin
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A synthetic 20 AA direct REVERSIBLE thrombin inhibitor
Tx: IV anticoagulant unstable angina undergoing PCI |
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Dabigatran Etexilate
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First ORAL Direct Thrombin Inhibitor
Reversible Tx: stroke prevention w/ afib No req monitoring and no food restrictions No antidote substrate for P-Glycoprotein |
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Rivaroxaban
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direct Factor Xa Inhibitor
Prophylaxis/Tx: DVT and PE in orthopedic surgeries Renal Clearance |
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Which warfarin in more powerful? S/R?
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S-Warfarin is stronger
S = stronger |
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Warfarin (coumadin)
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Oral Anticogulant
Monitor via PT inhibits vitamin K coagulation factors II, VII, IX, X Blocks reduction of vitamin K |
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How long is the latent period for Warfarin?
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8-12 hours
Due to the recycling of coagulation factors T1/2 life of coag factors |
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INR
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(PT/Mean PT)^(ISI)
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Worst Reaction for Warfarin?
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Skin Necrosis
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Where is Warfarin metabolized?
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Liver
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Barbituates cause drug interactions how?
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CYP Inducers
Increase clearance of certain drugs |
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Tx: overdose of Warfarin
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Prothrombin complex concentrate - FFP or VIIa
Oral Vitamin K |
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Alteplase
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tPA
activates plasminogen at site of clot Tx: acute ischemic stroke |
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Reteplase
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Mutant of tPA
longer half life Better penitence into thrombus |
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Tenecteplase
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Mutated tPA
Fibrin Specificity Resistant to PAI Single Bolus |
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Aminocaproic Acid
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Inhibitors of Fibrinolysis
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Tranexamic Acid
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Inhibitors of Fibrinolysis
Tx: Trauma and heavy menses |
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rFVIIa, NovoSeven
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Recombinant Factor VIIa
used in severe hemophilia |
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Aspirin
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COX 1 inhibitor at low doses
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Clopidogrel
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Plavix
ADP Pathway Inhibitor Blocks P2Y purinergic receptor |
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Prasugrel
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ADP Pathway Inhibitor
Blocks P2Y purinergic receptor Greater effect than clopidogrel |
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Abciximab
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Glycoprotein IIb/IIIa Antagonist
Slow PCI |
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Eptifibatide
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Glycoprotein IIb/IIIa Antagonist
Rapid PCI |
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Budesonide
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Inhaled Corticosteroid
DPI - dry powder inhaler Block late phase reaction to allergen Long term treatment |
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Fluticasone
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Inhaled Corticosteroid
DPI - dry powder inhaler and MDI - metered dose Block late phase reaction to allergen Long term treatment |
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Mometasone
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Inhaled Corticosteroid
DPI - dry powder inhaler Block late phase reaction to allergen Long term treatment |
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Adverse Effects of ICS
|
Oral Thrush
Reflex cough/bronchospasm Impaired linear growth in children Osteporosis Varicella |
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Prednisone
|
Systemic corticosteroid
Long term control/prevention of severe asthma |
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Salmeterol
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Inhaled long acting Beta 2 Agonist
DPI Use with ICS for long term control of moderate to severe asthma More efficacious in controlling asthma than increasing ICS alone |
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Formoterol
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Inhaled long acting Beta 2 Agonist
DPI Tx: COPD RAPID |
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Arformoterol
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Inhaled long acting Beta 2 Agonist
Nebulizer |
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Theophylline
|
Inhibits Phosphodiesterase
Increases cAMP Adenosine Antagonist Bronchodilator |
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Montelukast
|
Leukotriene Receptor Antagonist
Long term asthma control Can cause allergic rhinitis |
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Zileuton
|
Inhibits ALL Leukotrienes
Inhibits 5-lipoxygenase QID Possible liver toxicity Drug interactions: warfarin/theophylline |
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Omalizumab
|
Inhibits IgE binding to the high affinity FcE receptor on mast cells and basophils
Decreases number of receptors SubQ Tx: Severe persistant asthma Inadequate control with ICS |
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Albuterol
|
Short acting beta agonist
Quick relief of asthma attack Increase cAMP |
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Levabuterol
|
Short acting beta agonist
Quick relief of asthma attack Increase cAMP |
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Tiotropium
|
Cholinergic (muscarinic) receptor inhibitor
Chronic Bronchitis/COPD |
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Ipratropium
|
Cholinergic (muscarinic) receptor inhibitor
Additional benefit beyond b2 agonist |
