Pharmacology (Exam 3 Spring 2012)

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High levels of Atropine
Antimuscarinic, Skin is dry, difficulty with vision and sympathetic discharge
Alpha 1 Agonist
Phenylephrine
Phenylephrine
Increases Ca (intracellularly)-->activates phospholipase-->vasoconstriction-->constrict smooth muscle
Alpha 2 Agonists
Clondidine, methyldopa, guanfacine
Clondidine
Decreases adenylate cyclase-->opens K channels-->decreases Ca channels, decreases blood pressure and sympathetics
Beta 1 Agonist
Increases Ca (intracellularly)--> on heart increases HR and contractility
Beta 2 Agonist
Stimulates adenylate cyclase activity-->decreases Ca (intracellularly)-->on lungs relaxes smooth muscle-->vasodilation
Beta 2 Agonist
Albuterol
Beta 1 Agonist> Beta 2 Agonist
Dobutamine
Beta 1 = Beta 2
Isoproterenol
Isoproterenol
increases HR and bronchodilator
D1
CNS and periphery increases in cAMP and CO
D2-D4
decreases in cAMP in intra-renal arteries and arterioles, vasoconstriction
A1A2B1
NE
A1A2B1B2
Epi
Potent D1 Agonist that increases CO and decreased TPR
Fenoldopam
Nonselective Alpha blockers
Phentolamine
Alpha 1 Blockers
Prazosin
Alpha 1 Blockers
Vasodilation to decrease BP in hypertensive crisis
Nonselective Beta Blocker
Propanolol, timolol
Selective B1 Blocker
Atenolol
Alpha and Beta Blocker
Carvedilol
Treats Pheochromocytoma
Carvedilol
Dopamine
Directly stimulates alpha and beta receptors
M1
CNS, Gq, increases cAMP by increasing IP3
M2
Heart, Gi, decreases cAMP, efflux of K
M3
Smooth muscle, Gq increases Ca, smooth muscle contraction, NO synthase stimulated, not innervated
Baroreceptor reflex
carotid sinus and aortic sinus, primary response, increases stretch, fastest way to change HR.
Chemoreceptor reflex
Carotid Body and Aortic Body, secondary response
Increase in HR always
decreases duration of diastole
HMG-CoA R Inhibitors
Statins
D1
Low dose dopamine
D1b1
medium dose Dopamine
D1B1A1
high dose dopamine
statins
block formation of fatty acids, decrease LDL
Statin side effect
Myositis and rhabdomyolysis
Bile Acid binding resins
"Cole"
"Cole"
reduces gastric reabsorption of cholesterol, increase TG
Bile Acid binding resin side effect
increased TG, vitamin k deficiency
Cholesterol Absorption inhibitor
Ezetimibe
Ezetimibe
prevents uptake of cholesterol from gut to liver
Fibric Acid Derivatives
Fenofibrate or gemfibrozil
Fenofibrate
breaks down fatty acid
Fenofibrate side effect
rhabdomyolysis
Niacin
Inhibits cholesterol--> VLDL, increases HDL
Side effect of niacin
high doses cause flushing and Gout
Fish oil
decreases TG (side effect: fish burp)
Osmotic Diuretic
Mannitol
Mannitol
increases osmotic pressure which retains water in tubule
Mannitol side effect
Volume expansion
Carbonic Anhydrase Inhibitor
prevents reabsorption of HCO3 from Proximal Tubules
Carbonic Anhydrase Inhibitors
Acetazolamide, Dorzolamide
Carbonic Anhydrase Inhibitors Side Effect
Hypokalemia, metabolic acidosis, reduced Ca reabsorption, not reccommended for use in people with sulfa drug allergies or sickel cell anemia
Loop Diuretics
inhibits Na/K/2Cl symporter in ascending loop of hendle, reduced Na reabsorption, dilute outside of tubule, reduced water reabsorption
Loop Diuretics
Ethacrynic Acid, Furosemide, Torsemide
Loop Diuretic Side Affects
Hypokalemia potentiates digitalis toxicity, metabolic alkalosis, hypomagnesemia and Ca loss from decreased luminal K, hyperuriecemia due to hypovolemia
Thiazide Diuretic
Hydrochlorothiazide
Hydrochlorothiazide
acts on distal tubule, treats HTN, excretes Na, blocks Na/Cl symporter
Side effect of thiazide diuretic
K wasting
K Sparing Diuretics
acts on Collecting duct, allows Na and water excretion by retains K
K sparing diuretics
Amiloride, Spironolactone, Triamterene
Side effects of K sparing diuretics
promotes hyperkalemia, ACE inhibitors make hyperkalemia worse and NSAIDS reduce diuretic effiacy
ADH
acts of cortical collecting duct, stimulates renal synthesis of aquaporin (V2) receptors, permits renal H2O reabsorption
Treat scuba divers and astronauts with
ADH
Vasopressin Antagonist
acts on cortical collecting duct, Conivaptan, treats hyponatremia from SIADH and causes nephrogenic diabetes insipidus
Side affects of Vasopressin Antagonist
hypovolemia and increased blood osmolarity
Nitroglycerine is contraindicated in patients with
glaucoma, anemia, pregnancy, or Viagra
IV Nitroglycerine
First line to improve cardiac flow, nitric oxide donor
Sublingual Nitroglycerine
treats Angina
Disadvantage to Nitroglycerine
Tolerance develops, headache, reflex tachycardia
Sodium Nitroprusside
Nitric oxide donor, arterial/venous dilation, can cause cyanide poisoning
Sodium Nitroprusside is contraindicated in patients with
pre-eclampsia, hyponatremia, pregnancy, viagra
Phosphodiesterase inhibitor Type 3 Aminophylline
increases cAMP, dilates, even during alpha and beta blockade, amplify sympathetic activators, catastrophic if used with sympathetic mimetics
Phosphodiesterase inhibitor Type 5 Sildenafil
increases cGMP, vasodilation, DO NOT MIX WITH NITRATES OR CIRCULATORY COLLAPSE WILL HAPPEN!
Hydralazine
opens K channels, vasodilates
Minoxidil
opens K channels, vasodilates, unwanted body hair is a negative side effect
Non-selective Ca channel blocker
blocks blood vessels only
Selective Ca channel blocker
blocks blood vessels and heart
All Ca channel blockers promote
vasodilation and coronary blood flow
Verapamil and Diltiazem
Ca channel blocker, negative inotropic
Nifedipine, dihydropyridine
Ca channel blocker, vasodilator, CONTRAINDICATED IN HEART FAILURE
CA channel blocker side effect
breast enlargement
alpha 1 receptor antagonist
Doxazosin
Beta 1 Blocker can be taken with Doxazosin to
control the heart rate
ACE Inhibitor
"prils" and protects against cardiac remodeling, vasodilation
Angiotensin II receptor Antagonist
"artans" and protects against cardiac remodeling with less of a cough, vasodilation
Aldosterone receptor antagonist/blocker (ARB)
Spironolactone
Spironolactone
Spares K, protects against cardiac edema and remodeling, promotes Na loss
Direct renin antagonist
aliskire(causes vasodilation)
Vasodilators all cause
headaches, orthostatic hypotension, and hypotensive episodes
Na channel blocker class 1A
prolonged repolarization, procainamide
Na channel blocker class 1B
shorten time for repolarization, Lidocaine
First line of treatment for arrhythmias
Lidocaine (IV)
Na channel blocker class 1C
Flecainide
Class 2
Beta blockers, Esmolol
Class 3
block K channels
Amiodarone
Class 3, turns patient blue
Class 4
slow ca channel blocker, cardioselective Ca channel blocker
Diltiazem and Verapamil
Class 4
Digoxin
increases Ca storage in SR, slows HR and force of contraction, narrow therapeutic index, DANGEROUS WITH VERAPAMIL, AMIODARONE, ERYTHROMYCIN, and Epi
Magnesium Sulfate
controls torsades de pointes
Treatment for arrhythmias
IV Lidocaine, Class 1A to capture heart rate, if wolff parkinson white try class 1A with beta blocker, if fibrillation or torsade de Pointes try Magnesium Sulfate
Cardiac Glycosides
Digoxin, Digitoxin, Digoxin Immune Fab
Digoxin
Increase Ca storage in SR, slows HR, increases F of contraction, CLEARED THRU KIDNEY with a narrow therapeutic index
Adverse affects of Digoxin
arrthythmias, ventricular tachycardia, fibrillation, overdose in renal failure, women have 33% more fatalities than untreated
Digoxin directly blocks
Na/K ATPase
Digitoxin
Metabolized by liver
Digoxin Immune Fab
Treats digoxin overdose, not reccommended in patients with sheep allergies
Adrenoreceptor agonists
Epi, NE, Isoproterenol, Dopamine and Dobutamine
Epi and NE are used to treat
cardiac arrest
Low dose Dopamine
D1 (vasodilation)
Medium dose Dopamine
B1 (increased cardiac contractility)
High dose Dopamine
A1 (vasoconstriction)
Dopamine is best used for
Shock!
Can you use Epi and NE to treat shock?
No! Lactic acidosis causes the catecholamine receptors to loose their shape.
Phosphodiesterase Inhibitor 3
Milrinone, Inamrinone, Vesnarinone
Milrinone
Treats CHF, slow degradation of cAMP, restrores sympathetic drive in presence of adrenergic receptor antagonists, DON'T use with B agonists!
Ca Sensitizing Agent
Levosimendan
Hypertension treatment
1. Therapeutic lifestyle change. 2. hydrochlorthiazides or ACE inhibitors
Hydrochlorothiazide
acts of distal tubule to promote Na, H2O excretion, K wasting, Ca sparing and tachycardia
Use Hydrochlorothiazide with
Selective Beta 1 Blockers (to control tachycardia)
ACE Inhibitor
Protects against cardiac remodeling, vasodilator, Na/H2O excretion and limits K loss
ARB
Like ACE Inhibitor but LESS COUGHING
Use the following drugs in a Hypertensive Crisis
Esmolol, Nitroglycerin, Sodium Nitroprusside
Acute Coronary Syndrome
Ischemic heart disease
How to treat Acute Coronary Syndrome
MONA (Morphone, Oxygen, Nitrates, Aspirin)
Chronic Cardiac ischemia treatment
Nitrates, B-Blockers, non-selective Ca channel blockers
Should you use Beta-Blocker to treat CHF?
No! That would promote pulmonary edema.
How do you treat CHF?
ARB (Spironolactone) and ACE Inhibitor
How do you treat an emergency Beta-2 Blockade?
PDE-3 Inhibitor
High levels of ANP
is diagnostic of heart failure
Flow is the
name of the game!
Why use Spironolactone to treat CHF?
It counteracts aldosterone escape.