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cardiovascular Pharmacology
cardiovascular pharmacology by MS-II
114
Medical
Graduate
09/21/2010

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Term
Clonidine
Definition
primary effect on site 1 (decrease sympathetic outflow from vasomotor centers in CNS)
Term
methyldopa
Definition
primary effect on site 1 (decrease sympathetic outflow from vasomotor centers in CNS)
Term
propranolol
Definition
Primary mechanism: adrenergic (ß1 and 2) receptor inhibitor. Contributes to effect on site 1 (decrease sympathetic outflow from vasomotor centers in CNS). Contributes to action at ganglion (site 3)
Term
reserpine
Definition
Primary mechanism: depresses pre-synaptic, adrenergic transmission at nerve ending (site 3). Contributes to effect on site 1 (decrease sympathetic outflow from vasomotor centers in CNS)
Term
Trimethapham
Definition
Primary mechanism on Site two (inhibition of sympathetic outflow from ganglia)
Term
Phentolamine
Definition
primary: alpha1 and 2 adrenergic inhibitor. Site 4 (adrenergic receptor inhibitor)
Term
Phenoxybenzamine
Definition
primary: alpha1 and 2 adrenergic inhibitor. Site 4 (adrenergic receptor inhibitor)
Term
Prazosin
Definition
primary mechanism: alpha1 adrenergic receptor inhibitor. Site 4
Term
labetalol
Definition
primary mechanism: beta1 and 2 and alpha1 adrenergic receptor inhibitor (site 4)
Term
Direct acting vasodilators: list all
Definition
Hydralazine, minoxidil, nitroprusside, diazoxide, CCBs
Term
Functional vasodilators: list all
Definition
ACE-I (captoPRIL, enalaPRIL, lisinoPRIL, xx-PRIL). ARB (loSARTAN, ValSARTAN). Renin inhibitor (aliskirin). D1 receptor agonist (fenolDOPam)
Term
What are the ABCDs of HTN therapy?
Definition
ACEI, ARB, alpha blockers; Beta blocker, CCB, Diuretic
Term
What is the general flow of HTN perscription?
Definition
Monotherapy, then add second drug (one of the first two drugs should be diuretic), then increase dose, then modify combination (but keep diuretic), then add additional drug. Remember that the drugs should have different targets and toxicities.
Term
List the thiazides
Definition
choloTHIAZIDE, hydrochloroTHIAZIDE, polyTHIAZIDE, chlorthalidone
Term
What are the non-thiazides of similar action?
Definition
Metolazone, indapamide
Term
Thiazides: SOA and MOA?
Definition
SOA = primarily the DISTAL tubule. MOA: reduces NACl (inhibits co-transporter) and therefore REDUCES WATER REABSORPTION
Term
Thiazides: ADME?
Definition
A: oral, D: M:requires active secretion into renal tubule via ORGANIC ACID PATHWAY E: kidney
Term
Thiazides: Side effects?
Definition
Dose related therefore use lowest effective dose. HYPOKALEMIC (ARRHYTHMOGENIC), hypochloremic, ALKALOSIS. hyponatremia, hyperglycemia, hyperuricemia (gout), increased Triglycerides and total cholestereal (LDL) therefore increased CV disease. Chronic use: impotence.
Term
Loop Diuretics: list
Definition
furosemide (lasix), bumetanide (bumex), torsemide (demadex), ethacrynic acid (edecrin)
Term
Loop diuretics: SOA and MOA
Definition
SOA: THICK ASCENDING LIMB of loop of Henle; MOA: INHIBITION OF K+, NA+ AND Cl- reabsorption (cotransporter).
Term
LoopDiuretics: ADME
Definition
A: oral, D: M: E: renal excretion. ACTIVE SECRETION VIA ORGANIC ACID PATHWAY into tubule is NECESSARY for therapeutic effects
Term
Compare Loop Diuretics to Thiazides
Definition
Loop Diuretics are more efficacious and faster acting but have a shorter uration than thiazides.
Term
Loop Diuretics: Side Effects
Definition
OVERZEALOUS TREATMENT (as in edema): Dehydration, hypotension, marked hypokalemic, hypochloremic, alkalosis
Term
Potassium-sparing diruetics: list and general info
Definition
Spironolactone (Aldolactone), Eplerenone (Inspra), Triampterene (Dyrenium), Amiloride (Midamor).
Term
potassium-sparer: SOA and MOA
Definition
SOA: late distal tubule and cortical collecting duct. MOA: generally decrease Na reabsorption more specifically: Competitive antagonist of aldosterone (spironolactone, eplerenone), Decrease membrane permeability to sodium (triampterene, amiloride).
Term
Compare Spirolactone to triampterene or amiloride
Definition
Spirolactone has slower onset (2-3 days) but longer duration of action and produces more diureses than triampterene or amiloride.
Term
Potassium sparer: side effects
Definition
HYPERKALEMIA. spironolactone gives steroid-like effects (gynecomastia, amenorrhea) that can be minimized by using eplerenone
Term
what are the most frequently used diuretics in chronic HTN? how does dose differ between treating HTN and edema?
Definition
thiazides. Flat dose reponse curve = dose for HTN <<< dose for edema
Term
If a patient has decreased renal function or resistant "psuedotolerance" due to vasodilators, what is the diuretic class of choice?
Definition
loop diuretcs.
Term
How and when are K+ sparers used?
Definition
Rarely used without another diuretic class. Used to PREVENT HYPOKALEMIA. may also provide SOME ADDITIONAL DIURESIS and MINIMIZES TENDENCY FOR ALKALOSIS. Exception: Spirolactone has been used effecitely as monotherapy.
Term
Describe the general sequence of action of diuretics in MOA
Definition
first decrease in extracellular fluid causes CO to decrease and TPR to increase (reflex). TPR decreases, CO approaches, but does not reach, pre-treatment levels. This is clled adaptation or reverse autoregulation. Natriuresis is essential for antiHTN effect.
Term
When would you prescribe a diuretic?
Definition
monotheraphy in uncomplicated HTN, as a second drug to attenuate the "psuedo" tolerance d/t salt and water retention that develops with other HTN drugs.
Term
List the types of agents altering Sympathetic tone
Definition
alpha receptor antagonists, beta receptor antagonists, competitive alpha and beta antagonists, agents affecting adrenergic nerve endings, agents working through central mechanisms, Alpha 2 agonists
Term
Do alpha receptor antagonists work on alpha 1 or 2?
Definition
alpha 1
Term
List the alpha1 receptor antagonists
Definition
Prazosin (minipres), Terazosin (hytrin), Doxazosin (cardura)
Term
alpha 1 receptor antagonist: MOA
Definition
MOA: reduces TPR --> increase in sympathetic (HR). Increase venous capacitance,. AFFECTS BOTH ARTERIES AND VEINS. Prazosin = functional vasodilator. TPR remains reduced. HR returns to control.
Term
a1 receptor antagonist: ADME
Definition
A: rapidly absorped D: M: liver E: ; note: usually takes several weeks to attain maximal decrease in BP
Term
a1 receptor antagonist: Side Effects
Definition
Salt and water retention (Tx with diuretic); First dose phenomenon (orthostatic hypotension, syncope) with 1st or increased dose. occurs more in patients on diuretics, BB, or volume depleted. Tx: maintenance dose/2, give at bedtime during start or increase of dose.
Term
a1 receptor antagonist: uses
Definition
monotherapy; +diuretic to minimize psuedotolerance; +diuretic+BB ; (functional vasodilator +diuretic + BB = TPR, NaCl & H20 rentetion and CO are all reduced.
Term
Which Beta blockers are B1 vs B1 and B2
Definition
A-M = B1 (cardioselective); N-Z= B1 and 2. They all end in -olol
Term
Intrinsic Sympothomimetic Activity
Definition
weak, partial agonist activity. Seen in acebutolol and pindolol
Term
What are the long acting BB?
Definition
atenolol and nadolol. Long activing because they have little to no liver metabolism
Term
What are the sequence of effects on CV by BB
Definition
1. decrease HR and contractility --> decreased CO 2. TPR increases 3. TPR returns to pre-treatment or decreases.||| Decrease in Renin Release --> less salt and water retention.
Term
MOA for BB
Definition
inhibition of renin release. depress CNS outflow (not all the same solubility into CNS). decreased neurotransmitter (NE) release. Adaptive changes to reduction in CO include a decrease in resistance. Reverse autoregulation.
Term
BB: ADME?
Definition
A: oral absorption D: M: first pass liver (except nadolol and atenolol). wide variation = titers necessary to individualize dose! E:
Term
BB: Side Effects?
Definition
B1: CHF, Bradycardia, AV block, B2: bronchospams, hypoglycemia, aggravates peripheral vascular disease. CNS: depression, nightmares, hallucinations. decreased HDL and increased triglycerides. withdrawal. Sexual dysfunction
Term
BB: uses
Definition
monotherapy. +diuretic. +diuretic and vasodilator (propranolol + thiazide + hdyralazine = decreased CO, NaCl & H20 retention & TPR)
Term
Labetalol
Definition
competitive alpha1, beta1, beta2 adrenoreceptor. Beta>alpha
Term
Low dose propranolol + low dose prazosin acts as
Definition
comptetitive antatonist of both alpha and beta receptors. propranolol is (b1>b2); prazosin is alpha1
Term
what are the CV effects of coptetitive antagonist of alpha and ß receptors?
Definition
decrease in CO (d/t b1 receptors), TPR (d/t alpha 1 receptors) and therefore BP.
Term
Side effects of both alpha and ß receptor antagonist
Definition
orthostatic hypotension
Term
How do you prescribe competitive antagonists of both alpha and beta receptors?
Definition
usually w/ a diuretic but can be monotherapy.
Term
what agent affects adrenergic nerve endings?
Definition
Resperine: depletes neuronal stores of all catecholamines (NE, EPI, serotonin, DA). both centrally and peripherally.
Term
MOA for Reserpine
Definition
binds irreversibly to neuronal storage vesicles and prevents accumulation and storage of catecholamines which leads to depletion of neurotransmitter stores.
Term
CV effects of Reserpine
Definition
decreases CO (HR & SV). Decreases TPR. Decreases sympathetic tone to the heart (decreased CO, and arteries (decreases TPR) and veins. orthostatic hypotension
Term
ADME of Reserpine
Definition
A: D: high lipid solubility = wide distribution includying CNS and long duration M: E:
Term
Side effects of Reserpine
Definition
Na+and H20 Retention (treat with diuretic). PS predominance results in diarrhea, cramps, increased gastric acid secretion. Sedation and severe DEPRESSION (CNS). orthostatic hypotension. sexual dysfunction.
Term
How should you prescribe reserpine?
Definition
NOT as monotherapy -- NEED To add a DIURETIC. Reserpine +diuretic +vasodilator = decreased TPR and CO, Decreased H20 and NaclRetention + decreased TPR)
Term
what kind of agents work primarily through central mechanisms?
Definition
alpha2 receptor AGONISTS
Term
List the alpha2 receptor agonists
Definition
Methyldopa. Clonidine
Term
Methyldopa CV effects
Definition
Decreases CO (HR &SV), concomitant with decrease in TRP. Decreases venous return (relaxes capacitance)
Term
MOA of methydopa?
Definition
"prodrug". Metabolized to alpha methyl NE in CNS. stimulation of alpha2 receptors in CNS leads to a decreased in sympathetic outflow.
Term
ADME of METHYLDOPA.
Definition
A: variable D: CNS storage of active metabolites M: minimal liver but must be activated in CNS E:
Term
Side effects of Methyldopa
Definition
postive Coomb's test (10-30%). hemolytic anemia (5% of +coombs). dry mouth. sedation. DECREASED MENTAL ACUITY
Term
Prescription pattern of methyldopa
Definition
REQUIRES DIURETIC or combination with DIURETIC+VASODILATOR. (decrease CO, TPR, Nacl+H2O retention, tpr). Drug of choice for persistent HTN during pregnancy.
Term
what is the Drug of choice in persistent HTN that develops during pregnancy. what are alternatives?
Definition
Methyldopa. Alternatives: hydralazine and labetalol.
Term
Clonidine and guanafacine MOA
Definition
Alpha 2 receptor agonist in CNS. Causes decreased in sympathetic outflow from CNS. Alpha2 stimulation of periphery of unknown importance
Term
CV effects of Clonidine and guanafacine
Definition
lowers BP by decreasing both CO (HR and SV) and TPR
Term
ADME of clonidine
Definition
A: 70-80%, available via patch; D: M: 50%; E:
Term
Side effects of Clonidine and guanafacine
Definition
withdrawal syndrome (increased sympathetic activity, rebound HTN) when clonidine is rapidly discontinued. sedation and dry mouth
Term
Pattern of use of clonidine and guanafacine
Definition
use with diuretic or diuretic+vasodilator.
Term
first dose phenomenon is associated with what HTN med?
Definition
alpha1 receptor antagonists, especially in patients who are taking diuretics, beta blockers or who are already volume depleted.
Term
Cardio Farm II
Definition
https://spreadsheets.google.com/ccc?key=0Ar1HwrS70Eb7dEpXOGU4OEhMN3hyaHE1Z3c2T20tSUE&hl=en&authkey=COSU8ekC
Term
List the vasodilators. How are they usually used?
Definition
Hydralazine (apresoline). Minoxidil (loniten). CCBs. ACE-I. ARB. Renin inhibitors. usually used in 3 drug combination except CCBs that can be used alone
Term
Hydralazine MOA,
Definition
MOA: direct acting smooth muscle (SOA) relaxant. 1º effects resistance vessels (arteries) little/no effect on capacitance vessels (veins).
Term
Hydralazine CV effects
Definition
BP increased due to reduction in TPR. Reflex increase in HR and SV, renin release, and pseudotolerance
Term
Hydralazine ADME
Definition
A: absorbed well D: M: intestine and liver = rapid therefore, metabolite may be effector. Need to see if patient is a fast or slow metabolizer and adjust dose accordingly
Term
Side effects of hydralazine
Definition
drug induced LUPUS SYNDROME, especially in SLOW ACETYLATORS (more than 200 mg/day)
Term
Use of hydralazine
Definition
NEVER USE ALONE (reflex activation of sympathetic system d/t Na and H2O retention. usually +diuretic+sympathetic depressant. Hydralazine+diuretic+propranolol is effective (decrease TPR, NaCl/H2Oretention, CO). Used in elderly as second agent (+diuretic) d/t blunted baroreceptor reflex. safe alternative to methyldopa in prego HTN
Term
minoxidil (Loniten) MOA and CV effects
Definition
MOA: arterial smooth muscle relaxant; CV: decreases TPR then BP resulting in tachycardia so need to pair with sympathetic depressant. extensive salt and water retention (treat with loop diuretic)
Term
Minoxidil (Loniten) ADME and Side effects
Definition
A: good, D: may accumulate in smooth muscle, prolonging duration M: first pass liver metabolism. active metabolites. Side effects: hypertrichosis and hyperpigmentation (active ingredient in rogaine). pericardial effusions in patient with renal insufficiency.
Term
uses of minoxidil
Definition
RESERVED for patients with SEVERE HTN who are resistant to other regiments. +LOOP DIURETIC+BETA BLOCKER. (decrease TPR, Decrease retention, decrease CO)
Term
What are the three distinct groups of CCBs?
Definition
Phenylalkylamines (verapamil), Benzothiazepines (diltiazem), Dihydropyridines (end in dipine)
Term
CCB MOA
Definition
decrease membrane conducance through L-type, potential dependent (or voltage gated), calcium selective channels in vascular smooth muscle (artery>>>vein) and/or cardiac muscle leading to decreased TPR d/t vascular relaxation and/or myocardial depression (Decreased CO)
Term
Explain the cardiovascular pharmacodynamis of the CCB
Definition
In the heart (SOA): inhibition of Ca++ entry (MOA) results in negative inotrpic, chronotropic and dromotropic actions. In blood vessels (SOA), inhibition of Ca++ entry (MOA) results in vasodilation, primary site is artery>>>veins.
Term
Does verapamil or diltiazem have greater myocardial depressant effects?
Definition
verapamil = phenylalkylamine
Term
Rank the effect of CCB types on blood vessels from greatest to least.
Definition
nifedimpine (DHP) >verapamil (phenylalkylamine) =diltiazem (Benzothiazepine)
Term
What are the CV effects of CCBs?
Definition
reflex tachycardia that resolves over several weeks as BP decreases. ( not as much with diliazem or verapamil b/c they are myocardial depressors). Not as much Na+ retention. May have some diuretic protperties. Can be used as monotherapy in patients with low renin or AA patients
Term
ADME for CCBs
Definition
A: effective orally (verapamin=nifedipine>diltiazem). D: highly bound to plasma proteins M: first pass liver, some active metabolites (verapamil>diltiazam) short half life so either give frequently or use extended release formulation E: by Kidneys
Term
Side effects for CCBs
Definition
related to therapeutic effects: vascular effects seen most with DHPs (hypotension, dizziness, flushing, reflex tachycardia, peripheral edema). Cardiac: negative inotropism --> myocardial depression (CHF). SA or AV nodal depression --> decreased HR and conduction blocks (arrhythmias). Cardiac side effects seen more with verapamil and diltiazem. GI: constipation with verapamil.
Term
Uses of CCBs in HTN
Definition
monotherapy; +diuretic; +diuretic+sympathetic depressant other than an alpha blocker. (decreased TPR+decreased NaCl&H2O retention+decreased CO) or (decreased TPR and CO + decreased NaCl and H2O retention)
Term
ACE-Inhibitors: MOA
Definition
inhibit angiotensin converting enzyme thereby inhibit formation of Angiotensin II (vasoconstrictor). prolong action of bradykinin (vasodilator) because ACE breaksdown braydikinin. Reduced AII = reduced aldosterone secretion --> less salkt and water retention.
Term
What are the CV effects of ACE-Inhibitors?
Definition
reduction in BP d/t decreased TPR "functional vasodilator" with less reflex tachycardia or water retention. Not effective as monotherapy in AA patients.
Term
What are the ADME of ACE-Inhibitors?
Definition
A: orally effective M: liver, some are prodrugs (enalapril) E: Kidney
Term
Side effects of ACE-Inhibitors
Definition
loss of sense of taste, hypotension, hyperkalemia, neutropenia and proteinuria with renal disease, persistent non, productive cough with crhonic use, DO NOT SURE WHEN PREGO. angioedema, rash.
Term
Uses of ACE-inhibitors
Definition
monotherapy; +diuretic; +diuretic+sympathetic depressant. (decrease TPR, and salt and water retention) or (decrease TPR, salt and water, CO and/or TPR)
Term
ARBs: MOA and SOA
Definition
MOA: blocks binding of angiotensin II to type I angiotensin II receptors. SOA: blood vessels, heart and kidney
Term
List some ARBs
Definition
all end in -sartan. Losartan, candesartan...
Term
List some ACe-Inhibitors
Definition
all end in -PRIL. Captopril (Capoten), enalapril (Vasotec), lisinopril (prinvil)
Term
ARBs: CV effect
Definition
decrease in BP d/t reduced TPR. Relaxes BOTH resistance and capacitance vessels (functional vasodilator). Less salt and water retention because aldosterone secretion is reduced.
Term
ARBs: side effects
Definition
lower incidence of, hyperkalemia, and cough than in ACE-inhibitors. neutropenia and proteinuria with renal disease, DO NOT SURE WHEN PREGO. angioedema, rash. loss of sense of taste, hypotension
Term
ARB: Uses
Definition
monotherapy; +diuretic; +diuretic+betablocker
Term
Aliskirin (Tekturna): class and MOA, ADME and Uses
Definition
Renin inhibitor = vasodilator. MOA: inhibits conversion of angiotensinogen to angiotensin I. ADME: orally effective. USE: in combo with diuretic and an ARB (valsartan)
Term
What situations require a prompt reduction in BP?
Definition
malignant, accelerated HTN; HTN-encephalopathy; HTN-complicated by stroke; dissecting aortic aneurysm; heart failure and cerebrovascular insufficiency; eclampsia; pheochromocytoma or MAO-inhibitor induced HTN
Term
What is the primary concern with HTN urgencies.
Definition
prevent target organ damage.
Term
what is a caveat in lowering BP in patients with atherosclerosis?
Definition
don't want to lower it to fast because patients are prone to cerebral or coronary insufficiency
Term
Nitroprusside: MOA, SOA and CV effects?
Definition
MOA: Direct acting vascular (SOA) relaxant effecting both resistance (afterload) and capacitance (preload) vessels [balanced effort]. Metabolized locally to NO. CV: decreased TPR, decreased CO d/t decreased venous return. Can cause reflex tachycardia. Titrate to desired BP response
Term
Nitroprusside ADME and Side Effects
Definition
A: NOT ORALLY, IV ONLY! rapid onset and offset. M: metabolized to cyanide in RBC (methylglobinemia, infrequently: cyanide toxicity =acutely). Cyanide metabolized to thiocynate in liver (thiocynate toxicity develops in >72 hrs)
Term
What is the drug of choice in emergencies associated with acute MI or LV failure?
Definition
Nitroprusside. Alternatives: IV nitroglycerine and IV labetalol
Term
What is diazoxide (hyperstat), when it is it used and how does it work?
Definition
Non-diuretic, thiazide derivative. Used IV in emergency HTN situations but NOT A FIRST CHOICE. MUST COMBINE WITH DIURETIC for extended use. MOA: direct relaxation of resistance vessels ONLY (SOA). capacitance vessels are uneffected. therefore CV effect is to decrease TPR and therefore BP. Results in reflex tachycardia and salt and water retention.
Term
ADME and SIde effects of Diazoxide (Hyperstat)?
Definition
A: orally effective but used IV only in blolus or continuous drip.D: 90% bound to albumin M: first pass liver. Side effects: FLUID RETENTION. hyperglycemia, hyperuricemia. NOT A FIRST CHOICE
Term
what are examples of non-selective alpha receptor blocking agents? Side effects?
Definition
phentolamine (regitine) and phenoxybenzamine (dibenzyline). Used in HTN criss associated with EXCESS OF CIRCULATING CATECHOLAMINES (MAO inhibitor, pheochromocytoma, clonidine withrawal). Pair with a beta blocker to prevent excessive cardiac stimulation. Side effects: reflex tachycardia, orthostatic hypotension, nasal congestion, GI distress and sexual dysfunction.
Term
What is the MOA of the emergency HTN medication that is contraindicated in patients with glaucoma?
Definition
Fenoldopam is a selective, peripheral dopaminergic (D1) receptor agonist given IV. Lowers pressure while maintaining or increasing renal perfusion pressure.
Term
What agent is used to decrease BP in order to minimize bleeding during surgery?
Definition
Trimethaphan (Arfonad). MOA: non-depolarizing ganglionic blocking agent (comptetitive ACh inhibitor at nicotinic receptors (sympathetic depressant). Results in decreased CO and TPR. Orthostatic effect on BP causes more dramatic effect to be seen if elevate head of bead. ADME: sulfonium compound (doesn't cross lipid membranes) so IV only. NOT USED MUCH EXCEPT FOR: DISSECTING AORTIC ANEURYSM OR SURGERY.
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