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PHM - Exam 4 - Cardiac Drugs
N/A
43
Medical
Graduate
06/20/2013

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Term
bile-acid binding resins
Definition
dyslipidemia

remains in GI---> binds bile acids---> increased HEPATIC BILE A. SYN.---> uses up HEPATIC CHOL.---> more LDL R's---> more LDL extracted from blood

adjunctive therapy for HYPERCHOLESTEREMIA

+ STATINS to blk chol. synth.; blks absorption of others
Term
Statins
Definition
dyslipidemia

blk HMG-CoA reductase---> more LDL Rs---> LARGE removal of blood LDL (more than bile acid-binding resins); and additional therapeutic benefits

primary and secondary prevention of CAD;

MYOPATHY;
Term
Chol. Absoprtion Blkrs (Ezitimibe)
Definition
dyslipidemia

blks NPC1L1-transport of chol. in JEJUNUM---> decreased supply to liver---> increase in hepatic production, LDL-R expn---> more removed from bld

absorption inhibited by BILE A-BINDING RES's
Term
Niacin
Definition
"nia-ah - thin and skinny"---> dyslipidemia blks adenyl cyclase---> blks lipase---> blks lipolysis of TG's---> less FFA's to liver; blks esterification of FFA's--> blks hepatic FFA synth; higher HDL-C; macrophage lipid scavenging; sustained release---> safest HIGHER HDL Tx: HYPERTRIGLYCERIDEMIA; elevated LDL; low HDL SE: HEPATOTOXCITY; INSULIN RESISTANCE; GOUT; + statin = MYOPATHY;
Term
Fibrates
Definition
"nia-ah eats fiber to stay skinny"---> dyslipidemia bind PPAR-alpha (txn factor in liver and ("brown rice has a lot of fiber")---> brown adipose tissue)---> FFA oxidation (= LESS TGs); lipoprotein lipase synth; more HDLs LESS TG's Tx: HYPERTRIGLYCERIDEMIA associated with METABOLIC SYNDROME SE: urticaria, hair loss, + statin = MYOPATHY; additional benefits: FIBRINOLYSIS, less coagulation
Term
Nitrates
Definition
angina
ACUTE DECOMPENSATION HF (IV/sublingual)

release NO---> cGMP production---> vasorelaxation, blks platelet aggregation---> DECREASED PRELOAD and AFTERLOAD

+ Direct arterial vasodilator (HYDRALAZINE)

Tx: sublingual/IV = treatment; oral = prophylaxis; decrease myo. O2 demand: less venous contraction---> less preload, wall stress; less arterial contraction increase myo O2 supply: less coronary aa contraction---> less spasms

SE: headache; HYPOTENSION}---> worse with SILDENAFIL (ED drugs)---> blk cGMP metabolism; TOLERANCE
Term
beta-blockers
Definition
angina

lower heart rate---> lower arterial bld pressure(decrease O2 demand); more time in DIASTOLE---> more coronary bld flow (increased O2 supply);

Tx: oral; prophylaxis of STABLE angina; less mortality post MI

SE: BRONCHOCONSTRICTION; HYPOGLYCEMIA; DEPRESSION, nightmares---> worsening of symptoms from abrupt withdrawal; NEVER with cardiac dysunction or obstructive pulm. disease
Term
Ca2+ channel blockers
Definition
angina

bind alpha-1 subunit of L-type channels ("ine"---> effect on bld. vessel)---> blk Ca2+ movement; SLOW channel recovery---> decreased O2 demand: slow HR and contractility; less contractility; increased O2 supply:less aa contraction

tx: oral; prophylaxis of stable AND variant angina

SE: HYPOTENSION, flushing, headache, EDEMA; NEVER with beta-blockers
Term
Ranolazine
Definition
STABLE angina "runner aren't slow"---> blck late SODIUM current---> no increase Na+ and Ca2+ in cell---> less wall tension; blk FFA ox.n. Tx: oral; "runners have stable legs"---> prophylaxis of STABLE angina (reduces O2 demand)
Term
Aspirin
Definition
anti-platelet

COX-1 acetylation---> blks TxA2 synth in platelets---> less aggregation (5-8% pts resistant to this effect); reduces MORTALITY and occurrence of MI

Tx: LOW DOSE (less risk of bleeding); NEVER with NSAIDs (cause they impair response)

SE: bleeding, allergies...especially the 5-8% that are resistant
Term
ADP Inhibitors
Definition
anti-platelet

INSTEAD of Aspirin; blk ADP binding to platelets---> less aggregation; LARGE reduction in MORTALITY;

Tx: oral + Aspirin

SE: neutropenia; THROMBOTIC THROMBOCYTOPENIC PURPURA;
Term
GP IIb/IIIa receptor inhibitors
Definition
anti-platelet

blks platelet x-linking---> less aggregation; lower MORTALITY

Tx: IV, SHORT duration, + aspirin

SE: THROMOCYTOPENIA; bleeding
Term
Heparin
Definition
anticoagulant

blks coagulation proteases via ANTITHROMBIN---> blks coagulation factors; MAJOR drop in mortality

Tx: IV/SQ

SE: bleeding, thrombocytopenia
Term
Fondaparinux
Definition
"become attached to fondu, so binds right away"---> anticoagulant binds antithrombin---> blks factor Xa; similar reduction in MORTALITY as that of HEPARIN Tx: once-daily; "would like to eat "fond"u w/out monitoring"---> NO monitoring needed SE: less adverse than HEPARIN;
Term
Direct Thrombin Inhibitors
Definition
anticoagulant

binds and blks thrombin

Tx: IV; replaces HEPARIN if prone to THROMBOCYTOPENIA
Term
Fibrinolytics
Definition
MI: Fibronolysis binds fibrin---> activates BOUND plasminogen (region spec.)---> recanalization of occlusion---> flow restored, infarct SIZE - REDUCED Tx: IV; most useful to DIABETICS; least useful to pts with HTN and elderly SE: + heparin = STROKE
Term
Analgesics
Definition
MI - Analgesics

u-type R stimulation in CNS---> less neural effects and ANS activity---> VESSEL RELAXATION---> reduced O2 demand

Tx: IV as needed

SE: hypotension, depression of resp., vomiting
Term
Renal Angiotensin Inhibitors (ACE Inhibitors and ARBs - Angioten. Receptor Blkrs)
Definition
MI

blck ACE or blk angiotensin access to AR--> vessel relaxation---> less SYMPATHETIC activity---> more Na+/H2O secretion---> less VENTRICULAR REMODELING--> lower MORTALITY---> best for ELDERLY, hx of MI, and reduced ventricular function (e.g. CHF)

Tx: last resort

SE: HYPOTENSION, cough
Term
Oral Anticoagulants (Warfarin)
Definition
secondary prevention of MI

blk formation of reduced Vit. K---> no coagulation factors---> slower growth of existing thrombi, blk synth of new ones---> reduces MORTALITY

Tx: several days for effect, response monitored via PROTHROMBIN TIME; NEVER with high Vit. K diet ("just eat the drug, not Vit. K"); more effective with LIVER DISEASE

SE: skin necrosis, MANY DRUG INTERACTIONS
Term
Dabigatran
Definition
secondary prevention of MI

("dabig shit, so blocks active site itself") reversible blk of thrombin active site---> ditto as oral anticoagulants, prevents STROKE in ATRIAL DIFIBRILLATION

Tx: "dabig shit so"--> NO monitoring;

SE: less than Warfarin, rapid action, less interactions
Term
Class 1A
Definition
tachyarrhytmias

blk Na+ and K+ channels---> less conductance and automaticity (LONGER QRS); more refractoriness (LONGER QT); muscarinic antagonist

Tx: WIDE-SPECTRUM; against RE-ENTRY conduction or ECTOPIC automaticity; VENTRICULAR arrhythmias;
Term
Class 1B
Definition
tachyarrhytmias

blk Na+---> lower conductance---> slightly shorter QT

Tx: LONG QT SYNDROME; against RE-ENTRY conduction or ECTOPIC automaticity; best in patient with high HR, w/ ISCHEMIC or DAMAGED tissue
Term
Class 1C
Definition
tachyarrhytmias

blk Na+ channels---> lower conduction---> INCREASE QRS; decreased ventricular contractility

Tx: ventricular arrythmias from re-entry conduction; atrial arrhythmia
Term
Class 2
Definition
tachyarrhytmias

blks beta-adrenergic receptors---> lower AV conduction---> LONGER PR

Tx: during sympathoexcitatory state; VENTRICULAR RATE CONTROL; long QT syndrome; DECREASES SUDDEN DEATH post MI
Term
Class 3
Definition
tachyarrhytmias

blks K+ channels---> longer refractory---> LONGER QT, shorter PR

Tx: re-entry of ectopic; after CARDIAC RESUSCITATION; LEAST likely to cause arrhythmias;
Term
Class 4
Definition
tachyarrhytmias

blks L-type Ca2+ channels---> same ECG as Class 2 (less AV conduction longer PR)

Tx: Ventricular rate control
Term
Digoxin
Definition
HF
tachyarrhytmias

blks N+-K+-ATPase---> more intracellular Na+ and Ca2+---> increased CONTRACTILICY;
lowers AV conduction---> longer PR

Tx: therapeutic rate control

SE: overdose tx: ANTIBODIES or K+
Term
Adenosine
Definition
tachyarrhytmias

more K+ opening---> lower AV conduction---> longer PR; lower sinus node rate; blks adenylate cyclase---> less cAMP

Tx: IV; SHORT lasting;
Term
Thiazide Diuretics
Definition
HT
CHRONIC STABLE HF (oral)

reversible blk of Na+/Cl- on luminal DISTAL tubule cotransporter; MORE ion and water excretion---> CO drops---> lower PRELOAD; LIMITED by RAA (renin-angiotensin-aldosterone) system

SE: higher uric acid and glucose---> NEVER for pt with GOUT or DIABETES
Term
Loop Diuretics
Definition
HT
CHRONIC HF (oral) and Acute Decompensation (IV)

reversible blk of Na+/K+/2Cl- transporter of ascending LOOP--->increased renal secretion of ions and H2O; VASODILATION---> decrease PRELOAD; lowers EDEMA limited by RAA

Tx: not as effective as thazide diuretics---> so for resistive HT

SE: metabolic alkalosis (renal excretion of H+); limited by decreased kidney perfusion and eventual reduction in delivery to kidneys
Term
K+-sparing Diuretic
Definition
HT HF blks luminal Na+ channels of distal and collecting duct---> increased ion and H2O secretion SE: hyperkalemia
Term
Aldosterone Antagonists
Definition
HT SEVERE CHRONIC HF---> INCREASED SURVIVAL ditto as K+ sparing diuretics; "aldos guys trying to get into your heart"---> competitive ALDOSTERONE RECEPTOR ANTAGONIST in kidney and heart---> blks VENTRICULAR REMODELING Tx: beneficial for HT pts with HEART FAILURE; SE: hyperkalemia; GYNECOMASTIA, IMPOTENCE, manstrual irregularities;
Term
Beta-Adrenergic Blockers
Definition
HT
CHRONIC STABLE HF (oral)--->INCREASED SURVIVAL

blocks beta-1---> lower CO, lower renin release--->blks VENTRICULAR REMODELING

SE: MENTAL: depression, nightmares; abrupt withdrawal is bad
Term
Ca2+ Channel Blockers
Definition
non-competitive blk of L-type Ca2+ channels---> less arteriolar contraction---> lower TPR; good for STROKE pts; OKAY for pts using NSAIDs

SE: well tolerated
Term
Renin-Angiotensin Inhibitors
Definition
HT
HF (SYSTOLIC Dysfunction)---> INCREASED SURVIVAL

blks ACE and blks AT-1 type angiotensin tissue receptor---> vessel relxation; less sympathetics; increased renal SODIUM/H2O SECRETION; lower TPR---> blks VENTRICULAR REMODELING

Tx: protection against NEUROPATHY in diabetics and CAD in HF pts

SE: well tolerated
Term
Renin Angiotensin Inhibitors
Definition
blks renin---> less angiotensin 1 and 2 formation; relaxed vessels; less sympathetics; renal Na+/H2O secretion; lower TPR

Tx: better + diuretics

SE: NEVER in PREGNANT women
Term
Alpha-adrenergic Blockers
Definition
HT

blks alpha-1---> vessel relaxation---> lower TPR

Tx: TOLERANCE is prob; causes fluid RETENTION---> so + diuretic

SE: hypotension
Term
Centrally Acting Sympatholytics
Definition
activates alpha-2- adrenergcs in BRAINSTEM---> LOWER SNS activity; lower CO and TPR; METHYLDOPA: "sympathetic towards moms"---> okay in pregnant women Tx: for resistant HT SE: sedation, dry mouth, BRADYCARDIA
Term
Direct Arterial Vasodilators
Definition
HT
HF (PROLONGED SURVIVAL with + nitrates)

unknown mech.---> relaxed arterioles---> lower TPR---> decreased AFTERLOAD---> decreased cardiac O2 demand; activate SNS and RAS so + diuretic and beta-blocker!

+ NO

SE: tachycardia, edema, HAIR GROWTH (MINIDOXIDIL)
Term
Phosphodiesterase Inhibitors
Definition
ACUTE DECOMPENSATED HF blks phosphodiesterase--->"phos-sy about camping"---> more cAMP in SR---> more intracellular Ca2+---> increased contractility; vessel relaxation---> reduced filling pressures Tx: "phos-sy supports for beta girls"---> for pts on beta-blockers in need of INOTROPIC SUPPORT SE: hypotension, arrhythmias; chronic use---> decreased survival
Term
Vasopressin Antagonists
Definition
ACUTE DECOMPENSATED HF

blks V2 and V1a renal receptors in collecting DUCTS and VSLS---> higher Na+ plasma concentration; REDUCED FILLING PRESSURES

Tx: correct HYPONATREMIA

SE: dry mouth and thirst
Term
Nesiritide
Definition
ACUTE DECOMPENSATED HF B-type natriuretic peptide---> "nesi smoothe talking"---> vessel relaxation---> LOWER filling pressures; "nesi gets blood pumping"---> increased CO SE: hypotension; "nesi creating the mood"--->  INCREASED PLASMA CREATININE
Term
Beta-agonists
Definition
HF (ACUTE DECOMPENSATED)

INOTROPY---> MORE CO; less filling pressure

SE: Tachyarrhytmia
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