binds LDL receptor->internalization->lysosomes

intracellular cholesterol

inhibits HMG coA reductase

activates ACAT (esterifies->storage)

inhibits LDLr gene expression

fx as vitamin after conversion to NAD

anticholesterol require much larger dosage than vitamin effect dosages

30-40% changes in LDL, HDL, and triglycerides

-reduces TG synth in liver-> lower VLDL production

-decr lipolysis in adipose, reduces FFA trans to liver

-reduces hepat clearance of HDL-ApoA-I, raises HDL-C

t: hepato, hypergly, hyperuric, myopathy, tachyarry,

triglyceridemia, lowers VLDL, varies LDL-C, moderate incr HDL-C,

 synthetic ethyl chlorophenoxyisobutyrates

PPARa (peroxisome proliferator actived receptor)

incr LPL synth

inh apoCIII expression->incr LDL clearance

stim apoAI and apoAII which incr HDL

t: 2nd gen good, potentiate oral coagulants by competing for albumin, increase lithogenicity of bile->gall stones

cholestyramine, colestipol, colesevelam

reduce LDL-C 25%

highly positive charge->bind negatively charged bile acids

t: increase TG levels, bloating, dyspepsia, interfere with cardiac glycoside and coumadin absorption, and fat vit.

reduced free cholesterol in hepatocytes->SREBP->incr LDLr transcription and decr degredation

decr synth of chol->decr VLDL

t1/2 1-4, atorva and rosuva much longer, chol synth mainly 12-2am--take in evening

inhibitors of statin metabolism: age, hepatic/renal dys, perioperative, hpothyr, diabetes, only use at 25%max

t:myopathy (rhabdo)

aldo receptor blockers, gynecomastia

hyperK with- ARB, b-blocker, ACEI, and HF

a2 agonist,

maint Renal BF,  fall in renin, fluid retention, dcreased alertness, sedation, dry mouth, rebound hypertension

l: high a blockade, hypertensive emergency

se: ortho hypo, scalp itching, bronchospasm, hepatotox

c: some a blockade, increases NO production,

less lipids/insulin effects

prevents oxidation of NO

se: reflex symp, lupus, nonspecific (anorex, n/v)

opens SM ATP-senstive K channels

se: hirsutism, pericard effusion

if lipophilic- enter brain-> reflex sympathetic activation

interact with L-type voltage gated CA channels

nondihydropyridines- diltiazem (IV form), verapamil- rate slowing, vasodilation, decr contractility, inh av conduction, verapamil- constipation, av block, less with diltiazem

dihydropyridines- (vasoselective) dilate coronary, arterioles (nifedipine (older) has some contractility effects), amlodipine, felodipine, isradipine- less cardiac

increase bradykinin, increase tPA, suppress endothelin, reduction in ox stress, blunts increased sympathetic drive

se:hyerK from decr perfusion/decr aldo, hypogly from incr insulin sens, anemia-int w.EPO

fetal injury and death, angioedema, bradykinin->cough

captopril- sulfa->taste interruption, rash, leukopenia

as AII goes up-> AT2 stim->hypertrophy/antiangiogenic

losartan- uricosuric

valsartan- enhances ins sens

telmisartan- red glu/ins/TG

tox: decr dgf, hyperK, hypotension

inward K, inh of Ca->hyperpolarization

more in AV than SA node

10s t1/2

Ia, sodium ch block, hypotension (ganglionic blocking), lupus->limited to in-patient

n-acetyl has class 3 properties

IA, na and k blocking

afib, brugadas, long QT

polyarythmia, quinidine syncope

IA, direct vagal block and VTach

urinary retention, blurred vision, worsened glaucoma

IB, works fast and only at diseased tissue, works in ventricular myocardium, decreases automaticity

Vtach, neurotoxicities if more than 24-48 hrs

mexiletine- oral lidocaine.

IC, potent Na blocker, prolonged atrial refractory

contraind in CAD or LV dysf

uses: PVC, AFib

dronaderone: no pulm tox, no iodine->no thyroid tox

k, na, ca, beta blocking, vasodilation->hypotension

k blocker (class III), prolongs AP, ERP

b-blocker, urine excretion

pure IKr blocker (phase 3)

good bioav, renal excr,

init in hospital->proarrythmia, afib

IKr blocker, activates slow inward Na,

more atr flutter than AFib

p2y12 adp receptor blocker

risk for fatal bleeds

limited to young fat people with no pos history

increases platelet cAMP

inhibits adenylate cyclase, uptake of adenosine, inhibits phosphodiesterase

can enhance exercise induced ishcemia

metoprolol, atenolol, bisoprolol- 1 selective

propran, carved

demonstrated HF benefit: biso, carved, metop

removes wall stress by reducing preload via venous relaxation

contr: hypertrophic myopathy, aort sten, hypotens, viagra

b1 agonist

at low: b2 vasodilation

at high: alpha constriction

does not bind Dopamine receptors->no NE release

phosphodiesterase IIIa inh, incr [cAMP]

increased inotropy, chronotropy and lusitropy (relaxation), vasodilation

recombinant bnp

no significant data on benefit

disrupt heme poly to hemozin-> oxidative damage

chloro- pro/acute, crosses membranes

 meflo- " neurotox, used in resistance?

quinine/quinidine- only parenteral in US

pyrimethamine

chloroguanide

sulfonamides

DHFR inh

proguanil combo with atovaquone

depolarizes parasitic mito, inhibits electron chain

proguanil combo

used in chloroquine resistance (except vivax)

lumefantrine or benflumetol- aminoalcohol class

artemether, artesunate

sim to thapsigargin, inhibits SERCA in falciparum

inhibits exoerythrocytic division

quinoline-quinone intermediates->ox membrane

only drug for latent infections

NOT in G6PD def

schistosomiasis

increases perm to Ca

contraction and paralysis of worm vasculature->

outer membrane breaks down->

immune recognition