DRUG MECHANISMS and indications (final) Flashcards
PDE-5 Inhibitor; sustains the vasodilatory effects of nitric oxide-dependent synthesis of cGMP
sildenafil moa
indications for sildenafil
ED and pulmonary arterial HTN
Inhibits vitamin K-dependent coagulation factor synthesis (II, VII, IX, X, proteins C and S)
coumadin moa
indication for coumadin
anticoagulation
Binds to Antithrombin-III and accelerates its activity, inhibiting thrombin and Factor-Xa
enoxaparin moa
indication for enoxaparin
post op DVT prophylaxis, unstable angina
Prodrug: metabolized to active metabolite by the CYP450 enzyme CYP2C19
Irreversible inhibition of platelet ADP receptors which normally trigger platelet activation and aggregation via downstream activation of the GP llb/llla complex
clopidogrel moa
indication for clopidogrel
acute coronary syndrome, thrombotic event prophylaxis
- Fab Fragment: a chimeric human-murine mAB
- Binds to the GP llb/llla receptor of human platelets and inhibits platelets aggregation
- Binds to the vitronectin (αvβ3) receptor on platelets and vessel wall endothelial and smooth muscle cells
moa for abciximab
indication for abciximab
An adjunct to percutaneous coronary intervention (PCI) for the prevention of cardiac ischemic complications, Unstable Angina
Competitively inhibits HMG-CoA Reductase which is responsible for an early, rate-limiting step in cholesterol biosynthesis
Increases hepatic LDL receptors, enhancing catabolism
atorvastatin moa
atorvastatin indication
hyperlipidemia/cvd prevention
Stimulates nuclear receptor PPAR which modulates transcription of insulin sensitive genes in liver, muscle and adipose tissue
Enhances HDL production; inhibits triglyceride synthesis and stimulates catabolism of triglyceride-rich lipoproteins
fenofibrate moa
indications for fenofibrate
hypertriglyceridemia and hypercholesterolemia
Inhibits lipolysis in adipose tissue, resulting in reduced hepatic VLDL synthesis and production of LDLs in the plasma
nicotinic acid moa
indication for nicotinic acid
hypertriglyceridemia
hypercholesterolemia
mixed dyslipidemia
Biguanide-based; activates AMP-activated protein kinase (AMPK) which in turn suppresses hepatic gluconeogenesis & intestinal glucose absorption; increases insulin sensitivity
metformin moa
indication for metformin
DM 2 and PCOS
Stimulates pancreatic islet beta cell insulin release
Actions involve binding to an ATP-dependent K+ channel: blocked efflux leads to depolarization, Ca++ release and insulin vesicle effusion
moa for glipizide
indication for glipizide
DM 2
A thiazolidinedione (aka glitazone) insulin sensitizer selectively stimulates nuclear receptor PPAR which increases insulin sensitivity in liver, skeletal muscle and adipose tissue
MOA of pioglitazone
indication of pioglitazone
dm 2
sitagliptin moa
Inhibits dipeptidyl peptidase-4, slowing incretin breakdown, increasing insulin synthesis/release, decreasing glucagon levels
indiaction for sitagliptin
dm2
Slow release, micro-crystallized rDNA insulin analog for stable day-long blood sugar regulation to be used in post-prandial combination with fast acting insulin
moa for insulin glargine
Irreversibly inhibits gastric parietal cell H+-K+-ATPase, thereby inhibiting gastric acid secretion
esomeprazole moa
indication for esomeprazole
GERD
Gastric ulcer prophylaxis (nsaid associated)
hypersecretory disorders
h. pylori infection
Selective antagonism of gastric parietal cell H2 receptors
cimetidine moa
cimetidine indications
gerd
peptic ulcer
dyspepsia
Synthetic T4 (tetra-iodothyronine)
levothyroxine
indication for levothyroxine
hypothyroidism
Binds to estrogen receptors, developing and maintaining female sex characteristics and reproductive systems
estrone moa
estrone indication
Menopause, Breast Cancer, Prostate Cancer, Osteoporosis prevention
Having a strong affinity for Ca2+, these drugs accumulate in bone where, upon ingestion by osteoclasts, they inhibit the HMG-CoA reductase pathway and leads to cell death, reducing bone resorption and turnover (bisphosphonate)
alendronate moa
indication for alendronate
Osteoporosis
Paget’s Bo Dz
Acts as a folic acid analogue, inhibits DHFR, thus preventing formation of FH4
Inhibits lymphocyte proliferation
methotrexate moa
indication for methotrexate
RA
psoriasis
Choriocarcinoma