Bone/Obesity/Diabetes/Lipids Flashcards
Atorvastatin
MOA:
HMG-CoA reductase inhibitor
Clinical uses:
hyperlipidemia, coronary artery disease, acute coronary syndrome
Toxicity:
myopathy, hepatic dysfunction
Extra info:
effective at night, long duration of action
Evolocumab
MOA:
PCSK9 inhibitor, increases the number of cell surface LDL receptors
Clinical uses: hyperlipidemia, coronary artery disease, acute coronary syndrome
Toxicity:
myopathy, nausea, cognitive effects
Extra info: monoclonal antibody, 2x month SC injection, price ($$$)
Gemfibrozil
MOA:
PPAR-α agonist
lower TG and raise HDL
Clinical uses:
hypertriglyceridemia, dysbetalipoproteinemia
Toxicity:
myopathy, hepatic dysfunction
Extra info:
combine with statins
Colestipol
MOA:
bile acid binding resin
Clinical uses:
primary hypercholesterolemia, high LDL
Toxicity:
GI effects
Extra info:
combine with statins
Ezetimbe
MOA:
inhibits NPC1L1 cholesterol transporter
Extra info:
primary hypercholesterolemia, high LDL
Toxicity:
GI effects, hepatic dysfunction
Extra info:
combine with statins
Niacin
MOA:
diacylglycerol acyl-transferase 2 inhibitor, GPCR 109A agonist
inhibits production of VLDL and delays HDL clearance
Toxicity:
primary hyperlipidemias, high LDL/VLDL
Toxicity:
flushing, hyperuricemia, pruritus, diabetes, gout
Extra info:
combine with statins, bile acid binding resin
Glipizide
MOA:
K+ channel blocker in pancreatic beta cells, increases insulin secretion
Clinical uses:
Type 2 diabetes
Toxicity:
hypoglycemia, weight gain
Extra info:
oral
Metformin
MOA:
decreases hepatic gluconeogenesis, molecular mechanism not understood
Clinical uses:
Type 2 diabetes, polycystic ovarian syndrome
Toxicity :
GI disturbances
Extra info:
oral
Pioglitazone
MOA:
PPAR- agonist
Clinical uses:
Type 2 diabetes
Toxicity:
fluid retention, anemia, weight gain, myocardial ischemia risk, bone fractures in women
Extra info:
oral, increases transcription of genes involved in carbohydrate and lipid metabolism
Empagliflozosin
MOA:
sodium glucose co-transporter 2 (SGL2) inhibitor
located in the proximal tubule responsible for glucose reasbp.
Clinical uses:
Type 2 diabetes
Toxicity:
osmotic diuresis, UTIs
Extra info:
oral, blocks glucose reabsorption in the kidney proximal tubule
Liraglutide
MOA:
glucagon receptor agonist
Clinical uses:
Type 2 diabetes
Toxicity:
hypoglycemia
Extra info:
stimulates insulin secretion, once daily injectable derivative of human GLP-1, long-acting due to serum albumin binding
Sitagliptin
MOA:
dipeptidyl peptidase-4 inhibitor
Clinical uses:
Type 2 diabetes
Toxicity:
rhinitis, upper respiratory tract infections
Extra info:
oral
Insulin glargine
MOA:
insulin analog
Clinical uses:
type 1 and type 2 diabetes
Toxicity :
hypoglycemia
Extra info:
long-acting (>20 hours), SC injection
Insulin lispro
MOA:
insulin analog
Clinical uses:
type 1 and type 2 diabetes
Toxicity:
hypoglycemia
Extra info:
rapid-acting (minutes), injected SC postprandial
Insulin
MOA:
insulin receptor agonist
Clinical uses:
type 1 and type 2 diabetes
Toxicity:
hypoglycemia
Extra info:
short-acting, multiple delivery systems
Phentermine + Topiramate
MOA:
Phentermine: stimulates release of biogenic amines (NE, 5-HT, dopamine) Topiramate: mechanism unclear, may bind and effect Na+ and Ca2+ channels, GABAa receptors, and others
Clinical uses:
weight loss
Toxicity:
parasthesia, dizziness, dysgeusia, insomnia, constipation, dry mouth
Extra info:
oral, once daily pill, contraindicated in pregnancy, glaucoma, hyperthyroidism and with MAO inhibitors
Lorcarserin
MOA:
5-HT2C serotonin receptor agonist
Clinical uses:
weight loss
Toxicity:
headache
Extra info:
oral, stimulates 5-HT2C receptor in the hypothalamus to promote satiety
Acarbose
MOA:
intestinal alpha-glucosidase inhibitor
Clinical uses:
obesity, type 2 diabetes
Toxicity:
GI disturbances
Extra info:
oral, prevents conversion of complex polysaccharides into monosaccharides and subsequent transportation into the bloodstream
Naltrexone + Buproprion
MOA:
Buproprion: 5-HT/NE reuptake inhibitor Naltrexone: Opioid receptor antagonist
Clinical uses:
obesity
Toxicity: psychiatric disturbances (increased risk of suicide, mood changes)
Extra info:
Blocking opioid and enhancing monoamine effects in the POMC-hypothalamus reduces food-associated cravings; numerous contraindications
Orlistat
MOA:
lipistatin derivative, inhibits pancreatic lipases that degrade triglycerides
clinical uses:
obesity
Toxicity:
GI disturbances
Extra info:
oral before meals, increases excretion of unmetabolised triglycerides
Cinacalcet
MOA:
Ca2+ sensing receptor positive allosteric modulator
Clinical uses:
primary and secondary hyperparathyroidism
Toxicity:
nausea, hypocalcemia, adynamic bone
Extra info: oral; calcium mimetic (caclimimetic) that lowers serum PTH levels via negative feedback regulation; CYP3A4, 2D6 substrate
Denosumab
MOA:
monoclonal antibody, inhibits RANK-ligand (RANKL)
Clinicial uses:
post-menopausal osteoperosis (PMO)
Toxicity:
opportunistic infections
Extra info:
SC every 6 months; RANKL is the ligand for RANK, which when stimulated, promotes bone turnover by activating osteoclasts
Calcitrol
MOA:
vitamin D nuclear receptor (aka calcitrol receptor) agonist
Clinical uses:
vitamin D deficiency, hypocalcemia, osteoperosis
Toxicity:
hypercalcemia, hyperphosphatemia, hypercalciuria
Extra info:
oral 1,25-dihydroxycholecalfierol (or 1,25-dihydroxyvitamine D2), which is the hormonally active metabolite of vitamin D; activation of vitamin D receptor increases the transcription of genes that increase serum Ca2+ levels
Alendronate
MOA:
bisphosphonate, suppresses osteoclast-mediated bone resorption
Clinical uses:
osteoperosis, Paget’s disease
Toxicity:
adynamic bone, esophageal irritation
Extra info:
oral; mimicks endogenous pyrophosphate to block bone resorption but permits bone mineralization
