Bone/Obesity/Diabetes/Lipids Flashcards

1
Q

Atorvastatin

A

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

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2
Q

Evolocumab

A

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 ($$$)

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3
Q

Gemfibrozil

A

MOA:
PPAR-α agonist

lower TG and raise HDL

Clinical uses:
hypertriglyceridemia, dysbetalipoproteinemia

Toxicity:
myopathy, hepatic dysfunction

Extra info:
combine with statins

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4
Q

Colestipol

A

MOA:
bile acid binding resin

Clinical uses:
primary hypercholesterolemia, high LDL

Toxicity:
GI effects

Extra info:
combine with statins

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5
Q

Ezetimbe

A

MOA:
inhibits NPC1L1 cholesterol transporter

Extra info:
primary hypercholesterolemia, high LDL

Toxicity:
GI effects, hepatic dysfunction

Extra info:
combine with statins

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6
Q

Niacin

A

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

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7
Q

Glipizide

A

MOA:
K+ channel blocker in pancreatic beta cells, increases insulin secretion

Clinical uses:
Type 2 diabetes

Toxicity:
hypoglycemia, weight gain

Extra info:
oral

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8
Q

Metformin

A

MOA:
decreases hepatic gluconeogenesis, molecular mechanism not understood

Clinical uses:
Type 2 diabetes, polycystic ovarian syndrome

Toxicity :
GI disturbances

Extra info:
oral

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9
Q

Pioglitazone

A

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

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10
Q

Empagliflozosin

A

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

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11
Q

Liraglutide

A

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

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12
Q

Sitagliptin

A

MOA:
dipeptidyl peptidase-4 inhibitor

Clinical uses:
Type 2 diabetes

Toxicity:
rhinitis, upper respiratory tract infections

Extra info:
oral

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13
Q

Insulin glargine

A

MOA:
insulin analog

Clinical uses:
type 1 and type 2 diabetes

Toxicity :
hypoglycemia

Extra info:
long-acting (>20 hours), SC injection

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14
Q

Insulin lispro

A

MOA:
insulin analog

Clinical uses:
type 1 and type 2 diabetes

Toxicity:
hypoglycemia

Extra info:
rapid-acting (minutes), injected SC postprandial

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15
Q

Insulin

A

MOA:
insulin receptor agonist

Clinical uses:
type 1 and type 2 diabetes

Toxicity:
hypoglycemia

Extra info:
short-acting, multiple delivery systems

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16
Q

Phentermine + Topiramate

A

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

17
Q

Lorcarserin

A

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

18
Q

Acarbose

A

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

19
Q

Naltrexone + Buproprion

A

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

20
Q

Orlistat

A

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

21
Q

Cinacalcet

A

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

22
Q

Denosumab

A

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

23
Q

Calcitrol

A

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

24
Q

Alendronate

A

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

25
Q

Zoledronic acid

A

MOA:
bisphosphonate, suppresses osteoclast-mediated bone resorption

Clinical uses:
osteoperosis, Paget’s disease, hypercalcemia

Toxicity:
(~2% of patients) nausea, fatigue, flu-like symptoms, cough, dizziness, headache

Extra info:
IV, renal excretion, can cause severe renal impairment in small number of patients

26
Q

Estrogen-progestin

A

MOA:
estrogen receptor agonist

Clinical uses:
osteoperosis, reduce risk of bone fractures

Toxicity:
increased risk of breast cancer, stroke and blood clots

Extra info:
oral, not recommended for post-menopausal women

27
Q

Raloxifiene

A

MOA:
selective estrogen receptor modulator (SERM, competitive estrogen receptor partial agonist)

Clinical uses:
post-menopausal osteoperosis (PMO), breast cancer

Toxicity:
hot flushes, leg cramps, thromboembolism

Extra info:
oral; acts as an estrogen receptor agonist in bone, and as an estrogen receptor antagonist in the uterus and breast