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Drugs/Physiology Keystone Exam 1 > Drugs/Physiology: Osteoporosis, DM, Endocrine > Flashcards

Drugs/Physiology: Osteoporosis, DM, Endocrine Flashcards

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1
Q

Raloxifene

A

Selective estrogen receptor modulator (SERM)

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2
Q

Bisphosphonate Action

A

The “dronate’s”- Impair osteoclast function (decrease differentiation/increase apoptosis) via inhibiting farnesyl pyrophosphate (FPP) synthase in mevalonate pathway > disrupts protein prenylation > cytoskeletal abnormalities
Increase bone mineral density (BMD)/decrease fractures

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3
Q

Bisphosphonate SEs

A

Esophagitis with orals, flu like symptoms with IV, bone/muscle pain (rare), hypocalcemia
Long Term SEs: atypical subtrochanteric fractures > micro cracks- avoid via “drug holidays”, micro cracks can also lead to osteonecrosis of jaw +/- infection
Contraindicated if Creatinine clearance

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4
Q

Alendronate

A

Bisphosphonate: PO

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5
Q

Risedronate

A

Bisphosphonate: PO

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6
Q

Ibandronate

A

Bisphosphonate: PO, IV

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7
Q

Xolendronic acid (zolendronate)

A

Bisphosphonate: IV

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8
Q

Selective Estrogen Receptor Modulator (SERM) Action

A

Binds to estrogen receptor:
Agonist in bone > inhibit osteoclast
Antagonist in Breast tissue > reduced BC risk

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9
Q

SERM SEs

A

DVT, hot flushes

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10
Q

Denosumab

A

Monoclonal Antibody, SubQ injection/6 months

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11
Q

Denosumab Action

A

directly binds to RANKL (secreted via osteoblasts and responsible for osteoclast activation), similar to osteoprotegerin (OPG) > blocks maturation of osteoclast

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12
Q

Denosumab SEs

A

Hypocalcemia, potential neoplastic due to lymphocytes requiring RANKL
NO renal restrictions (can treat Creatinine

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13
Q

Teriparatide (human recombinant PTH-34)

A

Anabolic (unique in respect to osteoporosis drugs): stimulates osteoblast activity

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14
Q

Teriparatide Action

A

Induces differentiation/maturation of osteoblast, reduces osteoblast apoptosis (given daily SubQ)

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15
Q

Teriparatide SEs

A

Increase uric acid (3% of patients), hypercalcemia, osteosarcoma (seen in lab only > 2 yr treatment limit)
Contraindicated at high risk osteosarcoma (Paget, radiation, open epiphyses), cancer diagnosis in past 5 yrs, elevated PTH

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16
Q

Cinacalcet

A

Calcium mimetic > binds to CaSR on parathyroid gland > decrease Ca release from bone but DOES NOT normalize PTH
SE: nausea

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17
Q

Calcitriol

A

1,25 OH2 Vitamine D: treat hypoparathyroidism > attempt to get Ca levels to 8.5-9.5 to prevent hypercalciuria

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18
Q

Propanonlol

A

B-blocker: used to treat sympathetic symptoms of hyperthyroidism (only necessary treatment to thyroiditis)

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19
Q

Methimazole

A

Thionamide used in hyperthyroidism to decrease production of T4

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20
Q

Propylthiouracil

A

Thionamide used in hyperthyroidism to decrease production of T4

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21
Q

Most common treatment modality for Grave’s disease

A 
Radioactive iodine (I-131) > radiation ablates thyroid gland and follow with supplemental thyroid hormone
SEs: don't give to patients with proptosis > can worsen
May cause iodine-induced thyroiditis initially
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22
Q

Thioamide SEs

A

Thionamides = proplythiouracil and methimazole
Rash, agranulocytosis (neutr), cholestasis, fulminant liver failure with PTU, Methimazole - teratogenic during 1st trimester (use PTU during 1st then Methimazole for remaining)

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23
Q

How do you treat primary adrenal insufficiency?

A

Glucocorticoid (prednisone or hydrocortisone) + mineralcorticoid (fludrocortisone)

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24
Q

Metyrapone

A

Inhibit cortisol synthesis (used in ectopic Cushing’s)

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25
Ketoconazole
Inhibit cortisol synthesis (used in ectopic Cushing's)
26
Mifepristone
Cortisol receptor blocker (used in ectopic Cushing's)
27
What Abs are found in Hashimot's thyroiditis?
Thyroid peroxidase antibodies (TPO)
28
Levothyroxine
T4- treatment of primary hypothyroidism
29
Triiodothyronine
T3- treatment of primary hypothyroidism but always used in combination with levothyroxine, 80% levo + 20% triiodo
30
Goal of therapy for primary hypothyroidism
Achieve a normal TSH
31
Goal of therapy for secondary hypothyroidism
Achieve a normal freeT4 levels, as TSH will always be low
32
What are dopamine agonist used for?
Treatment of prolactinomas > very effective (>95%)
33
Bromocriptine
Dopamine agonist > decrease prolactin synthesis, cell multiplication and tumor size
34
Cabergoline
Dopamine agonist > decrease prolactin synthesis, cell multiplication and tumor size
35
SEs of Dopamine Agonists?
Nausea (more so for bromocriptine, can increase dose slowly), Valvular regurgitation (more so for cabergoline @ very high doses used for parkinson's disease, use much lower dose for PRLoma)
36
Glargine
Long acting insulin (1/day)
37
Detemir
Long acting insulin (2/day)
38
NPH
Long acting insulin (2/day)
39
Regular insulin
Short/intermediate acting insulin (give before B and L when given with NPH)
40
Aspart
Short acting insulin (give before B, L and D), onset 15 min, peak 30 min, duration 4 hrs
41
Lispro
Short acting insulin (give before B, L and D), onset 15 min, peak 30 min, duration 4 hrs
42
Glulisine
Short acting insulin (give before B, L and D), onset 15 min, peak 30 min, duration 4 hrs
43
Treatment of Type II
Rule 1: everyone starts with metformin Rule 2: every non-insulin agent drops HbA1c by 1% Use non-insulin agents if HbA1c
44
Metformin Action
Biguanide: inhibits mitochondrion-specific glycerophoshate dehydrogenase (mGPD) > decreases gluconeogenesis in liver cells > decrease glucose release In addition, decreases lactic acid clearance
45
Metformin SEs
Nausea, abdominal pain, bloating, diarrhea | Not associated with weight gain/hypoglycemia, no affect on insulin sensitivity
46
Acarbose Action
Alpha glucosidase inhibitor: inhibits enzyme responsible for converting complex polysaccharides > monosaccharides = slow absorption of glucose
47
Acarbose SEs
flatulence and diarrhea
48
Pioglitazone Action
Thiazolidinediones > PPAR-gamma agonist > increases glucose uptake in adipose tissue + some increased of glucose uptake in skeletal muscle Overall: lower serum glucose by enhancing insulin effects, lower plasma Fatty Acids
49
Pioglitazone SEs
weight gain, fluid retention (contraindicated for CHF)
50
Glipizide
sulfonylurea
51
glimpiride
sulfonylurea
52
glyburide
sulfonylurea
53
Sulfonylurea action
Bind to sulfonylurea receptor on pancreatic Beta cells which is located on ATP sensitive K+ channels > leads to inhibition > cell depolarization > activation of Ca2+ voltage gated Ca2+ channels > Ca2+ intracellular lead to insulin release Give 1-2/day
54
Sulfonyurea SEs
Hypoglycemia due to glucose independent release of insulin
55
Meglitinides
Same action/SEs as SUs > different sight than SUR but same receptor
56
Exanatide
GLP-1 agonist
57
Liraglutide
GLP-1 agonist
58
GLP-1 agonist action
Enhance insulin secretion from Beta cell in a glucose dependent manner
59
GLP-1 agonist SEs
Nausea, pancreatitis, WEIGHT LOSS (5 Lb)
60
Sitagliptin
DPP-IV inhibitor
61
Saxagliptin
DPP-IV inhibitor
62
Linagliptin
DPP-IV inhibitor
63
DPP-IV inhibitor action
Inhibit DPP-IV from breaking down GLP-1 > increase endogenous GLP-1 > increase insulin secretion in glucose-dependent manner
64
DPP-IV inhibitor SEs
nausea, pancreatitis, severe joint pain
65
Canagliflozin Action
SGLT-2 inhibitor: inhibit reuptake of glucose in proximal tubule
66
SGLT-2 inhibitor SEs
Decrease BP, weight loss, vulvovaginal candidiasis, UTI, DKA
67
Most common cause of primary hypercholesterolemia
polygenic hypercholesterolemia
68
Types of monogenic hypercholesterolemia
LDL receptor mutation (95%), PSCK9 mutation (2%), familial defective ApoB-100 Finding: premature corneal arcus, tendon xanthomas, xanthelasma
69
What two drugs are associated with cardiovascular disease risk reduction in the treatment of hypercholesterolemia
Statins and PSCK9 inhibitors
70
Statin benefit groups (4)
1. Individuals with atherosclerotic CVD 2. Individuals with LDL > 190 mg/dl 3. Individuals (45-75yo) with LDL 70-189 + DM 4. Individuals (45-70) with LDL 70-189 with no DM, no CVD but with 10 year risk of atherosclerotic CVD >/= 7.5%
71
SEs of statins
myopathy
72
Findings of hyperaldosteronism
``` fluid retention (Na+ reabsorption), hypokalemia, hypertension For diagnosis: measure aldosterone and renin: divide aldosterone/renin > high in hyperaldosteronemia (normal ```

Drugs/Physiology Keystone Exam 1 (2 decks)

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