Drugs/Physiology: Osteoporosis, DM, Endocrine Flashcards

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
Q

Ketoconazole

A

Inhibit cortisol synthesis (used in ectopic Cushing’s)

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26
Q

Mifepristone

A

Cortisol receptor blocker (used in ectopic Cushing’s)

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27
Q

What Abs are found in Hashimot’s thyroiditis?

A

Thyroid peroxidase antibodies (TPO)

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28
Q

Levothyroxine

A

T4- treatment of primary hypothyroidism

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29
Q

Triiodothyronine

A

T3- treatment of primary hypothyroidism but always used in combination with levothyroxine, 80% levo + 20% triiodo

30
Q

Goal of therapy for primary hypothyroidism

A

Achieve a normal TSH

31
Q

Goal of therapy for secondary hypothyroidism

A

Achieve a normal freeT4 levels, as TSH will always be low

32
Q

What are dopamine agonist used for?

A

Treatment of prolactinomas > very effective (>95%)

33
Q

Bromocriptine

A

Dopamine agonist > decrease prolactin synthesis, cell multiplication and tumor size

34
Q

Cabergoline

A

Dopamine agonist > decrease prolactin synthesis, cell multiplication and tumor size

35
Q

SEs of Dopamine Agonists?

A

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
Q

Glargine

A

Long acting insulin (1/day)

37
Q

Detemir

A

Long acting insulin (2/day)

38
Q

NPH

A

Long acting insulin (2/day)

39
Q

Regular insulin

A

Short/intermediate acting insulin (give before B and L when given with NPH)

40
Q

Aspart

A

Short acting insulin (give before B, L and D), onset 15 min, peak 30 min, duration 4 hrs

41
Q

Lispro

A

Short acting insulin (give before B, L and D), onset 15 min, peak 30 min, duration 4 hrs

42
Q

Glulisine

A

Short acting insulin (give before B, L and D), onset 15 min, peak 30 min, duration 4 hrs

43
Q

Treatment of Type II

A

Rule 1: everyone starts with metformin
Rule 2: every non-insulin agent drops HbA1c by 1%
Use non-insulin agents if HbA1c

44
Q

Metformin Action

A

Biguanide: inhibits mitochondrion-specific glycerophoshate dehydrogenase (mGPD) > decreases gluconeogenesis in liver cells > decrease glucose release
In addition, decreases lactic acid clearance

45
Q

Metformin SEs

A

Nausea, abdominal pain, bloating, diarrhea

Not associated with weight gain/hypoglycemia, no affect on insulin sensitivity

46
Q

Acarbose Action

A

Alpha glucosidase inhibitor: inhibits enzyme responsible for converting complex polysaccharides > monosaccharides = slow absorption of glucose

47
Q

Acarbose SEs

A

flatulence and diarrhea

48
Q

Pioglitazone Action

A

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
Q

Pioglitazone SEs

A

weight gain, fluid retention (contraindicated for CHF)

50
Q

Glipizide

A

sulfonylurea

51
Q

glimpiride

A

sulfonylurea

52
Q

glyburide

A

sulfonylurea

53
Q

Sulfonylurea action

A

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
Q

Sulfonyurea SEs

A

Hypoglycemia due to glucose independent release of insulin

55
Q

Meglitinides

A

Same action/SEs as SUs > different sight than SUR but same receptor

56
Q

Exanatide

A

GLP-1 agonist

57
Q

Liraglutide

A

GLP-1 agonist

58
Q

GLP-1 agonist action

A

Enhance insulin secretion from Beta cell in a glucose dependent manner

59
Q

GLP-1 agonist SEs

A

Nausea, pancreatitis, WEIGHT LOSS (5 Lb)

60
Q

Sitagliptin

A

DPP-IV inhibitor

61
Q

Saxagliptin

A

DPP-IV inhibitor

62
Q

Linagliptin

A

DPP-IV inhibitor

63
Q

DPP-IV inhibitor action

A

Inhibit DPP-IV from breaking down GLP-1 > increase endogenous GLP-1 > increase insulin secretion in glucose-dependent manner

64
Q

DPP-IV inhibitor SEs

A

nausea, pancreatitis, severe joint pain

65
Q

Canagliflozin Action

A

SGLT-2 inhibitor: inhibit reuptake of glucose in proximal tubule

66
Q

SGLT-2 inhibitor SEs

A

Decrease BP, weight loss, vulvovaginal candidiasis, UTI, DKA

67
Q

Most common cause of primary hypercholesterolemia

A

polygenic hypercholesterolemia

68
Q

Types of monogenic hypercholesterolemia

A

LDL receptor mutation (95%), PSCK9 mutation (2%), familial defective ApoB-100
Finding: premature corneal arcus, tendon xanthomas, xanthelasma

69
Q

What two drugs are associated with cardiovascular disease risk reduction in the treatment of hypercholesterolemia

A

Statins and PSCK9 inhibitors

70
Q

Statin benefit groups (4)

A
  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
Q

SEs of statins

A

myopathy

72
Q

Findings of hyperaldosteronism

A
fluid retention (Na+ reabsorption), hypokalemia, hypertension
For diagnosis: measure aldosterone and renin: divide aldosterone/renin > high in hyperaldosteronemia (normal