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Therapeutics > Exam 4 > Flashcards

Exam 4 Flashcards

1
Q

What are the vasomotor symptoms of menopause?

A

hot flashes and night sweats

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2
Q

What are the three indications for menopausal hormone therapy?

A

vasomotor symptoms, vulvovaginal atrophy, osteoporosis prevention

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3
Q

What are some contraindication to menopausal hormone therapy?

A

pregnancy, estrogen-dependent malignancies (endometrial and breast cancer)m stroke, thromboembolic disorders, liver disease

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4
Q

Estrogen monotherapy is only for women (with/without) a uterus

A

without

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5
Q

What are the three forms of oral estrogen monotherapy?

A

Premarin, Estrace, and Menest (PEM)

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6
Q

What are the six transdermal monotherapy products?

A

Alora, Climara, Menostar, Minivelle, Vivelle, Vivelle-dot

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7
Q

What are the two topical products for estrogen monotherapy?

A

Topical Gel (EstroGel, Divigel, Elestrin) and Topical Spray (Evamist)

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8
Q

What are the four intravaginal products for estrogen monotherapy?

A

Vaginal cream (Estrace, Premarin), vaginal insert (Imvexxy), Vaginal tablet (vagifem, yuvafem), vaginal ring (Estring, Femring)

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9
Q

Which intravaginal product has vasomotor symptoms?

A

Femring (the ring is bigger than the string)
Needs progesterone in intact uterus

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10
Q

What type of product should be prescribed for women exclusively experiencing vulvovaginal atrophy?

A

Topical vaginal products- minimizes systemic effect

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11
Q

Why should women with intact uterus be prescribed a progestin in addition to estrogen?

A

Decrease risk of endometrial hyperplasia and cancer

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12
Q

In the WHI study, what major clinical outcomes were increased risk with use of Estrogen and Progesterone (intact uterus)?

A

heart attacks, strokes, venous thromboembolism, and invasive breast cancer

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13
Q

In the WHI study, what major clinical outcomes were increased risk with use of Estrogen alone (hysterectomy)?

A

Increase stroke and venous thromboembolism.

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14
Q

What were the two critical factors in determining whether hormone therapy reduces or increases risk of CHD?

A

Time since menopause (within 10 yrs of last period) and age of initiation (<60)

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15
Q

Which age range and group (estrogen only vs E+P) had favorable outcomes for absolute risk of health outcomes by the WHI?
A. 40-49yrs
B. 50-59y
C. 60-69y

A

B. Estrogen only

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16
Q

Women with intact uterus was significantly associated with a (higher/lower) risk of breast cancer

A

higher

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17
Q

Women with prior hysterectomy had (higher/lower) risk of breast cancer

A

lower

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18
Q

What drugs are associated with continuous cyclic therapy?

A

Premphase (oral) and Combipatch (Transdermal)

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19
Q

How does continuous cyclic therapy (Sequential treatment) work? How is it viewed?

A

Estrogen admin daily, progesterone 12-14 days of 28 day cycle
Scheduled withdrawal bleeding- not favorable
Preferred in recently menopausal women (not long term)

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20
Q

How does continuous long cycle therapy (cyclic withdrawal) work? How is it viewed?

A

Estrogen daily, Progesterone 12-14 days every other month
Limited safety data and endometrial protection unclear, RARE

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21
Q

How does continuous combines therapy work? How is it viewed?

A

Daily E+P: Preferred!
Stops bleeding, recommended for women >2 yrs post-final period, long term endo protection

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22
Q

What are the 6 continuous combined E+P oral drugs?

A

Prempro, Angeliq, Activella, Amabelz, Mimvey, Bijuva, Fyavolv, Jinteli
(PAAAM Be for Jim -Michael Scott Tarzan voice)

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23
Q

What are the 2 continuous combined E+P transdermal products?

A

ClimaraPro and Combipatch

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24
Q

How does intermittent combined (pulsed-progesterone) work? How is it viewed?

A

3 days estrogen, 3 days E+P
Pulse prevents progesterone receptors, endo protection unknown

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25
Q

What drug is used for intermittent combined E+P?

A

Prefest-Oral

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26
Q

What oral E+P is best for endometrial protection?

A

Medroxyprogesterone (Provera), Norethindrone acetate (Aygestin), and micronized progestin (Prometrium) (PAP)

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27
Q

What vaginal/intrauterine E+P is best for endometrial protection?

A

levonorgestrel (Mirena IUD) and progesterone gel (Crinone)

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28
Q

What drug is used for Estrogen+SERM? What are the side effects?

A

Duavee-oral
GI track disrders, muscle spasm, neck pain, dizziness, oropharyngeal pain

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29
Q

What SSRI is FDA approved for hot flashes?

A

Paroxetine

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30
Q

What drug is used for bio-identical hormone replacement therapy? How is it viewed?

A

Bijuva-oral
Minimal insurance coverage and questionable safety

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31
Q

What is the first line treatment for Genitourinary Syndrome of Menopause? Second line?

A

First line: non-hormonal (Lubricants and vaginal moisturizers)
Second line: estrogen (topical, low dose oral contra)

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32
Q

What drug is used in the treatment of mod-severe dyspareunia using SERM? What are important clinical pearls?

A

Ospemifene (Osphena)
Black box: endo cancer, stroke, VTW
In postmenopausal women
SE: endo hyperplasia and hot flashes

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33
Q

What drug is used in the treatment of mod-severe dyspareunia using DHEA? What are important clinical pearls?

A

Prasterone (Intrarosa)
Postmenopausal women
Contraindicated for undiagnosed vaginal bleeding
Avoid with history of breast cancer
Costly

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34
Q

Hormone produced by C-cells that help regulate calcium and phosphate levels in the blood

A

calcitonin

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35
Q

Main hormone secreted from thyroid gland into the blood stream, controlling basal metabolic rate

A

Thyroxine

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36
Q

Which is more potent: T4 or T3?

A

T3

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37
Q

Which is produced more: T4 or T3?

A

T4

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38
Q

How is thyroid biosynthesized? (Iodide to T3 and T4)

A

Iodide in blood pairs with sodium to go through Na/I symporter into thyroid follicular cell
In follicular cell, iodide is pushed through pendrin to follicle colloid, meanwhile thyroglobulin is taken from the ER of cell and undergoes exocytosis into follicle colloid
In follicle colloid, Iodide gets oxidized and attaches to the aromatic rings of thyroglobulin
Once attached, complex undergoes endocytosis where it goes through proteolysis which separates into T3 and T4 in transport of follicular cell
Cell goes back into blood stream with T3 and T4

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39
Q

What makes T3 and T4 from MIT and DIT?

A

MIT + DIT= T3
DIT + DIT= T4

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40
Q

What hormone is released between the hypothalamus and anterior pituitary?
A. TSH
B. T4 and T3
C. TRH

A

C. TRH

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41
Q

What hormone is released between the anterior pituitary and thyroid gland?
A. TSH
B. T4 and T3
C. TRH

A

A. TSH

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42
Q

What hormone is secreted from the thyroid gland to cause physiological functions?
A. TSH
B. T4 and T3
C. TRH

A

B. T4 and T3

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43
Q

What condition can result from iodine deficiency?

A

Goiter- enlarged thyroid due to rise in TSH
Cretinism- stunted physical and mental growth

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44
Q

What are the three transport proteins of thyroid in plasma?

A

TBG, TTR, and albumin

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45
Q

Transport proteins have greater affinity to (T3/T4)

A

T4

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46
Q

(T3/T4) has a longer half life than (T3/T4), and (T3/T4) has a more rapid onset

A

T4 has a longer half life than T3, and T3 has a more rapid onset

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47
Q

Name the compound

A

T4

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48
Q

Name the compound and its activity

A

T3- active

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49
Q

Name the compound and its activity

A

rT3- inactive

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50
Q

Name the compound and its activity

A

3,3-T2 inactive

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51
Q

Thyroid condition characterized by decrease in metabolic rate, bradycardia, hypoglycemia, and drooping of eyelids

A

hypothyroidism

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52
Q

One of the most common thyroid autoimmune disease that destroys the thyroid gland

A

Hashimotos

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53
Q

Thyroid condition characterized by increased BMR, tachycardia, hyperglycemia, and retraction of upper lids (exophthalmos)

A

hyperthyroidism

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54
Q

One of the most common thyroid autoimmune diseases that cause enlargement of the entire thyroid gland

A

Graves’ disease

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55
Q

What are the 4 common thyroid hormone replacement options for hypothyroidism?

A

natural thyroid hormone preparations, Levothyroxine, Liothyronine, and Liotrix

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56
Q

Which hypothyroid medication is a T4 characterized by slow onset, long half life, and 6-8wk for steady state levels?

A

Levothyroxine

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57
Q

Which hypothyroid medication is a T3 characterized by rapid onset, short duration of action, requiring multiple daily doses.
Greater risk of cardiotoxicity

A

Liothyronine

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58
Q

Which hypothyroid medication is a 4:1 mixture of T4 and T3?

59
Q

What are the two common treatment methods for hyperthyroidism?

A

Thioamides and radioactive iodine (131I)

60
Q

What is the TSH reference range?

A

0.5-5.0 mlU/L

61
Q

What is the free T4 range?

A

0.7-1.9 ng/dL

62
Q

What are the three tests of autoimmunity for thyroid testing

A

ATgA, TPO-Ab, and TRAb

63
Q

Which autoimmunity test is positive for autoimmune thyroid diseases and undetectable during remission?

64
Q

Hyper or Hypo thyroidism: Lab finding of high TSH and low FT4, decreased HR and increased BP

A

Hypothyroidism

65
Q

Hyper or Hypo: Lab findings of low TSH and high FT4, Increased HR

A

hyperthyroidism

66
Q

What 4 drugs induce hyperthyroidism?

A

Iodinated compounds, Amiodarone, interferons, and lithium

67
Q

What 2 drugs are thioamides used for hyperthyroidism treatment?

A

Propylthiouracil (PTU) and methimazole

68
Q

PTU or Methimazole: longer half life

A

Methimazole

69
Q

PTU or Methimazole: less daily dosing

A

PTU- 2-3x day
Methimazole- daily

70
Q

PTU or Methimazole: Blocks T4 to T3 conversion

A

PTU- YES
Methimazole- NO

71
Q

PTU or Methimazole: Which trimester of pregnancy

A

PTU- 1st (less placental crossing)
Methimazole- 2nd + 3rd

72
Q

PTU or Methimazole: Can take during lactation

A

PTU- No
Methimazole- Yes (Preferred)

73
Q

PTU or Methimazole: Black box warning

A

PTU- Yes: hepatic failure
Methimazole- No: acute pancreatitis

74
Q

What is the initial, maintenance, and max dosing range for Methimazole?

A

Initial:
Free T4 1-1.5x, 5-10 mg/day
Free T4 1.5-2x: 10-20 mg/day
Free T4 >2x: 30-40 mg/day
Maintenance: 5-15 mg/day
Max: 60 mg/day

75
Q

What is the initial, maintenance, and max dosing range for PTU?

A

Initial: 50-150 mg TID
Maintenance: 50mg BID or TID
Max: 1200 mg/day

76
Q

Which rash requires stopping thioamides and going to RAI or surgery?
A. Maculopapular
B. Wheals, hives, SOB

A

B. Wheals, hives, SOB

77
Q

Which thioamide adverse effect leads to severely low white blood cell count?

A

agranulocytosis

78
Q

How often are lab test checked with thioamides until euthyroid?

A

every 4-8 weeks

79
Q

Short-term use of Beta blockers to alleviate symptoms are seen in (hyper/hypo)thyroidism

A

hyperthyroidism

80
Q

Can a patient with hyperthyroidism be placed on a cardio-selective beta-blocker with a HR of 105?

81
Q

What is the therapy dosing for levothyroxine and when should they take it?

A

1.6 mcg/kg/day on an empty stomach (60 min before breakfast or 4 hours after dinner)

82
Q

A patient who recently became pregnant was taking levothyroxine for hypothyroidism. Can she continue her meds?

A

Yes, adjust dose every trimester

83
Q

What are three reasons a patient has high or fluctuating TSH despite high levothyroxine dose?

A

Poor adherence, drug-food interaction, and drug-drug interaction

84
Q

What are the four drug interaction effects commonly seen in thyroid treatment?

A

Decreased T4 absorption, increased T4 requirement, increased serum TBG, and disease-drug interactions (warfarin)

85
Q

What is the calcium in bone’s crystalline formation called?

A

hydroxyapatite

86
Q

Bone forming cell that incorporates calcium and phosphate from plasma into bone

A

osteoblasts

87
Q

Bone resorption cells that release calcium and phosphate from bone into plasma

A

osteoclasts

88
Q

Regulates the release of osteoblast/clast activity in bone

A

osteocytes

89
Q

Increased BMD with increased load stimulates osteo(blast/clast) activity, while decrease BMD with decreased load stimulates osteo(blast/clast)

A

Increased BMD with increased load stimulates osteoblast activity, while decrease BMD with decreased load stimulates osteoclast

90
Q

Deletion from what amino acids in the parathyroid hormone eliminates activity?

A

Deletions 1&2

91
Q

Describe the effect of PTH and Ca sensor activity

A

When Ca sensor is low, PTH is secreted in blood
Increase in Ca bone resorption, kidney Ca reabsorption, and kidney dihydroxyl vit D occur.
An increase of Ca occurs, causing a negative feedback inhibiting PTH

92
Q

What is the first step of vitamin D synthesis?

A

Provitamin D is converted to cholecalciferol from UV irradiation of skin or diet

93
Q

Describe Vit D synthesis

A

Vit D3 is hydrophobic, needing a Vit D binding protein through liver
Processed to 25 hydroxyvitamin D3 which can undergo two pathways in kidney:
1.) 1-alpha-hydroxylase- stimulated by PTH leads to 1,25 Dihydroxy Vit D3, active form of Ca absorbing from the intestines
2.) 24-hydroxylase- PTH is not being released
24,25 Dihydroxy Vit D3, less active form of Ca uptake from intestine

94
Q

What are the actions of Vit D on calcium and phosphate (4)?

A
  1. increase calcium and phosphate absorption from small intestine (rapid effect on brush border)
  2. increase calcium and phosphate reabsorption
  3. indirect (slow) effects on cells (calbindins, Vit D binding proteins)
  4. Feedback inhibition of PTH
95
Q

Describe the absorption of Ca from the intestine (TrpV6, Calbindin, Ca-ATPase)

A

TrpV6 brings in calcium, which is transported in the cell by calbindin to the Ca-ATPase that pumps into serosal membrane

96
Q

What is the “phosphate specialist” that stimulates phosphate excretion, inhibits dihydroxyl Vit D synthesis, and inhibits PTH secretion?

97
Q

What conditions occur from high FGF23 levels?

A

Poor prognosis in CKD patients on dialysis
Autosomal dominant hypophosphatemic rickets

98
Q

Which of the following inhibit PTH secretion?
I,25-(OH)2 Vit D3
FGF23
Low Ca
High Ca

A

I,25-(OH)2 Vit D3, FGF23, and High Ca

99
Q

How is calcitonin a negative regulator of serum calcium?

A
  1. Inhibits osteoclastic bone resorption
  2. Increase calcium and phosphate loss in urine (less reabsorbed)
100
Q

Calcitonin is stimulated by (low/high) serum calcium levels

101
Q

Disease of uncontrolled osteoclastic bone resorption and secondary bone formation (high calcium turnover) resulting in bone pain, deformities, and loss of hearing, hypercalcemia.

A

Pagets disease

102
Q

What is used to suppress osteoclastic activity in Paget’s disease?

A

Bisphosphonates

103
Q

What part of the bone can obvious deterioration be found in osteoporosis

A

trabecular bone

104
Q

What two conditions are responsible for hypercalcemia?

A

Hyperparathyroidism and malignant tumors

105
Q

What condition is associated with hypocalcemia?

106
Q

What drug combo with Vit D is taken as a supplement with osteoporosis?

A

Vit D + Ca

107
Q

What drug combo with Vit D is taken as a supplement with hypo-calcemia/parathyroidism?

A

Vit D + Ca + rPTH

108
Q

What drug combo with Vit D is taken as a supplement with hyperparathyroidism?

A

Vit D analogs (suppress PTH)

109
Q

What bisphosphates are approved for Paget’s and cancer, NOT osteoporosis?
Alendronate
Etidronate
Ibandronate
Pamidronate
Risedronate
Zoledronate

A

Pamidronate and Etidronate (PE)

110
Q

What bisphosphates are approved for building bone mass in osteoporosis?
Alendronate
Etidronate
Ibandronate
Pamidronate
Risedronate
Zoledronate

A

Alendronate, Ibandronate, Risedronate, Zoledronate

111
Q

What drugs are approved for high risk fracture?

A

Teriparatide and abaloparatide

112
Q

What neutralizes RANKL in osteoclast differentiation?

A

OPG- Osteoprotegerin

113
Q

Should PTH in teriparatide be exposed intermittent or continuously?

A

Intermittent

114
Q

What is the max amount of years for Teriparatide?

A

2 years- black box bone cancer

115
Q

Which drug for osteoporosis binds to RANKL and prevents activation of RANK on osteoclast precursors?
Denosumab or Romosozumab

A

Prolia (Denosumab)

116
Q

Which drug for osteoporosis is a monoclonal antibody against sclerostin?
Denosumab or Romosozumab

A

Evenity (Romosozumab)

117
Q

Sclerostin (incre/decre) osteoblasts and (incr/decre) osteoclasts

A

Sclerostin decreases osteoblasts and increases osteoclasts

118
Q

Which part of sclerostin regulation is attacked to prevent loss of osteoblastic differentiation?

A

Inhibiting SOST (sclerostin) from binding to LRP 5/6

119
Q

What are clinical uses for calcitonin?

A

Paget’s disease, hypercalcemia

120
Q

What drug is used to provide calcitonin and what is its response to osteoclastic activity and renal reabsorption of phosphate and calcium

A

Salmon (Miacalcin)
Decrease osteoclast activity and block renal reabsorption

121
Q

What drug for calcium receptor sensitization is used for treatment of secondary hyperparathyroidism?

A

Cinacalcet (sensipar)

122
Q

Cinacalcet binds to the receptor as (this) being more responsive to calcium and inhibiting PTH secretion

123
Q

What drug is used for treatment of secondary hyperparathyroidism in CKD with dialysis?

A

Etelcalcetide (Parsabiv)

124
Q

What are the two phosphate binders and their effects on Ca and PO42-

A

Lanthanum Carbonate (Fosrenol)- decreases phosphate and calcium levels
Sevelamer (Renagel, Renvela)- decrease serum phosphate levels selectively

125
Q

What are contraindications for bisphosphonates?

A

Hypocalcemia, renal insufficiency, pregnancy

126
Q

T/F: Bisphosphonate should be taken on an empty stomach

127
Q

Which bisphosphates reduce vertebral, hip, and non-vertebral fractures?

A

Alendronate, Risedronate and Zoledronic acid

128
Q

Ibandronate reduces which fracture?
Vertebral, Hip and/or Non-vertebral

129
Q

What are counseling points for bisphosphonates?

A

Must take on empty stomach, take with full glass of plain water, do not lie down for at least 30 min and wait at least 30 min to eat

130
Q

What should be avoided with bisphosphonates?

A

Mineral water with high Ca content, do not chew, discontinue if heartburn, avoid antacids, increased GI effects with NSAIDs

131
Q

Which bisphosphonates can be used with glucocorticoid-induced osteoporosis?
Ibandroante
Zoledronic acid
Alendronate
Risedronate

A

Risedronate and Zoledronic acid

132
Q

Which fracture risk reduction is associated with menopausal hormone therapy?
Vertebral, hip, non-vertebral

A

Vertebral, hip, non-vertebral

133
Q

What are the two drugs used as Selective estrogen receptor modulators in fracture prevention and what do they reduce?
Vertebral, Hip, Non-vertebral

A

Raloxifene and Bazedoxifene
Vertebral

134
Q

What are black box warnings for raloxifene? Side effects?

A

increase risk of DVT, PE and stroke
SE: hot flashes

135
Q

Internasal Calcitonin effects what is fracture prevention?
Vertebral, Hip, Non-vertebral

136
Q

Denosumab decreases fracture risk in which
vertebral, hip, non-vertebral

A

vertebral, hip, non-vertebral

137
Q

What are denosumab’s clinical pearls?

A

Rebound effect: increase risk of vertebral fracture with discontinuation
Consider indefinite treatment of denosumab, bisphosphonate after discontinuation of denosumab

138
Q

How is denosumab administered?

A

60mg SQ q6 months

139
Q

What two drugs are associated with parathyroid hormone osteoporosis treatment?

A

Teriparatide and Abaloparatide

140
Q

Teriparatide and abaloparatide affect which fracture risk reduction?
Vertebral, Hip, Non-vertebral

A

Vertebral, Non-vertebral

141
Q

How is Teriparatide and Abaloparatide administered?

A

Teri: 20 mcg SQ daily, only 2 yrs
Abalo: 80 mcg SQ daily, only 18 mon

142
Q

What drug uses monoclonal anti-sclerostin antibody for osteoporosis treatment? Where (Vertebral, Hip, non-vertebral)

A

Romosozumab
Vertebral, Hip, non-vertebral

143
Q

Summary

Therapeutics (16 decks)

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