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Pharm Flashcards

1
Q

Names & Indications of estrogen

A

-estrols (Hexestrol & Diethylstibestrol)

Cancer therapy
HRT
Contraception

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2
Q

What are we trying to alter in estrogen therapy?

A

The estrogen response-the creation of proteins

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3
Q

Which pharmolocolgic agent is described as “flat and hydrophobic”?

A

Estrogen

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4
Q

Which estrogen receptor gene has a more specialized role and why?

A

Estrogen Receptor Gene-B: dominates in the lung and has limited tissue expression.

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5
Q

List the SERM corepressors

A

Raloxifene
Tamoxifen
Fulvestrant

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6
Q

What are the indications for SERMs?

A

They inhibit the estrogenic effects of breast cancer while maintaining bone mass.

Used in cancer therapy, HRT, and contraception

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7
Q

What are antihormones that inhibit activity by reducing P160 coactivator binding to estrogen receptor surfaces?

A

SERMs

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8
Q

Antagonists in breast, uterus, & CNS
Agonist in bone (bone sparing)
Unknown in liver

A

Raloxifeine - SERM

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9
Q

Antagonist in breast & CNS
Partial antagonist in uterus & liver
Agonist in bone

A

Tamoxifen - SERM

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10
Q

Largest “extra” structure of all anti-estrogens.

So large it degrades the protein

A

Fulvestrant - SERM

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11
Q

Compounds that can have estrogenic activity by binding the ER, but made in plants

A

Phytoestrogens

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12
Q

Give examples of phytoestrogens

A

Isoflavinoid: Soy beans, can relieve menopausal symptoms

Lignnas: High fiber foods

Coumestans: various beans. Alfalfa and clover sprouts are highest.

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13
Q

What are used as HRT?

A

Conjugated Estrogens (Premarin/Equine/Ethyinyl Estradiol)

Estradiols (Estrace and Estraderm)

Duavee

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14
Q

This addresses long-term issues of aging that result from loss of estrogen after menopause

A

HRT

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15
Q

Relief of menopausal symptoms is clear, but longer term benefits harder to prove

A

HRT

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16
Q

Oral Conjugated Estrogens

A

Premarin

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17
Q

Tablet/cream form of estrogen

A

Estrace

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18
Q

Dermal patch form of estrogen

A

Estraderm

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19
Q

HRT that combines SERM + E2 for those worried about endometrial cancer

A

Duavee

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20
Q

What’s the rule in dosing regarding HRT?

A

Use low does that works for a few years (CV benefit is greater in younger women closer to 5-7years post-menopause)

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21
Q

List the aromatase inhibitors

A

Anastorozole
Letrozole
Exemestane

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22
Q

In what population should aromatase inhibitors be used?

A

Only use in post menopausal women

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23
Q

MOA of aromatase inhibitors

A

Aromatase tissue is active in the breast, so we prevent androgens from turning into estrogens which cause growth of breast cancer

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24
Q

Describe the differences between the aromatase inhibitors

A

Anastorozole and Letrozole are competitive inhibitors (substrates) that bind to androgen.

Exemestane is a suicide substrate

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25
Q

List the bisphosphonates

A

Biphoshonates:

  • Alendronate (least potent)
  • Risendronate
  • Ibandronate
  • Zolendronic Acid (most potent)”
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26
Q

What’s the first line treatment of osteoporosis?

A

bisphosphonates

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27
Q

MOA of bisphosphonates

A

Inhibit farnesyl pyrophosphate synthase –> osteoclasts apoptose –> bone breakdown decreases

As osteoclasts die off, the messages they normally send to osteoblasts are reduced –> less osteoblast activity (which is why drug holidays are needed)

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28
Q

What drugs decrease vertebral and non-vertebral fx?

A

Bisphosphonates

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29
Q

Which drugs require a drug holiday and why?

A

Bisphosphonates - Needed to allow osteoblast activity to reset

Monitor bone mineral density and turnover markers during holiday

Re-initiate therapy if density declines or markers increase

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30
Q

AEs of bisphosphonates

A

Esophagitis (with oral forms)

Avascular necrosis/osteonecrosis of jaw

Atypical fragility fractures and delayed healing

Contraindicated in eGFR <30-35%”

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31
Q

Which drug is approved for women receiving aromatase inhibitors and men receiving hormone ablation for prostate cancer

A

Denosumab

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32
Q

MOA of denosumab

A

Humanized monoclonal antibody to RANKL put out by osteoblasts

Prevent formation of active osteoclasts and inhibit bone resorption

Does not absorb into bone matrix

Bone turnover is not suppressed after its cessation”

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33
Q

Things to keep in mind regarding denosumab

A

Shorter HL than Biphosphontes

Stopping therapy can lead to high risk of multiple vertebral fractures

Do NOT d/c without considering replacement with another anti-resorptive tx

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34
Q

AE of denosumab

A

Atypical fragility fractures

AVN of jaw

Increased risk of infections (cellulitis, endocarditis)

Suppression of bone turnover (delayed fx healing)

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35
Q

Contraindications of denosumab

A

Current hypocalcemia

Pregnancy

Hypersensitivy

36
Q

Indication of teriparatide

A

Moderate to severe osteoporosis (ex: from GC use)

37
Q

MOA of teriparatide

A

It’s a PTH analog.

  • Increases bone formation by the same mechanism as low levels of PTH.
  • Stimulates osteoclasts to release Ca2+ from bone and increase Ca2+ reabsorption from the gut and kidney.
  • Low levels are anabolic and stimulate collagen synthesis
38
Q

Which osteoporosis drug is administered SC

A

Teriparatide

39
Q

AEs of teriparatide

A

Mild hypercalcemia

Nausea, HA, dizziness, muscle cramps

Do NOT give >2yrs

Do not use with bisphosphonates

40
Q

Contraindications of teriparatide

A

Hypercalcemia

Multiple myeloma, bone metastasis, skeletal tumor

Children/teens with growing bones

41
Q

In which tissue does Estrogen Receptor Gene A dominate?

A

Reproductive tissue and the liver

42
Q

MOA of SERM coactivators

A

dimerize E2 –> less E2 affinity for DNA

–> increase transcription –> DNA relaxation

43
Q

MOA of SERM corepressors

A

tighten up DNA and suppress gene expression

44
Q

Which SERM is used for breast cancer treatment?

A

Tamoxifen

45
Q

Which SERM is used for bone retention?

A

Raloxifene

46
Q

Why does breast cancer best respond to this SERM drug?

A

Tamoxifen - due to its action on both the Estrogen-Receptor and Progesterone-Receptor

47
Q

AE of Tamoxifen

A
  • Increase in endometrial cancer in postmenopausal women
  • Thromboembolic events
  • Cataracts
48
Q

AE of aromatase inhibitors

A

Osteoporosis

49
Q

Indication of Trastuzumab

A

Breast cancer

50
Q

MOA of Trastuzumab

A

-Acts on protein made by Her2/neu

51
Q

AE of Trastuzumab

A
  • Heart failure (cardiotoxicity)
  • Respiratory problems
  • Serious allergic rx
52
Q

MOA of progestin

A
  • Thins endometrium: can lead to atrophy
  • Thickens cervical mucus
  • Decreases tubal motility
  • Several generations with varying androgen effects and bioavailability
53
Q

MOA of ethinyl estradiol

A
  • Suppress ovulation: along with progestin, negative feedback to hypothalamus and pituitary to decreased FSH/LH production
  • Estrogen suppression of FSH stops folliculogenesis
  • Cycle control: stabilizes endometrium
54
Q

Advantages of COC

A
  • Rapid reversibility
  • Decreased ovarian and endometrial cancer risk
  • Improved acne and hirsutism
  • Improved dysmenorrhea and AUB
  • Reduced symptoms of endometriosis
55
Q

Disadvantages of COC

A
  • Increased hypercoagulability: VTE (greatest risk in 1st year of use)
  • MI, stroke: MINIMAL increased risks in adolescents/young adults
56
Q

Contraindications of COC

A
  • Smokers >35yo should discontinue OCPs

- Hx of heart disease, HTN, VTE, stroke, breast cancer, migraines with aura

57
Q

Hormone in POP

A

Norethindrone (a progesterone)

58
Q

POP indication

A

Use in women in whom estrogen-containing pills are contraindicated

59
Q

Advantages of POP

A
  • Safety: lower dose of hormone - greater safety than COC

- Few contraindications: estrogen-free

60
Q

Disadvantages of POP

A
  • Decreased efficacy compared to COC
  • Menstrual cycle disturbances!!!
  • Strict compliance necessary: use back up method of contraception (condom) for 2 days if >3hrs late taking pill.
  • Increased rates of functional ovarian cysts
61
Q

Hormone(s) in the transdermal contraceptive patch

A

Estrogen and Progestin

62
Q

Which contraceptives only contain progestin?

A
  • POP
  • Depo
  • Implantables (Nexplanon, IUDs - except ParaGard)
  • Plan B - Levonorgestrel
63
Q

Advantages of the transdermal contraceptive patch

A
  • Increased compliance: 1 patch/week with 1 patch free week
  • Forgiving: 3 day error with decreased follicular size vs. pill
  • Does not cause weight gain
  • Good cycle control
  • Verifiable
64
Q

Disadvantages of the transdermal contraceptive patch

A
  • Possible increased risk of VTE (debatable)
  • Skin reactions: in up to 50%
  • Breast tenderness, headache, nausea
  • Less effective in those over 90 kg
65
Q

Which hormones does the Nuvaring contain?

A

Ethinyl estradiol and etonogestrel

66
Q

Advantages of the Nuvaring

A
  • Inhibits ovulation for at least 35 days
  • Increased bioavailability through vaginal absorption, allows lower dose
  • Low, steady release of hormone
  • Does not cause weight gain
  • No effect on bone density
67
Q

Disadvantages of the Nuvaring

A
  • Risks similar to OCPs
  • Headache: most common side effect
  • Vaginal symptoms: most common reason for discontinuation
  • Leukorrhea
  • Foreign body sensation
  • Expulsion
  • Comfort with insertion/removal
68
Q

Which hormones does the Depo injection contain?

A

Medroxyprogesterone acetate

69
Q

MOA of the Depo

A

Inhibits ovulation: eliminates LH surge

70
Q

Advantages of the Depo

A
  • *-Estrogen-free**
  • Lasts 3 months
  • Effective in obesity
  • Decreased/absent menses
  • Minimal drug interactions
  • Can reduce frequency of grand mal seizures and pain associated with endometriosis
71
Q

Disadvantages of the Depo

A
  • Menstrual cycle disturbances
  • *-Weight gain**
  • *-Decreased bone density (BBW)**
  • Depression (conflicting data)
  • Delayed fertility, continued side effects after discontinuation
  • Frequent visits to health care provider
72
Q

Which hormones does the Nexplanon contain

A

Etonogestrel

Progestin only

73
Q

Advantages of the Nexplanon

A
  • Highly effective
  • Lasts 3 years
  • Discreet
  • Decreased dysmenorrhea
  • Quick return to fertility
74
Q

Which hormone do the hormonal IUDs contain?

A

Levonorgestrel

Progestin only

75
Q

MOA of hormonal IUDs

A

Inhibits sperm capacitation and survival

76
Q

Which IUD works up to 7 years?

A

Mirena & Lilleta

77
Q

Which IUD works up to 5 years?

A

Kyleena

78
Q

Which IUD works up to 3 years?

A

Skyla

79
Q

Which IUDs lead to lighter and less frequent menses?

A

Mirena and Lilleta

80
Q

What is the most effective emergency contraceptive?

A

Copper IUD

It must be inserted 5-7 days post unprotected sex

81
Q

How long after sex can someone use Levonorgestrel as emergency contraception?

A

Ideally within 72hrs post-intercourse but can be effective up to 5 days (120hrs)

82
Q

Which contraceptive is a progesterone blocker?

A

Ulipristal Acetate (Ella)

83
Q

Other than the copper IUD, what is more effective in preventing pregnancy as an emergency contraceptive than Levonorgestrel Emergency Contraception?

A

Ulipristal Acetate (Ella)

84
Q

How long after intercourse must Ulipristal Acetate (Ella) be taken as an emergency contraceptive?

A

Within 5 days

85
Q

After using Ulipristal Acetate (Ella), how long should someone wait before starting hormonal contraception?

A

They can start hormonal contraception 5 days after using Ulipristal Acetate (Ella)

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