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MSK > Pharm 34 Objectives > Flashcards

Pharm 34 Objectives Flashcards

1
Q

What is the primary reason why women with a uterus also need progestin therapy if they are receiving pharmacologic therapy with an estrogen?

A
  • To oppose estrogen mediated stimulation of the endometrium.
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2
Q

What are the physiologic estrogens?

A
  1. Estrone (EI)
  2. Estradiol (E2)
  3. Estriol (E3)
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3
Q

What are the physiologic progestin?

A

Progesterone

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4
Q

What are the physiologic hormones that could be prescribed?

A

Estradiol and Progesterone

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5
Q

What is the primary ovarian estrogen, and the most abundant estrogen in a woman of reproductive age

A

Estradiol

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6
Q

What are the synthetic estrogens?

A

Ethinyl estradiol (EE) and diethystilbestril (DES)

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7
Q

The structural alteration of the estradiol to ethinyl estradiol causes what?

A

Greatly enhances the potency

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8
Q

What is the primary use of Ethinyl estradiol?

A

Contraceptives and by adding EE you confer the estrogen risks/adverse effects.

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9
Q

What are the synthetic progestins?

A

Medroxyprogesterone acetate (MPA) and Megestrol acetate

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10
Q

The injectable route of Medroxyprogesterone acetate (MPA) is used for what?

A

Progestin-only contraceptives

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11
Q

The oral route of Medroxyprogesterone acetate (MPA) is used for what?

A

Counter balance the effects of pharmacologic estrogen supplementation on the uterus.

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12
Q

What is the clinical use of Megestrol acetate?

A

Cachexia associated with AIDS and other wasting syndromes: breast, prostate and endometrium carcinoma

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13
Q

What are the non-physiologic sources of estrogenic substances?

A
  • Conjugated estrogens
  • Selective estrogen receptor modulators
  • Delestrogens
  • Some phenols
  • Estrogen mimic compounds (soybeans)
  • BPA in plastic bottles
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14
Q

Why is Premarin considered “natural” even though its estrogen content is different from the body’s physiologic estrogens?

A

Conjugated equine estrogens, contain estrogens that are not physiologic for humans but are most similar to estrone.

(come from pregnant horse urine.)

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15
Q

What does SERM mean?

A

Selective estrogen receptor modulator

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16
Q

What are the two classes of antiestrogens that may be used for secondary prevention of breast cancer?

A

SERMs and Aromatase inhibitors

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17
Q

What is the maximum accepted durations of Tamoxifen when using it for secondary prevention of breast cancer?

A

5 yrs

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18
Q

Why should Tamoxifen only be used for 5 yrs?

A

It is an estrogen receptor agonist at the uterus which results in proliferation of endometrial cells which can lead to endometrial, uterine and GI cancers.

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19
Q

Aside from cancer risks from Tamoxifen what other potential severe ASEs can occur if used for greater than 5 yrs?

A
  • Stroke
  • PE
  • QT prolongation
  • Cataracts
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20
Q

What are some common ASEs of Tamoxifen?

A
  • Hot flashes
  • Vaginal dischage
  • Amenorrhea or menstrual changes
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21
Q

Describe the paradigm shift in the medical community regarding the use of “hormone replacement therapy” after the publication of the Women’s Health Initiative study.

A
  • Women received conjugated equine estrogen plus medroxyprogesterone acetate or a placebo
  • Study was halted after 5.6 years due to increased coronary artery disease, stroke, and pulmonary embolism
  • May have reduced risk of colorectal cancer and hip fractures
  • WHI criticized for the older age of participants
    75% of women age 60 and above
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22
Q

What are the effects of administration of exogenous gonadotropin (or an antagonist) on circulating testosterone and estrogen levels?

A
  • Suppress gonadotropin production = decreased production of gonadal hormones
  • Clomiphene (SERM, partial agonism of central estrogen receptor) prevents estrogen’s negative feedback = increases gonadotropin levels
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23
Q

Why is testosterone best administered by non-enteral route?

A
  • High first-pass effect with oral dosage forms

- Liver toxicity occurs with oral testosterone

24
Q

What are the benefits of transdermal testosterone?

A

High transdermal bioavailability and can be administered by gel patches, and injectable.

25
Q

What are the appropriate techniques to reduce the risk for harmful accidental exposure of gonadal hormones?

A

Apply to axillary areas or use a patch

26
Q

Prior to initiating testosterone to treat hypogonadism what must be done?

A

Obtain 2 morning testosterone labs obtained on separate days and if these serum [ ] are below the normal range then you can diagnose with hypogonadism.
- if not than tx is not necessary and may in fact be risky.

27
Q

What hormone antagonist are useful for different hormone responsive cancers?

A
  • Raloxifene
  • Ospemifene
  • Tamoxifen
  • Anastrozole
28
Q

Raloxifene is FDA approved to do what?

A
  • Increase bone density
  • Reduce risk for vertebral fractures
  • decrease risk for uterine and breast cancer
    (used in menopausal women)
29
Q

Raloxifene is contraindicated in patients with what?

A
  • Hx of VTE/stroke

- Pregnancy

30
Q

Tamoxifen is the primary hormonal option for treating what?

A

ER positive breast cancer in post menopausal women and men

31
Q

Tamoxifen and SSRIs are commonly co-administered but what do you need to consider when these are taken together?

A

Consider strong CYPT2D6 inhibitor = can reduce production of the active metabolite.

32
Q

Ospemifene is both an ER antagonist and ER agonist, what does the antagonist aspect prevent?

A

Breast cancer

33
Q

Ospemifene is both an ER antagonist and ER agonist, what does the agonist aspect prevent?

A

Loss of bone density and vaginal atrophy

34
Q

Ospemifene is useful in what type of patients?

A

Pts who have difficulty apply vaginal estrogen therapy products due to dexterity or pain.

35
Q

All SERMs except for Bazedoxifene can increase what?

A

Increase menopausal symptoms

36
Q

What are the short term effects of GnRH agonist on gonadal hormones? (pulsatile administration)

A

Mimic the natural secretion of GNRH and is used to stimulate the release of FSH and LH from the anterior pituitary

37
Q

What are the long term effects of GnRH agonist on gonadal hormones? (sustained administration)

A

Leads to down regulation of the GnRH receptors and decreases secretion of FSH and LH, leading to decrease testosterone and estrogen secretion.

38
Q

What are the effects of GnRH antagonist on gonadal hormones?

A

Rapid reduction in gonadal hormone production, avoding the initial “flare-up” seen with the agonist.

39
Q

Sustained administration with GnRH in men with prostate cancer results in?

A

Synergistic anti-androgen therapeutic effect to simultaneously administered androgen receptor inhibitors

40
Q

What is the current most accepted clinical use of estrogens (and progestins) for “HRT” that is a temporary (months to a couple years) treatment of menopasusal symptom with the lowest effective dose/exposure?

A

Oral conjugated equine estrogens + medroxyprogesterone acetate

41
Q

What is the major use of topical vaginal estrogens?

A

Vulvar-vaginal atrophy sxs (dryness, irritation, soreness, and dyspareunia)

42
Q

Why would a pt want a systemic estrogen for menopause sxs over a topical?

A

If they are having hot flashes and other associated sxs

43
Q

What is the MOA of Tamsulosin?

A

Provides fairly rapid relief of urinary symptoms

44
Q

What is the MOA of Dutasteride?

A

Inhibits both type 1 and type 2, 5a-reductase

45
Q

What is the MOA of Finasteride?

A

Selectively inhibits type 2, 5a-reductase

46
Q

What timeline do you want to be sure to tell the patient when starting them on tx fro BPH?

A

Can take weeks to months to notice improvement in urinary symptoms and six months for the full effect

47
Q

What gonadal hormone agonist drug is not relatively or absolutely contraindicated during pregnancy? and why?

A

Progesterone and hydroxyprogesterone caproate can be supplemented in women who have experience miscarriages due to deficient physiologic progesterone production during pregnancy

48
Q

What are the ASEs of SERMS and aromatase inhibitors?

A

MSK pain and muscle cramps

49
Q

What are the ASEs of SERMS and clomiphene?

A

Thromboembolism

50
Q

What drug class has a lower risk for VTE?

A

Aromatase inhibitor

51
Q

5a-reductase inhibitor is what pregnancy category?

A
  • Cat. X

- women of childbearing age should avoid all contact, and not even touch any dosage forms of 5a-reductase inhibitors

52
Q

What should you counsel all pts on who are taking Tamsulosin?

A
  • Orthostatic Hypotension

- take 30 min after the same meal every day

53
Q

What are some drug classes that worsen urinary sxs in pts with BPH?

A
  • Alpha 1 agonist
  • Androgens
  • Antimuscarinic and anticholinergics
54
Q

Estrogen only tx should only be given to women who have had what?

A

Complete hysterectomy

55
Q

What are BBWs for oral progestins?

A
  • Breast cancer
  • Cardiovascular
  • Dementia

MSK (11 decks)

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