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Pharm 2 > Sex Hormones > Flashcards

Sex Hormones Flashcards

1
Q

Which drugs are GnRH agonists? How are they different from antagonists?

A

Leuprolide and Goserelin

They have a longer lasting effect

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2
Q

Which drugs are GnRH antagonists?

A

Cetrorelix and Ganirelix

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3
Q

What are GnRH drugs used for?

A

precocious puberty, endometriosis, etc.

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4
Q

How do you treat metastatic prostate cancer?

A

With an antiandrogen, avoid using an agonist because of initial surge of Testosterone

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5
Q

What two drugs are used to mimic LH and FSH? Which one is FSH only?

A

hMG and Urofollitropin; Uro is FSH only

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6
Q

What does LH do? Which drug is used to replace LH?

A

causes ovulation and increases progesterone; hCG is used to stimulate ovulation and for steroid production (controls when LH surge happens)

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7
Q

What are LH and FSH used for?

A

REVERSING INFERTILITY

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8
Q

What are the SE of gonadotropins?

A

Mostly trophic effects except for OHS: EMERGENT SITUATION! vascular perm increases, fluid builds up everywhere, hypovolemic, will go into shock! If you start feeling really bad, get to ER immediately

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9
Q

What is the MOA for estrogens?

A

binds to a nuclear receptor because they are lipophilic, but that means they take time

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10
Q

How are estrogens metabolized?

A

by the liver, they enter enterohepatic circ which increases T1/2

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11
Q

What are major adverse effects of estrogen?

A
  • Endometrial hyperplasia
  • Nausea and breast tenderness
  • MIGRAINES– leads to OHS
  • Gallbladder disease
  • HYPERTENSION
  • Thromboembolism, thrombophlebitis; increased platelet aggregation; accelerated blood clotting
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12
Q

What are contraindications for estrogen use?

A 
Estrogen-dependent neoplasms (e.g. breast cancer)
•Undiagnosed genital bleeding
•Uncontrolled hypertension
•Liver disease
•Thromboembolic disorders
•Smoking & over 35
•Pregnancy
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13
Q

What are the estrogens?

A

Ethinyl estradiol (Not available individually)
Estradiol (Estraderm®)
Conjugated estrogens (Premarin®)
Estropipate (Ogen®)

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14
Q

What are the SERMs (can be agonist or antagonist)?

A

Tamoxifen, Toremifene, Raloxifene, Clomiphene

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15
Q

What are indications for tamoxifen or toremifene use as an antagonist?

A

for palliative tx of PREMENOPAUSAL breast CA

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16
Q

What are effects of tamoxifen and toremifene as an agonist

A

LIMITS BONE LOSS but may increase risk of uterine CA

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17
Q

Which SERM is better to use for a person with already low HDL?

A

Toremifine

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18
Q

Which of the antiestrogens is not a SERM but a complete antagonist? What sx does it cause?

A

Fulvestrant; menopausal type sx

not used due to use of aromatase inhibitors

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19
Q

Which SERM antagonizes negative feedback of estrogen in hypothalamus to increase LH and FSH thereby inducing multiple pregnancies as a side effect of medication?

A

CLOMIPHENE

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20
Q

What drugs are aromatase inhibitors?

A

Anastrozole, letrozole, exemestrane

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21
Q

What drugs are used as the DOC for breast cancer treatment in postmenopausal women as well as for advanced breast cancer after tamoxifen failure in postmenopausal women?

A

Aromatase inhibs

22
Q

What are absolute CI of aromatase inhibs?

A

PGN, premenopause

23
Q

What are AR of aromatse inhibs?

A

Post menopausal, abd pain, N/V/D

24
Q

Which progestins have both progestin and androgenic activity? What are their names?

A 
19-nortestosterones:
Levonorgestrel (Plan B®)
Norethindrone (Aygestin®)
Norgestrel (Ovrette®)
Norgestimate
25
Q

What are some SE of progestins?

A

Possible increased blood pressure
High doses may reduce plasma HDL levels
(19-nortestosterones esp)
Depression and drowsiness

26
Q

Which antiprogestin acts as both a porgesterone and glucocoricoid receptor antagonist and is used for abortions? Who is it CI in?

A

Mifepristone; PGN

27
Q

Which antiprogestin is a weak progestin and androgen used to treat endometriosis?

A

danazol

28
Q

What are the two progesterone derivatives?

A

Medroxyprogesterone (Provera®)

Megestrol (Megace®)

29
Q

What drug has the ability to reduce water retention, thus it is the only combination pill that is FDA approved for reducing PMDD symptoms?

A

Drospirenone/ethinyl estradiol (Yasmin, Yaz); Estrogen and spiro derivative with progesterone agonist effects!!!

30
Q

What are main adverse effects of combination oral contraceptives?

A

–Increased breakthrough bleeding, especially during first year
–Hard to tell if you are pregnant and should have discontinued pill

31
Q

What are the combination oral contraceptives?

A

Norethindrone/ ethyinyl estradiol (Brevicon®, Modicon®, Ovcon®)
Levonorgestrel/ ethinyl estradiol (Triphasil®, Tri-Levlen®)
Norethindrone acetate/ ethinyl estradiol (Loestrin®)
Norgestrel/ ethinyl estradiol (Ovral®)
Norethindrone/mestranol (Norinyl®, Ortho-Novum®)
Norgestimate/ethinyl estradiol (Ortho Tri-Cyclen®)
Drospirenone/ethinyl estradiol (Yasmin®, Yaz®)
Dienogest/estradiol valerate (Natazia®)

32
Q

What three drugs are used for post-coital contraception?

A

Mifepristone, Levonorgesterel (P only), Preven (E&P)

33
Q

What are major adverse effects of combined oral contraceptives?

A
  • Cardiovascular problems, esp clotting in smoking women over 35, Mild hypertension, Migraine, MI/Stroke
  • Cholestatic jaundice and gallbladder disease
  • Teratogenesis
  • Fertility – can be suppressed for 3+ months
34
Q

What are some major benefits form combined oral contraceptives?

A

Ovarian & Endometrial cancer

50% reduction in endometrial and ovarian cancer, even after 2 years of treatment, lasts 15 years following d/c

35
Q

What are absolute contraindications for combined oral contraceptives (not progesterone based)?

A
  • Thrombophlebitis
  • Thromboembolic phenomena
  • Cerebrovascular disorders
  • Estrogen-dependent neoplasms
  • Pregnancy
36
Q

What are RELATIVE contraindications for combined oral contraceptives?

A 
LIVER DISEASE
•Adolescents prior to epiphyseal closure
•Asthma; eczema
•Migraine; hypertension
DIABETES
•Optic neuritis; retrobulbar neuritis
•Seizure disorders
SMOKING OVER 35
37
Q

What do oral contraceptives decrease the effectiveness of?

A 
–Anticoagulants
–Anticonvulsants
–Tricyclic antidepressants
–Guanethidine
–Oral hypoglycemics
38
Q

What drugs will reduce the effectiveness of oral contraceptives?

A

•P450 inducers reduce effectiveness
–phenytoin, rifampin, carbamazepine, etc.
•Antibiotics can reduce effectiveness
–Stop enterohepatic circulation

39
Q

What should you give a woman for HRT who has had a hyster?

A

Estrogen only because they have no endometrium for the progesterone to inhibit hyperplasia of

40
Q

What are adverse effects of HRT?

A 
–Endometrial cancer – progestins reduce
–Breast cancer – small risk (1.25 fold)
•8 cases per 10,000 women/year
–Gallbladder disease (2.5 fold)
–Cardiovascular
41
Q

In what age group could estrogen be the most effective for cardioprotection and breast cancer protection?

A

age 50-59

42
Q

What is the general guideline for HRT?

A

10 Years after menopause = HRT is not so great

43
Q

What is an option Dr. Call would recommend for using HRT?

A

Put a woman on ERT for 10 years, then 10 years with raloxifene, then switch something else, if anything because at this point we have protected bones for long enough that we are out of the woods and might not even need estrogen

44
Q

What are androgens used for in men? Women? Both?

A 
Men: Testicular deficiency
Female hypopituitarism (estrogens and androgens)
Both: to treat hypoproteinemia of nephrosis and negative nitrogen balance patients (burns, etc)
45
Q

What two drugs are found in the androgen category?

A

testosterone and methyl-testosterone

46
Q

What drugs are considered anti-androgens?

A

Flutamide, bicalutamide, nilutamide, spironolactone

47
Q

What drug works as an androgen receptor antagonist to treat prostate cancer in combo with a long acting GnRH agonist?

A

Flutamide, just given until GnRH agonist kicks in

48
Q

What drugs are considered 5a-reductase inhibitors?

A

Finasteride and Dutasteride

49
Q

What some indications for use of finasteride and dutasteride?

A

BPH, male pattern baldness: suppressess male sex accessory organs without affecting libido

50
Q

What are some side effects of 5-alpha reductase inhibitors?

A

POTENT TERATOGEN!

51
Q

Which SERM is used to treat breast cancer with a decreased risk of uterine CA?

A

Raloxifene

Pharm 2 (11 decks)

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