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Pharmacology II > Sex Hormones > Flashcards

Sex Hormones Flashcards

1
Q

Leuprolide (Lupron)

A

GnRH Drug - Long Acting Agonist

– Continuous administration suppresses release of LH
and FSH (after initial surge)
– Used in IVF, sex steroid-dependent
cancers, endometriosis, precocious puberty, gender
affirmation

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2
Q

Cetrorelix (Cetrotide®)

A

GnRH Drug - Antagonist

– Suppress LH and FSH
– Used in IVF, sex steroid-dependent
cancers, endometriosis, precocious puberty, gender
affirmation

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3
Q

Estrogens

A

• Major endogenous estrogens: Estradiol, estriol & estrone

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4
Q

Estrogen - MoA

A

Nuclear Receptor

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5
Q

Estrogen - Metabolism

A

• Conjugated by liver
–Excreted in bile

• Enterohepatic circulation
– Reverses conjugation
– Increases bioavailability

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6
Q

Estrogen Functions in the Ovary

A

prepare for ovulation

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7
Q

Estrogen Functions in the Uterus

A

endometrial growth

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8
Q

Estrogen Functions in the Vaginal Epithelium

A

proliferation, maintenance

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9
Q

Estrogen Functions in the Endocervical Glands

A

mucus

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10
Q

Estrogen Functions in the Breasts

A

growth – pregnancy & puberty

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11
Q

Estrogen Functions in Puberty

A
  • growth and maturation

- closes epiphyses

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12
Q

Estrogen Functions in the Bone

A

maintenance

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13
Q

Estrogen Functions in Blood Clotting

A

↑ synthesis of clotting proteins

↑ platelet adhesiveness

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14
Q

Estrogen Functions in Metabolism

A
  • liver (clotting factors and hormone binding proteins:
    SHBG, CBG, TBG)
  • ↑HDL and ↓LDL
  • Na+ and H2O retention
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15
Q

Exogenous Estrogens

A

– Ethinyl estradiol -> synthetic -> oral contraceptives
– Conjugated estrogens (Premarin®) -> HRT
– Estradiol (Estraderm®) -> creams/patches

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16
Q

Exogenous Estrogens - Uses

A

– Oral contraception
– Postmenopausal hormone replacement therapy (HRT)
– Stimulating pubertal development in hypogonadic
girls
– Decrease uterine bleeding
– Suppressing ovulation in dysmenorrhea
– Male-to-female gender-affirming hormonal treatment

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17
Q

Estrogen Adverse Effects

A

• Endometrial hyperplasia
• Nausea and breast tenderness
• Migraines
• Gallbladder disease
• Hypertension
• Thromboembolism, thrombophlebitis; increased
platelet aggregation; accelerated blood clotting

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18
Q

Estrogen - Contraindications

A
  • Estrogen-dependent neoplasms (e.g., breast cancer)
  • Thromboembolic disorders
  • Undiagnosed genital bleeding
  • Uncontrolled hypertension
  • Liver disease
  • Smoking & over 35
  • Pregnancy
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19
Q

Antiestrogens

A
  • Tamoxifen (Novaldex®)

* Clomiphene(Clomid®)

20
Q

Tamoxifen (Novaldex®)

A

– Selective estrogen receptor modulator (SERM)
– Antagonist:
• Breast - used as palliative and prophylactic
treatment in breast cancer (DOC in premenopausal
women): reduces risk of further breast cancer
– Agonist:
• Bone – limits bone loss
•Uterus – may ↑ risk of uterine cancer
– Raloxifene (Evista®) is better for this (antagonist
in uterus, agonist in bone) -> for osteoporosis

21
Q

Clomiphene (Clomid®)

A

– SERM
– Antagonizes negative feedback of estrogen in
hypothalamus
– Initial infertility therapy
• Stimulates LH & FSH, inducing ovulation
– Multiple pregnancies (5-10%)

22
Q

Aromatase Inhibitors: Anastrozole (Arimidex®) - Indications/Uses

A

– DOC - Breast cancer treatment in postmenopausal
women
– Advanced breast cancer after tamoxifen failure in
postmenopausal women

23
Q

Aromatase Inhibitors: Anastrozole (Arimidex®) - Adverse Effects

A 
Diarrhea
abdominal pain
nausea/vomiting
hot flashes
joint pain
24
Q

Aromatase Inhibitors: Anastrozole (Arimidex®) - Contraindications

A

– Premenopausal women

– Pregnancy Cat X

25
Q

Follicle Stimulating Hormone (FSH)

A
  • Women: develops ovarian follicles and supports estrogen synthesis
  • Men: stimulates spermatogenesis

•Human menopausal gonadotropins (hMG) is FSH & LH (aka menotropins, Humegon®) -> used for FSH

26
Q

Luteinizing Hormone (LH)

A 
•Stimulates ovulation
•Stimulates luteinization of follicles 
•Steroid production:
   –Women: estrogen/progesterone synthesis
   –Men: testosterone synthesis

•human Chorionic Gonadotropin (hCG, Pregnyl®) – Used
instead of LH, has same actions

27
Q

Uses for Gonadotropins

A

• Reversing infertility
• Men: Inducing spermatogenesis:
– LH increases testosterone (for up to a year), FSH
then induces spermatogenesis (take months)
• Women: IVF (ART)
• FSH (9-12 days) stimulates ovaries and estrogen
production, single dose of LH given to induce ovulation

28
Q

Adverse Effects of Gonadotropins

A 
•Side effects
   –Uncomplicated ovarian enlargement 
   –Ovarian hyperstimulation syndrome
   –Multiple births – 20%
   –Gynecomastia – Headache, depression, edema, 
     precocious puberty
29
Q

Contraindications of Gonadotropins

A

– Sex steroid-dependent cancers

30
Q

Progesterone - MoA

A
  • Produced by corpus luteum
  • Produced by fetal/placental unit in pregnant women

• Nuclear receptor

31
Q

Progesterone Biological Functions

A

•Uterus: converts endometrium to a secretory state
– Maintains pregnancy
– Suppresses contractility during pregnancy
• Endocervical glands: regulates cervical mucus
• Breasts: lobuloalveolar development at the end of the
mammary ducts during pregnancy and puberty
• Thermogenic action: increases body temperature

32
Q

Progestins - Uses

A

– Contraception
– Prevent endometrial hyperplasia in HRT
– Treatment of other problems when estrogens are
contraindicated

33
Q

Progestins - Adverse Effects

A

– Possible increased blood pressure
– High doses may reduce plasma HDL levels
• 19-nortestosterones
– Depression and drowsiness

34
Q

Antiprogestin: Mifepristone (RU 486, Mifeprix®)

A

– Progesterone/glucocorticoid receptor antagonist
– Uses:
•Terminate pregnancy (w/ prostaglandins)
•Prevent implantation
– Side effects: vomiting, diarrhea, abdominal or pelvic
pain, and vaginal bleeding

35
Q

Adverse effects of Combination Oral Contraceptives

A 
•Common
 – Weight gain
 – Nausea
 – Edema
 – Depression
•Breakthrough bleeding
 – Progestin alone or too little estrogen
•Try different combinations
•Cardiovascular problems 
 – Clotting
   •Women over 35
   •Smoking
 –Mild hypertension
 –Migraine
 –MI/Stroke
• Cholestatic jaundice and gallbladder disease
• Teratogenesis
• Fertility – can be suppressed for 3+ months
36
Q

Combination Oral Contraceptive Benefits

A

• Effective contraception
• Reduced risk for:
– Ovarian & Endometrial cancer
• 50% reduction, even after 2 years of treatment
• Protection lasts 15 years after discontinuation
– Ovarian cysts
– Benign breast disease
– Ectopic pregnancy
– Iron deficiency, rheumatoid arthritis, PMS, etc.

• Consensus: that it saves 1000s of lives, disease
episodes & hospitalizations every year.

37
Q

Combination Oral Contraceptive Absolute Contraindications

A 
• ASCVD, thromboembolic phenomena, 
  thrombophlebitis, cerebrovascular disorders
• Estrogen-dependent cancers
• Pregnancy
• Smokers & >35 years old
• Uncontrolled hypertension
• Uncontrolled diabetes
38
Q

Combination Oral Contraceptive Relative Contraindications

A 
• Liver disease
• Children who have not yet completed epiphyseal 
   closure
• Migraine
• Smoking
• >35 years old
39
Q

Combination Oral Contraceptive Drug Interactions

A 
• P450 inducers reduce effectiveness
 – phenytoin, rifampin, carbamazepine, etc.
• Antibiotics can reduce effectiveness
 – Stop enterohepatic circulation
• Oral contraceptives decrease effectiveness of:
 – Anticoagulants
 – Anticonvulsants
 – Tricyclic antidepressants
 – Guanethidine
 – Oral hypoglycemics
40
Q

Hormone Replacement Therapy - Adverse Effects

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

Androgens - Physiologic Effects

A

•Virilizing (androgenic) effects
– Spermatogenesis
– Sexual development
• Anabolic effects
– ↑ Bone density
– ↑ Amino acid incorporation into muscle
– ↑ Red blood cell mass
– Antagonize catabolic effects of glucocorticoids
• Puberty: development of secondary sexual
characteristics in males

42
Q

Testosterone Uses

A
  • Testicular deficiency
  • Female hypopituitarism (estrogens and androgens)
  • Hypoproteinemia of nephrosis
  • Negative nitrogen balance patients
  • Female-to-male gender-affirming hormonal treatment
43
Q

Androgens – Side Effects

A 
• Men
 – Decreased spermatogenesis 
 – May exacerbate prostate cancer
• Women
 – Masculinization
 – Pseudohermaphroditism of fetus in pregnant women
• Both Sexes
 – Baldness
 – Fluid retention, edema
 – Oily skin, acne
 – Decreased HDL, increased LDL
 – Psychological changes
44
Q

Androgen Receptor Antagonists

A

Flutamide (Eulexin®)

Spironolactone (Aldactone®)

45
Q

Flutamide (Eulexin®)

A

– Androgen receptor antagonist
– Used in prostate cancer w/ long-acting GnRH agonist
– Hepatotoxic – reversible

46
Q

Spironolactone (Aldactone®)

A 
– Mineralocorticoid antagonist
– High doses antiandrogen
– Uses: 
     •Hirsutism, PCOS, and PMS in women
     •Precocious puberty
47
Q

5α-Reductase Inhibitors: Finasteride (Propecia®)

A 
– Inhibits 5α-reductase (no DHT)
– Suppresses male sex accessory organs without 
   affecting libido
– Uses
     • Benign prostatic hyperplasia
     • Male pattern baldness
– Can cause gynecomastia or impotence(ED) 
– Teratogenic

Pharmacology II (4 decks)

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