Progestins, Estrogens and Androgens Flashcards

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1
Q

Estradiol

A
  • Estrogens
  • Rapidly inactivated when given orally - Prevent ovulation by inhibiting pituitary and hypothalamus, decrease amount and increase viscosity of cervical mucus
  • Contraception
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2
Q

Ethinyl estradiol

A
  • Estrogens
  • Prevent ovulation by inhibiting pituitary and hypothalamus, decrease amount and increase viscosity of cervical mucus
  • Nausea, headaches, CV effects, decreased glucose tolerance, weight gain
  • Combination OCP (continuous or discontinuous), ovarian dysfunction, PM symptoms
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3
Q

Tamoxifen

A
  • SERMs
  • Breast antagonist, agonist at other tissues (Raloxifene neutral at endometrium/vagina)
  • Estrogen dependent breast cancer, relief of PM symptoms, osteoporosis
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4
Q

Ospemifene

A
  • SERMs
  • Breast antagonist, agonist at other tissues, neutral at endometrium
  • Breast cancer, vaginal atrophy
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5
Q

Clomiphene

Fluvestrant

A
  • Estrogen receptor antagonists
  • Give in early follicular phase to antagonize inhibitory effects of estrogen on pituitary and hypothalamus
  • Ovulation induction
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6
Q

Anastrozole (non-steroid)

Exemestane (steroid)

A
  • Aromatase inhibitors
  • Inhibit conversion of androgens to estrogens
  • Hot flashes, effects on plasma lipids and bone resorption
  • Breast cancer, ovulation induction
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7
Q

Drospirenone

A
  • Progestins
  • Enhanced activity as mineralocorticoid and androgen antagonist - prevent ovulation by inhibiting hypothalamus and pituitary, prevent fertilization by decreasing amount and increasing viscosity of cervical mucus,
  • Nausea, headaches, CV effects, decreased glucose tolerance, weight gain
  • Combination OCP (continuous or discountinous), ovarian dysfunction, PM symptoms
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8
Q

Progesterone

A
  • Progestins
  • Rapidly inactivated when given orally –prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary
  • Headaches, abnormal menstrual bleeding (irregular periods)
  • Contraception (continuous), dysmenorrhea, endometriosis
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9
Q

Medroxyprogesterone acetate

A
  • Progestins – IM injection
  • Prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary
  • Headaches, abnormal menstrual bleeding (irregular periods)
  • Progestin only IM injections (every 3 months)
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10
Q

Norethindrone

A
  • Progestins – oral or IUD
  • Prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary
  • More cross reactivity – headaches, abnormal menstrual bleeding

Combination - Nausea, headaches, CV effects, decreased glucose tolerance, weight gain

*Progestin only OCP and IUD (continuous)

Combination OCP (continuous or discontinuous), ovarian dysfunction, PM symptoms

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11
Q

Norgestrel

A
  • Proogestins – oral or IUD
  • Prevent fertilization by decreasing amount and increasing viscosity of cervical mucus, prevent ovulation by inhibiting hypothalamus and pituitary (emergency)
  • Progestin - headaches, abnormal menstrual bleeding

Emergency – nausea and vomiting, headache, dizziness, breast tenderness, abdominal/leg cramps

*Progestin only OCP and IUD, dysmenorrhea, endometriosis

Emergency contraception (take within 72 hours – no prescription)

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12
Q

Ulipristal

A
  • SPRMs – more effective than norgestrel
  • Inhibits ovulation by antagonizing actions of progesterone on granulosa cell progesterone receptor
  • Emergency contraception within 5 days (oral, prescription required)
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13
Q

RU 486

A
  • Progestin receptor antagonists
  • Inhibits ovulation by antagonizing actions of progesterone on granulosa cell progesterone receptor
  • Emergency contraception within 5 days (oral, prescription required)
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14
Q

FSH

A
  • Gonadotropins
  • Used to induce follicular growth
  • In vitro fertilization
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15
Q

CG

A
  • Gonadotropins
  • Used to induce ovulation
  • Diagnostic for pregnancy, IVF
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16
Q

Gonadorelin

A
  • GnRH analog
  • Stimulate gonadotropin secretion (single injection or with a pump)
  • Delayed puberty, anovulatory disorders
17
Q

Luprolide

A
  • GnRH agonist (long acting)
  • Suppress gonadotropin secretion
  • Desensitization - injectable
18
Q

Cetrorelix

A
  • GnRH antagonist
  • Injectable – stop gonadotropin secretion in ovulation-induction protocols
  • Precocious puberty, androgen excess, endometriosis, dysmenorrhea
19
Q

Testosterone

Testosterone propionate

A

*Androgen
*Inactive when given orall but can be given transdermally or as buccal tablets
Propionate given IM
*Virilization feminization, suppression of HPG axis, edema, jaundice, hepatic carcinoma
*Male hypogonadism, muscle wasting in AIDS

20
Q

Methyltestosterone

Danazol

A
  • 17a-alkylated androgen
  • Given orally
  • More severe - virilization feminization, suppression of HPG axis, edema, jaundice, hepatic carcinoma
  • Male hypogonadism, muscle wasting in AIDS
21
Q

Dutasteride

Finasteride

A
  • 5a-reductase inhibitor (oral)

* Benign prostatic hyperplasia, prostate cancer, hirsutism, CAH, male precocious puberty

22
Q

Bicalutamide
Flutamide
Nilutamide

A
  • Androgen receptor antagonist (oral)

* Benign prostatic hyperplasia, prostate cancer, hirsutism, CAH, male precocious puberty