Repro-Endo: Female Repro Flashcards Preview

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Flashcards in Repro-Endo: Female Repro Deck (46)
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1

Mechanism of Leuprolide?

  • Leuprolide and Goserelin
  • GnRH anolog
  • Pulsatile --> Agonist
  • Continous -->Antagonist 
    --> Downregulates GnRH in Pituitary 
    --> Decrease LH and FSH

2

Clinical Use of Leuprolide?

  • Pulsatile --> Infertility
  • Continous --> w/ Flutamide for 1 wk Testosterone surge.
    • Prostate cancer
    • Uterine Fibroids
    • Endometriosis
    • Polycystic Ovary Syndrome
    • Precocious puberty

3

SEs Leuprolide?

  • Antiandrogen
  • Nausea
  • Vomiting
  • Headache (Light-headedness)
  • Hypoestrogenic state
    • Hot flashes
    • Vaginal dryness
    • Bone density loss

4

Mechanism of Estrogens?

  • Binds to Estrogen Receptors
  • Stimulates Endometrial Growth
  • Reduces LDL, Raises HDL
  • Steroidal: Ethinyl Estradiol and Mestranol
  • Nonsteroidal: Diethylstilbestrol (DES)
  • Natural: Premarin-conjugated estrogens
    • Soy Isoflavones, Red clover, Black cohosh, Vit. E

5

Clinical use of Estrogen?

Females:

  • Birth Control
  • Cycle regulation
  • Hypogonadism
  • Ovarian failure
  • Menstraul abnormalities
  • Hormone Replacement Therapy - post menopausal w/out a History of Breast Cancer
     
  • Men: Androgen-dependent Prostate cancer

6

SEs Estrogens?

  • Estrogen w/out Progesterone --> Endometrial cancer
  • DES --> Clear Cell Adenocarcinoma
  • Bleeding in the Postmenopausal women
    • Increased Risk of Thrombi (Hypercoagulable)
       
  • Contraindicated:
    •  ER+ Breast cancer and History of DVTs
    • ​Uncontrolled HTN
    • Migraines w/ Aura
    • Smokers > 35 y.om (microthrombi risk)

7

(3) Selective Estrogen Receptor Modulators (SERMs)?

  1. Clomiphene
  2. Tamoxifen
  3. Raloxifene

8

Mechanism of Clomiphene?

  • Estrogen receptors Antagonist in Hypothalamus
  • Prevents normal feedback inhibition
    --> Increased GnRH
    --> Increased Release of LH and FSH from Pituitary
    --> Stimulates ovulation (Increased)

9

Clinical use of Clomiphene?

  • Infertility due to Anovulation
    • PCOS
    • Fertility

10

SEs of Clomiphene?

  • Hot flashes - Temp. Control w/in Hypothalamus
  • Ovarian enlargment
  • Multiple simultaneous pregnancies
  • Visual Disturbances (Blurring, Diplopia)
  • GI and Breast Discomfort (tenderness)

11

Mechanism of Tamoxifen?

  • Partial Estrogen receptor Agonist/Antagonist (SERM)
  • Upregulates TGF-β
  • Must be activated by CYP2D6
    • ​SSRIs (Fluoxetine) inhibit CYP2D6 - contraindicated
  • AntagonistBreast tissue
  • Agonist - Uterus (Endometrial Tissue) and Bone
    • A/w Endometrial cancer
    • A/w Thomboemboitic events

12

Clinical use of Tamoxifen?

  • Post-Menopausal (50+) women
  • Hormone Replacement Therapy (HRT) w/ Family History
  • ER+ Breast cancer
  • Progesterone-resistant Endometrial and Ovarian cancer
  • Melanoma
  • Osteoporosis
  • Discontinue after 5 years: acts as an Agonist in Breast

13

Mechanims of Raloxifene?

  • SERM
  • Antagonist - Breast and Uterus (Endometrium)
  • Agonist - Bone
    • Increased risk of Thromboembolic events
    • Decreased Resportpion of bone
       
  • ER+ Breast Cancer w/ History of Endometrial cancer
  • Osteoporosis
  • SE: Hot flashes, Sweating/warmth, Increased Vaginal Discharge, Joint/Muscle pain, Increased Thromboembolism

14

Hormone Replacement Therapy (HRT)?

  • Relief or Prevention of Menopausal symptoms
    • Hot flashes, Vaginal atrophy
    • Osteoporosis (Increased Estrogen, Decreased Osteoclast activity)
  • Unopposed Estrogen Replacement Therapy (ERT)
    • Incrased Risk of Endometrial cancer so Progesterone is added
  • Increased Cardiovascular risk in Older women /w Higher doses

15

Anastrozole (Letrozole) / Exemestane?

  • Aromatase Inhibitors used in Postmenopausal women w/ Breast cancer
  • Better than Aminoglutethimid, no effect on Mineralocorticoid or Glucocorticoid synthesis
  • Continue to be effective beyond 5 years
  • No Risk of Endometrial cancer or Thromboemboilic events

16

Mechanism of Progestins?

  • Megestrol, Medroxyprogesterone
  • Bind Progesterone receptors
  • Decrease growth
  • Increased Weight gain
    • ​Anorexia-cachaexia related to Cancer and AIDS
  • Increase Vascularization of Endometrium
    --> Stimulates Endometrial glandular secretions
    --> Spiral artery development
    --> Suppresses ovulation

17

Clinical use of Progestins?

  • Birth Contorl and Ovulation suppresion
  • Menstrual cycle control
  • Stabilization of Endometrium
  • Uterine control and Protection
  • Stimulate appetitie in Cachectic patients

18

Mechanism of Mifepristone (RU-486)?

  • Competitive inhibitor of Progestins at Progesterone Receptors
    --> Lose Progesterone --> Lose Endometrial layer
    --> Lose Pregnancy

19

Clinical use of Mifepristone (RU-486)?

  • Termination of Pregnancy
    --> Inhibit Progesterones --> Lose Pregnancy
  • Administered w/ Misoprostol (PGE1)

20

SEs of Mifepristone (RU-486)?

  • Heavy Bleeding --> sloughing of Endometrial layer
  • Abdominal Pain
  • GI effects
    • Diarrhea
    • Nausea
    • Vomiting
    • Anorexia

21

Oral Contraception?

(Synthetic Progestins, Estrogen)

  • Estrogen and Progestin inhibit LH / FSH
    --> Prevent Estrogen surge
    --> No LH surge --> No Ovulation
  • Progestins cause thickening of the Cervical mucus
    --> Limiting access of Sperm to Uterus
  • Progestins inhibit Endometrial Proliferations
    --> Endometrium less suitbale for Implantation of Embryo
  • Contraindicated: Smokers > 35 y.o. (Cardiovascular events), History of Thromboemobilsm, Stroke, ER+ tumor

22

Terbutaline?

  • β2-adrenergic receptor agonist
  • Relaxes the Uterus (Myometrial relaxation)
  • Used to decrease Contraction Frequency in women during Labor

23

Mechanism of Danazol?

  • Synthetic Androgen that acts as a Partial agonist at Androgen receptors

24

Clinical use of Danazol?

  • Endometriosis
  • Hereditary Angioedema

25

SEs of Danazol?

  • Androgenic effects
    • Weight gain
    • Edema
    • Acne
    • Hirsuitism
    • Masculinization
  • Decreased HDL lvls
  • Hepatotoxicity

26

Mechanism of Testosterone, Methyltestosterone?

  • Agonist at Androgen receptors
  • Modifies gene transcription upon conversion to DHT
  • Negatively regulates LH production in Ant. Pit.

27

Clinical use of Testosterone, Methyltestosterone?

  • Hypogonadism - Testicular failure
  • Anemia
  • Promotes secondary Sex characteristics
  • Anabolic stimulation to Promote recovery after Burn or Injury

28

SEs of Testosterone, Methyltestosterone?

  • Premature closure of the Epiphyseal Plates
  • Increased LDL
  • Decreased HDL
  • Masculinization in Females
  • Decreased Intracellular Testosterone in Males by Inhibiting the release of LH (via negative feedback)
    --> Gonadal atrophy

29

Finasteride / Dutasteride?

  • 5α-reductase inhibitor (decreased conversion of Testosterone to DHT)
  • Benign Prostate Hyperplasia (BPH)
  • Promotes Hair growth --> Male pattern baldness
    • To prevent male-pattern hair loss, give a drug that will encourage female breast growth
  • SE: Breast enlargment/tenderness, Lip swelling, Testicular pain, GI distress (diarrhea, Ab pain) Loss of Libido, Erectile dysfunction
  • Pregnant women --> Hypospadias in Male fetus

30

Flutamide?

  • Anti-androgen that COMPLETELY antagonized the Testosterone receptor
  • Used w/ Leuprolide (GnRH) for Testosterone surge
  • Nonsteroidal Competitive Inhibitor of Androgens at the Testosterone Receptor
  • Prostate cancer
  • Hirsutism in Women
  • SE: Hot flashes, Diarrhea, Nausea, Gynecomastia, Impotence, Hepatitis, Loss of Libido, Low Volume Ejaculate, Breast Tenderness and Enlargement