Endocrine: Sex Hormones

Question 1

Clomiphene

Answer 1

SERM and estrogen antagonist at hypothalamus

Question 2

Indications of clomiphene

Answer 2

1. Anovulatory infertility

2. Oligospermia infertility

Question 3

S/Es of clomiphene

Answer 3

1. Multiple pregnancies
2. Hot flushes

Hot flushes because FSH and LH are vasodilatory

Question 4

Centchroman other name

Answer 4

Ormeloxifene

Question 5

Ormeloxifene action and indications

Answer 5

Estrogen receptor ANTAGONIST at ENDOMETRIUM

Indication: OCP, non-steroidal

Question 6

Ospenifene indication

Answer 6

Post menopausal dyspareunia

Question 7

Fulvestrant

• parent class
• MOA
• site of action
• indication
• RDA

Answer 7

• SERD: selective estrogen receptor downregulator
• Inhibits ER dimerization. Hence, increases its degradation
• Breast: selectively downregulates breast estrogen receptors
• Breast cancer: ER positive, tamoxifen resistant
• Monthly, i. m. in the butt

Question 8

Tibolone

• parent class
• MOA
• indications

Answer 8

• STEAR: selective tissue estrogen activity regulator
• metabolites exert estrogenic, progestational, weak androgenic effects in specific tissues
• designer HRT: relieves osteoporosis and vaginal atrophy with no increased cancer effect on breast and endometrium

Question 9

Third generation AIs

Answer 9

• Letrozole
• Anastrozole
• Exemestane

Question 10

AI indications

Answer 10

Postmenopausal breast cancer

Because aromatisation is the major source

Question 11

Generations of progesterone

Answer 11

1st Norethindrone
2nd Levonorgestrol
3rd Norgestimate
4th Drospirenone

Question 12

Pregesterones are usually androgenic. Name an anti-androgenic progesterone? Indications?

Answer 12

Drospirenone (of spironolactone group)

Indications

• combined OCP
• moderate acne (FDA app)
• PMS dysphoria (FDA app)

Question 13

SPRM examples

Answer 13

Selective progesterone receptor modulator

Mifepristone
Onapristone
Ulipristal

Question 14

Uses of mifepristone

Answer 14

Mm: MIFEPrIstone

Morning after pill (emergency contraceptive)
Induction of abortion ( <49 days)
Fibroids
Endometriosis
PR positive cancers : breast cancer, meningioma
Increased steroids (Cushing syndrome)

tone

Question 15

Mife is an antagonist at ?

Answer 15

1. Progesterone receptor
2. Androgen
3. Glucocorticoid

Question 16

Onapristone MOA and indications

Answer 16

MOA: antagonist at PR of endometrium ONLY

Indication: induction of abortion

Question 17

Ulipristal indication

Answer 17

Emergency contraceptive

Question 18

Exclusive actions of testosterone (not shared by dihydrotestosterone)

Shared actions

Answer 18

Mm: FISH

Feedback inhibition
Internal sex organs
Spermatogenesis
Hematopoeisis

Shared: Secondary sex characters, anabolic effects

Exclusive actions of testosterone are despite DHT having a higher affinity for androgen receptor than testosterone

Question 19

Harmful effects of excess testosterone

Answer 19

1. BPH

2. Prostate cancer

Question 20

Drugs for BPH and Prostate cancer

Answer 20

BPH: 5 alpha reductive inhibitor

• finasteride
• dutasteride

Prostate cancer: androgen receptor blocker

• flutaminde
• nilutamide
• bicalutamide

Androgen RBs are stronger than 5 alpha RBs

Question 21

Finasteride in BPH

Answer 21

Given for static component. Hence, takes 3-5 months for action.

Tamsulosin is for dynamic component. Acts immediately and gives symptomatic relief

Question 22

Indications and ADRs of 5 alpha reductive inhibitors

Answer 22

Indications

• BPH
• Androgenital alopecia

ADRs
-impotency

Question 23

Quantity used to compare testosterone and anabolic steroids

Answer 23

Androgen: Anabolic ratio
T- 1:1
Ana Ster- 1:2 to 1:3

Question 24

Anabolic steroids examples

Answer 24

Nandrolone

Stanozolol (not a beta blocker)

Question 25

Indications and Side effects of anabolic steroids

Answer 25

No clinical indications. Only abused by athletes - cholestatic jaundice - BPH and Prostatic cancer

Question 26

Disadvantages of anabolic steroids

Answer 26

- short lasting effect - unreliable (might be absent) - ADRs - cholestatic jaundice - BPH and prostate cancer

Question 27

Main MOA of - combined OCP - POP/ mini pills - emergency contraceptive

Answer 27

- combined: inhibit ovulation by feedback inhibiting LH - POP: thicken cervical mucus - emergency contraceptive: inhibit implantation

Question 28

Most common OCP combination

Answer 28

Ethinyl estradiol 30-40 ug Norethindrone 1000 ug Now we use 2nd/3rd gen progesterone

Question 29

Cause of breakthrough bleeding while on COMBINED OCP

Answer 29

Less estrogen endogenously

Question 30

Management of breakthrough bleeding

Answer 30

Theoretically, increase estrogen or decreases progesterone. Increasing estrogen incurs side effects. Hence, we decrease progesterone by switching to biphasic and triphasic pills, which mimic the gradual increase in progesterone concentration.

Question 31

Indications of POP

Answer 31

When estrogen is contraindicated eg. Past Hx of - DVT, VTE - MI - Lactation (estrogen inhibits lactation)

Question 32

Drug given in POP

Answer 32

Levonorgestrel 1 tab daily

Question 33

Examples of emergency contraceptives

Answer 33

1. C OCP- 2 tabs stat and 2 tabs after 12 hours 2. POP- levonorgestrel 1.5 mg stat 3. Mife- 600mg stat 4. Ulipristal- 30mg stat (up to 5 days post coitus)

Question 34

Mild ADRs of OCP

Answer 34

Mm: NORMAL Don't warrant withdrawal ``` Nausea Oedema Recurrent headache Mastalgia Abnormal bleeding Loss of withdrawal bleeding (amenorrhea for first few cycles) ```

Question 35

Moderate ADRs of OCP

Answer 35

Can stop but not necessary Include the androgenic side effects of progesterone - Acne - Wt gain - Chloasma

Question 36

Severe ADRs of OCPs

Answer 36

Mm: 4 C's CNS: depression CVS: thromboembolism like DVT, PE, MI, stroke Cholestatic jaundice Cancer: breast and cervical

Question 37

Benefits of OCPs

Answer 37

Mm: Other BENEFITS Decreases risk of the following ``` Ovarian cyst- is decreased (DOC in PCOD) Benign breast disease- fibrocystic disease Endometriosis Neoplasia- endometrial and ovarian Ectopic pregnancy (copper T increases risk) Fibroids Tension syndrome (PMS) Skeletal disease- osteoporosis ```