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Pharmacology > Endocrine: Sex Hormones > Flashcards

Endocrine: Sex Hormones Flashcards

1
Q

Clomiphene

A

SERM and estrogen antagonist at hypothalamus

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2
Q

Indications of clomiphene

A
  1. Anovulatory infertility

2. Oligospermia infertility

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3
Q

S/Es of clomiphene

A
  1. Multiple pregnancies
  2. Hot flushes

Hot flushes because FSH and LH are vasodilatory

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4
Q

Centchroman other name

A

Ormeloxifene

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5
Q

Ormeloxifene action and indications

A

Estrogen receptor ANTAGONIST at ENDOMETRIUM

Indication: OCP, non-steroidal

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6
Q

Ospenifene indication

A

Post menopausal dyspareunia

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7
Q

Fulvestrant

  • parent class
  • MOA
  • site of action
  • indication
  • RDA
A
  • 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
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8
Q

Tibolone

  • parent class
  • MOA
  • indications
A
  • 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
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9
Q

Third generation AIs

A
  • Letrozole
  • Anastrozole
  • Exemestane
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10
Q

AI indications

A

Postmenopausal breast cancer

Because aromatisation is the major source

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11
Q

Generations of progesterone

A

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

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12
Q

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

A

Drospirenone (of spironolactone group)

Indications

  • combined OCP
  • moderate acne (FDA app)
  • PMS dysphoria (FDA app)
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13
Q

SPRM examples

A

Selective progesterone receptor modulator

Mifepristone
Onapristone
Ulipristal

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14
Q

Uses of mifepristone

A

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

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15
Q

Mife is an antagonist at ?

A
  1. Progesterone receptor
  2. Androgen
  3. Glucocorticoid
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16
Q

Onapristone MOA and indications

A

MOA: antagonist at PR of endometrium ONLY

Indication: induction of abortion

17
Q

Ulipristal indication

A

Emergency contraceptive

18
Q

Exclusive actions of testosterone (not shared by dihydrotestosterone)

Shared actions

A

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

19
Q

Harmful effects of excess testosterone

A
  1. BPH

2. Prostate cancer

20
Q

Drugs for BPH and Prostate cancer

A

BPH: 5 alpha reductive inhibitor

  • finasteride
  • dutasteride

Prostate cancer: androgen receptor blocker

  • flutaminde
  • nilutamide
  • bicalutamide

Androgen RBs are stronger than 5 alpha RBs

21
Q

Finasteride in BPH

A

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

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

22
Q

Indications and ADRs of 5 alpha reductive inhibitors

A

Indications

  • BPH
  • Androgenital alopecia

ADRs
-impotency

23
Q

Quantity used to compare testosterone and anabolic steroids

A

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

24
Q

Anabolic steroids examples

A

Nandrolone

Stanozolol (not a beta blocker)

25
Q

Indications and Side effects of anabolic steroids

A

No clinical indications. Only abused by athletes

  • cholestatic jaundice
  • BPH and Prostatic cancer
26
Q

Disadvantages of anabolic steroids

A
  • short lasting effect
  • unreliable (might be absent)
  • ADRs
    • cholestatic jaundice
    • BPH and prostate cancer
27
Q

Main MOA of

  • combined OCP
  • POP/ mini pills
  • emergency contraceptive
A
  • combined: inhibit ovulation by feedback inhibiting LH
  • POP: thicken cervical mucus
  • emergency contraceptive: inhibit implantation
28
Q

Most common OCP combination

A

Ethinyl estradiol 30-40 ug

Norethindrone 1000 ug
Now we use 2nd/3rd gen progesterone

29
Q

Cause of breakthrough bleeding while on COMBINED OCP

A

Less estrogen endogenously

30
Q

Management of breakthrough bleeding

A

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.

31
Q

Indications of POP

A

When estrogen is contraindicated eg. Past Hx of

  • DVT, VTE
  • MI
  • Lactation (estrogen inhibits lactation)
32
Q

Drug given in POP

A

Levonorgestrel 1 tab daily

33
Q

Examples of emergency contraceptives

A
  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)
34
Q

Mild ADRs of OCP

A

Mm: NORMAL

Don’t warrant withdrawal

Nausea
Oedema
Recurrent headache
Mastalgia
Abnormal bleeding
Loss of withdrawal bleeding (amenorrhea for first few cycles)
35
Q

Moderate ADRs of OCP

A

Can stop but not necessary

Include the androgenic side effects of progesterone

  • Acne
  • Wt gain
  • Chloasma
36
Q

Severe ADRs of OCPs

A

Mm: 4 C’s

CNS: depression
CVS: thromboembolism like DVT, PE, MI, stroke
Cholestatic jaundice
Cancer: breast and cervical

37
Q

Benefits of OCPs

A

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

Pharmacology (9 decks)

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