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🄼💊MSY2 Pharm (Endocrine/Repro/Thyroid) > Estrogens & Progestins > Flashcards

Estrogens & Progestins Flashcards

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1
Q

Source of Estrogens (3)

A
  1. Ovaries
  2. Liver (from Estriol)
  3. Peripheral tissue (from androgens)
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2
Q

Source of Progestins (4)

A
  1. Ovaries
  2. Testis
  3. Adrenal Gland
  4. Placenta during pregnancy

comes from Cholesterol

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3
Q

Source of Androgens (2)

A
  1. 95% Testis
  2. 5% Adrenal Glands
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4
Q

List the natural estrogens (3). Which is most estrogenic?

A
  • Estrone (E1)
  • Estradiol (E2) = MOST ESTROGENIC
  • Estriol (E3) = not very active
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5
Q

Which natural estrogen is not very active?

A

Estriol (E3)

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6
Q

List the [synthetic steroidal estrogens] (3)

A
  • Ethinyl estradiol
  • Mestranol
  • Quinestrol
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7
Q

List the [Synthetic NonSteroidal Estrogens] (3)

A
  • DES (DiEthylStilbestrol)
  • Chlorotrianisene
  • Methallenestril
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8
Q

Activin is released from ___ and ____ cells. What does it do? What hormone blocks this action?

A

Activin is released from Sertoli and Granulosa cells

Stimulates FSH release only

Inhibin (A & B) comes from the same place and inhibits FSH release

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9
Q

Aromatase MOA (2)

A

Converts…

  • Androstenedione –> E2
  • Testosterone –> E2 and E1
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10
Q

How do Steroid Hormones molecularly work?

A

Hormone diffuses into target cell and binds to receptor. [Hormone-receptor complex dimerizes in nucleus] and binds to specific DNA regions (activators/repressors) –> Gene tx

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11
Q

Describe the Name and Hormone levels during the Menstrual cycle

A: Days 1-14

B: Day 14

C: Days 14-28

A

A: [Follicular Proliferative Phase] = low E2 with INC FSH and LH receptors on Dominant follicle

B: Ovulation (FSH & LH peak with LH surge)

C: [Luteal Secretory Phase]= Progesterone INC

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12
Q

Reproductive actions of Estrogen (5)

A
  1. Female Secondary Sex characteristics
  2. Puberty & Adolescent changes (epiphyseal closure)
  3. Menstrual cycle (gonadotropin secretion)
  4. Uterine Endometrial proliferation
  5. [Thin Cervical Mucus] secretion for sperm facilitation
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13
Q

Metabolic actions of Estrogen (5)

A
  1. [INC HDL and DEC LDL] :-)
  2. INC Bile saturation into cholesterol –> DEC cholelithiasis
  3. Stimulates Renin substrate release –> INC BP
  4. Clotting
  5. DEC Bone Resorption
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14
Q

CNS actions of Estrogen (2)

A
  1. Positive mood, cognition, memory
  2. Protects against Neurodegenerative DO
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15
Q

Estrogen Route of Administration (2)

A

Great GI tract absorption vs. transdermal

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16
Q

Describe Estrogen Metabolism

A

Absorption partially dependent on intestinal flora (be careful of certain abx). Substantial 1st pass hepatic metabolism (CYP450) after oral admin. E2 is metabolized –> E1 and then conjugated.

Drugs that induce CYPP450 INC metabolism –> DEC efficacy

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17
Q

Estrogen Clinical Indication (6)

A

OPRAHH

  1. OCP component (ethinyl estradiol)
  2. [HRT Menopausal (Premarin)]
  3. HypOgonadism for females
  4. [Perimenopause/Oligomenorrhea/Dysmenorrhea]
  5. Really behind (delayed) Puberty
  6. Acne (Estrostep)
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18
Q

Estrogens SE (6)

A

Beware of Estrogen’s CAVE

  1. Breast tenderness
  2. Venous Thrombosis
  3. Constitutional (HA/NV)
  4. Edema
  5. [Endometrial Hyperplasia/Carcinoma (Estrogen when taken alone)]
  6. Adenocarcinoma in offspring of pts who’ve taken DES
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19
Q

[T or F] Estrogen can be given in pts with Liver Tumors

A

FALSE

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20
Q

[T or F] Estrogen can be given in Pregnant Pts

A

FALSE

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21
Q

[T or F] Estrogen can be given in [Female Smokers > 35 y/o]

A

FALSE

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22
Q

SERM = ____. What is its MOA (2)

A

SERM = Selective Estrogen Receptor Modulator

  • Estrogen BLOCKER in some tissues
  • Estrogen Agonist in other tissues
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23
Q

Drug class of Tamoxifen

A

SERM

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24
Q

Tamoxifen Indication

A

Pre AND POSTMenopausal Breast CA that are (ER/PR +). Serves as [Adjuvant Hormonal Therapy]

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25
Tamoxifen SE (6)
* Endometrial Malignant Neoplasia (includes Polyps) = **no administration duration \> 5 years** * Cataracts * PE * Hot Flashes * Amenorrhea * Vaginal Discharge
26
Tamoxifen Contraindications (2)
1. DVT/PE Hx 2. Pregnancy
27
Drug class of Clomiphene
SERM
28
Clomiphene Indication
Female Infertility 2° to ovulation DO
29
Clomiphene MOA (2)
* Estrogen Blocker @ hypothalamus & pitutiary--\> INC LH & FSH * Partial agonist @ ovaries
30
Clomiphene SE (4)
* Thromboembolism * Ovarian Cyst & Hypertrophy * Flushing (vasomotor sx) * Abd pain
31
Clomiphene contraindications (6)
1. Pregnancy 2. Thyroid vs. Adrenal Dysfunction 3. Liver Dz 4. Endometrial Carcinoma 5. Ovarian Cyst 6. Organic intracranial lesion
32
[T or F] Clomiphene is not associated with [Ovarian Hyperstimulation Syndrome]
True
33
Drug Class of Raloxifene
SERM
34
Raloxifene Indication (2)
Osteoporosis & [Postmenopausal Breast CA **Px**] only
35
Raloxifene MOA (2)
* Estrogen R Agonist @ Bone * Estrogen R BLOCKER @ Uterus & Breast
36
Raloxifene SE (4)
1. Retinal Vascular occlusion 2. DVT 3. Hot flashes 4. Leg cramps
37
Raloxifene Contraindications (2)
1. Pregnancy 2. DVT Hx
38
Fulvestrant MOA
[Estrogen R BLOCKER] with **no agonist activity**
39
Fulvestrant Indication
[Estrogen Receptor positive metastatic Breast CA] in postmenopausal women following Tamoxifen therapy
40
Fulvestrant SE (4)
* Asthenia (physical/mental weakness) * Hot Flashes * HA * Pain
41
Fulvestrant Contraindication
Pregnancy
42
Name the [Aromatase inhibitors] (4)
Anastrozole Letrozole Exemestane - (Covalently Irreversible) Formestane - (Covalently Irreversible)
43
[Aromatase inhibitors] indication
[**ER+** Breast CA (Tx and Px)]
44
[Aromatase inhbitors] SE (8)
"**D**on't **FETCH** a **V**ile a**R**oma" 1. [**F**ractures & Arthralgia] 2. **T**hrombophlebitis 3. **H**ypercholesterolemia 4. **V**aginal Bleeding (profuse) 5. **E**dema-Peripheral 6. **C**onstitutional (HA/Nausea) 7. **D**yspnea 8. **R**ash
45
[Aromatase inhibitors] Contraindication
Hypersensitivity
46
Between SERMs and [Aromatase inhibitors] which are more effective with Breast CA?
[**Aromatase inhibitors**] but keep in mind the SE of [Fracture/Arthralgia] from heavy estrogen DEC
47
Physiological actions of Progesterone (7)
1. Menstrual cycle: Negative feedback during [Luteal secreotory phase] 2. Endometrial transformation --\> Secretory phase 3. Reverts [thin cervical mucus] back to [THICK cervical mucus] which inhibits any further sperm transport 4. INC body temp at Ovulation 5. Maintains Pregnancy: Inhibits Uterine contraction and suppresses immune system 6. Mammogenesis 7. Blocks and enhances actions of estrogens
48
Progestin Indication (5)
1. OCP alone or [OCP componenent] 2. Menopausal Endometrial Protection (medroxyprogesterone) 3. Oligomenorrhea vs. Amenorrhea 4. PCOS 5. Endometriosis
49
Name the [**Progestin only** OCP] (5)
1. Levonorgestrel 2. Norgestrel 3. Norethindrone 4. Medroxyprogesterone (injectable) 5. Etonogestrel (Implant)
50
How do [Progestin only OCP] perform their action (4)
Alters ... 1. GnRH pulsation and DEC ANT Pit responsiveness to GnRH 2. Tubal Peristalsis 3. Cervical Mucus Secretions 4. Endometrial Receptiveness
51
[Progestin only OCP] SE (3)
* Irregular periods * Breast tenderness * Constitutional (HA / Nausea / Dizziness)
52
[Progestin only OCP] contraindications (4)
1. Pregnancy 2. Acute Liver Dz 3. Liver Tumor 4. Breast CA
53
**Name** the [Progestin only OCP] and its **dosage** given for [spotting, irregular periods, oligmenorrhea]
Medroxyprogesterone given via injection q3 mo.
54
How long is [Etonogestrel implants] effective for?
3 mo.
55
Which [Progestin only OCP] is used for Emergency contraception (morning after)
Levonorgestrel (Blocks LH surge and impairs surge transport)
56
Classic regiment for [Combined OCP (estrogen AND progestin)]
[qd x 21 days] + 7 day placebo
57
[Combined OCP] MOA (2)
1. Negative feedback on Gonadotropin secretion --\> No ovulation 2. Progestin thickens Cervical mucus
58
Which Estrogens are used in [Combined OCP] (2)
* Ethinyl Estradiol = most commonly used * Mestranol
59
Which Progestins are used in [Combined OCP] (6)
* Anything with **Nor** (Norgestrel/Norethindrone/Norgestimate) * Levonorgestrel * Ethynodiol * Desgestrel * Drospirenone * Gestodene
60
[Combination OCP] SE (9)
**B**irthControl **G**ives **L**adies **A** **H**ome **W**ithout **T**erribly, **B**awling **B**abies 1. **B**reast Tenderness (don't use in Breast CA) 2. **G**allbladder Dz 3. **L**iver Neoplasm 4. **A**bnormal Menstruation 5. **H**TN 6. **W**eight change 7. **T**hromboembolism 8. **B**loating 9. **B**reakthrough Bleeding
61
Which Progestins have highest androgenic activity (2)
Norgestrel & Levonorgestrel
62
Which Progestins have medium androgenic activity
Norethindrone
63
Which progestin has **anti**Androgen activity
Drospirenone
64
Why is estrogen always coadministered with progestin in [women with uterus]
Estrogen, **given** **alone**, --\>Endometrial CA
65
How is DVT reduced when using [Combined OCP]
Use lowest effective dose of ethinyl estradiol
66
Mifepristone [Drug Class/MOA] (2)
[Progesterone R Blocker] and [Glucocorticoid R blocker at high dose]
67
Mifepristone Indication (2)
1. Abortion (only with pregnancy \<49 days) 2. Refractory Cushing's Syndrome
68
Mifepristone SE (5)
1. Prolonged Bleeding 2. Bacterial Infections 3. Sepsis 4. NVD (mostly from co-administered Misoprostol) 5. Cramps
69
Mifepristone Contraindications (7)
1. Chronic Adrenal Failure 2. Ectopic Pregnancy 3. Hemorrhagic DO 4. Anticoagulation therapy 5. Inherited Porphyria 6. IUD 7. Undiganosed adnexal mass
70
**Name** and **Describe** which drug Mifepristone is co-adminstered with
Misoprostol = prostaglandin analogue that simulates uterine contractions but also NVD
71
What's the effect of high-dose Mifepristone
Glucocorticoid R Blocker
72
Dosage Regimen for Emergency Contraceptive
1st: Within 72 hours of intercourse **take 2 T [0.75 mg of levonorgestrel**] 2nd: Wait 12 Hours 3rd: Repeat Step 1
73
Levonorgestrel (emergency contraceptive) SE (3)
* Dizziness * Mastalgia * Constitutional (NV/HA)
74
Menopause Dx (2)
1 year since last menses + [FSH \> 25]
75
When does **peri**menopause onset?
[Late 30's - Early 40's]
76
Menopause sx come from ___ deficiency and includes what 4 main EARLY sx?
Menopause sx come from **Estrogen** deficiency: 1. Mood Changes (95%) (HRT Tx indicated) 2. Fatigue (95%) 3. Vasomotor instability --\> Hot Flashes (70%) (HRT Tx indicated) 4. Insomnia (55%)
77
Menopause sx come from ___ deficiency and includes what PHYSICAL sx? (2)
Menopause sx come from **Estrogen** deficiency: 1. Urogenital Atrophy (60%)--\> Urinary incontinence and Recurrent UTI (HRT Tx indicated) 2. Skin Atrophy from collagen loss
78
Menopause sx come from ___ deficiency and includes what LONG TERM sx? (3)
Menopause sx come from **Estrogen** deficiency: 1. Osteoporosis (HRT Tx indicated) 2. CVD 3. Dementia
79
Compare Estrogen levels from HRT to OCP
OCP contains **higher** **estrogen** levels
80
HRT contraindications
Same as OCP
81
HRT SE (5)
1. Estrogen - Nausea, Mastalgia, Fluid Retention 2. Progestin- Wt. Gain and HA
82
Relationship between HRT and Endometrial CA
Unopposed estrogen, **taken alone**, for 5 years --\> INC risk of endometrial hyperplasia/CA x 5 and x8 if taken longer than 5 years. This is eliminated by adding Progestin
83
Relationship between HRT and Breast CA
Little to no risk if taken \< 5 years but Risk INC to 1.3 if taken 10-15 years. Eliminated with Progestin co-admin

🄼💊MSY2 Pharm (Endocrine/Repro/Thyroid) (6 decks)

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