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

Estrogens & Progestins Flashcards

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
Q

Tamoxifen SE (6)

A
  • Endometrial Malignant Neoplasia (includes Polyps) = no administration duration > 5 years
  • Cataracts
  • PE
  • Hot Flashes
  • Amenorrhea
  • Vaginal Discharge
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26
Q

Tamoxifen Contraindications (2)

A
  1. DVT/PE Hx
  2. Pregnancy
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27
Q

Drug class of Clomiphene

A

SERM

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28
Q

Clomiphene Indication

A

Female Infertility 2° to ovulation DO

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29
Q

Clomiphene MOA (2)

A
  • Estrogen Blocker @ hypothalamus & pitutiary–> INC LH & FSH
  • Partial agonist @ ovaries
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30
Q

Clomiphene SE (4)

A
  • Thromboembolism
  • Ovarian Cyst & Hypertrophy
  • Flushing (vasomotor sx)
  • Abd pain
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31
Q

Clomiphene contraindications (6)

A
  1. Pregnancy
  2. Thyroid vs. Adrenal Dysfunction
  3. Liver Dz
  4. Endometrial Carcinoma
  5. Ovarian Cyst
  6. Organic intracranial lesion
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32
Q

[T or F] Clomiphene is not associated with [Ovarian Hyperstimulation Syndrome]

A

True

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33
Q

Drug Class of Raloxifene

A

SERM

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34
Q

Raloxifene Indication (2)

A

Osteoporosis & [Postmenopausal Breast CA Px] only

35
Q

Raloxifene MOA (2)

A
  • Estrogen R Agonist @ Bone
  • Estrogen R BLOCKER @ Uterus & Breast
36
Q

Raloxifene SE (4)

A
  1. Retinal Vascular occlusion
  2. DVT
  3. Hot flashes
  4. Leg cramps
37
Q

Raloxifene Contraindications (2)

A
  1. Pregnancy
  2. DVT Hx
38
Q

Fulvestrant MOA

A

[Estrogen R BLOCKER] with no agonist activity

39
Q

Fulvestrant Indication

A

[Estrogen Receptor positive metastatic Breast CA] in postmenopausal women following Tamoxifen therapy

40
Q

Fulvestrant SE (4)

A
  • Asthenia (physical/mental weakness)
  • Hot Flashes
  • HA
  • Pain
41
Q

Fulvestrant Contraindication

A

Pregnancy

42
Q

Name the [Aromatase inhibitors] (4)

A

Anastrozole

Letrozole

Exemestane - (Covalently Irreversible)

Formestane - (Covalently Irreversible)

43
Q

[Aromatase inhibitors] indication

A

[ER+ Breast CA (Tx and Px)]

44
Q

[Aromatase inhbitors] SE (8)

A

“Don’t FETCH a Vile aRoma”

  1. [Fractures & Arthralgia]
  2. Thrombophlebitis
  3. Hypercholesterolemia
  4. Vaginal Bleeding (profuse)
  5. Edema-Peripheral
  6. Constitutional (HA/Nausea)
  7. Dyspnea
  8. Rash
45
Q

[Aromatase inhibitors] Contraindication

A

Hypersensitivity

46
Q

Between SERMs and [Aromatase inhibitors] which are more effective with Breast CA?

A

[Aromatase inhibitors] but keep in mind the SE of [Fracture/Arthralgia] from heavy estrogen DEC

47
Q

Physiological actions of Progesterone (7)

A
  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
Q

Progestin Indication (5)

A
  1. OCP alone or [OCP componenent]
  2. Menopausal Endometrial Protection (medroxyprogesterone)
  3. Oligomenorrhea vs. Amenorrhea
  4. PCOS
  5. Endometriosis
49
Q

Name the [Progestin only OCP] (5)

A
  1. Levonorgestrel
  2. Norgestrel
  3. Norethindrone
  4. Medroxyprogesterone (injectable)
  5. Etonogestrel (Implant)
50
Q

How do [Progestin only OCP] perform their action (4)

A

Alters …

  1. GnRH pulsation and DEC ANT Pit responsiveness to GnRH
  2. Tubal Peristalsis
  3. Cervical Mucus Secretions
  4. Endometrial Receptiveness
51
Q

[Progestin only OCP] SE (3)

A
  • Irregular periods
  • Breast tenderness
  • Constitutional (HA / Nausea / Dizziness)
52
Q

[Progestin only OCP] contraindications (4)

A
  1. Pregnancy
  2. Acute Liver Dz
  3. Liver Tumor
  4. Breast CA
53
Q

Name the [Progestin only OCP] and its dosage given for [spotting, irregular periods, oligmenorrhea]

A

Medroxyprogesterone given via injection q3 mo.

54
Q

How long is [Etonogestrel implants] effective for?

A

3 mo.

55
Q

Which [Progestin only OCP] is used for Emergency contraception (morning after)

A

Levonorgestrel (Blocks LH surge and impairs surge transport)

56
Q

Classic regiment for [Combined OCP (estrogen AND progestin)]

A

[qd x 21 days] + 7 day placebo

57
Q

[Combined OCP] MOA (2)

A
  1. Negative feedback on Gonadotropin secretion –> No ovulation
  2. Progestin thickens Cervical mucus
58
Q

Which Estrogens are used in [Combined OCP] (2)

A
  • Ethinyl Estradiol = most commonly used
  • Mestranol
59
Q

Which Progestins are used in [Combined OCP] (6)

A
  • Anything with Nor (Norgestrel/Norethindrone/Norgestimate)
  • Levonorgestrel
  • Ethynodiol
  • Desgestrel
  • Drospirenone
  • Gestodene
60
Q

[Combination OCP] SE (9)

A

BirthControl Gives Ladies A Home Without Terribly, Bawling Babies

  1. Breast Tenderness (don’t use in Breast CA)
  2. Gallbladder Dz
  3. Liver Neoplasm
  4. Abnormal Menstruation
  5. HTN
  6. Weight change
  7. Thromboembolism
  8. Bloating
  9. Breakthrough Bleeding
61
Q

Which Progestins have highest androgenic activity (2)

A

Norgestrel & Levonorgestrel

62
Q

Which Progestins have medium androgenic activity

A

Norethindrone

63
Q

Which progestin has antiAndrogen activity

A

Drospirenone

64
Q

Why is estrogen always coadministered with progestin in [women with uterus]

A

Estrogen, given alone, –>Endometrial CA

65
Q

How is DVT reduced when using [Combined OCP]

A

Use lowest effective dose of ethinyl estradiol

66
Q

Mifepristone [Drug Class/MOA] (2)

A

[Progesterone R Blocker] and [Glucocorticoid R blocker at high dose]

67
Q

Mifepristone Indication (2)

A
  1. Abortion (only with pregnancy <49 days)
  2. Refractory Cushing’s Syndrome
68
Q

Mifepristone SE (5)

A
  1. Prolonged Bleeding
  2. Bacterial Infections
  3. Sepsis
  4. NVD (mostly from co-administered Misoprostol)
  5. Cramps
69
Q

Mifepristone Contraindications (7)

A
  1. Chronic Adrenal Failure
  2. Ectopic Pregnancy
  3. Hemorrhagic DO
  4. Anticoagulation therapy
  5. Inherited Porphyria
  6. IUD
  7. Undiganosed adnexal mass
70
Q

Name and Describe which drug Mifepristone is co-adminstered with

A

Misoprostol = prostaglandin analogue that simulates uterine contractions but also NVD

71
Q

What’s the effect of high-dose Mifepristone

A

Glucocorticoid R Blocker

72
Q

Dosage Regimen for Emergency Contraceptive

A

1st: Within 72 hours of intercourse take 2 T [0.75 mg of levonorgestrel]
2nd: Wait 12 Hours
3rd: Repeat Step 1

73
Q

Levonorgestrel (emergency contraceptive) SE (3)

A
  • Dizziness
  • Mastalgia
  • Constitutional (NV/HA)
74
Q

Menopause Dx (2)

A

1 year since last menses + [FSH > 25]

75
Q

When does perimenopause onset?

A

[Late 30’s - Early 40’s]

76
Q

Menopause sx come from ___ deficiency and includes what 4 main EARLY sx?

A

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
Q

Menopause sx come from ___ deficiency and includes what PHYSICAL sx? (2)

A

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
Q

Menopause sx come from ___ deficiency and includes what LONG TERM sx? (3)

A

Menopause sx come from Estrogen deficiency:

  1. Osteoporosis (HRT Tx indicated)
  2. CVD
  3. Dementia
79
Q

Compare Estrogen levels from HRT to OCP

A

OCP contains higher estrogen levels

80
Q

HRT contraindications

A

Same as OCP

81
Q

HRT SE (5)

A
  1. Estrogen - Nausea, Mastalgia, Fluid Retention
  2. Progestin- Wt. Gain and HA
82
Q

Relationship between HRT and Endometrial CA

A

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
Q

Relationship between HRT and Breast CA

A

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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