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Pharm #3 - Endocrine/Repro > Pharm#2 - Estrogen Progesterone > Flashcards

Pharm#2 - Estrogen Progesterone Flashcards

1
Q

Indications for Estrogen Preperations

A
  1. Vasomotor symptoms of menopause. (flushing due to lack of estrogen)
  2. Vulvar and vaginal atrophy.
  3. Female hypoestrogenism secondary to hypogonadism
    castration or primary ovarian failure.
  4. In combination with other therapeutic measures to retard bone loss
    and osteoporosis in post-menopausal women.
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2
Q

Estrogen increases incidence of what 2 chances?

other side effects?

A 
Nausea & vomiting
 Edema
 Headache
 Breast tenderness
 Venous thrombosis
 Breakthrough bleeding
 Estrogen alone (without progesterone) causes endometrial
   hyperplasia and possible endometrial carcinoma.

Increased incidence of adenocarcinoma of the vagina in
female offsprings of patients who have taken Diethylstilbestrol

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3
Q

Contraindications for estrogen (7 major)

A
  1. Breast & Endometrial cancers
  2. Cerebral vascular coronary artery disease
  3. Benign or malignant liver tumors
  4. Sever hypertension
  5. Pregnancy
  6. Female smokers over 35 years of age
  7. Thrombotic disorders (estrogen inc clotting factors)
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4
Q

explain how SERMS work

A

are Estrogen antagonist in some tissues and estrogen agonist in other tissues.

The basis for tissue selectivity may be related to tissue-specific expression of estrogen-receptor subtypes and the differential ability of the ligand-receptor complex to recruit transcriptional co-activators and co-repressors as well different Transcription Factors.

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5
Q

Tamoxifen

  1. MOA
  2. major indication
A
  1. Estrogen receptor ANTAGONIST in breast tissue, and partial agonist in endometrium and bone
  2. Tamoxifen is used for prevention, palliative, and as an adjuvant therapy for breast cancer.
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6
Q

Tamoxifen

SE (6)

Contra (2)

A
  1. Malignant neoplasma of endometrium (due to agonist effect)
  2. Cataract
  3. Pulmonary embolism (blocks estrogen signaling)
  4. Hot flashes
  5. Abnormal menstruation
  6. Vaginal discharge

Contra:
History of deep vein thrombosis or pulmonary embolism

Pregnancy

*** Tamoxifen administration is associated with 4-6 fold increase in the incidence of endometrial cancer

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7
Q

____ administration is associated with 4-6 fold increase in the incidence of endometrial cancer

Administered for no more than 5 years, to minimize the risk of endometrial cancer

A

Tamoxifen

  • cancer due to PARTIAL AGONIST effects
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8
Q

Clomiphene

  1. indications
  2. MOA
A
  • Female infertility due to ovulatory disorder

MOA: estrogen receptor antagonist in hypothalamus and pituitary

  • estrogen PARTIAL AGONIST in ovaries
  • disinhibits GnRH release and increases the level of Lh and FSH
  • increased FSH stimulates follicle growth, LH Surge and ovulation
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9
Q

CLomiphene
- SE (4)

Contra

A

Thromboembolism
Ovarian cysts and hypertrophy
Flushing and vasomotor symptoms
Abdominal discomfort

  1. Pregnancy
  2. Thyroid or adrenal dysfunction
  3. Liver disease
  4. Endometrial carcinoma
  5. Ovarian cysts
  6. Organic intracranial lesion
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10
Q

Raloxifene

  • Indications
  • MOA
A
  1. Osteoporosis prevention and treatment

2. MOA: estrogen receptor AGONIST in bone and ANTAGONIST in uterus and breast

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11
Q

Raloxifene

SE

COntra

A 
SE:
Retinal vascular occlusion **                
 Venous thromboembolism
 Hot flashes
 Leg cramps

Contra:

  • Pregnancy
  • History or presence of venous thromboembolism
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12
Q

Fulvestrant

Indications
MOA

A
  1. Treatment of estrogen receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy
  2. Competitively inhibit estrogen binding to receptor, blocking the action of estrogen on target tissues

Pure estrogen receptor antagonist with no agonist activity

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13
Q

Fulvestrant

SE (1 main)

Contra

A 
SE:
- Nausea
 Asthenia (lack of strength)
 Pain 
 Vasodilation (hot flashes)
 Headache

Contra:
- pregnancy

** Pure estrogen receptor antagonist with no agonist activity

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14
Q

4 aromatase inhibitors

2 irreversible
2 reversible

A

Anastrozole
Letrozole
Exemestane
Formestane

Irreversible:

  1. exemestane
  2. formestane

Letrozole and Anastrozole are competitive inhibitors of aromatase

*Aromatase inhibitors may be more effective than SERMs for the treatment of breast cancer

Extreme suppression of estrogen action could lead to high risk of osteoporotic factures in women taking aromatase inhibitors

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15
Q

SE of Aromatase Inhibitors

yowza

A 
Osteoporotic fractures
 Thrombophlebitis
 Hypercholesterolemia
 Profuse vaginal bleeding
 Peripheral edema
 Rash
 Nausea
 Arthralgia
 Bone pain
 Headache
 Depression
 Dyspnea

Contra: hypersensitivity

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16
Q

Clinical use of progestins

A

In OCs, alone, or in combination with ethinyl estradiol.

Component of HRT in menopause (endometrial protection).

Rx of dysmenorrhea, oligomenorrhea, endometriosis, polycystic ovarian syndrome.

17
Q

MOA of progestin only

A

Alter frequency of GnRH pulsing and decrease anterior pituitary gland responsiveness to GnRH.

Secondary mechanisms of pregnancy prevention include alterations in tubal peristalsis, endometrial receptivity, and cervical mucus secretions, which together prevent the proper transport of both egg and sperm.

18
Q

Progestin only

SE

COntra

A 
SE
-  Irregular periods
 Breast tenderness
 Nausea
 Dizziness
 Headaches
COntra
-  Acute liver disease
 Benign or malignant liver tumors
 Known or suspected breast cancer
 Pregnancy
19
Q

___can be given parenterally every 3 months

___ (implant) is effective for 3 years, and

___ (orally) can be used in case of emergency contraception

A

Medroxyprogesterone acetate

Etonogestrel

Levonorgestrel

20
Q

MOA of estrogen - progestin combo

A

Suppress GnRH, LH and FSH secretion and follicular development, thereby inhibiting ovulation; secondary mechanisms of pregnancy prevention include alterations in tubal peristalsis, endometrial receptivity and cervical mucus secretions which together prevent the proper transport of both egg and sperm.

21
Q

SE estrogen - progestin combo

A 
Arterial and venous thromboembolism
 Pulmonary embolism
 Cerebral thrombosis
 Gallbladder disease
 Hypertension
 Hepatic neoplasm
 Abnormal menstruation
 Breakthrough bleeding
 Breast tenderness
 Bloating symptoms
 Migraine
 Weight change
22
Q

2 progestins with highest androgenic activity

A

Norgestrel and levonorgestrel have the highest androgenic activity

23
Q

___ is used as morning-after contraception.

A

Levonorgestrel

24
Q

Mifepristone (RU-486)

MOA

Indications

A

MOA: inhibits progesterone binding to receptor

indications: Abortion (thru day 49 of pregnancy)

25
Q

Mifepristone

  • main SE
  • contra
A

Prolonged bleeding time
Bacterial infections
Sepsis

Contra
 Chronic adrenal failure
 Ectopic pregnancy
 Hemorrhagic disorders
 Anticoagulation therapy
 Inherited porphyrias
 Intrauterine device
 Undiagnosed adnexal mass

**Higher concentration of mifepristone also blocks the glucocorticoid receptors

26
Q

Levonorgestrel

  • MOA
  • indication
A

MOA: Levonorgestrel is a potent progestin that can block the LH
surge, disrupting normal ovulation, and produce
endometrial changes for implantation.

Indication: Morning after

The first dose should be taken anytime within 72 hrs after
intercourse and second dose after 12 hrs of first dose.

27
Q

Other mechanisms of Levonorgestrel MOA

A

Inhibition of ovulation via strong negative feedback
Impairment of sperm transport
Interference with endometrial receptivity

28
Q

Consequences of estrogen def

Early
intermediate
long term

A

Early

  • vasomotor
  • insomnia
  • fatigue
  • mood changes

Intermediate

  • urogenital atrophy
  • urinary incontinence
  • genital tract infection
  • skin changes

Long term

  • osteoporosis
  • CV disease
  • cognitive
29
Q

Adverse effects of HRT

A

Estrogen assoc. w/: nausea, mastalgia, headache, fluid retention

Progestin component assoc. w/ weight gain, headache

Contraindications same as for COCs

30
Q

Effects of HRT

A

Relief from vasomotor symptoms; urogenital atrophy and recurrent urinary symptoms
Relief from fatigue, depression
Maintenance of bone mineral density

31
Q

Major concern of estrogen alone

A

Estrogen alone assoc. w/ 5-8-fold risk of endometrial carcinoma
Inclusion of progestin eliminates risk

Pharm #3 - Endocrine/Repro (3 decks)

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