Pharm Block 2 (reproductive)
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What are The sources of estrogen?
- Liver- Converts estradiol to estrone and estriol
- Adipose tissue, Testes, bone, and placenta
- Breast and CNS
What are the Metabolic effects of Estrogen?
- Stimulates osteoblasts and increases collagen synthesis
- increases HDL and decreases LDL
- increases binding proteins ( Cortisol, thyroxin sex hormones)
- Slightly decrease glucose and insulin, and slightly increases coagulation factors
What are the two types of estrogen receptors?
is it taken orally?
- ERalpha and ERbeta
- No because it is not orally bioavaiable (due to first pass effect)
What are some unwanted effects of Estrogen?
- may increase the rist of Thrombosis in premenopausaal women (esspecially if they smoke)
- may increase the risk of dementia
What are some therapeutic uses of Estrogen?
- Oral COntraceptives
- Hormonal replacement theropy
- Vaginal Dryness
- Urogenital atrophy
- Cardiovascular disease (reduces risk)
- Treatment for menopausal symptoms
Name the SERMs (serum estrogen receptor modulators).
Name some Estrogen Antagonists.
Tamoxifen, Taloxifen and Toremifen
Antagonists are Clomiphene (use for infertility in anovulatory women), and Fulvestrant (use in breast cancer)
When is Tamoxifen used?
What are its effects?
Used in Breast cancer.
- Inhibits proliferation of breast cancer cells
- – Reduces the size and number of tumors
- – Decreases total cholesterol and LDL
- – Increases risk of deep vain thrombosis
- – Increases risk of pulmonary embolism
- – Increases risk of endometrial carcinoma
- – Induces hot flashes
- – Does not increase incidence of bone fractures
When is Raloxifen used ?
used in Breast cancer and Osteoporosis
- Estrogen Agonist in Bone and Serum
- - reduces the number of bone fractures and reduces total LDL levels
- Estrogen Antagonist effects:
- - Hot flashes
- - Antiproliferative in Estrogen Breast Cancers.
When is Clomiphene used ?
What are its effects?
Used in Infertile women with functional Hypothalmic hypophyseal ovarian system and adequate estrogen production
- – Increases FSH
- – Enlargement of ovaries
What are some Unwanted effects of Clomiphene?
When should you NOT give this drug?
- – Increased rate of multiple birth
- – Hot flashes
- – May increase risk of ovarian cancer
Do not give for Breast cancer or if patient is infertile because of no ovaries.
When do you use Fluvestrant?
Use it in Tamoxifen resistant breast cancers.
What are Armomatase Inhibitors?
When do you used them?
They inhibit Aromatase which is an essential enzyme needed for estrogen production.
- 1. Exemestin
- 2. Letrozole
- 3. Anastrozol
Use it is Breast Cancer, used mainly to decrease biosynthesis of estrogens
What are the Effects of Progestins?
Note does everything it can to protect the Egg and prepare for Pregnancy.
- Decreases the Frequency of GnRH pulse
- • Reproductive tract– Decreases the endometrial proliferation– Increases the endometrial secretion and viscosity– Prepares the uterus for implantation and pregnancy
- • Decreases the motility
- • Suppresses the menstruation– Abrupt decrease in progesterone at the end of cycle casesmenstruation
- • Mammary glands– Increases the proliferation of mammary glands– Increases vascularization of mammary glands (late in pregnancy)
- • CNS– Increases body temperature about 1°C– Increases ventilatory response to CO2 and reduces PCO2– May cause depressant and hypnotic effects
- • Metabolic effects– Increases insulin level– Enhances fat deposition
What are some Theropeutic Uses for Progestins?
- Hormonal replacement in menopause
- Amenorrhea and abdominal bleeding
- Luteal Phase support in Infertility
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