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Sex Hormones and Disease Flashcards

1
Q

What are the uses for oestrogen as a drug?

A

hypogonadism in children, primary amenorrhea, contraception, hormone replacement therapy for menopause

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2
Q

What are the benefits of postmenopausal hormone therapy?

A

improve bone density, relief from hot flushes, fatigue and vaginal dryness, reverses atrophy of vulva, vagina and urethra, improved sleep, reduced incidence of colorectal cancer, reduced incidence of coronary heart disease (?), delayed onset of alzheimers (?)

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3
Q

What are the risks of postmenopausal hormone therapy?

A

breast tenderness, nausea, fluid retention, increased risk of breast/uterine cancer, risk of thromboembolism and stroke

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4
Q

What is the mechanism of action of oestrogen?

A

binds to intracellular receptor to form a homodimer which can bind to DNA and regulate gene transcription or can form a heterodimer with other transcription factors such as AP1 to have a different effect on gene expression or can bind to membrane receptors or a GPR30 to have more rapid effects

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5
Q

What are the different oestrogen receptors?

A

ERalpha and ERbeta - or GPR30

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6
Q

What is the link between oestrogen and breast cancer?

A

ER promotes cell growth and promotes expression of the progesterone receptor which in turn promotes cell division - so an increase in receptor expression is linked to cancer

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7
Q

What are SERMs?

A

selective oestrogen receptor modulators - drugs that have different effects on different oestrogen receptors in different tissues

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8
Q

What is tamoxifen?

A

a SERM - an agonist in uterus, bone and CVS and an antagonist in breast and CNS

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9
Q

What is raloxifene?

A

a SERM - an agonist in bone and CVS and an antagonist in breast, CNS and uterus

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10
Q

What is fulvestrant?

A

an oestrogen antagonist at all locations

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11
Q

What is the basis of SERMs?

A

different tissues express different receptor subtypes and the different endogenous oestrogens (oestradiol, oestrone and oestriol) bind with different affinities so drugs have been designed to also do this

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12
Q

What is the use of tamoxifen?

A

palliative treatment of breast cancer

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13
Q

What are the adverse effects of tamoxifen?

A

endometrial hyperplasia, polyps and cancer, thromboembolic events, thrombocytopenia, ocular toxicity, menopausal symptoms

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14
Q

What is the use of aromatase inhibitors?

A

improves disease free survival in breast cancer after the use of tamoxifen - reduced incidence of contralateral breast cancer - reduced number of thromboembolic events - reduced incidence of endometrial cancer

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15
Q

What are the adverse effects of aromatase inhibitors?

A

increase bone loss and fracture risk, increase arthralgia, poorer lipid profile, metabolic syndrome, menopausal signs

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16
Q

What is the mechanism of action of testosterone?

A

testosterone enters the cell, is sometimes converted to dihydrotestosterone by 5-alpha reductase and then binds to the androgen receptor, dimerises and acts as a transcription factor

17
Q

What is the role of dihydrotestosterone?

A

prostate development, external virilisation, sexual maturation

18
Q

What are the therapeutic uses of androgens?

A

hypogonadism, senile osteoporosis, speed recovery from surgery and chronic debilitating diseases, promote skeletal growth in pituitary dwarfism, helps with pain in endometriosis

19
Q

What are the adverse effects of androgens?

A

increase risk of coronary heart disease, acne, facial hair, deepening voice, male pattern baldness, excessive muscle development, menstrual irregularities, priapism, impotence, decease spermatogenesis, gynaecomastia, premature closure of epiphyseal plates, abnormal sexual maturation, liver damage, aggression, psychosis

20
Q

What is cyproterone?

A

an antiandrogen - a steroidal receptor antagonist

21
Q

What is the use of cyproterone?

A

prostate cancer, androgenisation in females

22
Q

What are the adverse effects of cyproterone?

A

cognitive changes, fatigue, oedema, reduced spermatogenesis

23
Q

What is flutamide?

A

a non steroidal antiandrogen

24
Q

What is the use of flutamide?

A

metastatic prostate cancer

25
Q

What are the advserse effects of flutamide?

A

diarrhoea, anemia, hepatic injury, oedema, dizziness, blurred vision

26
Q

What is finasteride?

A

a 5-alpha reductase inhibitor

27
Q

What is the use of finasteride?

A

benign prostatic hypertrophy and hair loss

28
Q

What are the adverse effects of finasteride?

A

Impotence, decreased libido and ejaculation

disorder, breast enlargement, tenderness, breast cancer has been reported

29
Q

What is exemestane?

A

an aromatase inhibitor

Reproduction (21 decks)

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