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Pharmacology > Sex Hormones > Flashcards

Sex Hormones Flashcards

1
Q

Estrogen is produced by

A

developing ovarian follicles

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2
Q

Which are the natural Estrogens

A

17-B Estradial
Estrone
Estriol

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3
Q

Metabolism of Natural Estrogens

A

Large 1st pass hepatic metabolism
short T1/2

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4
Q

What is a Natural Estrogen

A

most potent and principal Estrogen secreted by ovary

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5
Q

Which are the Synthetic Estrogens

A

Ethinyl Estradial
Mestranol

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6
Q

Metabolism of Synthetic Estrogens

A

less 1st pass metabolism
much longer T1/2

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7
Q

How are Estrogens transported

A

by binding to SHBG(binds NE more) and Albumin

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8
Q

Action of Synthetic Estrogens

A

Decr. GNRH from hypothalamus–> decr. FSH and LH release

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9
Q

Metabolic effects of Estrogen

A

Bone mass: decr. activity of osteolcasts–> decr. bone resorption
Lipid M: incr. in trigs and HDL, decr. in cholesterol and LDL
Carbohydrate M: can impair glucose tolerance and induce insulin resistance
Protein M
Blood: decr. Antithrombin III levels=incr risk of blood clots and thrombosis
CVS: causes arteriolar vasoldilation
Skin: decr. sebum production

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10
Q

AEs of Estrogen

A

NV
Fullness and tenderness of breast
Oedema
Migraine
Reactive/exacerbate Endometriosis
Gallbladder disease
Thromboembolis
Carcinogenic actions: endometrial+breast cancer
Glucose intolerance
Post menopausal uterine bleeding

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11
Q

Uses of HRT

A

used to treat symptoms associated with meonopause

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12
Q

Effects of Menopause

A

marked decr. in Ovarian Estrogen production–> low serum [Estradiol] + vasmotor symptoms like hot flashes

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13
Q

What is a combined continuous HRT

A

progestin given daily with estrogen to prevent Endomterial proliferation and avoids bleeding

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14
Q

What is a combined Sequential HRT

A

Progestin added for the last 10-14 days of the cycle to produce endometrial shedding and withdrarwal bleeding

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15
Q

Indications of Estrogen Therapy

A

Osteoporosis: prevents bone loss
Urogenital Atrophy: dryness and itching of vagina, painful intercourse and urination, sudden/unexpected incontinence
Vasomotor symptoms: hot flushes, chilly sensations inappriopriate sweating and paresthias

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16
Q

HRT CIs

A

Breast cancer
Past DVT or Pulmonary embolism: incr. risk of blood clotting bcos it decr. Antithrobin III
Active liver disease

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17
Q

Cautions in HRT

A

Diabetes
Hypercholesterolaemia
Hypertension

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18
Q

Indications of Estrogen Monotherapy

A

ONLY for women who had a Hysterectomy as progesterone unfavourably alters HDL:LDL ration

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19
Q

Preparations of Estrogen Monotherapy

A

Conjugated estrogens
Estradiol
Estriol
Estrone

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20
Q

Admin of Estrogen Monotherapy

A

Transdermal patch
SC implants
Vaginal Pessaries: oil based
Rings
Topical gel applications like sprays, patchs

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21
Q

Which admin route of Estrogen bypassess 1st pass effect

A

Parenteral admin

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22
Q

Which are the selective Estrogen Receptor Modulators

A

TTCR
Tamoxifen
Toremifene
Raloxifene
Clomiophen

23
Q

Activity of SERMs

A

have tissue selective activity
–> are Estrogenic on bone BUT have Anti-Estrogenic effects in Breast tissue

24
Q

Indications of Tamoxifen & Toremifene

A

Estrogen-dependent Breast cancer

25
Q

Effects of Tamoxifen & Toremifene

A

decr. total cholesterol and LDL
No incr. in HDL and Trigs
Incr. risk of DVT and pulmonary embolism

26
Q

Estrogenic effects of Tamoxifen & Toremifene

A

Estrogenic on bone, in blood and in Endometrium

27
Q

AEs of Tamoxifen & Toremifene

A

Hot flushes
Vagial dryness/discharge
Cataracts
Nasuea

28
Q

Indications of Raloxifene

A

Prevention and Treatment of Osteoporosis

29
Q

Effects of Raloxifene

A

decr total Cholesterol
Decr. LDL
No effect on HDL

30
Q

Raloxifene have no effects on

A

breast tissue and endometrium
Vasmotor symptoms

31
Q

Raloxifene is an agonist in

A

bone: distal sites and spinal column

32
Q

AEs of Raloxifene

A

Hot flushes
Leg cranps
Incr. risk of DVT and Pulmonary Embolism

33
Q

Estrogenic effects of Raloxifene

A

Estrogenic on bone and in blood

34
Q

Name an Antiestrogen

A

Clomiphene

35
Q

Indications of Clomiphene

A

treatment of infertility
–> inhibits Estrogen Rs in Hypothalamus
–> triggers PG to incr FSH+LH=initiation of ovulation

36
Q

Clomiphene is used in conjunction with

A

hCG

37
Q

Clomiphene acts as an

A

SERM: Selective Estrogen Receptor Modulator

38
Q

AEs of Clomiphene

A

Ovarian Hyperstimulation
Incr. incidence of multiple births
Ovarian Cysts
Blurred vision
Acidic mucous
Hot flushes

39
Q

What is Tibolone

A

agent that acts as an agonist at Estrogen Rs

40
Q

Activity of Tibolone

A

Estrogenic
Progestogenic
Weak Androgenic

41
Q

Indications of Tibolone

A

HRT
Endometriosis
Breast cancer

42
Q

Tibolone relieves

A

Hot flushes
insomnia
vaginal dryness
Prevents bone loss

43
Q

Tibolone is an Anti-Estrogenic at

A

Endometrium: has less stimulatory effects

44
Q

Name an Estrogen Receptor Antagonist/Downregulator

A

Fulvestrant

45
Q

Indications of Fulvestrant

A

hormone receptor positive or metasttatic cancer

46
Q

MOA of Estrogen Synthesis inhibitors

A

Continuous admin of long acting GNRH agonists–> inhibit ovarian synthesis of Estrogen

47
Q

Indications of Estrogen Synthesis inhibitors

A

Endometriosis
Uterine Fibroids

48
Q

What is Aromatase

A

Enzyme that converts androgens to Estrogen

49
Q

MOA of Non-steroidal Aromatase Inhibitors

A

Decr. Estrogen by inhibiting Aromatase enzyme=decr. breast cancer risk
*also inhibit testosterone conversion to Estradiol

50
Q

Which are the Non-steroidal Aromatase Inhibitors

A

Anastrozole
Letrozole
Exemestane

51
Q

Effects of Non-steroidal Aromatase Inhibitors

A

lead to Hypoestrogenic states

52
Q

AEs of Non-steroidal Aromatase Inhibitors

A

Insomnia
vaginal dryness
hot flushes

53
Q
A

Pharmacology (50 decks)

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