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Pharmacology Endocrine > Oestrogen > Flashcards

Oestrogen Flashcards

1
Q

Most potent and main estrogen in ovary

A

Estradiol

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2
Q

Where is estriol formed

A

Liver

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3
Q

Where is estrone formed

A

Fat cells

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4
Q

Synthetic steroidal estrogen

A

Ethynyl estradiol
Tibolone

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5
Q

Synthetic non steroidal estrogen

A

Diethylstilbestrol
Dienestrol

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6
Q

Does estrogen have negative feedback on both hypothalamus and anterior pituitary

A

No only anterior pituitary

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7
Q

How many types of oestrogen receptors present in body

A

2
=ERalpha
=ERbeta

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8
Q

ER alpha present in

A

Ovary
Uterus
Vagina
Breast
Hypothalamus
Blood vessels

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9
Q

ER beta present in

A

Ovary
Prostate

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10
Q

Why estrogen not effective orally

A

High fast pass metabolism

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11
Q

Enterohepatic cycle of estrogen

A

All 3 natural forms undergo glucose idle and sulaate conjugation
Excreted in bile
In intestines they undergo deconjugation by bacterial flora
Then reabsorbed to complete the cycle

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12
Q

Therapeutic uses of estrogen

A
  1. delayed puberty in girls (due to turner syndrome,hypopituitarysm)
  2. Oral Contraceptives along with progestin (to reduce risk of endometrial carcinoma)
  3. Dysmenorrhea (suppress ovulation and anovulatory cycles are painless)
  4. Dysfunctional uterine bleeding (if estrogen withdrawal is the cause)
  5. Post menopausal hormone replacement therapy(to alleviate vasomotor symptoms,hot flushes,genital atrophy,osteoporosis,sleep disturbances,night sweats)
  6. Senile vaginitis(topical use)
  7. Prostatic carcinoma(by suppressing androgen production)
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13
Q

Advantage of tibolone

A
  1. Has estrogenic,progesterogenic,and weak androgenic activity
  2. Can be used in hormone replacement therapy without cyclic progesterone
  3. Does not cause endometrial proliferation
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14
Q

Adverse effects of oestrogen

A
  1. Water retention,Edema
  2. Weight gain
  3. Increased gall stones,liver diseases
  4. Thromboembolism
  5. Increased endometrial and breast cancer
  6. Nausea , vomiting
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15
Q

Which estrogen dose is lower :HRT or oral contraceptives

A

HRT(one -fifth)that of contraceptives
So low side effects

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16
Q

Name a prodrug of estrogen used in prostate carcinoma

A

Fosfestrol

17
Q

Anti estrogen

A

Clomiphine citrate

18
Q

Drug interactions of estrogen

A

Ampicillin: inhibit enterohepatic cycling of estrogen
Rifampicin: increase estrogen metabolism

19
Q

Side effects of diethylstilbesterol

A

In infants:
1. Hypospadia
2. Vaginal and cervical adenocarcinoma

20
Q

Uses of clomiphene citrate

A
  1. Female infertility
  2. Male infertility
  3. ART
    4 GIFT
21
Q

Major adverse effect of clomiphene citrate

A

Hyper stimulation syndrome
Polycystic ovary disease
Multiple pregnancy

22
Q

Uses of tamoxifene

A

Breast cancer both pre and post menopausal females

23
Q

Use of raloxifene

A

Osteoporosis in post menopausal females

24
Q

Side effects of tamoxifene

A

Endometrial cancer
Thromboembolism
Hot flushes

25
Q

Side effect of raloxifene

A

Thromboembolism
Hot flushes

26
Q

Use of selective estrogen receptor downregulator

A

Fulvestrant is used in breast carcinoma not responding to tamoxifene

27
Q

Advantage of SERD over SERM

A
  1. Faster
  2. Longer duration action
  3. Safer
28
Q

Mechanism of action of fulvestrant in tamoxifene resistant breast cancer

A
  1. 100 times more affinity towards estrogen receptor
  2. Prevents dimerisation of estrogen receptors
  3. Degradation and down regulation of estrogen receptors
  4. No transcription
  5. No ER mediated gene expression
    So due to differences in mechanism of action fulvestrant is used in tamoxifene resistant breast cancer
29
Q

STEAR example and use

A

Tibolone
:HRT
;osteoporosis

30
Q

Non steroidal reversible aromatase inhibitors

A

Letrozole
Anastrozole

31
Q

Steroidal reversible aromatase inhibitors

A

Exemestane
Formestane

32
Q

Benefit of aromatase inhibitors over tamoxifine

A

No endometrial cancer

33
Q

Why aromatase inhibits not used for post menopausal breast cancer

A

Osteoporosis

Pharmacology Endocrine (4 decks)

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