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Obstetrics and Gynaecology > Drugs affecting Reproduction > Flashcards

Drugs affecting Reproduction Flashcards

1
Q

List 3 locations whereby oestrogen is produced

A
  • Ovary
    
- Placenta
    
- Adrenal cortex
    
- Testis
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2
Q

List the 3 main endogenous oestrogens in humans.

A
  • Oestradiol (most potent and 1º secreted from ovaries)
    
- Oestrone
    
- Oestriol
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3
Q

Outline the MOA by which oestrogens induce their effect.

A

Oestrogens bind: 1) nuclear receptor (ERa/ERß) to ∆ gene transcription ; 2) GPER membrane receptors to mediate rapid vascular actions 


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4
Q

Give 3 therapeutic uses of Oestrogen

A

HRT

Contraception

Prostate/Breast Ca

Feminisation

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5
Q

List 3 ways Oestrogen can be administered.

A
  • Oral
  • Transdermal
  • Intramuscular
  • Implantable
  • Topical
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6
Q

What is a SERM?

A

Competitive antagonists or partial agonists of oestrogens

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7
Q

Give an example of a SERM.

A

Tamoxifen: Oestrogen-dependent breast Ca with anti-oestrogenic effect on tissue

Raloxifene: Post-menopausal OP, anti-oestrogenic effects on breast and uterus but oestrogen on bone

Clomiphene: Oestrogen antagonist at hypothalamus and pituitary to block negative feedback mediated by oestrogen = increase GnRH and FSH/LH causing ovulation

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8
Q

Which enzyme converts cholesterol to pregnenolone?

A

CYP11A1

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9
Q

Which enzyme converts pregnenolone to 17a-hydroxypregnenolone?

A

17a-hydroxylase

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10
Q

Which enzyme converts 17a-hydroxypregnenolone to DHEAS/Andreostenediol?

A

17,20 lyase

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11
Q

Which enzyme converts 17a-hydroxypregnenolone to 17a-hydroxyprogesterone?

A

3ß-HSD

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12
Q

What enzyme converts DHEAS to Androstenedione?

A

3ß-HSD

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13
Q

What enzyme converts Androstenediol to Testosterone?

A

3ß-HSD

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14
Q

What enzyme can convert androstenedione or testosterone to estrone and estradiol ± estriol?

A

Aromatase

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15
Q

What enzyme converts testosterone to Dihydrotestosterone?

A

5a-reductase

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16
Q

What is the drug target in its MOA for Finasteride?

A

5a reductase

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17
Q

What is the drug target in its MOA for Anastrazole?

A

Aromatase

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18
Q

Which enzyme can convert deoxycorticosterone to corticosterone?

A

11ß-hydroxylase

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19
Q

Which enzyme an convert 11-deoxycortisol to cortisol?

A

11ß-hydroxylase

20
Q

Which enzyme converts progesterone to deoxycorticosterone?

A

21a-hydroxylase

21
Q

Which enzyme converts 17a-hydroxyprogesterone to 11-deoxycortisol?

A

21a-hydroxylase

22
Q

Which enzyme converts progesterone to 17a hydroxyprogesterone?

A

17a-hydroxylase

23
Q

Outline 3 sources of Progesterone in the body.

A

Corpus luteum
Placenta
Testis
Adrenal cortex

24
Q

Outline the mechanism of action of Progesterone.

A

Acts on Progesterone Receptor (PR) to ∆ gene transcription in target tissues

25
Q

Give an example of a natural progesterone and a testosterone-derivative

A

Natural: Hydroxyprogesterone, medroxyprogesterone, dydrogesterone
- Inactive orally b/c presystemic hepatic metabolism
Administration: IM or topical

Testosterone-derivatives: Norethisterone, norgestrel, ethynodiol 

- Absorbed orally

26
Q

Give 3 effects of Progesterone

A

Inhibit oestrogen synthesis

Maintenance of endometrium

Stimulate glands in endometrium and mammary milk gland development

27
Q

Give 3 adverse effects of Progesterone Rx.

A 
Acne 
Fluid retention
Weight gain
Depression
Change in libido
Breast discomfort
Menstrual cycle irregularity 
Increased VTE %
28
Q

What is anti-progestogen?

A

Progestogen antagonist

29
Q

Give an example of an anti-progesterone used in medical ToP.

A

Mifepristone

30
Q

In the COCP, what two elements are involved?

A

Oestrogen

Progesterone

E.g. Drospirenone/Ethinylestradiol

31
Q

What is the standard regime of COCP.

A

21 days + 7 day break

32
Q

Outline the MOA of COCP

A

Oestrogen: negative feedback at Hyp and Ant. Pituitary to reduce GnRH and FSH/LH thus reduced development of ovarian follicle and ovulation; Build up of endometrium 


Progestin: Inhibit LH secretion and prevent ovulation; Maintenance of endometrium + endometrium glands; mucous plug at cervix

33
Q

Give 3 adverse effects of the COCP.

A 
Mild nausea 
Flushing
Dizziness
Bloating 
Weight gain
Skin changes (acne or pigmentation)
Depression 
Amenorrhoea or variable duration

VTE

34
Q

Give an example of a Progesterone Only Pill (POP)

A

Norethisterone

Levonorgestrel

Ethynodiol diacetate

35
Q

Outline the regime of a POP.

A

Daily

No disruption

36
Q

Which form of contraception is more effective, COCP or POP?

A

COCP

37
Q

A 21 year old girl presents after an UPSI 48 hours ago and seeks a form of contraception.

What would you give?

When would you need to give it by?

How would this be administered

A

Levonorgestrel ± oestrogen

< 72 hours

Oral

38
Q

State 3 forms of LARCs and explain what is given for each

A

1) IUS: Levornogestrel from T-shaped tube in uterus releasing progestogen to prevent implantation + thicken cervical mucous + thin endometrium to prevent implantation
2) IUD: Copper Plastic and Copper device implanted in uterus presenting sperm survival
3) IM Injection: Medroxyprogesterone acetate to prevent ovulation and thicken cervical mucus plug
4) SC Implant: Levornorgestrel administration via flexible subcutaneous rod in upper arm releasing progesterone to stop ovulation and thicken cervical mucus and thinning of uterus to prevent implantation

39
Q

Give 5 Sx of the Menopause

A 
Hot flushes
Headaches
Drier mucosal membranes 
Body and pubic hair become darker 
Bone loss mass and more fragile 
Vaginal dryness, itching and shrinking 
Nipples smaller and flatten
Breasts droop and flatten 
Risk of CVD 
Teeth loosen and gums recede
40
Q

Give 3 sites of production of Androgens in the body.

A

Leydig cells
Adrenal glands
Ovaries 


41
Q

Outline the MOA of Androgens

A

Bind nuclear receptors to ∆ gene expression

42
Q

Give 3 therapeutic uses of Androgens and where they may be used.

A

Male hypogonadism: IM testosterone injections

Prostatic cancer (anti-androgens): Flutamide, cyproterone

Benign prostatic hypertrophy (Dihydrotestosterone synthesis inhibitors - 5a-reductase): Finasteride

Aplastic anaemia: Anabolic steroids such as nandrolone

43
Q

What are anabolic steroids?

A

Modified androgens e.g. nandrolone = increase protein synthesis and muscle development

44
Q

Give 3 side effects for anabolic steroids.

A

Infertility
Salt and water retention
Coronary heart disease
Liver disease

45
Q

What is a GnRH analogue?

A

GnRH decapeptide analogue to manipulate reproductive axis

46
Q

Give an example of a GnRH analogue

A

GnRH pump

Gonadotropin

Gonadorelin

Nafarelin

47
Q

What regime would you administer GnRH analogues in?

A

Pulsatile to stimulate gonadotropins (FSH + LH) and induce ovulation

Obstetrics and Gynaecology (8 decks)

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