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MD3002 Pharmacology > Drugs Affecting Reproductive Function > Flashcards

Drugs Affecting Reproductive Function Flashcards

1
Q

Where are oestrogens synthesised?

A
  • Ovary and placenta

- Small amounts in adrenal cortex and testes

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2
Q

What are the 3 main endogenous estrogens in humans?

A
  • Oestradiol
  • Oestrone
  • Oestriol
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3
Q

What are oestrogens main mechanism of action?

A

Interaction with nuclear receptors (ERa and ERB) to regulate gene transcription

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4
Q

What are some oestrogen effects (like rapid vascular actions) initiated by?

A

Interaction with membrane receptors (e.g/ GPER)

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5
Q

WHat do oestrogen effects depend on?

A

State of sexual maturity

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6
Q

How can artificial menstrual cycle be stimulated in a female with amenorrhea?

A

Given progesterone cycilcally

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7
Q

What can low oestrogen lead to?

A

Bone loss, low bone density

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8
Q

What can oestrogen-replacement therapy increase the risk of?

A

Coagulability of blood and increase the risk of thromboembolism

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9
Q

What menopausal symptoms can oestrogen replacement therapy protect against?

A
  • FLushing
  • Vaginal dryness
  • Osteoporosis
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10
Q

Where can oestrogens be absorbed?

A
  • Well absorbed from gut, across skin and mucous membranes

- Many different preparations exist (oral, transdermal, IM, implantable, topical)

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11
Q

What are the different natural oestrogens which can be administered?

A
  • Estradiol

- Estriol

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12
Q

What are the different types of synthetic oestrogens prescribed?

A
  • Mestranol
  • Ethinylestradiol
  • Diethylstilbestrol
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13
Q

What are oestrogens bound to in the blood?

A

Albumin and a sex hormone-binding globulin (active estrogen are in the unbound state)

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14
Q

What are the unwanted effects of estrogens?

A
  • Breast tenderness
  • nausea
  • Vomiting
  • Anorexia
  • Retention of salt and water with resultant oedema
  • Increased risk of thromboembolism
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15
Q

What are competitive antagonists or partial agonists of estrogens called?

A

Selective estrogen receptor modulators (SERMS)

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16
Q

What is the function of Tamoxifen?

A
  • SERM
  • Used in estrogen-dependant breast cancer
  • Anti-estrogenic action on mammary tissue
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17
Q

What is the function of Raloxifene?

A
  • SERM
  • Used to treat and prevent post-menopausal osteoporosis (antiestrogenic effects on breat and uterus but estrogenic action on bone)
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18
Q

What is the function of Clomiphene?

A
  • SERM
  • Pure estrogen antagonist at the hypothalamus and pituitary
  • Acts to block negative feedback which leads to increased Gonadotropin secretion, increased E2 and ovulation
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19
Q

What are progesterones secreted by?

A
  • Corpus luteum in late menstraul cycle

- Placenta during pregnancy

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20
Q

What is used as a progestogen therapeutically instead of progesterone?

A

Progestins are used instead of progesterone as progesterone is cleared rapidly by the body

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21
Q

What are some derivatives of natural progesterone?

A
  • Medroxyprogesterone

- Hydroxyprogesterone

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22
Q

What are some testosterone derivatives?

A
  • Norethisterone
  • Ethynodiol
  • Desogestrel
  • Gestodene (these are newer and have less androgenic activity)
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23
Q

What are the therapeutic uses of progestogens?

A
  • Main therapeutic uses are in the oral contraceptive pill alone or in combination with estrogen
  • Used as progesterone only injectable or implantable contraception or part of an intrauterine contraceptive
  • Combined with estrogen for replacement therapy
24
Q

What does progestrone combined with estrogen in replacement therapy prevent?

A
  • Endometrial hyperplasia
  • Carcinoma
  • Endometriosis
25
Q

What are some adverse effects of progestogens?

A
  • Acne
  • Fluid retention
  • Weight gain
  • Depression
  • Change in libido
  • Breast discomfort
  • Menstraul cycle irregularity
  • Increased thromboembolism
26
Q

What can medication can be used as an alternative to surgical termination of early pregnancy (up to 9 wks)?

A

Mifepristone, in combination with prostalglandin analogues

27
Q

What oestrogen is used in most combined pills?

A
  • Ethinyloestradiol

- Mestranol

28
Q

What can the progestogen be in the combined pill?

A
  • Norethisterone
  • Levonorgesterl
  • Ethynodiol
  • 3rd generation pills: desogestrel or gestodene (more potent and have less androgenic actions)
29
Q

What is the estrogen content in a combined pill generally?

A

20 - 50 ug

- Advice is to use the lowest does that is well tolerated and gives good cycle control

30
Q

How are most combined pills taken (what is the cycle like)?

A
  • Taken for 21 consecutive days

- Followed by 7 days pill free to allow for a withdrawl bleed

31
Q

How does estrogen inhibit the secretion of FSH?

A

Via negative feedback on the anteriorpituitary (results in suppression of development of ovarian follicle)

32
Q

What does progestin inhibit?

A

LH secretion and prevents ovulation

33
Q

What are the adverse effects of the combined contraceptive pill?

A
  • Mild nausea, flushing, dizziness and bloating
  • Weight gain, skin changes (acne or pigmentation), depression or irritability
  • Amenrrhea of variable duration after cessation of taking the pill
  • Serious withdrawl effects are rare
  • A small number of women develop reversible hypertension
  • Asmall increase in the risk of thromboembolism
34
Q

Give examples of the progestin only contraceptive pill?

A
  • Norethisterone
  • Levonorgestrel
  • Ethynodiol diacetate
35
Q

What is the primary action of the progesterone only contraceptive pill?

A
  • Primarily on cervical mucous which is made inhospitable to sperm
  • Probably also hinders implantation through its effect on the endometrium and on the motility and secretions of the fallopian tubes
36
Q

When are progesterone only contraceptive pills used as an alternative to the combined pill?

A
  • When oestrogen -containing medications are contraindicated
  • Suitable for women whose blood pressure rises unacceptably during treatment with combined pill
37
Q

What is the downside to the progesterone only pill?

A

Less reliable than the combined pill

38
Q

What is the post-coital (emergency) contraception?

A
  • Oral administration of levonogesterl alone or in combination with estrogen is effective if taken within 72 hours and repeated 12 hours later
39
Q

What are some of the long-acting progesterone only contraceptions?

A
  • Medroxyprogesterone acetate can be given IM as contraception
  • Levonorgestrel implanted subcutaneouly (capsules release progestogen slowly over 5 years)
  • Intrauterine levonorgestrel device (can last 35 years)
40
Q

What are the symptoms of menopause?

A
  • Headaches and hot flashes
  • Hair becomes thinner and loses luster
  • Teeth loosen and gums recede
  • Breasts droop and flatten
  • Risk of CV disease
  • Nipples become smaller and flatten
  • Backaches
  • Skin and mucous membranes become drier, skin develops a rougher texture
  • Abdomen loses some muscle tone
  • Body and pubic hair becomes thicker and darker
  • Stress or urge incontinance
  • Bones lose mass and become more fragile
  • Vaginal dryness, itching and shrinking
41
Q

What does postmenopausal hormone replacement therapy involve?

A

Either cyclic or continous administration of low dose estrogens (estradiol, estriol) with or without progestogens

  • Improves symptoms caused by reduced estrogen such as hot flushes and vaginal dryness
  • Prevents and treats osteoporosis
42
Q

What are the drawbacks of postmenopausal hormone replacement therapy?

A
  • Withdrawl bleeding
  • Increased risk of breast cancer (risk disappears after 5 yrs of HRT)
  • Increased risk of endometrial cancer (if estrogens unopposed by progesterone)
  • Increased risk of thromboembolism
43
Q

What is the principle androgen?

A

Testosterone

44
Q

What hormone stimulatees androgen secretion?

A

LH

45
Q

What are used as part of the treatment of prostatic cancer?

A

Antiandrogens

  • Flutamide
  • Cyproterone
46
Q

What are IM injections or patches of testosterone esters used for?

A
  • Replacement therapy in male hypogonadism due to pituitary or testicular disease and female hyposexuality following overiectomy
47
Q

What medication is used to treat benign prostatic hypertrophy?

A

Dihydrotestosterine synthesis inhibitors such as finasteride

48
Q

Give an example of an anabolic steroid?

A

Nandrolone

49
Q

What can anabolic steroids such as nandrolone be used to treat?

A

Aplastic anaemia (abused by some athletes)

50
Q

What are some side effects of anabolic steroids?

A
  • Infertility
  • Salt and water retention
  • Coronary heart disease
  • Liver disease
51
Q

How can the reproductive axis be manipulated above the level the gonads?

A

Maipulate the levels of LH and FSH through giving analogues of GnRH

52
Q

How many amino acids make up Gonadotrophin-releasing hormone (GnRH)?

A

10 (decapeptide)

53
Q

What are some examples of GnRH analogues?

A
  • Gonadorelin - same exact aa sequence as GnRH

- Nafarelin - more potent

54
Q

What can GnRH analogues be used to treat?

A

INfertility - release of them in a pulsatile fashion will induce ovulation through stimulation of release of FSH and LH (also hypogonadotrophic hypogonadism)
- Sex-hormone dependant conditions - will induce gonadal suppression (prostate and breast cancers, endometriosis and large uterine fibroids)

55
Q

How are gonadotropins made?

A

Through recombinant DNA technology or extracted from urine of pregnant or post-maopausal women

MD3002 Pharmacology (7 decks)

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