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MD3002 Reproductive > Drugs Affecting Reproduction > Flashcards

Drugs Affecting Reproduction Flashcards

1
Q

What are the sources of oestrogen?

A
  • ovary
  • placenta
  • small amount in adrenal cortex and testis
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2
Q

What effects do oestrogen have on hypogonadism, amenorrhoea and menopause?

A
  • in primary hypogonadism they stimulate development of secondary sexual characteristics and accelerate growth
  • in adults with amenorrhoea given cyclically with progestogen, they induce an artificial menstrual cycle
  • given at or after menopause to prevent its symptoms and protect against bone loss (but increase coagulability of blood and can cause thromboembolism)
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3
Q

What is the mechanism of action of oestrogens?

A
  • interaction with nuclear receptors to regulate gene transcription (ER-alpha, ER-beta)
  • some effects initiated by interaction with membrane receptors (GPER)
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4
Q

What are the therapeutic uses of oestrogens?

A
  • replacement therapy in primary ovarian failure (Turner’s Syndrome) to promote sexual maturation
  • replacement therapy for menopausal symptoms like flushing, vaginal dryness and osteoporosis
  • in contraception
  • prostate and breast cancer
  • in males they cause feminisation
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5
Q

What are some unwanted side effects of oestrogen?

A
  • breast tenderness
  • nausea
  • vomiting
  • anorexia
  • retention of salt and water with resultant oedema and increased risk of thromboembolism
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6
Q

What are anti-oestrogen drugs?

A
  • selective oestrogen receptor modulators (SERMs)

- competitive antagonists or partial agonists of oestrogens

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7
Q

What are some examples of SERMs?

A
  • tamoxifen: used in oestrogen-dependent breast cancer
  • raloxifene: used to treat and prevent post-menopausal osteoporosis
  • clomiphene: pure oestrogen antagonist at hypothalamus and pituitary that blocks negative feedback leading to increased gonadotropin secretion, E2 and ovulation
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8
Q

What are the sources and mechanism of action of progesterone?

A
  • corpus luteum late in menstrual cycle
  • placenta in pregnancy
  • acts on progesterone receptor to regulate gene transcription in target tissues
  • oestrogen stimulates receptor synthesis (progesterone inhibits oestrogen receptor synthesis)
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9
Q

What are the therapeutic uses of progestogens?

A
  • oral contraceptive pill (either alone or in combination with oestrogen)
  • progesterone only injectable or implantable contraception
  • intrauterine contraceptive
  • combined with oestrogen for oestrogen replacement therapy in women to prevent:
  • endometrial hyperplasia
  • carcinoma
  • endometriosis
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10
Q

What are the adverse effects of progestogens?

A

Progestogens:

  • acne
  • fluid retention
  • weight gain
  • depression
  • change in libido
  • breast discomfort
  • menstrual cycle irregularity
  • increased thromboembolism
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11
Q

What is an example and use of anti-progestogens?

A
  • mifepristone
  • used in combination with prostaglandin analogues is effective medical alternative to surgical termination of early pregnancy (up to 9 weeks)
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12
Q

What are the common types of oestrogen and progesterone used in the combined pill?

A

Oestrogen::

  • ethinyloestradiol
  • mestranol

Progesterone:
- norethisterone
- levonorgestrel
(or if 3rd gen: desogestrel or gestodene)

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13
Q

Describe the mechanism of action of the combined pill

A
  • oestrogen inhibits secretion of FSH by negative feedback on anterior pituitary
  • progestin inhibits LH secretion and ovulation
  • act together to alter endometrium to discourage implantation
  • can interfere with coordinated contractions of cervix, uterus, and fallopian tubes that facilitate fertilisation and implantation
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14
Q

What are the adverse effects of the combined pill?

A
  • mild nausea, flushing, dizziness, bloating
  • weight gain, skin changes, depression
  • amenorrhea variable during cessation of taking it
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15
Q

What are some examples of the progestin only pill?

A
  • norethisterone
  • levonorgestrel
  • ethynodiol diacetate
  • desogestrel
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16
Q

What is the mechanism of action of the progestin only pill?

A
  • reduces LH secretion and makes cervical mucus inhospitable to sperm
  • hinders implantation through its effect on the endometrium and on motility and secretions of fallopian tubes
17
Q

What are some other regimens of contraception?

A
  • emergency contraception: oral levonogestrel on its own or in combination with oestrogen within 72 hrs of unprotected sex and repeated 12 hours after

Long acting progestogen only contraception:

  • levonorgestrel: subcutaneous implant (5yr) or etonogestrel subdermal implant (3yr)
  • medroxyprogesterone acetate given intramuscularly
  • levonorgestrel impregnated intrauterine device that can last for 35 years
18
Q

What are some of the changes that occur with menopause?

A
  • headaches and hot flushes
  • hair becomes thinner
  • teeth loosen and gums recede
  • breasts droop and flatten
  • backache
  • stress/urge continence
  • body and pubic hair become thicker and darker
  • bones loose mass
  • vaginal dryness, itching and shrinking
19
Q

Describe the process of post-menopausal HRT and its pros and cons

A
  • cyclic or continuous administration of low dose oestrogens with or without progestins
  • pros: improves symptoms caused by reduced oestrogen like hot flushes, vaginal dryness and prevents and treats osteoporosis
  • cons: withdrawal bleeding, increased risk of breast and endometrial cancer, increased risk of thromboembolism
20
Q

What are the modes of administration and uses of androgen HRT and anti-androgens with examples?

A
  • intramuscular depot injections or patches
  • androgen HRT: used for replacement therapy in male hypogonadism due to pituitary or testicular disease and female hyposexuality following removal of ovaries
  • antiandrogens (flutamide, cryproterone): prostatic cancer
21
Q

What are anabolic steroids, their uses and side effects?

A
  • androgens that have been modified to alter anabolic effects such as to increase protein synthesis and muscle development
  • used for aplastic anaemia
  • abused by athletes
  • side effects: infertility, salt and water retention, coronary heart disease and liver disease
22
Q

What are gonadotropin-releasing hormone analogues, examples and the process of administration?

A
  • decapeptides, analogs used to manipulate the reproductive axis
  • eg. gonadorelin (same as endogenous form made synthetically) and nafarelin (more potent)
  • given in pulsatile fashion: stimulate release of FSH and LH inducing ovulation and used in infertility
  • continuous administration: gonadal suppression for sex hormone-dependent conditions (breast/prostate cancer, endometriosis)

MD3002 Reproductive (35 decks)

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