Reproductive Pharmacology Flashcards

1
Q

Clomiphene

A
  • used to treat anovulatory infertility and PCOS
  • competitively antagonizing oestrogen receptors in the hypothalamus
  • interferes with normal negative feedback loops and increases release of FSH and LH
  • half life of 5-7 days - ovulation occurs 6-12 days post treatment
  • courses may be repeated
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2
Q

Gonadotrophin

A
  • for male ‘infertility’
  • increase spermatogenesis (sperm quantity)
  • administered as hCG for several months
  • exogenous FSH analogue added for several months for further treatment
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3
Q

Sildenafil

A
  • viagara, used to treat erectile dysfunction
  • PDE 5 inhibitor
  • enhance erectile function by preventing the breakdown of cGMP
  • adverse effects related to effects on systemic vasculature (sever hypotension)
  • contraindicated in men with CV conditions such as unstable angina due to use of nitrate or selective a-blockers
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4
Q

Tadalafil

A
  • PDE 5 inhibitor used to treat erectile dysfunction
  • enhance erectile function by preventing the breakdown of cGMP
  • longer time to onset of action and longer half life
  • adverse effects related to effects on systemic vasculature (sever hypotension)
  • contraindicated in men with CV conditions such as unstable angina due to use of nitrate or selective a-blockers
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5
Q

Testosterone

A
  • most important androgen in humans
  • under the control of GnRH
  • testes in males/ovaries in females but in smaller amounts
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6
Q

Progestogen

A
  • natural hormone is progesterone, which supports egg whilst placenta is grown
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7
Q

What is the mode of action of progestogen-only contraception?

A
  1. altering frequency of GnRH
  2. decreasing responsiveness of anterior pituitary to GnRH
  3. act on hypothalamus and suppress pituitary LH surge
  4. alters tube peristalsis, endometrial receptivity and cervical mucous secretion preventing proper transport of both egg and sperm
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8
Q

Medroxyprogesterone acetate

A
  • progestogen-only I/M injection
  • given every 12 weeks
  • immediate effect in 1st 5 days of menstrual cycle
  • delayed return of fertility after cessation of therapy
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9
Q

Etonogestrel

A
  • progestogen-only implant
  • inserted sub-dermally into non-dominant arm
  • immediate effect in 1st 5 days of menstrual cycle
  • unpredictable bleeding or periods cease
  • fertility returns 1-2 months after removal
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10
Q

Levonorgestrel

A
  • progestogen-only oral tablet
  • recommended for lactating women
  • ovulation suppressed in <50% of women
  • must be taken at the same time of day within 3 hours
  • some women experience menstrual chaos
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11
Q

Norethisterone

A
  • progestogen-only oral tablet
  • recommended for lactating women
  • ovulation suppressed in <50% of women
  • must be taken at the same time of day within 3 hours
  • some women experience menstrual chaos
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12
Q

Oestrogen

A
  • released by the follicle
  • strong proliferator of cells and angiogenesis
  • prepares uterus for implantation
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13
Q

Ethinyloestradiol

A
  • oestrogen used in the combined oral contraceptive pill
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14
Q

Combined Oral Contraceptive Pill

A
  • suppress GnRH, LH and FSH secretion and follicular development, thus inhibiting ovulation
  • alters tubal peristalsis, endometrial receptivity, and cervical mucous secretion - preventing proper transport of both egg and sperm
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15
Q

Why is progestogen included in the COC?

A
  • progestogen decreases the risk of thromboembolism and cancer (breast and ovary)
  • combination gives high reliability and good control
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16
Q

Oestradiol

A

Oestrogen

17
Q

Tibolone

A
  • Selective tissue oestrogen activity regulator
  • acts as an oestrogen on vagina, bone and thermoregulatory centres in the brain
  • anto-oestrogenic and progestognenic activity on breasts and endometrium (reduces cancer risk)
  • acts as an androgen to improve energy and well-being complex effect on lipid profile
18
Q

What are androgens?

A

Group of steroids with anabolic properties.

19
Q

What are the causes of delayed puberty?

A
  • dysfunction of hypothalamic-pituitary axis
  • end organ function
  • chronic and severe medical conditions
  • weightless and malnourishment
  • physical stress
20
Q

What is dysmenorrhoea?

A
  • Falling progesterone towards the end of the menstrual cycle leads to local production of prostaglandin by the decidua.
  • PGs cause vasospasm of the spiral arteries of the uterus and subsequent ischaemia, and uterine cramping
21
Q

What is perimenopause?

A
  • unpredictable ovarian function and menstrual irregularity
  • may continue for a number of years before menopause
  • attributed to oestrogen withdrawal but believed to be also affected by psychosocial response to middle age and ageing
22
Q

What is menopause?

A
  • long-term disease processes influenced by oestrogen withdrawal
  • a post-menopausal ovary will still produce androgens and convert them to oestrogen
  • can only be retrospectively recognized by the final menstrual period
23
Q

Does male menopause exist?

A
  • not technically
  • secretion of testosterone declines but not enough to affect libido or erectile dysfunction
  • other anabolic steroids decline markedly and affect musculoskeletal strength
24
Q

What is tricycling?

A
  • taking the pill three months in a row and skipping withdrawal bleeding
  • can be useful if headaches/migraines or heavy bleeding associated with withdrawal of hormones
  • some women prefer the normality of a ‘period’
25
Q

What are the formulations of the COC?

A
  1. Monophasic: fixed dose of oestrogen and progestogen.

2. Multiphasic: either both oestrogen and progestogen or just the progestogen varies throughout the cycle

26
Q

When is the COC contraindicated?

A
  1. smoking
  2. BMI
  3. hypertension, ischaemic heart disease etc.
27
Q

What is an intrauterine device?

A
  • a small flexible device/s of metal or plastic
  • copper OR levonorgestrel
  • inhibits sperm migration and ovum transport, thus preventing implementation
28
Q

What is emergency contraception?

A
  • post-coital contraception
  • levonorgestrel is most common either in 1 dose or 2 half doses, prevents or delays ovulation
  • copper IUD
  • can be taken up to 5 days after sex
29
Q

What other treatments are available for female infertility besides Clomiphene?

A
  • in-vitro fertilisation (IVF)

- gamete intra-fallopian transfer (GIFT)

30
Q

What hormones are involved in the hormone regime for IVF?

A
  • GnRH agonist
  • FSH analogue and hCG to induce ovulation
  • progesterone to assist in maintaining endometrium
31
Q

How is infertility associated with hyperprolactinaemia treated?

A

With cabergoline, a dopamine agonist with high affinity for D2 receptors.