Women's Health Flashcards
What are the oestradiol formulations for HRT available in NZ? (4 points)
- oral tablet
- nasal spray [discontinued]
- vaginal tablet
- transdermal patches
What are the brands of transdermal oestradiol patches (4 points)
- Estroderm
- Climara
- Femtran
- Estrodot
What are the main components of Estraderm TTS? (4 points)
- Estradiol containing reservoir
- Release controlling membrane
- Adhesive backing
- protective liner
Can a estraderm TTS be halved?
-no as halving it would damage the release controlling membrane.
What are the main differences between the stengths of Estroderm TTS? (4 points)
- Nominal rate of estradiol release
- Content of estradiol
- Drug releasing area
- Imprint
How does norminal rate of estradiol release differ between the estraderm patches? (3 points)
- Estraderm TTS 25 releases 24mcg/day
- Estraderm TTS 50 releases 50mcg/day
- Estraderm TTS 100 releases 100mcg/day
How does the content of estradiol differ between the estraderm patches? (3 points)
- estraderm TTS 25 contains 2mg
- Estraderm TTS 50 contains 4mg
- Estraderm TTS 100 contains 8mg
How does the drug releasing area differ between the estraderm patches? (3 points)
- estraderm TTS 25 releases over 5cm^2
- estraderm TTS 50 releases over 10cm^2
- estraderm TTS 100 releases over 20cm^2
How long is the release of the active substance maintained for?
-4 days
How long does it take for the patches to reach steady state concentration? (2 points)
- 8 hours after administration of any sized patch
- this concentration is maintained for the duration of the treatment
What are the key points for administration of estroderm TTS? (4 points)
- remove protective liner
- immediately apply patch to clean, dry and intact area of skin
- select an area that will not be exposed to sunlight and which undergoes minimal wrlinking during normal movement
- rotate areas of application
What symptoms are affected by progesterone therapy? (4 points)
- hot flushes
- endometrial protection
- bone mineral density
- improved lipid profile
What are the effects of the oral progesterone formulations? (4 points)
- unknown effect on HF
- positive effect on endometrial protection
- unknown effect on BMD
- Positive effect on lipid profile
What are the effects of vaginal progesterone formulations? (4 points)
- unknown effect on HF
- positive endometrial protection
- unknown effect on BMD
- unkonwn effect on lipid profile
What are the effects of transdermal progesterone formulations? (4 points)
- positve effect on HF
- Positive effect on endometrial protection
- Positive effect on BMD
- No effect on lipid profile
what are the issues related to transdermal progesterone? (5 points)
- Lack of data on risks/beneits
- transport not fully understood
- no standardisation of formulations due to limited comparative data
- lack of knowledge on dose response relationships
- low bioaailability due to metabolism by 5-alpha-reductase in the skin
What was the formulation which helped to prevent progesterone metabolism in the skin? (1 point)
Dutasteride cream which contained a 5-alpha reductase inhibitor
How is post menopausal OP treated? (3 points)
- calcium
- vitamin D
- bisphosphonates (Alendronate)
What are the physicochemical characteristics of alendronate? (3 points)
- water solubility 10mg/mL
- various pKa values of phosphate groups
- largely ionised in GIT
What are the pharmacokinetics of alendronate? (5 points)
-oral bioavailability
what is the issue with alendronate generics? (3 points)
- due to additives in the generic formulation, mucoadhesiveness occurred
- this caused esophageal adhesiveness and irritation especially in patients who ingest little water or who recline shortly after taking the dose
- fosamax showed little or no bioadhesion
What are the different contraceptive methods? (6 points)
- Non pharmacological methods
- oral
- nasal
- IUD
- depot injection
- implants (norplant, Jadelle, implanon)
What is Mirena? (5 points)
- IU system which is long acting reversible contraceptive
- contains 52mg Levonorgestrel
- Indicated for contraception, menorrhagia, HRT
- fitted by medical doctor
- PHARMAC funded by SA with conditions around menorrhagia, not funded for contraception alone
How does Mirena work? (3 points)
- there is a hormone elastomer core mounted on the vertical stem of a T body
- covered with opaque tubing which releases levonorgestrel
- Release rate is 20mcg/24 hours which declines to 10mcg/24 hours after 5 years
Why is the dosing in Mirena lower than oral tablet (30mcg)? (1 point)
-the oral tablet has to have enough levonorgestel to account for first pass metabolism, elimination etc.
What are the local effects of mirena?
- thickens normal mucous in cervical canal so sperm cannot enter uterus to fertilise egg
- inhibits normal sperm function and movement preventing fertilisation
- reduces monthly growth of the lining of uterus making period lighter and preventing pregnancy.
What is depo-provera? (3 points)
- IM depot injection
- Medroxyprogesterone acetate oily suspension
- administered ever 12-13 weeks
Why is depot provera formulated as a suspension? (4 points)
- in a suspension there is a equilibrium between solid particles and liquid phase
- in the liquid phase particles can migrate out of the depot and have effect on the body
- Where particles have migrated out, the equilibrium wil allow more solid particles to dissolve
- essentially the suspension is the method of controlled release.
What is Norplant? (3 points)
- older implantable contraceptive technology first approved in finland 1983, then USA 1990
- SR levonorgestrel providing contraception for 5 years
- release rate slow decreases from 85ug/day in the 1st month to 30ug/day by the 60th month
What is Jadelle? (5 points)
- Subdermal implant containing 2 x 75 mg levonorgestrel
- flexible rods 43mm in length and 2.5mm in diameter
- funded in NZ
- provides contraception for up to 5 years
- Removeable with minor procedure
How does the rate of levonorgestrel release differ with its duration for Jadelle? (4 points)
- after 1 month, 100mcg/day
- end of 1 year, 40mcg/day
- end of 3 years, 30mcg/day
- end of 5 years, 25mcg/day
What is the newer implantable contraceptive device? (7 points)
- implanon was first approved in indonesia 1998, followed by USA in 2006
- contains etonogestrel release providing contraception for 3 years
- single stiff rod
- marketed as easier to insert and remove
- registered in NZ but not currently funded
- each rod is 4cmx 2mm
- rate or release decreases over 3 years, but sufficient to cover for 3 years
What are the current options for male contraception? (3 points)
- condoms
- withdrawal
- timing of female cycle
- vasectomy
What are the potential issues with oral male contraceptives? (2 points)
- women don’t trust men to take a pill every day
- men nervous of contraceptive pill having witnessed the evolution of the female oral contraceptive
What are the aims of male contraceptives? (2 points)
- prevent sperm from reaching the egg
- prevent sperm from fertilising the egg
What are the approaches towards male contraception? (4 points)
- hormonal suppression of spermatogenesis
- non hormonal suppression of spermatogenesis
- blocking sperm functions needed for fertilisation
- immunocontraceptive approaches
What are the limitations with male hormonal contraception? (4 points)
- more difficult to achieve azospermia in men than anovulation in women
- Sex hormones can be administered to lower sperm count however also reduces testosterone production having its own adverse effects
- small pilot studies have been able to achieve azoospermiea however no hormonal contraceptive is ready for clinical use.
What are the considerations for moving towards male contraception? (4 points)
- ideally a pill with low frequency of administration required
- minimal side effects
- non-hormonal medicines may be preferred
- needs to be a shift in contraceptive culture and responsibility and acceptability needs to be shared.
