contraceptives: Flashcards
moa of contraceptives:
- oestrogen-> FSH inhibited-> ovarian follice supressed.
- progestrone-> block LH-> ovulation prevention.
- both steroids discourage endometrium implantation.
oral contraceptives can be divided into several:
- progesterone only.
- monophasic- estrogen and prog fixed.
- biphasic- estrogen fixed and progestrone increased.
- triphasic- estrogen fixed or changed, prog increased 3x times in cycle.
duration- 21-24 days actives, 4-7 placebo–> total 28 days.
most common estrogen is ethinylestradiol and most common progestins- norethindrone, northindrone acetate, levonorgestrel, desogestrel, noregestimate, drosiprenone.
adverse
- weight gain.
- nausea flushing dizziness, depression.
- acne pigmentation.
- amenorrhea- once pills are withdrawn.
- Thromboemboli.
- decreased ovarian and endometrial cancer, hepatic adenoma (controversial).
- HDL increased and decrease LDL.
- GI- cholestasis, gallbladder disease.
contraindication
cardiovascular disorders.
estrogen dependent neoplasm
vaginal bleed of unknown cause.
before epiphyseal closure—> not to be given to younglings.
minipill
2) Oral contraceptives progestins alone („minipill”)
• daily progestin tablets: norethindrone (0,35mg) or norgestrel (0,075mg)
• useful in patients for whom estrogens are undesired or contraindicated (e.g. hepatic disease, prior thromboembolism) • side effects: headache, dizziness, weight gain, impaired glucose tolerance, abnormal (irregular) bleeding.
depot contraceptives
3) Parenteral (depot) contraceptives
• injection of depot medroxyprogesterone acetate (150 mg i.m.) every 2-3 months
• common side effects: headache, impaired glucose tolerance, disadvantageous lipid changes, abnormal (irregular) bleeding
• long amenorrheal episodes after the discontinuation of the treatment (6-12 months)- may delay fertility for months.
• estrogen+progestin depot injections - like the oral combination.
contraceptive patch
4) Contraceptive patches
• estrogen+progestin combinations
• ethinylestradiol 0,6 mg + norelgestromin 6 mg (active metabolite of norgestimate)
• daily release of 20 μg ethinylestradiol és 0,15 mg norgestromin
• adverse effects - like oral combinations—less liver effects.
5) Contraceptive implantates
5) Contraceptive implantates
• sc. implantates of norgestrel or etonorgestrel (active metabolite of desogestrel)
• duration of action: 3-6 years
• low incidence of adverse effects (low hormone level)– headache, dizziness, acnes, alopecia, mood changes, breast tenderness, decreased libido, weight gain, vasomotor problems
• major bleeding disturbances (mostly irregular cycles).
local contraceptives
6) Local contraceptives
6)A) • intrauterine device cont.: levonorgestrel- daily release of 20micrograms.
• duration of action: 5 years
• low systemic hormone level
6)B) vaginal ring: 15 μg ethinylestradiol and 12 mg etonorgestrel released every day
• 3 week use - 1 week pause
6)C) • spermicidal desinfectants
• benzalkonium, nonoxinol
• less effective, but inhibit the transmission of STD.
morning after pill
7) „morning after” pill
• progestin alone or in combination with estrogen, should be taken within 3 days (best in 12hours)
• high dose (e.g. 0,75-1,5 mg levonorgestrel)
• common side effects: nausea, vomiting, headache, dizziness, breast tenderness, abdominal and leg crumps
• ulipristal-acetate (alternative drug): SPRM, within 5 days (best – earlier)
• side effects: similar to progestins
8) abortion pill: mifeprostone (RU 486)