contraceptives: Flashcards Preview

pharmacology second semsester > contraceptives: > Flashcards

Flashcards in contraceptives: Deck (10):

moa of contraceptives:

1. oestrogen-> FSH inhibited-> ovarian follice supressed.
2. progestrone-> block LH-> ovulation prevention.
3. both steroids discourage endometrium implantation.


oral contraceptives can be divided into several:

1. progesterone only.
2. monophasic- estrogen and prog fixed.
3. biphasic- estrogen fixed and progestrone increased.
4. 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.



1. weight gain.
2. nausea flushing dizziness, depression.
3. acne pigmentation.
4. amenorrhea- once pills are withdrawn.
5. Thromboemboli.
6. decreased ovarian and endometrial cancer, hepatic adenoma (controversial).
7. HDL increased and decrease LDL.
8. GI- cholestasis, gallbladder disease.



cardiovascular disorders.
estrogen dependent neoplasm
vaginal bleed of unknown cause.
before epiphyseal closure---> not to be given to younglings.



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)