B-24. Contraceptives. Flashcards
Oral contraceptive are usually administered how? Given in which phases?
Oral contraceptives are usually administered as a combination of estrogen and gestagen, given in phases. This can be done in a monophasic, biphasic or triphasic manner, or as a gestagen-only “minipill”.
The estrogen component of the pill is? The gestagen component is?
The estrogen component is always ethinylestradiol and the gestagen component varies.
Biphasic hormone doses different between which days of treatment
Biphasic hormone doses generally differ btwn days 1-10 and 11-21 of treatment
Triphasic hormone doses different between which days of treatment
Triphasic differs btwn days 1-7, 8-14 and 11-21.
How many days are skipped in the cycle?
1 week of the 28 day cycle is skipped to allow for menstruation (usually ‘sugar pills’ taken during this time to help pt remember to take pill daily)
Estrogen and gestagen combo effect on sex organs. MOA?
MOA: Inhibition of pituitary function (neg. feedback on FSH/LH); inhibition of ovulation; changes in cervical mucus, endometrium (inhibit implantation), motility (of Fallopian tube cilia) etc.
Effect on sexual organs (estrogen and gestagen combo)
● Depression of ovarian function - chronic use → ovaries shrink; discontinuation of drug can result in a long amenorrheic period
● Uterine / cervical effects - result in cervical hypertrophy (possibly w/ polyp formation) with thicker / less cervical mucus; 19-steroid preparations cause uterine glandular atrophy with reduced bleeding
● Breast effects - enlargement and lactation suppression
Advantageous side effects of estrogen and gestagen combo
Advantageous side effects:
● Cancer prevention - ↓ incidence of ovarian/endometrial cc. as well as ovarian cysts and mastopathy
● Menstrual effects - ↓ bleeding and anemia
● Also improve conditions such as endometriosis (gestagens ↓ endometrial prolif.) and dysmenorrhea
Adverse effects of gestagen and estrogen
Adverse effects:
● Mild - nausea, mastalgia, edema, HA (migraine incidence ↑) , endocrine changes, loss of “withdrawal bleeding” (aka hormonal period / fake period, monthly bleeding while on OCPs)
● Moderate - breakthrough bleeding, acne, weight gain / worsened lipid profile (gestagens), hyperpigmentation, hirsutism, ureteral dilation, vaginal infections (pH changes) and amenorrhea
● Severe:
○ Vascular - ↑ risk of venous thrombi (coag. factor changes), MCI and cerebrovascular disease
○ GI disorders - ↑ risk of cholestasis, gallbladder disease, and hepatic adenoma
○ Depression
○ May increase risk of cervical and breast cancers (unclear research on this)
Contraindication of gestagen and estrogen
Contraindications:
● Vascular disorders - such as thromboembolism or cerebrovascular disease
● Certain cancers - estrogen-dependent neoplasms, mostly breast cc. ● Vaginal bleeding of unknown origin
● Before closure of the epiphyseal plate - estrogens induce closure + thus would stunt growth
Progestin/gestagen-only therapy (minipill) drugs
Norethindrone
Norgestrel (minipill)
Indication and side effects of Norethindrone or norgestrel
Norethindrone or norgestrel - “minipill”
● Indication: pts in whom estrogens are CI, such as those w/ hepatic disease or thromboemboli
● Side Effects:
○ HA, dizziness, weight gain
○ Impaired glucose tolerance - CI in pts with family history of DM
○ Irregular bleeding
Parenteral depot injection drugs
Medroxyprogesterone acetate
Medroxyprogesterone acetate pharmacokinetics and side effects
Medroxyprogesterone acetate
● Given i.m. every 2-3 months
● Side Effects:
○ Common - HA, impaired glucose tolerance, irregular bleeding, worsens lipid profile
○ Long amenorrheic period after discontinuation (6-12 months)
Contraceptive patches drugs
Ethinylestradiol and norelgestromin combination
