Contraceptives Flashcards
Estrogen MOA:
- transcription factor
- directly modifies mRNA synthesis
- influences gene transcription
Estrogen reproductive effects:
-sexulan maturation, endometrial growth, breast tissue stimulation
How does estrogen increase clotting tendency?
increases levels of vit. K
Estrogen effects on skin?
- inc. pigment
- inc. colagen/ thickness
- skin moisture
Estrogen metabolic effects:
- dec. bone resorption
- inc. HDL
- Dec. LDL
- inc. trigs
Estrogen indications:
- Contraception
- menopausal hormone replacement therapy (vasomotor symptoms or vulvovaginal atrophy)
- endometriosis tx
- dysfunctional uterine bleeding
- osteoporosis prevention
Estrogen contra:
- undiagnosed genital bleeding
- breast cancer or chance of
- DVT or PE or hx of
- clotting disorders
- liver disease
- protein C, S or antithrombin deficiency
- prego
how is progesterone metabolized?
3A4
how does progesterone interact with ketoconazole?
its inhibited by it
Progesterone warnings:
DVT, PE, CVA, AMI, dementia, breast ca.
Progesterone indications:
secondary amenorrhea, DUB, PMS, HRT, cervical ripening, Mastodynia, endometrial hyperplasia, infertility, anovulatory bleeding
First Gen Progestins:
- steroids with similar activity to progesterone
- Megestrol acetate
- medroxyprogesterone acetate (proverà)
2nd gen progestins:
- norethindrone
- ethynodial
- have some androgenic effects
3rd gen progestins
- Norgestrel, Levonorgestrel
- Desogestrel
- Norgestimate
- Dienogest
- oral or injectable
- less androgenic
non steroidal progestins:
- Derived from spironolactone
- Drospirenone
Progestins MOA:
- directly modify RNA synthesis
- influence gene transcription
reproductive effects of progestins:
- feedback loop with FSH and LH
- decline determines onset of menstruation
- changes endocervical gland secretions from watery to viscous (reducing sperm entry into uterus)
- maintains pregnancy
- mild sedative
- inc body temp with preovulatory surge
progestins metabolic effects:
- inc insulin secretion and peripheral insulin resistance
- inc lipase activity
- inc LDL, dec HDL
Indic of progestins:
- contraception
- post-menopause HRT
- dysfunctional uterine bleed
- pregnancy maintenance
progestins contra:
- DVT, PE
- severe migraine
- unexplained vag bleed
- breast Ca
- liver disease
- CV risk
Progestin ADRs:
- Acne
- hirutism
- inc LDL
- insulin resistance
- DVT (esp. 3rd gen)
- vag bleeding
- bone loss