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
Oral contraceptive Estrogens:
- Ethinyl estradiol
- Mestranol
- Estradiol valerate
Oral contraceptive Progestins:
- Medroxyprogesterone
- norethindrone
- levonorethindrone
- ethynodiol acetate
- desogestrol
- drospirenone
- norgestimate
- dienogest
Oral contraceptive estrogen MOA:
- cycle control
- contraceptive activity
- stabilize endometrium
- minimizes irregular shedding
- inhibits FSH release
- potentiates LH surge inhibition
oral contraceptive progestin MOA:
- primary contaceptive
- prevents LH surge (no ovum release)
- thickens cervical mucus
- decrease tubal motility
- thin endometrium
oral contraceptives contraindications:
- clot disorders
- diabetes
- migraine with aura
- uncontrolled HTN
- surgery with prolonged immobilization
- thrombogenic mutations
- breast Ca
- liver dz
- age 35+ and smoker
- pregnant
- breastfeeding
OC drug interactions:
- all reduce efficacy
- rifampin
- phenobarb
- carbamazepine
- phenytoin
antibiotic interactions with OC:
- tetracyclines and PCNs reduce ethanol estradiol concentration
- ampicillin may cause breakthrough bleeding
OC adverse effects:
-breakthrough bleeding
estrogen OC adverse effects:
- HA
- breast tenderness
- DVT, Clot
- nausea
progesterone androgenic OC adverse effects:
- acne
- hirsutism
Excess estrogen symptoms:
N, breast tenderness, HA, fluid rendition weight gain, dysmenorrhea , menorrhagia, uterine fibroid growth
estrogen deficiency symptoms:
-vasomotor symptoms, nervousness, decreased libido, early cycle BTB, amenorrhea
excess progestin symptoms
-inc appetite, wt. gain, bloating, constipation, depression, fatigue, irritability, acne, oily skin, hirsutism
progestin deficiency symptoms:
-dysmenorrhea, menorrhagia, late cycle BTB
Ortho evra patch
norelgestromin and ethanol estadiol
-increased clot risk over OC
patch directions
- new patch weekly x3 weeks, no patch week 4
- dont cut, dose dump
- less effective in heavier patients over 90 kg
Nuvaring
-Etonogestrel + EE
insert vaginally, 3 weeks in, 1 week off
nuvaring side effects:
irritation, infection, secretion
Progestin only pills
- norethindrone
- start any time in cycle. within first 5 days, no backup needed
- used postpartum
- ok with breast feeding
- need to take on time, within 3 hrs
Depo-provera
- medroxyprogesterone acetate injection
- long acting, no ovulation for 3 months
- repeat dose at 12 weeks
- sasfest 30 days after delivery min breast feeding women
Depo-provera ADRs
- irreg menstrual bleeding, breast tenderness, wt gain, depression
- decrease BMD (make sure pt gets calcium and vit D
implants
- etonogestrel
- reversible
impact side effects:
- irregular bleeding
- HA, vaginitis, wt gain, acne, breast and ab pain
Emergency contraceptive
- yuzpe method
- levonorgesterol
- ulipristal
- mifepristone
- Cu-IUD
- use within 5 days of unprotected intercourse
yuzpe method side affects
N, V
ulipristal acetate:
-selective progesterone modulator
ulipristal acetate MOA:
delays or inhibits ovulation
ulipristal ADRs:
HA, N, ab pain, dysmenorrhea, fatigue, dizziness, acne
Levonorgestrel MOA:
- inhibits/delays ovulation
- prevents fertilization
levonorgestrel side effects:
-irregular menses, N, ab pain, fatigue, dizziness, breast tenderness
what do you have tom do before emergency contraception?
prego test
Mifepristone MOA:
progesterone and cortisol receptor antagonist
- abortion pill
- watch for sepsis
how is mifepristone metabolized
p450
