Contraceptives Flashcards
what are the two types of estrogen that are seen in oral contraceptives and mention their activity
- ethinyl estradiol: pharmacologically active
- mestranol: converted by the liver to ethinyl estradiol
what are the progestins in oral contraceptives
LMNNNDD
Levonorgestrel Medroxyprogesterone Norethindrone Norgestimate Norgestrel Desogestrel Drospirenone
how do the progestins in OC differ
- based on their androgenic activity
- Levonorgestrel and Norgestrel have the highest androgenic activity
- Desogestrel and Norgestimate have lower androgenic activity
- Drospirenone has anti androgenic effect
what is the combined oral contraceptive most commonly used today and what does it contain
“low dose” combined oral contraceptive and it contains 35 microgram of ethinyl estradiol or less
what do most formulation of OC have
21 hormonally active pills followed by 7 placebo pills to allow for withdrawal bleeding
mechanism of combined oral contraceptive
- prevents ovulation by suppressing LH and FSH release
- progestin thickens cervical mucus so sperm cannot penetrate
- induces changes in endometrium so that implantation is unlikely
when can women start taking OC and be immediately protected
- anywhere from Day 1 to 5 of her period –> immediate protection unless cycle is less than 23 days
- if that’s the case then must be taking pill for at least 7 days for protection to begin
non contraceptive benefits of OC
- reduction in endometrial cancer risk
- reduction in ovarian cancer risk
- regulation of menses
- prevent ovarian cysts
- relief of benign breast cancer
- reduced risk for symptomatic PID
- improve acne control
AE of OC and how it can be avoided
BHAIM
Breakthrough Bleeding (most common) Hirsutism Amenorrhea Insulin Resistance (progestin competes for its receptors) Melasma (brown gray patches on face)
adjust estrogen/progestin content of OC
the AE hirsutism is associated with which contraceptives
those with androgenic properties so main ones – Levonorgestrel and Norgestrel
most serious AE of OC though very rare
cardiovascular disorders such as thromboembolism, hypertension etc
what drugs taken concomitantly with OC can cause OC failure and why
CYP450 inducer such as RIFAMPIN, Carbamazepine, Oxycarbazepine, Phenytoin, Phenobarbitol, Topiramate, and St. John’s Wort
-the increase the metabolism of estrogen hence failure of the OC
how does Rifampin as an antibiotic affect circulating estrogen (other than being a CYP450 inducer)
decreases intestinal bacteria needed to hydrolyze ethinyl estradiol –> its reabsorption as an active drug
absolute contraindications of OC
- Pregnancy
- Thromboembolic or Thrombophlebitis disorder
- Breast Cancer
- Undiagnosed abnormal vaginal bleeding
- Stroke or CAD
- Estrogen Dependent Cancer
- Tumor of liver
- Migraine with aura
- DM with vascular disease
- Uncontrolled hypertension
- Older than 35 and smoke heavily
- Surgery requiring prolonged immobility
- Active hepatitis
what is given to women who can’t take estrogen containing OC and give example
progestin-only contraceptives called minipills –> norethindrone or norgestrel
disadvantage of taking mini pills (name them)
norethindrone or norgestrel
they are less effective and must be taken at same time every day
who is most likely to take progestin only OC (name them)
norethindrone or norgestrel
- if increased risk of thromboembolic event
- over 35 and smoke
mechanism of progestin only OC (name what they contain)
norethindrone or norgestrel
- thickening of cervical mucus –> sperm cant penetrate
- endometrial alteration –> impair implantatio
when can woman take progestin only OC and be immediately protected
Day 1-5 of period unless cycle 23 days or less –> must then take pill for at least two days before protection (compare to estrogen OC where must take 7 days)
what does the contraceptive patch and ring contain
ethinyl estradiol and a progestin
what is Depo-provera and its main mechanism
progestin only injectable contraceptive that contains depot medroxyprogesterone acetate (DMPA) –> high enough progesterone that it causes negative feedback
AE of depo provera
significant loss of bone mineral density
what is subdermal progestin implant
implant containing only progestin that is placed just under the skin of upper arm and is effective for 3 years
what is intrauterine systems
contraceptive that contains levonorgestrel and lasts for 5 years
what can diaphragm and cervical caps lead to if left longer than 24-48 hours
toxic shock syndrome
used together with spermicides to prevent pregnancy
what is the name of the spermicide
nonoxynol-9
what is Plan B and One choice
used after unprotected sex to prevent pregnancy
-contain levonorgestrel: 1st taken within 72 hours and next 12 hours later
available over the counter for those 17 and older
what is Ella
tablet taken within 5 days of unprotected sex to prevent pregnancy
-contains Ulipristal acetate, progesterone antagonist, to inhibit or delay ovulation
