Contraceptives Flashcards
what are 3 different options of contraceptives?
pill, patch, vaginal ring
what is combined oral contraceptives (COCs)?
combo of estrogen and progesterone - closely mimic the menstrual cycle and provide predictable monthly bleeding
what are other advantage of COCs?
treat acne, hirsutism (abnormal hair growth), dysmenorrhea (painful menstruation), menorrhagia (heavy menstrual bleeding), endometriosis
what is the effectivenss of COC?
prevent 99%; all agents in this class equally efficacious
what is endometriosis?
endometrial tissue (the tissue that lines the uterus) grows on the outside of the uterus in other areas of the body such as the abdomen, the outer surface of the uterus, etc.
can lead to severe pelvin pain and COCs can help treat this condition by slowing the growth of the endometrial issue
what are the most commonly used estrogen component in COCs?
dose?
ethinyl estradiol;
10-50 mcg daily, but most patients take low-dose formulations (<35 mcg/day)
what is another type of estrogen found in COC than ethinyl estradiol?
- estradiol valerate; this is converted to the naturally occurring estrogen, estradiol - hoping to reduce the incidence of adverse effects but no evidence that this is the case
- estetrol - available in combo with drospirenone - plant-derived estrogen that could have less impact on certain tissues (e.g. breast) or metabolic changes (e.g. lipids) but no evidence that estetrol reduces the risks seen with estrogens (e.g. breast cancer, blood clots, etc.)
what are the progestins in COCs - first generation?
Norethindrone
Norethindrone acetate
Ethynodiol diacetate
what are the progestins in COCs - second generation?
Norgestrel
Levonorgestrel
what are the progestins in COCs - third generation?
Norgestimate
Desogestrel
what are the progestins in COCs - Other generation?
drospirenon
dienogest
segesterone
The different progestins all have a high affinity for the progesterone receptors, but differ in ?
their affinity for other receptors such as androgen and glucocorticoid receptors;
The contraceptive effects of the various synthetic progestins are mediated by the progestin’s activity on progesterone
receptors in the reproductive tissue, while the side effects are often due to the progestin’s activity on other receptors.
what are the first generation progestins have affinity for in addition to progesterone receptors?
androgen receptors;
what is the difference between 1st and 2nd gen progestins?
1st gen bind with lower affinity to progesterone and androgen receptors when compared to second-generation progestins.
2nd gen cause less breakthrough bleeding and spotting because they have a higher affinity for progesterone receptors;
2nd gen progestins bind with higher affinity to androgen receptors than other progestins, they have more androgenic effects which can cause acne, abnormal hair growth (hirsutism), dyslipidemia, and weight gain.
what is the difference of 3rd gen and other gen?
Third-generation progestins don’t have much
activity on the androgen receptors and may be associated with fewer androgenic side effects.
what is the difference of other newer progestins , such as drospirenone and dienogest?
Other newer progestins, such as drospirenone and dienogest, have been designed to bind primarily to progesterone receptors with little to no affinity for other steroid receptors. They have antimineralocorticoid and antiandrogenic effects.
what is the major but rare adverse effect associated with COCs?
venous thromboembolism (VTE)
what is the risk of clotting thought to be caused by?
the effect of estrogen on the coagulation cascade
who is at higher risk for VTE with COC use?
smoker, older age, obese
how to reduce the risk of VTE?
use lowest effective and tolerated dose of estrogen - Generally, a patient shouldn’t need a product with more than 30 mcg of ethinyl estradiol.
which progestins have also been associated with a possible increased risk of VTE?
The newer progestins (desogestrel, norgestimate), compared to the older progestins (levonorgestrel);
BUT, This risk is only an association. A meta-analysis of eight observational studies of various progestin-only contraception showed that it was
not associated with an increased risk of VTE. The use of progestins is considered medically acceptable in patients at risk of thrombosis.
in a patient complaining of excessive breast tenderness, what COCs do you switch to?
a COC with less estrogen can be considered
if you have too much estrogen, what are the symptoms?
nausea, breast tenderness, headache, bloating, increased blood pressure, melasma (grey-brown patchees on the face)
if you have too little estrogen, what are the symptoms?
spotting, breakthrough bleeding early/mid-cycle
if you have too much progestin, what are the symptoms?
Breast tenderness, headache,
fatigue, mood changes
if you have too little progestin, what are the symptoms?
Breakthrough bleeding late cycle
if you have too much androgen, what are the symptoms?
Weight gain, acne, hirsutism, ↑ low
density lipoprotein (LDL), ↓ high
density lipoprotein (HDL)
within the COC category, there are 6 formulations, what are they?
monophasic, biphasic, triphasic, and quadriphasic formulations,
as well as extended- and continuous-cycle formulations
what is monophasic (one phase) COC?
the most common and contain
the same amounts of estrogen and progestin for 21 days, typically followed by a seven-day hormone-free interval
(unless it’s an extended-cycle regimen)
why were Multiphasic pills developed?
what are disadvantages?
in an attempt to better mimic the levels of estrogen and progesterone during the menstrual cycle.
However, these pills don’t necessarily decrease side effects. They also may be more confusing to use when handling a missed dose compared to
monophasic products
what does Extended-cycle regimens provide?
more days of hormones, with some products providing up to 84 days of hormone
containing pills followed by a seven-day hormone-free interval.
Continuous-cycle regimens?
taking hormone
containing pills daily throughout the year, with no hormone-free interval.
Both extended- and continuous-cycle COCs
are useful for patients with ?
menstrual-related symptoms or those who prefer not to have monthly bleeding;
These regimens can reduce symptoms of hormone withdrawal, dysmenorrhea, heavy bleeding, and help with severe
premenstrual symptoms.
Continuous-cycle contraception can be safe and effective. It does not have a significantly different risk of venous
thromboembolism compared to traditional cyclic use.
Keep in mind that to avoid monthly bleeding, patients can also use traditional monophasic
COCs by continuing to take active pills throughout the hormone-free interval. This may be a more cost-effective
approach.
when do you select ethniyl estradoil 20mcg + [levonorgestrel 0.1mg (Alesse) / norethindrone acetate 1mg / drospirenon 3mg (Yaz)?
Ethinyl estradiol 20 mcg monophasic
regimens are a good starting dose for
patients who want to use a COC.
May cause more breakthrough bleeding
than higher doses of ethinyl estradiol in
some patients.
when do you select ethniyl estradoil 30mcg + [levonorgestrel 0.15mg (Min-Ovral) / norethindrone acetate 1.5mg / norgestrel 0.3mg / desogestrel 0.15mg (Marvelon)/ drospirenone 3mg (Yasmin)]?
Consider higher doses of estrogen (30 mcg
of ethinyl estradiol or more) for patients
taking CYP3A4 enzyme inducers.
May be useful for patients who experience
bothersome breakthrough bleeding on
lower doses of ethinyl estradiol.
Consider avoiding levonorgestrel and
norgestrel products for patients concerned
with gaining weight.
Some products, such as Safyral and
Tydemy, contain folate in addition to
ethinyl estradiol and drospirenone; it may
be cheaper for patients to take a different
COC and add folate supplementation.
when do you select ethniyl estradoil 35mcg + [ethynodiol diacetate 1mg / norgestimate 0.25mg / norethindrone 0.4mg / norethindrone 0.5mg (Brevicon 0.5/35) / norethindrone 1mg (Brevicon 1/35)]?
Consider higher doses of estrogen (30 mcg
of ethinyl estradiol or more) for patients
taking CYP3A4 enzyme inducers.
May be useful for patients who experience
bothersome breakthrough bleeding on
lower doses of ethinyl estradiol.
when do you select ethniyl estradoil 50mg + ethynodiol diacetate 1mg ?
Consider higher doses of estrogen (30 mcg
of ethinyl estradiol or more) for patients
taking CYP3A4 enzyme inducers.
Avoid in obese patients and smokers.
what are multiphasic COCs available?
ethyinyl estradiol 10 and 20mcg + desogenstrel 0.15mg
ethinyl estradiol 35mcg + norethindrone acetate 0.5-1mg (Synphasic) / norgestimate 0.18 - 0.25mg (Tri-Cyclen)
ethinyl estradiol 20-35mcg + norethindrone acetate 1mg
ethinyl estradiol 25mcg + norgestimate 0.18-0.25mg (Tri-Cyclen Lo) / desogestrel 0.1-0.15mg (Linessa)
ethinyl estradiol 30-40mcg + levonorgestrel 0.05-0.125mg (Triquilar)
estradiol valerate 1-3mg + dienogest 2-3mg
what is the product selection consideration for multiphasic COC regimens?
Multiphasic COCs haven’t
been found to be better at
preventing side effects than
monophasic pills.
Patients interested in COCs
should be initiated on
monophasic pills due to more
safety data and easier
instructions if a dose is missed