contraception drugs – Flashcards
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the last step is ________?It develops______?
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Cytokinesis,two daughter cells
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What estrogen is used in all COCs
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(+what kind of estrogen is it) Ethinyl estradiol, which is a synthetic estrogen
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What form of progestin is used in COCs
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(that includes: 5 divided in 4 categories Synthetic: 1st gen - Estranes: norethinedrone, 2nd gen – Gonanes: levonorgestrel, 3rd gen – Gonanes w/o Andro : Desogestrel & Norgestimate, 4th gen – Spironolactone derivative w/ anti-andro and minero: Drosperin
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What is diethylstilbestrol
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(+kind of compound) A drug not used anymore that “prevents” miscarriage. Stopped cause it also causes cancer and infertility in offspring. Diethylstilbestrol is a non-steroidal estogen
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What is medroxyprogesterone
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(2 uses, kind of compound) Used in both hormonal replacement and depot (IM long-term release) contraception. It is a chemically modified progestin
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COC are made of
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(2, general) 1.Synthetic estrogen (ethinyl estradiol), 2.Synthetic progestin
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HRT are made of
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(2~3) 1.Conjugated Equine Estrogen (equilin sulfate, estrone sulfate), 2.Chemically modified progestin (medroxyprogesterone)
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What phase of the menstrual cycle are COC trying to mimic
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Luteal phase
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Why are COC trying to mimic the luteal phase
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Luteal phase has high E and high P, which prevents the release of GnRH, LH and FSH
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By preventing the surge in LH and FSH (especially LH) of the luteal phase, COC prevent:
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Ovulation
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What predominates in COC: E or P
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(be precise) P which is in mg, E is in µg
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Which of E or P has much more complicated interaction in the body
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(explain 4 things) E only binds ER. P binds PRs but also to a lesser degree AR (androgen), ER, GR (glucocorticoid). Furthermore PR are dependent on some E.
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What is one explanation for P to be so promiscuous with other receptors
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P is a the beginning of the pathways to make E (estradiol), A (testosterone), and G (cortisol)
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What are the effects of estrogen on the body
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(9) 1.secondary sex, 2.ovulatory cycle, 3.pregnancy, 4.increase thrombosis, 5.hypertension (increase Na retention), 6.Increase TGs, HDL, decrease LDL (no net effect), Stimulate cell proliferation: 7.breast cancer, 8.uterine (endometrial) cancer, 9.vasodi
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What are the effects of progestin on the body
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(2) 1.booby development, 2.maintains pregnancy (w/o P: lining softens like at the end of menstrual cycle)
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The increase in thrombosis w/ E can lead to
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(1~2) DVT then PE
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Discuss the potency of the different types of E
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(3) Synthetic > Conjugate Equine > Natural
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Discuss the absorption of E
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Good/rapid
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Why aren’t natural E not used in COC or HRT (2)
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1st pass effect is huge (has to be IV) + short T1/2
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What is the only pharmacokinetic difference btw conjugated equine and synthetic
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Synthetic have even longer T1/2 (they both have low first pass effect and can be taken orally)
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Discuss the metabolism of estrogen (5)
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Mostly in the liver: 1.-OH by P450, 2.conjugated to glucoronide, 3.E-glucoronide is extred in bile, 4.cleaved by bacteria back to E, 5.reabsorbed - remember this is called enterohepatic circulation
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How can antibiotics use prevent the proper functioning of contraceptive
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Block bacteria cleaving of E-glucoronide, thus E is excreted and you get lower serum levels
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What other drug greatly influence E levels
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Dilantin (in epileptic patients) activates Cyp 3A4, and thus decrease E levels
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What has been the trend in the past 50 years in terms of COCs (2)
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Decrease the amounts, and use mutliphasic COCs
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What was the 1st generation of COCs problem
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Blood clots
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What was the 2nd generation’s COCs name + 2 problems
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Sequential. They did not work well (too little P), and caused endometrial cancer
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What was the 3rd gen’s COCs name
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Lo-dose
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What is the current 4st gen COCs
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Multiphasic (to lower P levels)
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What are OCs with only P called (2)
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POPs or minipills
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What is the dosing range of E in COCs
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20 to 50 ?g
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Name the P used in COCs in order of potency (4, don’t include drosperinone)
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LNG > DSG > NGM > NE
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What is the advantage of triphasics
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15% less exposure to P
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When are monophasics preferred (2)
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1.late-cycle bleeding (need more progestin), 2.mood-swings on tri-cyclics
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Usually COCs are started with average amounts on E (30?g), when is this not the case
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Fat women probably need more E
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What is the usually cycle of monophasic COCs, in terms of taking the pill
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21 days on, 7 days off
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What is the point of starting the pill of Sunday
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No periods during the weekends
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What are the 3 ways to start the pill
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1.Day 1 start (1st pill on 1st day of period), 2.Sunday Start, 3.Quick start (in doctor’s office)
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What is the advantage of Day 1 start
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You don’t need to use backup contraception for any time (you need 1 week for Sunday Start and Quick Start)
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What should do if they missed one pill
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Take two the next day
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What should one do if they missed 2 pills
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If week one or two: take two pill, then two pill again the next day. Supplement with a week of backup. If week three: start new pack (+ one week backup)
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What P is used in POP (2)
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Norethindrone or norgestrel
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What doses are used in POP
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The lowest needed for efficacy
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What is very important with taking POP
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You need to take it at the same exact time very day.
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What is a very common time in a women life, when she would be told to use a POP
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Lactating mother, the E in COCs can lead to vaginal bleeding in girls and gynecomastia in males
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Other than POP (minipills) what are other P only contraceptions (3) (+ duration of each + P used in each)
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1. Depot shot (IM, medroxyprogesterone) – 3 months, 2. Implanon (subdermal implant, etonorgestrel) – 3 years, 3. IUD (levonorgestrel) – 5 years
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What are the AE of P only OC (5 + 3 specific to one kind)
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1.higher failure, 2.irregular bleeding, 3.some women get amenorrhea (think they are pregnant), 4.acne (P activates AR), 5.depression, Depo-provera also has: 1.bone loss, 2.weight gain, 3.return to fertility delayed
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How do COC and P-only prevent pregnancy (3)
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1.inhibit ovulation by inhibiting LH and FSH level, 2.they thicken the mucosa (physical barrier to sperms), 3.they alter the mucosal lining (sperm can’t stick)
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How many COCs can you miss before being at risk
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More than 2 and you are at risk
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How many P-only can you miss before being at risk
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Only be 3 hours late and you are at risk
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Other than preventing pregnancies what are the other benefits of COCs
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(5~6) 1.decrease ovarian cancer, 2.decrease endometrial cancer (thx to P, E does increase), 3.decrease fibrocystic disease/fibroadenomas, 4.decrease PID (blocks sperm and infections from sticking and passing through), 5.lower blood loss during menses, ~6
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What is the greatest AE of COCs (think back about the AE of E & P) (+ thus who should not get COCs)
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Thrombosis, thus be careful or do not use in women older than 35 and smokers (this is due to Estrogen)
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Other than thrombosis the main AE of COCs are: (5 for E, 3 for P – include name of drug for P)
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Estrogen: 1.breast cancer, 2.hypertension (temporary), 3.gall bladder disease (stones, E increases stasis), 4.CVD/stroke, 5.cervical dysplasia/cancer Progesterone: 1.change HDL/LD
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When is the increase in risk for breast cancer the highest when talking COCs
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If taken before 1st pregnancy (remember: lifetime exposure to E is the reason for breast cancer)
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What drug is linked to increase CVD/stroke risk in women taking COCs
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Levonorgestrel
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What two thinks correlate strongly with cervical cancer
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Smoking, HPV
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What are the mild AE of COCs (1 for E, 2 for P)
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Estrogen: fluid retention (due to Na retention effect), Progesterone: acne/weight gain (androgen effects
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Separate the bleeding cause by E deficiency and P deficiency:
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E deficiency: early bleeding, P deficiency: late bleeding
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What are the contraindication for COCs, (10) which ones can be fixed by using P-only (8)
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1.Hx of clots, 2.>35+smoke, 3.Hx of stroke/MI/CVD, 4.Hypertension, 5.Migraines, 6.Has to go through surgery (clots), 7.Lactating/had pregnancy, 8.high TGs, 9.has hormone sensitive cancer, 10.predispose for booby cancer
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What is newer about Yasmin/Yaz (include 1 AE, and 1 advantage)
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P is drospirenone, which is antimineralcorticoid thus less fluid retention. However K can become high.
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Difference btw Yasmin and Yaz
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Yaz is 24/4 schedule thus shorter period and thus less PMDD and less Acne
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Describe orthe-evra (+ 1 contraindication + 1 AE)
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It is patch (21/7). Does not work as well in heavy women, increase risk for clots.
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Describe nuvaring
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Ring (21/7)
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What is the morning after pill (also called) (what is the timeline)
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2 pills containing High dose levo, also called Plan B. you have 72hrs after event (this is not an abortion pill, no ovulation, no implementation)
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What is RU-486 (also called) (timeline)
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Mifepristone, you have 49 days
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What are the two extended cycle COCs, what is their 2 uses
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Seasonale and lybrel: prevent painful periods/excessive bleeding as well as PMDD
