GENERIC NAME(S): Cyclessa-Ethinyl Estradiol
OTHER NAME(S): Cyclessa-Ethinyl Estradiol Tablet
Do not use this medication if you smoke cigarettes/use tobacco and are over 35 years old. Smoking raises your risk of stroke, heart attack, blood clots, and high blood pressure from hormonal birth control (such as the pill, patch, ring). The risk of these serious problems increases with age and with the number of cigarettes you smoke. Do not smoke or use tobacco.
This combination hormone medication is used to prevent pregnancy. It contains 2 hormones: a progestin and an estrogen. It works mainly by preventing the release of an egg (ovulation) during your menstrual cycle. It also makes vaginal fluid thicker to help prevent sperm from reaching an egg (fertilization) and changes the lining of the uterus (womb) to prevent attachment of a fertilized egg. If a fertilized egg does not attach to the uterus, it passes out of the body.
Besides preventing pregnancy, birth control pills may make your periods more regular, decrease blood loss and painful periods, decrease your risk of ovarian cysts, and also treat acne.
Using this medication does not protect you or your partner against sexually transmitted diseases (such as HIV, gonorrhea, chlamydia).
Diet, Oral Contraceptives, and Cardiovascular Disease
The RCGP study was among the first to show that the risk of cardiovascular disease among pill users is concentrated mainly in users who smoke, especially in older women. The study was also the first to demonstrate a link between the risk of hypertension or arterial disease and the progestogen content of the pill. Most excess cardiovascular disease among users of OCs is due to thrombosis (not atherosclerosis); studies indicate that the lower the OC estrogen dose, the lower this risk. OCs containing the third-generation progestins Cyclessa and gestodene have been associated with greater risks of venous thromboembolism than are associated with older progestins, although there is some controversy surrounding these findings.
OC users have lower dietary carotenoid intakes than nonusers. Since OC users smoke and drink more than nonusers, and both factors are associated with lower carotenoid intakes, OC users form a potential high-risk group for disease.
Conflicting reports regarding the possible effect of OCs on folate status prompted researchers to evaluate the relationship between dietary folate intake and the concentration of folate in serum and erythrocytes among users and nonusers of OCs. The authors concluded that the use of OCs produces significantly lower serum folate levels during the first week of the menstrual cycle in spite of adequate folate intake.
Recent epidemiologic studies have shown an increased mortality from cardiovascular diseases in people with higher serum copper levels. Even though a higher serum copper concentration in women using OCs is well known, there is still uncertainty about the influence of newer progestin compounds in OCs on serum copper concentration. This issue is of particular interest in the light of recent findings of an increased risk of venous thromboembolism in users of OCs containing newer progestins like Cyclessa compared to users of other OCs. While an elevated serum copper concentration was found in users of all types of OCs, the elevation was more pronounced among women taking OCs with antiandrogen effective progestins such as third-generation OCs containing Cyclessa. Further investigation is required to shed light on the possible role of high serum copper concentration in increasing the cardiovascular or thrombotic risk of women using OCs.
DESOGEN® Tablets (Cyclessa and ethinyl estradiol tablets USP) is indicated for the prevention of pregnancy in women who elect to use this product as a method of contraception.
Interactions between Cyclessa/ethinyl estradiol and other drugs have been reported in the literature (see PRECAUTIONS).
Contraceptive Vaginal Ring
The vaginal mucosa offers excellent absorption of sex steroids. The only contraceptive vaginal ring available in the United States is the NuvaRing, a flexible plastic ring that is 4 mm thick and has an outside diameter of 54 mm. 77 The ring releases 15 µg daily of ethinyl estradiol along with etonogestrel, the biologically active metabolite of the progestin Cyclessa ( Fig. 18-3 ). The ring does not require individual fitting; as long as it remains in the vagina, appropriate absorption of steroids occurs. Expulsion is uncommon. Women's interest in using a contraceptive vaginal ring varies; some women are highly motivated and comfortable with this method. Some users keep the ring in place during sexual relations; in this setting, male discomfort is not common. Other users prefer to remove the ring before intercourse, and removal for less than 48 hours does not appear to impair efficacy. 9 Backup contraception is required for 7 days if the ring is removed for 48 hours or longer.
Oral contraceptives should not be used in women who currently have the following conditions:
- Thrombophlebitis or thromboembolic disorders
- A past history of deep vein thrombophlebitis or thromboembolic disorders
- Cerebral vascular or coronary artery disease (current or history)
- Valvular heart disease with thrombogenic complications
- Inherited or acquired hypercoagulopathies
- Severe hypertension
- Diabetes with vascular involvement
- Headaches with focal neurological symptoms
- Major surgery with prolonged immobilization
- Known or suspected carcinoma of the breast (or personal history of breast cancer)
- Carcinoma of the endometrium or other known or suspected estrogen-dependent neoplasia
- Undiagnosed abnormal genital bleeding
- Cholestatic jaundice of pregnancy or jaundice with prior hormonal contraceptive use
- Hepatic tumors (benign or malignant) or active liver disease
- Known or suspected pregnancy
- Smoke, if over age 35 (see BOXED WARNING and WARNINGS)
- Hypersensitivity to any of the components of DESOGEN® Tablets (Cyclessa and ethinyl estradiol tablets USP)
- Receiving Hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, due to the potential for ALT elevations (see WARNINGS, Risk Of Liver Enzyme Elevations With Concomitant Hepatitis C Treatment).
There is no information to determine the effect of race on the pharmacokinetics of DESOGEN® Tablets (Cyclessa and ethinyl estradiol tablets USP).
What are some things I need to know or do while I take Ethinyl Estradiol and Cyclessa?
- Tell all of your health care providers that you take ethinyl estradiol and Cyclessa. This includes your doctors, nurses, pharmacists, and dentists. This medicine may need to be stopped before certain types of surgery as your doctor has told you. If ethinyl estradiol and Cyclessa is stopped, your doctor will tell you when to start taking ethinyl estradiol and Cyclessa again after your surgery or procedure.
- This medicine may raise the chance of blood clots, a stroke, or a heart attack. Talk with the doctor.
- Talk with your doctor if you will need to be still for long periods of time like long trips, bedrest after surgery, or illness. Not moving for long periods may raise your chance of blood clots.
- If you have high blood sugar (diabetes), talk with your doctor. This medicine may raise blood sugar.
- Check your blood sugar as you have been told by your doctor.
- High blood pressure has happened with drugs like this one. Have your blood pressure checked as you have been told by your doctor.
- Have blood work checked as you have been told by the doctor. Talk with the doctor.
- Be sure to have regular breast exams and gynecology check-ups. You will also need to do breast self-exams as you have been told.
- If you drink grapefruit juice or eat grapefruit often, talk with your doctor.
- This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take ethinyl estradiol and Cyclessa.
- Certain drugs, herbal products, or health problems could cause ethinyl estradiol and Cyclessa to not work as well. Be sure your doctor knows about all of your drugs and health problems.
- This medicine does not stop the spread of diseases like HIV or hepatitis that are passed through blood or having sex. Do not have any kind of sex without using a latex or polyurethane condom. Do not share needles or other things like toothbrushes or razors.
- If you are allergic to tartrazine, talk with your doctor. Some products have tartrazine.
- Do not use in children who have not had their first menstrual period.
- If you have any signs of pregnancy or if you have a positive pregnancy test, call your doctor right away.
💡Key facts about Cerazette
- Cerazette is a brand name for Cyclessa 75 microgram tablets.
- It can be taken by most women, including breastfeeding mothers, heavy smokers and those with high blood pressure, migraine or a risk of blood clots.
- Cerazette is 99% effective when taken correctly, but missing pills, vomiting, diarrhoea and taking certain other medicines can make it less effective. See below.
- One Cerazette tablet should be taken every day, at the same time each day. With this type of pill you don't have a break between packs.
- If you're more than 12 hours late taking a pill you won't be protected against pregnancy and you'll need to use condoms for the next two days. See below.
- Cerazette won't protect you against sexually transmitted infections; you'll still need to use condoms for that.
- The most common s >It's worth noting that the advice below may differ from that in the leaflet you get with your pills, which tends to err on the side of caution. Our information and advice is the same as that given by the NHS and the Faculty of Sexual Health and Reproductive Healthcare UK, and is based on systematic reviews of the currently available evidence. If you are concerned or have any questions, talk to your doctor, nurse, pharmacist or local family planning centre.
Drospirenone is the only progestin derived from 17a-spironolactone. It helps suppress the secretion of the hormones that regulate the body's water and electrolytes. It also has low androgenic activity. Drospirenone and estrogen seem to lessen symptoms associated with mild PMS (increased appetite, negative mood, and water retention). Drospirenone may cause higher potassium levels, so women with kidney, liver, or adrenal disease should not use it.
The brands YAZ and Beyaz have 24 days of active pills and four days of placebo pills. This combination may cause fewer hormone fluctuations than typical pill packs. YAZ has also been FDA-approved to help treat a premenstrual dysphoric disorder.
Drospirenone has been linked to an increased risk of blood clots in several studies. A 2017 review looked at 17 studies that found the risk of blood clots ranged from no increase to a 3.3 times increased risk of blood clots in comparison to levonorgestrel (the birth control pill thought to have the lowest risk). The conclusion was that based on the best studies, the risk is only slightly increased.
Looked in another way, however, some of the same researchers looked at the risk of blood clots in first-time users and restarters of oral contraceptives in over 55,000 women in another 2017 study. They found that the risk of blood clots was 3.19 times higher with drospirenone that with levonorgestrel for first-time users and 1.96 times higher in restarters.
Given this risk, women who have other risk factors for blood clots may wish to consider a birth control pill other than those with drospirenone or Cyclessa, or another form of birth control altogether.
Advantages: May help reduce PMS symptoms (PMDD) and acne
Disadvantages: Increased risk of blood clots; Increased serum potassium levels
Examples: YAZ and Beyaz; Yasmin; Zarah; Loryna; Syeda; Gianvi; Ocella; Vestura; Nikki
The use of DESOGEN® Tablets (Cyclessa and ethinyl estradiol tablets USP) for contraception may be initiated 4 to 6 weeks postpartum in women who elect not to breast-feed. When the tablets are administered during the postpartum period, the increased risk of thromboembolic disease associated with the postpartum period must be considered (see CONTRAINDICATIONS and WARNINGS concerning Thromboembolic Disorders. See also PRECAUTIONS for Nursing Mothers).
If the patient starts on DESOGEN® postpartum, and has not yet had a period, she should be instructed to use another method of contraception until a white tablet has been taken daily for 7 consecutive days.
How to use Cyclessa-Ethinyl Estradiol
Read the Patient Information Leaflet provided by your pharmacist before you start using this product and each time you get a refill. The leaflet contains very important information on when to take your pills and what to do if you miss a dose. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth as directed by your doctor, usually once daily. Pick a time of day that is easy for you to remember, and take your pill at the same time each day.
It is very important to continue taking this medication exactly as prescribed by your doctor. With certain brands of birth control pills, the amount of estrogen and progestin in each active tablet will vary at different times in the cycle. Therefore, it is very important that you follow the package instructions to find the first tablet, start with the first tablet in the pack, and take them in the correct order. Do not skip any doses. Pregnancy is more likely if you miss pills, start a new pack late, or take your pill at a different time of the day than usual.
Vomiting or diarrhea can prevent your birth control pills from working well. If you have vomiting or diarrhea, you may need to use a back-up birth control method (such as condoms, spermicide). Follow the directions in the Patient Information Leaflet and check with your doctor or pharmacist for more details.
Taking this medication after your evening meal or at bedtime may help if you have stomach upset or nausea with the medication. You may choose to take this medication at another time of day that is easier for you to remember. No matter what dosing schedule you use, it is very important that you take this medication at the same time each day, 24 hours apart. Ask your doctor or pharmacist if you have any questions.
Your pill pack contains 21 pills with active medication. It may also contain 7 reminder pills with no medication. Take one active pill (with hormones) once daily for 21 days in a row. If you are using a product with 28 tablets, take an inactive pill once daily for 7 days in a row after you have taken the last active pill unless otherwise directed by your doctor. If you are using a product with 21 tablets, do not take any tablets for 7 days unless otherwise directed by your doctor. You should have your period during the fourth week of the cycle. After you have taken the last inactive tablet in the pack or gone 7 days without taking an active tablet, start a new pack the next day whether or not you have your period. If you do not get your period, consult your doctor.
If this is the first time you are using this medication and you are not switching from another form of hormonal birth control (such as patch, other birth control pills), take the first tablet in the pack on the first Sunday following the beginning of your menstrual period or on the first day of your period. If your period begins on a Sunday, begin taking this medication on that day. For the first cycle of use only, use an additional form of non-hormonal birth control (such as condoms, spermicide) for the first 7 days to prevent pregnancy until the medication has enough time to work. If you start on the first day of your period, you do not need to use back-up birth control the first week.
Ask your doctor or pharmacist about how to switch from other forms of hormonal birth control (such as patch, other birth control pills) to this product. If any information is unclear, consult the Patient Information Leaflet or your doctor or pharmacist.
A 21-year-old female presented with 4-day history of right brow pain exacerbated by eye movement and 3-day history of blurring of the right temporal field of vision. The patient was taking Cyclessa 75 mg and cyproterone acetate 50 mg, an ADT, for 2 months for hormone imbalance. The patient displayed signs of hirsutism and acne and was overweight. Laboratory workup was unremarkable and Goldmann perimetry showed right enlarged blind spot with temporal visual loss. Discontinuation of antiandrogen therapy led to resolution in eye pain and improved visual acuity within 3 weeks. There was a temporal correlation between discontinuation of antiandrogen therapy and improvement in visual symptoms. This was one of few cases demonstrating ocular side effects of cyproterone. A possible hypothesis of isolated optic neuropathy is lower systemic levels of testosterone or estrogen .
Cyclessa is rapidly and completely metabolized by hydroxylation in the intestinal mucosa and on first pass through the liver to etonogestrel. In vitro data suggest an important role for the cytochrome P450 CYP2C9 in the bioactivation of Cyclessa. Further metabolism of etonogestrel into 6β-hydroxy, etonogestrel and 6β13-ethyl-dihydroxylated metabolites as major metabolites is catalyzed by CYP3A4. Other metabolites (i.e., 3α-OH-Cyclessa, 3β-OH-Cyclessa, and 3α-OH-5α-H- Cyclessa) also have been identified and these metabolites may undergo glucuronide and sulfate conjugation.
Ethinyl estradiol is subject to a significant degree of presystemic conjugation (phase II metabolism). Ethinyl estradiol, escaping gut wall conjugation, undergoes phase I metabolism and hepatic conjugation (phase II metabolism). Major phase I metabolites are 2-OH-ethinyl estradiol and 2-methoxy-ethinyl estradiol. Sulfate and glucuronide conjugates of both ethinyl estradiol and phase I metabolites, which are excreted in bile, can undergo enterohepatic circulation.
Cyclessa is a third-generation progestin with high progestational selectivity, minimizing androgenic effects and estrogenic activity. It shows a lower negative impact on metabolism, weight gain, acne, and other side effects typical of older progestins. It shows positive effects on lipoproteins as seen by a slight rise of HDL cholesterol.
Clinical trials show a possibly higher risk of non-fatal venous thrombosis (blood clots) with Cyclessa pills versus those with levonorgestrel. Mircette (a low-dose estrogen/Cyclessa pill) provides a shorter placebo interval, which may be helpful for women who have migraines, dysmenorrhea, or other negative issues during that week. A low estrogen/varying Cyclessa triphasic pill, Cyclessa, is also available.
Along with drospirenone, Cyclessa appears to have a higher risk of blood clots than other options, especially levonorgestrel, with the highest risk of all combination birth control pills being Cyclessa combined with 30 to 40 micrograms of ethinyl estradiol (see 2017 study below under Cyclessa).
Advantages: May help with menstrual cramps; Reduced risk of menstrual migraines; positive effects on lipids; Less weight gain
Disadvantages: Higher risk of blood clots
Examples: Mircette; Ortho-Cept; Apri; Solia; Desogen; Cesia; Reclipsen; Velivet; Casiant
In looking at the specific progestins, it's also helpful to define them by groups. Progestins are classified as first to fourth generation progestins based on when they were first available, but different generations also have some different characteristics. Keep in mind that newer isn't necessarily better.
- First Generation: Norethindrone, norethindrone acetate, and ethynodiol
- Second Generation: Cyclessa and norgestrel
- Third Generation: Norgestrel and norgestimate
- Fourth Generation: Drospirenone
When looking at progestins, it's noteworthy that some combination pills that sound very similar have different progestins. For example, Ortho-novum 1/35 and 7/7/7/ contain norethindrone whereas Ortho-novum 1/50 contains norgestrel.