Cyclessa Information
Cyclessa (Ethinyl)
Cyclessa (Ethinyl) Description
Cyclessa (Ethinyl) Tablets (desogestrel and ethinyl estradiol tablets USP) is a triphasic oral contraceptive containing two active components, desogestrel and ethinyl estradiol. Each 28-day treatment cycle pack consists of three active dosing phases: 7 light yellow tablets containing 0.100 mg desogestrel (13-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-17-ol) and 0.025 mg ethinyl estradiol (19-nor-17α-pregna-1,3,5(10)-trien-20-yne-3, 17-diol); 7 orange tablets containing 0.125 mg desogestrel and 0.025 mg ethinyl estradiol, and 7 red tablets containing 0.150 mg desogestrel and 0.025 mg ethinyl estradiol. Inactive ingredients include vitamin E, pregelatinized starch, stearic acid, lactose monohydrate, hydroxypropyl methylcellulose, polyethylene glycol, titanium dioxide, talc, yellow ferric oxide (in light yellow and orange tablets), and red ferric oxide (in orange and red tablets). Cyclessa (Ethinyl) also contains 7 green tablets with the following inert ingredients: lactose monohydrate, corn starch, magnesium stearate, hydroxypropyl methylcellulose, polyethylene glycol, titanium dioxide, FD&C Blue No. 2 aluminum lake, yellow ferric oxide, and talc. The molecular weights for desogestrel and ethinyl estradiol are 310.48 and 296.40, respectively. The structural formulas are as follows:
Cyclessa (Ethinyl) Clinical Pharmacology
Combination oral contraceptives act by suppression of gonadotropins. Although the primary mechanism of this action is inhibition of ovulation, other alterations include changes in the cervical mucus (which increase the difficulty of sperm entry into the uterus) and the endometrium (which reduce the likelihood of implantation).
Receptor-binding studies, as well as studies in animals, have shown that etonogestrel, the biologically active metabolite of desogestrel, combines high progestational activity with minimal intrinsic androgenicity (91,92). The relevance of this latter finding in humans is unknown.
Cyclessa (Ethinyl) Indications And Usage
Cyclessa (Ethinyl) Tablets (desogestrel 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.
Oral contraceptives are highly effective. Table 2 lists the typical unintended pregnancy rates for users of combination oral contraceptives and other methods of contraception. The efficacy of these contraceptive methods, except sterilization, the IUD, and implants, depends upon the reliability with which they are used. Correct and consistent use of these methods can result in lower failure rates.
Cyclessa (Ethinyl) Contraindications
Oral contraceptives should not be used in women who currently have the following conditions:
Cyclessa (Ethinyl) Warnings
Cigarette smoking increases the risk of serious cardiovascular side effects from oral contraceptive use. This risk increases with age and with heavy smoking (15 or more cigarettes per day) and is quite marked in women over 35 years of age. Women who use oral contraceptives should be strongly advised not to smoke.
The use of oral contraceptives is associated with increased risks of several serious conditions including venous and arterial thrombotic and thromboembolic events (such as myocardial infarction, thromboembolism, and stroke) hepatic neoplasia, gallbladder disease, and hypertension, although the risk of serious morbidity or mortality is very small in healthy women without underlying risk factors. The risk of morbidity and mortality increases significantly in the presence of other underlying risk factors such as certain inherited thrombophilias, hypertension, hyperlipidemias, obesity, and diabetes.
Practitioners prescribing oral contraceptives should be familiar with the following information relating to these risks.
The information contained in this package insert is principally based on studies carried out in patients who used oral contraceptives with formulations of higher doses of estrogens and progestogens than those in common use today. The effect of long-term use of the oral contraceptives with formulations of lower doses of both estrogens and progestogens remains to be determined.
Throughout this labeling, epidemiologic studies reported are of two types: retrospective or case control studies and prospective or cohort studies. Case control studies provide a measure of the relative risk of a disease, namely, a of the incidence of a disease among oral contraceptive users to that among non-users. The relative risk does not provide information on the actual clinical occurrence of a disease. Cohort studies provide a measure of attributable risk, which is the in the incidence of disease between oral contraceptive users and non-users. The attributable risk does provide information about the actual occurrence of a disease in the population (Adapted from refs. 2 and 3 with the authors' permission). For further information, the reader is referred to a text on epidemiological methods.
One study gathered data from a variety of sources which have estimated the mortality rate associated with different methods of contraception at different ages (Table 4). These estimates include the combined risk of death associated with contraceptive methods plus the risk attributable to pregnancy in the event of method failure. Each method of contraception has its specific benefits and risks. The study concluded that with the exception of oral contraceptive users 35 and older who smoke and 40 and older who do not smoke, mortality associated with all methods of birth control is low and below that associated with childbirth.
The observation of a possible increase in risk of mortality with age for oral contraceptive users is based on data gathered in the 1970's - but not reported until 1983 (35). However, current clinical practice involves the use of lower estrogen formulations combined with careful restriction of oral contraceptive use to women who do not have the various risk factors listed in this labeling.
Because of these changes in practice and, also, because of some limited new data which suggest that the risk of cardiovascular disease with the use of oral contraceptives may now be less than previously observed (100,101), the Fertility and Maternal Health Drugs Advisory Committee was asked to review the topic in 1989. The Committee concluded that although cardiovascular disease risks may be increased with oral contraceptive use after age 40 in healthy non-smoking women (even with the newer low-dose formulations), there are also greater potential health risks associated with pregnancy in older women and with the alternative surgical and medical procedures which may be necessary if such women do not have access to effective and acceptable means of contraception.
Therefore, the Committee recommended that the benefits of low-dose oral contraceptive use by healthy non-smoking women over 40 may outweigh the possible risks. Of course, older women, as all women who take oral contraceptives, should take the lowest possible dose formulation that is effective and meets the individual patient needs.
Numerous epidemiologic studies have been performed on the incidence of breast, endometrial, ovarian, and cervical cancer in women using oral contraceptives. Although the risk of breast cancer may be slightly increased among current users of oral contraceptives (RR = 1.24), this excess risk decreases over time after oral contraceptive discontinuation and by 10 years after cessation the increased risk disappears. The risk does not increase with duration of use, and no relationships have been found with dose or type of steroid. The patterns of risk are also similar regardless of a woman's reproductive history or her family breast cancer history. The subgroup for whom risk has been found to be significantly elevated is women who first used oral contraceptives before age 20, but because breast cancer is so rare at these young ages, the number of cases attributable to this early oral contraceptive use is extremely small. Breast cancers diagnosed in current or previous oral contraceptive users tend to be less advanced clinically than in never-users. Women who currently have or have had breast cancer should not use oral contraceptives because breast cancer is a hormone-sensitive tumor.
Some studies suggest that combination oral contraceptive use has been associated with an increase in the risk of cervical intra-epithelial neoplasia in some populations of women (45–48). However, there continues to be controversy about the extent to which such findings may be due to differences in sexual behavior and other factors.
In spite of many studies of the relationship between oral contraceptive use and breast and cervical cancers, a cause-and-effect relationship has not been established.
Benign hepatic adenomas are associated with oral contraceptive use, although the incidence of benign tumors is rare in the United States. Indirect calculations have estimated the attributable risk to be in the range of 3.3 cases/100,000 for users, a risk that increases after four or more years of use especially with oral contraceptives of higher dose (49). Rupture of rare, benign, hepatic adenomas may cause death through intra-abdominal hemorrhage (50,51).
Studies from Britain have shown an increased risk of developing hepatocellular carcinoma (52–54) in long-term (>8 years) oral contraceptive users. However, these cancers are extremely rare in the U.S. and the attributable risk (the excess incidence) of liver cancers in oral contraceptive users approaches less than one per million users.
Extensive epidemiologic studies have revealed no increased risk of birth defects in women who have used oral contraceptives prior to pregnancy (55–57). Studies also do not suggest a teratogenic effect, particularly in so far as cardiac anomalies and limb reduction defects are concerned (55,56,58,59), when oral contraceptives are taken inadvertently during early pregnancy.
The administration of oral contraceptives to induce withdrawal bleeding should not be used as a test for pregnancy. Oral contraceptives should not be used during pregnancy to treat threatened or habitual abortion. It is recommended that for any patient who has missed two consecutive periods, pregnancy should be ruled out. If the patient has not adhered to the prescribed schedule, the possibility of pregnancy should be considered at the first missed period. Oral contraceptive use should be discontinued if pregnancy is confirmed.
Oral contraceptives have been shown to cause a decrease in glucose tolerance in a significant percentage of users (17). Oral contraceptives containing greater than 75 micrograms of estrogens cause hyperinsulinism, while lower doses of estrogen cause less glucose intolerance (65). Progestogens increase insulin secretion and create insulin resistance, this effect varying with different progestational agents (17,66). However, in the non-diabetic woman, oral contraceptives appear to have no effect on fasting blood glucose (67). Because of these demonstrated effects, prediabetic and diabetic women should be carefully monitored while taking oral contraceptives.
A small proportion of women will have persistent hypertriglyceridemia while on the pill. As discussed earlier (see and ), changes in serum triglycerides and lipoprotein levels have been reported in oral contraceptive users.
Women with severe hypertension should not be started on hormonal contraceptives. An increase in blood pressure has been reported in women taking oral contraceptives (68) and this increase is more likely in older oral contraceptive users (69) and with continued use (61). Data from the Royal College of General Practitioners (12) and subsequent randomized trials have shown that the incidence of hypertension increases with increasing quantities of progestogens.
Women with a history of hypertension or hypertension-related diseases, or renal disease (70) should be encouraged to use another method of contraception. If women elect to use oral contraceptives, they should be monitored closely and if significant elevation of blood pressure occurs, oral contraceptives should be discontinued. For most women, elevated blood pressure will return to normal after stopping oral contraceptives (69), and there is no difference in the occurrence of hypertension between ever- and never-users (68,70,71).
Breakthrough bleeding and spotting are sometimes encountered in patients on oral contraceptives, especially during the first three months of use. If bleeding persists or recurs, non-hormonal causes should be considered and adequate diagnostic measures taken to rule out malignancy or pregnancy, as in the case of any abnormal vaginal bleeding. If pathology has been excluded, time or a change to another formulation may solve the problem. In the event of amenorrhea, pregnancy should be ruled out.
Some women may encounter post-pill amenorrhea or oligomenorrhea, especially when such a condition was pre-existent.
Cyclessa (Ethinyl) Precautions
Patients should be counseled that this product does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
Women who are being treated for hyperlipidemias should be followed closely if they elect to use oral contraceptives. Some progestogens may elevate LDL levels and may render the control of hyperlipidemias more difficult.
In patients with familial defects of lipoprotein metabolism receiving estrogen-containing preparations, there have been case reports of significant elevations of plasma triglycerides leading to pancreatitis.
Cyclessa (Ethinyl) Information For The Patient
Cyclessa (Ethinyl) Adverse Reactions
An increased risk of the following serious adverse reactions has been associated with the use of oral contraceptives (see section):
There is evidence of an association between the following conditions and the use of oral contraceptives:
The following adverse reactions have been reported in patients receiving oral contraceptives and are believed to be drug-related:
The following adverse reactions have been reported in users of oral contraceptives and the association has been neither confirmed nor refuted:
Cyclessa (Ethinyl) Overdosage
Serious ill effects have not been reported following acute ingestion of large doses of oral contraceptives by young children. Overdosage may cause nausea, and withdrawal bleeding may occur in females.
Cyclessa (Ethinyl) Non-contraceptive Health Benefits
The following non-contraceptive health benefits related to the use of oral contraceptives are supported by epidemiologic studies which largely utilized oral contraceptive formulations containing estrogen doses exceeding 0.035 mg of ethinyl estradiol or 0.05 mg of mestranol (73–78).
Effects on menses:
Effects related to inhibition of ovulation:
Effects from long-term use:
Cyclessa (Ethinyl) Dosage And Administration
To achieve maximum contraceptive effectiveness, Cyclessa (Ethinyl) Tablets (desogestrel and ethinyl estradiol tablets USP) must be taken exactly as directed, at the same time every day, and at intervals not exceeding 24 hours. Cyclessa (Ethinyl) may be initiated using either a Sunday start or a Day 1 start.
NOTE: Each cycle pack dispenser is preprinted with the days of the week, starting with Sunday, to facilitate a Sunday start regimen. Six different "day label strips" are provided with each cycle pack dispenser in order to accommodate a Day 1 start regimen. In this case, the patient should place the self-adhesive "day label strip" that corresponds to her starting day over the preprinted days.
Cyclessa (Ethinyl) How Supplied
Cyclessa (Ethinyl) Tablets (desogestrel and ethinyl estradiol tablets USP) is available in a 28-day blister card within a recyclable plastic dispenser. Each 28-day treatment cycle pack consists of four different dosing phases, as follows: 7 coated, round light yellow tablets (debossed with " " on one side and "Organon*" on the other side) containing 0.100 mg desogestrel and 0.025 mg ethinyl estradiol; 7 coated, round orange tablets (debossed with " " on one side and "Organon*" on the other side) containing 0.125 mg desogestrel and 0.025 mg ethinyl estradiol; and 7 coated, round red tablets (debossed with " " on one side and "Organon*" on the other side) containing 0.150 mg desogestrel and 0.025 mg ethinyl estradiol. Seven round green tablets (debossed with " " on one side and "Organon*" on the other side) contain inert ingredients.
Boxes of 6 NDC 0052-0283-06
Cyclessa (Ethinyl)
Cyclessa (Ethinyl)
Cyclessa (Ethinyl) Patient Package Insert
Oral contraceptives, also known as "birth control pills" or "the pill", are taken to prevent pregnancy. When taken correctly, oral contraceptives have a failure rate of about 1% per year (1 pregnancy per 100 women per year of use) when used without missing any pills. The typical failure rate of large numbers of pill users is less than 5% per year (5 pregnancies per 100 women per year of use) when women who miss pills are included. Forgetting to take pills increases the chances of pregnancy.
For the majority of women, oral contraceptives can be taken safely. But, there are some women who are at high risk of developing certain serious diseases that can be life-threatening or may cause temporary or permanent disability. The risks associated with taking oral contraceptives increase significantly if you:
You should not take the pill if you are pregnant or have unexplained vaginal bleeding.
Although cardiovascular disease risks may increase with oral contraceptive use after age 40 in healthy, non-smoking women (even with the newer low-dose formulations), there are also greater potential health risks associated with pregnancy in older women.
Cyclessa (Ethinyl) Detailed Patient Package Insert
Cyclessa (Ethinyl) Tablets (desogestrel and ethinyl estradiol tablets USP) is a triphasic oral contraceptive product, containing a combination of a progestin and estrogen, the two kinds of female hormones.
Each light yellow tablet contains 0.100 mg desogestrel and 0.025 mg ethinyl estradiol; each orange tablet contains 0.125 mg desogestrel and 0.025 mg ethinyl estradiol; and each red tablet contains 0.150 mg desogestrel and 0.025 mg ethinyl estradiol. Each green tablet contains inert ingredients.
Any woman who considers using oral contraceptives (the birth control pill or the pill) should understand the benefits and risks of using this form of birth control. This leaflet will give you much of the information you will need to make this decision and will also help you determine if you are at risk of developing any of the serious side effects of the pill. It will tell you how to use the pill properly so that it will be as effective as possible. However, this leaflet is not a replacement for a careful discussion between you and your doctor or healthcare provider. You should discuss the information provided in this leaflet with him or her, both when you first start taking the pill and during your revisits. You should also follow your doctor's or healthcare provider's advice with regard to regular check-ups while you are on the pill.
Oral contraceptives or "birth control pills" or "the pill" are used to prevent pregnancy and are more effective than other non-surgical methods of birth control. When they are taken correctly, the chance of becoming pregnant is less than 1% (1 pregnancy per 100 women per year of use), when used perfectly, without missing any pills. Typical failure rates are actually 5% (5 pregnancies per 100 women per year of use). The chance of becoming pregnant increases with each missed pill during a menstrual cycle.
In comparison, typical failure rates for other methods of birth control during the first year of use are as follows:
Cyclessa (Ethinyl)
Cyclessa (Ethinyl) Principal Display Panel - Tablet Carton
