Cyproterone acetate, ethinylestradiol.
SUCEE: 21 active tablets containing 2 mg cyproterone acetate and 0.035 mg ethinyl estradiol.
SUCEE 28: 21 active tablets containing 2 mg cyproterone acetate and 0.035 mg ethinyl estradiol.
7 white placebo tablets that do not contain any active ingredients.
Because of the small amount of hormone, SUCEE is considered a low-dose oral contraception.
Pharmacology: SUCEE is an estrogen/progestogen combination oral contraceptive that inhibits ovulation.
Pharmacodynamics: SUCEE contains cyproterone acetate which inhibits androgen activities which are produced by ovaries and adrenal glands. It is possible to treat diseases causing either an increased production of androgens or a particular sensitivity to these hormones such as acne, hirsutism, alopecia. SUCEE reduces the increased sebaceous gland function, which plays an important role in the development of acne and seborrhea. This leads, usually after 3 to 4 months of therapy, to the healing of existing acne efflorescences. The excessive greasiness of the hair and skin generally disappears earlier. The loss of hair which frequently accompanies seborrhoea likewise diminishes. Treatment with SUCEE is indicated in women of child-bearing age who exhibit mild forms of hirsutism, and in particular in slightly increased facial hair; result do not, however, become apparent until after several months of use. SUCEE also contains ethinyl estradiol, which inhibits ovulation thus preventing a possible conception.
Pharmacokinetics: Ethinyl estradiol is rapidly absorbed with peak concentrations attained within 2 hours. It undergoes considerable first-pass elimination. Ethinyl estradiol is 97% to 98% bound to plasma albumin. Half-life varies from 6 to 20 hours. It is excreted in bile and urine as conjugates and undergoes some enterohepatic recirculation.
Cyproterone acetate is completely absorbed. The bioavailability after oral administration is 88-100% and Tmax occurred within 2-3 hours post dose.
Cyproterone acetate is 93% bound to serum albumin. It is metabolized by various pathways, including hydroxylation, de-acetylation and conjugation. The main metabolite in human plasma is 15β-hydroxy-cyproterone acetate which show antiandrogenic activity, similar to that of cyproterone acetate, but the metabolite has only 10% of the progestrogenic potency of cyproterone acetate. Following oral administration, the terminal half-life is approximately 1.6-3.6 days.
For the treatment of androgen-dependent diseases in women, such as pronounced forms of acne especially those which are accompanied by seborrhea or by inflammation or formation of nodes (acne papulopustulosa, acne nodulocystica), androgenetic alopecia and mild forms of hirsutism. Sucee is also used for contraception in woman with these symptoms.
How to take SUCEE: 28-day regimen (SUCEE 28): Tablets must be taken in the order directed on the package every day at about the same time with some liquid as needed. One tablet is to be taken daily for 28 consecutive days. Start with the number 1 tablet in the top comer. Follow the direction of the arrows until all 28 tablets have been taken. Each subsequent pack is started the day after the last tablet of the current pack. During placebo days a withdrawal bleeding usually occurs. This usually starts on day 2 - 3 after the last active tablet and may not have finished before the next pack is started.
21-day regimen (SUCEE): For day-1 start, the first day of menstrual bleeding should be counted as day-1. The cycle is to take 1 tablet per day for 21 days; no tablets for 7 days. During tablet-free interval of 7 days, a withdrawal bleeding may occurs. Whether bleeding has stopped or not, the patients should start a new course of the 21-day regimen.
How to start SUCEE: No preceding hormonal contraceptive use (in the past month): Tablet-taking has to start on day 1 of the menstrual. Starting on days 2-5 is allowed, but during the first cycle a barrier method is recommended in addition for the first 7 days of tablet-taking.
Changing from another combined oral contraceptive: The women should start SUCEE preferably on the day after the last active tablet of previous combined oral contraceptive, but at latest on the day following the placebo tablet interval of previous combined oral contraceptive.
Changing from a progestagen-only-method (minipill, injection, implant): The women may switch any day from the minipill (from an implant on the day of its removal, from an injectable when the next injection would be due), but should in all of theses cases be advised to additionally use a barrier method for the first 7 days of tablet taking.
Following first-trimester abortion: The women may start immediately. When doing so, she need not take additional contraceptive measures.
Following delivery: In the nonlactating mother, may be initiated no earlier than day 28 postpartum for contraception because of the increased risk for thromboembolism. Advise the patient to use a barrier method for first 7 days of tablet taking. However, if intercourse has already occurred, consider the possibility of ovulation and conception prior to initiation of medication.
Missed Active Dose: While there is little likelihood of ovulation occurring if only 1 tablet is missed, the possibility of spotting or bleeding is increased. The possibility of ovulation occurring increases with each successive day that scheduled tablets are missed. This is particularly likely to occur if ≥ 2 consecutive tablets are missed. Any time ≥ 1 active tablets have been missed, the patient should use another method of contraception for the balance of the cycle until tablets have been taken for 7 consecutive days. If a patient forgets to take ≥ 1 tablet, the following is suggested: One active tablet: Have the patient take this as soon as remembered, even if this means taking two tablets at the same time. She then continues to take tablets at her usual time.
If missed at week 3 the next pack must be started as soon as active tablets in the current pack are finished, i.e., no placebo tablets should be taken. The user is unlikely to have a withdrawal bleed until the end of the second pack, but she may experience spotting or breakthrough bleeding on "active-tablet" taking days.
Two consecutive active tablets: The patient should take 2 tablets as soon as remembered with the next pill at the usual time or she should take 2 tablets daily for the next 2 days, then resume the regular schedule.
Serious ill effects have not been reported following acute overdosage of OCs in young children.
Overdosage may cause nausea. Withdrawal bleeding may occur in females.
There are no antidotes and further treatment should be symptomatic.
Thrombophlebitis, Thromboembolic disorders (e.g. valvular heart disease with thrombogenic complications), History of deep-vein thrombophlebitis, Cerebral vascular disease, MI, Coronary artery disease.
Known or suspected breast carcinoma or estrogen-dependent neoplasia, carcinoma of endometrium.
Hepatic adenomas/carcinomas.
Undiagnosed abnormal genital bleeding.
Known or suspected pregnancy.
Cholestatic jaundice of pregnancy/jaundice with prior pill use.
Hypersensitivity to any component of the product.
Acute liver disease.
Uncontrolled hypertension.
Diabetes mellitus with vascular complications.
Smoking: Cigarette smoking increases the risk of serious cardiovascular side effect from SUCEE. This risk increases with age and with heavy smoking (≥ 15 cigarettes per day) and is quite marked in women > 35 years of age. Women who use SUCEE should not smoke.
Thromboembolism: Be alert to the earliest symptoms of thromboembolic and thrombotic disorders. Should any of these occur or be suspected, discontinue the drug immediately.
MI: MI risk associated with SUCEE use is increased. The risk is primarily in smokers or women with other underlying risk factors for coronary artery disease such as hypertension, hypercholesterolemia, morbid obesity and diabetes. The risk is very low in women < 30 years of age.
Cerebrovascular diseases: SUCEE increase the risk of cerebrovascular event (thrombotic and hemorrhagic strokes), although, in general, the risk is greatest in hypertensive women > 35 years of age who also smoke.
Age: The risk of cerebrovascular and circulatory disease in SUCEE users is substantially increased in women ≥ 35 years of age with other risk factor (e.g. smoking, uncontrolled hypertension, hypercholesterolemia [LDL 190], obesity, diabetes).
Carcinoma: Numerous epidemiological studies have been performed on the incidence of breast, endometrial, ovarian, and cervical cancer in using combined oral contraceptives.
Some studies suggest that oral contraceptive use has been associated with an increase in the risk of cervical intraepithelial neoplasia in some women. There continues to be controversy about the extent to which such findings may be because of differences in sexual behavior and other factors.
Close clinical surveillance of all women taking oral contraceptives is essential; they should be reexamined at least once a year. Monitor women with a strong family history of breast cancer or who have breast nodules, fibrocystic disease of the breast, cervical dysplasia or abnormal mammograms.
Benign and malignant hepatic adenomas have been associated with the use of oral contraceptives, but this is a relatively rare disease.
Elevated blood pressure: Elevated blood pressure and hypertension may occur within a few months of beginning use. High blood pressure returns to normal in most women after oral contraceptives discontinuation.
Monitoring: It is good medical practice for all women to have annual history and physical examinations. Physical examination may be deferred until after initiation of OCs if requested by the patient and judged appropriately by the health care provider.
Women should be advised that oral contraceptives do not protect against HIV infections (AIDS) and other sexually transmissible disease.
Pregnancy: Category x. Rule out pregnancy before initiating or continuing OCs and always consider it if withdrawal bleeding does not occur.
If pregnancy is confirmed, apprise the patient of the potential risks to the fetus.
Lactation: Combination OCs given in the postpartum period may interfere with lactation, decreasing the quantity and quality of breast milk. Furthermore, a small amount of OC steroids is excreted in breast milk. If possible, defer use until the infant has been weaned.
Serious adverse reactions: See Warnings: Arterial thromboembolism; cerebral hemorrhage; cerebral thrombosis; coronary thrombosis, gall bladder disease, hepatic adenomas or benigh liver tumors, hypertension. MI, pulmonary embolism, thrombophlebitis and venous thrombosis with or without embolism.
Other possible side effects: These side effects may occur in the first few months and usually lessen with time.
CNS: Dizziness, headache, mental depression, migraine.
Dermatologic: Melasma, rash.
Endocrine: Breast tenderness, enlargement, secretion.
GI: Abdominal cramps, nausea and vomiting, Cholestatic jaundice.
GU: Amenorrhea during and after treatment, change in cervical secretion, vaginal candidiasis.
Ophthalmic: Contact lens intolerance (discomfort of the cornea if contact lenses are used).
Miscellaneous: Edema, reduced carbohydrate tolerance; change in body weight.
Anticoagulants: Oral contraceptive can increase levels of certain circulating clotting factors and reduce Antithrombin III levels, therapeutic efficacy of the anticoagulants may be decreased. However, both an increased and decreased effect has occurred.
Antidepressants, Tricyclic, Beta blockers, caffeine, corticosteroids, theophyllines: The hepatic metabolism of these agents may be decreased, resulting in increased therapeutic effects or toxicity.
Benzodiazepines: Oral contraceptives may increase the clearance of the benzodiazepines that undergo glucuronidation (e.g. lorazepam, oxazepam, temazepam) because of increased metabolism. Combination oral contraceptives with alprazolam, Chlordiazepoxide, diazepam, and triazolam may inhibit hepatic rnixed-function oxidases leading to a decrease in benzodiazepines oxidation rate (may prolong the half-life of benzodiazepines).
Antibiotics: Coadministration of griseofulvin, penicillins, or tetracyclines with oral contraceptives (OCs), may decrease the pharmacologic effect of the oral contraceptives, possibly because of altered steroid gut metabolism secondary to changes in the intestinal flora. Menstrual irregularities and pregnancy may occur. An alternate or additional form of birth control may be advisable during concomitant use.
Barbiturates, Carbamazepine, Hydantoins, Phenytoin, Rifamycins, St. John's wort: These agents may increase the hepatic metabolism of the oral contraceptives via hepatic microsomal enzyme induction, possibly resulting in decreased effectiveness of the oral contraceptives. Menstrual irregularities and pregnancy may occur. An alternate or additional form of birth control may be advisable during concomitant use.
Store at temperature not exceeding 30°C. Protect from light and moisture.
G03HB01 - cyproterone and estrogen ; Belongs to the class of antiandrogen preparations in combination with estrogens. Used to counter androgenic activities.
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