B-Lady

Cyproterone acetate, ethinylestradiol.

Each tablet contains Cyproterone acetate 2.0 mg, Ethinyl estradiol 0.035 mg.

Pharmacology: Pharmacodynamics: Ethinyl estradiol: Estrogen is responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormones, and follicle-stimulating hormone through a negative feedback system. Estrogen increases levels of sex hormone-binding globulin (SHBG) and may reduce unbound androgen levels. Ethinyl estradiol is a synthetic derivative of estradiol. The addition of the ethinyl group prevents rapid degradation by the liver.
Cyproterone: Steroid compound with anti-androgenic, anti-gonadotropic and progestin-like activity.
Pharmacokinetics: Cyproterone: Cyproterone acetate is completely absorbed. Cyproterone is metabolized by liver. Half-life elimination is 38 hours (range 33-43 hours). Time to peak is 3-4 hours and excreted in feces (60%) and urine (33%).
Ethinyl estradiol: Estradiol is well absorbed from the gastrointestinal tract, mucous membranes, and the skin. It is widely distributed with high concentrations in the sex hormone target organs. Ethinyl estradiol is bound to sex hormone-binding globulin and albumin. Ethinyl estradiol is partially lipid metabolized by CYP3A4 hepatic enzymes. Oral estradiol also undergoes enterohepatic recirculation by conjugation in the liver. Estradiol is excreted in urine.

1. For contraception which is particularly useful in women with Androgen-dependent disease symptom e.g. acne, androgenic type baldness etc. Use for prevention of pregnancy in women with the previously mentioned symptoms.
2. For the treatment of acne.

Recommended Dose: Before starting B-LADY a thorough general medical and gynecological examination (including breasts) should be carried out and pregnancy must be excluded. As a precaution, physical examinations should be conducted at intervals of about 6 months during long term treatment with the tablets.
Wait for the menstrual period (monthly bleeding). Take 1 tablet daily, on the first day of the menstrual bleeding. Start with the tablet corresponding to the day of the week, e.g. "Mon" for Monday. Then follow the arrows until all the tablets in the package have been taken. When the first package is finished, a tablet-free interval of 7 days is required during that time a menstruation like bleeding occur.
Take the tablet at the same time each day, preferably at bedtime.
In case the patient forgot to take the tablet for 12 hours, take the tablet as soon as possible. If forgotten to take the tablet for over 12 hours, take 2 tablets on that day and use other means of contraception (e.g. condom) for at least 7 days.
The length of use depends on the desired pregnancy interval and the severity of the clinical sign. In general, therapy should be discontinued 3 - 4 cycles after resolution of symptoms.
Mode of Administration: Oral.

Preparations containing ethinyl estradiol, cyproterone combinations should not be used in the presence of any of the conditions listed as follows: 1. Hypersensitivity to ethinyl estradiol, cyproterone, or any component of the formulation.
2. Current or history of breast cancer or other estrogen-dependent or progestin-dependent neoplasm.
3. Hepatic tumors or liver disease.
4. History of cholestatic jaundice.
5. Pregnancy.
6. Undiagnosed abnormal vaginal bleeding.
7. Ocular lesions arising from ophthalmic vascular disease.
8. History of otosclerosis with deterioration during pregnancy.
9. Women at high risk of arterial or venous thrombotic disease including cerebrovascular disease, coronary artery disease, MI, diabetes mellitus with vascular disease.

Consult the physician if any of the following signs occur while taking this medication, these are feeling of discomfort, headaches, nausea, or other gastrointestinal upsets, breast tenderness, spotting or break bleeding.
B-LADY may increase the risk of thromboembolism; discontinue use if an arterial or venous thrombotic event occurs.
Progesterone and/or estrogen should not be taken while on B-LADY.
The risk of cardiovascular side effects is increased in women who smoke cigarettes; risk increases with age (especially women > 35 years of age) and the number of cigarettes smoked (≥ 15 cigarettes per day); women who use B-LADY should be strongly advised not to smoke.
May have adverse effects on glucose tolerance; use caution in woman with diabetes. If patient has diabetes, hypertension, and obesity or if this triad of conditions develops, B-LADY should be discontinued.
Malignant liver tumors leading to isolated cases of life-threatening intraabdominal hemorrhage have been observed. If severe upper-abdominal complaints, liver enlargement or signs of intra-abdominal hemorrhage occur a liver tumors should be included in the differential diagnostic considerations.
Use with caution in patients with hepatic or renal impairment, cardiac disease, depression, asthma, epilepsy, or history of migraine. Estrogen may induce or exacerbate symptoms of angioedema, particularly in women with hereditary angioedema. Discontinuation of B-LADY may be necessary.
B-LADY may change the results of some laboratory test (e.g. coagulation factors, lipids, glucose tolerance, binding proteins).

Pregnancy: Pregnancy should be ruled out prior to treatment and discontinued if pregnancy occurs.
Lactation: B-LADY is not recommended in breast-feeding because it enters breast milk.

Cardiovascular: Varicosities, edema, arterial thromboembolism, cerebral hemorrhage, cerebral thrombosis, hypertension, mesenteric thrombosis, MI, Raynaud's phenomenon.
Central nervous system: Headache, nervousness, depression, dizziness, migraine, pre-menstrual syndrome, stroke.
Dermatologic: Chloasma, acne, angioedema, erythema multiforme, erythema nodosum, hirsutism, loss of scalp hair, melasma, rash.
Endocrine & metabolic: Dysmenorrhea, breast tenderness, libido changes, amenorrhea, breakthrough bleeding, breast changes, carbohydrate intolerance, lactation decreased, menstrual flow changes, spotting, temporary infertility, thyroid-binding globulin increased, triglycerides increased.
Gastrointestinal: Nausea, abdominal bloating/cramps, appetite changes, cholestasis, colitis, gallbladder disease, pancreatitis, vomiting, weight gain/loss.
Genitourinary: Cervical erosion change, cervical secretion change, cystitis-like syndrome, endocervical hyperplasia, uterine fibroid enlarged, vaginal candidiasis, vaginitis.
Hematologic: Factors VII, VIII, IX, and X increased, folate levels decreased, hemolytic uremic syndrome, porphyria, prothrombin increased.
Hepatic: Alkaline phosphatase increased, AST increased, benign liver tumors, Budd-Chiari syndrome, cholestatic jaundice, GGT increased, hepatic adenomas, jaundice.
Neuromuscular & skeletal: Chorea, rheumatoid arthritis exacerbation, synovitis exacerbation.
Ocular: Cataracts, change in corneal curvature, contact lens intolerance, optic neuritis, retinal thrombosis.
Otic: Auditory disturbances.
Renal: Renal function impaired.
Respiratory: Pulmonary thromboembolism, rhinitis.
Miscellaneous: Hemorrhagic eruption, systemic lupus erythematosus (SLE).

Avoid concomitant use of cyproterone acetate and ethinyl estradiol with any of the following: anastrozole, conivaptan, pimozide, pirfenidone.
Cyproterone acetate and ethinyl estradiol may increase the effects of aripiprazole, benzodiazepines, corticosteroid, CYP1A2 substrates, HMG-CoA reductase inhibitors, lomitapide, pimozide, pirfenidone, ropinirole, selegiline, theophylline derivatives, tipranavir, tizanidine, tranexamic acid, voriconazole.
The level of cyproterone acetate and ethinyl estradiol may be increased by: ascorbic acid, conivaptan, CYP3A4 inhibitors (strong, moderate), ivacaftor, mifepristone, NSAID (COX-2 inhibitor), voriconazole.
Cyproterone acetate and ethinyl estradiol may decrease the effects of anastrozole, chenodiol, CYP1A2 substrates, CYP2E1 substrates, hyaluronidase, lamotrigine, thyroid products, ursodiol, vitamin K antagonists.
The level of cyproterone acetate and ethinyl estradiol may be decreased by aminoglutethimide, aprepitant, armodafinil, artemether, barbiturates, bexarotene, bile acid sequestrants, boceprevir, bosentan, carbamazepine, clobazam, cobicistat, colesevelam, CYP3A4 inducers (strong), deferasirox, elvitegravir, exenatide, felbamate, fosaprepitant, fosphenytoin, griseofulvin, mifepristone, modafinil, mycophenolate, nafcillin, nevirapine, oxcarbazepine, phenytoin, protease inhibitors, prucalopride, retinoic acid derivatives, rifamycin derivatives, rufinamide, St. John's Wort, telaprevir, tipranavir, tocilizumab, topiramate.

Store below 30°C.

Oral Contraceptives / Acne Treatment Preparations

G03HB01 - cyproterone and estrogen ; Belongs to the class of antiandrogen preparations in combination with estrogens. Used to counter androgenic activities.

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