YAZ- drospirenone and ethinyl estradiol
Bayer HealthCare Pharmaceuticals Inc.
WARNING: CIGARETTE SMOKING AND SERIOUS CARDIOVASCULAR EVENTS
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptives (COC) use. This risk increases with age, particularly in women over 35 years of age, and with the number of cigarettes smoked. For this reason, COCs should not be used by women who are over 35 years of age and smoke [see Contraindications (4)].
1 INDICATIONS AND USAGE
1.1 Oral Contraceptive
Yaz® is indicated for use by women to prevent pregnancy.
1.2 Premenstrual Dysphoric Disorder (PMDD)
Yaz is also indicated for the treatment of symptoms of premenstrual dysphoric disorder (PMDD) in women who choose to use an oral contraceptive as their method of contraception. The effectiveness of Yaz for PMDD when used for more than three menstrual cycles has not been evaluated.
The essential features of PMDD according to the Diagnostic and Statistical Manual-4th edition (DSM-IV) include markedly depressed mood, anxiety or tension, affective lability, and persistent anger or irritability. Other features include decreased interest in usual activities, difficulty concentrating, lack of energy, change in appetite or sleep, and feeling out of control. Physical symptoms associated with PMDD include breast tenderness, headache, joint and muscle pain, bloating and weight gain. In this disorder, these symptoms occur regularly during the luteal phase and remit within a few days following onset of menses; the disturbance markedly interferes with work or school, or with usual social activities and relationships with others. Diagnosis is made by healthcare providers according to DSM-IV criteria, with symptomatology assessed prospectively over at least two menstrual cycles. In making the diagnosis, care should be taken to rule out other cyclical mood disorders.
Yaz has not been evaluated for the treatment of premenstrual syndrome (PMS).
Yaz is indicated for the treatment of moderate acne vulgaris in women at least 14 years of age, who have no known contraindications to oral contraceptive therapy and have achieved menarche. Yaz should be used for the treatment of acne only if the patient desires an oral contraceptive for birth control.
2 DOSAGE AND ADMINISTRATION
2.1 How to Take Yaz
Take one tablet by mouth at the same time every day. The failure rate may increase when pills are missed or taken incorrectly.
To achieve maximum contraceptive and PMDD effectiveness, Yaz must be taken exactly as directed, in the order directed on the blister pack. Single missed pills should be taken as soon as remembered.
2.2 How to Start Yaz
Instruct the patient to begin taking Yaz either on the first day of her menstrual period (Day 1 Start) or on the first Sunday after the onset of her menstrual period (Sunday Start).
Day 1 Start
During the first cycle of Yaz use, instruct the patient to take one light pink Yaz daily, beginning on Day 1 of her menstrual cycle. (The first day of menstruation is Day 1.) She should take one light pink Yaz daily for 24 consecutive days, followed by one white inert tablet daily on Days 25 through 28. Yaz should be taken in the order directed on the package at the same time each day, preferably after the evening meal or at bedtime with some liquid, as needed. Yaz can be taken without regard to meals. If Yaz is first taken later than the first day of the menstrual cycle, Yaz should not be considered effective as a contraceptive until after the first 7 consecutive days of product administration. Instruct the patient to use a non-hormonal contraceptive as back-up during the first 7 days. The possibility of ovulation and conception prior to initiation of medication should be considered.
During the first cycle of Yaz use, instruct the patient to take one light pink Yaz daily, beginning on the first Sunday after the onset of her menstrual period. She should take one light pink Yaz daily for 24 consecutive days, followed by one white inert tablet daily on Days 25 through 28. Yaz should be taken in the order directed on the package at the same time each day, preferably after the evening meal or at bedtime with some liquid, as needed. Yaz can be taken without regard to meals. Yaz should not be considered effective as a contraceptive until after the first 7 consecutive days of product administration. Instruct the patient to use a non-hormonal contraceptive as back-up during the first 7 days. The possibility of ovulation and conception prior to initiation of medication should be considered.
The patient should begin her next and all subsequent 28-day regimens of Yaz on the same day of the week that she began her first regimen, following the same schedule. She should begin taking her light pink tablets on the next day after ingestion of the last white tablet, regardless of whether or not a menstrual period has occurred or is still in progress. Anytime a subsequent cycle of Yaz is started later than the day following administration of the last white tablet, the patient should use another method of contraception until she has taken a light pink Yaz daily for seven consecutive days.
DOSAGE FORMS AND STRENGTHS
Yaz (drospirenone/ethinyl estradiol tablets) is available in blister packs.
Each blister pack (28 film-coated tablets) contains in the following order:
24 light pink tablets each containing 3 mg drospirenone (DRSP) and 0.02 mg ethinyl estradiol (EE) as betadex clathrate
4 white inert tablets
Do not prescribe Yaz to women who are known to have the following:
A high risk of arterial or venous thrombotic diseases. Examples include women who are known to:
Smoke, if over age 35 [see Boxed Warning and Warnings and Precautions (5.1)]
Have deep vein thrombosis or pulmonary embolism, now or in the past [see Warnings and Precautions (5.1)]
Have cerebrovascular disease [see Warnings and Precautions (5.1)]
Have coronary artery disease [see Warnings and Precautions (5.1)]
Have thrombogenic valvular or thrombogenic rhythm diseases of the heart (for example, subacute bacterial endocarditis with valvular disease, or atrial fibrillation) [see Warnings and Precautions (5.1)]
Have inherited or acquired hypercoagulopathies [see Warnings and Precautions (5.1)]
Have uncontrolled hypertension [see Warnings and Precautions (5.5)]
Have diabetes mellitus with vascular disease [see Warnings and Precautions (5.7)]
Have headaches with focal neurological symptoms or have migraine headaches with or without aura if over age 35 [see Warnings and Precautions (5.8)]
Undiagnosed abnormal uterine bleeding [see Warnings and Precautions (5.9)]
Breast cancer or other estrogen- or progestin-sensitive cancer, now or in the past [see Warnings and Precautions (5.3)]
Liver tumors, benign or malignant, or liver disease [see Warnings and Precautions (5.4) and Use in Specific Populations (8.7)]
Pregnancy, because there is no reason to use COCs during pregnancy [see Warnings and Precautions (5.10) and Use in Specific Populations (8.1)]
5 WARNINGS AND PRECAUTIONS
5.1 Thromboembolic Disorders and Other Vascular Problems
Stop Yaz if an arterial or venous thrombotic (VTE) event occurs.
Yaz (drospirenone/ethinyl estradiol tablets) provides an oral contraceptive regimen consisting of 24 light pink active film-coated tablets each containing 3 mg of drospirenone and 0.02 mg of ethinyl estradiol stabilized by betadex as a clathrate (molecular inclusion complex) and 4 white inert film coated tablets.
The inactive ingredients in the light pink tablets are lactose monohydrate NF, corn starch NF, magnesium stearate NF, hypromellose USP, talc USP, titanium dioxide USP, ferric oxide pigment, red NF. The white inert film-coated tablets contain lactose monohydrate NF, microcrystalline cellulose NF, magnesium stearate NF, hypromellose USP, talc USP, titanium dioxide USP.
Drospirenone (6R,7R,8R,9S,10R,13S,14S,15S,16S,17S)-1,3',4',6,6a,7,8,9,10,11, 12,13,14,15,15a,16-hexadecahydro-10,13-dimethylspiro-[17H-dicyclopropa- [6,7:15,16]cyclopenta[a]phenanthrene-17,2'(5H)-furan]-3,5'(2H)-dione) is a synthetic progestational compound and has a molecular weight of 366.5 and a molecular formula of C24H30O3.
Ethinyl estradiol (19-nor-17α-pregna 1,3,5(10)-triene-20-yne-3, 17-diol) is a synthetic estrogenic compound and has a molecular weight of 296.4 and a molecular formula of C20H24O2.
12.1 Mechanism of Action
COCs lower the risk of becoming pregnant primarily by suppressing ovulation. Other possible mechanisms may include cervical mucus changes that inhibit sperm penetration and the endometrial changes that reduce the likelihood of implantation.
Drospirenone is a spironolactone analogue with anti-mineralocorticoid and antiandrogenic activity. The estrogen in Yaz is ethinyl estradiol.