Ethinyl Estradiol/Drospirenone

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[edit] BRAND NAMES

  • International: Yasmin, Yasminelle, Yaz
  • Italy: Yasmin (21 tablets 0,03mg + 3mg), Yasminelle (21 tablets 0,02mg + 3mg), Yaz (24 tablets 0,02mg+3mg plus 4 placebo (non-hormonal tablets)
  • U.S.: Yasmin (28 tablets: 21 yellow tablets tablets 0,03 mg+3 mg and 7 inert white tablets)PI, Yaz (24 tablets 0,02mg+3mg plus 4 placebo (non-hormonal tablets)) PI

[edit] STRUCTURE

[edit] MECHANISM OF ACTION

Combination oral contraceptives, containing both estrogen and progestins, act by suppression of gonadotropins (FSH and LH). 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).

Drospirenone is a fourth-generation progestin that has antimineralocorticoid, and antiandrogenic activity, which are unique characteristics compared with the other progestogens contained in most of the other Oral contraceptives currently marketed.

[edit] INDICATIONS

Ethinyl Estradiol/Drospirenone combination is indicated for use by women to prevent pregnancy and to treat moderate acne for women at least 14 years old only if the patient desires an oral contraceptive for birth control.

[edit] DOSAGE

  • 28-day regimen of tablets: The possibility of ovulation and conception prior to initiation of medication should be considered.
    The patient should be instructed to begin taking Ethinyl Estradiol/Drospirenone tablets on either Day 1 of menstruation (Day 1 Start) or the first Sunday after the onset of menstruation (Sunday Start).
    Patient should take one tablet in the order directed on the package at the same time every day, preferably after the evening meal or at bedtime with some liquid. The failure rate may increase when pills are missed or taken incorrectly.
    During the first cycle of Ethinyl Estradiol/Drospirenone, when beginning on the first Sunday after the onset of menstrual period, Ethinyl Estradiol/Drospirenone should not be considered effective as a contraceptive until after the first 7 consecutive days of product administration. Patients should use a non-hormonal contraceptive as back-up during the first 7 days.
    Patients should begin the next and all subsequent 28-day regimens of Ethinyl_Estradiol/Drospirenone on the same day of the week that they began their first regimen, following the same schedule.

[edit] CONTRAINDICATIONS

  • Renal impairment
  • Adrenal insufficiency
  • A high risk of arterial or venous thrombotic diseases
  • Undiagnosed abnormal uterine bleeding
  • Breast cancer or other estrogen- or progestin-sensitive cancer
  • Liver tumors or liver disease
  • Known or suspected pregnancy

[edit] WARNINGS AND PRECAUTIONS

  • Cigarette smoking increases the risk of serious cardiovascular side effects from oral contraceptive use. This risk increases with age and with the extent of smoking (in epidemiologic studies, 15 or more cigarettes per day was associated with a significantly increased risk) and is quite marked in women over 35 years of age. Women who use oral contraceptives should be strongly advised not to smoke or not to take Ethinyl Estradiol/Drospirenone.
  • Oral contraceptives does not protect against HIV infection (AIDS) and other sexually transmitted diseases
  • Vascular risks: Stop the pill if a thrombotic event occurs. Stop at least 4 weeks before and through 2 weeks after major surgery. Start no earlier than 4 weeks after delivery, in women who are not breastfeeding. Combined oral contraceptives containing Drospirenone may be associated with a higher risk of venous thromboembolism (VTE) than combined oral contraceptives containing levonorgestrel or some other progestins. Before initiating Ethinyl Estradiol/Drospirenone in a new combined oral contraceptives user or a woman who is switching from a contraceptive that does not contain Drospirenone, consider the risks and benefits of a Drospirenone-containing combined oral contraceptives in light of her risk of a venous thromboembolism.
  • Hyperkalemia: Drospirenone has antimineralocorticoid activity. Do not use in patients predisposed to hyperkalemia. Check serum potassium concentration during the first treatment cycle in women on long-term treatment with medications that may increase serum potassium concentration.
  • Liver disease: Discontinue if jaundice occurs.
  • High blood pressure: Do not prescribe Ethinyl Estradiol/Drospirenone for women with uncontrolled hypertension or hypertension with vascular disease.
  • Carbohydrate and lipid metabolic effects: Monitor prediabetic and diabetic women taking Ethinyl Estradiol/Drospirenone. Consider an alternate contraceptive method for women with uncontrolled dyslipidemia.
  • Headache: Evaluate significant change in headaches and discontinue the drug if indicated.
  • Uterine bleeding: Breakthrough bleeding and spotting are sometimes encountered in patients on oral contraceptives, especially during the first three months of use. If bleeding persists or occurs after previously regular cycles check for causes such as pregnancy or malignancy. If pathology and pregnancy are excluded, bleeding irregularities may resolve over time or with a change to a different COC.

[edit] INTERACTIONS

  • Anti-infective agents and anticonvulsants: Contraceptive effectiveness may be reduced when hormonal contraceptives are coadministered with antibiotics, anticonvulsants, and other drugs that increase the metabolism of contraceptive steroids. This could result in unintended pregnancy or breakthrough bleeding. Examples include rifampicin, barbiturates, phenylbutazone, phenytoin, carbamazepine, felbamate, oxcarbazepine, topiramate, and griseofulvin.
  • Anti-HIV Protease inhibitors: significant changes (increase and decrease) in the plasma levels of the estrogen and progestin have been noted in some cases. The safety and efficacy of combination oral contraceptive products may be affected with coadministration of anti-HIV protease inhibitors. Refer to the label of the individual anti-HIV protease inhibitors for further drug-drug interaction information.
  • Herbal products: St. John’s Wort (hypericum perforatum) may induce hepatic enzymes (cytochrome P450) and p-glycoprotein transporter and may reduce the effectiveness of contraceptive steroids. This may also result in breakthrough bleeding.
  • Increase in plasma levels of estradiol associated with co-administered drugs:
    • Atorvastatin : Co-administration of atorvastatin and certain combination oral contraceptives containing ethinyl estradiol increase AUC values for ethinyl estradiol by approximately 20%.
    • Ascorbic acid and acetaminophen may increase plasma ethinyl estradiol levels, possibly by inhibition of conjugation.
    • CYP3A4 inhibitors such as itraconazole or ketoconazole may increase plasma hormone levels.

[edit] PREGNANCY AND LACTATION

  • Pregnancy: There is little or no increased risk of birth defects in women who inadvertently use COCs during early pregnancy. Epidemiologic studies and meta-analyses have not found an increased risk of genital or non-genital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to low dose COCs prior to conception or during early pregnancy.
  • Nursing mothers: Small amounts of oral contraceptive steroids and/or metabolites have been identified in the milk of nursing mothers and a few adverse effects on the child have been reported, including jaundice and breast enlargement. In addition, combination oral contraceptives given in the postpartum period may interfere with lactation by decreasing the quantity and quality of breast milk. If possible, the nursing mother should be advised not to use combination oral contraceptives but to use other forms of contraception until she has completely weaned her child.

[edit] SIDE EFFECTS

The most frequent adverse reactions are premenstrual syndrome (physical and mood disturbances that occur in the last half of a woman's menstrual cycle after ovulation), headache /migraine, menstrual irregularities, breast pain/tenderness/discomfort, nausea/vomiting, abdominal pain/tenderness/discomfort and mood changes.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES