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[×] Vaginal ring
 BRAND NAMES
- International: Cilest
- UK: Cilest (21 tablets 0,035 mg Ethinyl Estradiol and Norgestimate 0.25 mg)
- MonoNessa, Ortho-Cyclen PI, Sprintec (21 tablets 0,035 mg Ethinyl Estradiol and Norgestimate 0.25 mg + 7 placebo tablets)
- Ortho-Tri-Cyclen PI (tablets containing a fixed dose of ethinyl estradiol [0.035 mg] and increasing doses of norgestimate [0.180 mg, 0.215 mg, 0.250 mg]) followed by 7 days of inactive tablets).
 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).
Norgestimate is a third-generation progestin. It combines high progestational activity with minimal intrinsic androgenicity. Its low androgenic effects have resulted in successful treatment of acne.
Ethinyl Estradiol/Norgestimate combination is indicated for use by women to prevent pregnancy.
Triphasic combination of ethinyl estradiol and norgestimate (Ortho-Tri-Cyclen) is an effective treatment for moderate acne vulgaris in females at least 15 years of age with no known contraindication to oral contraceptive therapy
28-pill packages: The possibility of ovulation and conception prior to initiation of medication should be considered.
The patient should be instructed to begin taking the first tablet 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, for 28 days. The failure rate may increase when pills are missed or taken incorrectly.
During the first cycle of Ethinyl Estradiol/Norgestimate, when beginning on the first Sunday after the onset of menstrual period, Ethinyl Estradiol/Norgestimate 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.
21-pill packages: The possibility of ovulation and conception prior to initiation of medication should be considered.
The patient should be instructed to begin taking the first tablet on Day 1 of menstruation. 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, for 21 days, followed by a seven day break from pill-taking. During the seven day break, the levels of the hormones in blood drop, which results in a withdrawal bleed (called Hormone Withdrawal Bleeds) that is similar to normal period.
After the seven pill-free days are up, even if the patient is still bleeding, a new course should be started. After 28 tablets have been taken, a new course should be started
Oral contraceptives should not be used in women who currently have the following conditions:
- Known or suspected pregnancy
- A history of heart attack or stroke
- Blood clots in the legs (thrombophlebitis), lungs (pulmonary embolism), or eyes
- A history of blood clots in the deep veins of your legs
- Hereditary or acquired thrombophilias (a condition that makes blood clot more than normal)
- Chest pain (angina pectoris)
- Known or suspected breast cancer or cancer of the lining of the uterus, cervix, or vagina
- Unexplained vaginal bleeding (until your doctor reaches a diagnosis)
- Hepatitis or yellowing of the whites of your eyes or of the skin (jaundice) during pregnancy or during previous use of hormonal contraceptives
- Benign or cancerous liver tumor (Hepatic adenomas or carcinomas)
- Severe high blood pressure
- Diabetes with complications of the kidneys, eyes, nerves, or blood vessels
- Headaches with neurological symptoms
- Disease of heart valves with complications
- Major surgery with prolonged immobilization
 WARNINGS AND PRECAUTIONS
- Oral contraceptives do not protect against HIV infection (AIDS) and other sexually transmitted diseases such as chlamydia, genital herpes, genital warts, gonorrhea, hepatitis B, and syphilis.
- Cigarette smoking increases the risk of serious cardiovascular (heart and blood vessel problems) from hormonal contraceptives, including death from heart attack, blood clots, or stroke. 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.
- Vascular risks: Stop taking oral contraceptives 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.
- Liver disease: Discontinue if jaundice occurs.
- High blood pressure: Women with significant hypertension or hypertensive with vascular disease, should not be started on hormonal contraception.
- Carbohydrate and lipid metabolic effects: Monitor prediabetic and diabetic women taking oral contraceptives. Consider an alternate contraceptive method for women with uncontrolled dyslipidemia.
- Headache: Evaluate significant change in headaches and discontinue oral contraceptives if indicated.
- Uterine bleeding: Unscheduled (breakthrough) bleeding and spotting sometimes occur in women taking oral contraceptives. Consider non-hormonal causes and take adequate diagnostic measures to rule out malignancy, other pathology, or pregnancy in the event of unscheduled bleeding, as in the case of any abnormal vaginal bleeding. If pathology and pregnancy have been excluded, time or a change to another contraceptive product may resolve the bleeding. Some women may encounter post-pill amenorrhea or oligomenorrhea, especially when such a condition was pre-existent.
- 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 and menstrual irregularities. Examples include: Rifampicin, Barbiturates, Phenylbutazone, Phenytoin, Carbamazepine, Felbamate, Oxcarbazepine, Topiramate, Griseofulvin , Ampicillin and other penicillins and tetracyclines (Certain antibiotics may decrease enterohepatic circulation of estrogens).
- Anti-HIV Protease inhibitors: some protease inhibitors may decrease the plasma levels of the estrogen and progestin. 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.
- Combined hormonal contraceptives have been shown to significantly decrease plasma concentrations of lamotrigine when co-administered due to induction of lamotrigine glucuronidation. This may reduce seizure control; therefore, dosage adjustments of lamotrigine may be necessary.
- 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.
 PREGNANCY AND LACTATION
- Pregnancy Category X (US)
- Nursing mothers: Not recommended; can decrease milk production. Ethinyl Estradiol/Norgestimate can be started no earlier than 4 weeks after delivery, in women who are not breastfeeding.
 SIDE EFFECTS
Possible adverse reactions include: headache, vaginal candidiasis, nausea, menstrual cramps, breast tenderness, vaginitis (bacterial), abnormal cervical smear, urinary tract infection, mood swings including depression, weight gain, vomiting, and metrorrhagia (abnormal bleeding between periods). (See also WARNINGS AND PRECAUTIONS for serious possible adverse events)