norelgestromin/ethinyl estradiol(redirected from Ortho Evra)
Pharmacologic class: Estrogen
Therapeutic class: Hormone
Pregnancy risk category X
FDA Box Warning
Cigarette smoking increases risk of serious cardiovascular adverse effects from hormonal contraceptive use. Risk increases with age and with heavy smoking (15 or more cigarettes per day) and is quite marked in women older than age 35. Strongly advise women who use hormonal contraceptives not to smoke.
Risk of venous thromboembolism (VTE) among women ages 15 to 44 who used the transdermal patch compared to women who used oral contraceptives containing 30 to 35 mcg of ethinyl estradiol (EE) and either levonorgestrel or norgestimate was assessed in four U.S. case-control studies using electronic health care claims data. Odds ratios ranged from 1.2 to 2.2; one of the studies found a statistically significant increased risk of VTE for current patch users.
The pharmacokinetic (PK) profile for the transdermal patch is different from the PK profile for oral contraceptives in that it has higher steady state concentrations and lower peak concentrations. Area under the time-concentration curve and average concentration at steady state for EE are approximately 60% higher in women using the patch compared with women using an oral contraceptive containing 35 mcg of EE. In contrast, peak concentrations for EE are approximately 25% lower in women using the patch. It's unknown whether there are changes in risk of serious adverse events based on the differences in PK profiles of EE in women using the patch compared with women using oral contraceptives containing 30 to 35 mcg of EE. Increased estrogen exposure may increase risk of adverse events, including VTE.
Suppresses gonadotropin and inhibits ovulation by causing changes in cervical mucus and endometrium, thereby preventing egg implantation
Transdermal patch: 6 mg norelgestro-min and 0.75 mg ethinyl estradiol (releases 150 mcg norelgestromin and 20 mcg ethinyl estradiol q 24 hours)
Indications and dosages
➣ To prevent pregnancy
Adults: Apply patch on day 1 of menstrual cycle (or first Sunday after period begins). Change patch weekly thereafter for 3 weeks (on same day each week), and then remove patch for fourth week. Repeat q month.
• Hypersensitivity to drug or its components
• Undiagnosed abnormal genital bleeding
• Known or suspected breast cancer or history of such cancer
• Endometrial carcinoma or other known or suspected estrogen-dependent neoplasia
• Thromboembolism, history of thromboembolic disease, known thrombophilic conditions
• Current or past cerebrovascular or coronary artery disease
• Valvular heart disease with complications
• Diabetes with vascular involvement
• Persistent blood pressure values at or above 160 mm Hg systolic or 100 mm Hg diastolic
• Headache with focal neurologic symptoms
• Cholestatic jaundice of pregnancy, jaundice with previous hormonal contraceptive use
• Acute or chronic hepatic disease with abnormal liver function
• Hepatic adenomas or carcinomas
• Major surgery with prolonged immobilization
• Known or suspected pregnancy
Use cautiously in:
• cardiovascular disease, renal disease, asthma, bone disease, migraine, lipid disorders, fibrocystic breasts, increased risk for endometrial cancer, sexually transmitted diseases
• family history of breast or genital tract cancer
• abnormal mammogram
• elderly patients (use not indicated)
• women with body weight at or abovel98 lb (90 kg)
• breastfeeding patients
• children before menarche (use not indicated).
• Apply patch to clean, dry, intact skin on buttock, abdomen, upper torso, or upper outer arm.
• Change patch on same day each week (except for fourth week, when patch is removed).
CNS: headache, dizziness, lethargy, depression, emotional lability, increased risk of cerebrovascular accident
CV: edema, hypertension, myocardial infarction, thromboembolism
EENT: contact lens intolerance, worsening of myopia or astigmatism
GI: nausea, vomiting, jaundice, abdominal cramps, bloating, anorexia, gallbladder disease, pancreatitis
GU: amenorrhea, dysmenorrhea, breakthrough bleeding, cervical erosion, vaginal candidiasis, breast tenderness, breast enlargement or secretion, menstrual cramps, libido loss, increased risk of breast or endometrial cancer
Hepatic: cholestatic jaundice, hepatic adenoma
Metabolic: hyperglycemia, hypercal-cemia, sodium and water retention
Musculoskeletal: leg cramps
Respiratory: upper respiratory infection, pulmonary embolism
Skin: acne, oily skin, increased pigmentation, urticaria, patch site reaction
Other: increased appetite, weight changes
Drug-drug. Acetaminophen, ascorbic acid, atorvastatin, miconazole (vaginal capsules): increased ethinyl estradiol blood level
Antibiotics, barbiturates, carbamazepine, fosphenytoin, phenobarbital, phenytoin, rifampin: decreased contraceptive efficacy
Corticosteroids: enhanced corticosteroid effects
Cyclosporine: increased risk of cyclosporine toxicity
CYP3A4 inhibitors (such as ketocona-zole, itraconazole): increased hormone level
Dantrolene, other hepatotoxic drugs: increased risk of hepatotoxicity
Insulin, oral hypoglycemics, warfarin: altered requirements for these drugs Protease inhibitors: increased contraceptive metabolism
Tamoxifen: interference with tamoxifen effects
Drug-diagnostic tests. Antithrombin III, folate, low-density lipoproteins, pyri-doxine, total cholesterol, urine pregnane-diol: decreased levels
Cortisol; factors VII, VIII, IX, and X; glucose; high-density lipoproteins; phos-pholipids; prolactin; prothrombin; sodium; triglycerides: increased levels
Metyrapone test: false decrease Thyroid function tests: false interpretation
Drug-food. Caffeine: increased blood caffeine level
Drug-herbs. Black cohosh: increased adverse drug effects
Red clover: interference with hormonal therapy
Saw palmetto: antiestrogenic effects St. John's wort: decreased drug blood level and effects
Drug-behaviors. Smoking (15 or more cigarettes daily): increased risk of adverse cardiovascular reactions
• Evaluate menstrual pattern.
Monitor blood pressure. Watch for signs and symptoms of thrombo-embolic disease (swelling or warmth in calf, sudden chest pain, shortness of breath).
• Check blood glucose level in diabetic patient.
• Instruct patient to start using patch on first day of menstrual period or on first Sunday after period starts. Advise her to use calendar to keep track of which day each week to change patch.
• Tell patient to remove patch during fourth week of each cycle. Explain that she will have bleeding that week.
• Advise patient to check daily to ensure that patch is attached firmly to skin. Explain that if patch is detached for 1 day or less, she should try to reattach it more firmly. If patch is detached for more than 1 day or for an unknown length of time, she should start with new patch and new calendar.
• Instruct patient to use alternative contraception during first week of patch use.
Inform patient that smoking while using patch increases risk of thrombo-embolic disease and other serious cardiovascular reactions. Stress importance of not smoking. Tell her to immediately report swelling or warmth in calf, chest pain, or shortness of breath.
• Advise breastfeeding patient to use other forms of contraception until she has completely weaned her infant.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.