Comparative Pharmacology
Head-to-head clinical analysis: ORTHO EVRA versus ORTHO CEPT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ORTHO EVRA versus ORTHO CEPT.
ORTHO EVRA vs ORTHO-CEPT
Head-to-head clinical comparison of therapeutic indices and safety profiles.
Combination hormonal contraceptive containing ethinyl estradiol and norelgestromin. Ethinyl estradiol suppresses gonadotropin (FSH and LH) release, preventing ovulation. Norelgestromin is a progestin that also inhibits ovulation and induces changes in cervical mucus and endometrium to impede sperm penetration and implantation.
Combination oral contraceptive containing desogestrel and ethinyl estradiol. Inhibits ovulation by suppressing gonadotropin secretion; increases viscosity of cervical mucus, impeding sperm penetration; alters endometrial development.
Prevention of pregnancy in women who choose to use a transdermal patch as their method of contraception
Prevention of pregnancy
Transdermal: Apply one patch (releases 150 mcg norelgestromin and 20 mcg ethinyl estradiol per 24 hours) weekly for 3 weeks, followed by 1 patch-free week. Apply to clean, dry, intact skin on lower abdomen, buttock, upper arm, or upper torso (excluding breasts).
One tablet (0.15 mg desogestrel / 0.03 mg ethinyl estradiol) orally once daily at the same time each day for 21 days, followed by 7 placebo tablets (or 7 hormone-free days).
None Documented
None Documented
Norelgestromin: ~28 hours (range 21-36) allowing weekly dosing; Ethinyl estradiol: ~17 hours (range 13-21)
Desogestrel: 23 hours (terminal), Etonogestrel active metabolite: 30 hours (terminal); clinical steady state after 7-10 days
Ethinyl estradiol is primarily metabolized by CYP3A4, with conjugation to sulfate and glucuronide. Norelgestromin is extensively metabolized via reduction to norgestrel and conjugation, with CYP3A4/5 involved in minor pathways.
Ethinyl estradiol: primarily metabolized by CYP3A4; desogestrel: prodrug converted to active metabolite etonogestrel via CYP2C9 and CYP2C19.
Renal: ~50% (as glucuronide conjugates of norelgestromin and ethinyl estradiol); Fecal: ~35% (as metabolites); Biliary: minor
Renal: 50% (metabolites), Biliary/fecal: 40% (metabolites and unchanged drug), 10% unchanged in urine
Norelgestromin: >99% bound (albumin and SHBG); Ethinyl estradiol: ~97% bound (albumin, not SHBG)
Desogestrel: 99% (SHBG), Etonogestrel: ~66% (albumin and SHBG); Ethinyl estradiol: 98% (albumin)
Norelgestromin: ~2.4 L/kg; Ethinyl estradiol: ~4.3 L/kg; indicates extensive tissue distribution
Desogestrel: 1.5 L/kg, Etonogestrel: 1.7 L/kg; indicates extensive tissue distribution
Transdermal: ~100% systemic absorption; oral norelgestromin: ~60% (not administered orally)
Desogestrel: 76% (oral, as prodrug converted to etonogestrel); Ethinyl estradiol: 45-50% (oral, first-pass metabolism)
No dose adjustment recommended for mild to moderate renal impairment. Contraindicated in severe renal impairment or end-stage renal disease (CrCl <30 mL/min).
No dose adjustment required for mild to moderate renal impairment. Limited data in severe renal impairment; use is not recommended due to potential fluid/electrolyte disturbances.
Contraindicated in acute or chronic hepatic disease, including Child-Pugh class A, B, or C cirrhosis. Discontinue if jaundice develops.
Contraindicated in Child-Pugh class B or C (severe hepatic impairment) and in acute liver disease. Caution in Child-Pugh class A; monitor liver function; consider alternative method.
Not indicated for use prior to menarche. For postmenarchal adolescents, dosing is same as adults: apply patch weekly for 3 weeks, then 1 week off.
Post-menarchal adolescents: Same dosing regimen as adults (1 tablet daily). Not indicated for use before menarche.
Not indicated for use after menopause. No specific geriatric dosing studies; use not recommended due to lack of need for contraception in this population.
Not indicated for use in postmenopausal women. Contraceptive efficacy not applicable; estrogen-containing combination contraceptives are generally not recommended in women over 35 who smoke or have other cardiovascular risk factors.
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptives. This risk increases with age, especially in women over 35 years, and with the number of cigarettes smoked. Women who use combination hormonal contraceptives should be strongly advised not to smoke.
Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptives. Women over 35 who smoke should not use this product.
["Increased risk of venous thromboembolism (VTE) including deep vein thrombosis and pulmonary embolism, especially in women with risk factors","Increased risk of arterial thrombotic events (e.g., myocardial infarction, stroke) particularly in smokers and women with hypertension or migraine with aura","Hepatic neoplasia (benign and malignant) reported; discontinue if jaundice or liver function abnormalities develop","Elevated blood pressure; monitor and discontinue if hypertension becomes significant","Gallbladder disease and cholestasis","Glucose intolerance; use with caution in diabetic women","Headache including migraine; discontinue if new or worsening migraine develops","Ocular lesions (e.g., retinal thrombosis); discontinue if sudden partial or complete vision loss occurs","Depression; monitor and discontinue if severe","Reduced efficacy in women weighing ≥90 kg (198 lbs); consider alternative contraception","Detachment or incomplete adhesion of patch; instruct on proper use"]
["Thrombotic disorders (venous thromboembolism, arterial thromboembolism)","Cerebrovascular disease","Cigarette smoking in women >35 years","Hypertension","Gallbladder disease","Hepatic neoplasia","Bleeding irregularities"]
["Thrombophlebitis, venous thromboembolism, or thromboembolic disorders (current or history)","Cerebrovascular or coronary artery disease","Known or suspected breast carcinoma or other estrogen-dependent neoplasia","Undiagnosed abnormal genital bleeding","Cholestatic jaundice of pregnancy or jaundice with prior hormonal contraceptive use","Hepatic adenoma or carcinoma, or active liver disease","Known or suspected pregnancy","Hypersensitivity to ethinyl estradiol, norelgestromin, or any component of the patch","Heavy smoking (≥15 cigarettes/day) in women over 35 years of age"]
["High risk of arterial or venous thrombotic events","Current or history of breast cancer or other estrogen-sensitive cancer","Hepatic adenoma or carcinoma","Undiagnosed abnormal uterine bleeding","Pregnancy","Hypersensitivity to any component"]
Data Pending Review
Data Pending Review
No specific food interactions. Grapefruit juice may increase estrogen exposure but clinical relevance uncertain.
Grapefruit juice may increase ethinyl estradiol levels via CYP3A4 inhibition, but effect is minor; typical dietary intake does not require restriction. High-fat meals may delay absorption but no dose adjustment needed. Maintain consistent dietary patterns for peak concentration predictability.
First trimester: Epidemiologic studies have not found an increased risk of major birth defects following inadvertent use of combination hormonal contraceptives (CHCs) in early pregnancy. Second and third trimesters: Use is contraindicated; exposure during gestation has been associated with fetal harm, including cardiovascular anomalies and masculinization of female fetuses (androgenic effects from progestin).
Contraindicated during pregnancy due to risk of fetal harm. First trimester exposure linked to cardiovascular defects and limb reduction defects. Second and third trimester exposure associated with fetal genital abnormalities and potential long-term effects from progestin activity.
CHCs reduce milk production and may affect composition. The manufacturer recommends avoiding use until breastfeeding is fully established (typically 6 months postpartum). Norelgestromin and ethinyl estradiol are excreted in breast milk; milk-to-plasma ratio not specified. Use an alternative contraceptive method during breastfeeding.
Small amounts of desogestrel and ethinyl estradiol excreted in breast milk; M/P ratio not well established. Use not recommended during breastfeeding as it may reduce milk production and quality. Alternative contraception advised.
Contraindicated in pregnancy. No dose adjustments apply as use is prohibited. Pharmacokinetic changes in pregnancy (increased clearance of steroids) are not relevant due to contraindication.
Not applicable; contraindicated in pregnancy. No dose adjustment recommendations exist as use is not recommended.
Category C
Category C
Ortho Evra is a combined hormonal contraceptive patch. Efficacy may be reduced in women weighing >90 kg. Patches are applied weekly for 3 weeks followed by a patch-free week. If patch falls off <24h, reapply; if >24h, start new cycle with backup contraception. Drug interactions include CYP3A4 inducers (e.g., rifampin) potentially reducing efficacy. Increased risk of thromboembolism, especially in smokers >35 years. Avoid in migraine with aura, uncontrolled hypertension, or history of VTE.
ORTHO-CEPT (desogestrel/ethinyl estradiol) is a monophasic oral contraceptive. Counsel patients that missed pills increase risk of breakthrough bleeding and pregnancy; refer to package insert for missed dose instructions. Consider reduced efficacy with hepatic enzyme inducers (e.g., rifampin, phenytoin). Caution in patients with migraine with aura due to increased stroke risk. May cause chloasma; advise sun protection.
Apply the patch to clean, dry, intact skin on buttock, abdomen, upper arm, or upper torso (avoid breasts).Change the patch on the same day of the week for 3 weeks, then no patch for 1 week.If the patch falls off and is off for less than 24 hours, reapply the same patch or replace with a new one; no backup needed.If the patch is off for more than 24 hours, start a new 4-week cycle with a new patch and use backup contraception for 7 days.Do not cut or alter the patch; apply immediately after opening.Report symptoms of DVT (leg pain/swelling, chest pain, sudden shortness of breath, headache, vision changes) immediately.
Take one pill daily at the same time each day for 21 days, then 7 placebo pills.If you vomit or have severe diarrhea within 4 hours of taking a pill, use backup contraception for 7 days.Do not smoke while taking this medication due to increased risk of blood clots.Inform your healthcare provider if you develop severe headache, chest pain, shortness of breath, or leg swelling.Use additional contraception if you miss two or more active pills in a row.