ORTHO-CEPT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORTHO-CEPT (ORTHO-CEPT).
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.
| Metabolism | Ethinyl estradiol: primarily metabolized by CYP3A4; desogestrel: prodrug converted to active metabolite etonogestrel via CYP2C9 and CYP2C19. |
| Excretion | Renal: 50% (metabolites), Biliary/fecal: 40% (metabolites and unchanged drug), 10% unchanged in urine |
| Half-life | Desogestrel: 23 hours (terminal), Etonogestrel active metabolite: 30 hours (terminal); clinical steady state after 7-10 days |
| Protein binding | Desogestrel: 99% (SHBG), Etonogestrel: ~66% (albumin and SHBG); Ethinyl estradiol: 98% (albumin) |
| Volume of Distribution | Desogestrel: 1.5 L/kg, Etonogestrel: 1.7 L/kg; indicates extensive tissue distribution |
| Bioavailability | Desogestrel: 76% (oral, as prodrug converted to etonogestrel); Ethinyl estradiol: 45-50% (oral, first-pass metabolism) |
| Onset of Action | Oral: 7 days (full contraceptive effect when started on day 1 of cycle); immediate if started within first 5 days with backup |
| Duration of Action | Oral: 24 hours (daily dosing required); contraceptive protection maintained with consistent daily use |
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).
| Dosage form | TABLET |
| Renal impairment | 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. |
| Liver impairment | 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. |
| Pediatric use | Post-menarchal adolescents: Same dosing regimen as adults (1 tablet daily). Not indicated for use before menarche. |
| Geriatric use | 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. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ORTHO-CEPT (ORTHO-CEPT).
| 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. |
| Teratogenic Risk | 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. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptives. Women over 35 who smoke should not use this product.
| Serious Effects |
["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"]
| Precautions | ["Thrombotic disorders (venous thromboembolism, arterial thromboembolism)","Cerebrovascular disease","Cigarette smoking in women >35 years","Hypertension","Gallbladder disease","Hepatic neoplasia","Bleeding irregularities"] |
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| Fetal Monitoring |
| If unintentional exposure occurs during pregnancy, monitor fetal development via ultrasound for structural anomalies. No routine monitoring required if contraindication is observed. |
| Fertility Effects | Reversible suppression of ovulation. Normal fertility typically resumes after discontinuation. No long-term negative impact on fertility. |