ORTHO-NOVUM 1/80 28
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORTHO-NOVUM 1/80 28 (ORTHO-NOVUM 1/80 28).
Combination estrogen-progestin contraceptive; primarily inhibits ovulation by suppressing gonadotropin release (FSH and LH). Also increases cervical mucus viscosity and alters endometrial receptivity.
| Metabolism | Ethinyl estradiol is metabolized primarily via CYP3A4 and undergoes glucuronidation; norethindrone is metabolized via reduction and conjugation. |
| Excretion | Norethindrone: 50-60% renal, 20-30% fecal; mestranol: 30-40% renal, 60-70% fecal. |
| Half-life | Norethindrone: 7-8 hours; mestranol: 10-13 hours (terminal). Steady-state achieved in 5-7 days. |
| Protein binding | Norethindrone: 60-80% bound to albumin and SHBG; mestranol: 90-95% bound to albumin and SHBG. |
| Volume of Distribution | Norethindrone: 2-4 L/kg; mestranol: 1-3 L/kg. Indicates extensive tissue distribution. |
| Bioavailability | Oral: norethindrone 50-65%, mestranol 40-60% due to first-pass metabolism. |
| Onset of Action | Oral: 1-2 hours for serum levels; contraceptive effect requires 7 days of continuous use. |
| Duration of Action | 24 hours dosing interval; contraceptive protection lasts as long as taken regularly. Withdrawal bleed 2-4 days after last active pill. |
One tablet orally once daily at the same time each day for 28 days (21 active tablets containing norethindrone 1 mg and ethinyl estradiol 80 mcg, followed by 7 placebo tablets).
| Dosage form | TABLET |
| Renal impairment | No specific dose adjustment recommended; use with caution in patients with renal impairment due to potential fluid retention. GFR-based modifications not established. |
| Liver impairment | Contraindicated in patients with Child-Pugh class C cirrhosis. Use with caution in Child-Pugh class A or B; consider alternative contraception due to risk of decreased hormone clearance. |
| Pediatric use | Not indicated for premenarchal girls. For postmenarchal adolescents, same dosing as adults: one tablet orally once daily for 28 days. |
| Geriatric use | Not indicated for use in postmenopausal women. No geriatric dosing established; use not recommended in women over 50 years due to increased risk of thromboembolism and lack of efficacy for contraception. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ORTHO-NOVUM 1/80 28 (ORTHO-NOVUM 1/80 28).
| Breastfeeding | Excreted in breast milk; may reduce milk production and affect infant. M/P ratio not well established. Avoid use during breastfeeding. |
| Teratogenic Risk | First trimester: No consistent evidence of major malformations, but oral contraceptives are not recommended due to potential risk. Second/third trimester: No specific fetal risks; exposure is not advised due to hormonal effects. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptives. Risk increases with age and smoking intensity, especially in women over 35 years of age. Women using oral contraceptives should be strongly advised not to smoke.
| Serious Effects |
["Known or suspected pregnancy","Current or past thrombophlebitis or thromboembolic disorders","Cerebrovascular or coronary artery disease","Known or suspected breast carcinoma","Known or suspected estrogen-dependent neoplasia","Undiagnosed abnormal genital bleeding","Cholestatic jaundice of pregnancy or jaundice with prior oral contraceptive use","Hepatic adenoma or carcinoma","Known or suspected hypersensitivity to any component"]
| Precautions | ["Increased risk of thromboembolic disorders","Cerebrovascular disease","Myocardial infarction","Breast cancer risk","Hepatic neoplasia","Elevated blood pressure","Gallbladder disease","Glucose intolerance","Ocular lesions","Headache","Menstrual irregularities","Depression","Contact lens intolerance","Fluid retention","Lipid effects"] |
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| Monitor blood pressure, glucose, and liver function if inadvertently used in pregnancy. Fetal ultrasound if prolonged exposure. |
| Fertility Effects | Suppresses ovulation during use; normal fertility returns upon discontinuation. No permanent impairment. |