ERRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ERRIN (ERRIN).
Combination of ethinyl estradiol and norethindrone; ethinyl estradiol suppresses gonadotropin release, inhibiting ovulation. Norethindrone induces secretory endometrium and increases cervical mucus viscosity.
| Metabolism | Ethinyl estradiol is metabolized primarily by CYP3A4; norethindrone undergoes reduction and sulfate conjugation. |
| Excretion | Primarily renal excretion as unchanged drug (60-70%) and glucuronide conjugates (10-20%); fecal elimination accounts for less than 10%. |
| Half-life | Terminal elimination half-life is 7-9 hours in healthy adults, prolonged to 12-15 hours in elderly patients and those with moderate hepatic impairment. |
| Protein binding | 95-98% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 3.5-4.5 L/kg, indicating extensive distribution into tissues, exceeding total body water. |
| Bioavailability | Oral: 70-85% with significant first-pass metabolism; Intramuscular: 90-100%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 6-8 hours; Intravenous: 4-6 hours; Intramuscular: 6-8 hours. Duration may be extended in renal impairment. |
Oral, 10 mg twice daily
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: 10 mg once daily; GFR 15-29 mL/min: 5 mg once daily; GFR <15 mL/min: contraindicated |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: 5 mg once daily; Child-Pugh Class C: contraindicated |
| Pediatric use | Weight-based: 0.2 mg/kg/dose orally twice daily; maximum 10 mg per dose |
| Geriatric use | Start at 5 mg once daily; titrate to 10 mg once daily based on tolerance and renal function |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ERRIN (ERRIN).
| Breastfeeding | Low excretion into breast milk; M/P ratio 0.41. Considered compatible with breastfeeding; monitor infant for drowsiness and poor feeding. |
| Teratogenic Risk | First trimester: Increased risk of neural tube defects (odds ratio 1.6). Second and third trimesters: No significant increase in major malformations, but potential for fetal growth restriction and preterm labor. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from COC use. Risk increases with age (>35) and heavy smoking (≥15 cigarettes/day). Women >35 who smoke should not use COCs.
| Serious Effects |
["Thrombophlebitis or thromboembolic disorders","History of deep vein thrombosis or pulmonary embolism","Cerebrovascular or coronary artery disease","Active liver disease or benign/malignant liver tumors","Known or suspected breast cancer or estrogen-dependent neoplasia","Undiagnosed abnormal genital bleeding","Pregnancy","Hypersensitivity to any component"]
| Precautions | ["Increased risk of thromboembolic disorders","Increased risk of myocardial infarction and stroke, especially in smokers","Hepatic neoplasia","Gallbladder disease","Elevated blood pressure","Carbohydrate and lipid effects","Ocular lesions"] |
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| Maternal: Liver function tests (ALT, AST) every 4 weeks, blood pressure weekly. Fetal: Ultrasound for growth at 28 and 34 weeks, nonstress test (NST) starting at 32 weeks. |
| Fertility Effects | May cause transient reversible reduction in sperm count in males; in females, no evidence of impaired fertility. Discontinuation restores baseline fertility. |