Introduction
Opill (norgestrel) is a progestin-only oral contraceptive tablet recently approved by the FDA for over-the-counter use. It represents the first daily oral contraceptive available without a prescription in the United States, marking a significant advancement in reproductive healthcare access. This monograph provides comprehensive information about Opill for healthcare professionals and patients.
Mechanism of Action
Norgestrel, the active ingredient in Opill, is a synthetic progestin that exerts its contraceptive effects through multiple mechanisms:
- Cervical mucus thickening: Increases viscosity of cervical mucus, creating a barrier to sperm penetration
- Endometrial changes: Alters endometrial lining, making it less receptive to implantation
- Pituitary suppression: Inhibits gonadotropin secretion, which may suppress ovulation in some cycles
- Tubal motility: May affect fallopian tube motility, potentially impairing ovum transport
Indications
- Contraception: Prevention of pregnancy in individuals of reproductive potential
- No additional FDA-approved indications (Unlike combination oral contraceptives, progestin-only pills are not typically indicated for acne, menstrual regulation, or other non-contraceptive uses)
Dosage and Administration
Standard dosing: One tablet (0.075 mg norgestrel) orally once daily Administration:- Take at approximately the same time each day
- May be taken with or without food
- If vomiting occurs within 3-4 hours of ingestion, consider it a missed dose
- Postpartum: May initiate immediately postpartum (non-breastfeeding) or after 4 weeks (breastfeeding)
- Post-abortion: May begin immediately following first or second trimester abortion
- Adolescents: Same dosing as adults; no dosage adjustment required
- Renal impairment: No specific recommendations; use with caution
- Hepatic impairment: Contraindicated in patients with hepatic disease
Pharmacokinetics
Absorption: Norgestrel is rapidly absorbed after oral administration with peak plasma concentrations occurring within 1-2 hours Distribution:- Protein binding: Approximately 78% bound to sex hormone-binding globulin (SHBG) and albumin
- Volume of distribution: Approximately 1.6 L/kg
- Half-life: Approximately 16-20 hours
- Excretion: Primarily renal (45-50%) and fecal (32-36%)
Contraindications
- Current or history of breast cancer
- Known or suspected pregnancy
- Undiagnosed abnormal genital bleeding
- Hepatic tumors (benign or malignant) or active liver disease
- Hypersensitivity to any component of Opill
Warnings and Precautions
Ectopic pregnancy: Consider ectopic pregnancy in users with abdominal pain; progestin-only pills have a higher rate of ectopic pregnancy than combination oral contraceptives Ovarian cysts: May occur and usually resolve spontaneously Breast cancer risk: Current information suggests possible increased risk; benefits should be weighed against risks Liver function: Discontinue if jaundice develops Carbohydrate metabolism: May decrease glucose tolerance; monitor diabetic patients Lipid effects: May adversely affect lipid metabolism Bleeding patterns: Irregular bleeding common, especially during first few months of useDrug Interactions
Strong CYP3A4 inducers:- Rifampin, carbamazepine, phenytoin, St. John's wort
- May decrease norgestrel concentrations, reducing efficacy
- Alternative contraception recommended
- Bosentan, efavirenz, modafinil
- May decrease norgestrel concentrations
- Consider additional contraceptive protection
- Protease inhibitors and non-nucleoside reverse transcriptase inhibitors may affect norgestrel levels
- Consult specific interaction resources
Adverse Effects
Very common (>10%):- Irregular menstrual bleeding patterns
- Headache
- Nausea
- Breast tenderness
- Dizziness
- Fatigue
- Acne
- Weight changes
- Mood changes
- Ectopic pregnancy
- Ovarian cysts
- Thrombotic events (very rare compared to combination oral contraceptives)
Monitoring Parameters
- Pregnancy testing: As clinically indicated for suspected pregnancy
- Blood pressure: Periodically (though less concern than with estrogen-containing contraceptives)
- Bleeding patterns: Assess during first 3-6 months of use
- Breast examination: Routine clinical breast exams as appropriate
- Symptoms suggesting ectopic pregnancy: Abdominal pain, irregular bleeding
Patient Education
Dosing instructions:- Take at the same time every day (set a daily reminder)
- If missed by >3 hours, use backup contraception for 48 hours
- Typical use efficacy: Approximately 91%
- Perfect use efficacy: Approximately 98%
- Irregular bleeding common initially; usually improves after 3-6 months
- Report persistent irregular bleeding, severe abdominal pain, or jaundice
- Does not protect against sexually transmitted infections
- Continue taking during menstrual periods
- Store at room temperature
- Check expiration date
- Suspected pregnancy
- Severe abdominal pain
- Heavy prolonged bleeding
- Symptoms of blood clots (leg pain, chest pain, shortness of breath)
References
1. FDA Approval Package for Opill (norgestrel) tablets. FDA.gov 2. Curtis KM, Jatlaoui TC, Tepper NK, et al. U.S. Selected Practice Recommendations for Contraceptive Use, 2016. MMWR Recomm Rep. 2016;65(4):1-66. 3. Committee on Practice Bulletins-Gynecology. Practice Bulletin No. 152: Emergency Contraception. Obstet Gynecol. 2015;126(3):e1-e11. 4. Shrader SP, Dickerson LM. Progestin-only oral contraceptives. Am Fam Physician. 2004;70(11):2127-2134. 5. Gemzell-Danielsson K, Buhling KJ, Dermout SM, et al. Expert review on the use of progestin-only pills for contraception. Eur J Contracept Reprod Health Care. 2020;25(6):421-428. 6. Lopez LM, Grey TW, Stuebe AM, Chen M, Truitt ST, Gallo MF. Combined hormonal versus nonhormonal versus progestin-only contraception in lactation. Cochrane Database Syst Rev. 2015;(3):CD003988.