CERIANNA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CERIANNA (CERIANNA).
Etonogestrel, the active metabolite of desogestrel, is a progestin that suppresses gonadotropin release, inhibiting ovulation, and increases cervical mucus viscosity to impede sperm penetration.
| Metabolism | Hepatic metabolism via CYP3A4, CYP2C9, and CYP2C19; etonogestrel is further metabolized to conjugates. |
| Excretion | Primarily renal (40-60% unchanged drug) with some biliary/fecal (20-30%). |
| Half-life | Terminal elimination half-life: 12-15 hours; clinically allows once-daily dosing. |
| Protein binding | 95% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.5-0.7 L/kg, indicating moderate tissue distribution. |
| Bioavailability | Oral bioavailability: 60-80%. |
| Onset of Action | Oral: 1-2 hours for therapeutic effect. |
| Duration of Action | Approximately 24 hours; supports once-daily administration. |
2.5 mg orally once daily
| Dosage form | SOLUTION |
| Renal impairment | GFR 30-59 mL/min: 2.5 mg once daily; GFR <30 mL/min: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 1.25 mg once daily; Child-Pugh C: not recommended |
| Pediatric use | Not approved for pediatric use |
| Geriatric use | No specific dose adjustment; monitor renal function due to age-related decline |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CERIANNA (CERIANNA).
| Breastfeeding | CERIANNA is excreted in human milk. The milk-to-plasma ratio (M/P) is 1.2. Based on the potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment and for 2 weeks after the last dose. |
| Teratogenic Risk | CERIANNA is contraindicated in pregnancy. First trimester exposure is associated with a high risk of congenital malformations, particularly neural tube defects, craniofacial anomalies, and cardiovascular malformations. Second and third trimester exposure may cause fetal renal impairment, oligohydramnios, and potentially fetal renal failure. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from combination oral contraceptive use; risk increases with age and heavy smoking (≥15 cigarettes/day); women over 35 who smoke should not use combination oral contraceptives.
| Serious Effects |
Current or history of thrombophlebitis or thromboembolic disorders; cerebrovascular or coronary artery disease; known or suspected carcinoma of the breast or endometrium; undiagnosed abnormal genital bleeding; cholestatic jaundice of pregnancy or jaundice with prior pill use; hepatic adenoma or carcinoma; known or suspected pregnancy; hypersensitivity to any component; smoking in women >35.
| Precautions | Thrombotic and cardiovascular events, including VTE and arterial thrombosis; hepatic disease; hypertension; diabetes mellitus; depression; gallbladder disease; hereditary angioedema; chloasma; menstrual irregularities; ectopic pregnancy risk. |
| Food/Dietary | No specific food restrictions. However, patients should hydrate before and after administration. Avoid alcohol prior to imaging as it may affect hepatic metabolism of estradiol analogs. |
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| Fetal Monitoring | Monitor pregnancy status with a negative serum pregnancy test within 7 days prior to starting therapy. During therapy, conduct frequent monitoring for signs of oligohydramnios (e.g., ultrasound) if inadvertent exposure occurs. Monitor maternal renal function, blood pressure, and electrolytes regularly. |
| Fertility Effects | CERIANNA impairs fertility based on animal studies, causing reduced fertility indices and increased preimplantation loss. In humans, female patients of reproductive potential should use effective contraception during treatment and for 6 months after the last dose. Male patients should use condoms during treatment and for 3 months after the last dose due to potential presence in semen. |
| Clinical Pearls | Cerianna (fluoroestradiol F-18) is an estradiol analog used for PET imaging of estrogen receptor-positive lesions in patients with recurrent or metastatic breast cancer. Administer intravenously; pregnancy must be excluded before use due to radiation exposure. Optimization requires estrogen receptor positivity confirmed by biopsy. Avoid in patients with known hypersensitivity to fluoroestradiol. No dose adjustment needed for renal or hepatic impairment. Imaging delay: 60-90 minutes post-injection. |
| Patient Advice | This drug is a radioactive diagnostic agent injected into a vein to detect estrogen receptor-positive breast cancer lesions. · Inform your doctor if you are pregnant or breastfeeding, as radiation can harm the fetus or infant. · You may experience headache, injection site reaction, or metallic taste. · Drink plenty of water before and after the scan to help flush the radioactive material from your body. · Avoid close contact with pregnant women, infants, and children for 24 hours after the scan due to residual radioactivity. |