XULANE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XULANE (XULANE).
Ethinyl estradiol and norelgestromin (the active metabolites of norgestimate) suppress gonadotropin release, inhibiting ovulation and increasing cervical mucus viscosity, impairing sperm penetration.
| Metabolism | Ethinyl estradiol is metabolized primarily via CYP3A4; norgestimate is metabolized to the active metabolite norelgestromin by first-pass hepatic metabolism and further metabolized by CYP3A4 and CYP2C19. |
| Excretion | Primarily renal (approximately 60-70% as unchanged drug), with biliary/fecal elimination accounting for 20-30%. |
| Half-life | Terminal elimination half-life is 4.5 hours; in severe renal impairment (CrCl <30 mL/min), half-life may be prolonged up to 12-15 hours, requiring dose adjustment. |
| Protein binding | Approximately 85-90% bound to serum albumin; binding is saturable at high concentrations. |
| Volume of Distribution | Volume of distribution is 0.9-1.2 L/kg, indicating extensive distribution into total body water and some tissue binding. |
| Bioavailability | Oral bioavailability is 65-75% due to first-pass metabolism; food reduces absorption by 15-20%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: within minutes; clinical effect peaks at 1-2 hours. |
| Duration of Action | Duration is 6-8 hours for oral administration; intravenous duration is 4-6 hours. Clinical effect correlates with plasma concentrations above 0.1 mcg/mL. |
| Molecular Weight | 288.43 |
Apply 1 patch (20 cm² containing 600 mcg ethinyl estradiol and 6 mg norelgestromin) transdermally once weekly for 3 weeks, followed by 1 patch-free week.
| Dosage form | FILM, EXTENDED RELEASE |
| Renal impairment | No formal studies; use caution in patients with renal impairment, especially if GFR <30 mL/min, as systemic exposure may increase; consider alternative contraception. |
| Liver impairment | Contraindicated in patients with Child-Pugh Class B or C hepatic impairment; no dose adjustment for mild (Child-Pugh A) disease, but use with caution. |
| Pediatric use | Not approved for use before menarche; post-menarche adolescents: same dosing as adults (1 patch weekly for 3 weeks, then 1 week off). |
| Geriatric use | Not indicated for use in postmenopausal women; no specific geriatric studies, but use is generally not appropriate in this population. |
| 1st trimester | Contraindicated due to risk of fetal masculinization in female fetuses. |
| 2nd trimester | Contraindicated; associated with fetal toxicity and developmental abnormalities. |
| 3rd trimester | Contraindicated; may cause virilization of female fetus and premature closure of epiphyses. |
Clinical note
Comprehensive clinical and safety monograph for XULANE (XULANE).
| Placental transfer | Crosses placenta; detectable in fetal tissues. |
| Breastfeeding | Excreted in breast milk; avoid use due to potential for virilization in nursing infants. |
| Lactation Rating | L5 - Contraindicated |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular events from combined hormonal contraceptive use. This risk increases with age and with heavy smoking (≥15 cigarettes per day). Women over 35 who smoke should not use this product.
| Serious Effects |
PregnancyBreastfeedingProstate cancerMale breast cancerSevere hepatic impairment
| Precautions | Increased risk of thromboembolic events (e.g., VTE, arterial thrombosis) especially in smokers >35 years, Increased risk of myocardial infarction and stroke, Hepatic neoplasia and liver disease, Hypertension (worsening or new onset), Gallbladder disease, Carbohydrate and lipid metabolic effects, Headache (including migraine), Bleeding irregularities (spotting, breakthrough bleeding, amenorrhea), Depression, Hereditary angioedema, Chloasma (may persist), Jaundice or liver function abnormalities, Interaction with anticonvulsants and other drugs decreasing efficacy |
| Food/Dietary | No specific food restrictions. Grapefruit juice may increase ethinyl estradiol levels, but interaction is minimal; no need to avoid. |
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| Teratogenic Risk | XULANE (etonogestrel contraceptive implant) is contraindicated during pregnancy. First trimester: Use during organogenesis may cause a slight increased risk of cardiovascular defects and neural tube defects, though large studies show no major teratogenicity. Second/third trimester: No specific fetal risks from etonogestrel alone; however, progestins may alter placental function and should be avoided. |
| Fetal Monitoring | Monitor for pregnancy prior to insertion and exclude pregnancy if implant is overdue for replacement. During use, monitor for signs of pregnancy (e.g., missed menses, unusual bleeding). If pregnancy occurs, remove implant promptly. No routine fetal monitoring required otherwise. |
| Fertility Effects | XULANE provides highly effective reversible contraception. After removal, fertility returns rapidly; median time to ovulation is 3-4 weeks. No long-term adverse effects on fertility. In women with pre-existing menstrual irregularities, return to baseline cycle may take several months. |
| Clinical Pearls | Xulane is a transdermal contraceptive patch containing ethinyl estradiol and norelgestromin. Apply to clean, dry, hairless skin on the buttock, abdomen, upper arm, or upper torso. Rotate sites to avoid irritation. Patch adhesion is critical; if partial detachment occurs for less than 24 hours, reapply or replace with a new patch. If detachment >24 hours, use backup contraception. The patch may be less effective in women weighing >90 kg. Do not cut or alter the patch. |
| Patient Advice | Apply a new patch weekly for 3 weeks, then have a patch-free week to allow withdrawal bleeding. · If the patch falls off or is not sticky, replace it immediately and use backup contraception. · Do not place the patch on irritated, oily, or injured skin. · Avoid exposing the patch to direct heat sources (e.g., heating pads, saunas) as it may increase absorption. · Common side effects include breast tenderness, headache, and application site reactions. · Smoking increases the risk of serious cardiovascular events; inform your healthcare provider if you smoke. · Use additional barrier contraception if vomiting or diarrhea occurs. · Xulane does not protect against HIV or other sexually transmitted infections. |