SIMPESSE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SIMPESSE (SIMPESSE).
Simpesse is a combination estrogen-progestin oral contraceptive that suppresses gonadotropin release, primarily inhibiting ovulation via negative feedback on the hypothalamic-pituitary-ovarian axis. Additionally, it alters cervical mucus viscosity and endometrial receptivity.
| Metabolism | Metabolized via cytochrome P450 enzymes (CYP3A4) in the liver; ethinyl estradiol undergoes sulfation and glucuronidation; levonorgestrel is conjugated and excreted in urine and feces. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 60-70% of elimination; hepatic metabolism produces inactive metabolites that are excreted renally (20-30%) and fecally (<10%). |
| Half-life | Terminal elimination half-life is 24 hours (range 20-28 hours), supporting once-daily dosing. |
| Protein binding | 95% bound primarily to albumin. |
| Volume of Distribution | 0.8 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 90%; intravenous: 100%. |
| Onset of Action | Oral: 1-2 hours; intravenous: 5-10 minutes. |
| Duration of Action | 24 hours for oral; intravenous duration is dose-dependent, typically 6-12 hours. |
Oral: 10 mg once daily, taken at least 1 hour before a meal.
| Dosage form | TABLET |
| Renal impairment | GFR ≥60 mL/min: No adjustment. GFR 30-59 mL/min: Reduce dose to 5 mg once daily. GFR <30 mL/min: Not recommended. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg once daily. Child-Pugh C: Contraindicated. |
| Pediatric use | Not approved for use in pediatric patients (<18 years). |
| Geriatric use | No specific dose adjustment recommended; monitor renal function and consider age-related decline in GFR. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SIMPESSE (SIMPESSE).
| Breastfeeding | Contraindicated in breastfeeding. M/P ratio not established; drug is present in human milk and may cause serious adverse effects in nursing infants. Discontinue nursing or drug. |
| Teratogenic Risk | Pregnancy Category X. First trimester: Major congenital malformations including craniofacial defects, CNS abnormalities, and cardiovascular defects. Second/third trimesters: Increased risk of spontaneous abortion, preterm labor, and intrauterine growth restriction. Contraindicated in pregnancy. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive use. This risk increases with age and with heavy smoking (≥15 cigarettes per day) and is quite marked in women over 35 years of age. Women who use combination hormonal contraceptives should be strongly advised not to smoke.
| Serious Effects |
["Known or suspected pregnancy","Current or past history of thrombophlebitis or thromboembolic disorders","Current or past history of 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 pill use","Hepatic adenoma or carcinoma","Known or suspected pregnancy (Category X)","Heavy smoking (≥15 cigarettes/day) in women over 35 years of age"]
| Precautions | ["Thrombotic disorders (venous thromboembolism, arterial thromboembolism, stroke, myocardial infarction)","Carcinoma of the breast and reproductive organs","Liver disease (hepatic adenomas, hepatocellular carcinoma)","Elevated blood pressure","Gallbladder disease","Carbohydrate and lipid metabolism effects","Headache/migraine","Uterine bleeding irregularities","Depression","Contact lens intolerance"] |
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| Prior to therapy: Negative pregnancy test confirmed. Monthly pregnancy tests during treatment. Fetal ultrasound for malformations if inadvertent exposure occurs. Monitor for signs of fetal distress. |
| Fertility Effects | May impair female fertility by disrupting ovulation. In males, may cause oligospermia or azoospermia; effects may be reversible upon discontinuation. |