SPRINTEC
Clinical safety rating
cautionComprehensive clinical and safety monograph for SPRINTEC (SPRINTEC).
Combination of ethinyl estradiol and norgestimate suppresses gonadotropin release, inhibiting ovulation and altering cervical mucus and endometrium to prevent pregnancy.
| Metabolism | Ethinyl estradiol is metabolized primarily by CYP3A4; norgestimate is rapidly metabolized to norelgestromin and norgestrel via first-pass metabolism. |
| Excretion | Renal: approximately 50-60% (metabolites, primarily glucuronide conjugates), Fecal: approximately 30-40% (biliary excretion of metabolites), with minimal unchanged drug in urine (<5%). |
| Half-life | Ethinyl estradiol: 13 ± 3 hours (variable, influenced by CYP3A4 activity); Norgestimate: 1.5-2 hours (rapidly converted to norelgestromin); Norelgestromin: 12-20 hours (active metabolite); clinical context: dosing interval of 24 hours supports once-daily administration. |
| Protein binding | Ethinyl estradiol: >97% bound to albumin; Norgestimate/norelgestromin: 99% bound to albumin and sex hormone-binding globulin (SHBG). |
| Volume of Distribution | Ethinyl estradiol: 2.5-4.0 L/kg; Norgestimate: not determined (extensive tissue distribution); clinical meaning: reflects distribution into total body water and tissues. |
| Bioavailability | Ethinyl estradiol: 38-48% due to first-pass metabolism; Norgestimate: 100% (prodrug, rapidly hydrolyzed in gut wall and liver). |
| Onset of Action | Oral administration: contraceptive effect achieved within 7 days of consistent daily dosing; immediate if started on first day of menses. |
| Duration of Action | Contraceptive effect: sustained with daily dosing; return of fertility may be delayed up to 3-6 months after discontinuation. |
| Molecular Weight | Ethinyl estradiol: 296.4 Da; Norgestimate: 369.5 Da |
| Action Class | Combination Oral Contraceptive (Estrogen-Progestin) |
One tablet (0.25 mg norgestimate, 0.035 mg ethinyl estradiol) orally once daily at the same time each day for 21 days, followed by 7 days of placebo tablets.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment; use caution. |
| Liver impairment | Contraindicated in patients with acute or chronic hepatic dysfunction (Child-Pugh class B or C). No data for mild impairment; use with caution. |
| Pediatric use | Safety and efficacy have not been established in postmenarchal pediatric patients. Use after first menses; dosing same as adults. |
| Geriatric use | Not indicated for use in postmenopausal women. No specific dose adjustment needed for elderly patients beyond contraindications. |
| 1st trimester | Contains ethinyl estradiol and norgestimate. Oral contraceptive use during pregnancy is contraindicated; but unintentional exposure during early pregnancy does not suggest significant teratogenic risk based on large epidemiological studies. |
| 2nd trimester | Avoid use during second trimester; no evidence of fetal harm from inadvertent exposure, but continued use is not indicated. |
| 3rd trimester | Avoid use during third trimester due to potential adverse effects (e.g., jaundice, fluid retention) and because pregnancy confirmation is expected before continuation. |
Clinical note
Comprehensive clinical and safety monograph for SPRINTEC (SPRINTEC).
| Placental transfer | Ethinyl estradiol and norgestimate cross the placenta; norgestimate is extensively metabolized to norelgestromin and other metabolites which are detectable in fetal tissues. |
| Breastfeeding | Combined hormonal contraceptives may reduce milk production and pass into breast milk in small amounts. Use is generally not recommended during breastfeeding, especially in the early postpartum period. Progestin-only methods are preferred. |
| Lactation Rating | L3 - Moderate Risk |
| Teratogenic Risk | FDA Pregnancy Category X. Use contraindicated in pregnancy. First trimester: Major congenital anomalies including cardiovascular and limb defects; increased risk of neural tube defects. Second and third trimesters: Fetal genital abnormalities in females (diethylstilbestrol-like effect); potential for long-term reproductive tract changes. Postnatal: Possible increased risk of neurodevelopmental issues. |
| Fetal Monitoring | Pregnancy test before initiation; monthly pregnancy tests if sexually active. Ultrasound for fetal anomalies if accidental exposure occurs. Monitor for signs of thromboembolism, hypertension, and hepatic dysfunction. Fetal monitoring for growth restriction if exposure in second/third trimester. |
| Fertility Effects | Suppresses ovulation by inhibiting gonadotropin release. Reversible upon discontinuation; no evidence of permanent fertility impairment. May delay return to fertility for several cycles after cessation. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from combined oral contraceptive use. Risk increases with age (>35 years) and number of cigarettes smoked. Women over 35 who smoke should not use combined oral contraceptives.
| Common Effects | Nausea, Vomiting, Headache, Breast tenderness, Weight changes, Irregular uterine bleeding, Amenorrhea, Melasma |
| Serious Effects | Venous thromboembolism (VTE), Arterial thromboembolism (e.g., stroke, myocardial infarction), Hepatic adenoma or hepatocellular carcinoma, Hypertension, Gallbladder disease, Thrombotic thrombocytopenic purpura (TTP), Hemolytic uremic syndrome (HUS) |
Known or suspected pregnancyCurrent or history of thrombosis (venous or arterial)Cerebrovascular or coronary artery diseaseValvular heart disease with thrombogenic complicationsAtrial fibrillationUncontrolled hypertension (systolic ≥160 mmHg or diastolic ≥100 mmHg)Diabetes mellitus with vascular involvement or age >35 with diabetesHeadaches with focal neurological symptoms, including migraine with aura (age ≥35)Major surgery with prolonged immobilizationHistory of breast cancer or other estrogen-sensitive neoplasiaSevere liver disease, hepatic adenoma, or hepatocellular carcinomaUndiagnosed abnormal genital bleedingCigarette smoking in women >35 years old
| Precautions | Increased risk of thromboembolic disorders, Increased risk of myocardial infarction and stroke, especially in smokers, Increased risk of hepatic neoplasia, Elevated blood pressure, Gallbladder disease, Carbohydrate and lipid effects, Ocular lesions, Hereditary angioedema, Chloasma |
| Food/Dietary | Avoid grapefruit juice as it may increase estrogen levels and risk of adverse effects. No other significant food interactions are known; maintain consistent dietary habits to minimize gastrointestinal side effects. |
| Clinical Pearls | SPRINTEC (ethinyl estradiol/norgestimate) is a combined oral contraceptive. Prescribe with caution in women with migraine with aura due to increased stroke risk. If a dose is missed, take as soon as remembered; if >24 hours late, use backup contraception for 7 days. Monitor blood pressure at initiation and annually. Discontinue if pregnancy is suspected or confirmed. Advise that antibiotics (e.g., rifampin) and anticonvulsants (e.g., phenytoin) may reduce efficacy. |
| Patient Advice | Take one tablet daily at the same time each day, in the order directed on the pill pack. · If you miss a pill, refer to the package insert or consult your healthcare provider; use backup contraception as directed. · This medication does not protect against HIV or other sexually transmitted infections. · Common side effects include nausea, breast tenderness, and breakthrough bleeding; these often improve within a few cycles. · Seek immediate medical attention for symptoms of blood clots: sudden leg pain/swelling, chest pain, shortness of breath, or sudden severe headache. · Inform your provider about all medications, including over-the-counter drugs and herbal supplements, especially St. John's Wort. |
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