TRI-LO-LINYAH
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRI-LO-LINYAH (TRI-LO-LINYAH).
Combination estrogen-progestin oral contraceptive: suppresses gonadotropins (FSH and LH) via negative feedback, inhibiting ovulation; increases cervical mucus viscosity, reducing sperm penetration; alters endometrial structure, impairing implantation.
| Metabolism | Hepatic metabolism via CYP3A4 isoenzymes; ethinyl estradiol undergoes conjugation (sulfation and glucuronidation), while norgestimate is rapidly deacetylated to norelgestromin (active metabolite) and further hydroxylated and conjugated. |
| Excretion | Renal: ~60% as unchanged drug; fecal/biliary: ~40% as metabolites. |
| Half-life | Terminal elimination half-life: 12-15 hours; allows once-daily dosing but requires dose adjustment in renal impairment. |
| Protein binding | Approximately 99% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 80-90% (high bioavailability). |
| Onset of Action | Oral: peak plasma concentration at 2-4 hours, clinical effect within 24 hours. |
| Duration of Action | 24 hours (once-daily dosing); steady state achieved after 5-7 days. |
| Molecular Weight | 312.446 |
One tablet orally once daily for 21 days, followed by 7 days of placebo. Each tablet contains 0.180 mg norgestimate and 0.025 mg ethinyl estradiol for days 1-7, 0.215 mg/0.025 mg for days 8-14, and 0.250 mg/0.025 mg for days 15-21.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe impairment or end-stage renal disease; use with caution due to potential fluid and electrolyte changes. |
| Liver impairment | Contraindicated in acute hepatic disease or severe cirrhosis (Child-Pugh class C). Use caution in Child-Pugh class A or B; start with lowest effective dose if benefits outweigh risks, as steroids may be less well metabolized. |
| Pediatric use | Approved for postmenarchal adolescents; dosing same as adults. Safety and efficacy in premenarchal patients not established. |
| Geriatric use | Not indicated for use in postmenopausal women. No specific dose adjustment studies; use generally avoided due to increased risk of thromboembolism and cardiovascular events. |
| 1st trimester | Contraindicated due to risk of oral contraceptive-related birth defects; contains levonorgestrel and ethinyl estradiol. |
| 2nd trimester | Contraindicated; may cause fetal harm; use of CHCs in pregnancy is not recommended. |
| 3rd trimester | Contraindicated; may cause fetal harm; use of CHCs in pregnancy is not recommended. |
Clinical note
Comprehensive clinical and safety monograph for TRI-LO-LINYAH (TRI-LO-LINYAH).
| Placental transfer | Levonorgestrel and ethinyl estradiol cross the placenta; degree is dose-dependent. |
| Breastfeeding | Small amounts of contraceptive steroids and/or metabolites are excreted in breast milk; may reduce milk production and change composition; use only if benefits outweigh risks. |
| Lactation Rating |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events (e.g., stroke, myocardial infarction, thromboembolism) from combined oral contraceptive use. Risk increases with age (especially >35 years) and number of cigarettes smoked. Women who use combined oral contraceptives should be strongly advised not to smoke.
| Serious Effects |
Breast cancer (current or history)Estrogen-dependent neoplasiaUndiagnosed abnormal uterine bleedingThrombophlebitis or thromboembolic disordersHistory of DVT/PECerebrovascular diseaseCoronary artery diseaseValvular heart disease with complicationsSevere hypertension (≥160/100 mmHg)Diabetes with vascular involvementHeadaches with focal neurological symptomsMajor surgery with prolonged immobilizationSmoking >15 cigarettes/day in women ≥35 yearsPregnancyLiver disease or hepatic adenoma/carcinoma
| Precautions | Increased risk of thromboembolic disorders (venous and arterial), especially in smokers, obesity, hypertension, or hyperlipidemia., Elevated risk of hepatic neoplasia (benign and malignant)., Worsening of depression, migraine, or glucose tolerance., May cause fluid retention, hypertension, irregular bleeding, or amenorrhea., Cessation if jaundice, visual disturbances, or thrombotic events occur. |
Loading safety data…
| L3 |
| Teratogenic Risk | Pregnancy Category X. Contraindicated in pregnancy due to known teratogenic effects, including cardiovascular and limb defects, and increased risk of miscarriage. Use should be discontinued if pregnancy occurs. |
| Fetal Monitoring | Not applicable for ongoing use as drug is contraindicated in pregnancy. If inadvertent exposure occurs, monitor for fetal anomalies via ultrasound and consider fetal echocardiography. |
| Fertility Effects | Suppresses ovulation and may delay return to fertility after discontinuation. No permanent effects on fertility expected. |
| Food/Dietary |
| No significant food interactions. Grapefruit juice may modestly increase EE levels but not clinically relevant. St. John's Wort reduces contraceptive efficacy. High-fat meals may slightly delay absorption but does not affect overall exposure. Patients with lactose intolerance: contains lactose, may cause GI upset. Avoid excessive alcohol. |
| Clinical Pearls | Tri-Lo-Linyah is a low-dose combination oral contraceptive containing ethinyl estradiol (EE) and norgestimate. It is indicated for pregnancy prevention. The 91-day extended regimen (84 active + 7 placebo) reduces withdrawal bleeding frequency. Counsel patients to take at the same time daily; missed pills increase breakthrough bleeding and pregnancy risk. Use with caution in smokers over 35, hypertension, migraine with aura, or history of thromboembolism. Consider alternative contraception in patients with liver disease or breast cancer. Prescribe as first-line for dysmenorrhea, menorrhagia, and menstrual regulation. |
| Patient Advice | Take one tablet daily at the same time, even during bleeding. Missed pills require backup contraception. · Use condoms initially for 7 days if starting for first time or after a break. · Common side effects include nausea, headache, breast tenderness, and breakthrough bleeding especially in first 3 months. · Serious risks: blood clots (leg pain, chest, sudden SOB), stroke (vision/speech changes), liver tumors (abdominal pain). · Do not smoke while on this pill; smoking greatly increases clotting risk. · Antibiotics (except rifampin) and many anticonvulsants may reduce effectiveness; use backup. · Keep pack away from heat/moisture; do not skip placebo pills. · Consult healthcare provider before starting if you have migraine with aura, high blood pressure, or liver disease. |