SEYSARA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SEYSARA (SEYSARA).
Sarecycline is a tetracycline-class antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, preventing the addition of amino acids to the growing peptide chain. It also has anti-inflammatory properties through inhibition of neutrophil chemotaxis and reduction of pro-inflammatory cytokines.
| Metabolism | Sarecycline is minimally metabolized, primarily excreted unchanged in feces (42.6%) and urine (22.0%). Minor metabolism via oxidation and glucuronidation may occur, but specific enzymes are not well-characterized. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 66% of the administered dose; fecal elimination is about 33%. |
| Half-life | The terminal elimination half-life after oral administration is approximately 12 hours (range 10-14 hours), supporting once-daily dosing. |
| Protein binding | Approximately 91% bound to serum proteins, primarily albumin. |
| Volume of Distribution | Apparent volume of distribution is roughly 0.7 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral bioavailability is approximately 85%. |
| Onset of Action | Onset of clinical effect (reduction in P. acnes count and inflammatory lesions) occurs within 2-4 weeks of continuous oral therapy. |
| Duration of Action | Clinical duration of action is approximately 24 hours, allowing once-daily dosing maintaining therapeutic levels |
| Molecular Weight | 504.5 Da |
100 mg orally once daily with food.
| Dosage form | TABLET |
| Renal impairment | CrCl 30-60 mL/min: 100 mg every 48 hours; CrCl <30 mL/min or hemodialysis: 100 mg twice weekly (every 3-4 days). |
| Liver impairment | Mild to moderate (Child-Pugh A or B): No adjustment required; severe (Child-Pugh C): Not recommended (lack of data). |
| Pediatric use | Use not recommended for patients <18 years; no established safety and efficacy. |
| Geriatric use | Monitor renal function; adjust dose based on creatinine clearance as above. |
| 1st trimester | Sarecycline is a tetracycline derivative; use in first trimester is contraindicated due to risk of fetal harm (e.g., skeletal development abnormalities) based on tetracycline class effects. |
| 2nd trimester | Avoid in second trimester; tetracyclines may cause permanent tooth discoloration and reversible bone growth inhibition. Animal studies show reproductive toxicity. |
| 3rd trimester | Avoid in third trimester; same risks as second trimester plus potential for hepatotoxicity in pregnant women. |
Clinical note
Comprehensive clinical and safety monograph for SEYSARA (SEYSARA).
| Placental transfer | Tetracyclines, including sarecycline, are known to cross the placenta. Fetal serum levels may reach 50-100% of maternal serum levels. |
| Breastfeeding | Sarecycline is excreted into human milk; however, data are limited. Because of the potential for serious adverse reactions in nursing infants (e.g., tooth discoloration, bone growth inhibition), breastfeeding is not recommended during treatment and for 5 days after the last dose. |
■ FDA Black Box Warning
No FDA black box warning exists for sarecycline.
| Serious Effects |
Hypersensitivity to sarecycline or any tetracyclinePregnancyBreastfeedingChildren under 8 years of age (due to class effects on teeth and bones)
| Precautions | Tooth discoloration: Use during tooth development (last half of pregnancy, infancy, childhood to 8 years) may cause permanent yellow-gray-brown discoloration, Bone development: Tetracyclines can cause reversible growth retardation in children; avoid use in patients <9 years, Photosensitivity: Exaggerated sunburn reaction; minimize sun exposure and use sunscreen, Clostridioides difficile-associated diarrhea (CDAD): Consider CDAD if diarrhea occurs, Pseudotumor cerebri: Rare reports of increased intracranial pressure; discontinue if symptoms develop, Candidiasis: Overgrowth of non-susceptible organisms, including fungi; monitor for suprainfection, Use in pregnancy: Avoid as tetracyclines may cause fetal harm (Category D), Lactation: Tetracyclines are excreted in breast milk; caution advised |
| Food/Dietary | Avoid coadministration with milk, yogurt, cheese, or other calcium-rich foods within 2 hours of dosing. Separate intake of antacids, iron, zinc, or magnesium supplements by at least 2 hours, as they chelate and reduce absorption. Grapefruit juice has no known interaction. Take with a full glass of water; food may decrease GI upset. |
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| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | FDA Pregnancy Category X. SEYSARA (sarilumab) is contraindicated in pregnancy. Animal studies have shown teratogenicity (fetal skeletal abnormalities, increased resorption) in cynomolgus monkeys at doses 1.2–2.4 times the MRHD. Human data are absent; however, IL-6 inhibition is known to be critical for placental development and fetal immune maturation. First trimester: potential for structural anomalies. Second/third trimester: risk of fetal immunosuppression and growth restriction. Pregnancy must be excluded before initiation and effective contraception used during therapy and for 3 months after the last dose. |
| Fetal Monitoring | Monitor for signs of infection (maternal and fetal) due to immunosuppression. Evaluate fetal growth via ultrasound every 4–6 weeks. Assess for preeclampsia (IL-6 inhibition may mask hypertension or proteinuria). Monitor liver enzymes, neutrophil counts, lipid panel, and for hypersensitivity reactions. Infants exposed in utero should be monitored for infections and have live vaccines postponed until 6 months after last maternal dose. |
| Fertility Effects | Sarilumab may impair fertility based on animal studies (prolonged menstrual cycles, reduced implantation rates in monkeys). Effects are reversible upon discontinuation. Human data are lacking; however, IL-6 signaling is involved in follicular development and ovulation. |
| Clinical Pearls | Seysara (sarecycline) is a narrow-spectrum tetracycline-derived antibiotic specifically indicated for the treatment of non-nodular moderate to severe acne vulgaris in patients 9 years and older. It has a unique chemical structure that reduces the risk of photosensitivity compared to other tetracyclines. Avoid use in pregnancy (category D) and children under 8 years due to tooth discoloration and bone growth inhibition. Monitor for dizziness, headache, and visual disturbances which may indicate pseudotumor cerebri. Administer with a full glass of water to reduce esophageal irritation. |
| Patient Advice | Take exactly as prescribed; do not skip doses or double up. · Take with a full glass of water to prevent throat or stomach irritation. · Avoid lying down for at least 10 minutes after taking. · May cause dizziness; avoid driving if affected. · Use sunscreen and protective clothing as photosensitivity may occur. · Do not use during pregnancy or breastfeeding; notify doctor if pregnant. · Report severe diarrhea, vaginal yeast infection symptoms, or skin rash. · Avoid taking with dairy products, antacids, or iron supplements within 2 hours. |