Sarecycline (Monograph)
Brand name: Seysara
Drug class: Aminomethylcyclines
Chemical name: (4S,4aS,5aR,12aS)-4-(Dimethylamino)-3,10,12,12a-tetrahydroxy-7-[(methoxymethylamino) methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide monohydrochloride
Molecular formula: C24H29N3O8•HCl
CAS number: 1035979-44-2
Introduction
Antibacterial; tetracycline anti-infective agent.
Uses for Sarecycline
Acne Vulgaris
Treatment of inflammatory lesions of non-nodular moderate to severe acne vulgaris.
Not evaluated for treatment of infections.
Sarecycline Dosage and Administration
Administration
Oral Administration
Administer orally once daily with or without food.
Take sarecycline tablets with adequate amounts of fluid to reduce risk of esophageal irritation and ulceration.
Dosage
Available as sarecycline hydrochloride; dosage expressed in terms of sarecycline.
Pediatric Patients
Acne Vulgaris
Oral
Pediatric patients ≥9 years of age with non-nodular moderate to severe acne vulgaris: Dosage is based on weight. (See Table 1.)
If no improvement after 12 weeks of treatment, reassess use of sarecycline. Efficacy for >12 weeks and safety for >12 months not established.
Body Weight (kg) |
Dosage |
---|---|
33–54 kg |
60-mg tablet once daily |
55–84 kg |
100-mg tablet once daily |
85–136 kg |
150-mg tablet once daily |
Adults
Acne Vulgaris
Oral
Non-nodular moderate to severe acne vulgaris: Dosage is based on weight. (See Table 2.)
If no improvement after 12 weeks, reassess use of sarecycline. Efficacy for >12 weeks and safety for >12 months not established.
Body Weight (kg) |
Dosage |
---|---|
33–54 kg |
60-mg tablet once daily |
55–84 kg |
100-mg tablet once daily |
85–136 kg |
150-mg tablet once daily |
Special Populations
Hepatic Impairment
Mild or moderate hepatic impairment (Child-Pugh class A or B): Dosage adjustments not needed.
Severe hepatic impairment (Child-Pugh class C): Data not available.
Renal Impairment
Mild, moderate, or severe renal impairment: Dosage adjustments not needed.
End-stage renal disease: Data not available.
Cautions for Sarecycline
Contraindications
-
Known hypersensitivity to any tetracycline.
Warnings/Precautions
Sensitivity Reactions
Photosensitivity Reactions
Photosensitivity, manifested by an exaggerated sunburn reaction, reported in patients receiving tetracyclines.
Minimize or avoid exposure to natural or artificial sunlight (tanning beds or UVA/B treatment) during sarecycline treatment. If patient needs to be outdoors, advise them to wear loose-fitting clothes that protect skin from sun exposure and to consider other sun protection measures.
Dental and Bone Effects
Use of tetracyclines during tooth development (e.g., second and third trimesters of pregnancy, infancy, children ≤8 years of age) may cause permanent yellow-gray to brown discoloration of teeth and enamel hypoplasia. These dental effects are most common following long-term use of tetracyclines, but may occur following repeated short-term use.
Tetracyclines form a stable calcium complex in any bone-forming tissue. Reversible decrease in fibula growth rate has occurred in premature infants given oral tetracycline in a dosage of 25 mg/kg every 6 hours.
Fetal/Neonatal Morbidity
Animal studies indicate tetracyclines cross the placenta, are found in fetal tissue, and can cause fetal toxicity (e.g., retardation of skeletal development) and embryotoxicity.
If sarecycline is used during pregnancy or if patient becomes pregnant while taking sarecycline, apprise patient of potential hazard to the fetus. (See Pregnancy under Cautions.)
CNS Effects
Adverse CNS effects (e.g., lightheadedness, dizziness, vertigo) reported with tetracyclines and may impair ability to drive vehicles or operate hazardous machinery. These symptoms may disappear during therapy or when drug discontinued.
Intracranial hypertension reported in adults and adolescents receiving tetracyclines; usually manifested as headache, blurred vision, and papilledema. Although signs and symptoms usually resolve after the tetracycline discontinued, possibility exists that sequelae (e.g., visual loss) may be permanent or severe. Women of childbearing age who are overweight have a greater risk for developing intracranial hypertension.
Because systemic retinoids also known to cause intracranial hypertension, do not use concomitantly with sarecycline. (See Specific Drugs under Interactions.)
Question patients about presence of visual disturbances prior to initiating a tetracycline. If visual disturbances occur during treatment, check for papilledema.
Superinfection/Clostridium difficile-associated Colitis
Possible overgrowth of nonsusceptible organisms, including fungi. Discontinue sarecycline and institute appropriate therapy if superinfection occurs.
Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile. C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) reported with nearly all systemic anti-infectives and may range in severity from mild diarrhea to fatal colitis. C. difficile produces toxins A and B which contribute to development of CDAD; hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.
Consider CDAD if diarrhea develops during or after anti-infective therapy. Obtain careful medical history since CDAD may occur as late as ≥2 months after anti-infective therapy discontinued.
If CDAD suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible. Initiate anti-infective therapy directed against C. difficile (e.g., vancomycin, fidaxomicin, metronidazole), appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), and surgical evaluation as clinically indicated.
Selection and Use of Anti-infectives
Use of sarecycline for treatment of acne vulgaris may result in emergence of bacteria resistant to tetracyclines.
To reduce development of drug-resistant bacteria and maintain effectiveness of other antibacterials, use sarecycline only when indicated.
Specific Populations
Pregnancy
Like other tetracyclines, may cause fetal harm, permanent discoloration of teeth, and reversible inhibition of bone growth if administered during pregnancy.
Human data insufficient to inform a drug-associated risk for birth defects or miscarriage with sarecycline; consider that tetracyclines cross the placenta.
If used during pregnancy or if patient becomes pregnant while taking sarecycline, apprise patient of potential hazard to the fetus.
Because potential risks to the fetus outweigh potential benefits to the mother, discontinue sarecycline as soon as pregnancy recognized.
Lactation
Tetracyclines are distributed into human milk. Advise women that breast-feeding is not recommended during sarecycline treatment.
Fertility
Manufacturer states avoid use of sarecycline in males attempting to conceive a child.
In animal fertility study, oral sarecycline adversely affected spermatogenesis (decreased sperm motility, decreased sperm count and concentration, increased percentage of abnormal sperm) in male rats; did not affect fertility in female rats.
Pediatric Use
Safety and efficacy not established in pediatric patients <9 years of age.
Safety and efficacy for treatment of inflammatory lesions of non-nodular moderate to severe acne vulgaris established in pediatric patients ≥9 years of age based on controlled clinical studies.
Geriatric Use
Insufficient experience in geriatric patients ≥65 years of age to determine whether they respond differently than younger adults.
Hepatic Impairment
Mild to moderate hepatic impairment (Child-Pugh class A or B): No clinically important effects on pharmacokinetics of sarecycline.
Severe hepatic impairment (Child-Pugh class C): Effects on sarecycline pharmacokinetics not studied.
Renal Impairment
Mild, moderate, or severe renal impairment: No clinically important effects on pharmacokinetics of sarecycline.
End-stage renal disease: Effects on sarecycline pharmacokinetics not studied.
Common Adverse Effects
Nausea.
Drug Interactions
Does not inhibit CYP isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4/5 in vitro; does not induce CYP1A2, 2B6, or 3A4/5 in vitro.
Minimally metabolized by hepatic microsomal enzymes.
Inhibits P-glycoprotein (P-gp) in vitro; not a substrate of P-gp.
Drugs Affected by P-glycoprotein Transport System
P-gp substrates: Possible increased concentrations of P-gp substrates. Monitor for toxicities associated with the P-gp substrate; may need to reduce dosage of the P-gp substrate.
Specific Drugs
Drug |
Interaction |
Comments |
---|---|---|
Antacids (aluminum-, bismuth-, calcium-, or magnesium-containing) |
Possible decreased sarecycline absorption and decreased efficacy |
Do not administer concomitantly |
Anticoagulants, oral |
Sarecycline may depress plasma prothrombin activity and increase risk of bleeding in patients receiving anticoagulants |
Adjust anticoagulant dosage as needed |
Digoxin |
Increased digoxin concentrations |
Monitor for digoxin toxicity; may need to reduce digoxin dosage |
Estrogens and progestins |
Oral contraceptive containing ethinyl estradiol and norethindrone: Increased concentrations and AUC of ethinyl estradiol and norethindrone |
Oral contraceptive containing ethinyl estradiol and norethindrone: Interaction not considered clinically important |
Iron-containing preparations |
May decrease sarecycline absorption and decrease efficacy |
Do not administer concomitantly |
Penicillins |
Possible antagonistic antibacterial effects |
Avoid concomitant use |
Retinoids, systemic (acitretin, isotretinoin) |
Oral retinoids may cause intracranial hypertension and increase intracranial pressure |
Avoid concomitant use with oral retinoids |
Sarecycline Pharmacokinetics
Absorption
Food
High-fat or high-caloric meal delays time to peak plasma concentrations by approximately 0.53 hours and decreases peak plasma concentrations and AUC by 31 and 27%, respectively. Not considered clinically important.
Plasma Concentrations
Median time to peak plasma concentrations following oral administration: 1.5–2 hours.
Once-daily oral administration: Steady-state reached by day 7.
Distribution
Extent
Tetracyclines cross the placenta.
Tetracyclines distributed into milk.
Plasma Protein Binding
63–75%.
Steady-state mean apparent volume of distribution: 91.4–97 L.
Elimination
Metabolism
In vitro studies in human liver microsomes indicate minimal metabolism by hepatic enzymes (<15%).
Minor metabolites resulting from nonenzymic epimerization, O/N-demethylation, hydroxylation, and desaturation identified.
Elimination Route
After a single 100-mg oral dose, 43% recovered in feces (14.9% as unchanged drug) and 44% in urine (24.7% as unchanged drug).
Half-life
Mean elimination half-life: 21–22 hours.
Stability
Storage
Oral
Tablets
20°–25°C (may be exposed to 15–30°C). Protect from moisture and excessive heat.
Actions and Spectrum
-
Tetracycline anti-infective; aminomethylcycline.
-
Mechanisms of action in the treatment of acne vulgaris not known. May result from a combination of anti-infective and anti-inflammatory effects similar to that reported with other tetracyclines.
-
Has a narrower spectrum of activity compared with other commercially available tetracyclines. Like other tetracyclines used in treatment of acne vulgaris (e.g., doxycycline, minocycline, tetracycline), sarecycline is active in vitro against Cutibacterium acnes (formerly Propionibacterium acnes), a gram-positive anaerobe that is a factor in the etiology of acne; however, sarecycline is less active in vitro than the other tetracyclines against enteric gram-negative bacteria or other anaerobic bacteria.
Advice to Patients
-
Advise patients to read manufacturer’s patient information.
-
Importance of drinking sufficient quantities of fluids when taking sarecycline tablets to reduce the risk of esophageal irritation and ulceration.
-
Importance of taking as directed because of potential for development of drug-resistant bacteria. Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with other antibacterials in the future.
-
Inform patients that photosensitivity manifested by an exaggerated sunburn reaction reported in some individuals taking tetracyclines. Advise patients to minimize or avoid sunlight or artificial UV light (e.g., tanning beds, UVA/B treatment) during sarecycline treatment and to discontinue the drug at first sign of skin erythema. If patient needs to be outdoors, advise them to wear loose-fitting clothes that protect skin from sun exposure and also consider other sun protection measures.
-
Inform patients that intracranial hypertension can occur with tetracyclines. Importance of seeking medical attention if headache or blurred vision occurs.
-
Advise patients to use caution when driving vehicles or using hazardous machinery if they experience CNS effects (lightheadedness, dizziness, vertigo) during sarecycline treatment. Importance of seeking medical attention if these CNS effects persist.
-
Advise patients that C. difficile colitis can occur with anti-infective therapy. Importance of seeking medical attention if watery or bloody stools occur.
-
Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, and any concomitant illnesses.
-
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Advise patients that sarecycline should not be taken by pregnant women or by women or men attempting to conceive a child. (See Pregnancy and see Fertility under Cautions.) Advise women not to breast-feed during sarecycline treatment.
-
Importance of advising patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Oral |
Tablets, film-coated |
60 mg (of sarecycline) |
Seysara |
Almirall |
100 mg (of sarecycline) |
Seysara |
Almirall |
||
150 mg (of sarecycline) |
Seysara |
Almirall |
AHFS DI Essentials™. © Copyright 2025, Selected Revisions April 15, 2019. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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