Version July 2025
Cystitis, acute uncomplicated or acute simple cystitis (infection limited to the bladder without signs/symptoms of upper tract or systemic infection): Females ≥40 kg: Oral: 1.5 g twice daily for 5 days.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Altered kidney function:
eGFR ≥30 mL/minute: No dosage adjustment necessary.
eGFR <30 mL/minute: Avoid use.
Hemodialysis, intermittent: Avoid use.
Mild or moderate impairment (Child-Turcotte-Pugh class A or B): No dosage adjustment necessary.
Severe impairment (Child-Turcotte-Pugh class C): Avoid use.
Refer to adult dosing.
(For additional information see "Gepotidacin: Pediatric drug information")
Urinary tract infection, uncomplicated:
Children ≥12 years and Adolescents: Females weighing ≥40 kg: Oral: 1,500 mg every 12 hours for 5 days.
Children ≥12 years and Adolescents: Females weighing ≥40 kg:
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: Avoid use (increased gepotidacin exposure and risk of QTc prolongation).
Children ≥12 years and Adolescents: Females weighing ≥40 kg:
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: Avoid use (increased gepotidacin exposure and risk of QTc prolongation).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adolescents and adults.
>10%: Gastrointestinal: Diarrhea (16%)
1% to 10%:
Gastrointestinal: Abdominal pain (4%), flatulence (3%), nausea (9%), vomiting (2%)
Genitourinary: Vulvovaginal candidiasis (1%)
Nervous system: Dizziness (2%), headache (2%)
<1%:
Cardiovascular: Presyncope, tachycardia
Dermatologic: Hyperhidrosis, skin rash
Endocrine & metabolic: Hot flash
Gastrointestinal: Abdominal distention, Clostridioides difficile-associated diarrhea, dyspepsia
Hepatic: Increased serum alanine aminotransferase, increased serum aspartate aminotransferase
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis)
Nervous system: Dysarthria, fatigue, vertigo
Neuromuscular & skeletal: Muscle spasm
Ophthalmic: Blurred vision
Frequency not defined:
Cardiovascular: Prolonged QT interval on ECG
Gastrointestinal: Sialorrhea
History of severe hypersensitivity to gepotidacin or any component of the formulation.
Concerns related to adverse effects:
• Acetylcholinesterase inhibition: Gepotidacin is a reversible acetylcholinesterase inhibitor in vitro; adverse reactions potentially attributed to acetylcholinesterase inhibition (eg, abdominal pain, diarrhea, dysarthria, hyperhidrosis, hypersalivation, muscle spasms, nausea, presyncope, vomiting) have been reported in clinical trials. Increased cholinergic effects can be associated with severe adverse reactions (eg, atrioventricular block, bradycardia, bronchospasm, seizures/convulsions, vasovagal syncope).
• Hypersensitivity reactions: Hypersensitivity reactions, including anaphylaxis, have been reported. Inquire about previous hypersensitivity reactions to gepotidacin prior to use. Discontinue use and institute supportive measures if an allergic reaction occurs.
• QTc prolongation: Dose and concentration-dependent QTc interval prolongation has been observed. Avoid use in patients with a history of QTc interval prolongation, relevant preexisting cardiac disease, or those on concomitant antiarrhythmic agents or other medications that may prolong the QTc interval. If use in these patients cannot be avoided, correct any serum electrolyte abnormalities prior to and during treatment, as indicated.
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Kidney impairment: Avoid use in severe impairment (eGFR <30 mL/minute), including patients receiving dialysis, because of an increase in exposure (Cmax) and the risk of QTc interval prolongation.
• Liver impairment: Avoid use in severe impairment (Child-Turcotte-Pugh class C) because of an increase in exposure (Cmax) and the risk of QTc interval prolongation.
Blujepa: FDA approved March 2025; availability anticipated in 2nd half of 2025.
Oral: Administer doses ~12 hours apart. Administer after a meal to decrease risk of GI intolerance.
Oral: Administer after a meal to decrease risk of GI intolerance.
Missed dose: Administer dose as soon as possible; do not double the dose to make up for the missed dose.
This medication is not on the National Institute for Occupational Safety and Health (NIOSH) (2024) list; however, it may meet the criteria for a hazardous drug. Gepotidacin may cause developmental toxicity.
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Cystitis, acute uncomplicated or acute simple cystitis: Treatment of uncomplicated urinary tract infection caused by susceptible Escherichia coli, Klebsiella pneumoniae, Citrobacter freundii complex, Staphylococcus saprophyticus, and Enterococcus faecalis, in female adult and pediatric patients ≥12 years of age weighing ≥40 kg.
Gepotidacin may be confused with gentamicin.
Substrate of CYP3A4 (Major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Acetylcholinesterase Inhibitors: Gepotidacin may increase therapeutic effects of Acetylcholinesterase Inhibitors. Risk C: Monitor
Agents with Clinically Relevant Anticholinergic Effects: Gepotidacin may decrease anticholinergic effects of Agents with Clinically Relevant Anticholinergic Effects. Risk C: Monitor
Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor
CYP3A4 Inducers (Moderate): May decrease serum concentration of Gepotidacin. Risk C: Monitor
CYP3A4 Inducers (Strong): May decrease serum concentration of Gepotidacin. Risk X: Avoid
CYP3A4 Inhibitors (Moderate): May increase serum concentration of Gepotidacin. Risk C: Monitor
CYP3A4 Inhibitors (Strong): May increase serum concentration of Gepotidacin. Management: Avoid coadministration of gepotidacin and strong CYP3A4 inhibitors if possible. If coadministration cannot be avoided, conduct a baseline ECG, monitor closely for altered electrolytes, and correct electrolyte abnormalities as needed. Risk D: Consider Therapy Modification
CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors): Gepotidacin may increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Digoxin: Gepotidacin may increase serum concentration of Digoxin. Risk C: Monitor
Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification
Grapefruit Juice: May increase serum concentration of Gepotidacin. Risk C: Monitor
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may increase QTc-prolonging effects of Haloperidol. Risk C: Monitor
Neuromuscular-Blocking Agents (Nondepolarizing): Gepotidacin may decrease therapeutic effects of Neuromuscular-Blocking Agents (Nondepolarizing). Risk C: Monitor
Neuromuscular-Blocking Agents: Gepotidacin may increase therapeutic effects of Neuromuscular-Blocking Agents. Risk C: Monitor
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Adverse events were observed in animal reproduction studies conducted in rats and mice following oral administration of gepotidacin in oral doses ≤1 times the maximum recommended human dose based on AUC. Decreased fetal weight and increased late fetal resorptions were observed in some studies; malformations were not observed.
Data collection to monitor pregnancy and infant outcomes following exposure to gepotidacin is ongoing. Health care providers are encouraged to notify the manufacturer of patients exposed to gepotidacin during pregnancy (1-888-825-5249).
It is not known if gepotidacin is present in human milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Baseline and periodic kidney function tests; baseline and periodic serum electrolytes in patients with risk factors for QTc interval prolongation; signs/symptoms of hypersensitivity reactions. Monitor patients with conditions that may be exacerbated by acetylcholinesterase inhibition for signs/symptoms of acetylcholinesterase inhibition. For patients receiving concomitant acetylcholinesterase inhibitors, monitor for exaggerated neuromuscular blockade or excessive cholinergic effects. Monitor patients receiving concomitant systemic anticholinergics or nondepolarizing neuromuscular blocking agents; gepotidacin may antagonize effects of these agents.
Gepotidacin is a triazaacenaphthylene antibacterial that inhibits type II topoisomerases, including bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, resulting in inhibition of DNA replication.
Distribution: Vdss: 172.9 L.
Protein binding: ~25% to ~41%.
Metabolism: Primarily by oxidative metabolism mediated by CYP3A4, producing several circulating metabolites; M4 (major metabolite) accounts for ~11% of circulating drug-related materials.
Bioavailability: ~45%.
Half-life elimination: 9.3 hours.
Time to peak: ~2 hours.
Excretion: Feces: 52% (30% as unchanged drug); Urine: ~31% (20% unchanged drug; major route of elimination for absorbed gepotidacin).
Altered kidney function: Cmax and AUC were 1.2-fold and 1.5-fold higher in subjects with moderate impairment (eGFR 30 to 59 mL/minute), 1.7-fold and 2.1-fold in subjects with severe impairment/end-stage kidney disease (ESKD) (eGFR <30 mL/minute) not on intermittent hemodialysis, 2.3-fold and 2.5-fold higher in subjects with ESKD requiring intermittent hemodialysis before hemodialysis, and 6.2-fold and 4.2-fold higher in subjects with ESKD requiring intermittent hemodialysis after hemodialysis, respectively.
Hepatic function impairment: Cmax and AUC were ~1.9-fold and 1.7-fold higher in subjects with severe impairment (Child-Turcotte-Pugh class C), respectively.
