gepotidacin

Contraindicated in:

Severe hypersensitivity;
QT interval prolongation or pre-existing cardiac disease;
Severe renal impairment or end-stage renal disease;
Severe hepatic impairment.

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Children <12 yr and <40 kg (safety and effectiveness not established;
Geri: Consider age-related impairment of renal function in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: QT interval prolongation

GI: diarrhea, abdominal pain, CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), flatulence, nausea, vomiting

GU: vulvovaginal candidiasis

Neuro: dizziness, headache

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHLYAXIS)

Interactions ⬆ ⬇

Drug-drug:

Antiarrhythmics and QT interval prolonging medications may ↑ risk of QT interval prolongation; avoid concurrent use.
Strong CYP3A4 inhibitors, including itraconazole or ketoconazole, may ↑ levels and risk of QT interval prolongation; avoid concurrent use.
Strong CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness; avoid concurrent use.
May ↑ levels and risk of toxicity of CYP3A4 substrates, including cyclosporine, midazolam, or quinidine; avoid concurrent use.
May ↑ levels and risk of toxicity of digoxin; closely monitor digoxin levels.
May exaggerate the neuromuscular effects of succinylcholine.
May ↑ risk of cholinergic adverse effects of other acetylcholinesterase inhibitors, including donepezil.
May antagonize the effects of anticholinergic drugs, including benztropine or oxybutynin and non-depolarizing neuromuscular blockers.

Availability ⬆ ⬇

Film-coated tablets: 750 mg

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥12 yr and ≥40 kg): 1,500 mg twice daily for 5 days.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a triazaacenaphthylene antibacterial that inhibits type II topoisomerases including bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, which then inhibits DNA replication. Also acts as a reversible acetylcholinesterase inhibitor.

Therapeutic effects:

Death of susceptible bacteria with resolution of infection.

Spectrum:

Active against Escherichia coli, Klebsiella pneumoniae, Citrobacter freundii, Staphylococcus saprophyticus, and Enterococcus faecalis.

Classifications ⬆ ⬇

Therapeutic Classification: anti-infectives

Pharmacologic Classification: Triazaacenaphthylene

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A isoenzyme. 52% excreted in feces (30% as unchanged drug); 31% excreted in urine (20% as unchanged drug).

Half-Life: 9 hr.

Time/Action Profile ⬆ ⬇

( plasma concentrations)

ROUTE		ONSET		PEAK		DURATION
IV		rapid		end of infusion		unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of gepotidacin. Instruct patient to take medication as directed after a meal. If a dose is missed, take it as soon as possible; do not double the dose to make up for the missed dose. Keep out of children’s reach. Do not share medication with others, even if they have similar symptoms; may be harmful. Advise patient to read Patient Information before starting therapy.
Warn patient to report symptoms of arrhythmias and QT interval prolongation (fast heart beat, skipped beats, palpitations, dizziness, lightheaded, trouble breathing, faintness).
Advise the patient to report signs and symptoms of excessive cholinergic symptoms such as dizziness, trouble breathing, sweating a lot, feeling very weak, stomach cramps, nausea, vomiting, diarrhea, or drooling.
Advise patients and family to call 911 and seek urgent treatment for signs and symptoms of hypersensitivity reactions such as difficulty breathing, chest tightness, hives, rash, feeling lightheaded, itching, swelling of the face, lips, tongue or throat.
Instruct patient to notify health care professional immediately if diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professionals.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Encourage pregnant patient to enroll in registry that monitors outcomes in women exposed to gepotidacin during pregnancy by calling 1-888-825-5249.

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Indications ⬇

Contraind./Precautions ⬆ ⬇