- Tablets 200 mg
Bactericidal against Clostridium difficile in vitro, inhibiting RNA synthesis by RNA polymerases.
Minimal systemic absorption. C max was approximately 5.2 ng/mL and T max was approximately 2 h (range, 1 to 5 h). C max of fidaxomicin and OP-1118 (its main metabolite) decreased by 21.5% and 33.4%, respectively, when administered with a high-fat meal, which is not considered clinically significant.
Mostly confined to GI tract.
Transformed by hydrolysis at the isobutyryl ester to form its main active metabolite (OP-1118).
Mainly excreted in feces (more than 92% as fidaxomicin and OP-1118) and very little in urine (0.59% of dose recovered). Elimination half-life was approximately 11.7 h (fidaxomicin) and 11.2 h (OP-1118 metabolite).
Special PopulationsRenal Function Impairment
Plasma concentrations did not vary by severity of renal impairment. No dosage adjustment is recommended based on renal function.Hepatic Function Impairment
Pharmacokinetics have not been evaluated in hepatic impairment.Elderly
Plasma concentrations were approximately 2- to 4-fold higher in elderly patients versus nonelderly patients. No dosage adjustment is recommended for elderly patients.Gender
Plasma concentration did not vary by gender. No dosage adjustment is necessary based on gender.
Indications and Usage
For treatment of C. difficile –associated diarrhea (CDAD).
None well documented.
Dosage and AdministrationAdults
PO 200 mg twice daily for 10 days.
- May administer with or without food.
Store between 68° and 77°F; excursions are permitted between 59° and 86°F.
Coadministration of cyclosporine, a P-glycoprotein (Pgp) inhibitor, may increase plasma concentrations of fidaxomicin and its metabolite, OP-1118. In addition, concentrations of fidaxomicin and OP-1118 may be reduced at the site of action (ie, GI tract) via Pgp inhibition. However, cyclosporine does not appear to affect the safety or treatment outcome of fidaxomicin. Fidaxomicin may be coadministered with Pgp inhibitors and no dose adjustment is recommended.Food
Administration of fidaxomicin with a high-fat meal decreases the C max of fidaxomicin and OP-1118, while the AUC is unchanged compared with administration under fasting conditions. The magnitude of the decrease in C max is not considered to be clinically important. Fidaxomicin may be given without respect to food.
Drug eruption, pruritus, rash (less than 2%).
Nausea (11%); vomiting (7%); abdominal pain (6%); GI hemorrhage (4%); abdominal distension, abdominal tenderness, dyspepsia, dysphagia, flatulence, intestinal obstruction, megacolon (less than 2%).
Anemia, neutropenia (2%).
Decreased blood bicarbonate, decreased platelet count, increased blood alkaline phosphatase, increased hepatic enzymes (less than 2%).
Hyperglycemia, metabolic acidosis (less than 2%).
Monitor patient for response to therapy and resolution of CDAD symptoms.
Category B .
Safety and efficacy in patients younger than 18 y have not been established.
No dosage adjustment is recommended based on renal function.
Because there is minimal systemic absorption, fidaxomicin is not effective for treatment of systemic infections.
- Inform patients that fidaxomicin tablets may be taken with or without food.
- Remind patients that fidaxomicin is an antibiotic that should only be used to treat bacterial infections and does not treat viral infections.
- Advise patients that the drug only treats CDAD and should not be used to treat any other infection.
- Inform patients that it is common to feel better early in the course of therapy and to take the medication exactly as directed. Skipping doses or not completing the full course of therapy may decrease the effectiveness of treatment and increase the likelihood that bacteria will develop resistance and will not be treatable by fidaxomicin or other antibacterial drugs in the future.
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