XACIATO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XACIATO (XACIATO).
Clindamycin is a lincosamide antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, thereby preventing peptide bond formation.
| Metabolism | Clindamycin is primarily metabolized by the liver via CYP3A4 to active and inactive metabolites. |
| Excretion | Clindamycin is primarily excreted via bile (approximately 85% of the dose as metabolites and parent drug) and feces (10%), with renal excretion accounting for less than 10%. |
| Half-life | Terminal elimination half-life is approximately 2-3 hours in adults with normal renal function. Half-life may be prolonged in patients with severe hepatic impairment or neonates. |
| Protein binding | Approximately 94% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Apparent volume of distribution is 0.6-1.2 L/kg, indicating distribution into total body water and extensive tissue penetration. |
| Bioavailability | Following intravaginal administration, systemic bioavailability is low (approximately 2-5% of the dose absorbed), with local concentrations sufficient for antibacterial effect. |
| Onset of Action | Following topical application (intravaginal gel), therapeutic concentrations are achieved within 12-24 hours; systemic absorption is minimal, and local effect begins within days. |
| Duration of Action | The recommended dosing regimen (single-dose vaginal gel) provides coverage for 7 days, based on sustained local concentrations. |
Administer one vaginal gel (50 mg clindamycin) intravaginally as a single dose.
| Dosage form | GEL |
| Renal impairment | No dosage adjustment required for renal impairment, including end-stage renal disease. |
| Liver impairment | No dosage adjustment required for hepatic impairment, including severe hepatic impairment. |
| Pediatric use | Not indicated for use in prepubertal females. Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dosage adjustment recommended; however, consider age-related vaginal atrophy and potential for decreased efficacy in elderly women. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XACIATO (XACIATO).
| Breastfeeding | Clindamycin is excreted into human breast milk in low concentrations (M/P ratio approximately 0.5-0.7). After vaginal administration, systemic absorption is minimal (about 4% of dose), thus expected milk levels are negligible. However, caution is advised due to potential for infant gastrointestinal effects (e.g., diarrhea, sensitization). The American Academy of Pediatrics considers clindamycin compatible with breastfeeding. Monitor nursing infant for loose stools or rash. |
| Teratogenic Risk | XACIATO (clindamycin phosphate) vaginal gel is categorized as FDA Pregnancy Category B. Animal reproduction studies in rats and mice using subcutaneous doses up to 600 mg/kg/day (approximately 5 times the human vaginal dose based on body surface area) revealed no evidence of fetal harm. However, no adequate and well-controlled studies exist in pregnant women. Clindamycin crosses the placenta and may accumulate in fetal tissues. Use during first trimester only if clearly needed. During second and third trimesters, no increased risk of major congenital malformations has been reported based on limited observational data. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to clindamycin, lincomycin, or any component of the formulation","History of antibiotic-associated colitis"]
| Precautions | ["Clostridium difficile associated diarrhea (CDAD) has been reported with nearly all antibacterial agents including clindamycin.","May result in overgrowth of nonsusceptible organisms including fungi.","Use with caution in patients with history of gastrointestinal disease, particularly colitis.","Safety and efficacy in pediatric patients not established."] |
Loading safety data…
| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond routine prenatal care. Patients should report signs of vaginal irritation, allergic reactions, or development of C. difficile-associated diarrhea. In pregnancy, if treatment persists >7 days, monitor for overgrowth of non-susceptible organisms. |
| Fertility Effects | No specific studies on fertility effects are reported for XACIATO. Clindamycin systemic absorption is minimal with vaginal use; therefore, significant impact on fertility is unlikely. Animal studies with high-dose subcutaneous clindamycin showed no impairment of mating or fertility in rats. |