BUTOCONAZOLE NITRATE
Clinical safety rating: safe
Animal studies have demonstrated safety
Inhibits fungal cytochrome P450 14α-demethylase, blocking ergosterol synthesis and disrupting fungal cell membrane integrity.
| Metabolism | Primarily hepatic via CYP3A4; undergoes oxidation and N-dealkylation. |
| Excretion | Primarily hepatic metabolism with <5% excreted unchanged in urine; fecal elimination accounts for ~30% of metabolites. |
| Half-life | Terminal half-life is approximately 21–24 hours, supporting once-daily or twice-weekly dosing for vaginal candidiasis. |
| Protein binding | Approximately 98%, primarily to albumin. |
| Volume of Distribution | Approximately 1.3 L/kg, indicating extensive tissue distribution beyond plasma volume. |
| Bioavailability | Topical (vaginal): Minimal systemic absorption (<2%) due to poor mucosal permeability. |
| Onset of Action | Topical (vaginal): Symptom relief begins within 24–72 hours after application. |
| Duration of Action | Vaginal cream: Clinical cure typically achieved with 3–7 days of treatment; single-dose regimens provide therapeutic concentrations for up to 3 days. |
| Molecular Weight | 475.53 |
Intravaginal administration: 100 mg (one applicatorful of 2% cream) once daily for 3 days; or 100 mg (one suppository) once daily for 3 days; or 5 g (one applicatorful of 4% cream) as a single dose.
| Dosage form | CREAM |
| Renal impairment | No dose adjustment required based on GFR; minimal systemic absorption. |
| Liver impairment | No dose adjustment required based on Child-Pugh class; minimal systemic absorption. |
| Pediatric use | Safety and efficacy not established in pediatric patients below 12 years of age. For adolescents 12 years and older, dosing is same as adult. |
| Geriatric use | No specific dose adjustment; use same as adult dosing. Consider potential for concurrent medications and comorbidities. |
| 1st trimester | No evidence of harm in animal studies; limited human data. Generally considered safe for short-term use during pregnancy, but avoid if possible. |
| 2nd trimester | No evidence of fetal risk; minimal systemic absorption. Clinically acceptable for treatment of vulvovaginal candidiasis. |
| 3rd trimester | Considered safe; minimal systemic absorption. Preferred over oral antifungals due to lower risk. |
Clinical note
No significant drug interactions For vaginal use only not for ophthalmic or oral use.
| Placental transfer | Minimal to negligible due to low systemic absorption after topical/vaginal application. |
| Breastfeeding | Minimal systemic absorption after vaginal application; unlikely to be detectable in breast milk. Considered compatible with breastfeeding. |
■ FDA Black Box Warning
None.
| Common Effects | Vaginal burning |
| Serious Effects |
Hypersensitivity to butoconazole or any component of the formulation
| Precautions | Use only if pregnant or breastfeeding if potential benefit justifies potential risk to fetus or infant., Not for oral or ophthalmic use., Discontinue if hypersensitivity or irritation occurs. |
| Food/Dietary | No significant food interactions. Avoid alcohol as a general precaution with any infection, though no direct interaction is known. Maintain a diet low in sugar to potentially reduce yeast overgrowth; no specific dietary restrictions required. |
Loading safety data…
| Lactation Rating |
| L2 |
| Teratogenic Risk | FDA Pregnancy Category C. No evidence of teratogenicity in animal studies; limited human data. Fetal risk cannot be ruled out. Avoid use in first trimester unless clearly needed. |
| Fetal Monitoring | No specific clinical monitoring required. Use only if potential benefit justifies potential risk to fetus. |
| Fertility Effects | No effects on fertility reported in animal studies. No human data; unlikely systemic absorption limits reproductive impact. |
| Clinical Pearls | Butoconazole nitrate is an imidazole antifungal used intravaginally for vulvovaginal candidiasis. It is available as a 2% vaginal cream (single-dose or 3-day regimen). Advise patients to use the applicator as directed and to avoid oil-based lubricants which may degrade latex condoms and diaphragms. Systemic absorption is minimal (<1%), but caution is warranted in pregnant patients (Category C) – use only if clearly needed, especially in first trimester. Recurrent infections may require culture confirmation due to non-albicans species or resistance. |
| Patient Advice | Insert the cream high into the vagina at bedtime using the provided applicator. · Complete the full course even if symptoms improve. · Do not use tampons, douches, spermicides, or other vaginal products during treatment. · Avoid sexual intercourse during treatment to prevent reinfection or irritation. · Notify your doctor if symptoms persist beyond 7 days or if you have abdominal pain, fever, or foul-smelling discharge. · If pregnant, consult your doctor before use. |