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Micah Johnson

Doctor of Pharmacy Candidate Preceptor: Dr. Monika Daftary


Howard University College of Pharmacy Ambulatory Care Rotation

Secnidazole (Solosec) is a 5-nitroimidazole indicated for bacterial vaginosis in adult women. It


enters the bacterial cell as an inactive prodrug where the nitro group is reduced by bacterial
enzymes to radical anions that interfere with bacterial DNA synthesis. The recommended dose
of secnidazole is one 2 gram packet of granules once. The packet is to be sprinkled onto or
gently mixed into applesauce, yogurt, or some other semi-solid food. It is not to be dissolved
into liquid or crushed.

CDC: Bacterial Vaginosis 2015 Guidelines


Oral Intravaginal
Recommended Metronidazole 500 mg orally twice Metronidazole gel 0.75%, one full
a day for 7 days applicator (5 g) intravaginally, once
a day for 5 days
Clindamycin cream 2%, one full
applicator (5 g) intravaginally at
bedtime for 7 days
Alternative Tinidazole 2 g orally once daily for 2 Clindamycin ovules 100 mg
days intravaginally once at bedtime for 3
Tinidazole 1 g orally once daily for 5 days
days
Clindamycin 300 mg orally twice
daily for 7 days

Comparing Secnidazole to Metronidazole: Therapeutic Success in Phase III Trial


Primary Endpoint: Therapeutic Therapeutic Success at Day 14
Success at Day 28 (mITT) (mITT)

Secnidazole 60.1% (146/243) 65.0% (158/243)

Metronidazole 59.5% (141/237) 66.2% (157/237)

95% CI Secnidazole- 0.082; 0.094 0.097; 0.073


Metronidazole

1. Therapeutic success was defined as a composite of clinical cure and bacteriological cure
2. Clinical cure was defined as the normalization of the three Amsel criteria (homogeneous, thin, greyish-white
vaginal discharge, positive potassium hydroxide whiff test results, and a vaginal pH above 4.5)
3. Bacteriological cure was defined as a Nugent score lower than or equal to three.
Pharmacokinetic Comparison of Oral Products for Bacterial Vaginitis
Metronidazole (PO) Secnidazole Tinidazole Clindamycin
Absorption With food, lower, delayed No difference between Food increases time to peak No difference between
peak. Bioavailability not fasting or fed state. by 2 hours and lowers peak fasting or fed state.
affected. by 10%.
AUC (0) 198 mcg*hr/mL 1261.5 mcg*hr/mL 901.6 mcg*hr/mL 10.6 mcg*hr/mL
Distribution Distributes into most tissues, Volume of distribution (42L) Distributes into most tissues, Distributes into tissues,
bones, CNS, and bile. suggests distribution into fluids, and CNS. bone, and fluids. Poor CNS
tissues and bodily fluids. penetration.
Protein < 20% 5% 12% 80% - 95%
Binding
Metabolism CYP3A4 substrate (30-60%) CYP450 ( 1% converted to CYP3A4 substrate CYP3A4 substrate
- Active metabolite metabolites)
Half-life 8 hours 17 hours 13.2 hours 2.4 hours
Time to peak IR: 1-2 hours 4 hours after fasting 1.6 hours fasting 0.75 hours
ER: ~5 hours
Excretion Urine (60-80%) Urine: 15% Urine: 20-25% Urine: 10%
Feces (6-15%) Fecal: 12% Feces: 3.6%
Drug Lithium No major CYP450 Oral anticoagulants Neuromuscular blockers
Interactions Oral anticoagulants interactions Lithium Erythromycin antagonism
CYP450 inducers/inhibitors Phenytoin, fosphenytoin
CYP3A4 inducers/inhibitors
Disufiram-like Yes. Avoid alcohol for the No effect on aldehyde Yes. Avoid alcohol for the No effect on aldehyde
reaction? duration of therapy plus up dehydrogenase activity. duration of therapy plus up dehydrogenase activity.
to three (3) days. to three (3) days.
References:
1. Bohbot, J., Vicaut, E., Fagnen, D., & Brauman, M. (2010). Treatment of Bacterial Vaginosis: A Multicenter, Double-Blind, Double-Dummy, Randomised
Phase III Study Comparing Secnidazole and Metronidazole. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2946572/
2. Cleocin (clindamycin capsules) package insert. New York, NY: Pharmacia and Upjohn Co; 2017 May.
3. Product Information: FLAGYL(R) oral tablets, metronidazole oral tablets. G.D. Searle (per FDA), New York, NY, 2013.
4. Product Information: SOLOSEC oral granules, secnidazole oral granules. Symbiomix Therapeutics LLC (per FDA), Newark, NJ, 2017.
5. Product Information: TINDAMAX(TM) oral tablet , tinidazole oral tablet. Presutti Laboratories, Inc, Arlington Heights, IL, 2004.
6. Bohbot, J., Vicaut, E., Fagnen, D., & Brauman, M. (2010). Treatment of Bacterial Vaginosis: A Multicenter, Double-Blind, Double-Dummy, Randomised
Phase III Study Comparing Secnidazole and Metronidazole. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2946572/