NORITATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NORITATE (NORITATE).
Metronidazole, after intracellular reduction, forms toxic intermediates that disrupt bacterial DNA and inhibit nucleic acid synthesis. It has anti-inflammatory and immunosuppressive properties in dermatological conditions.
| Metabolism | Hepatic metabolism via oxidation and glucuronidation; major enzyme: CYP450 (unknown specific isoform). |
| Excretion | Primarily renal (approximately 90% as unchanged drug) and biliary/fecal (approximately 10%). |
| Half-life | Approximately 10 hours; may be prolonged in severe renal impairment. |
| Protein binding | Approximately 20-30%, primarily to albumin. |
| Volume of Distribution | 0.3-0.5 L/kg, suggesting distribution into total body water. |
| Bioavailability | IV: 100%; topical: negligible systemic absorption (less than 1%). |
| Onset of Action | 3-5 minutes after intravenous administration; topical: 1-2 hours for visible effect. |
| Duration of Action | 6-12 hours after IV; topical: 12-24 hours, though prolonged in renal impairment. |
Topical application of a thin layer to affected area twice daily (morning and evening).
| Dosage form | CREAM |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established. |
| Geriatric use | No specific dose adjustment recommended; use caution due to potential for increased skin fragility. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NORITATE (NORITATE).
| Breastfeeding | Metronidazole is excreted into breast milk with an M/P ratio of approximately 0.9. The American Academy of Pediatrics considers it compatible with breastfeeding, but due to potential exposure, caution is advised; some recommend pumping and discarding milk for 12-24 hours after a single dose. |
| Teratogenic Risk | NORITATE (metronidazole) is contraindicated in the first trimester due to potential teratogenic effects based on animal studies. In the second and third trimesters, use only if clearly needed; available data do not show increased risk of major birth defects, but a small increased risk of cleft lip/palate has been suggested in some studies. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to metronidazole or any component","Use in pregnancy (contraindicated in first trimester; use only if clearly needed in later trimesters)"]
| Precautions | ["Use with caution in patients with blood dyscrasias","Avoid prolonged use; potential for peripheral neuropathy","Photosensitivity may occur","Avoid contact with eyes and mucous membranes"] |
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| Fetal Monitoring | Monitor maternal liver function tests due to rare hepatotoxicity. In prolonged therapy, monitor for peripheral neuropathy. No specific fetal monitoring required, but ultrasound may be considered if used in first trimester. |
| Fertility Effects | Metronidazole has not been associated with significant effects on fertility in animal studies or human data. Rare reports of reversible impairment of spermatogenesis with high doses. |