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Noritate (Metronidazole Topical) - Description and Clinical Pharmacology

 
 



FOR TOPICAL USE ONLY
(NOT FOR OPHTHALMIC USE)

DESCRIPTION

NORITATE ® (metronidazole cream) Cream, 1%, contains metronidazole, USP. Chemically, metronidazole is 2-methyl-5-nitro-1H-imidazole-1-ethanol. The molecular formula for metronidazole is C6H9N3O3. It has the following structural formula:

Metronidazole has a molecular weight of 171.16. It is a white to pale yellow crystalline powder. It is slightly soluble in alcohol and has a solubility in water of 10 mg/mL at 20°C. Metronidazole is a member of the imidazole class of anti-bacterial agents and is classified as an antiprotozoal and anti-bacterial agent.

NORITATE is an emollient cream; each gram contains 10 mg micronized metronidazole USP, in a base of purified water USP, stearic acid NF, glyceryl monostearate NF, glycerin USP, methylparaben NF, trolamine NF and propylparaben NF.

CLINICAL PHARMACOLOGY

Pharmacokinetics

When one gram dose of NORITATE cream, 1%, was applied in a single application to the face of 16 healthy volunteers, low concentrations of metronidazole were detected in the plasma of 7 of the volunteers. The mean ± SD Cmax of metronidazole was 27.6 ± 7.3 ng/mL, which is about 1% of the value reported for a single 250 mg oral dose of metronidazole. The time to maximum plasma concentration (Tmax) in the volunteers with detectable metronidazole was 8–12 hours after topical application.

Pharmacodynamics

The mechanisms by which metronidazole acts in reducing inflammatory lesions of rosacea are unknown.

Clinical Studies

Safety and efficacy of NORITATE were evaluated in two randomized vehicle-controlled clinical studies for the treatment of rosacea, which excluded patients who had nodules, moderate or severe rhinophyma, dense telangiectases, plaque-like facial edema or ocular involvement and those who had a history of not responding to metronidazole therapy for rosacea. Of the patients included in the efficacy database (n=416), there were 142 men and 274 women. Endpoint efficacy data comparisons for patients treated with daily NORITATE or vehicle applications are listed below.

Inflammatory Lesion Counts and Erythema Severity Scores in Two Clinical Trials for Rosacea
Noritate Vehicle
Study 1 Study 2 Study 1 Study 2
N Result N Result N Result N Result
Papules + Pustules Count
Baseline 89 15 92 19 50 18 49 17
Week-10 80 7 1 82 8 45 15 41 12
  Reduction 49% 58% 17% 30%
Papules Count
Baseline 89 13 92 17 50 15 49 15
Week-10 80 7 82 7 45 12 41 11
  Reduction 41% 55% 14% 28%
Erythema Score
Baseline 89 2.2 92 2.3 50 2.2 49 2.2
Week-10 80 1.3 82 1.4 45 1.7 40 1.8
  Reduction 42% 40% 25% 19%

1 Statistically significant differences between NORITATE and vehicle groups with p≤0.05. Erythema scores: 0=none, 1=mild, 2=moderate and 3=severe.

Safety Studies

Studies of contact sensitization (n=258), phototoxicity (n=21), and photocontact sensitization (n=29) of NORITATE were conducted. No evidence of sensitization or phototoxicity was seen in these studies.

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