Vandazole Information
Vandazole () Indications And Usage
Vandazole () is indicated in the treatment of bacterial vaginosis (formerly referred to as vaginitis, vaginitis, nonspecific vaginitis, vaginitis, or anaerobic vaginosis) in non-pregnant women.
Vandazole () Dosage And Administration
The recommended dose is one applicator full of Vandazole () , (approximately 5 grams of gel containing approximately 37.5 mg of metronidazole) administered intravaginally once a day for 5 days. For once a day dosing, Vandazole () should be administered at bedtime [].
Not for ophthalmic, dermal, or oral use.
Vandazole () Dosage Forms And Strengths
Vandazole () is a vaginal gel 0.75% in a 70 g tube with 5 vaginal applicators (each applicator delivers approximately 5 g of gel containing 37.5 mg of metronidazole).
Vandazole () Adverse Reactions
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The data described below reflect exposure to Vandazole () compared to another formulation of vaginal metronidazole in 220 women in a single trial. The population was non-pregnant females (age range 18 to 72 years, the mean was 33 years +/- 11 years) with bacterial vaginosis. The racial demographic of those enrolled was 71 (32%) of White, 143 (65%) of Black, 3 (1%) of Hispanic, 2 (1%) of Asian, and 1 (0%) of other. Patients administered an applicator full of Vandazole () intravaginally once daily at bedtime for 5 days.
There were no deaths or serious adverse reactions related to drug therapy in the clinical trial. Vandazole () was discontinued in 5 patients (2.3%) due to adverse reactions.
The incidence of all adverse reactions in Vandazole () -treated patients was 42% (92/220). Adverse reactions occurring in ≥ 1% of patients were: fungal infection* (12%), headache (7%), pruritus (6%), abdominal pain (5%), nausea (3%), dysmenorrhea (3%), pharyngitis (2%), rash (1%), infection (1%), diarrhea (1%), breast pain (1%), and metrorrhagia (1%).
* Known or previously unrecognized vaginal candidiasis may present more prominent symptoms during therapy with Vandazole () . Approximately 10% of patients treated with Vandazole () developed vaginitis during or immediately after therapy.
Additional uncommon events, reported by
Other Vaginal Formulations
Other reactions that have been reported in association with the use of other formulations of metronidazole vaginal gel include: unusual taste and decreased appetite.
Topical (Dermal) Formulations
Other reactions that have been reported in association with the use of topical (dermal) formulations of metronidazole include skin irritation, transient skin erythema, and mild skin dryness and burning. None of these adverse reactions exceeded an incidence of 2% of patients.
Oral and Parenteral Formulations
The following adverse reactions and altered laboratory tests have been reported with the oral or parenteral use of metronidazole:
Cardiovascular:
Gastrointestinal:
Hematopoietic:
Renal:
Vandazole () Drug Interactions
The intravaginal administration of a single 5 gram dose of Vandazole () results in relatively lower mean systemic exposure to metronidazole that is approximately 2% to 5% of that achieved following a 500 mg oral dose of metronidazole []. The following drug interactions were reported for oral metronidazole.
Vandazole () Use In Specific Populations
Caution should be exercised when Vandazole () is administered to a nursing woman. Following oral metronidazole administration, concentrations of metronidazole in human milk are similar to concentrations in plasma. Since some metronidazole is systemically absorbed following vaginal administration of metronidazole, excretion in human milk is possible.
Because of the potential for tumorigenicity shown for metronidazole in animal studies, a decision should be made whether to discontinue nursing or to discontinue Vandazole () , taking into account the importance of the therapy to the mother. A nursing mother may choose to pump and discard her milk for the duration of Vandazole () therapy, and for 24 hours after therapy ends and feed her infant stored human milk or formula.
Vandazole () Overdosage
There is no human experience with overdosage of metronidazole vaginal gel. Vaginally applied metronidazole gel, 0.75% could be absorbed in sufficient amounts to produce systemic effects [ ].
Vandazole () Description
Vandazole () (metronidazole vaginal gel, 0.75%) is the vaginal dosage form of the nitroimidazole antimicrobial metronidazole at a concentration of 0.75%. Chemically, metronidazole is a 2-methyl-5-nitroimidazole-1-ethanol.
CHNO M.W. 171.16
Vandazole () is a colorless to yellow gel, containing metronidazole at a concentration of 7.5 mg/g (0.75%). The gel also contains edetate disodium, hypromellose, methylparaben, propylene glycol, propylparaben, purified water, and sodium hydroxide (to adjust pH).
Each applicator full of 5 grams of vaginal gel contains approximately 37.5 mg of metronidazole.
Vandazole () Clinical Pharmacology
Healthy Subjects
Following a single, intravaginal 5 gram dose of metronidazole vaginal gel (equivalent to 37.5 mg of metronidazole) to 38 healthy female subjects, a mean maximum serum metronidazole concentration of 281 ng/mL was reported (range: 134 to 464 ng/mL). The average time to achieve this C was 9.5 hours (range: 4 to 17 hours) after dosing with metronidazole vaginal gel. This C is approximately 2% of the mean maximum serum concentration reported in healthy subjects administered a single, oral 500 mg dose of metronidazole (mean C = 12,785 ng/mL).
The extent of exposure [area under the curve (AUC)] of metronidazole, when administered as a single intravaginal 5 gram dose of metronidazole vaginal gel (equivalent to 37.5 mg of metronidazole), was 5,989 ng•hr/mL (range: 2,797 to 10,515 ng•hr/mL). This AUC is approximately 5% of the reported AUC of metronidazole following a single oral 500 mg dose of metronidazole approximately 125,000 ng•hr/mL.
Patients with Bacterial Vaginosis
Following single and multiple 5 gram doses of a similar metronidazole vaginal gel product to 4 patients with bacterial vaginosis, a mean maximum serum metronidazole concentration of 214 ng/mL on day one and 294 ng/mL (range: 228 to 349 ng/mL) on day five were reported. Steady state metronidazole serum concentrations following oral dosages of 400 to 500 mg BID have been reported to range from 6,000 to 20,000 ng/mL.
Mechanism of Action
The intracellular targets of action of metronidazole on anaerobes are largely unknown. The 5-nitro group of metronidazole is reduced by metabolically active anaerobes, and studies have demonstrated that the reduced form of the drug interacts with bacterial DNA. However, it is not clear whether interaction with DNA alone is an important component in the bactericidal action of metronidazole on anaerobic organisms.
Activity
Metronidazole is an antibacterial agent active against most strains of the following organisms that have been reported to be associated with bacterial vaginosis:
Bacteroides
Gardnerella vaginalis
Mobiluncus
Peptostreptococcus
Standard methodology for the susceptibility testing of the potential bacterial vaginosis pathogens, and spp., has not been defined. Culture and sensitivity testing of bacteria are not routinely performed to establish the diagnosis of bacterial vaginosis [].
Vandazole () Clinical Studies
A single, randomized, double-blind, active-controlled clinical trial was conducted to evaluate the efficacy of Vandazole () for the treatment of bacterial vaginosis. A clinical diagnosis of bacterial vaginosis was defined by the presence of a homogeneous vaginal discharge that (a) has a pH of greater than 4.5, (b) emits a "fishy" amine odor when mixed with a 10% KOH solution, and (c) contains clue cells on microscopic examination. Gram's stain results consistent with a diagnosis of bacterial vaginosis include (a) markedly reduced or absent morphology, (b) predominance of morphotype, and (c) absent or few white blood cells. Non-pregnant females at least 18 years of age were randomized to receive treatment with either Vandazole () or another formulation of metronidazole vaginal gel 0.75% once daily at bedtime for 5 days. The modified intent-to treat population (patients who received study medication and had a Nugent score ≥ 4) consisted of 229 Vandazole () patients and 243 patients treated with another vaginal formulation of metronidazole. Therapeutic Cure defined as a clinical cure and Nugent score
Vandazole () How Supplied/storage And Handling
Vandazole () (metronidazole vaginal gel, 0.75%) is supplied in a 70 gram tube and packaged with 5 vaginal applicators.
Store at 20 to 25C (68 to 77F) [See USP Controlled Room Temperature]. Avoid exposure to extreme heat or cold. Protect from freezing.
Vandazole () Patient Counseling Information
Instruct the patient that Vandazole () (metronidazole vaginal gel, 0.75%) is supplied with 5 vaginal applicators. For once daily dosing, one applicator should be used per dose. See for complete instructions on how to use the product and the vaginal applicator.
US Patent No. 7,456,207
Manufactured For:
UPSHER-SMITH LABORATORIES, INC.
Minneapolis, MN 55447
Rev. F 1/2011
Vandazole () Patient Instructions For Use
Read this Patient Instructions for Use before you start using Vandazole () . This leaflet does not take the place of talking with your healthcare provider about your medical condition or your treatment.
Manufactured For:
Minneapolis, MN 55447
Rev. C 12/2010
Vandazole ()
