DRUGS & SUPPLEMENTS
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V-Zole is an antifungal agent of imidazole derivatives group for topical use. This medication has an effect at the expense of the synthesis of ergosterol, which is part of the cell membrane of fungi. V-Zole (Clotrimazole) has a broad spectrum of action.
V-Zole (Clotrimazole) is active against dermatophytes, molds, fungi of the genus Candida, Malassezia furfur.
This drug is also active against Corynebacterium minutissimum, Streptococcus spp., Staphylococcus spp., Trichomonas vaginalis.
For external use V-Zole (Clotrimazole) is well into the various layers of the skin reaching therapeutic concentrations. When this medication applied topically a small amount of it absorbed into the bloodstream.
Fungal skin and mucous membranes: ringworm, tinea, trichophytosis, athlete, mikrosporiya, candidiasis, a fungal interdigital erosion, fungal paronychia; fungal infections complicated by a secondary pyoderma; colorful lichen, erythrasma; thrush; Candida vulvitis, vulvovaginitis, balanitis, trichomoniasis; for the renovation of the birth canal before delivery.
When V-Zole used externally it applied to affected skin 2-3 times / day in 2-4 weeks.
For local orally this medicine used 1-2 times / day, no more than 7 days.
Intravaginal - on 100-500 mg for 1-6 days.
Local reactions: contact allergic dermatitis, redness, burning sensation.
When applied topically to the skin: erythema, blisters, swelling, burning and tingling, irritation and flaking skin.
When applied topically for the treatment of urogenital infections: itching, burning, redness and swelling of the mucous membrane, vaginal discharge, frequent urination, intercurrent cystitis, burning sensation in the penis with a partner, pain during sexual intercourse.
When applied topically in the oral cavity: redness of the oral mucosa, burning sensation and tingling at the site of application, irritation.
Hypersensitivity to V-Zole (Clotrimazole), I trimester of pregnancy.
In experimental studies there have been found that V-Zole used in high doses exerts embryotoxic effect.
It is not known whether V-Zole (Clotrimazole) released in breast milk. Although V-Zole (Clotrimazole) is not contraindicated during pregnancy and lactation, it should be considered a potential risk when selecting antifungal therapy.
Prescribed intravaginal Dosage forms of V-Zole (Clotrimazole) is not used during menstruation.
To prevent reinfection it should be simultaneous treatment of sexual partners.
V-Zole (Clotrimazole) is not recommended for use in ophthalmology.
Simultaneous administration of V-Zole (Clotrimazole) with amphotericin B, nystatin, natamycin activity of V-Zole (Clotrimazole) decreases.
Symptoms: anorexia, nausea, vomiting, stomachodynia, abnormal liver function, rarely - drowsiness, hallucinations, thamuria, allergic skin reactions.
Treatment: taking activated charcoal, symptomatic therapy.
WARNING: POTENTIAL RISK FOR CARCINOGENICITY
See full prescribing information for complete boxed warning.
Carcinogenicity has been seen in mice and rats treated chronically with metronidazole, another nitroimidazole agent ( 13.1). Although such data have not been reported for V-Zole (Tinidazole), the two drugs are structurally related and have similar biologic effects. Use should be limited to approved indications only.
Indications and Usage, Bacterial Vaginosis ( 1.4) 5/2007
Dosage and Administration, Bacterial Vaginosis ( 2.6) 5/2007
Other pathogens commonly associated with vulvovaginitis such as Trichomonas vaginalis, Chlamydia trachomatis, Neisseria gonorrhoeae, Candida albicans and Herpes simplex virus should be ruled out.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of V-Zole (Tinidazole) and other antibacterial drugs, V-Zole (Tinidazole) should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
Alcoholic beverages should be avoided when taking V-Zole (Tinidazole) and for 3 days afterwards .
Procedure for Extemporaneous Pharmacy Compounding of the Oral Suspension: Pulverize four 500 mg oral tablets with a mortar and pestle. Add approximately 10 mL of cherry syrup to the powder and mix until smooth. Transfer the suspension to a graduated amber container. Use several small rinses of cherry syrup to transfer any remaining drug in the mortar to the final suspension for a final volume of 30 mL. The suspension of crushed tablets in artificial cherry syrup is stable for 7 days at room temperature. When this suspension is used, it should be shaken well before each administration.
Amebic Liver Abscess: The recommended dose in adults is a 2 g dose per day for 3-5 days taken with food. In pediatric patients older than three years of age, the recommended dose is 50 mg/kg/day (up to 2 g per day) for 3-5 days with food. There are limited pediatric data on durations of therapy exceeding 3 days, although a small number of children were treated for 5 days without additional reported adverse reactions. Children should be closely monitored when treatment durations exceed 3 days.
To report SUSPECTED ADVERSE REACTIONS, contact Mission Pharmacal Company at 1-855-778-0177or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
Among 3669 patients treated with a single 2 g dose of V-Zole (Tinidazole), in both controlled and uncontrolled trichomoniasis and giardiasis clinical studies, adverse reactions were reported by 11.0% of patients. For multi-day dosing in controlled and uncontrolled amebiasis studies, adverse reactions were reported by 13.8% of 1765 patients. Common (≥ 1% incidence) adverse reactions reported by body system are as follows. (Note: Data described in Table 1 below are pooled from studies with variable designs and safety evaluations.)
Other adverse reactions reported with V-Zole (Tinidazole) include:
Central Nervous System: Two serious adverse reactions reported include convulsions and transient peripheral neuropathy including numbness and paresthesia . Other CNS reports include vertigo, ataxia, giddiness, insomnia, drowsiness.
Gastrointestinal: tongue discoloration, stomatitis, diarrhea
Hypersensitivity: urticaria, pruritis, rash, flushing, sweating, dryness of mouth, fever, burning sensation, thirst, salivation, angioedema
Renal: darkened urine
Hematopoietic: transient neutropenia, transient leukopenia
Other: Candida overgrowth, increased vaginal discharge, oral candidiasis, hepatic abnormalities including raised transaminase level, arthralgias, myalgias, and arthritis.
|2 g single dose||Multi-day dose|
|GI: Metallic/bitter taste||3.7%||6.3%|
|Total patients with adverse reactions||11.0% |
Adverse Reactions in Pediatric Patients: In pooled pediatric studies, adverse reactions reported in pediatric patients taking V-Zole (Tinidazole) were similar in nature and frequency to adult findings including nausea, vomiting, diarrhea, taste change, anorexia, and abdominal pain.
Bacterial vaginosis: The most common adverse reactions in treated patients (incidence >2%), which were not identified in the trichomoniasis, giardiasis and amebiasis studies, are gastrointestinal: decreased appetite, and flatulence; renal: urinary tract infection, painful urination, and urine abnormality; and other reactions including pelvic pain, vulvo-vaginal discomfort, vaginal odor, menorrhagia, and upper respiratory tract infection .
Severe acute hypersensitivity reactions have been reported on initial or subsequent exposure to V-Zole (Tinidazole). Hypersensitivity reactions may include urticaria, pruritis, angioedema, Stevens-Johnson syndrome and erythema multiforme.
The following drug interactions were reported for metronidazole, a chemically-related nitroimidazole and may therefore occur with V-Zole (Tinidazole):
Alcohols, Disulfiram: Alcoholic beverages and preparations containing ethanol or propylene glycol should be avoided during V-Zole (Tinidazole) therapy and for 3 days afterward because abdominal cramps, nausea, vomiting, headaches, and flushing may occur. Psychotic reactions have been reported in alcoholic patients using metronidazole and disulfiram concurrently. Though no similar reactions have been reported with V-Zole (Tinidazole), V-Zole (Tinidazole) should not be given to patients who have taken disulfiram within the last two weeks.
Lithium: Metronidazole has been reported to elevate serum lithium levels. It is not known if V-Zole (Tinidazole) shares this property with metronidazole, but consideration should be given to measuring serum lithium and creatinine levels after several days of simultaneous lithium and V-Zole (Tinidazole) treatment to detect potential lithium intoxication.
Phenytoin, Fosphenytoin: Concomitant administration of oral metronidazole and intravenous phenytoin was reported to result in prolongation of the half-life and reduction in the clearance of phenytoin. Metronidazole did not significantly affect the pharmacokinetics of orally-administered phenytoin.
Cyclosporine, Tacrolimus: There are several case reports suggesting that metronidazole has the potential to increase the levels of cyclosporine and tacrolimus. During V-Zole (Tinidazole) co-administration with either of these drugs, the patient should be monitored for signs of calcineurin-inhibitor associated toxicities.
Fluorouracil: Metronidazole was shown to decrease the clearance of fluorouracil, resulting in an increase in side-effects without an increase in therapeutic benefits. If the concomitant use of V-Zole (Tinidazole) and fluorouracil cannot be avoided, the patient should be monitored for fluorouracil-associated toxicities.
Cholestyramine: Cholestyramine was shown to decrease the oral bioavailability of metronidazole by 21%. Thus, it is advisable to separate dosing of cholestyramine and V-Zole (Tinidazole) to minimize any potential effect on the oral bioavailability of V-Zole (Tinidazole).
Oxytetracycline: Oxytetracycline was reported to antagonize the therapeutic effect of metronidazole.
V-Zole (Tinidazole), like metronidazole, may produce transient leukopenia and neutropenia; however, no persistent hematological abnormalities attributable to V-Zole (Tinidazole) have been observed in clinical studies. Total and differential leukocyte counts are recommended if re-treatment is necessary.
The use of V-Zole (Tinidazole) in pregnant patients has not been studied. Since V-Zole (Tinidazole) crosses the placental barrier and enters fetal circulation it should not be administered to pregnant patients in the first trimester.
Embryo-fetal developmental toxicity studies in pregnant mice indicated no embryo-fetal toxicity or malformations at the highest dose level of 2,500 mg/kg (approximately 6.3-fold the highest human therapeutic dose based upon body surface area conversions). In a study with pregnant rats a slightly higher incidence of fetal mortality was observed at a maternal dose of 500 mg/kg (2.5-fold the highest human therapeutic dose based upon body surface area conversions). No biologically relevant neonatal developmental effects were observed in rat neonates following maternal doses as high as 600 mg/kg (3-fold the highest human therapeutic dose based upon body surface area conversions). Although there is some evidence of mutagenic potential and animal reproduction studies are not always predictive of human response, the use of V-Zole (Tinidazole) after the first trimester of pregnancy requires that the potential benefits of the drug be weighed against the possible risks to both the mother and the fetus.
Pediatric Administration: For those unable to swallow tablets, V-Zole (Tinidazole) tablets may be crushed in artificial cherry syrup, to be taken with food .
Patients undergoing hemodialysis: If V-Zole (Tinidazole) is administered on the same day as and prior to hemodialysis, it is recommended that an additional dose of V-Zole (Tinidazole) equivalent to one-half of the recommended dose be administered after the end of the hemodialysis .
Treatment of Overdosage: There is no specific antidote for the treatment of overdosage with V-Zole (Tinidazole); therefore, treatment should be symptomatic and supportive. Gastric lavage may be helpful. Hemodialysis can be considered because approximately 43% of the amount present in the body is eliminated during a 6-hour hemodialysis session.
V-Zole (Tinidazole) is a synthetic antiprotozoal and antibacterial agent. It is 1-[2-(ethylsulfonyl)ethyl]-2-methyl-5-nitroimidazole, a second-generation 2-methyl-5-nitroimidazole, which has the following chemical structure:
V-Zole (Tinidazole) pink oral tablets contain 500 mg of V-Zole (Tinidazole). Inactive ingredients include croscarmellose sodium, FD&C Red 40 lake, FD&C Yellow 6 lake, hypromellose, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, pregelatinized corn starch, titanium dioxide, and triacetin.
Administration of V-Zole (Tinidazole) tablets with food resulted in a delay in T max of approximately 2 hours and a decline in C max of approximately 10% , compared to fasted conditions. However, administration of V-Zole (Tinidazole) with food did not affect AUC or T 1/2 in this study.
In healthy volunteers, administration of crushed V-Zole (Tinidazole) tablets in artificial cherry syrup, [prepared as described in Dosage and Administration ( 2.2) ] after an overnight fast had no effect on any pharmacokinetic parameter as compared to tablets swallowed whole under fasted conditions.
Distribution: V-Zole (Tinidazole) is distributed into virtually all tissues and body fluids and also crosses the blood-brain barrier. The apparent volume of distribution is about 50 liters. Plasma protein binding of V-Zole (Tinidazole) is 12%. V-Zole (Tinidazole) crosses the placental barrier and is secreted in breast milk.
Metabolism: V-Zole (Tinidazole) is significantly metabolized in humans prior to excretion. V-Zole (Tinidazole) is partly metabolized by oxidation, hydroxylation, and conjugation. V-Zole (Tinidazole) is the major drug-related constituent in plasma after human treatment, along with a small amount of the 2-hydroxymethyl metabolite.
V-Zole (Tinidazole) is biotransformed mainly by CYP3A4. In an in vitro metabolic drug interaction study, V-Zole (Tinidazole) concentrations of up to 75 µg/mL did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.
The potential of V-Zole (Tinidazole) to induce the metabolism of other drugs has not been evaluated.
Elimination: The plasma half-life of V-Zole (Tinidazole) is approximately 12-14 hours. V-Zole (Tinidazole) is excreted by the liver and the kidneys. V-Zole (Tinidazole) is excreted in the urine mainly as unchanged drug (approximately 20-25% of the administered dose). Approximately 12% of the drug is excreted in the feces.
Patients with impaired renal function: The pharmacokinetics of V-Zole (Tinidazole) in patients with severe renal impairment (CrCL < 22 mL/min) are not significantly different from the pharmacokinetics seen in healthy subjects. However, during hemodialysis, clearance of V-Zole (Tinidazole) is significantly increased; the half-life is reduced from 12.0 hours to 4.9 hours. Approximately 43% of the amount present in the body is eliminated during a 6-hour hemodialysis session . The pharmacokinetics of V-Zole (Tinidazole) in patients undergoing routine continuous peritoneal dialysis have not been investigated.
Patients with impaired hepatic function: There are no data on V-Zole (Tinidazole) pharmacokinetics in patients with impaired hepatic function. Reduction of metabolic elimination of metronidazole, a chemically-related nitroimidazole, in patients with hepatic dysfunction has been reported in several studies .
Antibacterial: Culture and sensitivity testing of bacteria are not routinely performed to establish the diagnosis of bacterial vaginosis ; standard methodology for the susceptibility testing of potential bacterial pathogens, Gardnerella vaginalis, Mobiluncus spp. or Mycoplasma hominis, has not been defined. The following in vitro data are available, but their clinical significance is unknown. V-Zole (Tinidazole) is active in vitro against most strains of the following organisms that have been reported to be associated with bacterial vaginosis:
Antiprotozoal: V-Zole (Tinidazole) demonstrates activity both in vitro and in clinical infections against the following protozoa: Trichomonas vaginalis; Giardia duodenalis (also termed G. lamblia); and Entamoeba histolytica.
For protozoal parasites, standardized susceptibility tests do not exist for use in clinical microbiology laboratories.
Drug Resistance: The development of resistance to V-Zole (Tinidazole) by G. duodenalis, E. histolytica, or bacteria associated with bacterial vaginosis has not been examined.
Cross-resistance: Approximately 38% of T. vaginalis isolates exhibiting reduced susceptibility to metronidazole also show reduced susceptibility to V-Zole (Tinidazole) in vitro. The clinical significance of such an effect is not known.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of V-Zole (Tinidazole) and other antibacterial drugs, V-Zole (Tinidazole) should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
V-Zole (Tinidazole) was mutagenic in the TA 100, S. typhimurium tester strain both with and without the metabolic activation system and was negative for mutagenicity in the TA 98 strain. Mutagenicity results were mixed (positive and negative) in the TA 1535, 1537, and 1538 strains. V-Zole (Tinidazole) was also mutagenic in a tester strain of Klebsiella pneumonia. V-Zole (Tinidazole) was negative for mutagenicity in a mammalian cell culture system utilizing Chinese hamster lung V79 cells (HGPRT test system) and negative for genotoxicity in the Chinese hamster ovary (CHO) sister chromatid exchange assay. V-Zole (Tinidazole) was positive for in vivo genotoxicity in the mouse micronucleus assay.
In a 60-day fertility study, V-Zole (Tinidazole) reduced fertility and produced testicular histopathology in male rats at a 600 mg/kg/day dose level (approximately 3-fold the highest human therapeutic dose based upon body surface area conversions). Spermatogenic effects resulted from 300 and 600 mg/kg/day dose levels. The no observed adverse reaction level for testicular and spermatogenic effects was 100 mg/kg/day (approximately 0.5-fold the highest human therapeutic dose based upon body surface area conversions). This effect is characteristic of agents in the 5-nitroimidazole class.
A repeated-dose toxicology study has been performed in beagle dogs using oral dosing of V-Zole (Tinidazole) at 100 mg/kg/day, 300 mg/kg/day, and 1000 mg/kg/day for 28-days. On Day 18 of the study, the highest dose was lowered to 600 mg/kg/day due to severe clinical symptoms. The two compound-related effects observed in the dogs treated with V-Zole (Tinidazole) were increased atrophy of the thymus in both sexes at the middle and high doses, and atrophy of the prostate at all doses in the males. A no-adverse-effect level (NOAEL) of 100 mg/kg/day for females was determined. There was no NOAEL identified for males because of minimal atrophy of the prostate at 100 mg/kg/day (approximately 0.9-fold the highest human dose based upon plasma AUC comparisons).
|Outcome||V-Zole (Tinidazole) |
1 g × 5 days
|V-Zole (Tinidazole) |
2 g × 2 days
|% Cure||% Cure||% Cure|
97.5% CI 3
97.5% CI 3
Nugent Score Cure
97.5% CI 3
Nugent score of at least 4
2Difference in cure rates (Tindamax-placebo)
3CI: confidence interval
p-values for both V-Zole (Tinidazole) regimens vs. placebo for therapeutic, clinical and
Nugent score cure rates for both 2 and 5 days <0.001
The therapeutic cure rates reported in this clinical study conducted with V-Zole (Tinidazole) were based on resolution of 4 out of 4 Amsel's criteria and a Nugent score of <4. The cure rates for previous clinical studies with other products approved for bacterial vaginosis were based on resolution of either 2 or 3 out of 4 Amsel's criteria. At the time of approval for other products for bacterial vaginosis, there was no requirement for a Nugent score on Gram stain, resulting in higher reported rates of cure for bacterial vaginosis for those products than for those reported here for V-Zole (Tinidazole).
Depending on the reaction of the V-Zole after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider V-Zole not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is V-Zole addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
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The information was verified by Dr. Rachana Salvi, MD Pharmacology