FAGYX

A nitroimidazole antitrichomonal agent effective against

Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections.

For the treatment of trichomoniasis caused by T. vaginalis in both female and male patients.

Also for the treatment of giardiasis caused by G. duodenalis in both adults and pediatric patients older than three years of age and for the treatment of intestinal amebiasis and amebic liver abscess caused by E. histolytica in both adults and pediatric patients older than three years of age.

Tinidazole is a synthetic antiprotozoal agent.

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.

Tinidazole does not appear to have activity against most strains of vaginal lactobacilli.

Rapidly and completely absorbed under fasting conditions.

Administration with food results in a delay in T max of approximately 2 hours and a decline in C max of approximately 10% and an AUC of 901.6 ± 126.5 mcg hr/mL.

Hepatic, mainly via CYP3A4.

Tinidazole, like metronidazole, is significantly metabolized in humans prior to excretion.

Tinidazole is partly metabolized by oxidation, hydroxylation and conjugation.

Tinidazole is the major drug-related constituent in plasma after human treatment, along with a small amount of the 2-hydroxymethyl metabolite.

Tinidazole crosses the placental barrier and is secreted in breast milk.

Tinidazole is excreted by the liver and the kidneys.

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.

The elimination half-life is 13.2±1.4 hours and the plasma half-life is 12-14 hours.

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There are no reported overdoses with tinidazole in humans.

In acute studies with mice and rats, the LD for mice was generally > 3,600 mg/kg for oral administration and was > 2,300 mg/kg for intraperitoneal administration.

In rats, the LD was > 2,000 mg/kg for both oral and intraperitoneal administration.

The use of tinidazole is contraindicated

In patients with a previous history of hypersensitivity to tinidazole or other nitroimidazole derivatives.

Reported reactions have ranged in severity from urticaria to Stevens-Johnson syndrome.

In patients with

Cockayne syndrome.

Severe irreversible hepatotoxicity/acute liver failure with fatal outcomes have been reported after intiation of metronidazole, another nitroimidazole drug, structurally related to tinidazole, in patients with Cockayne syndrome Prior history of hypersensitivity to tinidazole or other nitroimidazole derivatives Patients with Cockayne Syndrome.

a single 2 g oral dose taken with food.

Treat sexual partners with the same dose and at the same time Giardiasis: Adults: a single 2 g dose taken with food.

Pediatric patients older than three years of age: a single dose of 50 mg/kg (up to 2 g) with food Amebiasis, Intestinal: Adults: 2 g per day for 3 days with food.

Pediatric patients older than three years of age: 50 mg/kg/day (up to 2 g per day) for 3 days with food.

Amebic liver abscess

Adults: 2 g per day for 3-5 days with food.

Pediatric patients older than three years of age: 50 mg/kg/day (up to 2 g per day) for 3-5 days with food Bacterial vaginosis: Adult women: 2 g once daily for 2 days taken with food, or 1 g once daily for 5 days taken with food 2.1 Dosing Instructions It is advisable to take tinidazole with food to minimize the incidence of epigastric discomfort and other gastrointestinal side-effects.

Food does not affect the oral bioavailability of tinidazole.

Alcoholic beverages should be avoided when taking tinidazole and for 3 days afterwards. 2.2 Compounding of the Oral Suspension For those unable to swallow tablets, tinidazole tablets may be crushed in artificial cherry syrup to be taken with food.

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. 2.3 Trichomoniasis The recommended dose in both females and males is a single 2 g oral dose taken with food.

Since trichomoniasis is a sexually transmitted disease, sexual partners should be treated with the same dose and at the same time. 2.4 Giardiasis The recommended dose in adults is a single 2 g dose taken with food.

In pediatric patients older than three years of age, the recommended dose is a single dose of 50 mg/kg (up to 2 g) with food. 2.5 Amebiasis Intestinal: The recommended dose in adults is a 2 g dose per day for 3 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 days with food.

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. 2.6 Bacterial Vaginosis The recommended dose is a 2 g oral dose once daily for 2 days taken with food or a 1 g oral dose once daily for 5 days taken with food.

The use of tinidazole in pregnant patients has not been studied for bacterial vaginosis.

USP 250 mg are pink color, circular shaped film coated scored tablets with "250" debossed on one side and " T│P" on the other side, supplied in bottles with child-resistant caps as: NDC 64980-426-02 Bottle of 20 Tinidazole Tablets USP 500 mg are pink color, capsule shaped film coated scored tablets with "500" debossed on one side and " T│P" on the other side, supplied in bottles with child-resistant caps as: NDC 64980-427-12 Bottle of 12 Storage: Store at controlled room temperature 20-25° C (68-77° F); excursions permitted to 15-30° C (59-86° F) .

Protect contents from light.

Available published data from a case-control study and case report with Tinidazole Tablets use in pregnant women are insufficient to identify a risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.

There are risks associated with untreated lower genital tract infections during pregnancy.

In animal reproduction studies, oral administration of tinidazole to pregnant mice and rats during organogenesis at and 3 times, respectively, the maximum recommended human dose (based on body surface area comparison) showed a slight increase in fetal mortality in rats at the highest dose, with no other adverse fetal effects noted in either species.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.

All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

In the

U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Embryo-fetal developmental toxicity studies in pregnant mice administered oral tinidazole on gestation days (GD) 7 to 12 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 administered oral tinidazole on GD to 14, 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 surviving rat neonates following maternal doses as high as 600 mg/kg (3-fold the highest human therapeutic dose based upon body surface area conversions).

Females and Males of Reproductive Potential Infertility Infertility Males Based on findings in rodents, Tinidazole may impair fertility in males of reproductive potential.

It is not known whether effects on fertility are reversible.

Other than for use in the treatment of giardiasis and amebiasis in pediatric patients older than three years of age, safety and effectiveness of tinidazole in pediatric patients have not been established.

For those unable to swallow tablets, tinidazole tablets may be crushed in artificial cherry syrup, to be taken with food.

Clinical studies of tinidazole did not include sufficient numbers of subjects aged and over to determine whether they respond differently from younger subjects.

In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.