Tinidazole (tinidazole)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tinidazole, a nitroimidazole derivative, is an antiprotozoal and antibacterial agent.
Tinidazole is a 5-nitroimidazole antiprotozoal and antibacterial agent.
Tinidazole is amebicidal, trichomonacidal, and bactericidal in action. Tinidazole is a prodrug that is activated after entry into cells of susceptible organisms where the nitro group is reduced to form short-lived radical anions. Although the exact mechanism of action has not been fully elucidated, it is believed that these free radicals interfere with cellular DNA.
Studies using cell extracts of Trichomonas indicate that the nitroimidazole group of tinidazole is reduced within the cells and generates the free nitro radical, which appears to be responsible for the drug's anti-infective activity. Similarly, the nitro group is reduced within anaerobic bacteria resulting in reactive intermediates; chemically reduced tinidazole has been shown to release nitrites and cause damage to purified bacterial DNA in vitro. Specific information on the mechanism of tinidazole's activity against Giardia and Entamoeba histolytica is not available.
Following oral administration, tinidazole is rapidly absorbed and peak plasma concentrations of the drug are attained within about 2 hours. The estimated oral bioavailability of the drug exceeds 90%. Administration with food delays the time to peak plasma concentrations by approximately 2 hours and decreases peak plasma concentrations by 10%, but does not affect the area under the plasma concentration-time curve (AUC) or elimination half-life.
Pharmacokinetic parameters reported with an extemporaneous oral suspension of tinidazole containing 66.7 mg/mL (prepared using crushed 500-mg tablets and cherry syrup) in healthy individuals after an overnight fast are similar to those reported with tablets swallowed whole under fasted conditions. Tinidazole is 12% bound to plasma proteins. The drug is widely distributed into body tissues and fluids (e.g., saliva, female reproductive tract, gallbladder, bile, bowel, prostate tissue) and crosses the blood-brain barrier and placenta.
Tinidazole is partially metabolized via oxidation, hydroxylation, and conjugation; the drug is metabolized principally by cytochrome P-450 (CYP) isoenzyme 3A4. Approximately 20-50% of an oral dose is excreted unchanged in urine and approximately 12% is excreted in feces. The plasma half-life of tinidazole is approximately 12-14 hours.
USES: Tinidazole is an antibiotic that is used to treat certain types of vaginal infections (bacterial vaginosis, trichomoniasis). It is also used to treat certain types of parasite infections (giardiasis, amebiasis). It works by stopping the growth of certain bacteria and parasites.
This antibiotic treats only certain bacterial and parasitic infections. It will not work for viral infections (such as common cold, flu). Using any antibiotic when it is not needed can cause it to not work for future infections.
Generic name: tinidazole
Pronunciation: (tye-NID-a-zole)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Tinidazole
Indications
The following indications are listed for Tinidazole:
- Acute Intestinal Amebiasis Due To Entamoeba Histolytica
- Bacterial Vaginosis
- Giardiasis
- Liver Abscess Amebiasis Due To Entamoeba Histolytica
- Trichomoniasis
Also known as: Amebic Liver Abscess Due To Entamoeba Histolytica, Bacterial Vaginitis, Lambliasis, Lambliosis, Trichomonas Vaginalis Infection.
Dosing
No dosing information is available for this tab.
Tinidazole is administered orally with food.
Although food does not affect oral bioavailability of tinidazole, the drug should be given with meals to reduce the incidence of epigastric discomfort and other adverse GI effects.
Alcohol should be avoided during tinidazole treatment and for 3 days after the last dose of the drug. (See Drug Interactions: Alcohol and Propylene Glycol.)
Tinidazole is commercially available as tablets containing 250 or 500 mg of the drug. For children and other patients unable to swallow tablets, the 500-mg tablets can be used to prepare an extemporaneous oral suspension.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Formal drug interaction studies have not been performed to date with tinidazole; however, interactions reported with metronidazole, a nitroimidazole anti-infective chemically related to tinidazole, may also occur in patients receiving tinidazole. For further information on interactions associated with metronidazole, see Drug Interactions, in Metronidazole 8:30.92.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Tinidazole is contraindicated in patients with a history of hypersensitivity to tinidazole or other nitroimidazole derivatives.
Tinidazole is contraindicated during the first trimester of pregnancy. (See Pregnancy under Warnings/Precautions: Specific Populations, in Cautions.)
Tinidazole is contraindicated in breast-feeding women. (See Lactation under Warnings/Precautions: Specific Populations, in Cautions.)
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 1% or more of patients receiving a single 2-g dose of tinidazole include GI effects (metallic/bitter taste, nausea, anorexia, dyspepsia/cramps/epigastric discomfort, vomiting, constipation) and nervous system effects (weakness/fatigue/malaise, dizziness, headache).
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of tinidazole have not been established in pediatric patients 3 years of age or younger. Some data are available regarding safety and efficacy of the drug for the treatment of giardiasis in pediatric patients younger than 3 years of age+.
Safety and efficacy of tinidazole in pediatric patients have been established only for the treatment of amebiasis or giardiasis in children older than 3 years of age.
Pediatric patients should be monitored closely when the duration of tinidazole treatment exceeds 3 days (e.g., for treatment of amebic liver abscess). Only limited data are available regarding tinidazole treatment exceeding 3 days in pediatric patients, although the drug has been used for 5 days in a small number of children without an increase in the severity and incidence of adverse effects.
Adverse effects reported in pediatric patients receiving tinidazole are similar in nature and frequency to those reported in adults and include nausea, vomiting, diarrhea, taste change, anorexia, and abdominal pain.
Safety and efficacy of tinidazole have not been evaluated in pregnant women, including use of the drug for the treatment of bacterial vaginosis in pregnant women.
Because tinidazole crosses the placenta and enters fetal circulation, the drug is contraindicated during the first trimester of pregnancy. The US Centers for Disease Control and Prevention (CDC) states that use of tinidazole for the treatment of trichomoniasis or bacterial vaginosis in pregnant women should avoided.
Tinidazole is distributed into human milk in concentrations similar to serum concentrations and can be detected in milk for up to 72 hours after administration.
Tinidazole is contraindicated in breast-feeding women. Breast-feeding should be interrupted during tinidazole treatment and for 3 days (72 hours) following the last dose.
Dosage of tinidazole in geriatric patients generally should be selected with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.
Clinical studies of tinidazole did not include a sufficient number of patients 65 years of age or older to determine whether geriatric adults respond differently than younger adults.
Dosage for geriatric patients should be selected with caution because of possible age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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