Drug/Small Molecule:
tinidazole

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • tinidazole
Trade Names
  • Fasigyn
  • Tindamax
Brand Mixture Names

PharmGKB Accession Id:
PA10813

Description

A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections.

Source: Drug Bank

Indication

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.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Tinidazole is a prodrug and antiprotozoal agent. The nitro group of tinidazole is reduced in Trichomonas by a ferredoxin-mediated electron transport system. The free nitro radical generated as a result of this reduction is believed to be responsible for the antiprotozoal activity. It is suggested that the toxic free radicals covalently bind to DNA, causing DNA damage and leading to cell death. The mechanism by which tinidazole exhibits activity against Giardia and Entamoeba species is not known, though it is probably similar.

Source: Drug Bank

Pharmacology

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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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.

Source: Drug Bank

Protein Binding

Plasma protein binding of tinidazole is 12%.

Source: Drug Bank

Absorption

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.

Source: Drug Bank

Half-Life

Elimination half-life is 13.2 +/- 1.4 hours. Plasma half-life is 12 to 14 hours.

Source: Drug Bank

Toxicity

There are no reported overdoses with tinidazole in humans. In acute studies with mice and rats, the LD 50 for mice was generally > 3,600 mg/kg for oral administration and was > 2,300 mg/kg for intraperitoneal administration. In rats, the LD 50 was > 2,000 mg/kg for both oral and intraperitoneal administration.

Source: Drug Bank

Route of Elimination

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.

Source: Drug Bank

Volume of Distribution

  • 50 L

Source: Drug Bank

Chemical Properties

Chemical Formula

C8H13N3O4S

Source: Drug Bank

Isomeric SMILES

c1ccc2c(c1)[nH]c(n2)c3cscn3

Source: OpenEye

Canonical SMILES

CCS(=O)(=O)CCN1C(C)=NC=C1[N+]([O-])=O

Source: PharmGKB

Average Molecular Weight

247.272

Source: Drug Bank

Monoisotopic Molecular Weight

247.062676609

Source: Drug Bank

Publications related to tinidazole: 1

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Assessment of the impact of renal impairment on systemic exposure of new molecular entities: evaluation of recent new drug applications. Clinical pharmacology and therapeutics. 2009. Zhang Y, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0178-8250-40
DrugBank:
DB00911
KEGG Drug:
D01426
PubChem Compound:
5479
PubChem Substance:
46506396
7848489
ChemSpider:
5279
FDA Drug Label at DailyMed:
a0d01539-8413-4703-94cc-d221918630a1

Clinical Trials

These are trials that mention tinidazole and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.