trovafloxacin

Action and Spectrum

Actions and spectrum: 

trovafloxacin is a broad-spectrum antibiotic that prevents the uncoiling of supercoiled DNA in bacteria by inhibiting the activity of DNA gyrase and topoisomerase IV. It works well against     gram +ve bacteria rather than on gram -ve bacteria. 

Due to its various adverse effects and hepatotoxicity, it has been withdrawn from the market in many countries. 

It is mainly used in the treatment of infections due to Neisseria gonorrhoeae i.e., uncomplicated urethral gonorrhoea in males and endocervical and rectal gonorrhoea in females. It is also used to treat cervicitis due to Chlamydia trachomatis. 

Drug Interaction

Adverse Reaction

Frequency not defined. 

Nausea 

Vomiting 

Diarrhea 

Headache 

Dizziness 

Tendon rupture 

Tendonitis 

Hepatic toxicity 

Rashes on skin 

Difficulty breathing 

Numbness 

Anxiety 

Depression 

Peripheral neuropathy 

Acute interstitial nephritis 

Black Box Warning

Black Box Warning: 

For restricted use only due to severe hepatotoxicity  

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Hepatic failure has been observed in both male and females receiving trovafloxacin treatment  

Anaphylactic or hypersensitivity reactions may occur  

Caution: 

trovafloxacin, like other quinolones, should be used with caution in individuals with known or suspected CNS problems, such as severe cerebral atherosclerosis, epilepsy, and other risk factors for seizures. 

early all antibacterial agents, including trovafloxacin, have been linked to pseudomembranous colitis, which can range in severity from moderate to life-threatening. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C 

Lactation:  

Studies show that Trovafloxacin can be detected in breast milk. It is not recommended for lactating mothers.  

Pregnancy category: 

 Category A: Studies that were well-controlled and met expectations revealed no risk to the foetus `in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

trovafloxacin is a broad-spectrum antibiotic used in the treatment of bacterial infections particularly effective against gram-positive bacteria. trovafloxacin is a fluoronaphtyridone belonging to fluoroquinolones. It is used mainly in the treatment of gonorrhoea and chlamydia.  

Pharmacodynamics: 

Inhibition of growth of bacteria by trovafloxacin results is due to alteration of DNA gyrase and topoisomerase IV. DNA gyrase, an important enzyme is known for the process of replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme that plays a key role in the separation of the chromosomal DNA during bacterial cell division. 

Pharmacokinetics:  

Absorption 

It is well absorbed in the gastrointestinal tract reaching an approximate bioavailability of about 88%.  

Distribution 

It is well distributed in the urinary tract, soft tissues and fluids, respiratory tract etc., owing to its good tissue penetration capacity. 

Metabolism 

It is mainly metabolized through Cytochrome P450 by conjugation. Major metabolites include, ester glucuronide excreted in urine and the N-acetyl metabolite that appears in faeces and urine. 

Elimination and excretion 

Approximately 50% of the orally administered dose is excreted unchanged through urine and faeces.  

Half-life:  

In case of oral administration, half-life ranges from 9.1 to 12.2 hours over the dose of 100 to 200 mg tablets. Following intravenous infusion, half-life ranges from 9.4 to 12.7 hours over a dose range of 100 to 300 mg. 

Adminstartion

Administration: 

It can be administered orally as tablets or through IV. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: trovaloxacin  

Why do we use trovafloxacin? 

trovafloxacin is a broad-spectrum antibiotic that falls under the class of fluoroquinolones. It is suggested in the treatment of gonorrhoea and chlamydia. Its use is restricted due to severe hepatic toxicity.