Description and Composition of Timofloxacin
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Pharmacodynamics of Timofloxacin
Timofloxacin is fluoroquinolone antibiotic. Ofloxacin is bactericidal and its mechanism or mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian.
Pharmacokinetics of Timofloxacin
Bioavailability of Timofloxacin in the tablet formulation is approximately 98%.
Maximum serum concentration is achieved in one to two hours after an oral dose. Protein binding of Ofloxacin is about 32%. Its elimination is mainly by renal excretion. Between 65% and 80% of an administered oral dose of ofloxacin is excreted unchanged via the kidneys within 48 hours of dosing. About 4 to 8% of an ofloxacin dose is excreted in the feces. This indicates a small degree of biliary excretion of ofloxacin. Half Life Ofloxacin is about 9 hours.
Indications and uses of Timofloxacin
Timofloxacin is recommended for the treatment of infections caused by Ofloxacin sensitive pathogens such as:
- Urinary tract infections
- Skin and soft-tissue infections
- Kidney infections
- Urethritis and Cervicitis gonorrhoea.
- Gastrointestinal tract infections including typhoid fever and paratyphoid
- Respiratory tract infections including ENT infections
- Bone and joint infections.
- Chronic and recurrent infections of the ear, nose, and throat, especially if caused by Gram-negative pathogens.
Dosage and Administration of Timofloxacin
Dosage of Ofloxacin depends on the severity and the nature of the Infection. Unless prescribed otherwise, the following doses are recommended:
Urinary tract infections
Mild to Moderate: 200mg daily
Severe: 400mg twice daily
Respiratory tract infections: 400mg daily
Other Infections: 400mg daily
Oral doses up to 400mg Ofloxacin may be given as single dose, preferably in the morning. It can equally be given in two divided doses.
Larger doses such as 800 mg must be divided into two separate doses. It is important that the tablets should be taken at approximately equal intervals.
Ofloxacin solution is only intended for SLOW intravenous infusion; it is administered once or twice daily. The infusion time for Ofloxacin IV should not be less than 30 minutes for 200 mg. This is of particular importance when ofloxacin is administered concomitantly with drugs that can lead to a reduction in blood pressure or with barbiturate-containing anaesthetics. Generally, individual doses are to be given at approximately equal intervals.
Timofloxacin should be used with caution in patients with epilepsy and those who have suffered from previous Central Nervous System disorders.
Contra-indications or when not to use Timofloxacin
Timofloxacin is contraindicated in patients who are hypersensitive to Ofloxacin or other Quinolone carboxylic acid derivatives. It is also contraindicated in epileptics, children, adolescents in the growth phase, pregnancy and breast feeding.
Side effects of Timofloxacin
Timofloxacin is generally well tolerated.
However, its side effects may include the following:
- allergic reactions
- Cardiovascular systems disturbance
- joint and muscle pains,
- blood dyscrasias,
- GIT disturbances
- transient rise of serum creatinine liver enzymes and bilirubin levels
Drug Interactions with Timofloxacin
- Antacids containing Aluminium or Magnesium hydroxidos or iron preparations reduce the absorption of Ofloxacin.
- Ofloxacin may cause a slight increase in serum concentrations of glibenclamide administered concurrently
- A pronounced lowering of the cerebral seizure threshold has been reported when quinolones are administered with other drugs that reduce seizure threshold or with certain nonsteroidal anti-inflammatory drugs
Timofloxacin Overdosage & Its Management
Symptoms of Timofloxacin overdose may include:
- numbness and
- swelling of the face,
- hot and cold flushes,
- slurred speech, and
In the event of an acute overdose, the stomach should be emptied. The patient should be observed and appropriate hydration maintained. Ofloxacin is not efficiently removed by hemodialysis or peritoneal dialysis.