novobiocin

Action and Spectrum

Actions and Spectrum 

Actions: 

novobiocin is an antibiotic that primarily acts by inhibiting DNA gyrase, an enzyme involved in bacterial DNA replication and transcription. This inhibition disrupts DNA synthesis and cellular processes, leading to bacterial cell death. 

Spectrum: 

novobiocin has a narrower spectrum of activity, mainly targeting gram-positive bacteria such as Staphylococcus, Streptococcus, and Enterococcus species. Depending on concentration and conditions, it can exhibit both bacteriostatic and bactericidal effects. Over time, bacterial resistance to novobiocin can develop. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Myocarditis 

Leukopenia 

Pancytopenia 

Eosinophilia 

Hemolytic anemia 

Jaundice 

Pneumonitis 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Severe liver impairment 

Cautions: 

• Renal impairment 
• Drug interactions 
• Bacterial resistance 
• Pediatric use 
• Elderly patients 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

The drug is contraindicated during pregnancy. 

Breastfeeding warnings:  

The drug is not indicated during lactation.  

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

<b>Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

novobiocin primarily targets bacterial DNA gyrase, an essential enzyme in DNA replication, transcription, and repair. DNA gyrase introduces negative supercoils into the bacterial DNA molecule to relieve torsional stress generated during these processes. novobiocin inhibits the activity of DNA gyrase by binding to its B subunit, preventing proper DNA supercoiling and disrupting bacterial DNA synthesis and replication. This ultimately leads to the inhibition of bacterial growth and, at higher concentrations, bacterial cell death. 

Pharmacodynamics: 

• Bacteriostatic: At lower concentrations, novobiocin primarily inhibits bacterial growth by interfering with DNA gyrase and causing disruptions in DNA-related processes. Bacterial replication is slowed down, and the bacterial population doesn’t increase. 
• Bactericidal: At higher concentrations or under certain circumstances, novobiocin can exert a bactericidal effect. This means that it directly leads to bacterial cell death. The disruption of DNA replication and transcription, along with other cellular processes, can culminate in the destruction of the bacterial cell. 

Pharmacokinetics: 

Absorption 

novobiocin is administered orally or intravenously. After oral intake, it is absorbed from the gastrointestinal tract. 

Distribution 

novobiocin, including various tissues and body fluids, is widely distributed in the body. It minimally crosses the blood-brain barrier. 

Metabolism 

novobiocin undergoes metabolism primarily in the liver through glucuronidation and other conjugation reactions. 

Elimination and Excretion 

The metabolites of novobiocin are primarily excreted in the urine. 

Adminstartion

Administration: 

novobiocin is available in tablet or capsule form for oral administration. These are taken by mouth with a glass of water. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: novobiocin 

Pronounced as: no-vo-by-o-sin 

Why do we use novobiocin? 

novobiocin is an antibiotic used to treat bacterial infections, particularly those caused by certain gram-positive bacteria. Its use has become less common over time due to the development of bacterial resistance and the availability of more effective and broader-spectrum antibiotics.