Pharmacopeia
MOXIFLOXACIN
Core pharmacology
- Class Group
ANTIBIOTIC:
QUINOLONE- Introduction
Quinolone
- Presentation
PO and IV
- Mechanism of action
Bacteriocidal antimicrobials that block DNA replication by blocking tropoisomerase enzymes, which are essential for the supercoiling, replication and separation of circular bacterial DNA
- Antimicrobial Spectrum
1. Gram positives
- Better strep pneumonia cover
2. Gram negatives
- Including salmonella, Neisseria, pseudomonas, E. Coli
3. Anaerobes
- Modest including B. Fragilis
4. Atypicals
Legionella, mycoplasma, Rickettsia, Chlamydia- Resistance Mechanism
Alteration in target enzyme – changes to the DNA binding surface of DNA supergyrase infers resistance
Alteration in drug entry – altered expression of outer membrane porin proteins that form channels for passive diffusion of moxifloxacin
Increase in efflux of drug – expression of nonspecific energy dependent efflux pumps which remove drug- Adverse Effects Toxicity
1. CNS Toxicity- GABA antagonists and may precipitate seizures in epileptic patients, particularly in presence of NSAIDs
2. Tendonitis and tendon rupture
3. QT prolongation- Low risk of Torsade’s in absence of other predisposing factors
4. Hemolysis in G6PD
5. Photosensitivity
6. Arthralgias and cartilage toxicity (generally avoided in children)
7. Dysglycaemia (hyper and hypoglycaemia)- Absorption
90% oral absorption
Coadministration of calcium or magnesium reduces absorption
- Distribution
High CSF and tissue penetration
- Protein binding
30% PB
- Metabolism
Little hepatic metabolism
- Excretion
Renal excretion
- Half-life
T1/2= 12 hours
Renal dose adjustment not required
Anti-infectives · Anti-infectives
- Legacy Cicm Level
Level 3
- Legacy Cicm Level
Level 1