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Mechanism of action:
Quinolones block bacterial DNA synthesis by inhibiting bacterial topoisomerase Quinolones
block bacterial DNA synthesis by inhibiting bacterial topoisomerase II (DNA gyrase) and
topoisomerase IV.
Inhibition of DNA gyrase (topoisomerase II) prevents the relaxation of positively supercoiled
DNA that is required for normal transcription and replication.
Inhibition of topoisomerase IV interferes with separation of replicated chromosomal DNA into
the respective daughter cells during cell division.
Antibacterial spectrum:
Moxifloxacin is usually bactericidal against susceptible organisms.
Moxifloxacin is slightly less active than ciprofloxacin and ofloxacin against gram-negative
bacteria including gonococci, E coli, Klebsiella pneumoniae, C jejuni, Enterobacter, P aeruginosa,
Salmonella, and Shigella species. but have greater activity against gram-positive Cocci, including
S pneumoniae and some strains of enterococci and Methicillin-resistant Staphylococcus aureus
(MRSA).
Broadest spectrum Fluoroquinolone with enhanced activity against atypical pneumonia agents
and anaerobes.
Pharmacokinetics:
Route of administration: Oral, IV, drops
Absorption: well absorbed from the GIT with 80-95% bioavailability
Distribution: widely distributed to body fluids and tissues
Metabolism: Metabolized in liver via sulfate conjugation
Half life: Long half life 12-15 hours permitting once daily dosing
Excretion: Non renal , fecal route
Dosing:
Adult dose: 400mg once every 24 hours
Children dose: use and dose must be determined by your doctor
Clinical uses:
Infections of soft tissues, bones, eyes including bacterial conjunctivitis and joints and in intra-
abdominal infections
Treatment of TB and atypical mycobacterial infections
Eradication of meningococcal from carriers or for prophylaxis of infection in neutropenic cancer
patient.
Treatment of upper and lower RTI (Pseudomonas and Enterobacter)
Adverse effects:
GIT distress – most common
QTc prolongation
Tendonitis
Atrial fibrillation
Agranulocytosis
Toxicity:
Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence,
tremor, convulsions, vomiting, and diarrhea.
Contraindications:
Not recommended for children or pregnant women because they may damage growing cartilage
and cause arthropathy.
Avoided in patients with known QTc prolongation
Drug interactions:
Fluoroquinolones may increase the plasma levels of theophylline and other methylxanthines,
enhancing their toxicity.
Avoided with antiarrhythmic or other drugs that increase the QTc interval.
References:
Katzung & Trevor's Pharmacology Examination and Board Review-11th.pdf
Pharmapedia
https://www.mayoclinic.org/drugs-supplements/moxifloxacin-oral-route/proper-use/drg-20072313