Ofloxacin

Registered South African indications:

• External ocular infections caused by ofloxacin susceptible bacteria

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to other quinolones

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Porphyria
• Infants
  - Treatment of conjunctivitis in neonates
  - Neonates with ophthalmia neonatorum caused by Neisseria gonorrhoeae or Chlamydia trachomatis
• Women
• Prolonged use
• Worsening of infection
• Pre-existing corneal epithelial defect
• Pre-existing corneal ulcer (including the presence of large ulcers)
• Concomitant ocular conditions (e.g. severe dry eye)
• Systemic inflammatory diseases (e.g rheumatoid arthritis)
• High doses
• Sun or UV-exposition
• Known risk factors for prolongation of QT interval
  - Cardiac disease (e.g. heart failure, myocardial infarction, bradycardia)
  - Congenital long QT syndrome
  - Uncorrected electrolyte imbalance (e.g. hypokalaemia, hypomagnesaemia)
  - Coadministration with agents that are known to prolong the QT interval (e.g. Class IA and III anti-arrhythmics, tricyclic antidepressants, macrolides, antipsychotics)
• Concomitant use of contact lenses
• Coadministration with ocular steroids or non-steroidal anti-inflammatory drugs
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: opd

Dosages below include:

• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

Infections caused by: Some Gram-negative bacteria, such as Acinetobacter calcoaceticus var. anitratum, and A. calcoaceticus var. iwoffi, Enterobacter sp. including E. cloacae, Haemophilus sp, including H. influenza and H. aegyptius, Klebsiella sp., including K. Pneumoniae, Moraxella sp., Morganella morganii, Proteus sp., including P. Mirabilis, Pseudomonas sp., including P. Aeruginosa, P. cepacia, and P. fluoroscens and Serratia sp., including S. marcescens; Some Gram-positive bacteria, such as Bacillus sp., Corynebacterium sp., Micrococcus sp., Staphylococcus sp., including S. aureus and S. epidermidis, Streptococcus sp., including S. Pneumoniae, S. viridans and Beta-haemolytic

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African registered indications and dosages

Bacterial conjunctivitis

• Ophthalmic (opd): Day 1-2: 1 drop in affected eye(s), 2-4hrly; Day 3 onwards: 1 drop, 6hrly; Max duration: 10 days

Bacterial corneal ulcer

• Ophthalmic (opd): Day 1-2: 1-2 drops into affected eye, every 30min while awake; Awaken at 4 and 6hrs after retiring to instil 1-2 drops; Day 3 through 7 to 9: 1-2 drops, hourly while awake; Day 7-9 until treatment completion: 1-2 drops, 6hrly

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Indications and dosages registered in other jurisdictions

External ocular infections caused by ofloxacin-sensitive organisms
- Conjunctivitis
- Keratoconjunctivitis

• Ophthalmic (opd): Day 1-2: 1-2 drops in affected eye(s), 2-4hrly; Day 3 onwards: 1-2 drops, 6hrly;  Max treatment duration: 10 days

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Topical ocular instillation

Paed. forms avail. in SA and covered in this monograph: opd

Paed. dosages below include:

• South African Standard Treatment Guideline indications and dosages
• South African registered indications and dosages
• Indications and dosages registered in other jurisdictions

Infections caused by: Some Gram-negative bacteria, such as Acinetobacter calcoaceticus var. anitratum, and A. calcoaceticus var. iwoffi, Enterobacter sp. including E. cloacae, Haemophilus sp, including H. influenza and H. aegyptius, Klebsiella sp., including K. Pneumoniae, Moraxella sp., Morganella morganii, Proteus sp., including P. Mirabilis, Pseudomonas sp., including P. Aeruginosa, P. cepacia, and P. fluoroscens and Serratia sp., including S. marcescens; Some Gram-positive bacteria, such as Bacillus sp., Corynebacterium sp., Micrococcus sp., Staphylococcus sp., including S. aureus and S. epidermidis, Streptococcus sp., including S. Pneumoniae, S. viridans and Beta-haemolytic

Specific doses based on individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African Standard Treatment Guideline indications and dosages

Surgical prophylaxis for middle ear ventilation tubes

• Ophthalmic (opd): 1 drop in the affected ear, after the procedure
  (STG, Paed. 2022)

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South African registered indications and dosages

Bacterial conjunctivitis
Bacterial corneal ulcer

Younger than 1 year

• Not established for use

Older than 1 year

• See adult dosage

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Indications and dosages registered in other jurisdictions

External ocular infections caused by ofloxacin-sensitive organisms
- Conjunctivitis
- Keratoconjunctivitis

Younger than 1 year

• Not established for use

Older than 1 year

• See adult dosage

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Safety and efficacy in the treatment of ophthalmia neonatorum has not been established

Pregnancy

• Caution; not recommended
• There have been no adequate and well-controlled studies performed in pregnant women. Since systemic quinolones have been shown to cause arthropathy in immature animals, it is recommended that ofloxacin not be used in pregnant women

Breastfeeding

• Caution; not recommended
• Because ofloxacin and other quinolones taken systemically are excreted in breast milk, and there is potential for harm to breastfeeding infants, a decision should be made whether to temporarily discontinue breastfeeding or not to administer the drug, taking into account the importance of the drug to the mother

Renal Impairment

• Caution; no information available
  The requirement for dose adjustment is unlikely due to low systemic absorption

Hepatic Impairment

• Caution; no information available
  The requirement for dose adjustment is unlikely due to low systemic absorption

Elderly

• Caution; no information available

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Dizziness

Cardiovascular Disorders

• Ventricular arrhythmia
• Torsades de pointes (predominantly in patients with risk factors for QT prolongation)
• QT prolongation

Gastrointestinal Disorders

• Nausea

Skin and Subcutaneous Tissue Disorders

• Stevens-Johnson syndrome
• Toxic epidermal necrolysis

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions
  - Signs and symptoms of eye allergy (e.g eye pruritus and eyelid pruritus)
• Anaphylactic reactions
  - Angioedema
  - Dyspnoea
  - Anaphylactic shock
  - Oropharyngeal swelling
  - Facial oedema
  - Tongue swollen

Sensory Disorders

• Eye irritation
• Ocular discomfort
• Keratitis
• Conjunctivitis
• Blurred vision
• Photophobia
• Eye oedema
• Foreign body sensation in eyes
• Increased lacrimation
• Dry eye
• Eye pain
• Ocular hyperaemia
• Periorbital oedema (including eyelid oedema)

• Caffeine
• Theophylline
• Non-steroidal anti-inflammatory drugs
• QT-prolonging agents
• Class IA antiarrhythmics
• Class III antiarrhythmics
• Tricyclic antidepressants
• Macrolides
• Antipsychotics

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No interaction studies have been performed. However, the above interactions have been shown with the systemic administration of some quinolones

None routine

The primary mechanism of action of ofloxacin is through inhibition of bacterial DNA gyrase, the enzyme responsible for maintaining the structure of DNA. Ofloxacin is not subject to degradation by beta-lactamase enzymes nor is it modified by enzymes such as aminoglycoside adenylases or phosphorylases, or chloramphenicol acetyltransferase. Ofloxacin is a synthetic fluorinated 4-quinolone antibacterial agent with activity against a broad spectrum of Gram-negative and to a lesser degree Gram-positive organisms. Ofloxacin has been shown to be active against most strains of the organisms stated below both in vitro and clinically in ophthalmic infections. Clinical trial evidence of the efficacy of ofloxacin against S. pneumoniae was based on a limited number of isolates.

Spectrum of activity: Some Gram-negative bacteria, such as Acinetobacter calcoaceticus var. anitratum, and A. calcoaceticus var. iwoffi, Enterobacter sp. including E. cloacae, Haemophilus sp, including H. influenza and H. aegyptius, Klebsiella sp., including K. Pneumoniae, Moraxella sp., Morganella morganii, Proteus sp., including P. Mirabilis, Pseudomonas sp., including P. Aeruginosa, P. cepacia, and P. fluoroscens and Serratia sp., including S. marcescens; Some Gram-positive bacteria, such as Bacillus sp., Corynebacterium sp., Micrococcus sp., Staphylococcus sp., including S. aureus and S. epidermidis, Streptococcus sp., including S. Pneumoniae, S. viridans and Beta-haemolytic

Eye drops (per ml) 3mg

• Exocin (Allergan) originator
• Octin (Cipla Medpro)

Also available in the following forms: Tablet and injection