Ciprofloxacin
CIPROFLOXACIN- ciprofloxacin hydrochloride solution/ drops
Aidarex Pharmaceuticals LLC
Sterile
DESCRIPTION
Ciprofloxacin Ophthalmic Solution, USP is a synthetic, sterile, multiple dose, antimicrobial for topical ophthalmic use. Ciprofloxacin is a fluoroquinolone antibacterial active against a broad spectrum of gram-positive and gram-negative ocular pathogens. It is available as the monohydrochloride monohydrate salt of 1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxo-7-(1-piperazinyl)-3-quinoline-carboxylic acid. It is a faint to light yellow crystalline powder with a molecular weight of 385.8. Its empirical formula is C17 H18 FN3 O3 •HCl•H2 O and its chemical structure is as follows:
Ciprofloxacin differs from other quinolones in that it has a fluorine atom at the 6-position, a piperazine moiety at the 7-position, and a cyclopropyl ring at the 1-position.
Each mL of Ciprofloxacin Ophthalmic Solution, USP contains:
Active: Ciprofloxacin HCl, USP 3.5 mg equivalent to 3 mg base.
Preservative: Benzalkonium Chloride 0.006%.
Inactives: Acetic Acid, Edetate Disodium 0.05%, Mannitol 4.6%, Sodium Acetate, Hydrochloric Acid and/or Sodium Hydroxide (to adjust pH) and Water for Injection. The pH is approximately 4.5 and the osmolality is approximately 300 mOsm.
CLINICAL PHARMACOLOGY
Systemic Absorption: A systemic absorption study was performed in which Ciprofloxacin Ophthalmic Solution was administered in each eye every two hours while awake for two days followed by every four hours while awake for an additional 5 days. The maximum reported plasma concentration of ciprofloxacin was less than 5 ng/mL. The mean concentration was usually less than 2.5 ng/mL.
Microbiology: Ciprofloxacin has in vitro activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of ciprofloxacin results from interference with the enzyme DNA gyrase which is needed for the synthesis of bacterial DNA.
Ciprofloxacin has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections (see INDICATIONS AND USAGE).
Gram-Positive:
Staphylococcus aureus
Staphylococcus epidermidis
Streptococcus pneumoniae
Streptococcus (Viridans Group)
Gram-Negative:
Haemophilus influenzae
Pseudomonas aeruginosa
Serratia marcescens
Ciprofloxacin has been shown to be active in vitro against most strains of the following organisms, however, the clinical significance of these data is unknown:
Gram-Positive:
Enterococcus faecalis (Many strains are only moderately susceptible)
Staphylococcus haemolyticus
Staphylococcus hominis
Staphylococcus saprophyticus
Streptococcus pyogenes
Gram-Negative:
| Acinetobacter calcoaceticus | Escherichia coli | Proteus mirabilis |
| subsp. anitratus | Haemophilus ducreyi | Proteus vulgaris |
| Aeromonas caviae | Haemophilus parainfluenzae | Providencia rettgeri |
| Aeromonas hydrophila | Klebsiella pneumoniae | Providencia stuartii |
| Brucella melitensis | Klebsiella oxytoca | Salmonella enteritidis |
| Campylobacter coli | Legionella pneumophila | Salmonella typhi |
| Campylobacter jejuni | Moraxella (Branhamella) | Shigella sonnei |
| Citrobacter diversus | catarrhalis | Shigella flexneri |
| Citrobacter freundii | Morganella morganii | Vibrio cholerae |
| Edwardsiella tarda | Neisseria gonorrhoeae | Vibrio parahaemolyticus |
| Enterobacter aerogenes | Neisseria meningitidis | Vibrio vulnificus |
| Enterobacter cloacae | Pasteurella multocida | Yersinia enterocolitica |
Other Organisms: Chlamydia trachomatis (only moderately susceptible) and Mycobacterium tuberculosis (only moderately susceptible).
Most strains of Pseudomonas cepacia and some strains of Pseudomonas maltophilia are resistant to ciprofloxacin as are most anaerobic bacteria, including Bacteroides fragilis and Clostridium difficile. The minimal bactericidal concentration (MBC) generally does not exceed the minimal inhibitory concentration (MIC) by more than a factor of 2. Resistance to ciprofloxacin in vitro usually develops slowly (multiple-step mutation).
Ciprofloxacin does not cross-react with other antimicrobial agents such as beta-lactams or aminoglycosides; therefore, organisms resistant to these drugs may be susceptible to ciprofloxacin.
Clinical Studies
Following therapy with Ciprofloxacin Ophthalmic Solution, 76% of the patients with corneal ulcers and positive bacterial cultures were clinically cured and complete re-epithelialization occurred in about 92% of the ulcers.
In 3 and 7 day multicenter clinical trials, 52% of the patients with conjunctivitis and positive conjunctival cultures were clinically cured and 70 to 80% had all causative pathogens eradicated by the end of treatment.
In a randomized, double-masked, multicenter, parallel-group clinical trial of pediatric patients with bacterial conjunctivitis, between birth and 31 days of age, patients were dosed with ciprofloxacin or another anti-infective agent. Clinical outcomes for the trial demonstrated a clinical cure rate of 80% at Day 9 and a microbiological eradication success rate of 85% at Day 9.
Please note that microbiologic eradication does not always correlate with clinical outcome in anti-infective trials.
INDICATIONS AND USAGE
Ciprofloxacin Ophthalmic Solution is indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below:
| Corneal Ulcers: | Pseudomonas aeruginosa |
| Serratia marcescens* | |
| Staphylococcus aureus | |
| Staphylococcus epidermidis | |
| Streptococcus pneumoniae | |
| Streptococcus (Viridans Group)* | |
| Conjunctivitis: | Haemophilus influenzae |
| Staphylococcus aureus | |
| Staphylococcus epidermidis | |
| Streptococcus pneumoniae |
*Efficacy for this organism was studied in fewer than 10 infections.
CONTRAINDICATIONS
A history of hypersensitivity to ciprofloxacin or any other component of the medication is a contraindication to its use. A history of hypersensitivity to other quinolones may also contraindicate the use of ciprofloxacin.
WARNINGS
NOT FOR INJECTION INTO THE EYE.
Serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported in patients receiving systemic quinolone therapy. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, tingling, pharyngeal or facial edema, dyspnea, urticaria, and itching. Only a few patients had a history of hypersensitivity reactions. Serious anaphylactic reactions require immediate emergency treatment with epinephrine and other resuscitation measures, including oxygen, intravenous fluids, intravenous antihistamines, corticosteroids, pressor amines and airway management, as clinically indicated.
Remove contact lenses before using.
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