Contra

Contra Uses, Dosage, Side Effects, Food Interaction and all others data.

Contra, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor, effective against gram positive and gram negative bacteria. The acute toxicity of Contra following systemic and topical ophthalmic application is low. Contra interferes with bacterial DNA related processes like initiation, elongation, and termination phases of replication, transcription, DNA repairing, recombination, transposition, supercoiling and relaxation of DNA. The target molecule for quinolones is the A-subunit of bacterial enzyme gyrase (topoisomerase II). The forming of a stable complex between the quinolone and the whole gyrase teramer A2B2 leads to impaired enzyme functions, resulting in a rapid killing of sensitive bacteria.

Cross-resistance has only been reported with other quinolones, but not with any other group of antibiotics. No clinical studies are available about the efficacy in cases of infections with chlamydia.

Contra is a fluoroquinolone antibiotic used to treat chronic bronchitis, as well as complicated and uncomplicated urinary tract infections. It is also used as a prophylactic or preventative treatment to prevent urinary tract infections in patients undergoing transrectal or transurethral surgical procedures. Flouroquinolones such as lomefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.

Trade Name Contra
Availability Discontinued
Generic Lomefloxacin
Lomefloxacin Other Names LFLX, Lomefloxacin, Lomefloxacine, Lomefloxacino, Lomefloxacinum
Related Drugs amoxicillin, doxycycline, ciprofloxacin, cephalexin, azithromycin, ceftriaxone, levofloxacin, Augmentin, nitrofurantoin, Keflex
Weight 0.3%, 15, 200mg
Type Eye/ear Drops, Capsule
Formula C17H19F2N3O3
Weight Average: 351.3479
Monoisotopic: 351.139447899
Protein binding

10%

Groups Approved, Investigational
Therapeutic Class 4-Quinolone preparations, Aural Anti-bacterial preparations
Manufacturer Beximco Pharmaceuticals Ltd, Jamjoom Pharmaceuticals Company
Available Country Bangladesh, Saudi Arabia
Last Updated: September 19, 2023 at 7:00 am
Contra
Contra

Uses

Contra oral preparation is used for the treatment of:

  • Uncomplicated urinary tract infections.
  • Complicated including recurrent and pyelonephritis, urinary tract infections.
  • Acute exacerbation of chronic bronchitis.
  • Skin and skin structure infections.

Prevention/Prophylaxis: Contra is used preperatively to prevent postoperative urinary tract infections in patients undergoing transurethral surgical procedures.

Contra ophthalmic preparation is used for the bacterial infections, including conjunctivitis, blepharitis, blepharoconjunctivitis which are due to Contra susceptible germs and Staphylococcus aureus- induced corneal ulcers.

Contra is also used to associated treatment for these conditions: Acute Bacterial Conjunctivitis, Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB), Blepharoconjunctivitis, Urinary Tract Infection, Bacterial blepharitis

How Contra works

Contra is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.

Dosage

Contra dosage

Typhoid fever: 400 mg once daily or 200 mg b.i.d 10-14 days. UTI infections:

  • Uncomplicated:400 mg once daily or 200 mg b.i.d 3 days.
  • Complicated:400 mg once daily or 200 mg b.i.d 10-14 days.

Bacterial Diarrhea: 400 mg once daily or 200 mg b.i.d 5-7 days.

Acute exacerbation of chronic bronchitis: 400 mg once daily 7-10 days.

Skin and skin structure infections: 400 mg once daily 10-14 days.

Prophylaxis of UTI following surgery: 400 mg Single dose 2-6 hours prior to transurethral surgery.

Adults and children (above 1 year of age): Instill 2-3 times daily 1 drop into the lower conjunctival sac. At the beginning of the treatment application should be more frequent, apply 5 drops within 20 minutes or 1 drop every hour during 6-10 hours. Duration of the treatment: 7 to 9 days.

Side Effects

Common side effects are Nausea, headache, photosensitivity, dizziness, diarrhea, dry mouth, fatigue, convulsions, CNS stimulation which may lead to tremors, restlessness, light headedness, confusion hallucinations and pseudomembranous colitis.

Slight and transient burning immediately after instillation of the eye drops has been reported in 4.7% of users. Although phototoxicity has not been reported after ophthalmic use, photosensitization is possible. Since the following allergic reactions have been reported after systemic use of Contra, they can not be excluded after topical ophthalmic use: allergic reactions, asthma, dyspnoea, urticaria, erythema, pruritus, and hypersensitization.

Toxicity

Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure.

Precaution

Alterations of the dosage regimen is recommended for patients with impairment of renal function (CrCl <40 ml/min/1.73 m2). Avoid exposure to excessive sunlight or artificial UV light. Phototoxicity reaction may occur if undue exposure occurs. Safety and efficacy of Contra has not been established in children, pregnant and lactating women.

Some isolated cases of phototoxicity have been reported after systemic but not after topical ophthalmic use of Contra. Nevertheless, during treatment with Contra intensive exposure to sunlight or UV-radiation should be avoided

Interaction

Contra does not alter theophylline clearance and concentration. No change of caffeine is reported. Sucralfate and antacid containing magnesium and aluminium interfere with its bioavailability. Enhances effects of warfarin. Probenecid slows renal elimination of Contra.

In order to avoid reduction of efficacy, no ophthalmic preparations containing heavy metals, such as zinc, should be used during 15 minutes preceding and following application of Contra. Bacteriostatic ophthalmic antibiotics should not be used concomitantly with Contra eye drops.

Food Interaction

  • Avoid multivalent ions. Separate the administration polyvalent ions, including magnesium and aluminum-containing antacids, from lomefloxacin by at least 4 hours before and 2 hours after lomefloxacin dosing.
  • Take with or without food. The rate and extent of absorption may be reduced when lomefloxacin is taken with food.

Contra multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Oral preparations that contain magnesium, aluminum, or calcium may significantly decrease the gastrointestinal absorption of quinolone antibiotics.

Absorption may also be reduced by sucralfate, which contains aluminum, as well as other polyvalent cations such as iron and zinc.

The mechanism is chelation of quinolones by polyvalent cations, forming a complex that is poorly absorbed from the gastrointestinal tract.

The bioavailability of ciprofloxacin has been reported to decrease by as much as 90% when administered with antacids containing aluminum or magnesium hydroxide.

When coadministration cannot be avoided, quinolone antibiotics should be dosed either 2 to 4 hours before or 4 to 6 hours after polyvalent cation-containing products to minimize the potential for interaction.

When coadministered with Suprep Bowel Prep (magnesium

Please consult individual product labeling for specific recommendations.

Elimination Route

Rapid and nearly complete with approximately 95% to 98% of a single oral dose being absorbed.

Half Life

8 hours

Clearance

  • 271 mL/min/1.73 m2 [creatinine clearance of 110 mL/min/1.73 m2]
  • 31 mL/min/1.73 m2 [creatinine clearance of 0 mL/min/1.73 m2]

Elimination Route

The urinary excretion of lomefloxacin was virtually complete within 72 hours after cessation of dosing, with approximately 65% of the dose being recovered as parent drug and 9% as its glucuronide metabolite.

Pregnancy & Breastfeeding use

Pregnancy Category C. Reproductive function studies have been performed in rats at doses up to 8 times the recommended human dose based on mg/m² (34 times the recommended human dose based on mg/kg), and no impaired fertility or harm to the fetus was reported due to lomefloxacin. Increased incidence of fetal loss in monkeys has been observed at approximately 3 to 6 times the recommended human dose based on mg/m² (6 to 12 times the recommended human dose based on mg/kg). No teratogenicity has been observed in rats and monkeys at up to 16 times the recommended human dose exposure. In the rabbit, maternal toxicity and associated fetotoxicity, decreased placental weight, and variations of the coccygeal vertebrae occurred at doses 2 times the recommended human exposure based on mg/m². There are, however, no adequate and well-controlled studies in pregnant women. Contra should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing mothers: It is not known whether lomefloxacin is excreted in human milk. However, it is known that other drugs of this class are excreted in human milk and that lomefloxacin is excreted in the milk of lactating rats. Because of the potential for serious adverse reactions from lomefloxacin in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Contra is contraindicated in patients with a history of hypersensitivity to Contra or to other quinolones. Contra like other drugs in its class, cause arthropathy in juvenile animals. Therefore, its use in children, growing adolescents, and pregnant women is not recommended.

Special Warning

Pediatric use: The safety and effectiveness of lomefloxacin in pediatric patients and adolescents less than 18 years of age have not been established. Contra causes arthropathy in juvenile animals of several species.

Geriatric use: Of the total number of subjects in clinical studies of lomefloxacin, 25% were ≥65 years and 9% were ≥ 75 years. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Acute Overdose

Practically there is no risk of adverse effects due to accidental oral ingestion, since a bottle of 5 ml eye drop solution contains only 15 mg Contra. This corresponds to 3.75% of the recommended oral daily dose for adults of 400 mg Contra.

Storage Condition

Should be stored in cool and dry place

Innovators Monograph

You find simplified version here Contra

Contra contains Lomefloxacin see full prescribing information from innovator Contra Monograph, Contra MSDS, Contra FDA label

FAQ

What is Contra used for?

Contra is used to treat certain kinds of bacterial infections.

How safe is Contra?

The results of these trials demonstrate that once-daily administration of 400 mg Contra is as safe and effective clinically as, and superior bacteriologically to, twice-daily administration of 400 mg norfloxacin in the treatment of acute uncomplicated urinary tract infections in adult patients.

How does Contra work?

Contra works by killing bacteria or preventing their growth.

What are the common side effects of Contra?

Common side effects of Contra are include :

  • nausea
  • vomiting
  • diarrhea
  • headache
  • lightheadedness
  • drowsiness
  • ringing in the ears
  • increased sensitivity of the skin to sunlight
  • insomnia
  • indigestion, and
  • abdominal pain

Is Contra safe during pregnancy?

Contra has been assigned to pregnancy category C by the FDA. Some animal studies failed to reveal evidence of fetal harm; however, studies using high doses demonstrated fetotoxicity and teratogenicity. There are no controlled data in human pregnancies.

Is Contra safe during breastfeeding?

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

When should be taken of Contra?

You can take Contra with or without food. Contra is usually taken once a day.

How long does Contra take to work?

Steady state concentrations were achieved within 48 hours of initiating therapy with one  a day dosing.

How long does Contra stay in my system?

The urinary excretion of Contra  was virtually complete within 72 hours after cessation of dosing, with approximately 65% of the dose being recovered as parent drug and 9% as its glucuronide metabolite.

Who should not take Contra?

Contra is not approved for use by children younger than 12 years of age. Contra may interfere with bone development.

What happens if I miss a dose of Contra?

Take the missed dose up to 2 hours late. If more than 2 hours have passed since you missed the dose, skip it and take the next regularly scheduled dose. Do not take a double dose of this medication unless otherwise directed by your doctor.

What happens if I overdose of Contra?

Seek emergency medical attention.The most common symptom of a Contra overdose is seizures.

*** Taking medicines without doctor's advice can cause long-term problems.
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