In clinical trials involving 52 healthy subjects and 1980 patients with urinary tract infections or prostatitis treated with multiple doses of Noroxine, 3.6% reported drug-related adverse experiences. However, the incidence figures below were calculated without reference to drug relationship.
The most common adverse experiences ( > 1.0%) were: nausea (4.2%), headache (2.8%), dizziness (1.7%), and asthenia (1.3%).
Additional reactions (0.3%-1.0%) were: abdominal pain, back pain, constipation, diarrhea, dry mouth, dyspepsia/heartburn, fever, flatulence, hyperhidrosis, loose stools, pruritus, rash, somnolence, and vomiting.
Less frequent reactions (0.1%-0.2%) included: abdominal swelling, allergies, anorexia, anxiety, bitter taste, blurred vision, bursitis, chest pain, chills, depression, dysmenorrhea, edema, erythema, foot or hand swelling, insomnia, mouth ulcer, myocardial infarction, palpitation, pruritus ani, renal colic, sleep disturbances, and urticaria.
Abnormal laboratory values observed in these patients/subjects were: eosinophilia (1.5%), elevation of ALT (SGPT) (1.4%), decreased WBC and/or neutrophil count (1.4%), elevation of AST (SGOT) (1.4%), and increased alkaline phosphatase (1.1%). Those occurring less frequently included increased BUN, increased LDH, increased serum creatinine, decreased hematocrit, and glycosuria.
- Didanosine, antacids, multivitamins, sucralfate, formulations containing iron or zinc, should not be taken within two hours of administration of Noroxine.
- Like other FQs, Noroxine can lead to increase in serum levels of theophylline when prescribed simultaneously.
- Like other FQs, Noroxine may enhance the effects of oral anticoagulants.
- Like other FQs, Noroxine when given with glyburide can rarely lead to severe decrease in the plasma glucose levels.
- Like other FQs, Noroxine inhibits CYP1A2 in vitro. When used with other drugs metabolized by CYP1A2 like ropinirole, clozapine, caffeine, tizanidine, theophylline it may lead to increased substrate drug concentrations when given in normal doses.
- Probenecid inhibits the renal elimination of Noroxine thereby increasing its levels.
- Nitrofurantion may antagonize the antibacterial effect of Noroxine in the urinary tract.
- Simultaneous prescription of Noroxine with NSAIDS can lead to increased probability of convulsions.
How to take Noroxine
- Before you start taking the tablets, read the manufacturer's printed information leaflet from ins >
- Musculoskeletal Disorders
An increased incidence of musculoskeletal disorders i.e. joint pain and inflammation and Tendinopathy has been observed.
- Deterioration of Myasthenia Gravis
Like other FQs, Noroxine can lead to deterioration of weakness of muscles in patients of myasthenia gravis.
- Rarely needle-shaped crystals can occur in the urine of patients taking Noroxine and they are more likely to occur if the recommended dose is exceeded or the patient is not well hydrated leading to inadequate urine output.
Food can delay absorption of Noroxine. Noroxine has a unique property i.e. it penetrates well into tissues of the genitourinary tract. Approximately 30% of a dose is eliminated unchanged in the urine thus producing high urinary concentrations. Urinary excretion is decreased by probenecid.
Noroxine , a poorly absorbed fluoroquinolone, has been used to achieve selective intestinal decontamination in cirrhotic patients; Noroxine has several characteristics that make it suitable for prophylaxis: ▪
Poor absorption when taken orally
Effectiveness against enteric gram-negative organisms
Sparing of gram-positive and anaerobic organisms to maintain their protective role in the normal gut flora
Noroxine reduces the incidence of SBP, delays progression to hepatorenal syndrome, and improves overall survival (see Table 11.8 ).
In patients who have survived an episode of SBP: ▪
Recurrence can be as high as 68% at 1 year without antibiotic prophylaxis.
Noroxine, 400 mg orally daily, has been shown to decrease the probability of recurrent SBP to 20% at 1 year.
Noroxine prophylaxis is cost effective in reducing recurrent SBP.
However, Noroxine treatment does not alter the overall mortality in these patients.
In patients with cirrhosis and gastrointestinal hemorrhage: ▪
The incidence of SBP can be as high as 45% to 66% at 1 year without antibiotic prophylaxis.
Antibiotic prophylaxis started immediately and continued for 7 days decreases the incidence of SBP to 10% to 20%.
Antibiotic prophylaxis may improve survival in these patients.
Intravenous ceftriaxone has been shown to be more effective than oral Noroxine for SBP prophylaxis in patients with advanced cirrhosis and gastrointestinal hemorrhage.
In hospitalized patients with ascitic flu > ▪
The overall probability of new-onset SBP is 20% in 1 year.
Prophylaxis with Noroxine 400 mg orally daily decreases in-hospital incidence of SBP from 22% to 0% without an effect on in-hospital mortality.
Trimethoprim–sulfamethoxazole, one double-strength tablet orally daily, has also been reported to be effective in preventing SBP.
Like other fluoroquinolones, resistance is mainly because of chromosomal mutation (Quinolone-Resistance Determining Regions
Due to the unique mechanism of action of fluoroquinolones plasmid mediated transferable resistance perhaps does not occur. A Qnr protein has been seen that offers protection to the DNA gyrase from damage by the FQs. Also modification of Noroxine can be caused by a different type acetyltransferase which is similar to the one which modifies aminoglycoside.
Cross resistance is seen within the FQs.
Microorganisms like Klebsiella pneumoniae, acinetobacter and pseudomonas aeruginosa have developed the most resistance to Noroxine.
Noroxine is usually active against the microorganisms which are not sensitive to nalidixic acid.
Fluoroquinolones, including NOROXIN, have been associated with an increased risk of peripheral neuropathy. Cases of sensory or sensorimotor axonal polyneuropathy affecting small and/or large axons resulting in paresthesias, hypoesthesias, dysesthesias and weakness have been reported in patients receiving fluoroquinolones, including NOROXIN. Symptoms may occur soon after initiation of Noroxine and may be irreversible in some patients (see WARNINGS). Discontinue NOROXIN immediately if the patient experiences symptoms of peripheral neuropathy including pain, burning, tingling, numbness, and/or weakness, or other alterations in sensations including light touch, pain, temperature, position sense and vibratory sensation, and/or motor strength in order to minimize the development of an irreversible condition. Avoid fluoroquinolones, including NOROXIN, in patients who have previously experienced peripheral neuropathy (see ADVERSE REACTIONS).
C Role of DNA Gyrase in the Quinolone–DNA Interaction
The key experimental ev >Noroxine binding to the enzyme–DNA complexes ( Shen et al., 1989a ). It was found that the binding of the drug to relaxed forms of DNA may be induced by the addition of DNA gyrase, and that the amount of the binding to the enzyme–DNA complex is far more than the sum of the separated bindings to the DNA and to the enzyme. The increased drug binding was not due to the conversion of the substrate DNA to the supercoiled form, since nonhydrolyzable triphosphate nucleotide was used in the binding mixture. As shown in Fig. 5 , the induced binding to the gyrase–DNA complex showed a saturable phase that highly resembles the binding pattern to the supercoiled DNA in terms of the amount of binding and the binding cooperativity ( Shen et al., 1989b ). When linear DNA was used, the specific type of binding may be obtained without requiring a nucleotide energy source. It is conceivable that the open DNA ends do not restrict the DNA conformational change or DNA unwinding that is necessary for the creation of the drug binding site during the enzyme-wrapping and gate-opening steps following the DNA cleavage. ATP was known to strikingly enhance DNA cleavage and change the gyrase cleavage sites on DNA ( Morrison et al., 1980 ); thus, the ATP-dependent binding phenomenon may be site specific. Above results suggested that the binding of DNA gyrase to the DNA substrate creates a specific site that allows the drug to bind in a cooperative manner.
NOROXIN® (Noroxine) Tablets
SERIOUS ADVERSE REACTIONS INCLUDING TENDINITIS, TENDON RUPTURE, PERIPHERAL NEUROPATHY, CENTRAL NERVOUS SYSTEM EFFECTS AND EXACERBATION OF MYASTHENIA GRAVIS
- Fluoroquinolones, including NOROXIN, have been associated with disabling and potentially irreversible serious adverse reactions that have occurred together, including:
- Tendinitis and tendon rupture
- Peripheral neuropathy
- Central nervous system effects (see WARNINGS).Discontinue NOROXIN immediately and avoid the use of fluoroquinolones, including NOROXIN, in patients who experience any of these serious adverse reactions.
- Fluoroquinolones, including NOROXIN, may exacerbate muscle weakness in patients with myasthenia gravis. Avoid NOROXIN in patients with known history of myasthenia gravis (see WARNINGS).
- Because fluoroquinolones, including NOROXIN, have been associated with serious adverse reactions (see WARNINGS), reserve NOROXIN for use in patients who have no alternative treatment options for uncomplicated urinary tract infections (including cystitis) (see INDICATIONS AND USAGE).
To reduce the development of drug-resistant bacteria and maintain the effectiveness of NOROXIN® and other antibacterial drugs, NOROXIN should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
You may be taking certain other medicines that should not be taken at the same time as Noroxine. Avoid taking the following medicines within 2 hours before or after you take Noroxine. These other medicines can make Noroxine much less effective when taken at the same time:
- antacids that contain magnesium or aluminum (such as Maalox, Mylanta, or Rolaids), or the ulcer medicine sucralfate (Carafate);
- didanosine (Videx) powder or chewable tablets;
- vitamin or mineral supplements that contain iron or zinc.
Do not take Noroxine with dairy products such as milk or yogurt. They could make the medication less effective.
Avoid caffeine while you are taking Noroxine, because the medication can make the effects of caffeine stronger.
Avoid exposure to sunlight or tanning beds. Noroxine can make you sunburn more easily. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors. Call your doctor if you have severe burning, redness, itching, rash, or swelling after being in the sun.
Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or bloody, stop taking Noroxine and call your doctor. Do not use anti-diarrhea medicine unless your doctor tells you to.
Noroxine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Noroxine, especially:
- cisapride, cyclosporine, erythromycin, nitrofurantoin, probenecid, ropinirole, tacrine, theophylline, tizanidine;
- a diuretic or "water pill";
- heart rhythm medication--amiodarone, disopyramide, dofetilide, dronedarone, procainamide, quinidine, sotalol, and others;
- medicine to treat depression or mental illness--amitriptylline, clomipramine, clozapine, desipramine, duloxetine, iloperidone, imipramine, nortriptyline, thioridazine, ziprasidone, and others; or
- NSAIDs (nonsteroidal anti-inflammatory drugs)--aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve), celecoxib, diclofenac, indomethacin, meloxicam, and others.
This list is not complete. Other drugs may interact with Noroxine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.
Generic Name: Noroxine (nor FLOKS a sin)
Medically reviewed by Drugs.com. Last updated on Jun 14, 2019.
Mechanism of action
Noroxine has a bactericidal action and it causes inhibition of bacterial DNA synthesis. Exactly Noroxine inhibits the DNA gyrase enzyme present in the bacteria which leads to hindrance in the normal supercoil formation of the DNA. It also inhibits the process of relaxation of the DNA which has undergone supercoiling and leads to increased damage to the DNA.
The cells of mammals have the enzyme topoisomerase II instead of DNA gyrase or topoisomerase IV which possesses very little affinity for Noroxine resulting in minimal damage to the host tissue.