Araxacina

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

Araxacina is a synthetic 4-quinolone derivative with bactericidal activity against a wide range of gram-positive and gram-negative organism. It is active against most gram-negative aerobic bacteria including Enterobacteriaceae and Pseudomonas aeruginosa. Araxacina is also active against gram-positive aerobic bacteria including penicillinase producing, non-penicillinase producing and methicillin resistant Staphylococci. However many strains of Streptococci are relatively resistant to the drug. The bactericidal activity of Araxacina results from interference with the enzyme DNA gyrase needed for the synthesis of bacterial DNA. The mode of action of Araxacina is different from other antibiotics like penicillins, cephalosporins, aminoglycosides, tetracyclines and for this reason it is observed that organisms resistant to these antibiotics are susceptible to Araxacina. Araxacina is well absorbed from the GIT after oral administration and it is widely distributed into the body tissues and fluid. The half-life of Araxacina is 3.5 - 4.5 hours. About 30-50% of an oral dose of Araxacina is excreted in the urine within 24 hours as unchanged drug and active metabolites.

Araxacina (Eye/Ear) drops (Araxacina Hydrochloride ophthalmic solution) is a synthetic, sterile, multiple dose, antimicrobial for topical use. Araxacina 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 C17H18FN3O3.HCl.H2O.

Araxacina is a second generation fluoroquinolone that is active against many Gram negative and Gram positive bacteria. It produces its action through inhibition of bacterial DNA gyrase and topoisomerase IV. Araxacina binds to bacterial DNA gyrase with 100 times the affinity of mammalian DNA gyrase. There is no cross resistance between fluoroquinolones and other classes of antibiotics, so it may be of clinical value when other antibiotics are no longer effective. Ciprofloxain and its derivatives are also being investigated for its action against malaria, cancers, and AIDS.

Trade Name Araxacina
Availability Prescription only
Generic Ciprofloxacin
Ciprofloxacin Other Names Ciprofloxacin, Ciprofloxacine, Ciprofloxacino, Ciprofloxacinum
Related Drugs amoxicillin, prednisone, albuterol, doxycycline, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin
Type
Formula C17H18FN3O3
Weight Average: 331.3415
Monoisotopic: 331.133219662
Protein binding

20-40%.

Groups Approved, Investigational
Therapeutic Class 4-Quinolone preparations, Anti-diarrhoeal Antimicrobial drugs
Manufacturer
Available Country Spain
Last Updated: September 19, 2023 at 7:00 am
Araxacina
Araxacina

Uses

Araxacina is used for the treatment of the following infections caused by sensitive bacteria:

Severe systemic infections: e.g; septicemia, bacteremia, peritonitis, infections in immunosuppressed patients with haematological or solid tumors and in patients in intensive care unit with specific problems such as infected burns.

Respiratory tract infections: Lobar and broncho pneumonia, acute and chronic bronchitis and empyema.

Urinary tract infections: Uncomplicated and complicated urethritis, cystitis, pyelonephritis, prostatitis and epididymitis.

Skin and soft tissue infections: Infected ulcers, wound infections, abscesses, cellulitis, otitis externa, erysipelas and infected burns.

Gastrointestinal infections: Enteric fever, infective diarrhea.

Infections of the biliary tract: Cholangitis, cholecystitis, empyema of the gall bladder.

Intra-abdominal infections: Peritonitis, intra abdominal abscesses.

Bone and joint infections: Osteomyelitis, septic arthritis.

Pelvic infections: Salpingitis, endometritis, pelvic inflammatory diseases.

Eye, ear, nose and throat infections: Otitis media, sinusitis, mastoiditis, tonsillitis.

Gonorrhoea: Urethral, rectal and pharyngeal gonorrhoea caused by beta-lactamase producing organism or organisms moderately sensitive to penicillin.

Araxacina (Eye/Ear) Solution is used for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below:

Eye

Corneal Ulcers:

• Pseudomonas aeruginosa

• Serratia marcescens

• Staphylococcus aureus

• Staphylococcus epidermidis

• Streptococcus pneumonia

• Streptococcus (Viridans Group)

Conjunctivitis:

• Haemophilus influenza

• Staphylococcus aureus

• Staphylococcus epidermidis

• Streptococcus pneumoniae

Ear

Otitis externa, acute otitis media, cronic suppurative otitis media. Prophylaxis in otic surgeries such as mastoid surgery.

Araxacina is also used to associated treatment for these conditions: Acute Otitis Externa, Acute Otitis Externa caused by Pseudomonas Aeruginosa, Acute Otitis Media, Acute Sinusitis, Acute Uncomplicated Pyelonephritis, Acute exacerbation of chronic bronchitis caused by Moraxella catarrhalis, Bone and Joint Infections, Chronic Otitis Media, Complicated Intra-Abdominal Infections, Complicated Urinary Tract Infection, Conjunctivitis caused by Haemophilus influenzae, Conjunctivitis caused by Staphylococcus epidermidis, Corneal Ulcers caused by Serratia marcescens, Corneal Ulcers caused by Staphylococcus aureus, Corneal Ulcers caused by Staphylococcus epidermidis, Corneal Ulcers caused by Streptococcus Pneumoniae, Corneal Ulcers caused by Streptococcus Viridans Group, Corneal Ulcers caused by pseudomonas aeruginosa, Escherichia urinary tract infection, External ear infection NOS, Febrile Neutropenia, Infection of the outer ear caused by susceptible bacteria, Infectious diarrhea, Lower respiratory tract infection caused by Enterobacter cloacae, Lower respiratory tract infection caused by Escherichia coli, Lower respiratory tract infection caused by Haemophilus influenzae, Lower respiratory tract infection caused by Haemophilus parainfluenzae, Lower respiratory tract infection caused by Klebsiella pneumoniae, Lower respiratory tract infection caused by Proteus mirabilis, Lower respiratory tract infection caused by penicillin-susceptible Streptococcus pneumoniae, Nosocomial Pneumonia, Otitis Media (OM), Otitis Media, Purulent, Plague caused by Yersinia pestis, Skin Infections, Typhoid fever caused by Salmonella typhi, UTI caused by Citrobacter diversus, UTI caused by Citrobacter frendii, UTI caused by Entercococcus faecalis, UTI caused by Enterobacter cloacae, UTI caused by Klebsiella pneumoniae, UTI caused by Morganella morganii, UTI caused by Proteus mirabilis, UTI caused by Providencia rettgeri, UTI caused by Pseudomonas aeruginosa, UTI caused by Serratia marcescens, UTI caused by methicillin-susceptible Staphylococcus epidermidis, Uncomplicated Urinary Tract Infections, Acute otitis externa caused by Staphylococcus aureus, Acute, uncomplicated Cystitis caused by Escherichia coli, Acute, uncomplicated Cystitis caused by Staphylococcus saprophyticus, Chronic Prostatitis caused by Escherichia coli, Chronic Prostatitis caused by Proteus mirabilis, Complicated Pyelonephritis caused by Escherichia coli, Complicated Urinary Tract Infection caused by Escherichia Coli, Inhaled anthrax caused by Bacillus anthracis, Uncomplicated Gonorrhea caused by Neisseria gonorrhoeae

How Araxacina works

Araxacina acts on bacterial topoisomerase II (DNA gyrase) and topoisomerase IV. Araxacina's targeting of the alpha subunits of DNA gyrase prevents it from supercoiling the bacterial DNA which prevents DNA replication.

Dosage

Araxacina dosage

Adult Dose:

For oral dosage &suspension:

Urinary Tract infection: Acute uncomplicated: 250 mg twice daily for 3 days; Mild/Moderate: 250 mg twice daily for 7 to 14 days; Severe/Complicated: 500 mg twice daily for 7 to 14 days; Chronic Bacterial Prostitis : 500 mg twice daily for 28 days; Lower Respiratory Tract infection: Mild/Moderate: 500 mg twice daily for 7 to 14 days, Severe/Complicated : 750 mg twice daily for 7 to 14 days; Acute Sinusitis : 500 mg twice daily for 10 days; Skin and Skin Structure infection: Mild/Moderate : 500 mg twice daily for 7 to 14 days, Severe/Complicated : 750 mg twice daily for 7 to 14 days, Bone and joint infection: Mild/Moderate 500 mg twice daily for 4 to 6 weeks, Severe/Complicated : 750 mg twice daily for 4 to 6 weeks, Intra Abdominal Infection: 500 mg twice daily for 7 to 14 days, Infectious Diarrhea: Mild/Moderate/Severe: 500 mg twice daily for 5 to 7 days, Typhoid Fever : 500 mg twice daily for 10 days, Urethral & Cervical Gonococcal Infections: Uncomplicated: 250 mg Single dose.

For IV infusion :

Urinary Tract Infection: Mild to Moderate: 200 mg 12 hourly for 7-14 days;Severe or Complicated: 400 mg 12 hourly for 7-14 days; Lower Respiratory Tract infection: Mild to Moderate: 400 mg 12 hourly for 7-14 days; Severe or Complicated: 400 mg 8 hourly for 7-14 days; Nosocomial Pneumonia: Mild/Moderate/Severe: 400 mg 8 hourly for 10-14 days; Skin and Skin Structure: Mild to Moderate: 400 mg 12 hourly for 7-14 days; Severe or Complicated: 400 mg 8 hourly for 7-14 days; Bone and Joint Infection: Mild to Moderate: 400 mg 12 hourly for more than 4-6 weeks; Severe/Comlicated: 400 mg 8 hourly for more than 4-6weeks; Intra abdominal (Acute abdomen): Complicated: 400 mg 12 hourly for 7-14 days; Acute Sinusitis: Mild/Moderate: 400 mg 12 hourly for10 days: Chronic Bacterial Prostatitis: Mild/Moderate: 400 mg 12 hourly for 28 Days.

Children and adolescents:

RTI & GI infections: Neonate-15mg/kg twice daily, Child (1 month -18 years)-20mg/kg (max 750 mg) twice daily; UTI: Neonate-10 mg/kg twice daily, Child (1 month -18 years)-10mg/kg (max 750 mg) twice daily; Pseudomonal lower respiratory tract infection in cystic fibrosis: Child (1 month -18 years) - 20mg/kg (max 750 mg) twice daily; Anthrax (treatment & post exposure prophylaxis): Child (1 month -18 years) - 20mg/kg (max 750 mg) twice daily.

Use in Pregnancy and Lactation

Reproduction studies performed in rats and rabbits using parenteral and oral administration did not reveal any evidence of teratogenicity, impairment of fertility or impairment of pre or postnatal development. However, as with other quinolones, Araxacina has been shown to cause arthropathy in immature animals and therefore, its use during pregnancy is not recommended. Studies in rats have indicated that Araxacina is secreted in milk, administration to nursing mothers is thus not recommended.

Eye

Corneal Ulcers: The recommended dosage regimen for the treatment of corneal ulcers is 2 drops into the affected eye every 15 minutes for the first 6 hours and then 2 drops into the affected eye every 30 minutes for the remainder of the first day. On the second day, instill 2 drops in the affected eye hourly. On the third through the fourteenth day, place 2 drops in the affected eye every four hours. Treatment may be continued after 14 days if corneal re-epithelialization has not occurred.

Conjunctivitis: The recommended dosage regimen for the treatment of bacterial conjunctivitis is 1 or 2 drops instilled into the conjunctival sac(s) every 2 hours while awake for 2 days and one or 2 drops every 4 hours while awake for the next 5 days.

Ear

For all infections, 2-3 drops every 2-3 hours initially, reducing the frequency of the instillation with control of infection. Treatment should be continued at least 7 days.

Information for patients: Should be swallowed whole with an adequate amount of liquid, it may be taken with or without meals. The preferred time of dosing is two hours after a meal and patients should not take antacid within two hours of dosing.

Directions for use of granules for suspension

Whole contents of the packet should be taken into a small glass containing 2-3 teaspoonful of water. Other liquids or foods should not be used. The mixer should be stirred well and drink immediately. The glass should be refilled with water and drink.

Direction for reconstitution of suspension (60 ml)

Shake the bottle well to loosen the granules. Add 50 ml (with the help of supplied measuring cup) of boiled cool water to the dry granules in the bottle. Shake the bottle vigorously until all the granules is in suspension.

Side Effects

Araxacina is generally well tolerated. Frequent adverse reactions are- Gastrointestinal disturbance: e.g. nausea diarrhea, vomiting, dyspepsia, abdominal pain. Disturbance of the CNS: e.g. dizziness, headache, tiredness, confusion, convulsions. Hypersensitivity reactions: e.g. skin rashes, pruritus, and possible systemic reactions. Other possible side effects are - joint pain, light sensitivity, transient increase in liver enzyme (especially in patients with history of liver damage), serum bilirubin, urea or serum creatinine. Arthralgia and myalgia may also occur.

The most frequently reported drug related adverse reaction is local burning or discomfort. In corneal ulcer studies with frequent administration of the drug, white crystalline precipitates were seen in approximately 17% of patients. Other reactions occurring in less than 10% of patients included lid margin crusting, crystals/scales, foreign body sensation, itching, conjunctival hyperemia and a bad taste following instillation. Additional events occurring in less than 1% of patients included corneal staining, keratopathy/keratitis, allergic reactions, lid edema, tearing, photophobia, corneal infiltrates, nausea and decreased vision.

Toxicity

Patients experiencing an overdose may present with nausea, vomiting, abdominal pain, crystalluria, nephrotoxicity, and oliguria. Araxacina overdose typically leads to acute renal failure. An overdose may progress over the next 6 days with rising serum creatinine and BUN, as well as anuria. Patients may require prednisone therapy, urgent hemodialysis, or supportive therapy. Depending on the degree of overdose, patients may recover normal kidney function or progress to chronic kidney failure.

The oral LD50 in rats is >2000mg/kg.

Araxacina for intratympanic injection or otic use has low systemic absorption and so it unlikely to be a risk in pregnancy or lactation. There is generally no harm to the fetus in animal studies, however high doses may lead to gastrointestinal disturbances in the mother which may increase the incidence of abortion. In human studies there was no increase in fetal malformations above background rates. The risk and benefit of ciprofloxacin should be weighed in pregnancy and breast feeding.

2/8 in vitro tests and 0/3 in vivo tests of mutagenicity of ciprofloxacin have yielded a positive result.

Oral doses of 200 and 300 times the maximum recommended clinical dose in rats and mice have shown no carcinogenicity or tumorigenicity.

Oral doses above the maximum recommended clinical dose have shown no effects on fertility in rats.

Precaution

Araxacina should be used with caution in patients with a history of convulsive disorders. Crystalluria related to the use of Araxacina has been observed only rarely. Patients receiving Araxacina should be well hydrated to avoid excessive alkalinity of the urine.

Beuflox Injection should only be administered by slow intravenous infusion over a period of 60 minutes. Local IV site reactions have been reported with the intravenous administration of Araxacina. These reactions are more frequent if infusion time is 30 minutes or less or if small vein of the hand are used.

Interaction

Increased plasma levels of theophylline have been observed following concurrent administration with Araxacina. Araxacina suspension should not be administered within 4 hours of medications containing magnesium, aluminium, calcium or iron salts as interference with absorption may occur.

Food Interaction

  • Avoid milk and dairy products. Dairy products and calcium fortified juices decrease the absorption of ciprofloxacin.
  • Limit caffeine intake.
  • Take with or without food. The absorption is not significantly affected by food.

[Moderate] ADJUST DOSING INTERVAL: Concurrent ingestion of dairy products (milk, yogurt) or calcium-fortified foods (i.e., cereal, orange juice) may decrease the activity of certain oral fluoroquinolone antibiotics.

The mechanism is chelation of calcium and the quinolone, resulting in decreased bioavailability.

In the case of orange juice, inhibition of intestinal transport mechanisms (P-glycoprotein or organic anion-transporting polypeptides) by flavones may also be involved.

One study reported an average 41% decrease in maximum plasma concentrations and a 38% decrease in AUC when ciprofloxacin was given with calcium-fortified orange juice instead of water.

Administration of ciprofloxacin tablets with enteral nutrition may reduce its bioavailability and maximum serum concentrations.

Data have been conflicting and variable by the type of enteral nutrition product, location of the feeding tube, and patient characteristics.

Decreased absorption is expected if ciprofloxacin is given by jejunostomy tube.



MANAGEMENT: Oral ciprofloxacin should not be taken with dairy products or calcium-fortified foods alone, but may be taken with meals that contain these products.

When taken alone, dairy products or calcium-fortified foods should be ingested at least 2 hours before or after ciprofloxacin administration.

When ciprofloxacin tablets are administered to patients receiving continuous enteral nutrition, some experts recommend that the tube feeding should be interrupted for at least 1 hour before and 2 hours after the dose of ciprofloxacin is given.

Patients should be monitored for altered antimicrobial efficacy and switched to intravenous ciprofloxacin if necessary.

If no enteral route besides a jejunostomy tube is available, it is also recommended to switch to intravenous ciprofloxacin.

According to the manufacturer, ciprofloxacin oral suspension should not be administered via nasogastric or feeding tubes due to its physical characteristics.

Araxacina 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.

Volume of Distribution

Cirpofloxacin follws a 3 compartment distribution model with a central compartment volume of 0.161L/kg and a total volume of distribution of 2.00-3.04L/kg.

Elimination Route

A 250mg oral dose of ciprofloxacin reaches an average maximum concentration of 0.94mg/L in 0.81 hours with an average area under the curve of 1.013L/h*kg. The FDA reports an oral bioavailability of 70-80% while other studies report it to be approximately 60%. An early review of ciprofloxacin reported an oral bioavailability of 64-85% but recommends 70% for all practical uses.

Half Life

The average half life following a 250mg oral dose was 4.71 hours and 3.65 hours following a 100mg intravenous dose. Generally the half life is reported as 4 hours.

Clearance

The average renal clearance after a 250mg oral dose is 5.08mL/min*kg. Following a 100mg intravenous dose, the average total clearance is 9.62mL/min*kg, average renal clearance is 4.42mL/min*kg, and average non renal clearance is 5.21mL/min*kg.

Elimination Route

27% of an oral dose was recovered unmetabolized in urine compared to 46% of an intravenous dose. Collection of radiolabelled ciprofloxacin resulted in 45% recovery in urine and 62% recovery in feces.

Pregnancy & Breastfeeding use

Reproduction studies performed in rats and rabbits using parenteral and oral administration did not reveal any evidence of teratogenicity, impairment of fertility or impairment of pre or postnatal development. However, as with other quinolones, Araxacina has been shown to cause arthropathy in immature animals and therefore, its use during pregnancy is not recommended. Studies in rats have indicated that Araxacina is secreted in milk, administration to nursing mothers is thus not recommended.

Contraindication

Araxacina is contra-indicated in patients who have shown hypersensitivity to Araxacina or other quinolones.

Acute Overdose

In case of acute overdose, the patient should be carefully observed and given supporative treatment, including monitoring of renal function. Adequate hydration must be maintained.

Interaction with other Medicine

Concurrent administration of Araxacina with theophylline may lead to elevated plasma concentrations of theophylline. Plasma level of theophylline should be monitored and dosage adjustments made as appropriate. Antacid containing magnesium hydroxide or aluminium hydroxide may interfere with the absorption of Araxacina & concurrent administration of these agents with Araxacina should be avoided. Probenecid interferes with renal tubular secretion of Araxacina and produces an increase in the level of Araxacina in the serum. As with other broad spectrum antibiotics prolonged use of Araxacina may result in over growth of non-susceptible organisms. Repeated evaluation of patient's conditions and microbial susceptibility testing is essential. If superinfections occur during therapy, appropriate measure should be taken.

Storage Condition

Store in a cool dry place protected from light. Keep out of reach of children.

Innovators Monograph

You find simplified version here Araxacina

Araxacina contains Ciprofloxacin see full prescribing information from innovator Araxacina Monograph, Araxacina MSDS, Araxacina FDA label

FAQ

What is Araxacina used for?

Araxacina is used to treat serious infections, or infections when other anitbiotics have not worked.Araxacina is used to treat bacterial infections, such as chest infections.

How safe is Araxacina?

Araxacina is a safe treatment for a urinary tract infection.

How does Araxacina work?

Araxacina works by stopping the growth of bacteria. This antibiotic treats only bacterial infections.

What are the common side effects of Araxacina?

Common side effects of Araxacina are include:

  • nausea
  • vomiting
  • stomach pain
  • heartburn
  • diarrhea
  • vaginal itching and/or discharge
  • pale skin
  • unusual tiredness
  • sleepiness

Is Araxacina safe during pregnancy?

Araxacina should not be used during pregnancy unless the benefit outweighs the risk to both fetus and mother.According to some authorities. As a precaution, avoiding use during pregnancy is preferred.

Is Araxacina safe during breastfeeding?

Use of Araxacina is acceptable in nursing mothers with monitoring of the infant for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis.

Can I drink alcohol with Araxacina?

Yes, you can drink alcohol with Araxacina.

Can I drink alcohol with Araxacina?

Do not drive or operate machinery if Araxacina makes you feel dizzy or tired. Avoid drinking alcohol.

How do I take Araxacina?

 Take this Araxacina by mouth with or without food as directed by your doctor.

When should be taken of Araxacina?

Araxacina usually taken twice a day in the morning and evening.

When should Araxacina start working?

You should begin to notice some easing of your symptoms a few days after you start taking Araxacina. However, it may be a week or more before you get the full benefit of this drug.

Is Araxacina best taken before or after meals?

You can take Araxacina before or after meals.

Should Araxacina be taken on an empty stomach?

Araxacina is best taken on an empty stomach, swallowed whole with a glass of water.

How long does it take for Araxacina to work?

You should feel better within a few days, but this depends on the type of infection. Tell your doctor if you do not start feeling better after taking or using Araxacina for 2 to 3 days, or if you feel worse at any time.

How long does Araxacina stay in my system?

Araxacina should be out of your system around 22 hours after your last dose. The serum elimination half-life of Araxacina with normal kidney function is approximately 4 hours.

Can I take Araxacina for a long time?

Araxacina side effects occur soon after the medication is taken. However, taking Araxacina long-term may increase the risk of experiencing severe side effects.

Is Araxacina hard on my body?

Araxacina can cause serious side effects, including tendon problems, damage to your nerves, serious mood or behavior changes or low blood sugar.

Is Araxacina safe for kidneys?

Araxacina is relatively safe regarding its nephrotoxicity, while caution is required in vulnerable patients.

Can Araxacina cause kidney stones?

Side effects of certain antibiotics, including widely used drugs like Araxacina, may increase the risk of developing kidney stones, according to the findings of new research.

What happens if I miss a dose of Araxacina?

Simply take the dose you missed as soon as you remember. However, if it's almost time to take your next dose of Araxacina, skip the missed dose and just take your normal amount of medicine.

What happens if I overdose on Araxacina?

If you take too much Araxacina, call your healthcare provider or get medical help immediately.

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