Exacinop exerts antibacterial action by inhibiting bacterial topoisomerase IV and DNA gyrase, the enzymes required for DNA replication, transcription repair and recombination. It has in vitro activity against a wide range of gm-ve and gm+ve microorganisms.
Exacinop is bactericidal and exerts its antimicrobial effects via inhibition of bacterial DNA replication. It has a relatively long duration of action in comparison with other antibiotics that allows for once or twice daily dosing. Exacinop is associated with QTc-interval prolongation and should be used with caution in patients with other risk factors for prolongation (e.g. hypokalemia, concomitant medications).
Exacinop has demonstrated in vitro activity against a number of aerobic gram-positive and gram-negative bacteria and may carry some activity against certain species of anaerobic bacteria and other pathogens such as Chlamydia and Legionella. Resistance to levofloxacin may develop, and is generally due to mutations in DNA gyrase or topoisomerase IV, or via alterations to drug efflux. Cross-resistance may occur between levofloxacin and other fluoroquinolones, but is unlikely to develop between levofloxacin and other antibiotic classes (e.g. macrolides) due to significant differences in chemical structure and mechanism of action.
As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.
Exacinop Tablet is used for Acute maxillary sinusitis , Acute bacterial exacerbation of chronic bronchitis , Nosocomial pneumonia Community acquired pneumonia, Uncomplicated urinary tract infections Complicated urinary tract infections, Acute pyelonephritis, Uncomplicated & complicated skin and skin structure infections, Chronic bacterial prostatitis
Exacinop Injection is used to treat Acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, nosocomial pneumonia, community acquired pneumonia, uncomplicated urinary tract infections, complicated urinary tract infections, acute pyelonephritis, uncomplicated & complicated skin and skin structure infections including abscesses, cellulitis, furuncles, impetigo, pyoderma, wound infections, chronic bacterial prostatitis and typhoid fever.
Exacinop Injection has
- Proven clinical success in hospital infections
- Reaches high concentrations in lung, urine, skin and prostate
- Ensures excellent gram-positive and gram-negative bacterial coverage, Offers better option for switch therapy
Exacinop Eye drops is used for the treatment of corneal ulcer caused by susceptible strains of the following bacteria:
- Gram-positive Bacteria: Corynebacterium species, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Viridans group streptococci
- Gram-negative Bacteria: Pseudomonas aeruginosa, Serratia marcescens.
Exacinop is also used to associated treatment for these conditions: Abscesses caused by susceptible bacteria, Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB) caused by susceptible bacteria, Acute Pyelonephritis caused by Infection Due to Escherichia Coli, Bacterial Conjunctivitis caused by susceptible bacteria, Cellulitis caused by susceptible bacteria, Community Acquired Pneumonia (CAP) caused by susceptible bacteria, Furuncle caused by susceptible bacteria, Impetigo caused by susceptible bacteria, Nosocomial Pneumonia caused by Pseudomonas Infections, Nosocomial Pneumonia caused by susceptible bacteria, Plague caused by Yersinia pestis, Pyoderma caused by susceptible bacteria, Wound Infections caused by susceptible bacteria, Acute bacterial sinusitis caused by susceptible bacteria, Chronic Bacterial prostatitis caused by susceptible bacteria, Chronic Pseudomonas Infections, Complicated Urinary Tract Infection caused by susceptible bacteria, Complicated skin and skin-structure infections caused by susceptible bacteria, Inhaled anthrax caused by Bacillus anthracis, Uncomplicated Urinary Tract Infection caused by susceptible bacteria, Uncomplicated skin and skin-structure infections caused by susceptible bacteria
How Exacinop works
Exacinop, like other fluoroquinolone antibiotics, exerts its antimicrobial activity via the inhibition of two key bacterial enzymes: DNA gyrase and topoisomerase IV. Both targets are type II topoisomerases, but have unique functions within the bacterial cell. DNA gyrase is an enzyme found only in bacteria that introduces negative supercoils into DNA during replication - this helps to relieve torsional strain caused by the introduction of positive supercoils during replication, and these negative supercoils are essential for chromosome condensation and the promotion of transcription initiation. It is comprised of four subunits (two A subunits and two B subunits) of which the A subunits appear to be the target of fluoroquinolone antibiotics. Bacterial topoisomerase IV, in addition to contributing to the relaxation of positive supercoils, is essential at the terminal stages of DNA replication and functions to “unlink” newly replicated chromosomes to allow for the completion of cell division.
Inhibition of these enzymes by levofloxacin likely occurs via complexation with the topoisomerase enzymes. The end result is a blockade of DNA replication, thus inhibiting cell division and resulting in cell death.
|Levofloxacin Other Names||(S)-Ofloxacin, L-Ofloxacin, Levofloxacin, Levofloxacine, Levofloxacino, Levofloxacinum|
|Related Drugs||amoxicillin, prednisone, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, Augmentin|
Levofloxacin is 24-38% protein-bound in plasma, primarily to albumin. The extent of protein-binding is independent of its plasma concentration.
|Therapeutic Class||4-Quinolone preparations|
|Last Updated:||June 7, 2022 at 8:59 pm|
Acute sinusitis: 500 mg once daily for 10-14 days or 750 mg once daily for 5 days
Exacerbation of chronic bronchitis: 500 mg once daily for 7 days
Community acquired pneumonia: 500 mg once daily for 7-14 days or 750 mg once daily for 5 days
Nosocomial pneumonia: 750 mg once daily for 7-14 days
Uncomplicated urinary tract infections: 250 mg once daily for 3 days
Complicated urinary tract infections and acute pyelonephritis: 250 mg once daily for 10 days
Complicated urinary tract infections and acute pyelonephritis: 750 mg once daily for 5 days
Uncomplicated skin and skin structure infections: 500 mg once daily for 7-10 daysComplicated skin and skin structure infections: 750 mg once daily for 7-14 days
Chronic bacterial prostatitis: 500 mg once daily for 28 days
Exacinop solution for infusion is administered by slow intravenous infusion once or twice daily. The dosage depends on the type and severity of the infection and the sensitivity of the causative pathogen. The duration of treatment varies according to the severity of the disease. Adult:
- Community-acquired pneumonia: 500 mg once or twice daily,
- Complicated urinary tract infections (including pyelonephritis): 250 mg once daily,
- Chronic bacterial prostatitis: 500 mg once daily,
- Skin and soft tissue infections: 500 mg twice daily
- Enteric fever: 500 mg once daily.
Exacinop can be used in children aged as low as 6 months. The usual dose for children in community acquired pneumonia is:
- Children aged 6 months to less than 5 years: 10 mg/kg b.i.d. (up to 500 mg per day) for 10 days,
- Children aged 5 years to 16 years: 10 mg/kg q.d. (up to 500 mg per day) for 10 days.
The usual dose for children in recurrent or persistent Acute Otitis Media is:
- Children aged 6 months to less than 5 years: 10 mg/kg per day (maximum dose: 500 mg/day) given twice daily for 10 days.
Paediatric Use: Exacinop is not recommended for children less than 6 (six) months of age.
Exacinop ophthalmic solution:
- Days 1 through 3: Instill one to two drops in the affected eye(s) every 30 minutes to 2 hours while awake and approximately 4 and 6 hours after retiring.
- Day 4 through treatment completion: Instill one to two drops in the affected eye(s) every 1 to 4 hours while awake.
0.5% ophthalmic solution:
- Days 1 and 2: Instill one to two drops in the affected eye(s) every 2 hours while awake, up to 8 times per day.
- Days 3 through 7: Instill one to two drops in the affected eye(s) every 4 hours while awake, up to 4 times per day.
Administration of Exacinop (solution for infusion) should be continued for a minimum of 48 to 72 hours after the patient has become febrile or evidence of bacterial eradication has been obtained. Exacinop solution for infusion is only intended for slow intravenous infusion; it is administered once or twice daily. The infusion time must be at least 30 minutes for 250 mg or 60 minutes for 500 mg Exacinop solution for infusion. It is possible to switch from an initial intravenous application to the oral route at the same dosage after a few days.
The most frequently reported adverse events were headache and a taste disturbance following instillation. Other adverse events included decreased/blurred vision, diarrhea, dyspepsia, fever, infection, instillation site irritation/discomfort, ocular infection, nausea, ocular pain/discomfort, and throat irritation.
The LD50 following oral administration in mice and rats is 1803 mg/kg and 1478 mg/kg, respectively.
Exacinop exhibits low potential for acute toxicity - following a single high dose of levofloxacin in several different test animals (e.g. mice, rats, monkeys) observed symptoms included ataxia, ptosis, decreased motor activity, dyspnea, tremors, and convulsions. Treatment of acute overdosage should involve stomach emptying (e.g. with activated charcoal) and general supportive measures. Consider monitoring of the patient's ECG to ensure QTc values remain within range. Exacinop is not efficiently removed by dialysis (peritoneal or hemodialysis) and is therefore of little benefit in cases of overdose.
The following measures should be taken during administration of Exacinop: While taking Exacinop adequate amount of water should be drunk to avoid risk of crystalluria. Dose adjustment should be exercised during Exacinop ingestion in presence of renal insufficiency & hepatic insufficiency.
While taking Exacinop adequate amount of water should be drunk to avoid risk of crystalluria. Dose adjustment should be exercised during Exacinop ingestion in presence of renal insufficiency & hepatic insufficiency.
Infusion of fluid should be immediately discontinued if rigor arises for any reason during the process. Do not use if the solution is cloudy, contains particles or after expiry date.
If an allergic reaction to levofloxacin occurs, discontinue the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.
Prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, discontinue use and institute alternative therapy. Patients should be advised not to wear contact lenses if they have signs and symptoms of corneal ulcer. Avoid contaminating the applicator tip with material from the eye, fingers or other source.
Specific drug interaction studies have not been conducted with this drug. However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, and enhance the effects of the oral anticoagulant warfarin and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving systemic cyclosporine concomitantly.
- Take with or without food. Food slightly alters kinetics but not to any clinically significant extent.
[Moderate] ADJUST DOSING INTERVAL: Food may reduce the oral absorption and bioavailability of levofloxacin.
According to the drug product labeling, administration of levofloxacin 500 mg with food prolonged the time to peak concentration by 1 hour and decreased the Cmax decreased by 25% following administration of the oral solution and by 14% following administration of the oral tablet.
MANAGEMENT: To ensure maximal and consistent oral absorption, levofloxacin oral solution should be taken at least one hour before or two hours after meals.
For administration of the oral solution with continuous enteral nutrition, some experts recommend that the tube feeding should be interrupted for one hour before and two hours after the dose of levofloxacin.
The oral tablets may be taken without regard to food.
Exacinop 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.
Exacinop Drug Interaction
Moderate: aspirin, albuterol / ipratropium, albuterol, budesonide / formoterol
Unknown: amoxicillin / clavulanate, diphenhydramine, apixaban, omega-3 polyunsaturated fatty acids, furosemide, pregabalin, metoprolol, metoprolol, acetaminophen / hydrocodone, acetaminophen, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, cetirizine
Exacinop Disease Interaction
Major: colitis, CNS disorders, myasthenia gravis, peripheral neuropathy, QT interval prolongation, tendonitis
Moderate: crystalluria, diabetes, hemodialysis, renal dysfunction
Volume of Distribution
Exacinop is widely distributed in the body, with an average volume of distribution following oral administration between 1.09-1.26 L/kg (~89-112 L). Concentrations in many tissues and fluids may exceed those observed in plasma. Exacinop is known to penetrate well into skin tissue, fluids (e.g. blisters), lung tissue, and prostatic tissue, amongst others.
Absorption of levofloxacin following oral administration is rapid and essentially complete, with an oral bioavailability of approximately 99%. Due to its nearly complete absorption, the intravenous and oral formulations of levofloxacin may be interchangeable. The Tmax is generally attained 1-2 hours following administration and the Cmax is proportional to the given dose - an intravenous dose of 500mg infused over 60 minutes resulted in a Cmax of 6.2 ± 1.0 µg/mL whereas a 750mg dose infused over 90 minutes resulted in a Cmax of 11.5 ± 4.0 µg/mL. Oral administration with food prolongs the Tmax by approximately 1 hour and slightly decreases the Cmax, but these changes are not likely to be clinically significant.
Systemic absorption following oral inhalation is approximately 50% lower than that observed following oral administration.
The average terminal elimination half-life of levofloxacin is 6-8 hours.
The average apparent total body clearance of levofloxacin ranges from 8.64-13.56 L/h, and its renal clearance ranges from 5.76-8.52 L/h. The relative similarity of these ranges indicates a small degree of non-renal clearance.
The majority of administered levofloxacin is excreted unchanged in the urine. Following the administration of a single oral dose of levofloxacin, approximately 87% was eliminated unchanged in the urine within 48 hours and less than 4% was eliminated in the feces within 72 hours.
Pregnancy & Breastfeeding use
Exacinop is not recommended for use during pregnancy or nursing, as the effects on the unborn child or nursing infant are unknown.
Exacinop is contraindicated in patients with a history of hypersensitivity to Exacinop, quinolone antimicrobial agents, or any other components of this product.
Use in Children: From clinical studies, it is evident that Exacinop can be used in children aged as low as 6 months.The usual dose for children in community acquired pneumonia (CAP) is-
- Children aged 6 months to less than 5 years: 10 mg/kg b.i.d. (up to 500 mg per day) for 10 days.
- Children aged 5 years to 16 years: 10 mg/kg q.d. (up to 500 mg per day) for 10 days.
The usual dose for children in recurrent or persistent Acute Otitis Media (AOM) is Children aged 6 months to less than 5 years: 10 mg/kg per day (maximum dose: 500 mg/day) given twice daily for 10 days.
Exacinop exhibits a low potential for acute toxicity. However, in the events of an acute overdosage, the stomach should be emptied. The patients should be kept under observation and appropriate hydration should be maintained.
Store in a cool & dry place, protected from light. Keep out of the reach of children.
You find simplified version here Exacinop
Exacinop contains Levofloxacin see full prescribing information from innovator Exacinop Monograph, Exacinop MSDS, Exacinop FDA label
What is Exacinop used for?
Exacinop is used to treat certain infections such as pneumonia, and kidney, prostate , and skin infections.
How safe is Exacinop?
Exacinop generally safe.It can cause serious side effects, including tendon problems, side effects on your nerves , serious mood or behavior changes, or low blood sugar (which can lead to coma).
How does Exacinop work?
Exacinop works by stopping the growth of bacteria.Exacinop treats only bacterial infections.
What are the common side effects of Exacinop?
Common side effects of Exacinop may include:
- nausea, constipation, diarrhea;
- headache, dizziness; or.
- trouble sleeping.
Is Exacinop safe during pregnancy?
Exacinop should be used during pregnancy only if the benefit outweighs the risk to the fetus.According to some authorities, use is contraindicated.
Is Exacinop safe during breastfeeding?
Use of Exacinop is acceptable in nursing mothers with monitoring of the infant for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis.Avoiding breastfeeding for 4 to 6 hours after a dose should decrease the exposure of the infant to levofloxacin in breastmilk.
Can I drink alcohol with Exacinop?
It is safe to drink alcohol in moderation while taking Exacinop.
Can I drive after taking Exacinop?
Do not drive or operate machinery if levofloxacin makes you feel dizzy or tired. Avoid alcohol.
When should be taken of Exacinop?
You can take Exacinop before or after meals. If you are taking one dose a day, it is preferable to take it in the morning. If you are taking more than one dose a day, try to space out your doses so ideally, take a tablet every 12 hours.
Should I take Exacinop at night?
Exacinop is best to take the doses at evenly spaced times, day and night.
Can Exacinop be taken on an empty stomach?
You may take Exacinop tablets with or without food. Take Exacinop oral solution (liquid) on an empty stomach, at least 1 hour before or 2 hours after a meal.
How long does it take for Exacinop to work?
Exacinop will begin working within a matter of hours, but it can be two to three days before symptoms begin to improve. Take the full course of antibiotics as prescribed by a healthcare provider, even if you feel better after a few days.
How long does Exacinop stay in my system?
If the patient generally has good health, the body can eliminate Exacinop in about 30 to 40 hours, or about a day and a half to two days, but some side effects of the drug can show up as long as two months or longer after taking Exacinop.
What happens if I take too much Exacinop?
Liver damage can happen in people who take Exacinop. Call your doctor right away if you have unexplained symptoms such as: nausea or vomiting. stomach pain.
Is Exacinop bad for kidneys?
Case reports have indicated acute kidney injury with use, and prescription labels carry a warning of kidney failure.
Who should not use Exacinop?
Should only be used by adults. Not suitable for people with myasthenia gravis, certain heart rhythm disturbances, or pediatric patients.
Is Exacinop safe for heart patients?
In general, clinicians should be aware that azithromycin and Exacinop are relatively safe for patients without complications or additional risk factors of QT prolongation, and decision regarding the initiation of medication therapy should be made on a case by case basis.
Can Exacinop cause heart palpitations?
If you have low blood potassium or an abnormally slow heartbeat,Exacinop may increase your risk of having a fast, slow, or irregular heartbeat, loss of consciousness, or fainting spells. If these symptoms occur, tell your doctor right away.
What happens if I stop taking Exacinop?
If you experience any of the following symptoms, stop taking Exacinop and call your doctor immediately: numbness, tingling, pain, burning, or weakness in the arms or legs; or a change in your ability to feel light touch, vibrations, pain, heat, or cold.
What happens if I miss a dose of Exacinop?
If you miss a dose of your Exacinop, take it as soon as you remember. If you remember relatively close to the time you take your next dose then you should skip the missed dose. You should then take your next dose and continue on with your normal dosing schedule. Do not double up on doses if you have missed one to avoid an overdose.