It is a synthetic antibiotic from the group of quinolones (fluoroquinolone).
The active ingredient of Elequine is Levofloxacin. It is a broad-spectrum antibacterial whose administration can be oral or intravenous.
The Equine comes in the following presentations:
- Tablets of 250 mg, 500 mg and 750 mg.
- Injectable solution with one container of 100 ml, with 500 mg and 750 mg.
It is also indicated in skin infections such as impetigo in children, abscesses, furunculosis, cellulitis, and erysipelas, as well as in urinary tract infections, including acute pyelonephritis, chronic bacterial prostatitis, and osteomyelitis.
In the case of anthrax by inhalation and exposure to Bacillus anthracis.
In general, Equine is indicated for infections caused by susceptible strains of bacteria in which its clinical efficacy has been demonstrated.
In gram-positive aerobic bacteria such as Streptococcus faecalis, S. agalactiae, S. pyogenes, S. pneumoniae, including multiresistant strains, Staphylococcus aureus, S. epidermidis, S. saprophyticus.
Además bacterias aerobias gramnegativas como: Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca y pneumoniae, Legionella pneumophila, Moraxella (Branhamella) catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens.
And other microorganisms such as Chlamydia pneumoniae, Mycoplasma pneumonia, and Bacillus anthracis.
Mechanism of action
Equine (levofloxacin) mechanism and other antibacterial quinolones act within the bacteria; they penetrate the bacteria through the porins.
These are proteins located in Gram-negative bacteria’s outer membrane and act as a transport channel for the different hydrophilic molecules.
The quinolones perform their bactericidal activity by binding to the bacterial topoisomerases inhibiting them.
Topoisomerases are the enzymes that control bacterial DNA, supercoiling, and unwinding.
Supercoiling allows the DNA molecule to package its long structure within a bacterial cell.
But, this structure must be unrolled to perform different functions such as replication, transcription, and DNA repair.
When the quinolones inhibit the activity of these enzymes, they prevent the bacterial cell from producing the proteins necessary to perform its functions; this very long inhibition leads to the death of the bacterial cell.
There are four types of topoisomerases, and the quinolones act on two of them at the level of DNA gyrase, also called topoisomerase type II and topoisomerase type IV.
The usual recommended dose of Elequine in tablets in patients with normal renal function is 500 or 750 mg orally every 24 hours.
When taken together with Elequine, antacids with components such as calcium, magnesium, or aluminum and sucralfate, cations such as iron, and vitamins with zinc should be administered two hours before or two hours after the administration of Equine.
Equine should only be administered intravenously, never intramuscularly, intraperitoneally, or subcutaneously.
Intravenous infusion should be performed slowly in a period of not less than 60 or 90 minutes when 750 mg doses are applied.
The recommended dose for adults of Elequine is 500 mg administered every 24 hours following the recommended schedule.
Equine is generally well tolerated by patients.
In tests involving Elequine, the incidence of adverse experiences related to the drug was very low.
These adverse events that most commonly occurred and were considered by researchers related to the administration of the drug were:
- The diarrheas.
- The flatulence.
- The abdominal pains.
- The pruritus.
- The dyspepsia.
- La vaginitis.
- Extrinsic allergic alveolitis.
- Anaphylactic clashes.
- Anaphylactic reactions.
- The dysphonia.
- The abnormal electroencephalograms.
- The encephalopathies.
- The eosinophilia.
- Erythema multiforme.
- Hemolytic anemias.
- The multi-system organic failures.
- The beatings.
- Prolongation time extension.
- El síndrome de Stevens Johnson .
Warnings and contraindications
The Equine should not be administered when the patient has hypersensitivity to levofloxacin or other quinolones or any of the components of this product.
Severe and occasionally fatal hypersensitivities and anaphylactic reactions have been reported in patients receiving levofloxacin treatments.
These reactions often occur after the first dose is administered.
The Equine or Levofloxacin should be interrupted when the first symptom appears, the appearance of rashes on the skin, or any other sign of hypersensitivity.
Some severe events caused by unknown immunological mechanisms have been reported in patients receiving quinolone therapy as:
- Dermatological reactions.
- Myalgias .
- The disease of serum.
- Allergic pneumonitis.
- Nefritis intersticiales.
- Insufficiency or acute renal failure
- Jaundice .
- Liver failure
- Liver necrosis
- Hemolytic and aplastic anemia.
- Thrombocytopenia .
- Pancytopenia and other hematologic abnormalities.
Seizures and some toxic psychoses increased intracranial pressure, and stimulation of the central nervous system have also been reported, which can cause symptoms such as:
Tremor, restlessness, anxiety attacks, stuns, confusion, hallucinations, seizures of paranoia, depressive states, restless sleep, nightmares, and insomnia.
These reactions may occur after the first dose is administered.
Quinolones should be used with caution in patients suffering from disorders of the central nervous system who have a predisposition to seizures.
As is the case of severe cerebral arteriosclerosis, epilepsies, or patients presenting other risk factors, such as being subjected to specific therapies for renal dysfunction.
Cases of pseudomembranous colitis have been reported with all antibacterial agents, including levofloxacin; its severity varies from very mild to life-threatening.
So it is essential to consider this diagnosis and the administration of any antibacterial agent when patients present with successive diarrhea.
Treatment with Elequine disrupts the normal flora of the colon and can cause an overgrowth of clostridia.
Some studies have indicated that a toxin caused by Clostridium difficile is one of the leading causes of colitis-associated with antibiotics.
Some quinolones, including levofloxacin, have been associated with prolonging the QT interval in electrocardiograms and infrequent cases of arrhythmia.
During the administration of levofloxacin, helical tachycardia has been reported, although in sporadic cases.
This chaos involves patients with concurrent diseases or concomitant medications.
The risk of symptoms such as arrhythmias can be reduced by avoiding using other medications that prolong the QT interval together with levofloxacin.
Furthermore, it should be avoided when the patient presents risk factors for helical tachycardia, such as low potassium levels, bradycardia, or cardiomyopathy.
There have been ruptures of tendons in the shoulders, hands, and Achilles tendons, which have even required surgery or have caused instability in patients who have received quinolones.
This risk may increase in patients who receive concomitant treatment with corticosteroids, especially in the case of the elderly.
The administration of levofloxacin should be interrupted if the patient experiences pain, tendinitis, or ruptures of a tendon.
Equine or levofloxacin should be used with great caution in patients suffering from renal failure.
In these cases, the dose should be adjusted if necessary and thus avoid the accumulation of levofloxacin due to the decrease in the elimination of the component in the urine.
Moderate to severe phototoxicity reactions have occurred in patients receiving quinolone therapy and exposed directly to light.
Although crystalluria has not yet been reported in clinical trials with levofloxacin, it is necessary to maintain adequate hydration when administering Equine.
It prevents the formation of high concentrations in the urine that could cause the formation of crystals.
When the treatment is administered intravenously, it can cause hypotension when the injection or intravenous bolus is quickly administered.
This medication should only be administered by intravenous infusion very slowly in 60 minutes.
Regarding its administration in patients in the growth stage as children and adolescents, the safety and efficacy of the medication have not yet been established.
It has been observed in growing animals of several species that the treatment with quinolones can produce an erosion in the joints of load, as well as other signs of arthropathy.
The effects on the ability to drive and use machines can be adverse, and neurological effects such as dizziness can occur in patients.
Therefore, patients undergoing therapies with levofloxacin should know these reactions before operating machinery, driving cars, or performing any activity that requires coordination and mental alertness.
There are still no studies on pregnant women, so its use is restricted in the gestation period and could only be used during pregnancy if the benefit of using the medication justifies the potential risk to the fetus.
Due to the potential of the medication to severe adverse reactions in the mothers and that may affect the baby, a decision should be made to interrupt breastfeeding or suspend the drug taking into account the importance for the patient.
Equine interactions orally can occur when administered concurrently with antacids containing calcium, magnesium, aluminum, and sucralfate.
Also, metal cations such as iron and multivitamin compounds containing zinc can obstruct the gastrointestinal absorption of levofloxacin, resulting in lower blood and urine contents than desired.
For this reason, this type of medication should be administered at least two hours before or two hours after administering levofloxacin.
Although it is worth saying that the poisoning caused by these divalent cations is less pronounced than with other quinolones.
Intravenously, there are no data regarding the interaction of quinolones with antacids, oral administration of sucralfate, multivitamin complexes, or metal cations.
However, it must be taken into account that quinolones should not be coadministered with a solution that includes multivalent cations, such as magnesium, through the same intravenous route.
The behavior of other quinolones is similar to the concomitant administration of levofloxacin.
This can lengthen the average life of theophylline, increase blood levels and increase the risk of the occurrence of adverse reactions related to theophylline.
Therefore, theophylline levels should be carefully monitored, and the dose of theophylline should be adjusted, if necessary when coadministered with levofloxacin.
Adverse reactions produced by theophylline, including seizures, may occur with or without elevation of serum levels.
No significant effect was detected in the plasma concentration curves or the arrangement of other parameters in the administration of Elequine together with theophylline.
Similarly, the effects of theophylline have not been observed in the absorption and disposition of Equine.
On the other hand, the concomitant administration of Elequine with digoxin and cyclosporine does not require modification in the dose of any of the compounds.
But, digoxin levels should be monitored in patients receiving concomitant digoxin therapy.
Equine may increase the anticoagulant effects of oral warfarin or one of its derivatives.
Prothrombin time or coagulation tests should be monitored when Elequine and warfarin are administered concomitantly, especially in geriatric patients.
Equine can be safely administered in patients receiving concomitant treatment with probenecid or cimetidine.
Since both reduce the clearance and prolong the half-life of the Equine, as long as the dose of the latter is the most appropriate to the renal function of the patient.
Concomitant administration of Elequine with non-steroidal anti-inflammatory drugs may increase the risk of stimulation of the central nervous system and the appearance of seizures.
Changes in blood glucose, including hyperglycemia and hypoglycemia, have been reported in patients treated concomitantly with Elequine and antidiabetic agents.
Blood glucose monitoring is recommended when these two agents are coadministered.
Like other quinolones, alterations in the results of laboratory tests have been reported.
In the case of glucose, it is common in diabetic patients who are under concomitant treatment with hypoglycemic agents or in therapy with insulin.
In these patients, it is advisable to monitor blood glucose levels.