Quinsair nebulizer solution contains levofloxacin. It is a broad-spectrum quinolone antibiotic that is used as an oral inhalation in the treatment of younger patients with cystic fibrosis and older patients with chronic or repeated pseudomonas infection.

Levofloxacin Oral Inhalation (Quinsair) Uses:

Note: Not approved in the US.

• Cystic fibrosis:

  • It is indicated for use in patients with cystic fibrosis in younger patients and chronic pulmonary Pseudomonas aeruginosa infected older patients.
  • Limitations of use: Safety and efficacy not demonstrated in patients with FEV <25% or >85% predicted, or patients colonized with Burkholderia cepacia.

Levofloxacin Oral Inhalation (Quinsair) Dose in Adults:

Levofloxacin Oral Inhalation (Quinsair) Dose for Cystic fibrosis:

• Inhalation: 240 mg every 12 hours in alternating cycles of 28 days on treatment followed by 28 days off treatment.
• Safety and efficacy of use beyond 6 months (3 consecutive cycles) have not been established.

Use in Children:

Not indicated.

Levofloxacin Pregnancy Risk Category: C

• The amniotic fluid can contain levofloxacin, as it crosses the placental barrier.
• [Canadian Boxed Warn]We have limited information on the safety of using levofloxacin during pregnancy. Studies that are not clinically based suggest that fluoroquinolones may cause damage to the growing organism's weight-bearing cartilage. Alternate inhalation therapy for levofloxacin should be considered during pregnancy.

Levofloxacin use during breastfeeding:

• [Canadian Boxed Warn]: Levofloxacin could be excreted from breast milk.
• Nonclinical studies have shown that fluoroquinolones can damage weight bearing cartilage in growing organisms.
• A case report shows that small amounts of levofloxacin can be found in breast milk after intravenous and oral administration.
• The manufacturer suggests that the mother decide whether to stop breast-feeding and/or discontinue using the drug. This is taking into consideration the importance of the mother's treatment.

Dose in Kidney Disease:

Note: For dosage modification purposes, the Cockcroft-Gault formula can be used to assess renal function.

• CrCl ≥20 mL/minute:
  • No dosage adjustment needed.
• CrCl <20 mL/minute:
  • Its use is not recommended.

Dose in Liver Disease:

No dosage adjustment is necessary.

This product can produce systemic exposure to levofloxacin. See systemic levofloxacin for additional reactions

Common Side Effects of Levofloxacin Oral Inhalation (Quinsair):

• Gastrointestinal:

  • Dysgeusia

Less Common Side Effects of Levofloxacin Oral Inhalation (Quinsair):

• Cardiovascular:

  • Chest discomfort

• Central nervous system:

  • Fatigue
  • Headache
  • Speech disturbance

• Dermatologic:

  • Skin rash

• Gastrointestinal:

  • Nausea
  • Vomiting

• Respiratory:

  • Cough
  • Increased bronchial secretions
  • Hemoptysis
  • Respiratory congestion
  • Thickening of bronchial secretions
  • Discoloration of sputum
  • Dyspnea
  • Paranasal sinus hypersecretion
  • Reduced forced expiratory volume

Contraindications to Levofloxacin Oral Inhalation (Quinsair):

Hypersensitivity to levofloxacin and other quinolones Tendonitis and tendon rupture have been reported in the past due to any quinolone.

Warnings and precautions

• Altered cardiac conduction: [Canadian boxed warning]

  • Fluoroquinolones may prolong QTc intervalArrhythmias are rare. Systemic use of Levofloxacin has been linked to torsades-de-pointes (rare).
  • Patients with a history of QTc prolongation, severe bradycardia or cardiomyopathy, cardiac infarction, untreated hypokalemia, and/or concurrent use of drugs that extend the QT interval, such as cisapride and Class Ia and III antiarrhythmics.

• Bronchospasm

  • It can cause bronchospasm.
  • If severe, symptomatic bronchospasm develops after the administration, you can try short-acting bronchodilators before you take any subsequent doses.
  • If an allergic reaction is suspected, discontinue use of the drug.

• Cough:

  • Use it if you have a persistent cough.

• CNS effects

  • Patients who have known unstable psychiatric symptoms should not take this drug.
  • It can cause toxic psychosis, restlessness, anxiety and dizziness as well as hallucinations, insomnia, depression, and other psychiatric symptoms.
  • This drug can cause an increase in intracranial pressure, so patients with CNS disorders should be cautious.
  • If you experience adverse CNS effects, stop using this drug.
  • Patients should not drive or use machinery if they experience dizziness, fatigue, or any other CNS effects that affect the ability to focus or react.

• Crystalluria

  • Crystalluria with other quinolones is rare; higher urine alkalinity could increase the risk.
  • The patient must be hydrated during the treatment.

• Regulation of Glucose

  • Administration of fluoroquinolones can result in severe, occasionally fatal hypoglycemia.
  • Patients with diabetes who have been treated with insulin and oral hypoglycemic medications experience these outcomes most frequently. They have also been noted in other cases, though.
  • It is important to immediately identify hypoglycemia and treat it.
  • This effect may be caused by quinolones that have different potencies.
  • The most prominent example of this was gatifloxacin, which is no longer marketed as a systemic medication.
  • Fluoroquinolone usage has been linked to hyperglycemia.
  • For signs/symptoms of disordered sugar regulation, strict monitoring is necessary.

• Hemoptysis

  • It can cause hemoptysis.
  • If the benefit outweighs the risk of hemorhage, or if there is a clinically significant hemoptysis, continue treatment.

• Hepatotoxicity:

  • Systemically administered levofloxacin has been linked to severe hepatotoxicity, including acute hepatitis (and fatalities), but it is not related to hypersensitivity.
  • This usually occurs within two weeks.
  • Patients who are older may be at higher risk.
  • Stop utilising medicines if the patient exhibits hepatitis symptoms or signs.

• Hypersensitivity reactions: [Canadian Boxed Warn]

  • When quinolones are administered, anaphylaxis and serious hypersensitivity events could occur.
  • These reactions can be varied in their spectrum.
  • They typically manifest after several doses as common allergic symptoms (such as itching, urticaria, and rash), severe idiosyncratic dermatologic reactions (such as Stevens-Johnson syndrome or toxic epidermal necrolysis), hepatic (such as hepatic failure or necrosis), or hematologic events (such as anaemia or cytopenias).
  • If you experience skin rash, or any other symptoms, stop administering drugs immediately.

• Ophthalmic effects

  • It can cause eye problems so it is important to consult an eye specialist immediately if you have any visual issues. Also, advise the patient to not drive or use machinery.

• Peripheral neuropathy:

  • It can cause irreversible peripheral neuropathy effects. If you experience symptoms of sensorimotor or sensory neuropathy, discontinue therapy.

• Phototoxicity:

  • To avoid phototoxicity, avoid excessive sun exposure and use sunscreen and loose-fitting clothes.
  • Stop using therapy if you experience photosensitivity.

• Seizures: [Canadian Boxed Warning]:

  • Seizures can occur. Be cautious if you are predisposed to seizures, or have conditions that lower your seizure threshold.
  • It is not recommended to use epilepsy medication if there are any history.

• Severe adverse reactions: [Canadian Boxed Warning]

  • Fluoroquinolones have the potential to have severe and possibly permanent side effects.
  • These include neuropsychiatric consequences, tendinitis, tendon rupture, and peripheral neuropathy.

• Superinfection

  • Long-term use may lead to fungal or bacterial superinfection, including pseudomembranous colitis and C. difficile-associated diarrhoea (CDAD); CDAD has been noted more than two months after antibiotic treatment.

• Tendon inflammation/rupture: [Canadian Boxed Warning]:

  • Quinzolone antibiotics have been linked to tendon inflammation and/or rupture.
  • The risk is increased in patients over 60 years, recipients of organ transplants, and patients who are taking concurrent corticosteroids.
  • Most often, rupture of the Achilles tendon has required surgery. However, other tendon sites have been reported (e.g., rotator Cuff, biceps and hand) as it can affect tendons.
  • Tendonitis risk factors include excessive physical activity, kidney failure, and previous tendon disorders, such as rheumatoid or rheumatoid.
  • If there is tendon inflammation, pain, or drug administration, stop immediately.
  • Several months after the therapy has been stopped, this can happen.

• Myasthenia gravis: [Canadian Boxed Warning]:

  • Myasthenia gravis may result in muscle weakness as a result of this.

• Renal impairment

  • Patients with impaired renal function should be cautious.
  • It is not recommended for patients suffering from CrCl levels below 20 mL/min.
  • Increased risk of tendon rupture.

• Rheumatoid arthritis:

  • Patients with rheumatoid arthritis should be aware of the potential for tendon rupture when using this drug.

Levofloxacin (United States: Not available) (oral inhalation): Drug Interaction

Monitoring parameters

• During treatment, perform routine checks on the kidney, liver, and hematopoietic systems.
• Monitor for the signs and symptoms of hypersensitivity or crystalluria;
• blood glucose (diabetic patients);
• Observe for bronchospasm or hemoptysis following administration.

How to administer Levofloxacin Oral Inhalation (Quinsair)?

Inhalation:

• Inhale over ~5 minutes using nebulizer handset recommended by the manufacturer (see product labeling).
• Do not mix levofloxacin with other medications.

The suggested sequence of administration is as follows for patients utilising several inhalation therapies:

• bronchodilators, dornase alfa, airway clearance techniques, levofloxacin, and lastly inhaled steroids.
• Use a short-acting inhaled bronchodilator 15 minutes to 4 hours before consecutive doses of levofloxacin if acute, asymptomatic bronchospasm follows levofloxacin delivery.

Mechanism of action of Levofloxacin Oral Inhalation (Quinsair):

The inhibition of the bacterial DNA gyrase (both are type II topoisomerases), which is required for DNA replication, transcription and repair.

Absorption-

• Systemic absorption after multiple-dose oral inhalation is roughly equal to that following systemic administrations of levofloxacin 250-500 mg

Protein binding:

• ~30% to 40%

Metabolism:

• Minimal

Half-life elimination:

• 5 to 7 hours

Time to peak:

• 0.5 to 1 hour

Excretion:

• Renal (>85%)

International Brand Names of Levofloxacin Oral Inhalation:

• Quinsair

Levofloxacin Oral Inhalation Brand Names in Pakistan:

Oral Inahaltional formulations are not available in Pakistan.