amikacin liposome (oral inhalation)

Action and Spectrum

Actions and Spectrum: 

Actions: 

• Antibacterial Activity: Like regular amikacin, amikacin liposome would likely have antibacterial activity, targeting a broad spectrum of Gram-negative and some Gram-positive bacteria. It could inhibit bacterial protein synthesis by binding to the bacterial ribosome. 
• Improved Delivery: The liposomal formulation might allow for targeted drug delivery to the respiratory tract, potentially enhancing the drug’s concentration at the site of infection and reducing systemic side effects. 
• Resistant Bacteria: If the liposomal formulation exhibits different pharmacokinetics than conventional amikacin, it may also affect its activity against certain resistant bacteria. 

Spectrum: 

The spectrum of amikacin liposome oral inhalation would be similar to that of conventional amikacin, targeting a range of bacterial species, including but not limited to: 

• Pseudomonas aeruginosa 
• Escherichia coli 
• Klebsiella pneumoniae 
• Acinetobacter baumannii 
• Mycobacterium tuberculosis (if indicated) 

Drug Interaction

Adverse Reaction

Frequency defined 

>10%  

Nausea (12%) 

Diarrhea (13%) 

Voice disorder (48%)
Asthenia (16%) 

Ototoxicity (17%) 

1-10% 

Chest discomfort (5%) 

Anxiety (5%) 

Dizziness (6%) 

Balance impairment (1%) 

Headache (10%) 

Pneumonia (9%) 

Respiratory failure (3%) 

Pneumothorax (2%) 

Black Box Warning

Black Box Warning: 

Respiratory adverse reactions are seen as a risk with hemoptysis, allergic pneumonitis, bronchospasm, and exacerbation of pulmonary diseases. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Renal impairment 
• Vestibular dysfunction 

Cautions: 

• Renal impairment 
• Neuromuscular dysfunction 
• Use in pregnancy & lactation 
•  Drug interactions 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available. 

Breastfeeding warnings:  

No data is available. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show fetal risks in the first or later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

amikacin is an aminoglycoside antibiotic with broad-spectrum antibacterial activity. It is effective against many Gram-negative and some Gram-positive bacteria. amikacin inhibits bacterial protein synthesis by binding to the bacterial ribosome, leading to the misreading of mRNA and inhibiting the production of essential bacterial proteins.

Liposomes are lipid-based vesicles that can encapsulate drugs. In this hypothetical formulation, amikacin would be encapsulated within liposomes. Liposomes can enhance drug delivery to specific tissues or organs, allowing targeted therapy and potentially reducing systemic side effects. 

Pharmacodynamics: Inhalation of liposomes can allow for targeted delivery of amikacin to the respiratory tract, particularly useful for treating respiratory infections caused by susceptible bacteria. 

• Liposomal Stability: The liposomal formulation would protect amikacin from degradation and enhance its stability, leading to a longer duration of action. 
• Inhalation Route: The inhalation route would allow amikacin to directly reach the site of infection in the lungs, optimizing drug concentrations at the target site. 
• Bacterial Protein Synthesis Inhibition: The primary pharmacodynamic action of amikacin involves inhibiting bacterial protein synthesis by binding to the bacterial ribosome. This action would remain the same in an inhalable liposomal formulation. 
• Bactericidal Effect: amikacin is a bactericidal antibiotic that kills bacteria rather than just inhibiting their growth. The bactericidal effect would likely be maintained in the liposomal formulation. 

Pharmacokinetics: 

Absorption 

amikacin is primarily administered intravenously for systemic infections. It is not well absorbed orally and is only sometimes available in oral formulations. 

Distribution 

After intravenous administration, amikacin rapidly distributes into various body tissues and fluids, including the lungs, kidneys, skin, and bones. It has a relatively large volume of distribution, indicating extensive tissue penetration. 

Metabolism 

amikacin is not significantly metabolized in the body.  

Elimination and Excretion 

The elimination of amikacin is predominantly through the kidneys via glomerular filtration. A small fraction may undergo some tubular reabsorption, leading to prolonged urinary excretion. 

Adminstartion

Administration: 

amikacin is delivered in the form of liposomes through oral inhalation. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: amikacin liposome oral inhalation 

Pronounced as: AM-i-KAY-sin 

Why do we use amikacin liposome oral inhalation? 

amikacin is an antibiotic with broad-spectrum activity against specific bacterial pathogens, including multidrug-resistant strains. It could treat respiratory infections caused by susceptible bacteria if formulated as an inhalable liposomal preparation.