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Questions and Answers
Which of the following is NOT a member of the aminoglycoside class?
Which of the following is NOT a member of the aminoglycoside class?
- Netilmicin
- Erythromycin (correct)
- Gentamicin
- Kanamycin
Which ring structure is common among aminoglycosides?
Which ring structure is common among aminoglycosides?
- Octose ring
- Pentose ring
- Hexose ring (correct)
- Heptose ring
Why should aminoglycosides be taken on an empty stomach?
Why should aminoglycosides be taken on an empty stomach?
- To enhance their stability in solution
- To allow for better absorption due to alkaline conditions
- To avoid interaction with acidic pH (correct)
- To reduce the risk of resistance mechanisms
What is the primary mechanism of action of aminoglycosides?
What is the primary mechanism of action of aminoglycosides?
What enhances the transport of aminoglycosides across the cell membrane?
What enhances the transport of aminoglycosides across the cell membrane?
All are established mechanisms of resistance to aminoglycosides, Except?
All are established mechanisms of resistance to aminoglycosides, Except?
What is the half-life of aminoglycosides in serum?
What is the half-life of aminoglycosides in serum?
Which of the following best describes the dosing preference for aminoglycosides?
Which of the following best describes the dosing preference for aminoglycosides?
What type of killing do aminoglycosides exhibit?
What type of killing do aminoglycosides exhibit?
How are aminoglycosides mainly eliminated from the body?
How are aminoglycosides mainly eliminated from the body?
In what condition can aminoglycoside concentrations increase in specific parts of the body?
In what condition can aminoglycoside concentrations increase in specific parts of the body?
What type of antibiotic when administered with aminoglycosides may exhibit synergistic killing against certain bacteria?
What type of antibiotic when administered with aminoglycosides may exhibit synergistic killing against certain bacteria?
Which type of bacteria are aminoglycosides primarily used against?
Which type of bacteria are aminoglycosides primarily used against?
In which scenario are aminoglycosides almost always used in combination with a β-lactam antibiotic?
In which scenario are aminoglycosides almost always used in combination with a β-lactam antibiotic?
Which class of drugs are aminoglycosides often combined with to extend empiric coverage?
Which class of drugs are aminoglycosides often combined with to extend empiric coverage?
What characteristic makes aminoglycosides more likely to be ototoxic and nephrotoxic?
What characteristic makes aminoglycosides more likely to be ototoxic and nephrotoxic?
Which type of damage can vestibulotoxicity caused by aminoglycosides result in?
Which type of damage can vestibulotoxicity caused by aminoglycosides result in?
Which aminoglycosides are known to cause auditory damage?
Which aminoglycosides are known to cause auditory damage?
What is the primary toxicity associated with aminoglycosides at certain threshold concentrations?
What is the primary toxicity associated with aminoglycosides at certain threshold concentrations?
Which dosing strategy results in a greater total time above the threshold concentration with aminoglycosides?
Which dosing strategy results in a greater total time above the threshold concentration with aminoglycosides?
Among Neomycin, Tobramycin, and Gentamicin, which aminoglycoside is the most nephrotoxic?
Among Neomycin, Tobramycin, and Gentamicin, which aminoglycoside is the most nephrotoxic?
Which aminoglycosides are considered the most vestibulotoxic?
Which aminoglycosides are considered the most vestibulotoxic?
In what form have creams, ointments, and solutions containing gentamicin sulfate been used?
In what form have creams, ointments, and solutions containing gentamicin sulfate been used?
What is the maximum daily dosage of streptomycin for adults?
What is the maximum daily dosage of streptomycin for adults?
What is the most serious toxic effect with streptomycin?
What is the most serious toxic effect with streptomycin?
What adverse effect can streptomycin cause if given during pregnancy?
What adverse effect can streptomycin cause if given during pregnancy?
Why should aminoglycosides NOT be used as single agents for therapy of pneumonia?
Why should aminoglycosides NOT be used as single agents for therapy of pneumonia?
Which bacterial strains are NOT inhibited by Gentamicin according to the text?
Which bacterial strains are NOT inhibited by Gentamicin according to the text?
Which local conditions contribute to the limited activity of aminoglycosides in treating pneumonia?
Which local conditions contribute to the limited activity of aminoglycosides in treating pneumonia?
Which bacterium is Streptomycin NOT commonly used to treat?
Which bacterium is Streptomycin NOT commonly used to treat?
What type of reactions are considered uncommon with gentamicin use?
What type of reactions are considered uncommon with gentamicin use?
Which condition is most likely to result from prolonged use of gentamicin?
Which condition is most likely to result from prolonged use of gentamicin?
Which aminoglycoside is known to have almost the same antibacterial spectrum as gentamicin but is slightly more active against Pseudomonas aeruginosa?
Which aminoglycoside is known to have almost the same antibacterial spectrum as gentamicin but is slightly more active against Pseudomonas aeruginosa?
Which aminoglycoside is resistant to many enzymes that inactivate gentamicin and tobramycin?
Which aminoglycoside is resistant to many enzymes that inactivate gentamicin and tobramycin?
Which aminoglycoside is available for inhalation form and as ophthalmic ointment or drops for the treatment of Superficial Eye Infections?
Which aminoglycoside is available for inhalation form and as ophthalmic ointment or drops for the treatment of Superficial Eye Infections?
Which aminoglycoside is an alternative treatment for drug-resistant gonorrhea?
Which aminoglycoside is an alternative treatment for drug-resistant gonorrhea?
Which aminoglycoside is more toxic in terms of its effects on the auditory portion of the eighth nerve?
Which aminoglycoside is more toxic in terms of its effects on the auditory portion of the eighth nerve?
Which bacteria are generally resistant to neomycin?
Which bacteria are generally resistant to neomycin?
Why is neomycin generally limited to topical and oral use?
Why is neomycin generally limited to topical and oral use?
For which condition can paromomycin be used?
For which condition can paromomycin be used?
Which drug is limited to the treatment of Multi-Drug-Resistant Tuberculosis?
Which drug is limited to the treatment of Multi-Drug-Resistant Tuberculosis?
What is the main route of excretion for absorbed neomycin?
What is the main route of excretion for absorbed neomycin?
Where are solutions containing neomycin primarily used when infection is present?
Where are solutions containing neomycin primarily used when infection is present?
What is the primary use of neomycin for oral administration?
What is the primary use of neomycin for oral administration?
Which group of drugs have significant nephrotoxicity and ototoxicity according to the text?
Which group of drugs have significant nephrotoxicity and ototoxicity according to the text?
How is neomycin primarily eliminated from the body?
How is neomycin primarily eliminated from the body?
What can act as antidotes in cases of kanamycin toxicity resulting in curare-like neuromuscular blockade and respiratory arrest?
What can act as antidotes in cases of kanamycin toxicity resulting in curare-like neuromuscular blockade and respiratory arrest?
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Study Notes
Aminoglycosides Overview
- Aminoglycosides are primarily used against gram-negative bacteria
- They inhibit protein synthesis by binding to the 30S ribosomal subunit
Mechanism of Action
- The primary mechanism of action of aminoglycosides is by binding to the 30S ribosomal subunit, inhibiting protein synthesis
- Polymyxin enhances the transport of aminoglycosides across the cell membrane
Pharmacokinetics
- Aminoglycosides have a half-life of 2-3 hours in serum
- They are mainly eliminated from the body through the kidneys
- Dosing preference for aminoglycosides is once-daily dosing
Resistance
- All mechanisms of resistance to aminoglycosides have been established, except for target modification
- Resistance to aminoglycosides can occur through enzymatic modification, target modification, and altered permeability
Adverse Effects
- Aminoglycosides are ototoxic and nephrotoxic due to their high positive charge and ability to accumulate in the inner ear and kidneys
- Ototoxicity can result in irreversible auditory damage
- Nephrotoxicity can occur at certain threshold concentrations
- Aminoglycosides can also cause vestibulotoxicity, resulting in balance and coordination problems
Specific Aminoglycosides
- Gentamicin, tobramycin, and amikacin are commonly used aminoglycosides
- Neomycin is not absorbed orally and is primarily used topically or orally for gut decontamination
- Streptomycin is used to treat tuberculosis and is teratogenic
Indications and Contraindications
- Aminoglycosides are used against gram-negative bacteria, such as Pseudomonas aeruginosa and E. coli
- They are often used in combination with β-lactam antibiotics for broad-spectrum coverage
- Aminoglycosides should not be used as single agents for therapy of pneumonia due to limited activity in the lungs
- Gentamicin is not effective against Streptococcus, anaerobes, and methicillin-resistant Staphylococcus aureus
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