Aminoglycosides Flashcards
Drugs from Streptomyces bacteria
Streptomycin
Tobramycin
Neomycin
Kanamycin
-mycin
Drugs from Micromonospora
Gentamicin
Amikacin
Netilmicin
-micin
Half-life of aminoglycosides
2-3 hours
Used for this kind of bacteria
Gram-negative enteric bacteria
Reversible or irreversible inhibitors of protein synthesis
Irreversible
Reversible: Tetracyclines
Inhibits the 30S portion (both aminoglycosides and tetracyclines)
Mechanism of action is enhanced by
Penicillin or Vancomycin
Due to the synergistic effect
Mechanism of action is inhibited by
Low extracellular pH and anaerobic conditions
Primary mode of resistance
Production of transferase enzyme that inactivate aminoglycosides by adenylation, acetylation, or phosphorylation (PAA)
Other modes of resistance: Deletion and alteration of a porin protein and deletion or alteration of the receptor protein
Route of administration for the treatment of gram-negative bacterial infections, gram-positive endocarditis, and tuberculosis
Intravenous
Administered as a 30-60 minute infusion
Route of administration that is well-absorbed
Intramuscular
Peak blood concentration: 30-90 minutes
Route of administration where the entire dose is excreted in the feces
Oral
Poor absorption in an intact GIT
Absorption may be increased in an ulcerated tract (like ulcerated colitis)
Bactericidal or bacteriostatic
Bactericidal
Higher concentration = higher antimicrobial activity
Route of elimination
Renal
Higher creatinine clearance = lower dosage needed
Do not penetrate cells readily due to its polarity
Dose adjustments for those with renal impairment
Most ototoxic
Neomycin, Amikacin, Kanamycin
NAK
Most vestibulotoxic
Streptomycin
Gentamicin
SG (Singapore)
Most nephrotoxic
Neomycin
Gentamicin
Tobramycin
NGT (Neomycin’s got talent lol)
Second-line agent for mycobacterial infections, such as TB
Streptomycin
Plague, tularemia, brucellosis, enterococcal endocarditis
Vestibulotoxicity of this drug is the most serious toxic effect and is irreversible
Streptomycin
Used for pediatric populations
Gentamicin
Drug with an IM or IV administration for sepsis and pneumonia
Gentamicin
Topical for burns, other skin lesions
Subconjunctival for ocular infections
Intrathecal for meningitis
Nephrotoxicity of this drug is mild and irreversible and ototoxicity is irreversible
Gentamicin
Used for conjunctivitis (sore eyes)
Tobramycin
Used for multidrug-resistant M. tuberculosis, including streptomycin-resistant strains
Amikacin
Both ototoxic and nephrotoxic
Amikacin
Gentamicin
Neomycin
Kanamycin
AGNK (agent K)
Used for Gentamicin- and Tobramycin-resistant strains
Netilmicin
IM or IV
Drugs under the Neomycin group
Paromomycin
Neomycin
Kanamycin
PNK (pink)
For gram-negative and gram-positive bacteria, and some mycobacteria
Neomycin
Kanamycin
Not active against P. aeruginosa and streptococci
Neomycin
Kanamycin
Used orally for elective bowel surgery preparation and intestinal amoebiasis
Neomycin
Kanamycin
Topical for infected surfaces (used in ophtha)
Injection for joints, pleural cavity, tissue spaces, abcess cavities
IV and IM for TB
Has an adverse reaction of curare-like neuromuscular blockade leading to respiratory paralysis or arrest
Neomycin
Kanamycin
Can be reversed by calcium gluconate or neostigmine
Used parenterally for visceral leishmaniasis
Paromomycin
Intestinal Entamoeba histolytica infection
An aminocyclitol antibiotic, which is structurally related to aminoglycosides, that lacks amino sugars and glycosidic bonds
Spectinomycin
Used as an alternative regimen for drug-resistant gonorrhea and gonorrhea in penicillin-allergic patients
Spectinomycin
IM, single dose
Not active against steptococci and enterococci
Gentamicin
