Apogen - General Information
A complex of three different closely related aminoglycoside sulfates, Apogens C1, C2, and C1(subA), obtained from Micromonospora purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit protein synthesis (genetic translation).
Pharmacology of Apogen
Apogen is a broad spectrum aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.
Apogen for patients
No information provided.
Hypersensitivity to gentamicin is a contraindication to its use. A history of hypersensitivity or serious toxic reactions to other aminoglycosides may contraindicate use of gentamicin because of the known cross-sensitivity of patients to drugs in this class.
Additional information about Apogen
Apogen Indication: For treatment of serious infections caused by susceptible strains of the following microorganisms: P. aeruginosa, Proteus species (indole-positive and indole-negative), E. coli, Klebsiella-Enterobactor-Serratia species, Citrobacter species and Staphylococcus species (coagulase-positive and coagulase-negative).
Mechanism Of Action: Aminoglycosides like gentamicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically gentamicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.
Drug Interactions: Atracurium The agent increases the effect of muscle relaxant
Doxacurium The agent increases the effect of muscle relaxant
Gallamine Triethiodide The agent increases the effect of muscle relaxant
Metocurine The agent increases the effect of muscle relaxant
Mivacurium The agent increases the effect of muscle relaxant
Pancuronium The agent increases the effect of muscle relaxant
Pipecuronium The agent increases the effect of muscle relaxant
Rocuronium The agent increases the effect of muscle relaxant
Succinylcholine The agent increases the effect of muscle relaxant
Tubocurarine The agent increases the effect of muscle relaxant
Vecuronium The agent increases the effect of muscle relaxant
Bumetanide Increased ototoxicity
Ethacrynic acid Increased ototoxicity
Furosemide Increased ototoxicity
Torasemide Increased ototoxicity
Thalidomide Thalidomide increases the renal toxicity of the aminoglycoside
Cisplatin Increased risk of nephrotoxicity
Cefradine Increased risk of nephrotoxicity
Cephapirin Increased risk of nephrotoxicity
Cefamandole Increased risk of nephrotoxicity
Cefazolin Increased risk of nephrotoxicity
Cefonicid Increased risk of nephrotoxicity
Cefoperazone Increased risk of nephrotoxicity
Ceforanide Increased risk of nephrotoxicity
Cefotaxime Increased risk of nephrotoxicity
Cefotetan Increased risk of nephrotoxicity
Cefoxitin Increased risk of nephrotoxicity
Ceftazidime Increased risk of nephrotoxicity
Ceftizoxime Increased risk of nephrotoxicity
Ceftriaxone Increased risk of nephrotoxicity
Cefuroxime Increased risk of nephrotoxicity
Cephalothin Group Increased risk of nephrotoxicity
Food Interactions: Not Available
Generic Name: Gentamicin
Synonyms: Not Available
Drug Category: Anti-Bacterial Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Gentamicin: Alcomicin; Apogen; Bristagen; G-Mycin; G-Myticin; Garamycin; Garamycin Otic Solution; Genoptic Liquifilm; Genoptic S.O.P.; Gentacidin; Gentafair; Gentak; Gentamar; Gentamcin Sulfate; Jenamicin; Ocu-Mycin; Spectro-Genta; U-gencin;
Absorption: Injections lead to peak serum concentrations in 30-60 minutes. Topical gentamicin is readily absorbed from large burned, denuded, or granulating areas but not through intact skin. Absorption of gentamicin is faster and greater with the cream compared to the ointment. Gentamicin is absorbed in small quantities following topical application to the eye. Gentamicin is also absorbed in small amounts following topical application to the ear (especially if the eardrum is perforated or if tissue damage is present).
Toxicity (Overdose): Mouse, intravenous LD50: 52 mg/kg; rat, intravenous LD50: 96 mg/kg.
Protein Binding: Low (between 0 and 30%)
Biotransformation: Not Available
Half Life: 3-3½ hours in infants one week to six months of age; this increases to 5½ hours in full-term and large premature infants less than one week old.
Dosage Forms of Apogen: Solution Intravenous
Solution / drops Auricular (otic)
Solution Auricular (otic)
Solution / drops Ophthalmic
Chemical IUPAC Name: 2-[4,6-diamino-3-[3-amino-6-(1-methylaminoethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-methylaminooxane-3,5-diol
Chemical Formula: C21H43N5O7
Gentamicin on Wikipedia: http://en.wikipedia.org/wiki/Gentamicin
Organisms Affected: Enteric bacteria and other eubacteria