Cefpimizole is an antibiotic of broad spectrum developed in Japan for the treatment of such conditions as uncomplicated gonorrhea and gynecologic infections. The drug was tested in clinical trials, however, its development was terminated.

Dequalinium is a quaternary ammonium cation commonly available as the dichloride salt. Dequalinium chloride has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Also, Dequalinium chloride is active against the bacteria which cause bacterial vaginosis. Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. Common side effects are: vaginal discharge; vaginal itching or vaginal burning; vaginal yeast infection (thrush); tender tongue.

Apalcillin is a naphthydridine derivative of ampicillin. Apalcillin has a broad spectrum of antibacterial activity that is very similar to that of piperacillin, except that apalcillin is significantly more active against Pseudomonas aeruginosa and Acinetobacter spp. Against Acinetobacter spp., apalcillin is uniquely active, compared to the other penicillins and comparison drugs. Strains producing high amounts of β-lactamases do become resistant to apalcillin. PAH (p-aminohippurate) clearance was significantly decreased during apalcillin infusion. Apalcillin appeared to compete with PAH for proximal tubular secretion but induced no further renal dysfunction.

Cefsulodin is a third-generation of cephalosporin antibiotic with a narrow spectrum of activity. It has a specific activity against Pseudomonas aeruginosa. Cefsulodin’s targets are bacterial penicillin binding proteins. Drug is indicated for the treatment of infections of lower respiratory tract, skin and skin structures, urinary tract, bone and joint; treatment of gynecological infections; treatment of intra-abdominal infections; treatment of septicemia and CNS infections including meningitis caused by susceptible strains of specific microorganisms. Cefsulodin appears to be well tolerated and relatively free of any significant toxicity except for nausea and vomiting.

Dequalinium is a quaternary ammonium cation commonly available as the dichloride salt. Dequalinium chloride has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Also, Dequalinium chloride is active against the bacteria which cause bacterial vaginosis. Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. Common side effects are: vaginal discharge; vaginal itching or vaginal burning; vaginal yeast infection (thrush); tender tongue.

Astromicin is an aminoglycoside antibiotic produced by Micromonospora spp. It is effective against major gram-negative bacterias such as Proteus, Serratia, Citrobacter, Enterobacter spp., Klebsiella, Escherichia coli and Staphylococcus aureus. Astromicin sulfate has been given by intramuscular injection or intravenous infusion. Side effects are: rash, urticaria, itch, erythema, fever, nausea, vomiting, and diarrhea. Combination with strong diuretics can cause nephrotoxicity and ototoxicity.

Cefprozil is a 2nd generation cephalosporin that is FDA approved for the treatment of mild to moderate infections of upper respiratory tract, lower respiratory tract, and uncomplicated skin and skin-structure infections. Cefprozil, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Common adverse reactions include diarrhea, nausea, vomiting, dizziness, abdominal pain and vaginitis. Nephrotoxicity has been reported following concomitant administration of aminoglycoside antibiotics and cephalosporin antibiotics. Concomitant administration of probenecid doubled the AUC for cefprozil.

Gentamicin is an antibiotic of the aminoglycoside group, is derived by the growth of Micromonospora purpurea, an actinomycete. Gentamicin is a complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1a. Gentamicin is a broad-spectrum antibiotic, but may cause ear and kidney damage. Gentamicin binds to the prokaryotic ribosome, inhibiting protein synthesis in susceptible bacteria. It is bactericidal in vitro against Gram-positive and Gram-negative bacteria. Adverse reactions include adverse renal effects, neurotoxicity (dizziness, vertigo, tinnitus, roaring in the ears, hearing loss, peripheral neuropathy or encephalopathy), respiratory depression, lethargy, confusion, depression, visual disturbances, etc.

Colistin sulfate is a polypeptide antibiotic which penetrates into and disrupts the bacterial cell membrane. It is a cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C). Colistin was first isolated in Japan in 1949 from a flask of fermenting Bacillus polymyxa var. colistinus and became available for clinical use in 1959. The following local adverse events have been reported with topical corticosteroids, especially under occlusive dressings: burning, itching, irritation, dryness, folliculitis, hypertrichosis, etc. Healthcare providers had largely stopped using colistin in the 1970s because of its toxicity. However, with antibacterial resistance on the rise, colistin is increasingly being used today to treat severe, multidrug-resistant Gram-negative bacterial infections, particularly among intensive care-based patients. The problem with re-introducing an older drug, such as colistin, though, is that techniques for evaluating new drugs have evolved since the 1950s, and therefore, little is known about the dose needed to effectively fight infection while limiting the potential emergence of antimicrobial resistance and reducing potentially toxic side effects. More data are needed to guide optimal use of these older medications. An international team of NIAID-funded researchers is making progress in obtaining better dosing information about colistin and how best to use the antibiotic to treat Gram-negative bacterial infections. Resistance to colistin is rare. The first colistin-resistance gene that is carried in a plasmid and can be transferred between bacterial strains was described in 2016. This plasmid-borne mcr-1 gene has since been isolated in China, Europeand the United States.

Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eye drops. In vitro tests have demonstrated that neomycin is bactericidal and acts by inhibiting the synthesis of protein in susceptible bacterial cells. It is effective primarily against gram-negative bacilli but does have some activity against gram-positive organisms. Neomycin is active in vitro against Escherichia coli and the Klebsiella-Entero. Topical uses include treatment for superficial eye infections caused by susceptible bacteria (used in combination with other anti-infective), treatment of otitis externa caused by susceptible bacteria, treatment or prevention of bacterial infections in skin lesions, and use as a continuous short-term irrigant or rinse to prevent bacteriuria and gram negative rod bacteremia in bacteriuria patients with indwelling catheters. May be used orally to treat hepatic encephalopathy, as a perioperative prophylactic agent, and as an adjunct to fluid and electrolyte replacement in the treatment of diarrhea caused to enter pathogenic E. coli (EPEC). Neomycin sulfate has been shown to be effective adjunctive therapy in hepatic coma by reduction of the ammonia forming bacteria in the intestinal tract. The subsequent reduction in blood ammonia has resulted in neurologic improvement. To reduce the development of drug-resistant bacteria and maintain the effectiveness of Neomycin Sulfate Oral Solution and other antibacterial drugs, susceptible bacteria should use Neomycin Sulfate Oral Solution only to treat or prevent infections that are proven or strongly suspected to be caused. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Neomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site near 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