Aminoglycoside antibiotics table

A new aminoglycoside antibiotic (5 mg/kg) was infused intravenously over 30 min to a 70-kg volunteer. The plasma concentrations of the drug were measured at various times after the end of the infusion, as recorded in the table and shown in the figure below. 

Commercial neomycin is a complex mixture of aminoglycoside antibiotics originally isolated from a culture of Stn.tptomyc.zi, ( n.adiaz by Waksman and his co-workers in 1949. The principle components of the mixture are neomycin B(I) and neomycin C(II) together with a small quantity of neaminel, a degradation product of neomycin formerly known as neomycin A. Table 1 shows the content variability of neomycin B and C and neamine in commercial samples of neomycin as reported in the literature. Neomycins LP-A, LP-B and LP-C which chemically are the mono N-acetyl derivatives of neomycins A, B and C may also be present in small amounts. Several other minor components have recently been identified as paromamine, paromomycin I and paromomycin II. (Also known as neomycins D, E and F respectively). 

TABLE 2.1. Aminoglycoside Antibiotics (AGAs), Designations, and Abbreviations Used Throughout This Chapter... 

Table 1.19. Some aminoglycoside antibiotics which have gained significant therapeutic application. Producer microorganisms are listed in brackets. In addition to naturally produced aminoglycosides, a number of semi-synthetic derivatives have also found medical application. Examples include amikacin, a semi-synthetic derivative of kanamycin and netilmicin, an N-ethyl derivative of sissomicin...

As previously noted, carbenicillin is the only widely used /3-lactam antibiotic for the treatment of infection caused by Ps. aeruginosa. Table 7.5 shows the MIC values of fifty strains of Ps. aeruginosa for a range of j8-lactam antibiotics. From the Table, carbenicillin is the only active drug and at the present time it is the least toxic agent with significant activity in the treatment of pseudomonas infections. It may be used alone or in combination with other antibiotics, e.g. aminoglycosides (see Table 7.1). 

Table 7.13. ANTIBACTERIAL ACTIVITY OF A NUMBER OF AMINOGLYCOSIDE ANTIBIOTICS AGAINST STRAINS OF PS. AERUGINOSA...

To date, six enzymes have been isolated and identified from strains of Ps. aeruginosa which modify aminoglycoside antibiotics. These are listed in Table 7.15. 

Table 7.18. RELATIVE ACTIVITY OF BB-K8, KANAMYCIN AND GENTAMICIN AGAINST STRAINS OF PS. AERUGINOSA RESISTANT TO ONE OR MORE AMINOGLYCOSIDE ANTIBIOTICS...

Table 1 Relative adverse effects of aminoglycoside antibiotics on eighth nerve function, the nervous system, and neuromuscularfunction...

Ototoxicity is a major adverse effect of aminoglycoside antibiotics (13). They all affect both vestibular and cochlear function, but different members of the family have different relative effects (Table 1). 

Although Table 20.7 lists only benzylpenicillin and ampicillin as being inactivated by p-lactamase (from B. cereus), other P-lactams may also be hydrolysed by P-lactamases. Other antibioticinactivating enzymes are also known (Chapter 13) and have been considered as possible inactivating agents, e.g. chloramphenicol acetyltransferase (inactivates chloramphenicol) and enzymes that modify aminoglycoside antibiotics. 

Because of the slow elimination (long half-life) of antimicrobial agents in reptiles, dosage intervals are substantially longer in reptilian compared with mammalian species (Jacobson, 1993) (Table 6.14). To avoid significantly decreased systemic availability of drugs that are eliminated by renal excretion (e.g. (3-lactam and aminoglycoside antibiotics), the site of intramuscular injection should be the anterior half of the body most reptilian species have a well-developed renal portal system. 

Excessive volume depletion, hyponatremia, and hypotension are major risks associated with the use of loop diuretics, and the side effects of hypokalemia, hyperuricemia, and hyperglycemia are always present. Loop diuretics should not be used concurrently with ototoxic aminoglycoside antibiotics (i.e., streptomycin, gentamicin, kanamycin, tobramycin) (see also Table 25). 

Neamine 8, a common structural element in aminoglycoside antibiotics, can be obtained easily through acidic hydrolysis of neomycin B. The modiflcation of its functional groups (Table 3) has a great influence on chemotherapeutic properties. 

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