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A Basic Overview of Penicillins and Their Use in Small Animal Medicine

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A Basic Overview of Penicillins and Their Use in Small Animal Medicine Volume 47 | Issue 1 Article 7 1985 A Basic Overview of Penicillins and Their seU in Small Animal Medicine Janel Ames Iowa State University Follow this and additional works at: https://lib.dr.iastate.edu/iowastate_veterinarian Part of the Pharmaceutical Preparations Commons, Small or Companion Animal Medicine Commons, and the Therapeutics Commons Recommended Citation Ames, Janel (1985) "A Basic Overview of Penicillins and Their sU e in Small Animal Medicine," Iowa State University Veterinarian: Vol. 47 : Iss. 1 , Article 7. Available at: https://lib.dr.iastate.edu/iowastate_veterinarian/vol47/iss1/7 This Article is brought to you for free and open access by the Journals at Iowa State University Digital Repository. It has been accepted for inclusion in Iowa State University Veterinarian by an authorized editor of Iowa State University Digital Repository. For more information, please contact [email protected]. A Basic Overview of Penicillins and Their Use in Small Animal Medicine by Janel Ames* There are many factors to consider when Penicillinase-resistant penicillins deciding upon antimicrobial therapy. Some of Penicillinase-resistant penicillins (e. g. them are suspected etiology, host status, organ methicillin, naficillin, cloxicillin, dicloxicillin, system affected, and the properties of the drug and oxacillin) were developed by adding sub­ being considered. Iv1icrobicidal drugs, such as stituents onto the aromatic ring of penicillin to penicillin, are superior to bacteriostatic drugs sterically inhibit beta-Iactamases.2 Methicillin in immunosuppressed patients, severe and/or was the first semisynthetic penicillin devel­ overwhelming infections where rapid action is oped but is poorly absorbed orally due to gas­ required, and for long-standing infections to tric acid instability, and is not very potent. All eliminate the pathogen, preventing carrier of the later developed drugs in this group are states or relapses. 1 well absorbed orally except for naficllin. All of Due to the thick cell wall of bacteria and these are effective against Gram-positive beta­ their capability of concentrating solutes, bac­ lactamase producing bacteria. 4 teria have a high intracellular osmolality. Temocillin is a recently developed penicil­ Penicillin causes cell wall defects by inactivat­ linase-resistant penicillin which is active ing bacterial transpeptidase, which prevents against almost all Gram-negative bacteria ex­ the maintenance of an osmolar gradient, cept Pseudomonas. Because of this, it is effective causing formation of spheroblasts, cell lysis, in treating coliform infections, especially en­ and death. 1 teritis and mastitis. It is poorly absorbed Many penicillins have been developed. orally, but when administered parenterally it They can be divided into; natural penicillins, has an unusually long half-life in humans.s semi-synthetic penicillins such as penicil­ linase-resistant penicillins, broad spectrum Broad-spectrum penicillins (amino-) penicillins, and antipseudomonas The broad spectrum penicillins (e. g. ampi­ and extended spectrum penicillins (See table cillin, amoxicillin, and hetacillin) are a very one). important group of drugs due to their activity against both Gram-positive and some Gram­ Natural penicillins negative organisms. They are, however, sus­ Natural penicillins (e. g. penicillin G, peni­ ceptible to penicillinase. This group is stable cillin V, and phenethicillin) were some of the in gastric acid, and therefore effective orally. original penicillins produced. They have a Amoxicillin and ampicillin have equal activ­ limited range of activity and are highly sus­ ity, but an10xicillin is absorbed better orally ceptible to beta-lactamases which are pro­ and has more rapid action. 2 Hetacillin is inac­ duced by many staphylococci and Gram­ tive as it exists in a preparation, but is n10re negative bacteria. They are also inactivated stable in gastric acid then amoxicillin and am­ by gastric acid. These are efficacious only 2 picillin' and therefore it is absorbed best. Af­ against Gram-positive bacteria. ,3 ter it enters the circulation, it is metabolized * Ms. Ames is a second-year student in the College of to ampicillin and becomes active. Amoxicillin Veterinary Medicine at Iowa State University. We would like to acknowledge Dr. R. A. Packer for his editorial and ampicillin are two of the most widely used assistance. penicillins because of their wide range of ac- vol. 47) No. 1 33 4 TABLE ONE: Properties of penicillin derivatives (taken from Greene ). Route of Gastric Beta- Generic Trade Adminis- Acid Lactamase Antimicrobial Name Name tration Stability Resistance Spectrum NATURAL PENICILLINS Penicillin G Many PO, 1M, Poor to fair (20%), No Narrow (gram-positive IV food decreases organisms) Penicillin V Many PO Good (60%) No Narrow (gram-positive organisms) Phenethicillin Many PO Good No Narrow (gram-positive organisms) BETA-LACTAMASE- RESISTANT PENICILLINS Methicillin Staphcillin, Celbenin 1M, IV Poor Yes Narrow (gram-positive beta-lactamase- producing organisms) ISOXAZOLYL PENICILLINSt Nafcillin Unipen, Nafcil 1M, IV Variable (not Yes Narrow (gram-positive, recommended for beta-lactamase- oral use) producing organisms) Cloxacillin Tegopen PO Good Yes Narrow (gram-positive, beta-lactamase - producing organisms) Dicloxacillin Veracillin, Pathocil, PO Good (50%), food Yes Narrow (gram-positive Dynapen decreases (30 %) beta-lactamase- producing organisms) Oxacillin Prostaphlin, Bactocil PO, 1M, Good Yes Narrow (gram-positive, IV beta-lactamase- producing organisms) AMINOPENICILLINStt Ampicillin Many PO, 1M, Good (40%), food No Extended (gram-positive IV decreases cocci, some gram- negative organisms) Amoxicillin Omnipen PO, 1M Excellent (75 %) No Extended (gram-positive cocci, some gram- negative organisms) Hetacillin Hetacin PO Good (40%) No Extended (gram-positive cocci, some gram- negative organisms) ANTIPSEUDOMONAS PENIC1LLINS§ Carbenicillin Pyopen, Geopen 1M, IV Poor No Greater against gram- negative organisms, Pseudomonas, anaerobes Ticarcillin Ticar 1M, IV Poor No Less active than penicillin G on gram-positive organisms EXTENDED-SPECTRUM PENICILLINS Mezlocillin Mezlin 1M, IV Poor No Greater against gram- negative organisms Piperacillin Pipracil 1M, IV Poor No Greater against gram- negative organisms PO =oral; 1M =intravenous; IV =intravenous t Also includes flu cloxacillin and floxacillin. ttAlso includes bacampicillin, cyclacillin, epicillin, pivampicillin, and talampicillin. §Also includes azlocillin, indamylcarbenicillin, carindacillin, and carfecillin. 34 Iowa State University Veterinarian tivity and their ability to produce good plasma skin lesions and pyodermas. The use for soft concentrations, although at similar dosages tissue, urinary, and respiratory infections in they are less effective than crystalline penicil­ humans indicates that the use in small ani­ 1S lin G. Other derivatives in this group are mals may spread in time. S bacampicillin, cyclacillin, epicillin, pivampi­ Sulbactam is also an excellent example of cillin, and talampicillin. 4 this class of drugs because it is an irreversible Antipseudomonas and Extended-spectrum beta-Iactamase inhibitor, yet provides no use­ penicillins ful antibiotic activity. Its main difference Antipseudomonas penicillins (e.g. carbeni­ when compared to clavulanic acid is the two cillin and ticarcillin) are more active against to five-fold decrease in potency. S Pseudomonas and some anaerobes. They are in­ Methicillin and cloxacillin can also provide activated by beta-Iactamases and gastric acid. protection for beta-lactam rings. They com­ Their activity is increased when aminoglyco­ pete for the penicillinase allowing a second "protected" antibiotic (e. g. penicillin G or am­ side antibiotics are also given. 4. 7 Penicillanic acid sulfone (sulbactam), 6-ha­ picillin) to exert its antibacterial effect vir­ lopenicillanic acids, 6-acetyl methylene peni­ tually unhindered. 6 There are four n1ain cri­ cillanic acid, and naturally occurring clavu­ teria that are met by these two drugs. They lanic acid, olivanic acids, and thienamycin are as follows: 1) Their action is primarily due are beta-Iactamase inhibitors that can Dotenti­ to beta-Iactamase inhibition, 2) The "protec­ ate the penicillin antibiotics. Clavula~ic acid tor" drug has a much greater affinity for the is an ideal exampIe of this group. It is a po­ penicillinase than the "protected" drug, 3) tent, irrreversible inhibitor of beta-Iactamase There is little or no hydrolysis of the "protec­ of staphylococci and many Gram-negative tor" drug by the penicillinase, 4) The "protec­ bacteria. It closely matches its antibiotic tor" drug shows no antibacterial activity at the partners, especially amoxicillin, (see figure 1) effective protection concentration. and has little antibacterial activity of its own Staphylococcal penicillinase has a low affin­ that might interfere with the action of the in­ ity for methicillin. Therefore, it is not effective tended primary antibiotic. The minimum in­ in protection of other penicillins from this 6 hibitory concentration required for amoxicil­ penicillinase. lin is markedly reduced when used with Since most penicillins are excreted in the cloxacillin against beta-lactamase producing urine, the blocking analog probenecid can be isolates. Clavulanic acid's wide range of effec­ given simultaneously to increase penicillin tiveness makes it a useful potentiator of many serum levels. This offers yet another alterna­ penicillins. This combination is effective in tive method
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