Penicillins Erythromycin

Penicillin, erythromycin, tetracycline, and cephalosporins are among the most widely used. Synthetic modifications of the naturally occurring antibiotic compounds have produced many variations that have the necessary clinical properties. 

Human tetanus immemoglobulin 150 units/kg should be given intramuscularly at multiple sites to neutralise unbound toxin. Where present, woimds should be debrided. Metronidazole is an antibiotic of choice for Clostridium tetani, but penicillin, erythromycin, tetracycline, chloramphenicol and clindamycin are acceptable alternatives (see p. 211). 

Penicillin, erythromycin, cephalosporin, streptomycin, vancomycin, bacitracin, etc. 

Neuhauser, M. M., Prause, J. L., Jung, R., Boyea, N., Hackleman J. M., Danziger, L. H., and Pendland, S. L. (1999). In vitro bactericidal activity of ABT-773, a new ketolide, versus clarithromycin (CL) and azithromycin (AZ) against penicillin/erythromycin-sensitive and -resistant Streptococcus pneumoniae (SP). Presented at 39th Intersci. Conf. Antimicrob. Agents Chemother. (Sept. 26-29, San Francisco). Abstr. No. 2139. 

ABT-773, 1 l-amino-3-O-descladinosyl-l l-deoxy-3-oxo-6-0-(3"-quinolyl-2 -propenyl) erythromycin A 11,12-cyclic carbamate, is a novel ketolide antimicrobial being developed for clinical use. ABT-773 has demonstrated in vitro activity against community-acquired respiratory pathogens including penicillin/ erythromycin sensitive and resistant strains of S. pneumoniae. Due to its in vitro activity against resistant pathogens, ABT-773 may represent another therapeutic option for community-acquired pneumonia and other respiratory infections [106]. To date, published pharmacokinetic information about clinical trials is not available. The following preclinical results could be used to assist in the prediction of potential in vivo human pharmacokinetic profiles with ABT-773. 

Agneu ( neu ) Moania complains to his physician of a fever and cough. His cough produces thick yellow-brown sputum. A stain of his sputum shows many Gram-positive, bullet-shaped diplococci. A sputum culture confirms that he has pneumonia, a respiratory infection caused by Streptococcus pneumoniae, which is sensitive to penicillin, erythromycin, tetracycline, and other antibiotics. Because of a history of penicillin allergy, he is started on oral erythromycin therapy. 

The data showed that E. coli was almost 100% resistant to therapeutic antibiotics such as penicillin, erythromycin, tetracycline and streptomycin, which have been in use for a long time. Newer antibiotics are still effective but E. coli may become resistant to them as well overtime. Due to this rapid development of resistance, E. coli diarrhoea in piglets, MMA in sows and umbilicus inflammation in chicks may become more severe, leading to higher economic losses in livestock production. Some potential problems in layers are displayed in table 2. 

Antimicrobials Penicillins, erythromycin, tetracyclines Diarrhea, esophageal inflanunation... 

Sensitivity to antimicrobial agents. P. acnes is sensitive to penicillin, erythromycin and novobiocin, and resistant to streptomycin and sulfamides (Pochi and Strauss, 1961). All strains are especially resistant to sulfamides, being able to grow in the presence of more than 500 ig/ml of these agents. Insensitive to lysozyme. 

Erythromycin is active against gram-positive and certain gram-negative bacteria, also against Rickettsia and spirochaetes. It is used for patients who are allergic to or do not respond to treatment with penicillins or tetracyclines. 

Antibiotics. Solvent extraction is an important step in the recovery of many antibiotics (qv) such as penicillin [1406-05-9] streptomycin [57-92-17, novobiocin [303-81-1J, bacitracin [1405-87-4] erythromycin, and the cephalosporins. A good example is in the manufacture of penicillin (242) by a batchwise fermentation. Amyl acetate [628-63-7] or -butyl acetate [123-86-4] is used as the extraction solvent for the filtered fermentation broth. The penicillin is first extracted into the solvent from the broth at pH 2.0 to 2.5 and the extract treated with a buffet solution (pH 6) to obtain a penicillin-rich solution. Then the pH is again lowered and the penicillin is re-extracted into the solvent to yield a pure concentrated solution. Because penicillin degrades rapidly at low pH, it is necessary to perform the initial extraction as rapidly as possible for this reason centrifugal extractors are generally used. 

The commercial production of penicillin and other antibiotics are the most dramatic in industrial microbiology. The annual production of bulk penicillin is about 33 thousand metric tonnes with annual sales market of more than US 400 million.8 The worldwide bulk sales of the four most important groups of antibiotics, penicillins, cephalosporins, tetracyclines and erythromycin, are US 4.2 billion per annum.10... 

The lincosamides, another group of anti-infectives, are effective against many gram-positive organisms, such as streptococci and staphylococci. However, because of their high potential for toxicity, the lincosamides are usually used only for the treatment of serious infections in which penicillin or erythromycin (a macrolide) is not effective... 

The results showed that the compounds studied with more frequency in the aquatic environment, and of which, logically, there is more information, are the antibiotics, analgesics and anti-inflammatories (like diclofenac, ibuprofen, naproxen, acetylsalicylic acid, and paracetamol), as well as the p-blocker atenolol. In the category of antibiotics, several families are included, like the macrolides (erythromycin), the fluoroquinolones (ofloxacin and ciprofloxacin), sulfonamides (sulfamethoxazole), penicillins (amoxicillin), the metronidazol, and trimethoprim. Other therapeutic groups also widely studied and frequently found in the environmental waters are the lipid regulators (gemfibrozil and bezafibrat), antiepileptic carbamaze-pine, and antidepressants (diazepam, fluoxetine, paroxetine) (see Table 3). 

In some infections the pathogenic organisms are located intracellularly within phagocytic cells and, therefore, remain relatively protected from drugs which penetrate cells poorly, such as the penicillins and cephalosporins. In contrast, erythromycin, rifampicin and chloramphenicol readily penetrate phagocytic cells. Legionnaires disease is an example of an intracellular infection and is treated with rifampicin and/or erythromycin. 

In some cases enzymes can increase the rate of reaction by up to lO times. Carnell and Roberts (1997) have briefly discussed the scope of biotransformations that are used to make pharmaceuticals like penicillins, cephalosporines, erythromycin, lovastatin, cyclosporin, etc., and for food additives like citric acid, L-glutamate, and L-lysine. A very successful transformation by Zeneca has been that of benzene reduction, with Pseudomonase Putida, to dihydrocatechol and catechol the dihydro derivative is used to produce (+/-) pinitol. Fluorobenzene has been converted to fluorodihydrocatechol, an intermediate for pharmaceuticals. The highly stereo selective Bayer-Villeger reaction has been carried out with genetically engineered S-cerevisvae. Hydrolases have allowed enantioselective, and in some cases regioselective, hydrolysis of racemic esters. 

Allopurinol, barbiturates, benzodiazepines, captopril, carbamazepine, erythromycin, fluoroquinolones, isoniazid, NSAIDs, penicillins, phenothiazines, phenytoin, rifampin, sulfonamides antimicrobials, and tetracyclines... 

Erythromycin (Ery-tab) Nipple Candidiasis 333 mg orally three times daily x 10-14 days Second-line agent in penicillin-allergic patients... 

Treat acute mastitis with antistaphylococcal antibiotics such as dicloxacillin or cephalexin for 10 to 14 days in order to prevent recurrent disease and breast abscess12 (Table 44-5). Penicillin-allergic women alternatively may be treated with erythromycin.12 Occasionally, intravenous antibiotics are needed for resistant, recurrent, or chronic cases. Encourage women to continue breast-feeding through acute mastitis and to empty all leftover milk from the affected breast.12... 

Children with SCD should receive prophylactic penicillin until at least the age of 5 years, even if they have been immunized appropriately with PCV 7 against pneumococcal infections. Penicillin V potassium typically is initiated at age 2 months with a dose of 125 mg orally twice daily until age 3 years and then 250 mg orally twice daily until 5 years of age. The intramuscular use of benzathine penicillin 600,000 units every 4 weeks from age 6 months to 6 years is also an option for non-compliant patients. Penicillin-allergic patients may receive erythromycin 10 mg/kg twice daily. Penicillin prophylaxis usually is not continued in children over the age of 6 years but may be considered in patients with a history of invasive pneumococcal infection or surgical splenectomy.6,18-20... 

Broad intravenous antibiotic coverage for the encapsulated organisms can include ceftriaxone or cefotaxime. For patients with true cephalosporin allergy, clindamycin may be used. If staphylococcal infection is suspected owing to previous history or the patient appears acutely ill, vancomycin should be initiated. Macrolide antibiotics, such as erythromycin and azithromycin, may be initiated if Mycoplasma pneumonia is suspected. While the patient is receiving broad-spectrum antibiotics, their regular use of penicillin for prophylaxis can be suspended. Fever should be controlled with acetaminophen or ibuprofen. Because of the risk of dehydration during infection with fever, increased fluid may be needed.6,27... 

Because GAS historically has been the primary causative organism, penicillin has been the mainstay of therapy. O However, the incidence ofS. aureus impetigo is increasing, so oral penicillinase-stable penicillins or first-generation cephalosporins are now preferred.3 Erythromycin is an alternative choice when penicillin allergy is a concern. Topical mupirocin may be used alone when there are few lesions.3... 

I Penicillin is the treatment of choice for erysipelas. In uncomplicated cases, a 5-day course is as effective as a 10-day course.3 Other agents that are acceptable for treatment include clindamycin, erythromycin, cephalexin, and dicloxacillin. 

Parenterally administered penicillin is recommended for all stages of syphilis. Alternative agents may be used in allergic individuals and include doxycycline, minocycline, tetracycline, or erythromycin base or stearate. Some patients may not respond favorably to alternative modalities. Therefore, in patients who must be administered penicillin (i.e., patients who are pregnant or have central nervous system [CNS] involvement) or are allergic, desensitization must be performed before the drug is initiated. 

---