Penicillin broad-spectrum

Beta-lactamase sensitive penicillins Broad-spectrum penicillins Beta-lactamase resistant penicillins Antipseudomonal penicillins... 

Norfloxacin (1, R = C2H5, R = H), a typical example, exhibits broad-spectrum activity and is useful in the treatment of upper respiratory tract and urinary infections [7] Lomefloxacin (2), a very recent introduction, is a third-generation product that, given once daily, is especially useful against pathogens resistant to cephalosponns, penicillins, and aminoglycosides [4] Floxacillin (J) is a stable, orally active antibacterial with improved activity over thenonfluonnated product (cloxacillin) [5]... 

Widespread clinical acceptance continues to be accorded to the cephalosporins, and the field is extremely active as firms search for the ultimate contender. Among the characteristics desired is retention of the useful features of the older members (relatively broad spectrum, less antigenicity than the penicillins, relative insensitivity toward 3-lactamases, and convenience of administration) while adding better oral activity and broader antimicrobial activity (particularly potency against Pseudomonas, anaerobes, meningococci, cephalosporinase-carrying organisms, and the like). To a considerable extent these objectives have been met, but the price to the patient has been dramatically increased. 

One of the most popular orally active penicillins in present clinical use is amoxicillin (12). Its oral effectiveness and broad spectrum of activity against common pathogens as well as its better absorption than its closest precedent competitor, ampicillin (14), largely accounts for this. Higher blood and tissue levels of antibiotics is another means of dealing with resistance. In an attempt to achieve yet further improvements in oral bioavailability and hence blood and ti.ssue levels of amoxicillin, the prodmg fumoxicillin (13) is prepared from amoxicillin (12) by treatment with furfural [3]. The imine moiety is less basic than the primary amine so that the isoelectric point of fumoxicillin is more on the acid side than is that of amoxicillin. 

Promoting Optimal Response to Therapy The results of a culture and sensitivity test take several days because time must be allowed for the bacteria to grow on the culture media However, infections are treated as soon as possible In a few instances, the primary health care provider may determine that a penicillin is the treatment of choice until the results of the culture and sensitivity tests are known. In many instances, the primary health care provider selects a broad-spectrum antibiotic (ie, an antibiotic that is effective against many types or strains of bacteria) for initial treatment because of the many penicillin-resistant strains of microorganisms. 

Acylation of 6-APA with appropriate substances results in new penicillins being produeed whieh differ only in the nature of the side chain (Table 5.1 Fig. 5.2). Some of these penieillins have considerable activity against Gram-negative as well as Grampositive baeteria, and are thus broad-spectrum antibiotics. Pharmacokinetic properties may also be altered. 

Penicillins (amoxicillin, ampicillin) Broad-spectrum antibiotics may alter intestinal flora, Decrease efficacy of COCs, although the... 

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... 

Ampicillin is the standard penicillin that has broad-spectrum activity, and is the drug of choice for enterococci sensitive to penicillin. Amoxicillin is frequently used as well. Increasing E. coli resistance has limited amoxicillin use in acute cystitis. Amoxicillin-clavulanate is empirically preferred due to resistance. 

A recent prospective study of AAD and CDAD in five Swedish hospitals showed an increased risk of AAD with cephalosporins, clindamycin and broad-spectrum penicillins [42], While CDAD is well recognized as the most common nosocomial gastrointestinal pathogen, some... 

The answer is b. (Hardman, pp 1077—1086.) Piperacillin is a broad-spectrum, semisynthetic penicillin for parenteral use. Its spectrum of activity includes various Gram-positive and Gram-negative organisms including Pseudomonas. The indications for piperacillin are similar to those for car-benicillin, ticarcillin, and mezlocillin, with the primary use being sus-... 

The answer is b. (Hardman, p 1077.) Unlike the other listed drugs, oxacillin is resistant to penicillinase. The other four agents are broad-spectrum penicillins, while oxacillin is generally specific for Gram-positive microorganisms Use of penicillinase-resistant penicillins should be resewed for infections caused by penicillinase-producing staphylococci... 

Only patients with severe AP complicated by necrosis should receive infection prophylaxis with broad-spectrum antibiotics. Agents that cover the range of enteric aerobic gram-negative bacilli and anaerobic organisms should be started within the first 48 hours and continued for 2 to 3 weeks. Imipenem-cilastatin (500 mg every 8 hours) may be most effective a fluoroquinolone (e.g., ciprofloxacin, levofloxacin) with metronidazole should be considered for penicillin-allergic patients. 

In search of novel and more effective antibacterial agents, numerous /1-lactam antibiotics bearing a pyridazine core have been synthesized mainly in Japan. Thus, the penicillin derivative (125) characterized by a 3-hydroxypyridazine-4-carboxamido subunit has been patented as a broad-spectrum bactericide [342-345] likewise, the corresponding cephalosporin analogue has been claimed in a patent [346]. 

Penicillinacylase is used industrially to catalyze the hydrolytic removal of the side chain in naturally occurring penicillins such as benzylpenicillin (4.49) and phenoxymethylpenicillin (4.50). The nucleus 6-aminopenicillic acid (4.48) is then used as the starting material for the preparation of semisynthetic penicillins. Appropriate acylation of the 6-NH2 group leads to )3-lactamase-stable and broad-spectrum penicillins. 

Amoxicillin is a broad spectrum penicillin antibiotic. Antibiotics tend to cause pseudomembranous colitis as a result of colonisation of the colon by Clostridium difficile following antibiotic therapy. 

A patient who is taking phenytoin and is hypersensitive to penicillin requires a broad-spectrum antibacterial agent for a respiratory tract infection. 

Three broad groupings, of the antibiotic substances presently used in animal production, include (a) broad-spectrum antibiotics, including penicillins and tetracyclines, which are effective against a wide variety of pathogenic and non-pathogenic bacteria (b) several narrow-spectrum antibiotics that are not used in human medicine and. (c) the ionophore antibiotics, monensin. lasalocid and salinomycin Monensin and lasalocid are used as rumen fermentation regulators in beef cattle, and the three ionophores are used as coccidiostats in poultry production. The ionophores. which are not used in human medicine, were first introduced in the 1970 s and account for most of the increase in antibiotic usage in animal production since the 1960 s. 

There are many beta-lactamases and they can be classified differently by type of substrate, replacement of genes (chromosomes or plasmids), and place of production. A few of these enzymes directly hydrolyze penicillins (penicillinases), others hydrolyze cephalosporins (cephalosporinases), and others extend to a broad spectrum of substrates. A few bacteria have the ability to induce synthesis of beta-lactamase. Synthesis of beta-lactamase, which in a normal condition is suppressed, is induced in the presence of some beta-lactam antibiotics. 

Clavulanic acid and sulbactam An addition of beta-lactamase inhibitors, such as clavu-lanic acid (32.1.1.35) and sulbactam (32.1.1.36) to penicillins or to aminopenicillins of a broad spectrum of action significantly expands their antimicrobial spectrum. 

Pharmacology Meropenem is a broad-spectrum carbapenem antibiotic. The bactericidal activity of meropenem results from the inhibition of cell-wall synthesis. Meropenem readily penetrates the cell wall of most gram-positive and gram-negative bacteria to reach penicillin-binding-protein (PBP) targets. 

Broad spectrum therapy is started on an empirical basis. Intra-abdominal infections can be treated by ampicillin (or amoxycillin) or clindamycin combined with aminoglycosides, penicillin-beta-lacta-mase inhibitors such as amoxycillin-clavulanic acid or a second or third generation cephalosporin combined with metronidazole are good alternatives. In patients with impaired immunity and/or prior use of antibiotics, i.e. when it is reasonable to expect resistant pathogens, a broad spectrum penicillin plus beta-lactamase inhibitor or a carbapenem can be used empirically in monotherapy. In septic patients, the rapidly bactericidal action of aminoglycosides is useful. Aminoglycosides should preferentially not be given for more than 3-5 days. 

COPD exacerbations. Therefore, in exacerbation treatment with antibiotics is justified when the patient has at least two of three features of increased dyspnea, increased sputum volume, and sputum pu-rulence. Antibiotic choice will depend on local experience derived from local bacteriological sensitivity data. Older, less costly compounds such as tetracycline, doxycycline, amoxicillin, erythromycin, cefaclor etc. are often as effective as newer, more expensive ones. If resistant organisms are suspected or when the severity of the patients clinical condition puts them at high-risk of treatment failure, a second or third generation cephalosporin, fluoroquinolone, newer macrolide or broad-spectrum penicillin may be preferred. In cases of recurrent infection prolonged courses of antibiotics continuous or intermittent, may be useful. 

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