Cephalosporins Health Dictionary

Cephalosporins: From 1 Different Sources


These are broad-spectrum antibiotics. Most are semi-synthetic derivatives of cephalosporin C, an antibiotic originally derived from a sewage outfall in Sardinia.

First-generation examples still in use include cephalexin and cefadroxil. They are orally active and, along with second-generation cefaclor, have a similar antimicrobial spectrum. They are used for ‘resistant’ urinary infections and urinary infections in pregnancy. Cephalosporins have a similar pharmacology to that of penicillin, and about 10 per cent of patients allergic to penicillin will also be hypersensitive to cephalosporins. They are e?ective in treating SEPTICAEMIA, PNEUMONIA, MENINGITIS, biliary-tract infections and PERITONITIS.

Second-generation cefuroxime and cefamandole are less vulnerable to penicillinases and are useful for treating ‘resistant’ bacteria and Haemophilus in?uenzae and Neisseria gonorrhoea. Third-generation cephalosporins include cefotaxime, ceftazidime and others; these are more e?ective than the second-generation in treating some gram-negative infections, especially those causing septicaemia.

Health Source: Medical Dictionary
Author: Health Dictionary

Antibacterial Drugs

A group of drugs, which include ANTIBIOTICS, used to treat infections caused by BACTERIA. Drugs include CEPHALOSPORINS and cephamycins, TETRACYCLINES, AMINOGLYCOSIDES, MACROLIDES, and antituberculous compounds.... antibacterial drugs

Antibiotics

Antibiotic is the term used to describe any antibacterial agent derived from micro-organisms, although most of them are now prepared synthetically. Such agents destroy or inhibit the growth of other micro-organisms: examples are penicillin, cephalosporin, amino-glycosides, streptomycin, and tetracycline.

Penicillin was the ?rst antibiotic to be discovered and used in the 1940s. The discovery and isolation in 1958 of the penicillin nucleus, 6-amino penicillanic acid (6-PNA), allowed many new penicillins to be synthesised. These are now the largest single group of antibiotics used in clinical medicine. Most staphylococci (see STAPHYLOCOCCUS) have now developed resistance to benzylpenicillin, the early form of the drug, because they produce penicillinases – enzymes which break down the drug. Other types of penicillin such as cloxacillin and ?ucoxacillin are not affected and are used against penicillin-resistant staphylococci.

The cephalosporins are derived from the compound cephalosporin C, which is obtained by fermentation of the mould cephalosporium.

The cephalosporin nucleus 7 amino cephalosporanic (7-ICA) acid has been the basis for the production of the semi-synthetic compounds of the cephalosporin nucleus. The ?rst semi-synthetic cephalosporin, cephalothin, appeared in 1962; it was followed by cephaloridine in 1964. The original cephalosporins had to be given by injection, but more recent preparations can be given by mouth. The newer preparations are less readily destroyed by betalactamases and so they have a much broader spectrum of antibacterial activity. The newer cephalosporins include cephalexin, cefazolin, cephacetrile, cephapirin, cefamandole, cefuroxine, cephrodine, cefodroxil and cefotaxine. Inactivation of beta-lactamase is the basis of bacterial resistance both to the penicillins and to the cephalosporins, so that attempts to prepare these antibiotics with resistance to betalactamase is of great importance. A synthetic inhibitor of beta-lactamase called clavulanic acid has been synthesised; this is used in combination with the penicillins and cephalosporins to prevent resistance. The cephamycins are a new addition to the beta-lactam antibiotics. They are similar in structure to the cephalosporins but are produced, not by fungi, but by actinomycetes.

Overuse and misuse of antibiotics have resulted in many bacteria becoming resistant to them. Hospitals, in particular, have problems with METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS (MRSA). Combinations of antibiotics are needed to combat resistant strains of bacteria, another example being Mycobacterium tuberculosis.... antibiotics

Beta Lactams

Antibiotics with a beta-lactam ring in their molecular structure, including the penicillins and the cephalosporins. Act on penicillin binding proteins in the mucopeptides of the bacterial cell wall. Can be destroyed bybacterial beta-lactamases.... beta lactams

Chemotherapy

The prevention or treatment of disease by chemical substances. The term is generally used in two senses: the use of antibacterial and other drugs to treat infections; and the administration of ANTIMETABOLITES and other drugs to treat cancer. The discovery by Paul Ehrlich in 1910 of the action of Salvarsan in treating syphilis led to the introduction of sulphonamides in 1935, followed by PENICILLIN during World War II, which revolutionised the treatment of common infections. Many ANTIBACTERIAL DRUGS have been developed since then: these include CEPHALOSPORINS, cephamycins, TETRACYCLINES, AMINOGLYCOSIDES, MACROLIDES and CLINDAMYCIN as well as antituberculous drugs such as STREPTOMYCIN and METRONIDAZOLE. Unfortunately, overuse of chemotherapeutic drugs in medicine and in animal husbandry has stimulated widespread resistance among previously susceptible pathogenic microorganisms. Chemotherapy also plays an important role in treating tropical diseases, especially MALARIA, SLEEPING SICKNESS and LEPROSY.

Recently chemotherapy has become increasingly e?ective in the treatment of cancer. Numerous drugs, generally CYTOTOXIC, are available; great care is required in their selection and to minimise side-effects. Certain tumours are highly sensitive to chemotherapy

– especially testicular tumours, LEUKAEMIA, LYMPHOMA and various tumours occurring in childhood (e.g. Wilm’s tumour – see NEPHROBLASTOMA) – and may even be cured.... chemotherapy

Penicillinase

A bacterial ENZYME capable of neutralising the antibacterial properties of PENICILLIN and other beta-lactam antibiotics such as the CEPHALOSPORINS. Most staphylococci are now resistant to benzylpenicillin because they produce this enzyme; cloxacillin, ?ucloxacillin and temocillin are not inactivated.... penicillinase

Cephalosporin Drugs

A large group of antibiotic drugs derived from the fungus

CEPHALOSPORIUM ACREMONIUM, which are effective against a wide range of infections.

Cephalosporins are used to treat ear, throat, and respiratory tract infections, and conditions, such as urinary tract infections and gonorrhoea, in which the causative bacteria are resistant to other types of antibiotics.

Occasionally, the drugs cause allergic reactions, such as rash, itching, and fever.

Rarely, anaphylactic shock occurs.

Other side effects include diarrhoea and blood disorders.... cephalosporin drugs

Beta-lactam Antibiotic

one of a group of drugs that includes the *penicillins and the *cephalosporins. All have a four-membered beta-lactam ring as part of their molecular structure. Beta-lactam antibiotics function by interfering with the growth of the cell walls of multiplying bacteria. Bacteria become resistant to these antibiotics by producing beta-lactamases, enzymes (such as *penicillinase) that disrupt the beta-lactam ring. To counteract this, beta-lactamase inhibitors (e.g. *clavulanic acid) may be added to beta-lactam antibiotics. For example, co-amoxiclav is a mixture of *amoxicillin and clavulanic acid.... beta-lactam antibiotic

Impetigo

An infectious skin disease caused usually by Staphylococcus aureus and less often by Streptococcus pyogenes. The itching rash is seen especially on the face but may spread widely. Vesicles and pustules erupt and dry to form yellow-brown scabs. Untreated, the condition may last for weeks. In very young infants, large blisters may form (bullous impetigo).

Treatment Crusts should be gently removed with SALINE. Mild cases respond to frequent application of mupiricin or NEOMYCIN/BACITRACIN ointment; more severe cases should be treated orally or, sometimes, intravenously with FLUCLOXACILLIN or one of the CEPHALOSPORINS. If the patient is allergic to penicillin, ERYTHROMYCIN can be used.

For severe, intractable cases, an oral retinoid drug called isotretinoin (commercially produced as Roaccutane®) can be used. It is given systemically but treatment must be supervised by a consultant dermatologist as serious side-effects, including possible psychiatric disturbance, can occur. The drug is also teratogenic (see TERATOGENESIS), so women who are, or who may become, pregnant must not take isotretinoin. It acts mainly by suppressing SEBUM production in the sebaceous glands and can be very e?ective. Recurrent bouts of impetigo should raise suspicion of underlying SCABIES or head lice. Bactericidal soaps and instilling an antibiotic into the nostrils may also help.... impetigo

Penicillin

The name given by Sir Alexander Fleming, in 1929, to an antibacterial substance produced by the mould Penicillium notatum. The story of penicillin is one of the most dramatic in the history of medicine, and its introduction into medicine initiated a new era in therapeutics comparable only to the introduction of ANAESTHESIA by Morton and Simpson and of ANTISEPTICS by Pasteur and Lister. The two great advantages of penicillin are that it is active against a large range of bacteria and that, even in large doses, it is non-toxic. Penicillin di?uses well into body tissues and ?uids and is excreted in the urine, but it penetrates poorly into the cerebrospinal ?uid.

Penicillin is a beta-lactam antibiotic, one of a group of drugs that also includes CEPHALOSPORINS. Drugs of this group have a four-part beta-lactam ring in their molecular structure and they act by interfering with the cell-wall growth of mutliplying bacteria.

Among the organisms to which it has been, and often still is, active are: streptococcus, pneumococcus, meningococcus, gonococcus, and the organisms responsible for syphilis and for gas gangrene (for more information on these organisms and the diseases they cause, refer to the separate dictionary entries). Most bacteria of the genus staphylococcus are now resistant because they produce an enzyme called PENICILLINASE that destroys the antibiotic. A particular problem has been the evolution of strains resistant to methicillin – a derivative originally designed to conquer the resistance problem. These bacteria, known as METHICILLINRESISTANT STAPHYLOCOCCUS AUREUS (MRSA), are an increasing problem, especially after major surgery. Some are also resistant to other antibiotics such as vancomycin.

An important side-e?ect of penicillins is hypersensitivity which causes rashes and sometimes ANAPHYLAXIS, which can be fatal.

Forms of penicillin These include the following broad groups: benzylpenicillin and phenoxymethyl-penicillin; penicillinase-resistant penicillins; broad-spectrum penicillins; antipseudomonal penicillins; and mecillinams. BENZYLPENICILLIN is given intramuscularly, and is the form that is used when a rapid action is required. PHENOXYMETHYLPENICILLIN (also called penicillin V) is given by mouth and used in treating such disorders as TONSILLITIS. AMPICILLIN, a broad-spectrum antibiotic, is another of the penicillins derived by semi-synthesis from the penicillin nucleus. It, too, is active when taken by mouth, but its special feature is that it is active against gram-negative (see GRAM’S STAIN) micro-organisms such as E. coli and the salmonellae. It has been superceded by amoxicillin to the extent that prescriptions for ampicillin written by GPs in the UK to be dispensed to children have fallen by 95 per cent in the last ten years. CARBENICILLIN, a semi-synthetic penicillin, this must be given by injection, which may be painful. Its main use is in dealing with infections due to Pseudomonas pyocanea. It is the only penicillin active against this micro-organism which can be better dealt with by certain non-penicillin antibiotics. PIPERACILLIN AND TICARCILLIN are carboxypenicillins used to treat infections caused by Pseudomonas aeruginosa and Proteus spp. FLUCLOXACILLIN, also a semi-synthetic penicillin, is active against penicillin-resistant staphylococci and has the practical advantage of being active when taken by mouth. TEMOCILLIN is another penicillinase-resistant penicillin, e?ective against most gram-negative bacteria. AMOXICILLIN is an oral semi-synthetic penicillin with the same range of action as ampicillin but less likely to cause side-effects. MECILLINAM is of value in the treatment of infections with salmonellae (see FOOD POISONING), including typhoid fever, and with E. coli (see ESCHERICHIA). It is given by injection. There is a derivative, pivmecillinam, which can be taken by mouth. TICARCILLIN is a carboxypenicillin used mainly for serious infections caused by Pseudomonas aeruginosa, though it is also active against some gram-negative bacilli. Ticarcillin is available only in combination with clarulanic acid.... penicillin

Pneumonia

Pneumonia is an in?ammation of the lung tissue (see LUNGS) caused by infection. It can occur without underlying lung or general disease, or in patients with an underlying condition that makes them susceptible.

Pneumonia with no predisposing cause – community-acquired pneumonia – is caused most often by Streptococcus pneumoniae (PNEUMOCOCCUS). The other most common causes are viruses, Mycoplasma pneumoniae and Legionella species (Legionnaire’s disease). Another cause, Chlamydia psittaci, may be associated with exposure to perching birds.

In patients with underlying lung disease, such as CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) or BRONCHIECTASIS as in CYSTIC FIBROSIS, other organisms such as Haemophilus in?uenzae, Klebsiella, Escherichia coli and Pseudomonas aeruginosa are more prominent. In patients in hospital with severe underlying disease, pneumonia, often caused by gram-negative bacteria (see GRAM’S STAIN), is commonly the terminal event.

In patients with an immune system suppressed by pregnancy and labour, infection with HIV, CHEMOTHERAPY or immunosuppressive drugs after organ transplantation, a wider range of opportunistic organisms needs to be considered. Some of these organisms such as CYTOMEGALOVIRUS (CMV) or the fungus Pneumocystis carinii rarely cause disease in immunocompetent individuals – those whose body’s immune (defence) system is e?ective.

TUBERCULOSIS is another cause of pneumonia, although the pattern of lung involvement and the more chronic course usually di?erentiate it from other causes of pneumonia.

Symptoms The common symptoms of pneumonia are cough, fever (sometimes with RIGOR), pleuritic chest pain (see PLEURISY) and shortness of breath. SPUTUM may not be present at ?rst but later may be purulent or reddish (rusty).

Examination of the chest may show the typical signs of consolidation of an area of lung. The solid lung in which the alveoli are ?lled with in?ammatory exudate is dull to percussion but transmits sounds better than air-containing lung, giving rise to the signs of bronchial breathing and increased conduction of voice sounds to the stethoscope or palpating hand.

The chest X-ray in pneumonia shows opacities corresponding to the consolidated lung. This may have a lobar distribution ?tting with limitation to one area of the lung, or have a less con?uent scattered distribution in bronchopneumonia. Blood tests usually show a raised white cell (LEUCOCYTES) count. The organism responsible for the pneumonia can often be identi?ed from culture of the sputum or the blood, or from blood tests for the speci?c ANTIBODIES produced in response to the infection.

Treatment The treatment of pneumonia involves appropriate antibiotics together with oxygen, pain relief and management of any complications that may arise. When treatment is started, the causative organism has often not been identi?ed so that the antibiotic choice is made on the basis of the clinical features, prevalent organisms and their sensitivities. In severe cases of community-acquired pneumonia (see above), this will often be a PENICILLIN or one of the CEPHALOSPORINS to cover Strep. pneumoniae together with a macrolide such as ERYTHROMYCIN. Pleuritic pain will need analgesia to allow deep breathing and coughing; oxygen may be needed as judged by the oxygen saturation or blood gas measurement.

Possible complications of pneumonia are local changes such as lung abscess, pleural e?usion or EMPYEMA and general problems such as cardiovascular collapse and abnormalities of kidney or liver function. Appropriate treatment should result in complete resolution of the lung changes but some FIBROSIS in the lung may remain. Pneumonia can be a severe illness in previously ?t people and it may take some months to return to full ?tness.... pneumonia

Antibiotic Drugs

A group of drugs used to treat infections caused by bacteria and to prevent bacterial infection in cases of immune system impairment.

Most of the commonly used antibiotic drugs belong to one of the following classes: penicillins, quinolones, aminoglycosides, cephalosporins, macrolides, and tetracyclines. Some antibiotics are effective against only certain types of bacteria; others, which are known as broad-spectrum antibiotics, are effective against a wide range.

Some bacteria develop resistance to a previously effective antibiotic drug. This is most likely to occur during long-term treatment. Some alternative antibiotics are available to treat bacteria that have become resistant to the more commonly prescribed drugs.

Most antibiotic drugs can cause nausea, diarrhoea, or a rash. Antibiotics may disturb the normal balance between certain types of bacteria and fungi in the body, leading to proliferation of the fungi that cause candidiasis (thrush). Some people experience a severe allergic reaction to the drugs, resulting in facial swelling, itching, or breathing difficulty.... antibiotic drugs

Cephalosporin

n. any one of a group of semisynthetic *beta-lactam antibiotics, derived from the mould Cephalosporium, which are effective against a wide range of microorganisms and are therefore used in a variety of infections. The older (first-generation) cephalosporins include *cefadroxil and *cefalexin; more recent (second-generation) drugs include *cefaclor and *cefuroxime. Third-generation cephalosporins, such as *ceftazidime, cefotaxime, and ceftriaxone, have greater activity against Gram-negative bacteria. Cross-sensitivity with penicillin may occur and the principal side-effects are allergic reactions and irritation of the digestive tract.... cephalosporin



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