Products
Cephalosporins are commercially available in the form of film-coated tablets, oral suspensions, granules, and injection and infusion preparations, among others. The basis for the discovery of cephalosporins was the isolation of the mold by the physician Giuseppe Brotzu. He found the fungus in wastewater from Cagliari in Sardinia in 1945. At the University of Oxford at the end of the decade, Edward Abraham and Guy Newton obtained the natural cephalosporins from the fungal cultures. In 1964, Eli Lilly’s Cefalotin, the first representative, came on the market.
Structure and properties
Like penicillins, cephalosporins contain a beta-lactam ring, i.e., they are cyclic amides. This is fused to a dihydrothiazine in the cephalosporins. The basic structure of the cephalosporins is also known as 7-aminocephalosporanic acid. Semisynthetic derivatives have been obtained from the natural active ingredients by modifying the two side chains to alter the pharmacodynamic and pharmacokinetic properties.
Effects
Cephalosporins (ATC J01D) have bactericidal properties. They inhibit bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs). PBPs include transpeptidases, which are responsible for cross-linking peptidoglycan chains during cell wall synthesis.
Indications
For the treatment of bacterial infectious diseases with susceptible pathogens. For example, in respiratory tract infections, skin infections, and urinary tract infections.
Dosage
According to the SmPC. The drugs are administered perorally and parenterally.
Active ingredients
Cephalosporins are classified into five generations depending on their spectrum of activity. However, this is sometimes inconsistent. The following list shows the active ingredients that are approved in many countries:
- Cefaclor (Ceclor)
- Cefamandol (Mandokef)
- Cefazolin (Kefzol, generics)
- Cefepime (Cefepime OrPha, Sandoz).
- Cefpodoxime (Podomexef, Generics)
- Ceftazidime (Fortam, generics)
- Ceftobiprole (Zevtera)
- Ceftriaxone (Rocephin, generic).
- Cefuroxime (Zinate, generic)
Out of commerce in many countries:
- Cefixime (Cephoral)
- Cefotaxime (Claforan)
- Cefprozil (Procef)
- Ceftibuten (Cedax)
Contraindications
Contraindications include:
- Hypersensitivity to the active ingredient or excipients.
- Hypersensitivity to other cephalosporins (possibility of cross-allergy).
- Severe hypersensitivity to beta-lactam antibiotics such as penicillins, carbapenems, and monobactams (possibility of cross-allergy).
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with nephrotoxic agents, drugs that affect gastric pH, vitamin K antagonists, and probenecid, among others.
Adverse effects
The most common potential adverse effects include:
