Antimicrobials and chemotherapeutics
Chapter 9
Antimicrobials and chemotherapeutics
22 topics, 14 written so far
β-lactams and glycopeptides: bacterial cell wall synthesis inhibitors
- β-lactam antibiotics: overviewWhat penicillins, cephalosporins, carbapenems and monobactams have in common, from the ring that defines them to how bacteria resist them, the allergy patients fear and their use in pregnancy.
- 70PenicillinsThe first antibiotic and its descendants, in three groups, each reaching bacteria the last could not, the inhibitors that protect them, and what to watch for with each.
- 71CephalosporinsFour generations from cefazolin to cefepime and the advanced generation beyond them, how the spectrum shifts between them, where each is used, and the few toxicities that set particular drugs apart.
- 72Carbapenems and monobactams. GlycopeptidesThe broadest β-lactams, the one whose ring stands alone, the glycopeptides, which stop the same wall being built by binding its building blocks instead of the enzyme, and fosfomycin and bacitracin, which stop it earlier still.
Bacterial protein synthesis inhibitors
- 73Aminoglycosides (30S inhibitors)Bactericidal antibiotics for aerobic gram-negatives, given by injection once a day for a high peak, whose levels are watched because they can harm the kidney and, often for good, the inner ear.
- 74Tetracyclines (30S inhibitors)Broad-spectrum antibiotics on the 30S subunit that stop bacteria growing, the first choice for rickettsiae, Lyme disease and chlamydia, which bind calcium wherever they meet it, in milk and antacids, and in a child's growing teeth.
- 75Macrolides and ketolides (50S inhibitors)Large-ringed antibiotics that block the exit tunnel of the 50S subunit, for the bacteria of the airways, atypical ones among them, and a few of the gut and genitals; and the interactions and heart rhythm to watch for with them.
- 76Lincosamides. Amphenicols (50S inhibitors)Clindamycin, for gram-positive cocci and anaerobes and to switch off bacterial toxins, with one of the highest risks of C. difficile colitis; and chloramphenicol, which reaches nearly everything and the brain, now kept for eye drops and a few grave infections because of what it does to the marrow.
- Linezolid and other protein synthesis inhibitorsLinezolid and tedizolid, as good by mouth as by drip, for MRSA, and linezolid for vancomycin-resistant enterococci too, with the blood count and serotonin to watch; the rarely used quinupristin–dalfopristin and lefamulin; and mupirocin and fusidic acid, mostly for the skin and the nose.
Synthetic chemotherapeutics
- 77SulfonamidesThe first drugs to cure a wide range of bacterial infections inside the body, which starve bacteria of folate. A sulfonamide and trimethoprim block two steps of one pathway, together, as co-trimoxazole, the first choice against Pneumocystis, and trimethoprim alone treats cystitis.
- 78QuinolonesSynthetic antibiotics that kill bacteria by trapping their topoisomerases on DNA they have cut. Well absorbed by mouth, they reach gram-negatives, Pseudomonas among them, and the newer ones pneumococci and tuberculosis, but Europe now restricts them, and the UK keeps them for when other antibiotics won't do, for rare harms that can last for good.
- Nitrofurantoin, daptomycin, polymyxins and other antibacterialsAntibiotics with a place of their own. Nitrofurantoin, nitroxoline and methenamine work only in the urine, for cystitis; daptomycin and the polymyxins break bacterial membranes, for MRSA and for gram-negatives that resist almost everything else; rifaximin and fidaxomicin stay in the gut, for travellers' diarrhoea, hepatic encephalopathy and C. difficile.
- 79Antituberculosis drugs. Antileprosy drugsDrugs given several at a time, for months. Rifampicin, isoniazid, pyrazinamide and ethambutol cure most tuberculosis in six months; regimens built on bedaquiline and linezolid now cure most strains that resist rifampicin in six months too; and rifampicin, dapsone and clofazimine cure leprosy. The liver, the eyes, the nerves and the patient's other medicines need watching throughout.
- 80Antimycotics (antifungal drugs)Not written yet
- 81Antiviral drugsNot written yet
- 82Antiprotozoal drugsNot written yet
- 83Antihelminthic drugsNot written yet
- 84Antiseptics and disinfectantsNot written yet
- 85Antitumor chemotherapeuticalsNot written yet
- 86Hormonal antitumor drugs. Targeted antitumor drugsNot written yet
- 87ImmunomodulatorsNot written yet