Antibiotics (overview)

Overview of commonly used antibiotics in internal medicine (varies n. H. Hof 2019)

Beta-lactam antibiotics (antibiotics with inhibition of bacterial cell wall synthesis, all characterized by a common structural feature-a beta-lactam ring)

Penicillins

Classical penicillins (effective against Gram-positive germs and Gram-negative cocci and even Pasteurella multocida; not effective against penicillinase-active staphylococci; Haemophilus species and all other Gram-negative rod bacteria).

• Penicillin G (depot form = benzathine penicillin G)
• penicillin V
• Phenoxymethylpenicillin (acid stable)

Penicillinase-solid penicillins (drug of choice against staphylococci; not effective against hospital staphylococci (MRSA); contraindication: severe renal insufficiency)

• Methicillin
• Oxacillin
• Flucloxacillin

Aminopenicillins (effective against some gram-positive bacteria and against some enterobacterales; not penicillinase-resistant, allergenic)

• Ampicillin
• Amoxicillin
• Mecillinam

Acylureidopenicillins (effective especially against many enterobacterales and pseudomonads; good penetration through cell wall; not penicillinase-resistant)

• Mezlocillin
• Piperacillin

Cephalosporins (all cephalosporins have a gap for enterococci!)

• 1st generation cephalosporins (well effective against staphylococci and streptococci, weak against Haemophilus, E. coli, Klebsiella; penicillinase-resistant, sensitive to cephalosporinases; cefazolin only i. v.)
  • Cefaclor
  • Cefalexin
  • Cefadroxil
  • Cefazolin and others
• Cephalosporins 2nd generation (improved effect against gram-negative germs compared to 1st generation; stable against penicillinase and many cephalosporinases)
  • Cefuroxime
  • Cefotiam
• Cephalosporins 3rd generation (very broad spectrum of activity with good effect against gram-negative bacteria, but weaker effect against gram-positive germs compared to 1st and 2nd generation)
  • Cefpodoxime
  • Ceftibuten
  • Cefixime
• Cephalosporins 3a. Generation (very broad spectrum of activity with good effect against gram-negative bacteria, but weaker effect against gram-positive germs compared to 1st and 2nd generation; only i.v. administration)
  • Cefotaxime
  • Ceftriaxone
• Cephalosporins 3b. Generation (strikingly good activity against P. aeruginosa; i.v. administration only)
  • Ceftazidime
• Cephalosporins 4th generation (very broad spectrum of activity with good effect against gram-negative bacteria, but weaker effect against gram-positive germs compared to 1st and 2nd generation; better against P. aeruginosa)
  • Cefepime
  • Cefpirome
• Cephalosporins 5th generation (good effect against anaerobes)
  • Cefoxitin
  • Ceftaroline
  • Ceftobiprole
  • Note: Ceftaroline and ceftobiprole are effective against MRSA.

Penems (often effective against germs resistant to cephalosporins; inactivation of imipenem by renal enzymes (application together with cilastatin, an enzyme inhibitor)

• Imipenem
• Meropenem
• Ertapenem

Monobactams (enterobacterials, not effective against gram-positive bacteria)

• Aztreonam

Oxalactams (inhibitor of beta-lactamases; has very low antibacterial activity itself; combination with amoxicillin and other penicillin derivatives; susceptible to spontaneous hydrolysis (do not let prepared solutions stand for long)

• Clavulanic acid
• Sulbactam
• Tazobactam

Other antibiotics with disruption of bacterial cell wall synthesis and the cytoplasmic membrane

Glycopeptides (only gram-positive bacteria; ototoxicity, nephrotoxicity)

• Vancomycin
• Teicoplanin
• Dalbavancin

Lipopeptides (Gram-positive bacteria only; bactericidal; good tissue penetration; inhibited by surfactant)

• Daptomycin
• Fosfomycin (limited spectrum; good penetration ability)
• Polypeptides
• Bacitracin (gram-positive bacteria; not suitable for system therapy)
• Polymyxin B (gram-negative rods; reserved for special situations; neuro- and nephrotoxicity; rapid development of resistance)
• Colistin (gram-negative rods; reserved for special situations; neuro- and nephrotoxicity; rapid development of resistance)

Ethambutol (tubercle bacilli, neurotoxic)

Antibiotics with inhibition of bacterial protein synthesis

Aminoglycosides

• Streptomycin (tuberclebacilli; frequent resistance; neurotoxicity; nephrotoxicity; ototoxicity)
• Gentamicin (broad activity, many gram-positive and gram-negative bacteria; no activity against anaerobes, streptococci, and enterococci (as single agent); caveat: contraindicated in 1st trimester pregnancy, neonates, and severe renal insufficiency)
• Tobramycin (broad activity, many Gram-positive and Gram-negative bacteria; no activity against anaerobes, streptococci and enterococci (as a single agent); caution: contraindicated in 1st trimester pregnancy, neonates and severe renal insufficiency)
• Amikacin (broad activity, many Gram-positive and Gram-negative bacteria; no activity against anaerobes, streptococci and enterococci (as a single agent); caution: contraindicated in 1st trimester pregnancy, neonates and severe renal insufficiency)
• Netilmicin (broad activity, many Gram-positive and Gram-negative bacteria; no activity against anaerobes, streptococci and enterococci (as a single agent); caution: contraindicated in 1st trimester pregnancy, neonates and severe renal insufficiency)
• Neomycin (broad activity, many gram-positive and gram-negative aerobic bacteria; topical and oral use)
• Paromomycin (broad activity, many Gram-positive and Gram-negative aerobic bacteria; topical and oral use; not absorbed after oral administration, oral for reduction of intestinal flora, for eradication of Entamoeba histolyticum)
• Kanamycin (broad activity, many gram-positive and gram-negative aerobic bacteria; topical and oral use)
• Spectinomycin (penicillinase-positive gonococci; currently not commercially available)
• Framycetin (only available as topical, ointment or powder)

Macrolides

Macrolides (also effective against intracellular bacteria; ineffective against enterobacterales; erythromycin increases motility of upper intestinal segments; the newer derivatives no longer have these side effects).

• Erythromycin
• Roxithromycin
• Clarithromycin
• Azithromycin

Lincosamide

Lincomycins (gram-positive aerobes and anaerobes as well as gram-negative anaerobes; increasing resistance; caution: good penetration into bone tissue. Watch out for possible development of pseudomembranous enterocolitis!)

• Lincomycin
• Clindamycin

Tetracyclines

Tetracyclines (Occasional resistance; deposition in deciduous teeth and bones; Cave: contraindicated in 1st trimester pregnancy, children and severe renal insufficiency)

• Tetracycline
• Oxytetracycline
• Doxycycline
• Minocycline
• Glycylcycline

Rifamycins (gram-positive pathogens, mycobacteria; also effective against intracellular bacteria and in biofilm)

• Rifampicin
• Rifabutin

Oxazolidinones (all gram-positive bacteria without exception; ADR: thrombocytopenia)

• Linezolid
• Tedizolid

Fusidic acid (Gram-positive bacteria; rapid development of resistance)

Hydroquinoline (Escherichia coli, other pathogens of urinary tract infections; ineffective against Pseudomonas; also effective against Candida spp.; effective against germs in biofilm)

• Nitroxoline

Antibiotics with disruption of folic acid synthesis and various other enzyme functions in the bacterial cell

Sulfonamides (effective against streptococci, pneumococci, actinomycetes, nocardia; frequent resistance; caution: contraindicated in pregnancy 1st trimester, newborns and severe renal insufficiency; allergy)

• Sulfanilamide
• Sulfamethoxazole
• sulfadiazine and others

Diaminopyrimidines (very broad spectrum; not effective against anaerobes, rickettsiae, chlamydiae, mycoplasma; also effective against the fungus Pneumocystis

• diaminopyrimidine/sulfamethoxazole
• Trimethoprim
• Cotrimoxazole

Paraaminosalicylic acid (tubercle bacilli)

• PAS

Nitrofurans (urinary tract infections; caution: contraindicated in pregnancy 1st trimester, neonates and severe renal insufficiency as well as in old age; neurotoxic, allergenic)

• Nitrofurantoin
• nitrofurazone and others

Isonicotinamide (tubercle bacilli; neurotoxic)

• Isoniazid (INH)

Antibiotics with effect on bacterial DNA

Nitroimidazole (strict action on anaerobes and various protozoa; caution: contraindicated in pregnancy, 1st trimester, alcohol consumption)

• Metronidazole

Quinolones (gyrase inhibitors)

• Quinolones 1st generation (gram-negative rods)
  • Nalidixic acid
  • Norfloxacin
• Quinolones 2nd generation (systemic infections with enterobacterales. Very effective against meningococci, also for prophylaxis; moderate effect against pseudomonads)
  • Ciprofloxacin (systemic infections with enterobacterales. Very effective against meningococci, also for prophylaxis; moderate effect against pseudomonads; ciprofloxacin is partly excreted via the intestine. Also high concentrations in secretions, e.g. ELF (epithelial lining fluid).
• Quinolones 3rd generation
  • Levofloxacin (quite good effect against gram-positive cocci; also against chlamydiae and mycoplasma; mainly excreted renally; also high concentrations in secretions)
• Quinolones 4th generation (quite good effect against gram-positive cocci; also against chlamydiae, mycoplasmas and anaerobes, is excreted to a large extent via the intestine; acts against the anaerobes of the intestinal flora; also high concentrations in secretions)
  • Moxifloxacin

1. Hof H et al. (2019) In: Hof H, Schlüter D, Dörries R, Duale Reihe Medizinische Mikrobiologie. 7th, completely revised and extended edition. Stuttgart: Thieme p.305-307