Antibiotics (overview)

Overview of common antibiotics in internal medicine (varies according to Hof 2019)

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

Penicillin

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-resistant penicillins (agent 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 enterobacteria; not penicillinase resistant, allergenic)

• Ampicillin
• Amoxicillin
• Mecillinam

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

• Mezlocillin
• Piperacillin

Cephalosporins (all cephalosporins have a gap in enterococci!)

• 1st generation cephalosporins (good effect on staphylococci and streptococci, weak against Haemophilus, E. coli, Klebsiella; penicillinase-resistant, sensitive to cephalosporinases; cefazolin only i. v.)
  • Cefaclor
  • Cefalexin
  • Cefadroxil
  • Cefazolin and others
• 2nd generation cephalosporins (compared to 1st generation improved effect against gram-negative germs; stable against penicillinase and many cephalosporinases)
  • Cefuroxime
  • Cefotiam
• 3rd generation cephalosporins (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
  • Cefixim
• Cephalosporins 3a. (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 (remarkably good activity against P. aeruginosa; only i. v. administration)
  • Ceftazidim
• 4th generation cephalosporins (very broad spectrum of activity with good effect against Gram-negative bacteria, but in comparison to 1st and 2nd generation weaker effect against Gram-positive bacteria; better against P. aeruginosa)
  • Cefepime
  • Cefpirome
• Cephalosporins 5th generation (good effect against anaerobes)
  • Cefoxitin
  • Ceftarolin
  • Ceftobiprole
  • Note: Ceftarolin and Ceftobiprole are effective against MRSA

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

• Imipenem
• Meropenem
• Ertapenem

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

• Aztreonam

Oxalactame (inhibitor of betalactamases; has very little antibacterial activity itself; combination with amoxicillin and other penicillin derivatives; susceptible to spontaneous hydrolysis (do not allow prepared solutions to 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 (only gram-positive bacteria; bactericidal; good tissue penetration; is inhibited by surfactant)

• Daptomycin
• Fosfomycin (limited spectrum; good penetration ability)
• polypeptides
• Bacitracin (gram-positive bacteria; not suitable for systemic 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 bacteria, neurotoxic)

Antibiotics with inhibition of bacterial protein synthesis

Aminoglycosides

• Streptomycin (tubercle bacteria; frequent resistances; neurotoxicity; nephrotoxicity; ototoxicity)
• Gentamicin (broad activity, many Gram-positive and Gram-negative bacteria; no effect against anaerobes, streptococci and enterococci (as single substance); Cave: contraindicated in 1st trimester pregnancy, newborns and severe renal failure)
• Tobramycin (broad activity, many Gram-positive and Gram-negative bacteria; no effect against anaerobes, streptococci and enterococci (as single substance); Cave: contraindicated in 1st trimester pregnancy, newborns and severe renal failure)
• Amikacin (broad activity, many Gram-positive and Gram-negative bacteria; no effect against anaerobes, streptococci and enterococci (as single substance); Cave: contraindicated in 1st trimester pregnancy, newborns and severe renal failure)
• Netilmicin (broad activity, many Gram-positive and Gram-negative bacteria; no effect against anaerobes, streptococci and enterococci (as single substance); Cave: contraindicated in 1st trimester pregnancy, newborns and severe renal failure)
• Neomycin (broad activity, many Gram-positive and Gram-negative aerobic bacteria; topical and oral application)
• Paromomycin (broad efficacy, many Gram-positive and Gram-negative aerobic bacteria; topical and oral application; is not absorbed after oral administration, orally to reduce intestinal flora, for eradication of Entamoeba histolyticum)
• Kanamycin (broad activity, many Gram-positive and Gram-negative aerobic bacteria; topical and oral application)
• Spectinomycin (penicillinase-positive gonococci; currently not commercially available)
• Framycetin (only available as a topical agent, ointment or powder)

Macrolides

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

• Erythromycin
• Roxithromycin
• Clarithromycin
• Azithromycin

Lincosamides

Lincomycins (Gram-positive aerobes and anaerobes and Gram-negative anaerobes; increasing resistance; Cave: Good penetration into bone tissue. Pay attention to the possible development of pseudomembranous enterocolitis).

• Lincomycin
• Clindamycin

Tetracyclines

tetracyclines (occasional resistance; deposition in the milk teeth and bones; Cave: contraindicated in 1st trimester pregnancy, children and severe renal failure)

• Tetracycline
• Oxytetracycline
• Doxycycline
• Minocycline
• Glycylcycline

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

• Rifampicin
• Rifabutin

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

• Linezolid
• Tedizolide

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

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

• Nitroxolin

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

sulfonamides (effective against streptococci, pneumococci, actinomycetes, nocardia; frequent resistances; Cave: contraindicated in pregnancy 1st trimester, newborns and severe renal failure; allergy)

• Sulfanilamide
• Sulfamethoxazole
• sulfadiazine and others

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

• diaminopyrimidine/sulfamethoxazole
• Trimethoprim
• Cotrimoxazole

paraaminosalicylic acid (tubercle bacteria)

• PAS

Nitrofurans (urinary tract infections; Cave: contraindicated in 1st trimester pregnancy, newborns and severe renal failure and in old age; neurotoxic, allergenic)

• Nitrofurantoin
• Nitrofurazone and others

Isonicotinamide (tubercle bacteria; neurotoxic)

• Isoniazid (INH)

Antibiotics with effect on bacterial DNA

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

• Metronidazole

Quinolones

• Quinolones 1st generation (gram negative rods)
  • Nalidixic acid
  • norfloxacin
• Chinolone 2nd generation (systemic infections with Enterobacteriales. Very effective against meningococci also for prophylaxis; moderate effect against pseudomonads)
  • Ciprofloxacin (systemic infections with Enterobacteriales. 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 chlamydia and mycoplasma; is mainly excreted renally; also high concentrations in secretions)
• Quinolone 4th generation (quite good effect against gram-positive cocci; also against chlamydia, mycoplasma and anaerobes, is excreted to a large extent via the intestine; acts against 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