The antibiotic class of drugs has proliferated immensely since the first clinical use of sulfonamide in 1936 and the mass production of penicillin in 1941. In general, harmful effects have resulted from allergic reactions or inadvertent intravenous overdose. Serious toxicity from a single acute ingestion is rare. Table II–4 lists common and newer antibacterial agents that have been associated with significant toxic effects.
Table II-4 Antibacterial Drugs |Favorite Table|Download (.pdf)
Table II-4 Antibacterial Drugs
Toxic Dose or Serum Level
Ototoxicity to vestibular and cochlear cells; nephrotoxicity causing proximal tubular damage and acute tubular necrosis; competitive neuromuscular blockade if given rapidly IV with other neuromuscular-blocking drugs. Threshold for toxic effects varies with the drug and dosage schedule.
Ototoxicity and nephrotoxicity
Chronic; >1 g every 6 h
Hypersensitivity reactions; seizures associated with renal dysfunction and high doses.
4 h (2.5 h in ages 3 mo–12 y)
Convulsions reported in patients with renal insufficiency; coagulopathy associated with cefazolin.
Proximal tubular necrosis
One case of symptomatic hepatitis. All these antibiotics have the N-methyltetra-zolethiol side chain, which may inhibit aldehyde dehydrogenase to cause a disulfiram-like interaction with ethanol (See Disulfiram) and coagulopathy (inhibition of vitamin K production).
4.3–4.6 h; extensive excretion in bile
IV bolus over <3–5 min
Pseudolithiasis (“gallbladder sludge”).
Should be administered IV over 30 minutes.
Leukopenia, reticulocytopenia, circulatory collapse (“gray baby” syndrome)
As little as 100 mg in an 18-month-old
Methemoglobinemia, sulfhemoglobinemia, hemolysis; metabolic acidosis; hallucinations, confusion; hepatitis (See Dapsone)
A cyclic lipopeptide. Available only as an injection. May cause muscle pain, weakness, or asymptomatic elevation of the CK level.
Optic neuritis, red-green color blindness, peripheral neuropathy
1.92 ± 0.27 h
Hypothyroid, hypoglycemia, photosensitivity, neurotoxic effects
1–2 g orally
Convulsions, metabolic acidosis (See Anion gap metabolic acidosis); hepatotoxicity and peripheral neuropathy with chronic use
Hypotension and cardiopulmonary arrest after rapid intravenous administration
Duration-related (>2 wk)
Thrombocytopenia, anemia; peripheral neuropathy. Linezolid is an inhibitor of monoamine oxidase (See Monoamine Oxidase Inhibitors).
Can prolong the QT interval and lead to torsade de pointes (atypical ventricular tachycardia).
Least likely of the macrolides to induce torsade in animal studies.
44 (16–55) h
Abdominal pain; idiosyncratic hepatotoxicity with estolate salt. Administration ...