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CHAPTER 2-9: ANTIBACTERIAL AGENTS

Conan MacDougall

INTRODUCTION

The antibacterial group 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
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TABLE II–4. ANTIBACTERIAL DRUGS
Drug Half-lifea Toxic Dose or Serum Level Toxicity

Aminoglycosides

 Amikacin

 Gentamicin

 Kanamycin

 Neomycin

 Streptomycin

 Tobramycin

 

2–3 h

2 h

2–3 h

 

2.5 h

2–2.5 h

 

Varies

Varies

>30 mg/L

0.5–1 g/d

>40–50 mg/L

Varies

 Toxic 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, dosage schedule, treatment duration, and sampling time.
Antimycobacterials     Used for treatment of tuberculosis and other mycobacterial infections
 Bedaquiline 4–5 mo Unknown QT prolongation, hepatotoxicity
 Ethambutol 4 h Chronic; 15 mg/kg/d and up Optic neuritis, red-green color blindness, peripheral neuropathy. Risk of ocular adverse effects increases with dose: 1% at 15 mg/kg/d, 5% at 25 mg/kg/d, 18% at 35 mg/kg/d.
 Ethionamide 1.92 ± 0.27 h GI intolerance acute; other effects chronic Severe nausea/vomiting, hepatitis, hypothyroidism, hypoglycemia, photosensitivity, neurotoxic effects
 Isoniazid (INH) 0.5–4 h 1–2 g orally Convulsions, metabolic acidosis, hypotension, acute hepatic failure; hepatotoxicity and peripheral neuropathy with chronic use
 Pyrazinamide 9–10 h 40–50 mg/kg/d for prolonged period Hepatotoxicity, hyperuricemia
 Rifampin, rifabutin, rifapentine 1.5–5 h, 36 h, 13 h 100 mg/kg/d (fatal exposures at 14–60 g) All patients will develop harmless red discoloration of urine, sweat, and tears. With acute exposure, abdominal pain, vomiting and diarrhea (may be red), facial edema, pruritus. Severe toxicity includes acute hepatic failure, seizures, cardiac arrest. Antibiotics of rifamycin class are inducers of hepatic cytochrome P450 enzymes, especially CYP3A4.
Bacitracin   Unknown Minimal enteric systemic absorption; if administered parenterally or absorbed via breaks in skin, ototoxicity and nephrotoxicity
Carbapenems     Hypersensitivity reactions; seizures associated with renal dysfunction and high doses
 Doripenem 1 h Chronic  
 Ertapenem 4 h (2.5 h in ages 3 mo–12 y) Chronic  
 Imipenems/cilastatin 1 h Acute: >1 g every 6 h; Chronic Highest seizure risk for imipenem
 Meropenem 1 h Chronic  
Cephalosporins     Hypersensitivity reactions; convulsions reported in patients with renal insufficiency and excessive doses

 Cefazolin

 Cephalothin

 90–120 min Unknown Coagulopathy associated with cefazolin
 Cefaclor 0.6–0.9 h Chronic Neutropenia

 Cefoperazone

 Cefamandole

 Cefotetan

 Moxalactam

 Cefmetazole

102–156 min

30–60 min

3–4.6 h

114–150 min

72 min

 3–4 mg/L One case of symptomatic hepatitis. All these antibiotics have the N-methylthiotetrazole side chain, which may inhibit aldehyde dehydrogenase to cause a disulfiram-like interaction with ethanol (Disulfiram) and coagulopathy (inhibition of vitamin K production).
 Ceftriaxone 4.3–4.6 h; extensive excretion in bile IV bolus over ...

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