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Chapter 2: Antimicrobial Medications

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TERMS TO LEARN

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Blackwater Fever Syndrome of hemolytic anemia, hemoglobinuria, and renal failure associated with massive parasitemia.
Cinchonism Poisoning syndrome associated with quinine, quinidine, and Cinchona; symptoms include tinnitus, deafness, headache, blurry vision, and nausea.
Disulfiram Reaction Syndrome that occurs due to coingestion of alcohol and disulfiram; disulfiram blocks aldehyde dehydrogenase, leading to accumulation of acetaldehyde; symptoms include nausea, headache, flushing, and hypotension.
G6PD Deficiency Lack of enzyme important in the oxidation/reduction capabilities of the red blood cell; deficiency leads to hydrogen peroxide accumulation, which causes hemolysis. Hemolysis often associated with drugs that produce oxidative stress (eg, sulfonamides).
Gray Baby Syndrome May be caused by deficiency of a hepatic enzyme required for the degradation of chloramphenicol or impaired renal function; syndrome is characterized by circulatory collapse, cyanosis (gray color), acidosis, abdominal distention, coma, and death.
Lassa Fever A hemorrhage febrile illness associated with arenavirus infection.
Mazzotti Reaction Syndrome of fever, urticaria, tender lymphadenopathy, arthralgias, abdominal pain, edema, hypotension, and tachycardia seen with treatment of microfilariasis with Ivermectin, Praziquantel, and Albendazole.
Methemoglobinemia Accumulation of methemoglobin, which is a form of hemoglobin with a low oxygen affinity. Methemoglobinemia results in pseudocyanosis, tissue hypoxia, and death.
Stevens-Johnson Syndrome Immunologic reaction characterized by lesions of the skin and mucous membranes; involves both the mouth and eyes.
Superinfection A novel infection in addition to a pre-existing one.
Trachoma Chronic inflammation of the conjunctiva caused by Chlamydia trachomatis.

I. CELL WALL SYNTHESIS INHIBITORS

ANTIBIOTIC MECHANISMS OF ACTION

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SUMMARY OF PENICILLINS

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Types Class Pharmacokinetics Mechanisms of Action and of Resistance Clinical Uses and Spectrum of Activity Drawbacks and Side Effects
Penicillin G and penicillin V

  • Derivatives of 6-aminopenicillanic acid

  • Contain a β-lactam ring

  • A: PO absorption inhibited by coingestion with meals

  • M: Polar compounds, so not extensively metabolized

  • E: Most are excreted in urine via glomerular filtration and tubular secretion; prolong effects by administration with Probenecid, which blocks tubular secretion

MOA:

  • Bactericidal

  • Inhibit cell wall synthesis by these three steps:

    1. Bind drug to specific receptors in the bacterial cell wall

    2. Inhibit transpeptidase enzymes that cross-link linear peptidoglycan chains that form bacterial cell walls

    3. Activate autolytic enzymes causing lesions in the bacterial cell wall

Resistance:

  • β-Lactamase produced by bacteria causes enzymatic hydrolysis of the β-lactam ring, which results in loss of antibacterial activity

  • Narrow spectrum

  • β-Lactamase susceptible

  • Streptococci, meningococci, G+ bacilli, spirochetes

  • Most staphylococci are drug resistant

Allergic reactions:

  • Ranges from urticaria to hemolytic anemia and anaphylaxis

  • Assume cross-reactivity throughout class

  • 10% of persons who are allergic to penicillin are also allergic to cephalosporins

GI disturbances:

  • Nausea and diarrhea caused by oral medications via direct irritation or overgrowth of G+ organisms or yeast

    ...

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