Pharmacology · Antimicrobials (Cell Wall Inhibitors, Protein Synthesis Inhibitors, Fluoroquinolones)

A 22-year-old receives intramuscular benzathine penicillin G 2.4 million units for early syphilis. The property of this formulation that permits single-dose therapy is:

  • A Very low solubility producing slow release and detectable serum concentrations for weeks
  • B Resistance to degradation by penicillinase allowing prolonged plasma levels
  • C Irreversible binding to serum proteins creating a depot reservoir
  • D Active uptake and storage within macrophages at the injection site
Correct answer: A. Very low solubility producing slow release and detectable serum concentrations for weeks

Explanation

Benzathine penicillin G is a poorly water-soluble salt of penicillin G with dibenzylethylenediamine. After deep intramuscular injection it dissolves slowly, maintaining low but treponemicidal plasma concentrations for 2 to 4 weeks. This repository property underlies its use in syphilis and rheumatic fever prophylaxis. Treponema pallidum remains exquisitely sensitive rather than the drug being penicillinase resistant, killing option B.

Reference: Katzung Basic and Clinical Pharmacology, 16th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.

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