Abstract

CLINICAL PHARMACOLOGY OF TETRACYCLINES IN CHILDREN

Gian Maria Pacifici

ABSTRACT

Tetracyclines used in children are doxycycline, demeclocycline, tetracycline, and minocycline. Tetracyclines inhibit bacterial protein synthesis by binding to the 30S bacterial ribosome and prevent access of aminoacyl tRNA to the acceptor (A) on the mRNA-ribosome complex. These drugs enter gram-negative bacteria by passive diffusion through channels formed by porins in the outer cell membrane and by active transport that pumps tetracyclines across the cytoplasmic membrane. Tetracyclines are bacteriostatic with activity against a wide range of bacteria and are more active against gram- positive than gram-negative organisms. Tetracyclines are active against Streptococcus pneumonia, penicillin-susceptible Staphylococcus aureus, Bacillus anthraces, listeria monocytogenes, Brucella, Burkholderia pseudomallei (the cause of melioidosis), Brucella species, Haemophilus ducreyi (cancroid), Vibrio cholera, Vibrio vulnificus, Campylobacter jejuni, Helicobacter pylori, Yersinia species, Francisella tularensis, Rickettsia, Coxiella burnetii, Mycoplasma pneumonia, Chlamydia species, Legionella species, Ureaplasma, atypical mycobacteria, Borrelia recurrentis, Borrelia burgdorferi (Lyme disease), Treponema pallidum (syphilis) and Treponema pertenue. Tetracyclines are not used in infants. Doxycycline is the most important tetracycline and has been investigated more extensively than the other tetracyclines. Doxycycline has been used to treat acute exacerbation of bronchiectasis, acne, syphilis, genital chlamydia infection, pelvic inflammatory disease, Lyme diseases, anthrax, malaria, periodontitis, and Rocky Mountain spotted fever. Tetracyclines are rapidly absorbed after oral administration and the time to reach the peak plasma concentration ranges from 1 to 4 hours. The aim of this study is to review the dosing, efficacy and safety, pharmacokinetics, effects, interaction with drugs, adverse-effects, prophylaxis, treatment, penetration into the cerebrospinal fluid, and treatment of meningitis with tetracyclines.

Keywords: adverse-effects, cerebrospinal-fluid, dosing, drug-interactions, effects, efficacy-safety, meningitis, pharmacokinetics, prophylaxis, tetracyclines, treatment.