TY - JOUR
T1 - Azithromycin concentration in rabbits' plasma and posterior segment of the eyes following oral drug administration
T2 - a dose-finding study for the application in ocular toxoplasmosis
AU - Daniel, Hisar
AU - Louisa, Melva
AU - Edwar, Lukman
N1 - Publisher Copyright:
© The Author(s) 2022. Published by Oxford University Press on behalf of the Royal Pharmaceutical Society. All rights reserved. For permissions, please e-mail: [email protected].
PY - 2022/11/25
Y1 - 2022/11/25
N2 - INTRODUCTION: Azithromycin has been used as an ocular toxoplasmosis alternative treatment due to its pharmacokinetic profiles. However, sufficient concentrations to promote toxoplasmosis eradication is still unknown. This study was aimed to evaluate azithromycin levels in rabbits after three regimens equivalent to human doses for ocular toxoplasmosis. METHODS: Three groups of New Zealand albino rabbits were given one of the following: azithromycin at 26 mg/kg BW daily (Group 1), 26 mg/kg BW every two days (Group 2), and 50 mg/kg BW once weekly (Group 3) for 14 days. Plasma and ocular azithromycin concentrations were examined. RESULTS: Following 14 days, median ratio of plasma maximum azithromycin concentration to the minimum inhibitory concentration for Toxoplasma gondii (C-max/MIC) for Group 1, and 2 were 51.29, 5.33, while Group 3 was undetected. The median azithromycin concentration in the retina-choroid was higher than the MIC in Group 1 (1356.0 ng/ml) and Group 2 (189.0 ng/ml), but not in Group 3. CONCLUSION: Azithromycin administered orally at the dose of 26 mg/kg BW daily or 26 mg/kg BW every two days resulted a sufficient criteria of C-max/MIC as well as retina-choroid concentration needed for its parasiticidal activity. However, well-conducted clinical trial is warranted to support its therapeutic potential in ocular toxoplasmosis.
AB - INTRODUCTION: Azithromycin has been used as an ocular toxoplasmosis alternative treatment due to its pharmacokinetic profiles. However, sufficient concentrations to promote toxoplasmosis eradication is still unknown. This study was aimed to evaluate azithromycin levels in rabbits after three regimens equivalent to human doses for ocular toxoplasmosis. METHODS: Three groups of New Zealand albino rabbits were given one of the following: azithromycin at 26 mg/kg BW daily (Group 1), 26 mg/kg BW every two days (Group 2), and 50 mg/kg BW once weekly (Group 3) for 14 days. Plasma and ocular azithromycin concentrations were examined. RESULTS: Following 14 days, median ratio of plasma maximum azithromycin concentration to the minimum inhibitory concentration for Toxoplasma gondii (C-max/MIC) for Group 1, and 2 were 51.29, 5.33, while Group 3 was undetected. The median azithromycin concentration in the retina-choroid was higher than the MIC in Group 1 (1356.0 ng/ml) and Group 2 (189.0 ng/ml), but not in Group 3. CONCLUSION: Azithromycin administered orally at the dose of 26 mg/kg BW daily or 26 mg/kg BW every two days resulted a sufficient criteria of C-max/MIC as well as retina-choroid concentration needed for its parasiticidal activity. However, well-conducted clinical trial is warranted to support its therapeutic potential in ocular toxoplasmosis.
KW - Toxoplasma gondii
KW - Azithromycin
KW - choroid
KW - minimum inhibitory concentration
KW - retina-choroid
UR - http://www.scopus.com/inward/record.url?scp=85143181039&partnerID=8YFLogxK
U2 - 10.1093/jpp/rgac059
DO - 10.1093/jpp/rgac059
M3 - Article
C2 - 36181765
AN - SCOPUS:85143181039
SN - 0022-3573
VL - 74
SP - 1743
EP - 1748
JO - The Journal of pharmacy and pharmacology
JF - The Journal of pharmacy and pharmacology
IS - 12
ER -