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Prednisone Pharmacokinetics During Pregnancy and Lactation
Author(s) -
Ryu Rachel J.,
Easterling Thomas R.,
Caritis Steve N.,
Venkataramanan Raman,
Umans Jason G.,
Ahmed Mahmoud S.,
Clark Shan,
KantrowitzGordon Ira,
Hays Karen,
Bennett Brooke,
Honaker Matthew T.,
Thummel Kenneth E.,
Shen Danny D.,
Hebert Mary F.
Publication year - 2018
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/jcph.1122
Subject(s) - pharmacokinetics , lactation , prednisone , pregnancy , medicine , obstetrics , pharmacology , physiology , biology , genetics
To evaluate the steady‐state pharmacokinetics of prednisone and its metabolite prednisolone in pregnant and lactating female subjects, 19 subjects received prednisone (4‐40 mg/day orally) in early (n = 3), mid (n = 9), and late (n = 13) pregnancy as well as postpartum with (n = 2) and without (n = 5) lactation. Serial blood and urine samples were collected over 1 dosing interval. Prednisone and its metabolite, prednisolone, steady‐state noncompartmental pharmacokinetic parameters were estimated. During pregnancy, prednisone apparent oral clearance increased with dose (35.1 ± 11.4 L/h with 5 mg, 52.6 ± 5.2 L/h with 10 mg, and 64.3 ± 6.9 L/h with 20 mg, P  = .001). Similarly, unbound prednisone apparent oral clearance increased with dose. In addition, prednisolone renal clearance increased with dose (0.3 ± 0.3 L/h with 5 mg, 0.5 ± 0.4 L/h with 10 mg, and 1.3 ± 1.1 L/h with 20 mg, P  = .002). Higher prednisone (r = 0.57, P ≤ .05) and prednisolone (r = 0.75, P ≤ .05) concentrations led to a higher percentage of unbound drug. Breast‐milk/plasma area under the concentration‐time curve ratios were 0.5‐0.6 for prednisone and 0.02‐0.03 for prednisolone. Relative infant doses were 0.35% to 0.53% and 0.09% to 0.18%, for prednisone and prednisolone, respectively. Prednisone and prednisolone exhibit dose‐ and concentration‐dependent pharmacokinetics during pregnancy, and infant exposure to these agents via breast milk is minimal.

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