Prednisone Pharmacokinetics During Pregnancy and Lactation.

Prednisone Pharmacokinetics During Pregnancy and Lactation. - 2018

Available online from MWHC library: 1999 - present, Available in print through MWHC library: 1999 - 2006

Copyright (c) 2018, The American College of Clinical Pharmacology. 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.


English

0091-2700

10.1002/jcph.1122 [doi]


*Glucocorticoids/pk [Pharmacokinetics]
*Lactation
*Prednisone/pk [Pharmacokinetics]
Area Under Curve
Female
Glucocorticoids/ad [Administration & Dosage]
Glucocorticoids/bl [Blood]
Half-Life
Humans
Postpartum Period
Prednisone/ad [Administration & Dosage]
Prednisone/bl [Blood]
Pregnancy


MedStar Health Research Institute


Journal Article

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