Quinapril and its metabolite quinaprilat in human milk

Aims  To measure the milk to plasma ratio (M/P) of quinapril and its active metabolite quinaprilat in lactating mothers and to assess likely infant exposure. Methods  A single dose of quinapril 20 mg was administered to six healthy mothers who had been breastfeeding their infants for at least 2 week...

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Bibliographic Details
Published in:British journal of clinical pharmacology 2001-05, Vol.51 (5), p.478-481
Main Authors: Begg, E. J., Robson, R. A., Gardiner, S. J., Hudson, L. J., Reece, P. A., Olson, S. C., Posvar, E. L., Sedman, A. J.
Format: Article
Language:English
Subjects:
Adolescent
Adult
Angiotensin-Converting Enzyme Inhibitors - metabolism
Angiotensin-Converting Enzyme Inhibitors - pharmacokinetics
Antihypertensive agents
Biological and medical sciences
Breast Feeding
Cardiovascular system
Female
Humans
Isoquinolines - blood
Isoquinolines - metabolism
Isoquinolines - pharmacokinetics
Medical sciences
Middle Aged
milk
Milk, Human - chemistry
Milk, Human - metabolism
pharmacokinetics
Pharmacology. Drug treatments
Quinapril
quinaprilat
Short Reports
Tetrahydroisoquinolines
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Summary:Aims  To measure the milk to plasma ratio (M/P) of quinapril and its active metabolite quinaprilat in lactating mothers and to assess likely infant exposure. Methods  A single dose of quinapril 20 mg was administered to six healthy mothers who had been breastfeeding their infants for at least 2 weeks. Blood was sampled for the measurement of quinapril and quinaprilat at 0, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h. Milk was collected for measurement of quinapril and quinaprilat concentrations over the periods −4–0, 0–4, 4–8, 8–12, 12–18, 18–24 h. The areas under the plasma and milk concentration‐time curves were estimated and an M/P ratio derived for both quinapril and quinaprilat. Results  The M/P ratio for quinapril was 0.12 (95% CI 0.09,0.14). No quinapril was detected in milk after 4 h. No quinaprilat was detected in any of the milk samples. The estimated ‘dose’ of quinapril that would be received by the infant was 1.6% (95% CI 1.0,2.2) of the maternal dose, adjusted for respective weights. Conclusions  Quinapril appears to be ‘safe’ during breastfeeding according to conventional criteria, although as always, the risk:benefit ratio should be considered when it is to be given to a nursing mother.
ISSN:0306-5251
1365-2125
DOI:10.1046/j.1365-2125.2001.01327.x