Transplacental passage and breast milk concentrations of hydralazine

Liedholm, Hans; Wåhlin-Boll, E; Hanson, Arne; Ingemarsson, Ingemar; Melander, Arne

doi:10.1007/bf00542329

Cited by 55 publications

(17 citation statements)

References 2 publications

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“…In a recent review of progress in this area, Wilson and coworkers (1980) emphasized the lack of quantitative studies of drug distribution in human breast milk. A number of recent and more definitive studies (Findlay et al, 1981a;Liedholm et al, 1981Liedholm et al, , 1982Lonnerholm & Lindstrom, 1982;Steen & Rane, 1982) published on a variety of therapeutic drug types also reflect the rapidly growing awareness that detailed investigation of this field with the use of modern analytical techniques has been neglected until the past several years. Since a variety of drugs may be prescribed for mothers during the period of infant nursing, and because a majority of mothers now breast feed their babies for some period after birth, questions about the safety of nursing the infant while taking medication often arise in pediatric practice.…”

Section: Introductionmentioning

confidence: 99%

Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers.

Jw¹,

Butz²,

Sailstad³

et al. 1984

Brit J Clinical Pharma

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1 Plasma and milk concentrations of pseudoephedrine and triprolidine were determined (by radioimmunoassay) in three lactating mothers over 12-48 h after ingestion of a combination medication containing 60 mg of pseudoephedrine hydrochloride and 2.5 mg of triprolidine hydrochloride monohydrate. J 2 Pseudoephedrine concentrations in milk were consistently higher than those in plasma. The total amount of drug in milk, as judged by areas under the respective curves (AUC), was two to three times greater than in plasma. 3 Triprolidine concentrations in milk and plasma were more variable between subjects than those of pseudoephedrine. AUC values for milk and plasma were similar for one subject, while the plasma value exceeded that for milk in another woman. 4 The fraction of the dose excreted in milk was estimated to be 0.4-0.7% for pseudoephedrine and 0.06-0.2% for triprolidine.

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Section: Introductionmentioning

confidence: 99%

Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers.

Jw¹,

Butz²,

Sailstad³

et al. 1984

Brit J Clinical Pharma

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“…Earlier studies of hydralazine exposure during gestation were limited to blood samples collected at the time of delivery or postpartum . These studies demonstrated transplacental fetal exposure to hydralazine, with a mean umbilical cord‐to‐maternal plasma concentration ratio of 2 ± 2.5 at the time of birth.…”

mentioning

confidence: 99%

Effect of N‐Acetyltransferase 2 Genotype on the Pharmacokinetics of Hydralazine During Pregnancy

Han

Ryu

Cusumano

et al. 2019

The Journal of Clinical Pharma

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Hydralazine, an antihypertensive agent used during pregnancy, undergoes N‐acetylation primarily via N‐acetyltransferase 2 (NAT2) to form 3‐methyl‐1,2,4‐triazolo[3,4‐a]phthalazine (MTP). To characterize the steady‐state pharmacokinetics (PK) of hydralazine during pregnancy and evaluate the effects of NAT2 genotype on hydralazine and MTP PK during pregnancy, 12 pregnant subjects received oral hydralazine (5‐25 mg every 6 hours) in mid‐ (n = 5) and/or late pregnancy (n = 8). Serial blood samples were collected over 1 dosing interval, and steady‐state noncompartmental PK parameters were estimated. Subjects were classified as either (rapid acetylators, n = 6) or slow acetylators (SAs, n = 6) based on NAT2 genotype. During pregnancy, when compared with the SA group, the RA group had faster weight‐adjusted hydralazine apparent oral clearance (70.0 ± 13.6 vs 20.1 ± 6.9 L/h, P < .05), lower dose‐normalized area under the concentration‐time curve (AUC; 1.5 ± 0.8 vs 5.9 ± 3.7 ng·h/mL, P < .05), lower dose‐normalized peak concentrations (0.77 ± 0.51 vs 4.04 ± 3.18 ng/mL, P < .05), and larger weight‐adjusted apparent oral volume of distribution (302 ± 112 vs 116 ± 45 L/kg, P < .05). Furthermore, the MTP/hydralazine AUC ratio was ∼10‐fold higher in the RA group (78 ± 30 vs 8 ± 3, P < .05) than in the SA group. No gestational age or dose‐dependent effects were observed, possibly because of the small sample size. This study describes for the first time, the PK of oral hydralazine and its metabolite, MTP, during pregnancy, and confirmed that the PK of oral hydralazine is NAT2 genotype dependent during pregnancy.

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“…Reserpine may cause some adverse effects in infants (Table 4). [28][29][30][31][32][33][34] β β-BLOCKERS β-Blockers are weak bases and tend to ionize when in breast milk, which is more acidic than plasma. This ionization allows for β-blockers to accumulate in milk.…”

Section: Antihypertensive Agents (Miscellaneous)mentioning

confidence: 99%

Medications and Breast-Feeding: A Guide for Pharmacists, Pharmacy Technicians, and other Healthcare Professionals Part II

Nice

DeEugenio

DiMino

et al. 2004

Journal of Pharmacy Technology

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The following discussion of medication categories, which includes drugs used in cardiology and general practice, will help pharmacists and other healthcare professionals understand which drugs are the optimal choices within specific categories for breast-feeding mothers to take while minimizing the impact on in-fants. Ambulatory care medications and analgesics and anesthetics were discussed in Part I of this 3-part series. 1 Objective: To provide a guide for practicing pharmacists, pharmacy technicians, and other healthcare professionals so that they are able to counsel and advise breast-feeding mothers and fellow healthcare professionals on the safety and use of common cardiology and general medications during breast-feeding.Data Sources: Primary texts used by the breast-feeding community (Medications and Mothers' Milk, Drugs in Pregnancy and Lactation, Drugs and Human Lactation) were searched, as well as Micromedex, MEDLINE, PubMed, EMBASE, and EMBASE2 (1984( -February 2004. Study Selection/Data Extraction:Multiple sources were used wherever available to validate the data, and primary articles were used to verify all tertiary source information. Search terms included breast-feeding, lactation, nursing, and medications, as well as specific drug names.Data Synthesis: Concerns regarding medication use during breast-feeding have caused mothers to either discontinue nursing or not take necessary medications. Complete avoidance of medications or cessation of breast-feeding is often unnecessary. Although there are drugs that can be harmful to nursing infants, breast milk concentrations of most drugs are insufficient to cause any harm. Conclusions:Having objective and reliable information on medications enables pharmacists, pharmacy technicians, healthcare providers, and mothers to make educated decisions regarding drug therapy and breast-feeding.

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Transplacental passage and breast milk concentrations of hydralazine

Cited by 55 publications

References 2 publications

Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers.

Pseudoephedrine and triprolidine in plasma and breast milk of nursing mothers.

Effect of N‐Acetyltransferase 2 Genotype on the Pharmacokinetics of Hydralazine During Pregnancy

Medications and Breast-Feeding: A Guide for Pharmacists, Pharmacy Technicians, and other Healthcare Professionals Part II

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