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Table 3 Summary of placental transfer and mammary excretion of various angiotensin receptor blockers

From: Placental transfer and mammary excretion of a novel angiotensin receptor blocker fimasartan in rats

Disposition site

Drug

Dose (mg/kg)

Route

Gestation or Lactation day

Time after dose

Maternal

Plasma conc. (PL)

Milk (MI) or Fetus (FE) conc.

KP % (MI/PL or FE/PL)

Reference

Fetus

Losartan

135

P.O.

(Multiple)

6 ~ 15

88a (μg · hr/mL)

[17]

15 ~ 20

194.8a (μg · hr/mL)

50.7a (μg · hr/mL)

26.0

Telmisartan

1

P.O.

12

4

43.56 (ng-eq/mL)

11.83 (ng-eq/g)

27.2

[18, 21]

12

8

34.47 (ng-eq/mL)

11.03 (ng-eq/g)

32.0

12

24

5.98 (ng-eq/mL)

7.98 (ng-eq/g)

133.4

12

48

3.65 (ng-eq/mL)

1.89 (ng-eq/g)

51.8

18

4

77.05 (ng-eq/mL)

13.72 (ng-eq/g)

17.8

18

24

19.73 (ng-eq/mL)

45.27 (ng-eq/g)

229.4

18

48

9.01 (ng-eq/mL)

17.65 (ng-eq/g)

195.9

Olmesartan

P.O.

18

>100

[19]

Valsartan

600

18

1

7 ~ 9 (μg-eq/g)

4 ~ 5 (μg-eq/g)

56.0

[20]

18

24

NDb

3 ~ 4 (μg-eq/g)

Milk

Losartan

135

P.O.

(Multiple)

7

3.86 (μg/mL)

1.16 (μg/mL)

30.1

[17]

14

3.00 (μg/mL)

1.96 (μg/mL)

65.3

21

3.14 (μg/mL)

1.71 (μg/mL)

54.5

Telmisartan

1

P.O.

0.5

23.77 (ng-eq/mL)

3.32 (ng-eq/mL)

14.0

[18, 21]

2

31.04 (ng-eq/mL)

30.6 (ng-eq/mL)

98.6

4

34.84 (ng-eq/mL)

54.24 (ng-eq/mL)

155.7

8

36.12 (ng-eq/mL)

66.08 (ng-eq/mL)

182.9

24

9.3 (ng-eq/mL)

13.52 (ng-eq/mL)

145.4

48

4.06 (ng-eq/mL)

6.79 (ng-eq/mL)

167.2

Olmesartan

P.O.

72

25.0

[19]

Valsartan

600

NDb

[20]

  1. aRepresented as AUC (μg · hr/mL), b ND: Not Detected