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Amiodarone Pharmacokinetics in Rats

This document presents pharmacokinetic parameters from studies comparing control groups and groups given oral lipid-based amiodarone formulations in rats. The key findings were: - Groups given oral lipid-based amiodarone had significantly higher AUC values for both amiodarone and its metabolite desethylamiodarone compared to control groups, indicating higher bioavailability when given with oral lipid. - Half-life values were similar between groups while clearance was lower and Cmax and Tmax values significantly higher for oral lipid groups compared to controls for both compounds. - A separate study found common side effects of oral amiodarone administration in rats included weakness, piloerection, decreased food intake, weight

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3 views4 pages

Amiodarone Pharmacokinetics in Rats

This document presents pharmacokinetic parameters from studies comparing control groups and groups given oral lipid-based amiodarone formulations in rats. The key findings were: - Groups given oral lipid-based amiodarone had significantly higher AUC values for both amiodarone and its metabolite desethylamiodarone compared to control groups, indicating higher bioavailability when given with oral lipid. - Half-life values were similar between groups while clearance was lower and Cmax and Tmax values significantly higher for oral lipid groups compared to controls for both compounds. - A separate study found common side effects of oral amiodarone administration in rats included weakness, piloerection, decreased food intake, weight

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chiru
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PK parameters

Group D (Control)
(n=6)

Group E (Oral lipid)


(n=6)

AUC0-24 h(mg-h/l)

6.95 +/-1.73
(5.369.17)

14.9 +/-3.11
(10.218.8)

14.3 _5.06
(8.1122.0)

26.1 _6.61
(17.133.9)

49.1 _28.0
(20.795.5)
ND

103 _83.7
(17.5254)
ND

ND

ND

662 +/-301
(317991)

1776 +/-759
(8282903)

8.09 +/-8.51
(2.0723.9)

5.73 +/-2.57
(2.9310)

52.0 +/-36.6

32.7 +/-34.8

9.13 +/-8.00

7.09 +/-2.44

12.6 +/-2.42 (8.4015.5)

AUC0- (mg-h/l)
20.3 +/-7.98 (11.835.8)

T1/2 (h)
44.0 _16.5 (26.074.8)

CL (ml/h/kg)
1378+/-465 (698-2121)

Vd (l/kg)
47.0 +/-14.9 (28.2-70.0)

Cmax (ng/ml)
ND
Tmax (h)
ND
Desethylamiodarone
Cmax (ng/ml)
135 +/-158

Tmax (h)
0.801 +/-1.30

Pk
Oral (50 mg/kg amiodarone HCl) (ref G)

PK

Amiodaron Amiodaron Desethylamiodaron


e
e
e
Control
Control
Oral lipid

Desethylamiodarone
Oral lipid

1967 611*
AUC0-24
h(ng- h Ml
1
)

5431 994

167 56*

681 253

AUC0- ng- 2893 666*


h ml-1)
16.20 9.98
T1/2 (h)

6892 897

322 191*

2481 1579

22.40 4.16

23.8 10.3

50.6 24.6

234 66*

731 209

16.80 7.76*

102.0 48.7

3.20 0.41*

5.4 2.0

3.5 2.5

54

Cmax (ng
ml-1)
Tmax (h)
)

*P < 0.05, compared with oral lipid.

Pharmacokinetic parameters after a single 10-mg kg-1 oral dose of amiodarone with and without
oral lipid (1% cholesterol in peanut oil) (ref C)

Side effects of amiodarone


Adverse effects of oral amiodarone administration in rats are:
-weakness.
-Piloerection,
- decreased food intake,
-weight loss and
-mortality (Nearly 50%).
Ref I
[Link],[Link],[Link],[Link],[Link],[Link],*[Link],R.B
oeri,[Link] , R. LATINI. Amiodarone induced phospholipidosis
biochemical, morphological and functional changes in the lungs of rats
chronically treated with Amiordarone, 1987 .(36): 3209-3214.)

[Link]

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