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Pharmacokinetics of carbetocin, a long-acting oxytocin analogue, in nonpregnant women

Sweeney, G.; Holbrook, A. M.; Levine, M.; Yip, M.; Alfredsson, K.; Cappi, S.; Ohlin, M. LU ; Schulz, P. and Wassenaar, W. (1990) In Current Therapeutic Research - Clinical and Experimental 47(3). p.528-540
Abstract

The safety and pharmacokinetics of carbetocin, a long-acting oxytocin analogue, were studied in 25 healthy nonpregnant women. The distribution and elimination half-lives of a 0.4-mg intravenous dose were found to be 5.5 ± 1.6 minutes and 41 ± 11.9 minutes, respectively. Similarly, the half-lives of a 0.8-mg intravenous dose were found to be 6.1 ± 1.2 minutes and 42.7 ± 10.6 minutes. Approximately 0.7% of the carbetocin dose was eliminated in the unchanged form by the kidney, indicating that carbetocin, like oxytocin, is eliminated primarily by nonrenal routes. Intramuscularly (IM) administered carbetocin was found to enter the circulation rapidly, with a time to peak concentration of less than 30 minutes. The absolute bioavailability of... (More)

The safety and pharmacokinetics of carbetocin, a long-acting oxytocin analogue, were studied in 25 healthy nonpregnant women. The distribution and elimination half-lives of a 0.4-mg intravenous dose were found to be 5.5 ± 1.6 minutes and 41 ± 11.9 minutes, respectively. Similarly, the half-lives of a 0.8-mg intravenous dose were found to be 6.1 ± 1.2 minutes and 42.7 ± 10.6 minutes. Approximately 0.7% of the carbetocin dose was eliminated in the unchanged form by the kidney, indicating that carbetocin, like oxytocin, is eliminated primarily by nonrenal routes. Intramuscularly (IM) administered carbetocin was found to enter the circulation rapidly, with a time to peak concentration of less than 30 minutes. The absolute bioavailability of carbetocin injected IM was approximately 80%. Doses of carbetocin of 0.05 to 0.8 mg produced very few side effects. Included were transient facial flushing and mild transient tachycardia accompanied by a decrease in diastolic blood pressure. The increase in heart rate was significant (P <0.05) after the administration of 0.4- and 0.8-mg IM doses, while the decrease in diastolic blood pressure was significant after the 0.8-mg IM dose only. No clinically significant changes between predrug and postdrug chemistry values of hematology parameters were noted.

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publishing date
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Contribution to journal
publication status
published
subject
in
Current Therapeutic Research - Clinical and Experimental
volume
47
issue
3
pages
13 pages
publisher
Excerpta Medica
external identifiers
  • Scopus:0025285197
ISSN
0011-393X
language
English
LU publication?
no
id
5b12de1c-9f3f-43fc-9d09-6a6ed739d843
date added to LUP
2016-04-20 16:24:54
date last changed
2016-07-06 14:22:59
@misc{5b12de1c-9f3f-43fc-9d09-6a6ed739d843,
  abstract     = {<p>The safety and pharmacokinetics of carbetocin, a long-acting oxytocin analogue, were studied in 25 healthy nonpregnant women. The distribution and elimination half-lives of a 0.4-mg intravenous dose were found to be 5.5 ± 1.6 minutes and 41 ± 11.9 minutes, respectively. Similarly, the half-lives of a 0.8-mg intravenous dose were found to be 6.1 ± 1.2 minutes and 42.7 ± 10.6 minutes. Approximately 0.7% of the carbetocin dose was eliminated in the unchanged form by the kidney, indicating that carbetocin, like oxytocin, is eliminated primarily by nonrenal routes. Intramuscularly (IM) administered carbetocin was found to enter the circulation rapidly, with a time to peak concentration of less than 30 minutes. The absolute bioavailability of carbetocin injected IM was approximately 80%. Doses of carbetocin of 0.05 to 0.8 mg produced very few side effects. Included were transient facial flushing and mild transient tachycardia accompanied by a decrease in diastolic blood pressure. The increase in heart rate was significant (P &lt;0.05) after the administration of 0.4- and 0.8-mg IM doses, while the decrease in diastolic blood pressure was significant after the 0.8-mg IM dose only. No clinically significant changes between predrug and postdrug chemistry values of hematology parameters were noted.</p>},
  author       = {Sweeney, G. and Holbrook, A. M. and Levine, M. and Yip, M. and Alfredsson, K. and Cappi, S. and Ohlin, M. and Schulz, P. and Wassenaar, W.},
  issn         = {0011-393X},
  language     = {eng},
  number       = {3},
  pages        = {528--540},
  publisher    = {ARRAY(0x9f2b610)},
  series       = {Current Therapeutic Research - Clinical and Experimental},
  title        = {Pharmacokinetics of carbetocin, a long-acting oxytocin analogue, in nonpregnant women},
  volume       = {47},
  year         = {1990},
}