Pharmacokinetics

not bound to plasma proteins

is eliminated by the kidneys and liver
T1/2 5 minutes.

Katzung, B. G., Masters, S. B., & Trevor, A. J. (2012). Basic &

clinical pharmacology. New York: McGraw-Hill Medical.
 Pharmacodynamics
acts through G protein-coupled receptors and
the phosphoinositide-calcium second-
messenger system
contract uterine smooth muscle, stimulates
the release of prostaglandins and leukotrienes
that augment uterine contraction.
small doses increases both the frequency
and the force of uterine contractions
higher doses produces sustained
contraction.

Katzung, B. G., Masters, S. B., & Trevor, A. J. (2012). Basic & clinical
pharmacology. New York: McGraw-Hill Medical.
 The general uses of these Oxytocin drugs would
include induction of labour .
at the time delivery,
a. Oxytocin binds to the receptors present in the
myometrium
b. activates the pathway of hydrolysis of
phoshotidyl inositol and diacyl glycerol
This activation causes the release of intracellular
Calsium which causes contraction of the uterus .

Kabilan A. J. Pharm. Sci. & Res. Vol. 6(4), 2014, 220-223

 Uterine contractions are seen after 3-5 minutes and
approx 1 minute of admistration through intramuscular
and intravenous routes respectively.
A steady state of the drug is reached after 40 mins of
parenteral route of administration. It is distributed
throughout extracellular fluid compartment of the
mother; small amounts may cross the placental barrier
and reach foetus. Metabolism takes place rapidly via the
liver and plasma by the enzyme oxytocinase a few steps
of metabolism also takes place via mammary gland. It
has a half-life of 1-5 minute.
Kidney and liver help in the elimination of Oxytocin drugs
unchanged form of this drug is rarely excreted in urine.

Kabilan A. J. Pharm. Sci. & Res. Vol. 6(4), 2014, 220-223

 Intravenous vs
Intramuscular
Using a radioinimunoassay for oxytocin, circulating levels of the Oxytocin were
measured following intravenous and intramuscular administration of Syntometrine.
1. After intramuscular injection oxytocin appeared in the circulation in as little as
30 seconds and continued to be detectable at levels around 25 pg. per ml. for
up to 60 minutes.
2. After intravenous injection there was a rapid rise to a peak of 530 pg. per ml. at
one minute.

The subsequent decay showed a bi-exponential pattern, and yielded an average

half-life of 3 minutes for the initial rapid phase of disappearance.

D. Gibbens et al. The Circulating Levels Of Oxytocin Following Intravenous

And Intramuscular Administration Of Syntometrine. The Journal of
Obstetrics and Gynaecology ojthe British Commonwealth. July 1972. Vol. 79. pp.
644-646.
D. Gibbens et al. The Circulating Levels Of Oxytocin Following Intravenous And
Intramuscular Administration Of Syntometrine. The Journal of Obstetrics and
Gynaecology ojthe British Commonwealth. July 1972. Vol. 79. pp. 644-646.
D. Gibbens et al. The Circulating Levels Of Oxytocin Following Intravenous And
Intramuscular Administration Of Syntometrine. The Journal of Obstetrics and Gynaecology
ojthe British Commonwealth. July 1972. Vol. 79. pp. 644-646.