The slide presents the conditions of pregnant and non-pregnant uterus contraction and focuses on the pharmacology of uterine stimulants and relaxants of pregnant women.
2. Non- pregnant Human:
Contracts spontaneously but weakly during 1st part of the cycle.
More strongly during luteal phase and menstruation.
Pregnant Human:
Uterine movements depressed in early pregnancy.
Towards end of gestation, contractions increase in force and
frequency.
Fully co-ordinated during parturition.
3. Introduction: A nonapeptide hormone synthesized in the
hypothalamus.
Storage: Neurohypophysis (posterior pituitary)
Actions:
1. Uterus: Contraction of the pregnant uterus.
2. Breast: Contraction of myoepithelial cells, causing milk ejection.
3. Kidney: ADH- like action, decreases urine output.
4. Blood vessels: Vasodilatation.
4. Oxytocin binds to specific G- protein coupled receptors on
myometrium.
This leads to:
1. Generation of Inositol trisphosphate (IP3)
2. Release of Ca2+ from intracellular stores
3. Increased production of Prostaglandins by endometrium
Contraction of the pregnant uterus
5. Induction of labour
Reasons:
a. Toxaemia of pregnancy
b. Erythroblastosis faetalis
c. Ruptured membrane
d. Diabetic mother
e. Placental insufficiency
To prevent postpartum haemorrhage (PPH)
To augment uterine contractions
Breast engorgement
9. Pharmacologic Action
1. Uterus: Stimulate contractions involving both upper and
lower segments.
2. CVS: Weak vasoconstriction.
3. GI tract: Peristalsis increased in high doses.
Therapeutic Use
1. Prevention and treatment of postpartum haemorrhage.
2. Prevention of uterine atony.
3. To hasten involution of uterus.
10. PGE2, PGF2α and 15- Methyl PGF2α are
potent uterine stimulants
They cause ripening and dilatation of cervix
12. Ritodrine, the preferred β2 selective agonist has
prominent uterine relaxant action and is approved
to suppress premature labor and to delay delivery.
Salbutamol and Terbutaline can be used
alternatively.
Isoxsuprine oral / i.m. has been used to stop
threatenend abortion, but its efficacy is uncertain.
13. Mechanism of Action
It acts by inhibiting the influx of Ca2+ ions and reducing
the tone of myometrium to oppose contractions.
Other info
It can postpone labour if used early enough.
It is used orally.
Adverse Effect
Tachycardia and hypotension.
14. It is a peptide analogue of oxytocin which competitively
blocks the oxytocin receptors of the uterus and induces
uterine relaxation.
It is given by i.v. infusion.
It suppresses premature uterine contractions and
postpones preterm delivery.
Its cardiovascular and metabolic complications are less
than β2 agonists.
15. It acts as a tocolytic by competing with Ca2+ ions for entry
into myometrium through both voltage sensitive as well as
ligand gated Ca2+ channels.
It is a first line drug for prevention and treatment of
seizures in preeclampsia and eclampsia.
It is given by i.v. infusion.
Currently, it is only used when β2 agonists are
contraindicated.
Its use to delay premature labour is not safe as it may
increase perinatal mortality.
16. 1. To delay preterm labour
2. Threatened abortion
3. Dysmenorrhoea