Tocolytics & Ecobolics

DR. SAMIA PERWAIZ KHAN

Professor & HOD
Pharmacology
Tocolytics

 Suppress premature labor

( Greek tokos, childbirth, lytic, capable of dissolving).
 given when delivery - result in premature birth.
 time for the administration of betamethasone, a
glucocorticoid -greatly accelerate fetal lung maturity.
 Tocolytics

Types of agents
1.MgSO4
2.β 2 receptor agonist.
 Ritodrine
 Salbutamol
 Terbutaline
3.Calcium channel blockers.
 Nifedipine
 Verapamil
4.OXYTOCIN ANTAGONIST
 Atosiban
5.NSAIDS
 Indomethacin
Tocolytics

Magnesium Sulfate (MgSO4)

 First line of therapy

 Acts as a calcium antagonist and membrane stabilizer-
decreasing the force of contractions
 Used prophylactically -in preeclampsia to prevent seizures
continued for 12-24 hrs after delivery
S/E:
 Fatigue
 Headaches
 Diplopia and flushing
Toxicity: hypoxia, respiratory depression and cardiac arrest
Tocolytics

Ritodrine
 β 2 receptor agonist.
 Acts on smooth muscle cells to increase levels of cAMP
(via adenylate cyclase), decreases levels of free calcium ions and
reduces contractions.
S/E :
 Tachycardia
 Headaches
 Anxiety
 Verapamil is commonly used for - tachycardia
Terbutaline
 β2 receptor agonist, long acting.
Tocolytics
Calcium channel blockers.
 Calcium is blocked from entering the smooth muscle cells, thus
preventing contractions

 Nifedipine and Verapamil commonly used

 S/E: Dizziness, flushing and headaches
Tocolytics
 NSAIDs:

 Indomethacin
 Inhibit PG synthesis ( PGE2, PGF2α) delay labour.
Tocolytics

 NSAIDs:
 Indomethacin
 Inhibit PG synthesis ( PGE2, PGF2α) delay labour.
TOCOLYTICS

OXYTOCIN ANTAGONIST
Atosiban
 Oxytocin receptor antagonist.
 Adm. i/v-2-48 hrs
 Fewer Side-effects.
CONTRAINDICATIONS TO TOCOLYSIS
 Fetus
 is older than 37 wks
 Weight more than 2500g or
 Intrauterine Growth Retardation.
 Fetus in acute distress

 Maternal:
 Dilation is greater than 4 cms.
 Intrauterine infections.
 Has PIH, eclampsia, vaginal bleed, cardiac diseases.
ECBOLICS
- Used to induce labour
ECBOLICS
 Classification:
 Oxytocin
 Ergot alkaloid (Ergonavine)
 Eicosanoids
Dinoprostone(PGE2)
Carboprost ( 15 methyl PGF2α)
Combination: Mifepristone ( antiprogestrone)
Misoprostol ( prostaglandin)
 Oxytocin
 Peptide hormone- posterior pituitary.
 Sec. trimester– increased oxytocin receptors.
 Pharmacological concentration--- strong contraction
 Adm i/v or i/m (PPH)
 Eliminated– kidney & liver (placental oxytocinase).
 PD
 G-protein coupled receptors & Phosphinositides – Ca+ second.
messenger system.
 Release of PG & Leukoterine.
 Contraction of myoepithelial cells.
 Weak antidiuretic.
CLINICAL PHARMACOLOGY:

 Used to induce labour

 Rh problems.
 Maternal diabetes
 Preeclampsia
 Ruptured membranes.
 Augment abnormal labour.
 Post Partum Hemorrhage.
 Second. trimester abortion.
Oxytocin
 Toxicity & Contraindications:

 Uterine rupture, fetal distress, plactental abruption,

uterine rupture,
 Excess fluid retention, water intoxication,
hyponatremia, heart failure, seizure, death.
 Hypotension-bolus & reflex tachycardia.
 C/I:
 Fetal distress, prematurity, abnormal presentation,
Cephlo-pelvic disproportion.
Ergot alkaloid (Ergonavine)

 Stimulant effects on uterus--- α agonist, serotonin.

 Increase during pregnancy– α1 receptors.
 Small dose– rhythmic cont.
 Higher concentration. – powerful & prolonged
contraction.
 Ergonavine is more selective– affecting uterus.
Ergot alkaloid (Ergonavine)

 Stimulant effects on uterus--- α agonist, serotonin.

 Increase during pregnancy– α1 receptors.
 Small dose– rhythmic cont.
 Higher concentration. – powerful & prolonged cont.
 Ergonavine is more selective– affecting uterus.
Ergot alkaloid (Ergonavine)

 S/E:
- vomiting- D2 receptors in chemoreceptor trigger zone.
- Vasoconstriction.
- Increase in BP,
- nausea, vomiting, blurred vision, headache.
- Vasospasm of coronary A.--- angina.
 Eicosanoids
Dinoprostone(PGE2)

 Synthetic - PGE2
 Induction of abortion- missed abortion, begnin
hydatiform mole.
 Induction of labour- term
 Effects collagenase of cervix– softening.
 Adm. Vaginally.
Carboprost ( 15- methyl –PGF2α)

 Uses:
 Second trimester abortion.
 Post partum hemorrhage.
 Side-Effects:
 Vomiting
 Diarrhea
 Caution in asthmatic patients.
Combination: Mifepristone ( antiprogestrone)
Misoprostol ( prostaglandin)

 Mifeprestone is an orally active steroid antagonist of progesterone and

glucocorticoid.
 Used as abortifacient in early pregnancy.
 Combination of mifeprestone and misoprostol(PGE2) achieve
complete abortion in 95% of early pregnancies.
 S/E:
 Nausea, vomiting and diarrhea. Cramping pain and vaginal bleed.
 Rare (infections).