Tocolytic agents
presented by:-
Krima patel
4 yr b.sc nursing, JCN
Roll no:-38
Definition:-
Preterm labor and delivery can be delayed by order
to improve the perinatal outcome.short-term delay of
48 hours allows the use of corticosteroids that reduce
the perinatal mortality and serious morbidity
significantly.
Commonly used drugs are:-
1.Betamimetics
2.Prostaglandin synthetase inhibitors
3.Magnesium sulfate
4.Calcium channel blockers
5.Oxytocin receptor antagonist
6.Nitric oxide donors and progesterone
1.Calcium channel blockers:-
Drugs:-nifedipine, nicadipine, verapamil
Mechanism of action:- nifedipine blocks the entry of calcium
inside the cell.it is equally effective to MgSO4.
Dose:- oral 10-20 mg every 3-6 hrs.( not sublingual)
Side effects & precautions:-
Maternal: hypotension,hedache flushing & nausea
Combined therapy with B mimetics or MgSO4 should be
avoided
2.Magnesium sulfate:-
Mechanism of action :-it acts by competitive
inhibition to calcium ion either at the cell membrane
reducing calcium influx decrease acetylcholine release
and its sensitivity at the motor end plate. Direct
depressant action on the uterine muscle.
Dose:- loading dose 4-6g IV (10-20%solution) over 20-
30 min followed by an infusion of 1-2g|hr.
To continue tocolysis for 12 hrs after the cntractions
have stopped.tocolytic effect is poor.
Cont…
Side effects and precautions:- MgSO4 is relatively
safe.
Common maternal side effects are
flushing,perspiration,hedache ,muscle
weakness,rarely pulmonary edema.
Neonatal side effects are lethargy ,hypotonia,rarely
respiratory depression.
Contraindications:- myasthenia gravis and impaired
renal function.
3. cyclo-oxygenase inhibitor:-
Drugs:-sulindac,ibuprofen,aspirin,indomethacin
Mechanism of action:- reduces synthesis of
PGs,theraby reduces intracellular free Ca++ activation
of MLCK and uterine contractions.
Dose:- loading dose 50mg PO or PR followed by 25
mg every 6 hrs for 48 hrs.
Cont…
Side effects and precautions:-
Maternal: heartburn,GI
bleeding,thrombocytopenia,renal injury,platelet
dysfunction
Neonatal sideeffects:
constriction of the ductud arteriosus.
Oligohydramnios
Neonatal pulmonary hypertension
IUGR
Cont…
Contraindications:- hepatic disease, active peptic
ulcer, coagulation disorder.
4. betamimetics:-
Drugs:- terbutaline,ritodrine,isoxsuprine
Mechanism of action:- activation of the intracellular
enzymes ,reduces intracellular free calcium and
inhibits activation of MLCK - reduced interaction of
actin and myosin -> smooth muscle relaxation
receptor stimulation causes smooth muscle
relaxation.
Cont…
Dose:-ritodrine is given by IV infusion ,infusion is
continued for about 12 hrs after the contraction ceases.
Terbutalinehas longer half-life and has fewer side
effects.SC injection of 0.25 mg every 3 to 4 hrs is given.
Side effects and precautions:-
Meternal: hedache,palpitation,tachycardia ,pulmonary
edema ,cardiac failure,hyperglycemia,hyperinsulinemia
hypokalemia and even death.
Cont…
fetal:-tachycardia,heart failure, IUFD.
Neonatal:- hypoglycemia and intraventricular
hemorrhage.
5. Oxytocin antagonist :-
Drug :- atosiban
MOA:-that blocks myometrial oxytocin receptors.it
inhibits intracellular calcium release ,thereby inhibits
myometrial contractions.
Dose: IV infusion
Side effects:- nausea ,vomiting, chest pain
6.Nitric oxide donors:-
Drugs:- glyceryl trinitrate (GTN)
MOA:- smooth muscle relaxant
Dose:-patches
Side effects:-may cause cervical ripening,
hedache
•Labor is the
Only blind date
Where you
Know you
Will meet the
Love of your life…
