DRUGS PRODUCING UTERINE

CONTRACTIONS (Oxytocic Drugs)

OXYTOCIN
ERGOT ALKALOIDS
PROSTAGLANDINS
 OXYTOCIN
• Is secreted by the posterior pituitary gland by sensory stimulation from cervix,
vagina, and from suckling at breast.
• Administered intravenously or as nasal spray
• Not bound to plasma proteins, eliminated by liver & kidneys with a Half life of 5
minutes.
• Breast: Contracts the myoepithelial cells of the breast → milk ejection
Major stimuli, baby cry and suckling
• Uterus: Mainly stimulates the contractility (frequency and force) of the fundus
segment of the uterus (resemble normal contractions).
• Cell membrane receptor:
stimulation of voltage-sensitive Ca++ channels, promotes the influx of Ca++
from extra cellular fluid and from S.R into the cell,
Stimulation of prostaglandin release
thereafter, stimulates uterine contraction.
 Contract uterine smooth muscle only at term (Immature uterus is
resistant to oxytocin).
 Sensitivity increases to 8 fold in last 9 weeks and 30 times in early
labor.
 Clinically, oxytocin is given only when uterine cervix is soft and
dilated.
Therapeutic Uses:
Induction & augmentation of labor (Drug of choice-slow I.V infusion)
Post partum uterine hemorrhage (I.V drip), I.M. Ergot alkaloid is
Better and less toxic.
Impaired milk ejection (One puff in each nostril 2-3 min before nursing)
Side Effects:
Uterine rupture (Major and most serious side effect)
Hypertension and Water intoxication (Has slight ADH-like activity)
Fetal death (ischemia)
Neonatal jaundice.

Contra-indications:
Hypersensitivity
Prematurity
Abnormal fetal position
Evidence of fetal distress
Cephalopelvic disproportion

Specific oxytocin antagonist

Atosiban, effective in the management of premature delivery
 Ergot Alkaloids
 Ergometrine (Ergonovine) & Methylergonovine. ‫أي حاجة فيها‬Ergo
 Induce Tetanic contraction of uterus without relaxation in between. These
does not resemble the normal physiological contractions.
It causes contractions of uterus as a whole; fundus and cervix (compress
rather than expel the fetus).
 Oral tablets or IM.
 Metabolized in liver and mainly excreted in bile.
 Post partum hemorrhage (can be given in combination with oxytocin).
 Prostaglandins
 PGE2 (Vaginal suppository & tab) & PGF2α (I.V infusion, IM
and intramniotic) & (PGE1) Vaginal suppository & tab.
 Contract uterine smooth muscle at any time during pregnancy
and it can soften the cervix.
• Therapeutic uses
Induction of abortion
Induction of labor (fetal death in uterus) as vaginal
suppository
Postpartum hemorrhage
 UTERINE RELAXANTS
(Tocolytic Drugs)
β-ADRENOCEPTOR AGONISTS.
CALCIUM CHANNEL BLOCKERS.
PROSTAGLANDIN SYNTHESES INHIBITORS.
MAGNESIUM SULFATE
PROGESTERONE
OXYTOCIN COMPETITIVE ANTAGONISTS

Mainly used to prevent premature delivery (weeks

20-36) → improve the survival of the newborn.
 β-ADRENOCEPTOR AGONISTS.

 Ritodrine, i.v. drip. Selective β2 receptor agonist used specifically

as a uterine relaxant.
 Increase in the level of cAMP reducing intracellular calcium
levels.
 Terbutaline, Oral, S.C, I.V: another less common agent.
 CALCIUM CHANNEL BLOCKERS.

 CALCIUM CHANNEL BLOCKERS.

Nifedipine
Cause relaxation of both spontaneous and oxytocin-induced
contractions.
 PROSTAGLANDIN SYNTHESES INHIBITORS.
NSAIDs: Aspirin, Indomethacin, Ibuprofen, …
However, premature closure of ductus arterious.
MAGNESIUM SULFATE
I.V infusion
Activates adenylate cyclase and stimulates Ca++ dependent ATPase
Uses: premature delivery and convulsions of pre-eclampsia.