Drugs acting on the

uterus

Dr.U.P.Rathnakar
MD. DIH. PGDHM
K.M.C.Mangalore
Drugs Acting on the Uterus
• Introduction
• Stimulants
1. Oxytocin
2. Desamino-oxytocin
3. Ergometrine, Methyl ergometrine
4. Prostaglandins
• Tocolytics (Relaxants)
1. Adr.agonists, Ca++ blockers,
Magnesium sulfate, oxytocin antagonist,
Misc *
 Drugs

• Drugs ---- Endometrium or myometrium

• Endometrium--- Estrogen or progesterone,

and antagonists
• Myometrium-
1. Indirectly acting-Symp or P.symp
[ANS drugs-non selective-other systems+]
2. Directly acting
1. Ut.stimulants (oxytocics)
2. Ut. Relaxants (Tocolytics)*
 UTERINE STIMULANTS

• Post. Pit. Hormone- Oxytocin

• Ergot alkaloids- Ergometrine

(Ergonovine),
Methylergometrine

• Prostaglandins- PGE2, PGF2a, 15-Methyl

PGF2a, Misoprostol

• Miscellaneous- Alcohol, Ethacridine,

Quinine*
 Oxytocin (Quick birth)
• Post Pit → Oxytocin and Vasopressin
• Synth. In hypothalumus → Transported
and stored in post. Pitutary
• Released after distension of the cervix
and vagina → birth
• Stimulation of the nipples →
breastfeeding, (Letdown or milk ejection
reflex)*
 Pharmacokinetics
• Not absorbed orally
• Administerd by i.v, i.m, rarely
nasal route.
• Not bound to plasma protiens-
t1/2- 2 -5mts
• Metabolized in liver and
kidney*
 Pharmacodynamics
• Acts → GPCR
• Small doses → Frequency and
force
• Large doses → Sustained
contraction
• Mammary alveoli-myoepethelial
cells → contraction
• Neurotransmitter in brain*
 Ph. Actions:
• Uterus:
• Sensitivity increases as pregnancy progresses-
9 fold [early&nonpregnant-resistant]
• Receptors increase- 30 times
• Estrogen facilitates, progesterone inhibits
• Lower segment not contracted
• Breast- Milk ejection
• CVS- Hypotension
• Kidney- ADH like
• CNS*
 Clinical uses of Oxytocin
• To induce, augment labor in
2. Premature rupture
3. Isoimmunization
4. Placental insufficiency
5. Toxemia, post maturity, DM

Verify fetal lung maturity, Exclude C.Is-

Position abnormalities, CPD,distress etc.
Monitor fetal HR
Look for fetal, maternal distress, ut.scar*
 Induction & Augmentation
 Oxytocin DOC
 i.v. infusion pump
 Dilution-5 IU in 500ml NS/Glucose
 0.2-2ml/mt. depending on response
 Precautions→ Monitor mother and
fetus. Over stimulation →
Discontinue*
 Why Oxytocin? Why not Ergometrine?

1. Short t ½
2. Normal relaxation of uterus allowed-
Good fetal oxygenation
3. Lower segment not affected-descent
free
4. Consistent augmentation in
ut.inertia*
 Other uses
1. Third stage of labour, puerperium: (Post
partum hemorrhage) 5 IU i.m or i.v
infusion.
Other drugs→Ergometrine, Misoprostol
3. Breast engorgement: Nasal spray before
suckling
4. Oxytocin challenge test: To assess
placental insufficiency
• AD.Effects: Rupture ut. Fetal distress,
maternal injury*
 Desamino-oxytocin

• Buccal formulation, uses same

as oxytocin, less consistent
action*
 Ergometrine and Methyl ergometrine
• Amine ergot alkaloid and methyl derivative.
• Increase force, frequency, duration of
ut.contractions
• Moderate increase of dose → Basal tone
increased
• Lower segment also contracts.
• 5HT2, α Adre.agonist
• Methyl ergometrine more potent action on
uterus and less on CVS, CNS, GIT etc.*
 Ad. Effects:
• Methyl ergometrine less toxic
Nausea, vomiting, rise in BP.
Decreases milk secretion
Avoided in
 Vascular disease, HTN, toxemia
 Sepsis→gangrene
 Liver and kidney disease.*
 [Safe in ob.doses]
C.I.in pregnancy & early stages of labour
 Uses:

• PPH→ After anterior shoulder presentation

 Prevention → 0.2-0.3 mg i.m
 Treatment → 0.5 mg i.v.
4. Prevent uterine atony[cesarian, instrument]
5. To promote involution in multipara →
0.125mg TDS -7days
6. Diagnosis of variant angina during Coronary
angio*
•The "Four Ts" for Causes of Postpartum Hemorrhage

Approximate
•Four Ts Cause incidence (%)
Tone Atonic uterus 70

Trauma Lacerations, 20
hematomas,
inversion,
rupture
Tissue Retained tissue, 10
invasive placenta
Thrombin Coagulopathies 1
Ergometrine
 Prostaglandins

• PGE2 (Dinoprostone)→ Vaginal application

→ Induce II trimester abortion, missed
abortion, ripening of cervix in near term
• Preperations-
 Misoprostol → with mifepristone for
early abortion
15-Methyl-PGF2α (Carboprost) → II
trimester abortions
Facilitate labour- Unlabelled use in
cardiac, renal disease, eclampsia*
 Uterine relaxants[Tocolytics]

• Adrenergic agonists[β2]
• Ca++ channel blockers
• Magnesium sulfate
• Atosiban
• Others*
 Adrenergic agonists:
• Ritodrine:
Ritodrine is a Beta-2 agonist
 ADE:
 CVS-
 Metaboloic-
 Use: To delay labour
 I.v infusion 50μg/mt
 CI: Heart disease, diabetes, on beta
blockers.
• Others: Isoxsuprine*
• Magnesium sulfate:
• Not routinely used because of toxicity.
[eclampsia-for siezures]
Ca++ channel blockers:
 Reduced Ca entry → Reduced tone
 Nifedipine → 10mg every 30 mts

Atosiban: Antagonist of oxytocin

receptors
Others: Ethyl alcohol, nitrates, Halothane
etc.*
 Indications & Contraindications for
tocolytics
Ind: Delay preterm labour
CI:
More than 37 weeks gestation
Fetus >2500g
Fetus in distress
Cx dilation > 4 cm
Ruptured membrane
Toxemia,
Cardiac diseases
