Drugs Acting On Uterus

DRUGS ACTING ON
UTERUS
INTRODUCTION
• Drugs affecting uterine endometrium and

myometrium
• Responsiveness depends on hormonal and

gestational status
Role of the Autonomic Nervous
System
α1-adrenergic activation
(↑Contraction)
• Uterine smooth muscles: contraction
• Blood vessels: vasoconstriction
.
ß2-adrenergic receptors
(↓ Contraction )
• Smooth muscle: relaxation.
Hormonal Factors
Estrogen:
• ↑es oxytocin receptors & α-adrenergic response.
• Stimulate prostaglandins: F2α and E2.
• Causes cervical ripening.
Progesterone:
• ↓es myometrial contractility
• ↑ uterine NO synthesis.
• ↓ PG production and oxytocin receptors.
• Inhibits cervical ripening.
Hormonal Factors
Oxytocin:
• Posterior pituitary in response to the declining
levels of progesterone.
• Stimulate release of PG E2 and PG F2α.
Prostaglandins:
• Increased by estrogen, CRH, and inflammation.
• Down-regulated by progesterone.
• Induces cervical ripening and dilation
UTERINE STIMULANTS
(Oxytocic drugs)
Post Pituitary hormone – Oxytocin
Desamino-oxytocin
Carbetocin
Ergot alkaloids – Ergometrine
Methylergometrine
Prostaglandins – PGE2 : Dinoprostone
PGF2α: Dinoprost
Carboprost
PGI2: Misoprostol
Miscellaneous – Ethacridine
Quinine
Why?
To enhance uterine contractions

• To induce/enhance contractions
• Help in restricting an extended pregnancy
• Minimize PPH
OXYTOCIN
• ‘Oxys’ – Quick
• ‘Tokos’ – child birth
Essential role in milk ejection

Facilitatory role in initiation of labour & parturation
UTERUS
Released during labour – Facilitatory role
Increase force and frequency of contractions
Points:
• Dose related
• Sensitivity
• Nature of contractions
MOA: Via GPCR - ↑IP3
Direct action on Ca channels
Release of PG and leukotrienes
Oxytocin receptor antagonist:

Atosiban
BREAST
• Contracts myometrium of mammary alveoli –
Milk ejection reflex
• Obligatory role
CVS
High dose – Vasodilatation (↓ BP)
Reflex Tachycardia
Flushing
Umbilical vessels constricted : help in closure at

birth
KIDNEYS
High dose – Weak ADH like action
CNS
(Peptide neurotransmitter)
Mating and parenting behaviour
PHARMACOKINETICS
• Peptide Hormone
• T1/2 - 6 min
Shorter at term (Oxytocinase)
PREPARATIONS
• 2 IU/2ml, 5 IU/ml, 5 IU/0.5ml Inj
• 1 IU = 2 µg of pure hormone
USES
1. Initiation & augmentation of labour:
(a) Conditions requiring early Vaginal delivery -
Rh incompatibility, Maternal diabetes, placental
insufficiency, ruptured membranes, pre-eclampsia, post
maturity
Dose:5 IU in 500ml of 5% glucose, slow iv infusion
Start at slow rate (0.1-0.2 ml/min)
Double every 20-30 min to 20ml/min (max)
(Total 2-4 IU)
Monitor uterine contractions and fetal HR
(b) Uterine inertia:
To augment contractions
DOC - Preferred over ergometrine & PGs
• Short T ½ & slow iv infusion
• Normal relaxation between contractions
• LUS not contracted
• Consistent action
Dose – 2-5 IU in 500ml glucose soln
Monitor mother and fetus
Precautions & contraindications:
• Check presentation (rule out Breech)

• Assess maturity of fetal lungs
• Rule out CPD, fetal distress, fetal scar
LSCS preferred
2. Control of PPH
Forceful contractions of uterine muscles –
compresses blood vessels
Dose – 5 IU im/iv infusion (immediate response)

Preferred in hypertensives
3. Breast engorgement
Due to inefficient milk ejection
Dose: Intranasal spray (25-30 IU)
2-3 min before nursing
Does not increase milk production
4. Oxytocin Challenge Test:

For Uteroplacental adequacy
DESAMINO OXYTOCIN
Buccal formulation (50 IU tab)
Less potent and inconsistent
• Induction of labour: 50 IU tab every 30 min
(Max 10 tab)
• Uterine inertia: 25 IU every 30 min
• Promotion of involution:
25-50 IU 5 times/day for 7 days
• Breast engorgement: 25 - 50 IU
CARBETOCIN
Long acting analogue of oxytocin
Use:
• Prevention of uterine atony after CS
• Control PPH
ADVERSE EFFECTS
Non judicious use :
• Fetal/maternal soft tissue injury
• Rupture of uterus
• Fetal asphyxia
Large dose with NS:

• Water intoxication
ERGOT ALKALOIDS
ERGOTAMINE & METHYLERGOMETRINE
Actions
• Uterus (Methylergometrine 1 ½ times more
potent)
- Increase force, frequency and duration of
contractions
- Affects LUS also
- Increase uterine tone ( 5HT3 and α adrenergic
receptors)
CVS:
- Higher dose - increase BP
CNS:
High dose – Partial agonist/antagonist on
adrenergic, 5HT and dopaminergic receptors in
brain stem
GIT:
High dose – Increase peristalsis
PHARMACOKINETICS
• Rapid and complete oral absorption
• Onset of action Oral - 15 min
IM - 5 min
IV - Immediate
Plasma t ½ : 1-2 hrs

Metab in liver, excreted in urine
ADVERSE EFFECTS
• Nausea, vomiting, rise in BP
• Decrease milk secretion (high dose)

Dopaminergic action ( inhibits prolactin release)
• Avoid in:
- Vascular disease, Htn & toxemia
- Sepsis (gangrene formation)
- Liver and kidney disease
USES
1. Control & prevention of PPH:
Prevention:
• 0.2-0.3 mg im at delivery of anterior shoulder
• Only those at risk – grand multipara, uterine
inertia, etc
• Multiple pregnancy excluded before injecting
Control:
• 0.5 mg iv
2. After Ceasarian section/ instrumental
delivery – prevent uterine atony
3. To ensure normal involution:

- 0.125 mg TDS orally for 7 days
- In multipara where slow involution is expected
4. Diagnosis of variant angina:

Small dose ergometrine Injected IV during
coronary angiography- prompt constriction of
reactive vessels
PROSTAGLANDINS
• PGE1 : Gemeprost
• PGE2 : Dinoprostone
• PGF2α: Dinoprost & Carboprost
• PGI2: Misoprostol
Role:
• Cervical ripening & induction of labour –
Misoprostol & Dinoprostone
• Control of PPH – Carboprost ( 0.25mg every hour)
USES
1. Therapeutic abortion – II/I Trimester
Gemeprost/Carboprost
Mefepristone 600mg orally followed by
misoprostol 400µg after 48 hrs
2. Cervical Priming
Dinoprostone
3. PPH
Carboprost (uterus unresponsive to
ergometrine/ oxytocin)
4. Induction & augmentation of term labour
Dinoprostone
ADVERSE EFFECTS & PRECAUTIONS
• Nausea, vomiting, watery diarrhoes,

• Uterine cramps, forceful uterine contractions,
vaginal bleeding
• Flushing, shivering, fever, malaise, fall in BP,
tachycardia, chest pain
Not used along with oxytocin (uterine rupture)

ETHACRIDINE
• 50mg/50ml inj
• Extra-amniotic infusion 150mg (150ml) for II
trimester MTP

Drugs Acting On Uterus

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Drugs Acting On Uterus

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DRUGS ACTING ON

• Drugs affecting uterine endometrium and

• Responsiveness depends on hormonal and

To enhance uterine contractions

Essential role in milk ejection

Oxytocin receptor antagonist:

Umbilical vessels constricted : help in closure at

• Check presentation (rule out Breech)

Dose – 5 IU im/iv infusion (immediate response)

Does not increase milk production

4. Oxytocin Challenge Test:

Large dose with NS:

Plasma t ½ : 1-2 hrs

• Decrease milk secretion (high dose)

3. To ensure normal involution:

4. Diagnosis of variant angina:

• Nausea, vomiting, watery diarrhoes,

Not used along with oxytocin (uterine rupture)

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