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DRUGS ACTING ON UTERUS

BY – Aishwarya Patil- 40
Anushka Shinde - 51
Surabhi Bhor- 9
Anushka Gaikwad - 15
Aarti Gurusthale - 18
Pallavi Kamble- 23
DRUGS EFFECTS ON UTERUS
UTERINE STIMULANTS
 Posterior Pituitary
hormones:Oxytocin,Desamino oxytocin
 Ergotalkaloids:Ergometrine,methylergom
etrine
 Prostaglandins: PGE2, PGF2α,misoprostol
 Miscellaneous: ethacridine and quinine
UTERINE RELAXANTS
Tocolytics – drugs
 Beta-sympathomimetics (beta-2)Ritodrine,
isoxsuprine, terbutaline and salbutamol
 Calcium channel blockers: Nifedepine
Magnesium sulfate
 Prostaglandin inhibiting agents:
Indomethacin
 Oxytocin antagonist: Atosiban
 Ethyl alcohol
INTRODUCTION TO OXYTOCIN

Oxys+ tokos="quick" + "birth This Photo by Unknown Author is licensed under

CC BY-SA

Oxytocin is a nonapeptide freely water soluble & acid stable – posterior pituitary
 Physiological Role 1. Labour
2. Milk ejection reflex
3. Neurotransmission
 Oxytocin secretion: Sensory stimuli from cervix, vagina and breast suckling
Expulsive phase is triggered by sustained distension of uterine cervix and vagina
Oestrogen Increases its secretion
Ovarian polypeptide relaxin inhibits its release
ADH: Pain, haemorrhage and dehydration increases secretion
PHARMACODYNAMIC ACTION
OF OXYTOCIN ON…….

•  On UTERUS:-
 ↑ in force and frequency of contractions in pregnancy
 Uterine sensitivity to oxytocin - ↑ by estrogen & ↓by progesterone This Photo by Unknown Author is licensed under CC BY-NC-ND

 Early pregnancy – high dose of oxytocin is necessary

 Contraction of upper segment & relaxation of lower segment of uterus → Expulsion of fetus
 Non-pregnant uterus → resistance to oxytocin
 In human – Small dose-↑Tone & Amplitude Large Dose- ↑ Frequency of contraction + Incomplete relaxation
Higher Dose- Sustained contraction without relaxation ↔ resulted in ↓Blood flow to fetal, fetal distress &
death (Asphyxial injury)
 During parturition- ↑ Number of Oxytocin receptor (↑ sensitivity )
 Exogenous oxytocin- initiate rhythmic contraction
ON BREAST:-
Suckling by infant
↓
Stimulate nipple mechanoreceptors
↓
Hypothalamus
↓
Posterior pituitary
↓
↑Oxytocin release
↓
Contraction of myoepithelial cells of mammary gland Milk ejection
CONTD…..
CVS Normal therapeutic dose
No effect High doses = vasodilatation
fall in BP ,
Reflex-tachycardia, and flushing 

Kidney
High doses- ADH like effect In ↓urine output , pulmonary edema etc..
OXYTOCIN - MECHANISM OF ACTION

 Specific G protein-coupled membrane receptors related to Vasopressin (V1 and V2) receptors
Depolarization of muscle fibres and Ca++ influx
 Human myometrium – receptors coupled to Gq activation leads to generation of IP3 – release of Ca++
ions
 Increase in local prostaglandin concentration –uterine contraction
 Kinetics
Being a peptide not effective orally
Short half life – 3 to 6 minutes
Available as injections for IM and IV use – 0.5 ml, 1 ml and 5ml etc.
THERAPEUTIC ACTIVITY:-

 Induction of labour
 In uterine inertia
 Postpartum haemorrhage
 Cesearean section
 Abortion
 Breast engorment and for milk ejection
ADVERSE EFFECT :-

Non judicious use can leads to serious reaction i.e. Fetal distress,
placental abruption or uterine rupture

 High concentration – excessive fluid retention, or water

intoxication : hyponatremia, heart failure, seizures, and death.

 Bolus injection - hypotension

ERGOMETRINE

• Ergot Alkaloids Source : CLAVICEPS PURPUREA a

fungus which infects grasses and grains

• Methyl ergometrine is semi-synthetic derivatives obtained

from lysergic acid
• It is more potent & preferred than ergometrine
• They ↑ strength , duration ,frequency of uterine contraction Of both upper &
lower segment
• Contraction involve- Fundus Body cervical segments
PHARMACOLOGICAL ACTIONS-
ERGOMETRINE

Uterus
Increases force, frequency and duration of contractions
At low dose contraction is phasic in nature with normal relaxation in between
But moderate increase in dose – sustained contraction occurs
More sensitive - Gravid uterus and at puerperium
Contractions involve lower segment also
CVS:
Weaker vasoconstrictors than their amino acid counterparts - less chance of developing
endothelial damage
No significant rise in BP
CNS:
Interacts partially with dopaminergic, adrenergic and serotonergic receptors
No significant effect in usual doses
GIT High doses cause increased peristalsis
:
PHARMAKOKINETICS AND ADVERSE
EFFECT
 Methylergometrine is preferred over ergometrine – higher potency and less
marked other effects
 Pharmacokinetics:
 Near complete absorption form GIT
 Immediate onset of action with IV route
 Metabolized in liver and excreted in urine
 Half life – 1 to 2 hrs

 Adverse effects:
 No complication in usual doses - Nausea, vomiting and rise in BPmay occur
 Decrease in milk secretion (dopaminergic)

 Contraindications: Pregnancy before 3rdstage of labour, vasculardisease, hypertension, liver and kidney
diseases
THERAPEUTIC USES

Management of third stage of

pregnancy
To control and prevent post partum
hemorrage
To ensure normal ovulation
UTERINE RELAXANTS

Tocolytics – drugs
 These are drugs that inhibit uterine contractions
 Beta-sympathomimetics (beta-2)
 Ritodrine isoxsuprine terbutaline and salbutamol

Calcium channel blockers

 Nifedipine ,Verapamil ,Nicardipine, Amlodipine

Magnesium sulfate
RITRODRINE : ARRTHYMIA
PULMONAR
Y EDEMA

MECHANISM, THERAPEUTIC
BRADYCARDIA HYPOKALAMIA
USES , ADVERSE EFFECT
It acts as Beta2
Inactive adenyl
andreno recepter
as agonist
cyclase HYPOTENSION
ADR HYPERGLYEMIA

Therapeutic
uses
SO inhibits CAMP So inhbits
dependent conversion of ATP
protein to CAMP Uterine relaxants

Dysmenorrhoea

Uterine muscle Threatened

Inhibits calcium abortion
relaxation
influx
(tocolytic action
 CALCIUM CHANNEL BLOCKERS :
MECHANISM THERAPEUTIC USES , ADVERSE EFFECTS
• Uterine relaxants
Calcium channel blockers blocks L-type of Therapeutic
voltage gated calcium channel in myometrium uses

• HYPTENSION
Inhibits calcium influx • BRADYCARDIA
ADR • FOETAL HYPOXIA

Uterine muscle relaxation (tocolytic action )

 Flushing,
MAGNESIUM SULFATE dry mouth
Feeling of Nausea ,
warmth, headache,
Sweating palpitation
Action:
It directly uncouple
 The intracellular calcium is the excitation
displaced by magnesium ion
leading to inhibition of the
coupling and
inhibits cellular ADR
action potential
uterine activity

 Uses Cause relaxation of

 Used for prevention of uterine muscle,
tocolytic action
seizures in eclampsia, not used
for arrest of preterm labour
for its toxicites
It is preferred over
beta 2 agonists if
the patients is
having cardiac and
hyperthyroidism
 REFERENCE
TEXT BOOK OF PHARMACOLOGY -2
BY NIRALI PRAKASHAN

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