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UTERINE STIMULANTS (Oxytocics, Abortifacients)
Drugs Used For Induction and Augmentation of
Labour
Posterior Pitutary Hormone: Oxytocin, Desamino
oxytocin
Prostaglandins: PGE2, PGE1, PGF2α , 15-methyl
PGF2α(Carboprost), Misoprostol (Methyl ester of
PGE1)
Ergot Alkaloids: Ergometrine, Methylergometrine
Miscellaneous: Ethacridine, Quinine
Anti Progestin: Mifepristone
OXYTOCIN
1. Effects on Uterus: Increases force and frequency
of uterine contraction
2. Effects on Breast: Milk ejection
3. Cardiovascular System (CVS): fall in blood
pressure, reflex tachycardia
4. Kidney: ADH like action at high doses
Mechanism of Action: Oxytocin action is mediated
through specific G-protein coupled oxytocin
receptors. When these receptors are activated, they
mediate response through:
Depolarization of muscle fibres and influx of Ca++
ions (main mechanism)
Through phosphoinsitide hydrolysis and
IP3mediated intracellular release of Ca++ ions.
Number of oxytocin receptors increases markedly
during later part of pregnancy
Also increases Prostaglandin (PG) synthesis and
release by the endometrium
Uses:
• Drug of Choice
• Induction of Labour (slow i.v. infusion 5IU in 500 ml
glucose or NS; 10milli IU/mL: 0.2-2.0 mL/min)
• Uterine Inertia
• Postpartum Haemorrhage
• Breast Engorgement (inefficient milk ejection reflex;
intra-nasally)
• Oxytocin Challenge Test (risky and rarely performed)
Side Effects:
• Injudicious use: maternal and foetal soft tissue injury,
ruptured uterus, foetal asphyxia/death
• Water intoxication
Prostaglandins
• Local Hormones, derived from breakdown of
membrane phospholipid (yielding arachidonic acid)
• PGE2 and PGF2α: commonly used clinically
• Dinoprostone (PGE2): cervical maturation/ripening
• 5 times potent than and less toxic than PGF2α; costly
• Dinoprost tromethammine (PGF2α): myometrial
contractility
• Promotes myometrial contraction irrespective of
duration of gestation
Mechanism of Action:
• Change in myometrial cell membrane permeability
and alteration of membrane bound Ca++.
• Also sensitizes uterus to oxytocin
Uses:
• Misoprostol/PGE1: induction of abortion/labour;
cervical ripening
• Induction of labour (poor pre-induction cervical
score as in Intrauterine Fetal Death, shorter
period of gestation, primigravida: PGE1)
• Acceleration of labour
• Cervical ripening for induction of labour/abortion
• Management of atonic postpartum haemorrhage
• Medical management of tubal ectopic pregnancy
Side effects:
• On systemic use:
• Nausea, vomiting, diarrhoea, pyrexia,
bronchospasm
• Cervical laceration when used as an abortifacient
• Tachysystole of uterus during induction
• Foetal Distress
• Rupture of uterus: Rare
• Should not be used in patients with previous
history of Caesarean Section
Ergot Alkaloids
Ergometrine and Methylergometrine
• Uterus: Force, frequency and duration of uterine
contraction increased
• Mechanism of action: partial agonistic action on
5-HT2 and alpha adrenergic receptors
• CVS: Weak vasoconstrictors, raise blood pressure
• Gastrointestinal Tract: Increased peristalsis
Uses:
• Control and Prevent Postpartum Haemorrhage
• After Caesarean Section
• To ensure normal involution
Side Effects: Nausea, Vomiting, Rise in blood pressure,
Decrease milk secretion if used in high dose for many
days
Contraindication:
• Vascular disease
• Presence of sepsis
• Liver and Kidney disease
UTERINE RELAXANTS (TOCOLYTICS)
• These are drugs which decrease uterine motility.
• Delay or postpone labour
• Arrest threatened abortion
• Used in Dysmenorrhoea
UTERINE RELAXANTS (TOCOLYTICS)
• Adrenergic (β2) agonist: Ritodrine, Isoxsuprine,
T Terbutaline, Salbutamol
• Calcium channel blockers: Nifedipine
• Oxytocin Antagonist: Atosiban
• Magnesium sulfate (MgSO4)
• Miscellaneous: Ethyl alcohol, nitrates,
progesterone, general anaesthetics, indomethacin,
Halothane
Ritodrine
Mechanism of action: Ritodrine acts as selective β2
agonist on uterus & causes uterine relaxation.
Use:
Supress premature labour
Delay delivery
• Started as 50 μg/min i.v. infusion, increased gradually
Side Effects: hypotension, tachycardia, arrhythmia,
pulmonary edema, metabolic complications
(hyperglycaemia, hyperinsulinemia, hypokalemia),
anexiety, restlessness, headache, foetal pulmonary
edema
Contraindication: Mother having diabetes or heart
disease, or receiving β blockers or steroids
• Salbutamol and Terbutaline are alternatives to
Ritodrine.
• Isoxsuprine is used to stop threatened abortion.
Nifedipine
• Mechanism of Action: Nifedipine is L-type Ca++
Channel Blocker. It Reduces the tone of myometrium
and opposes contraction. It has prominent smooth
muscle relaxant action.
• Uses: Postpone labour
• Oral nifedipine 10 mg repeated once or twice after
20–30 min, followed by 10 mg 6 hourly has been
used.
• Side Effects:
• Maternal - Tachycardia, Hypotension
• Foetal – Foetal Hypoxia due to placental perfusion
Other Tocolytics
Atosiban
Mechanism of Action: Atosiban acts as antagonist at
the oxytocin receptors.
Magnesium sulfate
• Mechanism of Action: Acts as tocolytics by
competiting with Ca++ ions for entry into
myometrium through both voltage gated and
ligand gated Ca++ channels.
• A/E: may increase perinatal mortality
………………THANK YOU!!!..............

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Uterine stimulants & relaxants

  • 1. UTERINE STIMULANTS (Oxytocics, Abortifacients) Drugs Used For Induction and Augmentation of Labour Posterior Pitutary Hormone: Oxytocin, Desamino oxytocin Prostaglandins: PGE2, PGE1, PGF2α , 15-methyl PGF2α(Carboprost), Misoprostol (Methyl ester of PGE1) Ergot Alkaloids: Ergometrine, Methylergometrine Miscellaneous: Ethacridine, Quinine Anti Progestin: Mifepristone
  • 2. OXYTOCIN 1. Effects on Uterus: Increases force and frequency of uterine contraction 2. Effects on Breast: Milk ejection 3. Cardiovascular System (CVS): fall in blood pressure, reflex tachycardia 4. Kidney: ADH like action at high doses
  • 3.
  • 4.
  • 5. Mechanism of Action: Oxytocin action is mediated through specific G-protein coupled oxytocin receptors. When these receptors are activated, they mediate response through: Depolarization of muscle fibres and influx of Ca++ ions (main mechanism) Through phosphoinsitide hydrolysis and IP3mediated intracellular release of Ca++ ions. Number of oxytocin receptors increases markedly during later part of pregnancy Also increases Prostaglandin (PG) synthesis and release by the endometrium
  • 6.
  • 7. Uses: • Drug of Choice • Induction of Labour (slow i.v. infusion 5IU in 500 ml glucose or NS; 10milli IU/mL: 0.2-2.0 mL/min) • Uterine Inertia • Postpartum Haemorrhage • Breast Engorgement (inefficient milk ejection reflex; intra-nasally) • Oxytocin Challenge Test (risky and rarely performed) Side Effects: • Injudicious use: maternal and foetal soft tissue injury, ruptured uterus, foetal asphyxia/death • Water intoxication
  • 8. Prostaglandins • Local Hormones, derived from breakdown of membrane phospholipid (yielding arachidonic acid) • PGE2 and PGF2α: commonly used clinically • Dinoprostone (PGE2): cervical maturation/ripening • 5 times potent than and less toxic than PGF2α; costly • Dinoprost tromethammine (PGF2α): myometrial contractility • Promotes myometrial contraction irrespective of duration of gestation Mechanism of Action: • Change in myometrial cell membrane permeability and alteration of membrane bound Ca++. • Also sensitizes uterus to oxytocin
  • 9.
  • 10. Uses: • Misoprostol/PGE1: induction of abortion/labour; cervical ripening • Induction of labour (poor pre-induction cervical score as in Intrauterine Fetal Death, shorter period of gestation, primigravida: PGE1) • Acceleration of labour • Cervical ripening for induction of labour/abortion • Management of atonic postpartum haemorrhage • Medical management of tubal ectopic pregnancy
  • 11.
  • 12. Side effects: • On systemic use: • Nausea, vomiting, diarrhoea, pyrexia, bronchospasm • Cervical laceration when used as an abortifacient • Tachysystole of uterus during induction • Foetal Distress • Rupture of uterus: Rare • Should not be used in patients with previous history of Caesarean Section
  • 13. Ergot Alkaloids Ergometrine and Methylergometrine • Uterus: Force, frequency and duration of uterine contraction increased • Mechanism of action: partial agonistic action on 5-HT2 and alpha adrenergic receptors • CVS: Weak vasoconstrictors, raise blood pressure • Gastrointestinal Tract: Increased peristalsis
  • 14.
  • 15. Uses: • Control and Prevent Postpartum Haemorrhage • After Caesarean Section • To ensure normal involution Side Effects: Nausea, Vomiting, Rise in blood pressure, Decrease milk secretion if used in high dose for many days Contraindication: • Vascular disease • Presence of sepsis • Liver and Kidney disease
  • 16. UTERINE RELAXANTS (TOCOLYTICS) • These are drugs which decrease uterine motility. • Delay or postpone labour • Arrest threatened abortion • Used in Dysmenorrhoea
  • 17. UTERINE RELAXANTS (TOCOLYTICS) • Adrenergic (β2) agonist: Ritodrine, Isoxsuprine, T Terbutaline, Salbutamol • Calcium channel blockers: Nifedipine • Oxytocin Antagonist: Atosiban • Magnesium sulfate (MgSO4) • Miscellaneous: Ethyl alcohol, nitrates, progesterone, general anaesthetics, indomethacin, Halothane
  • 18. Ritodrine Mechanism of action: Ritodrine acts as selective β2 agonist on uterus & causes uterine relaxation. Use: Supress premature labour Delay delivery • Started as 50 μg/min i.v. infusion, increased gradually Side Effects: hypotension, tachycardia, arrhythmia, pulmonary edema, metabolic complications (hyperglycaemia, hyperinsulinemia, hypokalemia), anexiety, restlessness, headache, foetal pulmonary edema Contraindication: Mother having diabetes or heart disease, or receiving β blockers or steroids
  • 19. • Salbutamol and Terbutaline are alternatives to Ritodrine. • Isoxsuprine is used to stop threatened abortion.
  • 20. Nifedipine • Mechanism of Action: Nifedipine is L-type Ca++ Channel Blocker. It Reduces the tone of myometrium and opposes contraction. It has prominent smooth muscle relaxant action. • Uses: Postpone labour • Oral nifedipine 10 mg repeated once or twice after 20–30 min, followed by 10 mg 6 hourly has been used. • Side Effects: • Maternal - Tachycardia, Hypotension • Foetal – Foetal Hypoxia due to placental perfusion
  • 21. Other Tocolytics Atosiban Mechanism of Action: Atosiban acts as antagonist at the oxytocin receptors. Magnesium sulfate • Mechanism of Action: Acts as tocolytics by competiting with Ca++ ions for entry into myometrium through both voltage gated and ligand gated Ca++ channels. • A/E: may increase perinatal mortality ………………THANK YOU!!!..............