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DEPARTMENT OF PHARMACEUTICAL SCIENCES,
MDU ROHTAK
Submitted to :-
Mrs. Anuradha Pannu
Pharmacology Theory Assignment
DRUGS ACTING ON THE UTERUS
STIMULANTS AND RELAXANTS
• Part of female reproductive system , known as womb.
• Consist of three layer
1. Endometrium – inner layer of uterus
2. Myometrium- smooth muscle, middle layer of uterus
3. Perimetrium- protective, upper layer of uterus
• Drugs acts on inner and middle layer mostly.
• Drugs classified as
1. Uterus stimulant 2. Uterus relaxant
Uterus – womb
Drugs acting on uterus
Uterine stimulants :
• These drugs increase uterine motility.
• They are classified as follows
1) Posterior pituitary hormone : Oxytocin,
Desamino oxytocin .
2) Ergot alkaloids: Ergometrine
(Ergonovine), Methylergometrine
3) Prostaglandins : PGE2, PGF2α, 15methyl
PGF2α, Misoprostol .
4) Miscellaneous : Ethacridine, Quinine.
Uterine relaxants
• Also known as tocolytics
• Decrease uterine motility.
• These are classified into 5 classes
1) Adrenergic agonists
2) Calcium channel blockers
3) Oxytocin antagonist
4) Magnesium sulfate
5) Miscellaneous drugs.
Oxytocin :-
• nonapeptide secreted by the posterior pituitary along with vasopressin (ADH).
• Both oxytocin and ADH are synthesized within the nerve cell bodies in supraoptic and
paraventricular nuclei of hypothalamus; are transported down the axon and stored in the
nerve endings within the neurohypophysis.
Pharmacological actions
1.Uterus
Increase contraction force and frequency
Estrogen sensitize the uterus and increase oxytocin receptors
Sensitivity increase in 3rd trimester
Oestrogens and estrogen increase uterus sensitivity towards oxytocin and
progestin decreases
2.Breast
 Contracts the myoepithelium of mammary alveoli
and forces milk to the bigger milk sinusoids.
 Milk ejection reflex
3.Cvs
• No effect except at high dose
4.Kidney
• No effect except at high dose
 Physiocological roles
 Milk Ejection Reflex.
 Labour.
 Neurotransmission.
 At low dose show normal relaxation between contractions
Pharmacokinetics
 Ineffective orally
 Administered by i.m. or i.v. routes
 Rapidly degraded in liver and kidney
 Induction of labor
 Uterine inertia
 Post partum hemorrhage and caesarean
section treatment
 Breast engorgement
Adverse effects
• Uterine hyperstimulation
• Water intoxication
• Headache
• Convulsions
Ergometrine and methylergometrine
• Natural ergot alkaloid while methylergometrine is semi synthetic.
Pharmacological actions
1.Uterus
 Increase forces and frequency, duration of contractions
 At low dose, normal relaxation
2.CVS
 Weaker vasoconstriction
 Raise in BP
3.CNS and GIT
 No effect except at high dose
Adverse effect:-
 Less toxic
 Nausea
 Rise in BP
 Vomiting
 Decrease milk secretion
 Avoided for GIT, liver and kidney patients
Pharmacokinetics
Administered orally
Takes less time on i.v. route
Half life time period is 1-2 hours
Prostaglandins:-
PGE2, PGF2α and 15methyl PGF2α
 potent uterine stimulants
Used in the later part of pregnancy
 cause ripening of cervix
Adrenergic Agonists:-
Ritodrine
 the β2 selective agonist
 prominent uterine relaxant action
Dose increase according to response
Adverse effects
a)Hyperglycemia
b)Hypokalamia
c)Headache
d)Arrhythmia
salbutamol and terbutaline are used as
alternative of ritodrine
Calcium channel blocker:-
• Because influx of Ca2+ ions plays an important role in uterine contractions, Ca2+ channel
blockers
• reduce the tone of myometrium and oppose contractions.
• can postpone labor if used early enough.
• Less side effects as compared to the β2 selective agonist
• Need intense care after calcium channel blocker therapy
Figure: different
mechanisms of
different uterus
relaxants
• Calcium channel blockers
• Magnesium sulfate
• β2 selective agonist
• NO donors
• Oxytocin antagonists
Magnesium sulphate
• First line drug got prevention and treatment of seizures in preeclampsia and eclalmpsia
• Acts as a tocolytic by competing with calcium ions entry into myometrium.
• Use to delay premature.
Miscellaneous drugs.
• Depress uterine contractions
• Not clinically used as tocolytics
• Halothane – effective uterine relaxant
• Used as anesthetics
Reference:-
• Tripathi KD, Essentials of Medical Pharmacology,7th edition, Jaypee Brothers Medical Publlishers, Private
limited ,Page no.329-34
• Shanbhag TV, Shenoy S, Pharmacology for Medical Graduates, 3rd edition, Elsevier Relax India private
limited, page no. 397-402
• Mudagal M.P., Sharma U. Raj, A textbook of Pharmacology-ii, 1st edition , sept,2019, Nirali Prakashan,
advancement of knowledge, page no. 23.1-23.6
• Brunton l, parker k, blumenthal d, buston l, goodman and gilman’s manual of pharmacology and
therapeutics, mc graw hill campanies , page no. 977-979
• Bruntoon l, goodman and gliman’s the pharmacological basis of therapeutics,13th edition, mc graw hill
education company, page no.783-785.
• https://www.slideshare.com.
• https://www. career medical.com
• https://www.pharmacy180.com
• https://www. researchgate.Com
THANKING YOU
Any Doubt ?

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Drugs acting in uterus - stimulant and relaxant

  • 1. DEPARTMENT OF PHARMACEUTICAL SCIENCES, MDU ROHTAK Submitted to :- Mrs. Anuradha Pannu Pharmacology Theory Assignment DRUGS ACTING ON THE UTERUS STIMULANTS AND RELAXANTS
  • 2. • Part of female reproductive system , known as womb. • Consist of three layer 1. Endometrium – inner layer of uterus 2. Myometrium- smooth muscle, middle layer of uterus 3. Perimetrium- protective, upper layer of uterus • Drugs acts on inner and middle layer mostly. • Drugs classified as 1. Uterus stimulant 2. Uterus relaxant Uterus – womb
  • 3. Drugs acting on uterus Uterine stimulants : • These drugs increase uterine motility. • They are classified as follows 1) Posterior pituitary hormone : Oxytocin, Desamino oxytocin . 2) Ergot alkaloids: Ergometrine (Ergonovine), Methylergometrine 3) Prostaglandins : PGE2, PGF2α, 15methyl PGF2α, Misoprostol . 4) Miscellaneous : Ethacridine, Quinine. Uterine relaxants • Also known as tocolytics • Decrease uterine motility. • These are classified into 5 classes 1) Adrenergic agonists 2) Calcium channel blockers 3) Oxytocin antagonist 4) Magnesium sulfate 5) Miscellaneous drugs.
  • 4. Oxytocin :- • nonapeptide secreted by the posterior pituitary along with vasopressin (ADH). • Both oxytocin and ADH are synthesized within the nerve cell bodies in supraoptic and paraventricular nuclei of hypothalamus; are transported down the axon and stored in the nerve endings within the neurohypophysis. Pharmacological actions 1.Uterus Increase contraction force and frequency Estrogen sensitize the uterus and increase oxytocin receptors Sensitivity increase in 3rd trimester Oestrogens and estrogen increase uterus sensitivity towards oxytocin and progestin decreases
  • 5. 2.Breast  Contracts the myoepithelium of mammary alveoli and forces milk to the bigger milk sinusoids.  Milk ejection reflex 3.Cvs • No effect except at high dose 4.Kidney • No effect except at high dose  Physiocological roles  Milk Ejection Reflex.  Labour.  Neurotransmission.  At low dose show normal relaxation between contractions
  • 6. Pharmacokinetics  Ineffective orally  Administered by i.m. or i.v. routes  Rapidly degraded in liver and kidney  Induction of labor  Uterine inertia  Post partum hemorrhage and caesarean section treatment  Breast engorgement Adverse effects • Uterine hyperstimulation • Water intoxication • Headache • Convulsions
  • 7. Ergometrine and methylergometrine • Natural ergot alkaloid while methylergometrine is semi synthetic. Pharmacological actions 1.Uterus  Increase forces and frequency, duration of contractions  At low dose, normal relaxation 2.CVS  Weaker vasoconstriction  Raise in BP 3.CNS and GIT  No effect except at high dose
  • 8. Adverse effect:-  Less toxic  Nausea  Rise in BP  Vomiting  Decrease milk secretion  Avoided for GIT, liver and kidney patients Pharmacokinetics Administered orally Takes less time on i.v. route Half life time period is 1-2 hours
  • 9. Prostaglandins:- PGE2, PGF2α and 15methyl PGF2α  potent uterine stimulants Used in the later part of pregnancy  cause ripening of cervix
  • 10. Adrenergic Agonists:- Ritodrine  the β2 selective agonist  prominent uterine relaxant action Dose increase according to response Adverse effects a)Hyperglycemia b)Hypokalamia c)Headache d)Arrhythmia salbutamol and terbutaline are used as alternative of ritodrine
  • 11. Calcium channel blocker:- • Because influx of Ca2+ ions plays an important role in uterine contractions, Ca2+ channel blockers • reduce the tone of myometrium and oppose contractions. • can postpone labor if used early enough. • Less side effects as compared to the β2 selective agonist • Need intense care after calcium channel blocker therapy
  • 12. Figure: different mechanisms of different uterus relaxants • Calcium channel blockers • Magnesium sulfate • β2 selective agonist • NO donors • Oxytocin antagonists
  • 13. Magnesium sulphate • First line drug got prevention and treatment of seizures in preeclampsia and eclalmpsia • Acts as a tocolytic by competing with calcium ions entry into myometrium. • Use to delay premature. Miscellaneous drugs. • Depress uterine contractions • Not clinically used as tocolytics • Halothane – effective uterine relaxant • Used as anesthetics
  • 14. Reference:- • Tripathi KD, Essentials of Medical Pharmacology,7th edition, Jaypee Brothers Medical Publlishers, Private limited ,Page no.329-34 • Shanbhag TV, Shenoy S, Pharmacology for Medical Graduates, 3rd edition, Elsevier Relax India private limited, page no. 397-402 • Mudagal M.P., Sharma U. Raj, A textbook of Pharmacology-ii, 1st edition , sept,2019, Nirali Prakashan, advancement of knowledge, page no. 23.1-23.6 • Brunton l, parker k, blumenthal d, buston l, goodman and gilman’s manual of pharmacology and therapeutics, mc graw hill campanies , page no. 977-979 • Bruntoon l, goodman and gliman’s the pharmacological basis of therapeutics,13th edition, mc graw hill education company, page no.783-785. • https://www.slideshare.com. • https://www. career medical.com • https://www.pharmacy180.com • https://www. researchgate.Com