Drugs acting in uterus - stimulant and relaxant

Drugs acting uterus are discussed in that ppt .
Uterus stimulants and uterus relaxants are discussed here
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1. DEPARTMENT OF PHARMACEUTICAL SCIENCES, MDU ROHTAK Submitted to :- Mrs. Anuradha Pannu Pharmacology Theory Assignment DRUGS ACTING ON THE UTERUS STIMULANTS AND RELAXANTS Submitted by Dheeraj Roll no. 1431 B.Pharm. 5 th sem

2. Part of female reproductive system , known as womb. Consist of three layer Endometrium – inner layer of uterus Myometrium - smooth muscle, middle layer of uterus Perimetrium - protective, upper layer of uterus Drugs acts on inner and middle layer mostly. Drugs classified as Uterus stimulant 2. Uterus relaxant Uterus – womb

3. Drugs acting on uterus Uterine stimulants : These drugs increase uterine motility. They are classified as follows Posterior pituitary hormone : Oxytocin, Desamino oxytocin . Ergot alkaloids : Ergometrine (Ergonovine), Methylergometrine Prostaglandins : PGE2, PGF2α, 15methyl PGF2α, Misoprostol . Miscellaneous : Ethacridine, Quinine. Uterine relaxants Also known as tocolytics Decrease uterine motility. These are classified into 5 classes Adrenergic agonists Calcium channel blockers Oxytocin antagonist Magnesium sulfate 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 Uterus Increase contraction force and frequency Estrogen sensitize the uterus and increase oxytocin receptors Sensitivity increase in 3 rd 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 Hyperglycemia Hypokalamia Headache 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,7 th edition, Jaypee Brothers Medical Publlishers, Private limited ,Page no.329-34 Shanbhag TV, Shenoy S, Pharmacology for Medical Graduates, 3 rd edition, Elsevier Relax India private limited, page no. 397-402 Mudagal M.P., Sharma U. Raj, A textbook of Pharmacology-ii, 1 st 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,13 th 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

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