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INDIRA GANDHI NATIONAL TRIBAL UNIVERSITY
(A Central University Established by an Act of Parliament)
AMARKANTAK 484 887, MADHYA PRADESH, INDIA
COURSE TITLE: pharmacology of drugs acting on uterus COURSE CODE: BP503T CONTENTS 1. ACKNOWLEDGEMENT 2. CERTIFICATE 3. INTRODUCTIONS 4. BACKGROUND 5. SYNTHESIS AND SECRETION OF OXYTOCIN 6. OXYTOCIN AS LOVE HORMONE 7. ROLE AND FUNCTION OF OXYTOCIN 8. PHASES OF LABOUR 9. MECHANISMS OF NORMAL LABOUR 10. ABNORMAL LABOUR: MALPOSITION AND MALPRESENTATION 11. Drug action 12. KEYWORDS 13. CONCLUSION AND REFERENCES ACKNOWLEDGEMENT It gives me a great pleasure in this assignment, which primarily aimed at complete coverage of drugs acting on uterus which used in clinical aspect of obstetrics and gynecology. The assignment cover all essential topic that is needed to understand the pharmacology of uterine acting drugs .I would like to thank Dr kunj sir for being a huge pillar of support to this assignment. I sincerely hope that this assignment will be of immense value to pharmacy students and practitioners . Any feedback regarding the assignment is highly appreciated. SHIVAM ADITYA Certificate The assignment entered here is satisfactorily performed by Master /MissSHIVAM ADITYAstudying in INDIRA GANDHI NATIONAL TRIBAL UNIVERSITY, AMARKANTAK course BPHARMACYsemester5th Enrollment no -2001109049 during the academic year 2022-23 Teachers signature……………………………………. Examiner signature………………………… Principal / HOD………………………………………….. Date : SEPTEMBER 11, 2022 OXYTOCIN: SYNTHESIS AND SECRETION ● Oxytocin is polypeptide hormone which is synthesized in supraoptic and paraventricular nuclei of hypothalamus and it is transported to posterior pituitary with help of axonal part present in it . ● It is released during parturition and nipple stimulation . OXYTOCIN AS A LOVE HORMONE: WHY? Oxytocin is said to be love hormone , because of it affinity towards the bonding in individuals. Though they are various ideas that can be presumed but some textual formats recognized it as the hormone of affectionate love . There is far difference between perfectionate love and affectionate love . Unless or until situation of love arousement is there this a perfectationate love with is developed by neurotransmitters serotonin and dopamine but the affinity towards the opposite gender till the baby planning and gestation is affectionate love which is mediated by oxytocin. Not only that even after parturition oxytocin produces in such amount that baby is recognized by mother very quickly . Some text said that when you in tension or having upset mind , just have a touch with mothers body or just talk from mother on phone call if you are far away , this touchwood triggers oxytocin amount in your body and it will releases the tension . Oxytocin: ROLES AND FUNCTION 1. Roles ● Sexual arousements ● Child mother bonding ● Recognition ● Trust ● Romantic attachment 2.FUNCTIONS ● Parturition of foetus as well as placenta ● Milk ejection reflex PHASES OF LABOUR:
Stage |
Latent phase
Fetus Uterus
Vagina
Umbilical cord
Stage Il
Fetus Uterus
Fully dilated
cervix
Umbilical Crowning
Sard of the head
Active phase
Fetus Effacement and
dilatation of
cervix
Uterus
a a Vagina
Umbilical cord
Stage III
Placenta
Cervix
Umbilical cord
clamp
Umbilical Vagin:
cord
ABNORMAL LABOUR: MALPOSITION AND MALPRESENTATION 1. Malposition and malpresentation are common causes of abnormal risk of labour and are associated with increased risk of maternal or fetal complications. ● Malposition: position such as occipitoanterior or occipitotransverse position is called malposition. ● Malpresentation: any presentation of the foetus other than the vertex presentation is termed as malpresentation . Brow , face , breech and transverse lie are included in this . BREECH PRESENTATION CLASSIFICATION: Posterior pituitary hormones ERGOT ALKALOIDS PROSTAGLANDIN S ANALOGUES MISCELLANEOUS Oxytocin Ergometrine Dinoprostone Dinoprost Ethacridine Desamino Oxytocin Methylergometrine Carboprost Quinine Misoprostol + mifepristone Action over organs : 1. UTERUS : increases the force and frequency of contraction and estrogen sensitize the uterus to oxytocin which increases the oxytocin receptors . 2. BREAST : it contract the myoepithelium of mammary alveoli and force of milk ejection in women on suckling process . 3. CVS: no any effective role but high dose can cause vasodilation and produces brief fall in blood pressure. 4. KIDNEY : at high doses it ADH like action which decreases the urine output . ● . PHARMACOKINETICS : ● Inactive orally ● Route of administration : intramuscular (i.m), intravenous ( i.v) or rarely by intranasal spray . 1. Dehydration : liver and kidney 2. Plasma t ½ :6-12 min 3. Enzyme detected in maternal plasma : oxytocinase 4. Unitage and preparation : 1 IU OF oxytocin = 2ug of pure hormone ● OXYTOCIN/ SYNTOCINON: 2IU/ 2 ml and 5 IU/ ml inj.. ● PITOCIN: 5IU/ 0.5 ml inj IU: INTERNATIONAL UNITS 2.ERGOMETRINE AND METHYLERGOMETRINE : Pharmacologically they are the amine ergot alkaloids which are used in obstetrics . 1. UTERUS: they increase the force of contraction as well as frequency 2. CVS: they are the weaker vasoconstrictors which can cause increment of blood pressure but that is insignificant in nature . 3. CNS: no any effect at usual doses but can cause complex action with adrenergic , serotonergic and dopaminergic receptors in brain 4. GIT: higher dose can cause increase in peristalsis activity . 1. Pharmacokinetic action : 1. Route of administration: oral : 15 min , im : 5 min and iv : immediate action 2. Metabolism : liver 3. Excretion: urine 4. Plasma t1/2 : 1-2 hr 5. Effect of single dose : 3-4 hrs 6. Adverse effects ● Gangrene ● Liver and kidney diseases ● Hypertension ● Nausea ● Vomiting 3. PROSTAGLANDINS ● Dinoprostone , dinoprost and carboprost are potent uterine stimulants. ● They promote the ripening of cervix ● Misoprostol an PG ANALOGUE produces less side effect . ETHACRIDINE : used for extra amniotic infusion ( 50 mg / 50 ml ) For medical termination of pregnancy in 2nd trimester ( 150mg / 150ml) An alternative method used occasionally . UTERINE RELAXANTS ( TOCOLYTICS) ● These are the drugs which decreases the uterine motility. ● They are used to delay or postpone labour . ● They are also used to arrest threatened abortion and in dysmenorrhoea ● Measures to delay labour should be undertaken if membranes have ruptured, antepartum hemorrhage and foetal death . Dysmenorrhea: menstrual cramp, , passing clot CALCIUM CHANNEL BLOCKERS ● Calcium plays an important role in contraction of smooth muscle or cells presents in tissues of the uterus . ● They show relaxant action to postpone or delay labour if used early . Eg : Nifedipine 10mg repeated once or twice after 20 - 30 min which is followed by 10 mg 6 hr been used . ADR’ ● tachycardia ● Hypotension ● Foetal hypoxia (deficiency in amount of oxygen reaching the tissue) OXYTOCIN ANTAGONISTS ● It is a peptide analogue of oxytocin. ● It produces affect which is antagonistic to oxytocin. ● Available in europe and U.k ● Not approved in USA AND INDIA . ● available for inhibition of labour between 24 to 33 week of gestation . CONTRAINDICATIONS: ● FEWER CARDIOVASCULAR COMPLICATIONS ● AND METABOLIC COMPLICATIONS MISCELLANEOUS DRUGS ● Magnesium sulphate is a first line drug for in pregnancy. ● Mostly used for treatment of preeclampsia(high blood pressure in pregnancy characterised by proteinuria{ >0.3g protein in 24 hr urine specimen})) and eclampsia. ● Act as a tocolytics by competing with calcium ions for entry into myometrium through both voltage gated as well as ligand gated calcium channel . ADR’S Perinatal mortality . Risk factor: Delay premature labour is risky . ● Ethyl alcohol , nitrates , progesterone , general anaesthetic and indomethacin , which can depress uterine contraction. ● Halothane is also used as anaesthetic . REFRENCES: ● Tripathi kd.Essential of Medical pharmacology 8th edition.NewDelhi: Jaypee Brothers pvt . Ltd; 2019.pg 354- 09 ● BabuArun sharmila. Clinical obstetrics and Gynecology 4th edition. Haryana ( Gurgoan) : wolter kluwer pvt . Ltd;2022.pg 552-72 THANK