Progesterone

https://www.facebook.com/profile.php?id=100007500842607

1. Presentation on Progesterone By : Sanjay kumar yadav Sangita Dhungana B. Pharmacy 6 th sem , 22 & 21 roll number 6/13/2017 1 6th batch B.pharm (SMTC)

2. Contents Sanjay kumar yadav by: Introduction of progestrone Menstruation & Uterine cycle Role of Progestrone Alteration of progesterone Release and regulation Sources of progesterone (site of synthesis) Sources of progesterone Types of progesterone Route of administration of progesterone Pharmacokinetics Clinical uses of progestin Contraceptives Emergency contraceptive Combination pills Progestin only pills Sangita Dhungana by: Anti- progestrin : Mifeprestone Mechanism of action pharmacokinetics Side effect Drug interactions Uses & doses References 6/13/2017 2 6th batch B.pharm (SMTC)

3. Introduction of Progesterone Is hormones which stimulates and regulates various functions. Produce secondary sexual character in mature girls. Like enlargement of breast & buttock , release of pubic hair on sex organ etc. Causes attracts towards the sex /sex drive. Plays a role in maintaining pregnancy. Helps to regulates the monthly menstrual cycle. 6/13/2017 3 6th batch B.pharm (SMTC)

4. Menstruation Periodic discharge of blood and cellular debris from the female genital tract is termed menstruation. Cyclical changes occurring from one menstruation to the next comprises a menstrual cycle. The duration of menstrual cycle is about 28 ± 4 days. 6/13/2017 4 6th batch B.pharm (SMTC)

5. 6/13/2017 5

6. 6/13/2017 6 6th batch B.pharm (SMTC)

7. 6/13/2017 7 6th batch B.pharm (SMTC)

8. Uterine cycle Menstrual phase (3 – 5 days): If ovum is not fertilized, corpus luteum regresses from 24 th day of cycle Causes decrease in estrogen and progesterone levels. Results in shrinkage of endometrium . Flow of menses normally serves as a sign that a woman has not become pregnant . Average blood loss during menstruation is 10 – 80 ml. When menstruation begins, dysmenorrhea , breast tenderness occurs. 6/13/2017 8 6th batch B.pharm (SMTC)

9. 6/13/2017 6th batch B.pharm (SMTC) 9

10. Cont…. 2. Proliferative phase ( follicular phase): Starts at the end of menstrual phase Duration is about 10 days Later endometrium starts healing and then proliferates rapidly from 5 th – 14 th day of menstrual cycle. Endometrium increases in thickness to about 3 -5mm. The endometrial glands produce a thick mucus. At the end of proliferative phase ovulation occurs. 10

11. 6/13/2017 11

12. Cont…. 3. Secretory phase ( luteal phase): This phase lasts for about 14 days. It starts after ovulation and extends upto the next menstrual phase. Endometrium thickens upto 6 mm. Glands become bigger, tortuous and filled with secretions. Stromal cells proliferate, spiral arteries become more coiled and dilated. due to action of progesterone & estrogen on uterine endometrium . 12

13. 6/13/2017 13 6th batch B.pharm (SMTC)

14. 6/13/2017 6th batch B.pharm (SMTC) 14

15. Role of Progestrone : 6/13/2017 15

16. Alteration of progesterone Low progesterone in women Depression, migraine headache Weight gain Infertility Miscarriage Polycystic ovary syndrome Menstrual problems High progesterone in women High levels before cycle Headaches Moodiness Pre_menstrual symptoms (PMS) 6/13/2017 16 6th batch B.pharm (SMTC)

17. Release & Regulation of Progesterone Hypothalamus Gn.R.H . anterior lobe of pituitary gland L.H. corpus luteum of ovary Progesterone 6/13/2017 17 6th batch B.pharm (SMTC)

18. Sources of progesterone (site of synthesis) Females Corpus luteum Placenta during pregnancy Adrenal cortex Males Testes Adrenal cortex 6/13/2017 18 6th batch B.pharm (SMTC)

19. 6/13/2017 19 6th batch B.pharm (SMTC)

20. Sources Plant ( Dioscorea mexicana )----- diosgenin production ----progesterone. Mammals, progestrone , like all other steroid hormones, is synthesized from pregnenolone which is derived from cholesterol . Chemically or synthetic prepared progesterone inside labs . 6/13/2017 20 6th batch B.pharm (SMTC)

21. Route of administration of progesterone Oral Vaginal suppositories Deep intramuscular injection Implant Intrauterine system 6/13/2017 21 6th batch B.pharm (SMTC)

22. Pharmacokinetics Absorption: Progesterone undergo high 1st pass metabolism , hence mostly given by i.m in oily solution . have a short half life in the plasma, So, usually prescribed for twice or thrice-daily administration. Distribution: extensively bound to plasma proteins, primarily albumin (50 to 54%) and cortisol -binding protein (43 to 48%). Metabolism: reduction to pregnanediol , pregnanetriol and pregnanolone . Subsequent conjugation results in the formation of glucuronide and sulfate metabolites. Excreation : Metabolites of pregnanediol and pregnanolone are excreted →urine or bile ( enterohepatic recycling or feces.) 6/13/2017 22

23. 6/13/2017 23 6th batch B.pharm (SMTC)

24. Contraceptives MOA: inhibition of release of FSH and LH, increase viscosity of cervical mucus, endometrial changes, contraction of cervix, uterus and fallopian tube S.E.: agglomeration of RBC, liver & breast cancer, jaundice, stone formation in gall bladder, depression, headache etc. C.I.: liver & heart diseases, hypersensitivity. 6/13/2017 24 6th batch B.pharm (SMTC)

25. 6/13/2017 6th batch B.pharm (SMTC) 25

26. 6/13/2017 26 6th batch B.pharm (SMTC)

27. 27 6th batch B.pharm (SMTC)

28. 6/13/2017 28 6th batch B.pharm (SMTC)

29. 6/13/2017 29 6th batch B.pharm (SMTC)

30. 6/13/2017 30 6th batch B.pharm (SMTC)

31. Mechanism of action 6/13/2017 31 6th batch B.pharm (SMTC) Follicular phase: attenuates mid-cycle gonadotrophin (FSH/LH) surge from pituitary ( antiprogestrin activity)  slowing of follicle development and delay/failure of ovulation. Secretory / Lutael phase: prevents secretory changes by blocking progesterone action on endometrium . Later stages of cycle: blocks progesterone support to endometrium and increases prostaglandin(PG) release  stimulates uterine contraction Sensitizes myometrium to PG and induces mensturation . Post implantation: blocks decidualization  conceptus gets dislodged  human chorionic gonadotrophin ( hCG ) falls, luteolysis occurs decreased endogenous progesterone and cervix softens abortion.

32. 6/13/2017 32 6th batch B.pharm (SMTC)

33. Drug interactions chlorpromazine ↔ mifepristone : can increase the risk of an irregular heart rhythm. haloperidol ↔ mifepristone : can increase the risk of an irregular heart rhythm. norfloxacin ↔ mifepristone : can increase the risk of an irregular heart rhythm. halothane ↔ mifepristone : can increase the risk of an irregular heart rhythm. heparin ↔ mifepristone : may increase the risk and/or severity of vaginal bleeding in women. 6/13/2017 33

34. 6/13/2017 34

35. References http://cephalicvein.com/wp-content/uploads/2016/08/pituitary-gland-definition-endocrine-system-members-anatomy-physiology.jpg https://www.slideshare.net/azheenkmuhamad/progesterone-and-related-drugs https://www.slideshare.net/namkhadorji/use-of-progesterone-in-obstetrics-amp-gynaecology-namkha-presents https://www.slideshare.net/LifecareCentre/role-of-progesterone-in-pregnancy-27354617 https://en.wikipedia.org/wiki/Menstrual_cycle#Cycles_and_phases 6/13/2017 35 6th batch B.pharm (SMTC)

36. 6/13/2017 36 6th batch B.pharm (SMTC) Any Questions ???

37. Thanks for your attention… There is many things in life that will catch your eye, but only a few will catch your Heart…….pursue those 6/13/2017 37 6th batch B.pharm (SMTC)