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Progesterone and related drugs

Azheen Kanabi
Azheen Kanabi

Progesterone and related drugs are hormones that have various effects on the female reproductive system and body. Progesterone was first isolated from animal ovaries in 1933. It supports pregnancy by preventing menstruation and sensitizing the uterus. Synthetic progestins are used in oral contraceptives and hormone replacement therapy. Common side effects include irregular bleeding, but progestins also have therapeutic effects like preventing endometrial cancer. Progestin antagonists like mifepristone are used to terminate early pregnancy.

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Progesterone and related drugs Prepared by: Soma rashad jawad Azheen kanabi muhammad Tamara bakr rasul
Introduction Defintion History Effects of progesterone on the body Drugs related to progesterone Progesterone antagonists Oral contraceptives
progestogens Natural progesterone Synthetic progestins
Willard M. Allen Willard Myron Allen along with George W. Corner isolated the hormone from corpora lutea of sows and named it progestin in 1933
Progesterone favours pregnancyby: Preventingendomaterial shedding reducingUterine motility Inhibitingimmunological reaction toward the foetus
females Corpus luteum Placenta during pregnancy Adrenal cortex males Testes Adrenal cortex brain
Progesterone and related drugs
males Secrete 1-5 mg /day Plasma level 0.03mcg/dl females During the follicular phase the level is only slightly higherthanthat of males But during the luteal phase The plasma levels range from 0.5 to 2 mcg/dl Reaches peak in in the 3rd trimester of pregancy Effect=?
receptors The progesterone receptor (PR) is a progestin- activated steroid receptor Also known as NR3C3 ; Nuclear receptor subfamily 3 group C member 3 It is an intranuclear receptor It has 2 isoforms : PR A PR B PR is expressed in the following organs: central nervous system (CNS) Endocrine gastrointestinal immune reproductive cardiovascular respiratory Uterus ovary cerebellum spinal cord hypothalamus
Progesterone and related drugs
Effects of progesterone on the body
Uterus: Progesterone brings about the secretory changes in the endometruim
Cervix : Progesterone causes the production of a viscid cervical secretion Vagina: It causes leukocyte infiltration in the epithelium Breast: Progesterone cause proliferation of the acini in the mammary glands CNS: High levels may cause sedation Body tempretaure: It causes a slight 0.5 rise in body tempreture Metabolism: Impairs glucose tolerance They may tend to raise LDL and lower HDL It stimulates respiration Pituitary: They have anti ovulatory activity by reducing LH secretion
Progesterone and related drugs
Progestin derivatives
Synthetic progestin (Agonist)s Progesterone derivatives (21 C) 19-nortestosterone derivatives (18 C)
Synthetic progestin (Agonist)s Progesterone derivatives (21 C) These are pure progestins. They have weaker anti-ovulatory action and are used primarily as adjutants to estrogens for HRT, threatened abortion and edometriosis. 19-nortestosterone derivatives (18 C) They have weak estrogenic, androgenic and anabolic action but have potent anti- ovulatory action. They are mainly used in combined contraceptive pills. Like desogestrel and norgestimate (prodrug)
Progesterone derivatives (21 C) Medroxyprogesterone acetate Megestrol acetate Dydrogesterone Hydroxyprogesterone caproate Newer compound Nomegestrol acetate 19-nortestosterone derivatives (18 C) old Norethindrone (Norethisterone) Lynestrenol (Ethinylestrenol) Allylestrenol Levonorgestrel (Gonane) 19-nortestosterone derivatives (18 C) new (Gonanes ) Desogestrel Norgestimate Gestodene
Pharmacokinetics Progesterone undergo high 1st pass metabolism , hence mostly given by i.m in oily solution . they have a short half life in the plasma , so usually prescribed for twice or thrice-daily administration. A micronized preparation of progesterone is rapidly absorbed after its administrated by any route, Absorption
Distribution Progesterone is extensively bound to plasma proteins, primarily albumin (50 to 54%) and cortisol-binding protein (43 to 48%)
reduction to pregnanediol, pregnanetriol and pregnanolone. Subsequent conjugation results in the formation of glucuronide and sulfate metabolites. The metabolites of pregnanediol and pregnanolone are excreted urine or bile enterohepatic recycling or feces. Metabolism Excretion
Clinical uses of progestins 1.Rectify hormonal deficiency and HRT. 2. Contraception. 3.Control of dysfunctional uterine bleeding. 4.Treatment of dysmenorrhea. 6.Management of endometriosis. 5.Suppression of postpartum lactation. 7.Treatment of endometrial carcinoma.
CONTRAINDICATIONS Other contraindications Undiagnosed vaginal bleeding. Missed abortion. Known sensitivity to Progesterone injection.
1.Breast engorgement, headache, in body temperature, acne, esophageal reflux and mood swings . 2.Irregular bleeding or amenorrhoea . 3.The 19- nortestosterone derivatives plasma HDL level . 4.In HRT may the risk of breast cancer . 5. Diabetes may be precipitated by long term uses of potent agents like levonorgestrol.
Antiprogestin (antagonist): Mifepristone
19-norsteroid. with potent competitive anti-progestational, anti-glucocorticoid, anti-androgenic and partial agonist activity. It is administered during different phases of ovarian cycle. Mifepristone Pharmacokinetics Is orally active , bioavailability 25% Mainly metabolized liver & excreted bile.
Uses 1.termination of early pregnancy 2.As a contraceptive given once a month 3.Cervical ripening 4.cushings syndrome Side effects Main side effects are significant uterine bleeding and possibility of an incomplete abortion Also Uterine cramps
Contraceptive
The birth control pill (also called "the Pill") is a daily pill that contains hormones to change the way the body works and prevent pregnancy. Hormones are chemical substances that control the functioning of the body's organs. In this case, the hormones in the Pill control the ovaries and the uterus.
Major classes of oral contraceptive
Combination pills Products containing a combination of an estrogen and progestin are the most common type of oral contraceptives . The estrogens that are commonly used in combination pills are Ethinyl estradiol and mestranol The progestin in this preparations is norethindrone
Progestin pills Products containing a progestin only usually Norethindrone or norgestrel (called a mini_pill)
Progestin implants Subdermal capsules containing levonorgestrel offer long term contraception Six capsules each the size of a matchstick are placed subcutaneously in the upper arm the progestin is slowly released from the capsules Provide contraceptive protection for approximately five years Totally reversible if the implants are surgically removed
Mechanism Inhibition of release of FSH and LH Increase viscosity of cervical mucus Endometrial changes Contraction of cervix , uterus and fallopian tube
Effects on the body
Progesterone and related drugs
Therapeutic uses Numerous studies have shown that oral contraceptives (OC) provide protection against a wide variety of illnesses and conditions, including :
Progesterone and related drugs
Adverse effects
Progesterone and related drugs
Contraindications
Progesterone and related drugs
Richard AH , Pamela CC .Lippincotts illustrated reviews .3rd edition . Donnelley W : USA ; 2006. K.D.Tripathi.Essentials of medical pharmacology.3rd edition.jitender p vij:new delhi;2008. Laurance L. Brunton , john S.Lazo , Keith L.Parker . Goodman and gilmans the pharmacologicalbasis of theraputics.11th edition.mcGraw-hill:New york;2005.
List of refrences (cont.): Bertram g. Katzung , Susan B.Masters, Anthony J.Trevor. Basic and clinical pharmacology.12th edition. mcGraw-hill :New york;2012. James M. Ritter , Lionel DL , Timothy GK , Albert f . Clinical pharmacology and therapeutics . Fifth edition . Great britain: Hodder armond ;2008 . Teferra A , Srinivasa A , Amare M , Solomomon W , Eshetu L , Musie A , Dawet . Lecture notes for health science students .ethiopia 2004
List of refrences (cont.): progeterone receptors [Internet] :NURSA; 2014[cited 25 April 2015] Available from: https://www.nursa.org/nursa/molecules/nr.jsf?doi=10.1621/9 NIE3U3DI6 progesterone[Internet] :Drugs.com;2013[cited 25 April 2015] .Available from: http://www.drugs.com/pro/progesterone.html Therapeutic use of contraceptive [Internet] london: contraceptive; 1999 [cited 2015 april 15 ].available from: http://www.ncbi.nlm.nih.gov/pubmed/10342095
List of refrences (cont.): Combined oral contraceptive pill [internet] U.S.A :contraindications of contraceptive ; 2015 [cited 2015 april 21] . Available from: http://en.wikipedia.org/wiki/Combined_oral_contraceptive_ pill#Development_of_an_effective_combined_oral_contrace ptive

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Progesterone and related drugs

  • 1. Progesterone and related drugs Prepared by: Soma rashad jawad Azheen kanabi muhammad Tamara bakr rasul
  • 2. Introduction Defintion History Effects of progesterone on the body Drugs related to progesterone Progesterone antagonists Oral contraceptives
  • 4. Willard M. Allen Willard Myron Allen along with George W. Corner isolated the hormone from corpora lutea of sows and named it progestin in 1933
  • 5. Progesterone favours pregnancyby: Preventingendomaterial shedding reducingUterine motility Inhibitingimmunological reaction toward the foetus
  • 8. males Secrete 1-5 mg /day Plasma level 0.03mcg/dl females During the follicular phase the level is only slightly higherthanthat of males But during the luteal phase The plasma levels range from 0.5 to 2 mcg/dl Reaches peak in in the 3rd trimester of pregancy Effect=?
  • 9. receptors The progesterone receptor (PR) is a progestin- activated steroid receptor Also known as NR3C3 ; Nuclear receptor subfamily 3 group C member 3 It is an intranuclear receptor It has 2 isoforms : PR A PR B PR is expressed in the following organs: central nervous system (CNS) Endocrine gastrointestinal immune reproductive cardiovascular respiratory Uterus ovary cerebellum spinal cord hypothalamus
  • 11. Effects of progesterone on the body
  • 13. Cervix : Progesterone causes the production of a viscid cervical secretion Vagina: It causes leukocyte infiltration in the epithelium Breast: Progesterone cause proliferation of the acini in the mammary glands CNS: High levels may cause sedation Body tempretaure: It causes a slight 0.5 rise in body tempreture Metabolism: Impairs glucose tolerance They may tend to raise LDL and lower HDL It stimulates respiration Pituitary: They have anti ovulatory activity by reducing LH secretion
  • 16. Synthetic progestin (Agonist)s Progesterone derivatives (21 C) 19-nortestosterone derivatives (18 C)
  • 17. Synthetic progestin (Agonist)s Progesterone derivatives (21 C) These are pure progestins. They have weaker anti-ovulatory action and are used primarily as adjutants to estrogens for HRT, threatened abortion and edometriosis. 19-nortestosterone derivatives (18 C) They have weak estrogenic, androgenic and anabolic action but have potent anti- ovulatory action. They are mainly used in combined contraceptive pills. Like desogestrel and norgestimate (prodrug)
  • 18. Progesterone derivatives (21 C) Medroxyprogesterone acetate Megestrol acetate Dydrogesterone Hydroxyprogesterone caproate Newer compound Nomegestrol acetate 19-nortestosterone derivatives (18 C) old Norethindrone (Norethisterone) Lynestrenol (Ethinylestrenol) Allylestrenol Levonorgestrel (Gonane) 19-nortestosterone derivatives (18 C) new (Gonanes ) Desogestrel Norgestimate Gestodene
  • 19. Pharmacokinetics Progesterone undergo high 1st pass metabolism , hence mostly given by i.m in oily solution . they have a short half life in the plasma , so usually prescribed for twice or thrice-daily administration. A micronized preparation of progesterone is rapidly absorbed after its administrated by any route, Absorption
  • 20. Distribution Progesterone is extensively bound to plasma proteins, primarily albumin (50 to 54%) and cortisol-binding protein (43 to 48%)
  • 21. reduction to pregnanediol, pregnanetriol and pregnanolone. Subsequent conjugation results in the formation of glucuronide and sulfate metabolites. The metabolites of pregnanediol and pregnanolone are excreted urine or bile enterohepatic recycling or feces. Metabolism Excretion
  • 22. Clinical uses of progestins 1.Rectify hormonal deficiency and HRT. 2. Contraception. 3.Control of dysfunctional uterine bleeding. 4.Treatment of dysmenorrhea. 6.Management of endometriosis. 5.Suppression of postpartum lactation. 7.Treatment of endometrial carcinoma.
  • 23. CONTRAINDICATIONS Other contraindications Undiagnosed vaginal bleeding. Missed abortion. Known sensitivity to Progesterone injection.
  • 24. 1.Breast engorgement, headache, in body temperature, acne, esophageal reflux and mood swings . 2.Irregular bleeding or amenorrhoea . 3.The 19- nortestosterone derivatives plasma HDL level . 4.In HRT may the risk of breast cancer . 5. Diabetes may be precipitated by long term uses of potent agents like levonorgestrol.
  • 26. 19-norsteroid. with potent competitive anti-progestational, anti-glucocorticoid, anti-androgenic and partial agonist activity. It is administered during different phases of ovarian cycle. Mifepristone Pharmacokinetics Is orally active , bioavailability 25% Mainly metabolized liver & excreted bile.
  • 27. Uses 1.termination of early pregnancy 2.As a contraceptive given once a month 3.Cervical ripening 4.cushings syndrome Side effects Main side effects are significant uterine bleeding and possibility of an incomplete abortion Also Uterine cramps
  • 29. The birth control pill (also called "the Pill") is a daily pill that contains hormones to change the way the body works and prevent pregnancy. Hormones are chemical substances that control the functioning of the body's organs. In this case, the hormones in the Pill control the ovaries and the uterus.
  • 30. Major classes of oral contraceptive
  • 31. Combination pills Products containing a combination of an estrogen and progestin are the most common type of oral contraceptives . The estrogens that are commonly used in combination pills are Ethinyl estradiol and mestranol The progestin in this preparations is norethindrone
  • 32. Progestin pills Products containing a progestin only usually Norethindrone or norgestrel (called a mini_pill)
  • 33. Progestin implants Subdermal capsules containing levonorgestrel offer long term contraception Six capsules each the size of a matchstick are placed subcutaneously in the upper arm the progestin is slowly released from the capsules Provide contraceptive protection for approximately five years Totally reversible if the implants are surgically removed
  • 34. Mechanism Inhibition of release of FSH and LH Increase viscosity of cervical mucus Endometrial changes Contraction of cervix , uterus and fallopian tube
  • 37. Therapeutic uses Numerous studies have shown that oral contraceptives (OC) provide protection against a wide variety of illnesses and conditions, including :
  • 43. Richard AH , Pamela CC .Lippincotts illustrated reviews .3rd edition . Donnelley W : USA ; 2006. K.D.Tripathi.Essentials of medical pharmacology.3rd edition.jitender p vij:new delhi;2008. Laurance L. Brunton , john S.Lazo , Keith L.Parker . Goodman and gilmans the pharmacologicalbasis of theraputics.11th edition.mcGraw-hill:New york;2005.
  • 44. List of refrences (cont.): Bertram g. Katzung , Susan B.Masters, Anthony J.Trevor. Basic and clinical pharmacology.12th edition. mcGraw-hill :New york;2012. James M. Ritter , Lionel DL , Timothy GK , Albert f . Clinical pharmacology and therapeutics . Fifth edition . Great britain: Hodder armond ;2008 . Teferra A , Srinivasa A , Amare M , Solomomon W , Eshetu L , Musie A , Dawet . Lecture notes for health science students .ethiopia 2004
  • 45. List of refrences (cont.): progeterone receptors [Internet] :NURSA; 2014[cited 25 April 2015] Available from: https://www.nursa.org/nursa/molecules/nr.jsf?doi=10.1621/9 NIE3U3DI6 progesterone[Internet] :Drugs.com;2013[cited 25 April 2015] .Available from: http://www.drugs.com/pro/progesterone.html Therapeutic use of contraceptive [Internet] london: contraceptive; 1999 [cited 2015 april 15 ].available from: http://www.ncbi.nlm.nih.gov/pubmed/10342095
  • 46. List of refrences (cont.): Combined oral contraceptive pill [internet] U.S.A :contraindications of contraceptive ; 2015 [cited 2015 april 21] . Available from: http://en.wikipedia.org/wiki/Combined_oral_contraceptive_ pill#Development_of_an_effective_combined_oral_contrace ptive