Pharmacology in Nursing Women’s Health Drugs Karen Ruffin RN, MSN Ed.

1. Pharmacology in NursingWomen’s Health DrugsKaren Ruffin RN, MSN Ed.

2. Female Reproductive Functions • Female sex steroid hormones • Estrogens • Progestins • Pituitary gonadotropin hormones • Follicle stimulating hormone (FSH) • Luteinizing hormone (LH)

3. Female Reproductive Functions (cont’d) Development of primary and secondary sex characteristics Menstrual cycle

5. Estrogens • Three major endogenous estrogens • Estradiol (principal & most active) • Estrone • Estriol • Synthesized from cholesterol in ovarian follicles • Basic chemical structure of a steroid

7. Exogenous Estrogenic Drugs–Synthetic • Steroidal • Conjugated estrogens, estradiol transdermal, many others • Nonsteroidal • Chlorotrianisene, diethylstilbestrol diphosphate, others • These drugs no longer available in the United States

8. Estrogens Required For The development and maintenance of the female reproductive system The development of female secondary sex characteristics

9. Estrogens: Indications • Treatment of or prevention of disorders that result from estrogen deficiency • Atrophic vaginitis • Hypogonadism • Oral contraception (given with a progestin) • Dysmenorrhea • “Hot flashes” of menopause

10. Estrogens: Indications (cont’d) • Treatment of or prevention of disorders that result from estrogen deficiency (cont’d) • Uterine bleeding • Palliative treatment of advanced breast and prostate cancer • Osteoporosis treatment and prophylaxis • Many other indications

11. Estrogens: Indications (cont’d) • Continuous-combined hormone replacement therapy (CCHRT) • Fixed estrogen/progestin combination products • Reduce complications, such as endometrial hyperplasia, that occur from using estrogen alone

12. Estrogens:Contraindications Allergy to the medication Any estrogen dependent cancer Undiagnosed abnormal vaginal bleeding Pregnancy Active thromboembolic disorder or history

13. Estrogens:Adverse Effects Thrombolytic events—most serious Nausea—most common Hypertension, thrombophlebitis, edema Vomiting, diarrhea, constipation, abdominal pain May cause photosensitivity, chloasma

14. Estrogens:Adverse Effects (cont’d) Amenorrhea, breakthrough uterine bleeding Tender breasts, fluid retention, headaches Others

15. Progestins • Synthetic derivatives of progesterone • medroxyprogesterone (Provera) • hydroxyprogesterone • megestrol (Megace) • Many others

16. Progestins: Indications • Treatment of functional uterine bleeding caused by: • Hormonal imbalance, fibroids, or uterine cancer • Treatment of primary and secondary amenorrhea

17. Progestins: Indications (cont’d) Palliative treatment of some cancers and endometriosis Prevention of threatened miscarriage Alleviation of symptoms of PMS

18. Progestins: Indications (cont’d) • megestrol • Adjunct therapy for treatment of breast and endometrial cancers • Also used for management of anorexia, cachexia, or unexplained weight loss in AIDS patients • Used to stimulate appetite and promote weight gain in patients with cancer • Used with estrogen replacement therapy after menopause

19. Progestins:Adverse Effects Liver dysfunction—cholestatic jaundice Thrombophlebitis, thromboembolic disorders, such as PE Nausea, vomiting Amenorrhea, breakthrough uterine bleeding, spotting Edema, weight gain or loss Others

20. Contraceptive Drugs • Medications used to prevent pregnancy • Oral medications • Monophasic, biphasic, and triphasic forms • Most contain estrogen-progestin combinations

21. Contraceptive Drugs (cont’d) • Other contraceptive forms available • Long-acting injectable form of medroxyprogesterone (Depo-Provera) • Transdermal contraceptive patch • Intravaginal contraceptive ring

22. Contraceptive Drugs: Mechanism of Action • Prevent ovulation by inhibiting the release of gonadotropins and increasing uterine mucous viscosity, resulting in: • Decreased sperm movement and fertilization of the ovum • Possible inhibition of implantation of a fertilized egg (zygote)

23. Contraceptive Drugs: Other Drug Effects Improve menstrual cycle regularity Decrease blood loss during menstruation Decreased incidence of functional ovarian cysts and ectopic pregnancies

24. Contraceptive Drugs: Indications • Primarily used to prevent pregnancy • Other uses • Treatment of endometriosis and hypermenorrhea • To produce cyclic withdrawal bleeding • Postcoital emergency contraception

25. Contraceptive Drugs:Adverse Effects • Drawbacks to the use of these drugs include: • Hypertension • Thromboembolism, possible PE, MI, stroke • Alterations in lipid and carbohydrate metabolism • Increases in serum hormone concentrations • These effects are due to the estrogen component

26. Contraceptive Drugs:Adverse Effects (cont’d) • May also cause: • Edema, dizziness, headache, depression, nausea, vomiting, diarrhea, increased appetite, increased weight, breast changes, many others

27. Contraceptive Drugs:Interactions • Drugs that decrease effectiveness of oral contraceptive drugs • Antibiotics, barbiturates, isoniazid, rifampin, griseofulvin

28. Contraceptive Drugs:Interactions (cont’d) • Drugs that may have reduced effectiveness if given with oral contraceptive drugs • Anticonvulsants, beta-blockers, hypoglycemic drugs, oral anticoagulants, theophylline, TCAs, vitamins, hypnotics

29. Osteoporosis Low bone mass Increased risk of fractures Primarily affects women 20% of those with this condition are men

30. Osteoporosis

31. Osteoporosis: Risk Factors • Caucasian/Asian descent • Slender body build • Early estrogen deficiency • Smoking • Alcohol consumption • Low-calcium diet • Sedentary lifestyle • Family history

32. Drug Therapy for Osteoporosis Calcium supplements and vitamin D may be recommended for women at high risk for osteoporosis

33. Drug Therapy for Osteoporosis (cont’d) • Bisphosphonates • alendronate (Fosamax), ibandronate (Boniva), risedronate (Actonel) • Selective estrogen receptor modifier (SERM) • raloxifene (Evista) • Hormone • calcitonin • teriparatide (Forteo)

34. Drug Therapy for Osteoporosis (cont’d) Biphosphonates Work by inhibiting osteoclast-mediated bone resorption, thus preventing bone loss SERMs Stimulate estrogen receptors on bone and increasing bone density

35. Drug Therapy for Osteoporosis (cont’d) calcitonin • Directly inhibits osteoclastic bone resorption teriparatide • Only drug that stimulates bone formation • Derivative of parathyroid hormone • Action similar to natural parathyroid hormone

36. Drug Therapy for Osteoporosis:Indications • Bisphosphonates and calcitonin • Both prevention and treatment of osteoporosis • Biphosphanates also used for glucocorticoid-induced osteoporosis and Paget’s disease

37. Drug Therapy for Osteoporosis:Indications (cont’d) • raloxifene • Prevention of postmenopausal osteoporosis • teriparatide • Used for those with highest risk of fracture (prior history of fractures)

38. Drug Therapy for OsteoporosisAdverse Effects • SERMs • Hot flashes, leg cramps • Can increase risk of venous thromboembolism • Not used if patient is near age of menopause due to possible hot flashes • Leukopenia

39. Drug Therapy for OsteoporosisAdverse Effects (cont’d) • Bisphosphonates • Headache, GI upset, joint pain • Risk of esophageal burns if medication lodges in esophagus before reaching the stomach

40. Fertility Drugs • Various medical techniques used to treat infertility • Include: • in vitro fertilization • Medication therapy: ovulation stimulation

41. Fertility Drugs (cont’d) • clomiphene (Clomid, others) • Nonsteroidal ovulation stimulant • Blocks estrogen receptors in the uterus and brain, resulting in a false signal of low estrogen levels

42. Fertility Drugs (cont’d) • Clomiphene (Clomid, others) (cont’d) • Causes increased production of Gn-RH, FSH, and LH • As a result, maturation of ovarian follicles is stimulated, leading to ovulation and increased chance of conception

43. Fertility Drugs (cont’d) • Mentropins (Pergonal) • Standardized mixture of FSH and LH • Stimulates development of ovarian follicles, leading to ovulation • May also be given to men to stimulate spermatogenesis

44. Fertility Drugs (cont’d) • chorionic gonadotropin alfa (Ovidrel) • Recombinant form of human chorionic gonadotropin • Causes rupture and ovulation of mature ovarian follicles, and maintenance of corpus luteum • Used to stimulate ovulation

45. Fertility Drugs:Indications Used primarily to induce ovulation in anovulatory patients Also may be used to promote spermatogenesis in infertile men

46. Fertility Drugs:Adverse Effects Tachycardia, phlebitis, DVT Dizziness, headache, flushing, depression, anxiety, nervousness, fatigue Nausea, bloating, constipation, others Ovarian hyperstimulation, multiple pregnancies, blurred vision, breast pain, others

47. Uterine-Active Medications • Medications used to alter uterine contractions • Used to: • Promote labor • Prevent the start or progression of labor • Postpartum use: to reduce the risk of postpartum hemorrhage

48. Uterine Stimulants Also called oxytocics Ergot derivatives Prostaglandins Progesterone antagonist oxytocin (hormonal drug)

49. Uterine Stimulants (cont’d) Ergot alkaloids Increase force and frequency of uterine contractions Used after delivery of the infant and placenta to prevent postpartum uterine atony and hemorrhage methylergonovine (Methergine)

50. Uterine Stimulants (cont’d) Prostaglandins Natural hormones Cause potent contraction of myometrium, smooth muscle fibers of the uterus Used to induce labor by softening the cervix and enhancing uterine muscle tone dinoprostone (Prostin E2) and misoprostol (Cytotec)