Pharmacology in Nursing Women s Health Drugs

1. Pharmacology in NursingWomen�s Health Drugs

2. Female Reproductive Functions Female sex steroid hormones Estrogens Progestins Pituitary gonadotropin hormones Follicle stimulating hormone (FSH) Luteinizing hormone (LH) Development of primary and secondary sex characteristics Menstrual Cycle Estrogen and progestins are secreted by the ovaries which are considered endocrine glands, these 2 hormones along with pituitary ganadotropins hormones are responsible for the development of the primary sex structures which start at puberty . The FSH and LH are responsible to the maintenance of these systems and the continuous regulation of the menstrual cycle from month to month Chemically speaking eachof these 2 major classes includes several hormones However only 2 of these hormones occure in significant amounts and have the greatest physiologic activity. They are estrogen estradiol and progestin progesterone. Estradiol is principle secretary product of the ovaries and has several estrogenic effects, one being to regulate FSH and LH secretion others include development of secondary sex characteristics. Progesterone is the principle secretary product of the coprpus luteim and has progestational effects. This includes the promotion of tissue growth and secretory activity on the endometrium following the estrogen driven proliferative phase of menstrual cycle. This is required for the egg implantation and the maintenance of pregnancy.Estrogen and progestins are secreted by the ovaries which are considered endocrine glands, these 2 hormones along with pituitary ganadotropins hormones are responsible for the development of the primary sex structures which start at puberty . The FSH and LH are responsible to the maintenance of these systems and the continuous regulation of the menstrual cycle from month to month Chemically speaking eachof these 2 major classes includes several hormones However only 2 of these hormones occure in significant amounts and have the greatest physiologic activity. They are estrogen estradiol and progestin progesterone. Estradiol is principle secretary product of the ovaries and has several estrogenic effects, one being to regulate FSH and LH secretion others include development of secondary sex characteristics. Progesterone is the principle secretary product of the coprpus luteim and has progestational effects. This includes the promotion of tissue growth and secretory activity on the endometrium following the estrogen driven proliferative phase of menstrual cycle. This is required for the egg implantation and the maintenance of pregnancy.

3. The menstrual cycle take about one month to complete. It starts with puberty (menarche and ends with menopause. Phases are on page 505-506The menstrual cycle take about one month to complete. It starts with puberty (menarche and ends with menopause. Phases are on page 505-506

4. Estrogens Three major endogenous estrogens Estradiol (principal & most active) Estrone Estriol Synthesized from cholesterol in ovarian follicles Basic chemical structure of a steroid b/c the have a chemical structure like a steroid they can be referred to as a steroidal hormone. Which is the most active of the 3?? Esterdiolb/c the have a chemical structure like a steroid they can be referred to as a steroidal hormone. Which is the most active of the 3?? Esterdiol

5. 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 Most common popular estrogen products in use today are known as estrogen mixture know as conjugated estrogens. It contains a combination of natural estrogen compounds. The non steroidal are not available in the US b/c of major adverse side effects.Most common popular estrogen products in use today are known as estrogen mixture know as conjugated estrogens. It contains a combination of natural estrogen compounds. The non steroidal are not available in the US b/c of major adverse side effects.

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

7. 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 is a medical term for a defect of the reproductive system that results in lack of function of the gonads is a medical term for a defect of the reproductive system that results in lack of function of the gonads

8. 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 Most commonly known for its benefits in trating menopausal symptoms ie hot flashesMost commonly known for its benefits in trating menopausal symptoms ie hot flashes

9. 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

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

11. Estrogens:Adverse Effects Thrombolytic events�most serious Nausea�most common Hypertension, thrombophlebitis, edema Vomiting, diarrhea, constipation, abdominal pain May cause photosensitivity, chloasma Amenorrhea, breakthrough uterine bleeding Tender breasts, fluid retention, headaches Changes in pigmentation primarily on face similar to shat happens during pregnancy.Changes in pigmentation primarily on face similar to shat happens during pregnancy.

12. Progestins Synthetic derivatives of progesterone medroxyprogesterone (Provera) hydroxyprogesterone megestrol (Megace) Many others What is progestins responsible for ????? Preparing the uterus for fertilization. The 2nd most active progestin is pregnenolone a chemical precursor to all steroidal hormones that are synthesized from cholesterol in the ovary. b/c oral admin of progesterone is relatively inactive and parenteral admin is painful and causes local reaction, synthetic forms of developed that are effective orally and also more potent, their actions are more specific and have a longer duration, but they still have the same function as the hormone does in the bodyWhat is progestins responsible for ????? Preparing the uterus for fertilization. The 2nd most active progestin is pregnenolone a chemical precursor to all steroidal hormones that are synthesized from cholesterol in the ovary. b/c oral admin of progesterone is relatively inactive and parenteral admin is painful and causes local reaction, synthetic forms of developed that are effective orally and also more potent, their actions are more specific and have a longer duration, but they still have the same function as the hormone does in the body

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

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

15. 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

16. 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

17. Contraceptive Drugs Medications used to prevent pregnancy Oral medications Monophasic, biphasic, and triphasic forms Most contain estrogen-progestin combinations Page 512, has a table of oral contraceptivesPage 512, has a table of oral contraceptives

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

19. 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)

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

21. Contraceptive Drugs: Indications Primarily used to prevent pregnancy Other uses Treatment of endometriosis and hypermenorrhea To produce cyclic withdrawal bleeding Postcoital emergency contraception a method used to prevent pregnancy after unprotected sexual intercourse,a method used to prevent pregnancy after unprotected sexual intercourse,

22. Contraceptive Drugs:Adverse Effects Drawbacks to the use of these drugs include (effects due to estrogen component): Hypertension Thromboembolism, possible PE, MI, stroke Alterations in lipid and carbohydrate metabolism Increases in serum hormone concentrations Edema, dizziness, headache, depression, nausea, vomiting, diarrhea, increased appetite, increased weight, breast changes, many others

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

24. 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, vitamins, hypnotics

25. Osteoporosis Low bone mass Increased risk of fractures Primarily affects women 20% of those with this condition are men 23 women in the US are currentlu affected by osteoporosis or low bone mass, nearly 40% of women over the age of 50 year of age will develop an osteoporotic fracture at an annual cost of $11 billion dollars��..23 women in the US are currentlu affected by osteoporosis or low bone mass, nearly 40% of women over the age of 50 year of age will develop an osteoporotic fracture at an annual cost of $11 billion dollars��..

26. Osteoporosis Osteoporosis is a condition that causes abnormally thin boneOsteoporosis is a condition that causes abnormally thin bone

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

28. Drug Therapy for Osteoporosis Calcium supplements and vitamin D may be recommended for women at high risk for osteoporosis A study found once a person has osteoporosis treatment with these 2 supplements alone are not effective. All women should take them to maintain bone health but the will not treat osteoporosis.A study found once a person has osteoporosis treatment with these 2 supplements alone are not effective. All women should take them to maintain bone health but the will not treat osteoporosis.

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

30. 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 Osteoclast are cone cells that g=break down bone causing calcium to be reabsorbed into the circulation system if not controlled can lead to osteoporosis Selective estrogen receptor modulators such as raloxifene help to prevent osteoporosis by stimulating estrogen receptors on the bone and increasing bone density in a manor similar to the estrogen themselvesOsteoclast are cone cells that g=break down bone causing calcium to be reabsorbed into the circulation system if not controlled can lead to osteoporosis Selective estrogen receptor modulators such as raloxifene help to prevent osteoporosis by stimulating estrogen receptors on the bone and increasing bone density in a manor similar to the estrogen themselves

31. 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 When it acts similar to the parathyroid hormone it modulates the body�s metabolism of calcium and phosphorus.When it acts similar to the parathyroid hormone it modulates the body�s metabolism of calcium and phosphorus.

32. 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 Paget�s disease causes a malfunction in the normal process of bone remodelling. Normally, bone is continually breaking down and rebuilding. This usually slow process of bone destruction and growth is somehow altered in Paget's disease. When an area of bone is destroyed in a person with Paget�s disease, the bone that replaces it is soft and porous. Soft bone can be weak and easily bend, leading to shortening of the affected part of the body.� The bone replacement also takes place very quickly and excess bone may be formed. This can cause the bone to get larger, be painful and break easily Paget�s disease causes a malfunction in the normal process of bone remodelling. Normally, bone is continually breaking down and rebuilding. This usually slow process of bone destruction and growth is somehow altered in Paget's disease. When an area of bone is destroyed in a person with Paget�s disease, the bone that replaces it is soft and porous. Soft bone can be weak and easily bend, leading to shortening of the affected part of the body.� The bone replacement also takes place very quickly and excess bone may be formed. This can cause the bone to get larger, be painful and break easily

33. 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)

34. 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 Leukopenia decrease circulating WBC Leukopenia decrease circulating WBC

35. 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

36. Fertility Drugs Various medical techniques used to treat infertility Include: in vitro fertilization Medication therapy: ovulation stimulation Infertility in women generally results from absence of ovulation which is normally due to various imbalances in female reproduction hormones. These imbalances can occur at the level of the hypothalamus, pituitary gland, the ovary or any combination the the 3.Infertility in women generally results from absence of ovulation which is normally due to various imbalances in female reproduction hormones. These imbalances can occur at the level of the hypothalamus, pituitary gland, the ovary or any combination the the 3.

37. Fertility Drugs (cont�d) clomiphene (Clomid Nonsteroidal ovulation stimulant Blocks estrogen receptors in the uterus and brain, resulting in a false signal of low estrogen levels 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 So what do you think will happen if your brain thinks there is low estrogen in the body?????? The hypothalamus and pituitary gland then increase their production of Gn-Rh and FSH and LH This will stimulate the maturation of ovarian follicles that will lead to ovulation and increase the likelihood of conception.So what do you think will happen if your brain thinks there is low estrogen in the body?????? The hypothalamus and pituitary gland then increase their production of Gn-Rh and FSH and LH This will stimulate the maturation of ovarian follicles that will lead to ovulation and increase the likelihood of conception.

38. 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

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

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

41. 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

42. 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

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

44. 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)

45. 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)

46. Uterine Stimulants (cont�d) Progesterone antagonist mifepristone (Mifeprex) RU-486, the �abortion pill� Stimulates uterine contractions to induce abortion Given with a prostaglandin drug for elective abortions

47. Uterine Stimulants: oxytocin (Pitocin)Synthetic Form Used to induce labor at or near full-term gestation, and to enhance labor when contractions are weak and ineffective Prevent or control postpartum uterine bleeding Complete an incomplete abortion (after miscarriage) Promote milk ejection during lactation

48. Uterine Stimulants:Adverse Effects Hypotension or hypertension, chest pain Headache, dizziness, fainting Nausea, vomiting, diarrhea Vaginal pain, cramping Leg cramps, joint swelling, chills, fever, weakness, blurred vision

49. Uterine Relaxants:Tocolytics Used to stop labor that begins before term to prevent premature birth Generally used after the 20th week of gestation to stop uterine contractions that occur between the 20th and 37th weeks of gestation (considered premature labor) Nonpharmacologic measures: Bedrest, sedation, hydration

50. Uterine Relaxants:Tocolytics (cont�d) Uterine contractions that occur between the 20th and 37th weeks of gestation are considered premature labor Nonpharmacologic measures Bedrest, sedation, hydration

51. Uterine Relaxants ritodrine (Yutopar) and terbutaline (Brethine) Beta-adrenergic drugs Stimulation of beta2-adrenergic receptors on the uterine smooth muscle Results in relaxation of the uterus, thus stopping premature contractions �Off-label� use Magnesium sulfate IV also used to stop labor

52. Uterine Relaxants:Adverse Effects Palpitations, tachycardia, hypertension Tremors, anxiety, insomnia, headache, dizziness Nausea, vomiting, anorexia, bloating, diarrhea, constipation Hyperglycemia, hypokalemia Dyspnea, hyperventilation

53. Nursing Implications Assess baseline VS, weight, blood glucose levels, renal and liver function studies Assess whether the patient smokes Assess history and medication history Assess contraindications, including potential pregnancy

54. Nursing Implications (cont�d) Before giving any uterine stimulants, assess the mother�s vital signs and fetal heart rate Uterine relaxants are used when premature labor occurs between the 20th and 37th weeks of gestation

55. Nursing Implications (cont�d) For bisphosphonate, ensure that the patient has no esophageal abnormalities and can remain upright or in a sitting position for 30 minutes after the dose

56. Nursing Implications (cont�d) Estrogens and progestins Take the smallest dose needed Give IM doses deep in large muscle masses, and rotate sites Give oral doses with meals to reduce GI problems Teach patient about correct self-administration and what to do if a dose is missed

57. Nursing Implications (cont�d) Estrogens and progestins (cont'd) Increased susceptibility to sunburn may occur�advise patient to wear sunscreen or avoid sunlight Patients should report weight gain Annual follow-up exams should be completed, including PAP smear and breast exam

58. Nursing Implications (cont�d) Follow specific administration guidelines carefully for IV administration of uterine relaxants or stimulants Monitor the patient�s vital signs and fetal condition during therapy Instruct patient taking fertility drugs to take the medication as ordered Recommend the patient keep a journal while on fertility drugs

59. Nursing Implications (cont�d) Biphosphonates Instruct patient to take medication upon rising in the morning, with a full glass of water, and 30 minutes before eating Emphasize that the patient should sit upright for at least 30 minutes after taking the medication

60. Nursing Implications (cont�d) SERMs Instruct patient that the medication will need to be discontinued 72 hours before and during any prolonged immobility (such as surgery or a long trip)

61. Nursing Implications (cont�d) Monitor for therapeutic responses Monitor for adverse effects