Therapeutics 2 Contraception Contraceptives 1 At the end

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Therapeutics 2 Contraception & Contraceptives 1

Therapeutics 2 Contraception & Contraceptives 1

At the end of this chapter, the students will be able to 1. Identify

At the end of this chapter, the students will be able to 1. Identify the main phases of menstrual cycle 2. Differentiate between contraceptives type ( mechanical or containing hormones) 3. Compare between different types of contraceptives in effectiveness, safety and contraindications aspects. 4. Choose appropriate contraceptive based on women condition 5. Describing the common and important adverse of contraceptives. 6. Identification the necessary laboratory monitoring parameters for patients on contraceptives 2

Introduction • 62 million U. S. women in their childbearing years (15– 44). About

Introduction • 62 million U. S. women in their childbearing years (15– 44). About 43 million of them (70%) are at risk of unintended pregnancy. • Couples who do not use any method of contraception have an 85% chance of experiencing a pregnancy over a year. . 3

 • 62% of all women of reproductive age are currently using a contraceptive

• 62% of all women of reproductive age are currently using a contraceptive method. • 64% of women who practice contraception currently use nonpermanent methods, primarily hormonal methods (the pill, patch, implant, injectable and vaginal ring, the IUD ) and condoms. The rest depend on female (27%) or male (10%) sterilization 4

Definitions Conception (Pregnancy) is the fertilization of mature ovum by a sperm , known

Definitions Conception (Pregnancy) is the fertilization of mature ovum by a sperm , known as an embryo or fetus, in a woman's uterus. http: //www. differencebetween. net/science/health/difference-between-conception-and-gestation 5

Contraception (birth control): the prevention of pregnancy following sexual intercourse by: 1. inhibiting sperm

Contraception (birth control): the prevention of pregnancy following sexual intercourse by: 1. inhibiting sperm from coming into contact with a mature ovum 2. preventing a fertilized ovum from implanting successfully in the endometrium. Contraceptive : A device, drug, or chemical agent that prevents conception. 6

Pathophysiology • The cycle of menstruation begins around the age of 12 years, and

Pathophysiology • The cycle of menstruation begins around the age of 12 years, and continues to occur in nonpregnant women until menopause, usually around age 50 years. • Menstrual cycle can be affected by: 1. Race 2. body weight 3. medical conditions 4. family history 7

 The first day of menses is referred to day 1 of the menstrual

The first day of menses is referred to day 1 of the menstrual cycle and marks the beginning of the follicular phase. The follicular phase continues until ovulation, which typically occurs on day 14. The time after ovulation is referred to as the luteal phase, which lasts until the beginning of the next menstrual cycle. The median menstrual cycle length is 28 days, but it can range from 21 to 40 days 8

 • epinephrine and norepinephrine • hypothalamus • gonadotropin-releasing hormone (Gn. RH) • anterior

• epinephrine and norepinephrine • hypothalamus • gonadotropin-releasing hormone (Gn. RH) • anterior pituitary gland • follicle-stimulating hormone (FSH), and luteinizing hormone (LH) • direct events in the ovarian follicles that result in the production of ovum. 9

http: //www. onlinebiologynotes. com/ovarian-cycle-menstrual-cycle 10

http: //www. onlinebiologynotes. com/ovarian-cycle-menstrual-cycle 10

Factors : 1. Effectiveness in preventing pregnancy • - depends on: Mechanism of action

Factors : 1. Effectiveness in preventing pregnancy • - depends on: Mechanism of action Availability (e. g. , prescription required) Patient concurrent medications (patients taking teratogenic - Past medical history Acceptability (e. g. , side effects, ease of use, adherence, cost, and medications or those with underlying medical conditions in which pregnancy may not be desired will require a highly effective birth control method or multiple methods), drug interaction which maybe decreases effectiveness of CHCs social beliefs) 11

2. Return to fertility time (Some contraceptive methods allow a woman to conceive shortly

2. Return to fertility time (Some contraceptive methods allow a woman to conceive shortly after discontinuation like in this case with S. F, whee as others may delay fertility longer) 3. Contraindications for her that may indicate one method over another. 4. Cigarettes smoking and CHCs - Women who are 35 years of age or older and smoke 15 or more cigarettes per day should not use CHCs - Smoking may decrease fertility and has adverse effects on birth outcomes 12

5. Cardiovascular disease - The increase in mortality is concentrated in smokers 35 years

5. Cardiovascular disease - The increase in mortality is concentrated in smokers 35 years and older. - Increase in LDL, TC, low HDL - MI: risk is higher with higher doses of estrogen and especially if the patient is a smoker or has hypertension. 6. Hypertension: - Combined hormonal contraceptives appear to increase blood pressure (sodium and water retention and increased renin activity) - Progestin-only contraceptives have not been shown to increase blood pressure and may be preferable for women with uncontrolled hypertension. - Hypertensive women who have end-organ vascular disease or who smoke should not use CHCs 13

7. Migraine and stroke: - if a patient experiences a migraine with aura while

7. Migraine and stroke: - if a patient experiences a migraine with aura while taking CHCs, she should discontinue the product and switch to a non estrogen method - Evidence does not show an increased stroke risk with progestin-only contraceptives - Stroke: highest risk of stroke are smokers, patients with hypertension, and patients older than 35 years 14

8. Thrombolytic events: • Estrogens increase coagulability and thereby increase the possibility of clot

8. Thrombolytic events: • Estrogens increase coagulability and thereby increase the possibility of clot formation. other studies have shown no changes or decreases in prothrombotic factors. (hypercoagulable states, acquired conditions (e. g. , obesity, pregnancy, immobility, trauma, surgery, and certain malignancies) - A greater risk is associated with ethinyl estradiol (EE) doses greater than 35 mcg 15

9. Diabetes: - low-dose COCs do not alter glucose tolerance - Progestins decrease and

9. Diabetes: - low-dose COCs do not alter glucose tolerance - Progestins decrease and estrogens increase the number of insulin receptors on the cell membrane. Progestins also may alter insulin receptor affinity - Pts with history of gestational DM, or family history are at greater risk for COC-induced glucose intolerance - For women with diabetes, the World Health Organization recommends avoiding COCs if they have been diabetic for more than 20 years or they have endorgan damage such as retinopathy, neuropathy, or nephropathy. 16

Applied Therapeutics, 10 th ed, Koda-Kimble, 2013 17

Applied Therapeutics, 10 th ed, Koda-Kimble, 2013 17

Non pharmacological therapy 1. Periodic Abstinence: avoiding sexual intercourse during the days of the

Non pharmacological therapy 1. Periodic Abstinence: avoiding sexual intercourse during the days of the menstrual cycle when conception is likely to occur. 2. Barrier Techniques: These methods include condoms, diaphragms, cervical caps. A major disadvantage is higher failure rates than with most hormonal contraceptives 3. Surgery: Female sterilization (tubal occlusion), Male sterilization (vasectomy) 18

 Condoms : for female and male, mainly made of rubber, provide protection against

Condoms : for female and male, mainly made of rubber, provide protection against STDs, need lubricant. Diaphragm: small dome shaped device that fit inside the vagina and need to be fitted by health provider, made of rubber and used with spermicides, may need lubricant and does not provide protection against STDs. 19

 • cervical cup: a small plastic dome that fits tightly over the cervix

• cervical cup: a small plastic dome that fits tightly over the cervix and stay in place by suction, used with spermicides, may need lubricant and does not provide protection against STDs. Cervical cup Diaphragm 20

Pharmacological therapy 1. Spermicides 2. Oral contraceptives 3. Parental contraceptives 4. Implemented devices 5.

Pharmacological therapy 1. Spermicides 2. Oral contraceptives 3. Parental contraceptives 4. Implemented devices 5. Others : transdermal patches Hormonal contraceptive 21

Spermicides Most contain nonoxynol-9, are chemical surfactants that destroy sperm cell walls and act

Spermicides Most contain nonoxynol-9, are chemical surfactants that destroy sperm cell walls and act as barriers that prevent sperm from entering the cervical origin. creams, films, foams, gels, suppositories, sponges, and tablets spermicides offer no protection against STDs by causing small disruptions in the vaginal epithelium, and High user failure rate 22

Oral contraceptives • Contain combination of estrogen and progestin, or progestin alone. • Work

Oral contraceptives • Contain combination of estrogen and progestin, or progestin alone. • Work primarily before fertilization to prevent conception. • Mechanism : Estrogens suppress FSH release from the pituitary, which may contribute to blocking the LH and preventing ovulation. 23

 Progestins provide most of the contraceptive effect by thickening cervical mucus to prevent

Progestins provide most of the contraceptive effect by thickening cervical mucus to prevent sperm penetration, slowing tubal motility and delaying sperm transport. Estrogens : Two synthetic are available in the United States, ethinyl estradiol (EE) and mestranol (up to 30 mcg/day, 50 mcg/day if drugs interaction, acne, absence of bleeding). Progestins : include drospirenone, levonorgestrel, norgestimate, norethindrone and others 24

 • Types: - Monophasic pills: contain a constant dose of estrogen and progestin

• Types: - Monophasic pills: contain a constant dose of estrogen and progestin given over 21 day, followed by 7 days of placebo pills. - Biphasic and triphasic pills: contain constant amounts of estrogen and increasing dose of progestin given over 2 , 3 successive 10, 7 days, also followed by a 7 -day placebo phase 25

- Extended-cycle pills : increase the number of hormonecontaining pills from 21 to 84

- Extended-cycle pills : increase the number of hormonecontaining pills from 21 to 84 days, followed by a 7 -day placebo phase, or low dose of estrogen, resulting in four menstrual cycles per year. Seasonique ® ( EE + Levonorgestrel) - Progestin only pills: breast feeding women, safer in women with migraine, thermoboembolic, poorly controlled HTN, DM, vascular disease, smokers and over 35 y. Micronor ® 26

- Emergency contraceptives( plan B): two high progestin pills level ( levonorgestrel 0. 75

- Emergency contraceptives( plan B): two high progestin pills level ( levonorgestrel 0. 75 mg in each ). Taken within 72 hr of unprotected intercourse or in cases of ripping , and considered for up to 5 days. 27

Type of oral contraceptive Example (in micrograms) Monophasic Yasmin ® Ethinyl estradiol 30 Drospirenone

Type of oral contraceptive Example (in micrograms) Monophasic Yasmin ® Ethinyl estradiol 30 Drospirenone 3 Biphasic Necon® 10/11 Day 1 -10 Ethinyl estradiol 0. 035 Norethindrone 0. 5 Day 11 -21 Ethinyl estradiol 0. 035 Norethindrone 1. 0 Triphasic NORTREL® 7/7/7 Day 1 -7 Ethinyl estradiol 0. 035 Norethindrone 0. 5 Day 8 -14 Ethinyl estradiol 0. 035 Norethindrone 0. 75 Day 15 -21 Ethinyl estradiol 0. 035 Norethindrone 1. 0 28

 Directions of use: - In the postpartum phase, there is concern about the

Directions of use: - In the postpartum phase, there is concern about the effects of OCs on hypercoagulability and lactation. - in the first 21 days postpartum estrogen-containing hormonal contraceptives should be avoided if possible. - Progestin-only pills do not adversely affect milk production, so they can be used after 6 weeks postpartum. 29

- Patient should be informed about both common and serious side effects. - The

- Patient should be informed about both common and serious side effects. - The benefits and risks should be discussed in terms that the patient can understand, including the fact that OCs provide no physical barrier to the transmission of STDs, including HIV. - OCs Should be taken at approximately the same time every day, and the first pill on the first day of the next menstrual cycle. 30

 Side effects : - breakthrough bleeding …. . . Less in biphasic and

Side effects : - breakthrough bleeding …. . . Less in biphasic and triphasic combined products - Acne …… exacerbate by progestins more than estrogens - weight gain…. More with progestins, modify diet - Headache, migraine …. . D/C therapy with migraine 31

- nausea; stomach cramps and bloating; vomiting …… shift to product contains small amount

- nausea; stomach cramps and bloating; vomiting …… shift to product contains small amount of estrogen - Breast pain , lumps, or discharge …. Occurs with high doses of estrogen or progestin - Amenorrhea …. . Increased with low progestin compounds - vision changes 32

Reference: Pharmacotherapy, Pathophysiologic Approach, 10 th edition, 2017 33

Reference: Pharmacotherapy, Pathophysiologic Approach, 10 th edition, 2017 33

 Drugs interactions • Anticonvulsants: barbiturates, carbamazepine; phenytoin Decreased contraceptive effect by inducing OCs

Drugs interactions • Anticonvulsants: barbiturates, carbamazepine; phenytoin Decreased contraceptive effect by inducing OCs metabolism …. Use OCs containing 50 mcg ethinyl estradiol and a second method of contraception or IUD. • Protease inhibitors: amprenavir, ritonavir Increased or decreased contraceptive Effect, Use IUD 34

 • Rifampin: Decreased contraceptive effect by inducing metabolism of OCs ……Use alternate method

• Rifampin: Decreased contraceptive effect by inducing metabolism of OCs ……Use alternate method (IUD) if concomitant use is long term • Ampicillin and doxycycline : which may cause problems "by impairing the bacterial flora responsible for recycling ethinyl estradiol from the large bowel 35

Parental contraceptives Progestins are used in existing injectable and implantable contraceptives. Mechanism: blocks LH,

Parental contraceptives Progestins are used in existing injectable and implantable contraceptives. Mechanism: blocks LH, thus preventing ovulation, reduces ovum motility in the fallopian tubes, thin the endometrium, reducing the chance of implantation, thicken the cervical mucus so producing a barrier to sperm penetration 36

 Used in: breast-feeding, intolerance to estrogens (i. e. , have a history of

Used in: breast-feeding, intolerance to estrogens (i. e. , have a history of estrogen-related headache, breast tenderness, or nausea), and those with concomitant medical conditions in which estrogen is not recommended (Ex: vascular or stroke). Depot Medroxy_progesterone acetate (DMPA )is administered by deep intramuscular injection within 5 days of onset of menstrual bleeding and inhibits ovulation for more than 3 months. 37

 • Used 6 weeks after postpartum for breastfeeding women • These long-acting methods

• Used 6 weeks after postpartum for breastfeeding women • These long-acting methods of contraception do not provide any protection from STDs. • (Depo-Provera) https: //drjengunter. wordpress. com/ 38

Implemented devices 1. Implant: Small flexible rod put under the skin of the upper

Implemented devices 1. Implant: Small flexible rod put under the skin of the upper arm. Releases the progestogen. it thickens cervical mucus to prevent sperm reaching an egg, and thins the lining of the uterus to prevent a fertilized egg implanting. • Works for 3 years. Periods may stop, be irregular. Acne may occur, or worsen. It requires a small procedure to fit and remove it. https: //askthegynaedoctor. com/birth-control-series-emphasis-on-implant/ 39

2. Intrauterine system (IUS): A small T-shaped plastic device, slowly releases the progestogen, has

2. Intrauterine system (IUS): A small T-shaped plastic device, slowly releases the progestogen, has the same mechanism of implant. Works for 5 years. Periods usually become lighter, shorter and sometimes less painful. Irregular bleeding or spotting is common in the first 6 months. Insertion can be uncomfortable https: //openi. nlm. nih. gov 40

3. Intrauterine device (IUD) A small copper (Copper T) or hormonal (Mirena) device is

3. Intrauterine device (IUD) A small copper (Copper T) or hormonal (Mirena) device is put into the uterus. It stops sperm reaching an egg, copper is toxic to sperms, and may also stop a fertilized egg implanting in the uterus. Can stay in 5– 10 y, May not be suitable for women at risk of getting a STD. Periods may be heavier or longer and more painful. Very small chance of getting an infection during the first 20 days after insertion. Insertion can be uncomfortable. 41

transdermal patches • The transdermal patch contains estrogen and norelgestromin, the active metabolite of

transdermal patches • The transdermal patch contains estrogen and norelgestromin, the active metabolite of norgestimate. • stuck on the skin releases two hormones, It stops ovulation, thickens cervical mucus to prevent sperm reaching an egg, and thins the lining of the uterus to prevent a fertilized egg implanting. 42

 • Not suitable for very over weight women or smokers over 35 years.

• Not suitable for very over weight women or smokers over 35 years. • Low risk of serious side-effects such as blood clots, breast and cervical cancer. • Temporary side-effects such as headaches, nausea, mood changes and breast tenderness. • Possible skin irritation 43

Case 1 (combination hormonal contraceptives ) • S. F. , a healthy 33 -year-old

Case 1 (combination hormonal contraceptives ) • S. F. , a healthy 33 -year-old woman, presents to clinic stating she is getting married soon and would like birth control pills as a method of contraception. • She does not have children but would like to start a family in a year or two. • Her past medical history : occasional headaches for which she takes ibuprofen 200 mg (PO) as needed. 44

 • Vital signs: Blood pressure, 122/72 mm Hg • Weight: 65 kg, Height:

• Vital signs: Blood pressure, 122/72 mm Hg • Weight: 65 kg, Height: 170 cm • Heart rate, 85 beats/minute • Temperature, 37. 2 C • Social history: Smokes 1 pack per day, denies alcohol • Family history: Sister gestational diabetes, mother hypertension 45

 • CASE 2 • D. S. comes to the family planning clinic after

• CASE 2 • D. S. comes to the family planning clinic after taking EE 20 mcg/drospirenone 3 mg (YAZ) for 2 months. She had been started on YAZ to help with her acne. She feels her acne has improved but reports irregular menstrual bleeding during her last two menstrual cycles that occurs around the third week of the pill pack, and has daily headaches during her placebo week but not when she is taking active pills. 46

 • Q 1: How should she be managed? • Most clinicians will recommend

• Q 1: How should she be managed? • Most clinicians will recommend that patients continue the same COC for at least 3 months if breakthrough bleeding or spotting is the only complaint because this complication usually resolves within 3 months. • The balance between estrogen and progestin components in COCs determines its endometrial activity and, therefore, the likelihood of intermenstrual bleeding problems. • If D. S. ’s intermenstrual bleeding continues late in her cycle after 3 months, another COC with the same estrogen activity, more progestin activity, and low androgen activity should be prescribed If D. S. had experienced intermenstrual bleeding early in the cycle after several months of use, she should be changed to a formulation with a higher ratio of estrogen to progestin 47

Headache • May be related to sensitivity of estrogen or during the placebo week

Headache • May be related to sensitivity of estrogen or during the placebo week as a result of the withdrawal of estrogen • Women with migraines may find that their headaches either improve or worsen when CHCs are initiated. • Mild headaches may improve with time or if the woman is changed to a pill with less estrogen or progestin. • Patients with severe headaches should discontinue CHCs and should be evaluated by their health care provider • headaches during the placebo week …. Skipping the placebo pills and using an extended-cycle regimen may help decrease headaches. 48

Intrauterine device (IUD), intrauterine system (IUS), The contraceptive implant • CASE 3 • P.

Intrauterine device (IUD), intrauterine system (IUS), The contraceptive implant • CASE 3 • P. K. is a 35 -year-old woman who concerned about weight gain and is not interested in a subdermal implant. • What other long-term, reversible contraceptive methods might work for her? • Is P. K. a candidate for an intrauterine device (IUD) or intrauterine system (IUS) • What information would you provide her? 49

References Pharmacotherapy, Pathophysiologic Approach, 10 th edition, 2017 Applied Therapeutics, 10 th ed, Koda-Kimble,

References Pharmacotherapy, Pathophysiologic Approach, 10 th edition, 2017 Applied Therapeutics, 10 th ed, Koda-Kimble, 2013 Contraceptive Use in the United States, 2013, G institute your guide to contraception, 2012 barrier methods of contraception, the American collage of obstetricians and gynecologists, 2011 pharmacology , 4 th edition, Lippincott's 2009 Hormonal contraception, pharmacist letter , 2006 basic and clinical pharmacology, 8 th edition, katzung 2001 www. thefreedictionary. com 50