Pharmacology Test 3 - Oral Contraceptive Pills

Risks and Benefits: of Estrogen and Progestin - Risks

Headache Blood Clots Thrombophlebitis Cerebral Hemorrhage Hypertension MI Gall bladder disease Depression Edema Acne Hair loss

Drospirenone has WHAT type of androgenic effect?

LESS androgenic effect!

POP Progestin Types: 1. _______(in Micronor) 2. _________ (in Overette). - POPS MUST be taken at the SAME TIME every day! Taking pills irregularly results in pregnancy. Backup contraception may be used if a pill is MISSED.

Norethinedrone; Norgestrel

Women whom have a history of migraine HA, uterine fibroids, fibrocystic breasts, heavy menses or nausea, edema, or hypertension in pregnancy - What is something to consider with this persons when giving an OC?

OC with lower estrogen content (EG - Alese or Loestrin 21 1/20)

Skyla:

and IUD is also available and releases LNG (levonorgestrel)

Most OCPs have SOME ________activity

androgenic (More recent generations have less androgen components (helpful for women with hirsutism or acne)

OCP safety: Safe for women with benign breast disease. NOT safe for women with a history or _____ or ______ cancer. Safe in those with mild lupus without antiphospholipid antibodies. Consultation with a specialist is recommended

breast; ovarian

Disadvantages of Nuva ring:

headache, vaginitis, nausea, breast tenderness, expulsion, feel the ring during intercourse, - can remove during intercourse but must reinsert within 3 hour window - risk of blood clots, even with lower hormone levels.

Progestins: The second hormone in combinded oral contraceptives. Different progestin formulations in hormone systems, each has different progestational, estrogenic, and adrogenic activity. Newer progestins have _________. Adrogen causes ________.

less androgen; acne, hirsutism, nausea, and can affect lipids.

Combined OCPs (COC): Contain BOTH estrogen and Progestin! They work by __________. Progesterone component alters cervical mucus making it _________. Overall it causes the endometrium to be less hospitable for implantation

preventing ovulation and inhibiting the normal midcycle surge of pituitary gonadotropins. Difficult for sperm to penetrate

Low-dose progesterone (e.g., Brevicon): can be used for women with a history of what?

varicosities in pregnancy, preeclampsia, excess weight gain, fatigue, depression, and premenstraul syndrome

Quick start depo:

Perfomed ONLY if patient (presenting beyond 5 days after menses) tests negative on serum (NOT URINE) HCG pregancy test. If patient had unprotected sex within past 5 days, emergency contraception pills are given in office. Use of condoms for 7 days is advised, along with follow up in 2-3 weeks for another pregnancy test

Disadvantages of the Patch:

- Not as effective in women who weight more than 198 lbs - increase in blood clots - more expensive than oral contraceptives - breakthrough bleeding - suboptimal privacy because it's visible at times - detachment issues for some - same potential for health complications as contraceptive pill

Disadvantages of Implanon

-Irregular bleeding -Weight gain -Headaches -Acne eruption -Nausea -Mood swings -Local reactions -Risk of blood clots

Advantages of Nuva ring:

Conveinent, works well, fewer problems with breakthrough bleeding, not as bothersome as taking medicine every day - teens do no like to use this method

Monophasic OCPs have a ________.

Constant dose of estrogen and progestin for 21 days.

Estrogen suppresses _______. Speeds ovum transport, decreasing fertilization time. Affects uterus to discourage implantation.

FSH and LH release

Side Effects of Depo:

weight gain, mood swings, breast tenderness, delayed return to fertility, decrease in bone density (most concerning) - counseling needed about adequate calcium intake not recommended for use beyond 2 years Decreases HDLs (good cholestrol), LdLs (low-density lipoprotein and total cholestrol

Taking OC's : The First MOnth: Quick start: _______ First day: ________ Sunday Start: _________

- Patient takes her first dose the day you see her. Uses back up contraception for the first week. - Patient takes the first pill on first day of next menstrual period; no back up birth control is needed. - Advantage - patient won't have period on the weekend; patient takes first pill on first sunday after period starts. Use backup birth control for 7 days

Seasonique: Lo Seasonique:

- Takes pill (EE 30mcg and levonogestrel 0.15mg) eary day for 12 weeks. In the 13th week they take daily pill with only 10mcg of EE. Seasonique users have only 4 withdrawal bleeds a year. - is taken each day for 91 days the first 84 days contain 0.02 mg of EE and 0.1 mg of levonorgestrel. The last 7 tabs only contain 0.01mg of EE. Lo seasonique can have more episodes of breakthrough bleeding which stops women from taking it

TOP CHOICES : Ortho Tri-cyclen: Alesse: Mircette, Loestrin 1/20: Yasmin: Cyclessa:

- good for young, nonsmokers - 20mcg estrogen - 20mcg estrogen - May cause hyperkalemia/mood swings - newer triphasic

MANIPULATING CYCLES

- taking 21 active pills in one pill pack, discarding placebo pills and starting second pack immediately; patient takes all pills in second pack including placebo - taking all active hormone pills from three packs and discarding the placebos from the first 2 packs - patient takes all pills in third pack including placebos

Mirena

ALso a Tshaped but releases 20mg of levonorgestrel (LNG) into the uterus daily - affects sperm motility and causes inflammatory response which atrophies lining of uterus - Lasts for 5 years and is very effective

When NOT to use Plan B :

Allergy ; allergic reaction such as angioedema, or hypersensitivity that occured in past. Known pregnancy. Undiagnosed vaginal bleeding

CLASSIFYING PROGESTINS: LATER-generation progestins are less _______and have INCREASED progestational activity. Can be classified as estranes or gonanes (testosterone derivatives). Exception: ___________. Derivation from estranes/gonanes does NOT describe pharmacological activity. TWO pills could have the same mg of progestines but their intrinsic potency could be DIFFERENT due to the type of _______.

Androgenic ; Drospirenone is a derivative of aldactone; PROGESTIN

Contraindications for OCPs :

Cardiovascular ischemia, atrial fibrillation, strokes, CAD, Heart failure, previous history of blood clots, or ovarian/breast cancer Smoker over 35 years old Pregnant Liver tumor, liver disease, hepatic adenoma, renal dysfunction, or undiagnosed genital bleeding Uncontrolled hypertension: SBP >160; DBP >100 Uncontrolled DM or who have complications associated with diabetes

Plan B Mechanism of Action: -Remember Plan B does NOT work if patient is pregnant. Check for pregnancy even though studies have shown no serious harm to pregnant patients.

Cervical mucus is thickened preventing sperm passage. Ovulation may be inhibited due to negative feedback system affecting hypothalamus. Decreased secretion of FSH and LH, possibly preventing implantion.

Side Effects of IUD :

Early - on complaints of bleeding and some cramping Uterine perforation can occur especially with insertion No loss of bone density Expulsion may occur but usually within first month - WOmen are encouraged to feel for string monthly and alert provider if not tangible/seen. - ALthough rare to not see string, providers shouldn't assume device was expelled. If no string is seen upon examination, order sonogram of uterus If no device is seen on sonogram order CT scan of pelvis and abdomen

Estrogen and Progestin in Oral Contraceptives: Estrogen-progesterone oral contraceptives work by suppressing ___________releasing factor.

Hypothalamic

STOP USING OCPs when:

Headache pattern changes, more frequent or more severe Age over 35 and a smoker Renal dysfunction Pregnancy Severe liver disease or hepatic adenoma

Candidates for OCPs :

Healthy, nonsmoking women under 55 - if hypertension, diabetes, or dyslipidemia is well controlled Women with depression or migraine, if monitored Red flags for migraine patients: - Family history of aneurysm or blood clots -Request a neuro exam Women with depression or dyslipidemia should be monitored

About Implanon:

Implanted rod containing 68mg of etonogestrel Inserted into medial surface of upper arm 6-8cm from elbow, in biceps groove within 5 days of onset of menses Defers contrception for 3 years and can then be replaced

Decreased Estrogen in OCPs : What they do to the body -

Increased breakthrough bleeding ; Uncertain effectiveness; Earlier pills with more estrogen anecdotally resulted in LESS bleeding and FEWER pregnancies. Important to take the PILL at the same TIME every day LOWER estrogen may result in Pregnancy if ONE PILL is skipped!

OCP side Effects and OTHER NOTABLES: Dosage: Usually start with_______. E.G., 20-35mcg of estrogen (EE) plus progestin, low androgenicity. Advantage: shorter menses, (less than 3 days), increased suppression of follicular development. If a patient weights over 160 lbs what should you consider?

Lower dose and titrate UP ; INCREASING the dosage, May need OC with higher amounts of estrogen and progesteron (Demulen or OrthoCept)

Progestin: Inhibits ovulation by suppressing release of _________. Creates a thick cervical mucus barrier to retard ___________ of the ovum.

Luteinizing hormone; sperm transport/inhibit penetration

Three basic types of OCPs :

Monophasic; Biphasic; and Triphasic

Other Considerations for OCPs:

Past medical history of jaundice while on OCPs or cholestatic jaundice during pregnancy - Obesity/age increase risk of blood clots -STOP OCP therapy 4 to 6 weeks before an elective surgery or be certain the patient receives heparin prophylaxis

Pill Regimens : Different pill variations:

Patient takes a pill for 21 days, stops for a week, and then restarts a new pill pack.(increased likelyhood of forgetting to restart pills) Daily pill regimens - 28-day pill pack 21days of active medication and 6 or 7 days of placebo Seasonale: 90-day cycle Lybrel: One year cycle

Starting the Nuva ring:

Place within 5 days of menses onset After 3 weeks remove for 7 days to allow withdrawal bleeding. If left in for the 4th week pregnancy should be ruled out, a new ring iserted, and patient will need to use barrier contraception. Can be a delayed return to fertility. If expelled, it can be washed in lukewarm water and reinserted within 3 hours without decreased effecacy. - If out longer than 3 hours and reinserted, backup birth control is necessary for 7 days

DEPO's Effects:

Prevents ovulation by blocking positive feedback or estradiol on the pituitary, eliminating LH surge Decreases and thickens cervical mucus Causes endometrial change less favorable to implantation

Patient F/U with OC: Three month check up: _________. Patients should be informed about STDs and the need for condoms. The pill provides protection against pregnancy, not STDs including HIV/AIDS. HIV infection is spreading at a rate of one person every 9 minutes!

Review of systems, ACHES, blood pressure, and eye check

Risks and Benefits: of Estrogen and Progestin - Benefits:

Safe and effective; Less menstrual bleeding/risk of anemia

Extended Cycle Contraceptives: 1_______ 2_________ 3________. Long-term safety is unknown. 21 and 28 day cycle packs have been studied and found safe over a much longer period of time

Seasonique, Seaonale, and Lybrel

Danger SIGNS of an OC: Discuss signs requiring an IMMEDIATE call to the nurse practitioner, doctor, or visit to the ER. ACHES: ______________. These are potential signs of serious side effects

Severe ABDOMINAL pain CHEST pain HEADACHES EYE problems SWELLING and/or aching in the legs

Paragard :

T shaped device, wrapped in copper wire, good for 10 years Copper wire can cause inflammatory reaction in uterus to prevent implantation.

Brand-Name OCPs - What we need to know about them!:

They are expensive, Insurance frequently only covers generic pills, Insurance companies/pharmacies can substitute a pill with same hormonal content. Companies sometimes stop production of a drug.

PLAN B - emergency contraception pill most widely used - d/t nausea, Yuzpe method proved problematic. Plan B - one step is even easier; one dose, less nausea, more effective. If pain associated pt needs seen to r/o ________.

Tubal pregnancy

WHen to use plan B:

Unprotected intercourse Barrier contraceptive failure Diaphragm or cervical cap dislodgement, misinsertion, early removal, or torn barrier. Missing too many oral contraceptive pills

Nuva Ring:

Used 3 weeks on, 1 week off. Topical preparation, no first pass effect, and when used correctly - quite effective. Lower hormone levels than other contraceptives (EE less than progestin component) - Ovulation suppressed despite lower levels

Generations of the 19-nortestrosterone derivatives: First generation: __________; less androgenic than the second-generation progestins, more than the fourth generation. Second generation: _________. Includes Levonorgestrel and Norgesterel. Third generation: ____________; have the LEAST androgenic effects, but may INCREASE risk for blood clots. Generations of 17 a-spironolactone derivatives Fourth generation prototype YASMIN contains _______. Antimineralocorticoid acivity; possible risk of hyperkalemia!

estranes (Norethindrone); gonanes; gonanes, Desogestrel and Norgestimate; drospirenone

Biphasic have 2 different combinations of _______. Biphasic have 3 different combinations. Progestin may ________ in steps during the cycle. Estrogen amounts may alter during the cycle. and Estrosept holds _________ constant, increases estrogen late in the cycle. ALL designed to model normal menstrual patterns.

estrogen; progestin - increase - progestin

Starting someone on an OC: What should you know about the patient before you begin prescribing?

history, including smoking, last menstrual period, and family history. Determine any contraindications to hormonal contraception Consider the best hormonal preparation for the patient Discuss any associated s/e and what to do if the a pill is missed Explain the importance of taking contraceptives faithfully Take blood pressure, do physical exam, and give a pregnancy test

Emergency Contraception : The sooner an emergency contraception is used the more effective it becomes. Yuzpe method as estrogen component, which can cause nausea. When ordering Yuzpe you should also order _________. NP will order two tablets each of 50mcg ethiyl estradiol and 250mcg levonorgestrel, given 12 hours apart, within 72 hours of unprotected intercourse. Oral generics can also be used. (Two tablets of Ovral or Ogestrel, or four tablets of Lo-Ovral, Levlen, or Nordette.)

meclizine (50mcg) or Metoclopramide (10mcg) to calm stomachs. Benadryl can also be given.