Adult Dosing

Contraception

ethinyl estradiol 0.03 mg/norgestrel 0.3 mg

• 1 tab PO qd
• Start first active tablet on day 1 of menstrual cycle or 1st Sunday after onset of menses x 21 days, followed by inert tablets x 7 days or 7 days drug free interval
• Start subsequent courses of tablets on the day after taking last inert tablet or after 7 days of last active tablets

ethinyl estradiol 0.05 mg/norgestrel 0.5 mg

• 1 tab PO qd
• Start first active tablet on day 1 of menstrual cycle or 1st Sunday after onset of menses x 21 days, followed by inert tablets x 7 days
• Start subsequent courses of tablets on the day after taking last inert tablet

• Tablets to be taken at the same time each day
• During the first cycle of medication ask patient to use nonhormonal back-up method of birth control for 7 consecutive days of starting the tablet

Pediatric Dosing

Contraception

ethinyl estradiol 0.03 mg/norgestrel 0.3 mg

• 1 tab PO qd
• Start first active tablet on day 1 of menstrual cycle or 1st Sunday after onset of menses x 21 days, followed by inert tablets x 7 days or 7 days drug free interval
• Start subsequent courses of tablets on the day after taking last inert tablet or after 7 days of last active tablets

ethinyl estradiol 0.05 mg/norgestrel 0.5 mg

• 1 tab PO qd
• Start first active tablet on day 1 of menstrual cycle or 1st Sunday after onset of menses x 21 days, followed by inert tablets x 7 days
• Start subsequent courses of tablets on the day after taking last inert tablet

• Tablets to be taken at the same time each day
• During the first cycle of medication ask patient to use nonhormonal back-up method of birth control for 7 consecutive days of starting the tablet

[Outline]

• Adult Dosing
• Pediatric Dosing

• Prevention of pregnancy

• Hypersensitivity to any of the ingredients of the product
• Thrombophlebitis or thromboembolic disorders
• History of deep-vein thrombophlebitis or thromboembolic disorders
• Cerebrovascular or coronary artery disease (current or past history)
• Valvular heart disease with thrombogenesis
• Thrombogenic rhythm disorders
• Hereditary or acquired thrombophilias
• Major surgery with prolonged immobilization
• Diabetes with vascular involvement
• Headaches with focal neurological symptoms
• Uncontrolled hypertension
• Known or suspected or history of carcinoma of the breast
• Carcinoma of the endometrium or other known or suspected estrogen-dependent neoplasia
• Undiagnosed abnormal genital bleeding
• Cholestatic jaundice of pregnancy or jaundice with prior use of pill
• Hepatic adenomas or carcinomas
• Active liver disease
• Known or suspected pregnancy

• Women using oral contraceptives should be strongly advised not to smoke, as cigarette smoking increases the risk of serious cardiovascular side effects in these women. The risk further increases with age and with the extent of smoking (15 cigarettes/day) and is quite marked in women over 35 years of age

Renal Dose Adjustment

• Severe renal impairment: Use with caution, dose adjustments not defined

Hepatic Dose Adjustment

• Active hepatic disease: Contraindicated

See Supplemental Patient Information

• Cigarette smokers are more prone to risk of serious cardiovascular side effects due to oral contraceptives. Advise women who use contraceptives to avoid smoking [US Black Box Warning]
• Oral contraceptives can contribute to risk factors such as hypertension, diabetes, hyperlipidemias, obesity; these risk factors have been associated with an increased risk of heart disease. Use cautiously in women with cardiovascular disease risk factors
• Increased risk of thromboembolic and thrombotic disease has been reported with use of OCP; risk of post-operative thromboembolic complications increases on use of use of oral contraceptives. Discontinue use at least 4 weeks prior to and for 2 weeks after elective surgery and during and following prolonged immobilization; initiate use not earlier than 4 to 6 weeks after delivery in women electing not to breast feed
• Increases risk of cerebrovascular events (thrombotic and hemorrhagic strokes). Age >35 yrs and hypertension are the risk factor for hemorrhagic strokes
• Decrease in serum HDL is associated with an increased risk of ischemic heart disease. As progestational agents decreases serum HDL, and estrogens increase HDL cholesterol, the net effect of an oral contraceptive depends on a balance achieved between doses of estrogen and progestogen and the nature and absolute amount of progestogen used in the contraceptive
• Individualized dosage in a way that it contains the least amount of estrogen and progestogen that is compatible with a low failure rate; start on preparations containing the lowest estrogen content producing satisfactory results
• Prolong use of OCP containing 50 mcg or higher estrogens, shown to cause persistence risk of vascular diseases
• Oral contraceptives increase the risk of breast and cervical cancer. Discontinuation of OCP decreases the risk. Do not use in females with known or suspected carcinoma of the breast or personal history of breast cancer
• Rarely fatal benign hepatic adenomas have been reported with oral contraceptive use. Rupture of these benign hepatic adenomas can cause intra-abdominal hemorrhage leading to death
• Oral contraceptives can cause retinal thrombosis leading to partial or complete loss of vision. Discontinue the drug if there is unexplained partial or complete loss of vision; onset of proptosis or diplopia; papilledema; or retinal vascular lesions and provide appropriate measures
• Do not use during pregnancy to treat threatened or habitual abortion
• Combination oral contraceptives may worsen existing gallbladder disease and may accelerate the development of this disease in previously asymptomatic women
• Estrogens at higher dose >75 mcg causes hyperinsulinism, while lower doses cause less glucose intolerance and progestogens increase insulin secretion and create insulin resistance. Hence use cautiously in prediabetic and diabetic women with careful monitoring
• Hypertension may occur; closely monitor hypertensive women electing to use oral contraceptives. Discontinue use in women with significant elevation of blood pressure
• Discontinue therapy on onset or exacerbation of migraine, development of new pattern headache that is recurrent, persistent or severe
• Bleeding irregularities especially during the first 3 months may occur. Consider non-hormonal and adequate diagnostic measures to rule out malignancy/pregnancy in the event of breakthrough bleeding or any abnormal vaginal bleeding
• Counsel the patients that this product does not protect against HIV infection (AIDS) and other sexually transmitted diseases
• Consider physical examination and follow up in relevance to blood pressure, breasts, abdomen and pelvic organs, including cervical cytology, and perform relevant laboratory tests in all the women taking OCP
• Carefully monitor women with a strong family history of breast cancer or having breast nodules
• Closely monitor women who are being treated for hyperlipidemias. Consider nonhormonal contraception in women with uncontrolled dyslipidemias
• OCP can cause fluid retension; Use cautiously with careful monitoring, in patients with conditions which might be aggravated by fluid retention
• Closely monitor the women with a history of depression, discontinue use if depression recurs to a serious degree

Cautions: Use cautiously in

• Renal impairment
• Hepatic impairment
• Hypertension
• Hyperlipidemia
• Cardiovascular disease risk factors
• Diabetes mellitus
• Hypercholesterolemia
• Sensitive to fluid retention
• History of depression
• Migraine
• Gallbladder diseases
• Headaches without neurologic symptoms

Supplemental Patient Information

• Inform patients that this product does not protect against HIV infection (AIDS) and other sexually transmitted diseases
• Instruct patients to take pill exactly as directed and at intervals not exceeding 24 hrs
• Advise women to use an additional method of protection until after the first 7 days of administration in the initial cycle
• Inform patients to start oral contraceptives no earlier than 4 to 6 weeks after delivery due to its association with an increased risk of thromboembolism. On termination of pregnancy, instruct patients to start oral contraceptives immediately or within 7 days after termination
• Advise patients to report physician on spotting or persisting breakthrough bleeding
• On missing one pill, instruct patients to take it as soon as they remember and then to take the next pill at the regular time
• Educate patients that missing a pill would cause spotting or light bleeding, and they may experience gastric irritation if they take the missed pill along with their regularly scheduled pill
• In case of a missed menstrual period, inform patients to consider the possibility of pregnancy, withholding oral contraceptives until pregnancy has been ruled out. Instruct patients to rule out pregnancy before continuing the contraceptive regimen even in patients who have adhered to the prescribed regimen but missed 2 consecutive periods

Pregnancy Category:X

Breastfeeding: Combination oral contraceptives probably do not affect the composition of milk substantially in healthy, well-nourished mothers and do not adversely affect long-term infant growth and development, but can transiently affect growth during the first month after introduction. Rarely reversible breast enlargement has been reported with higher dose of estrogen. Ethinyl estradiol in doses of 30 mcg daily or greater suppresses lactation leading to earlier discontinuation of breastfeeding, than nonhormonal or progestin-only contraception. The magnitude of the effect on lactation depends on the dose and the time of introduction postpartum. As per US expert opinion the risks of combination contraceptive products usually outweigh the benefits before 4 weeks postpartum. Between 4 weeks and 6 months postpartum, the advantages of using the method generally outweigh the theoretical or proven risks. After 6 months postpartum, combination contraceptives can be used, but progestin-only methods are preferred if breastfeeding will be continued. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 27 June 2011).Small amounts of oral contraceptive steroids are excreted in milk of nursing mothers and a few adverse effects on the child have occurred, including jaundice and breast enlargement. Oral contraceptives given in the postpartum period may interfere with lactation by decreasing the quantity and quality of breast milk. Manufacturer advises the nursing mother to avoid use of oral contraceptives and the use other forms of contraception until she has completely weaned her child.

• CV: Thrombophlebitis, MI, cerebral thrombosis, cerebral hemorrhage, coronary thrombosis, pulmonary embolism, edema, hypertension, thromboembolic phenomena, arterial thromboembolism, varicose veins
• CNS: Migraine, exacerbation of chorea, dizziness, mood changes, nervousness
• GI: Colitis, abdominal cramps, bloating, gallbladder disease, mesentric thrombosis, pancreatitis, nausea, vomiting
• HEPA: Budd-Chiari syndrome, hepatic adenoma, hepatic carcinomas, benign liver tumors, cholestatic jaundice
• EENT: Contact lens intolerance, ocular lesions, optic neuritis, retinal thrombosis, cataracts, changes in corneal curvature
• REPRODUCTIVE: Cancer of reproductive organ, amenorrhea, altered menstrual flow, breakthrough bleeding, dysmenorrhea, spotting, cervical erosion and secretion, vaginal candidiasis, vaginitis, decreased lactation, changes in libido, breast tenderness, breast enlargement, breast secretion, temporary infertility
• GU: Cystitis-like syndrome, hemolytic uremic syndrome, impaired renal function, fluid retention
• DERM: Acne, erythema multiforme, erythema nodosum, focal nodular, rash hyperplasia, hirsutism, melasma/chloasma, loss of scalp hair
• MISC: Anaphylactic/anaphylactoid reactions (urticaria, angioedema, and severe respiratory and circulatory reactions), exacerbation of porphyria, exacerbation of SLE

Ethinyl estradiol

• Estrogen; suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH). inhibits ovulation and alters cervical mucus and the endometrial environment, preventing penetration by sperm and implantation of the egg
• Metabolized by liver; CYP450: 3A4 substrate
• Excreted in urine and feces
• Half-life: 18+/-4.7 hrs

Norgestrel

• Contraceptive agent; binds to the receptors and slow down the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge
• Metabolized by liver
• Excretion: Unknown
• Half-life: 5-14 hrs

US Trade Name(s)

• Cryselle
• Elinest
• Lo/Ovral-28
• Low-Ogestrel
• Ogestrel

US Availability

Cryselle, Low-Ogestrel (ethinyl estradiol/norgestrel) (generic drug)

• TABS: 0.03 mg/0.3 mg (21 tabs)
• TABS: 0.03 mg/0.3 mg (21 tabs), 7 inert tabs

Elinest, Lo/Ovral-28 (ethinyl estradiol/norgestrel)

• TABS: 0.03 mg/0.3 mg (21 tabs), 7 inert tabs

Ogestrel (ethinyl estradiol/norgestrel)

• TABS: 0.05 mg/0.5 mg (21 tabs), 7 inert tabs

Canadian Trade Name(s)

• Lo-Femenal 21
• Lo-Femenal 28

Canadian Availability

Lo-Femenal 21 (ethinyl estradiol/norgestrel)

• TABS: 30 mcg/300 mcg (21 tabs)

Lo-Femenal 28 (ethinyl estradiol/norgestrel)

• TABS: 30 mcg/300 mcg (21 tabs), 7 inert tabs

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

[Outline]

Obstetrics/Gynecology

Contraceptives

Estrogen And Progestin Combination

Pricing data from www.DrugStore.com in U.S.A.

• Cryselle-28 0.3-30 MG-MCG TABS [Disp Pack] (TEVA PHARMACEUTICALS USA)
  28 mg-mcg = $29.99
  84 mg-mcg = $79.97
• Low-Ogestrel 0.3-30 MG-MCG TABS [Disp Pack] (WATSON LABS)
  28 mg-mcg = $31.99
  84 mg-mcg = $75.97
• Ogestrel 0.5-50 MG-MCG TABS [Disp Pack] (WATSON LABS)
  28 mg-mcg = $44.99
  84 mg-mcg = $119.97

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

Drug Name: Low-Ogestrel 28 Day Pack

Ingredient(s): Ethinyl Estradiol mixture with Inert Ingredients and Norgestrel

Imprint: P1;WATSON

Color(s): Orange

Shape: Round

Size (mm): 6.00

Score: 1

Inactive Ingredient(s): anhydrous lactose / fd&c yellow no. 6 lake / magnesium stearate / microcrystalline cellulose

Drug Label Author:
WATSON PHARMA, INC.

DEA Schedule:
Non-Scheduled