Yes

Contraceptive

Prevention of pregnancy; treatment of hypermenorrhea, endometriosis, female hypogonadism [monophasic oral contraceptive]

X

Known or suspected breast cancer, undiagnosed abnormal vaginal bleeding, carcinoma of the breast, estrogen-dependent tumor, pregnancy

Use with caution in patients with a history of thromboembolism, stroke, myocardial infarction, liver tumor, hypertension, cardiac, renal or hepatic insufficiency; use of any progestin during the first 4 months of pregnancy is not recommended; risk of cardiovascular side effects increases in those women who smoke cigarettes and in women >35 years of age

>10%:

Cardiovascular: Peripheral edema

Central nervous system: Headache

Endocrine: Enlargement of breasts, breast tenderness, increased libido

Gastrointestinal: Nausea, anorexia, bloating

1% to 10%: Gastrointestinal: Vomiting, diarrhea

<1%: Hypertension, thromboembolism, edema, stroke, myocardial infarction, depression, dizziness, anxiety, chloasma, melasma, rash, decreased glucose tolerance, amenorrhea, alterations in frequency and flow of menses, increased triglycerides and LDL, GI distress, cholestatic jaundice, intolerance to contact lenses, increased susceptibility to Candida infection, breast tumors

Hormonal Balance in Oral Contraceptives:

Estrogen Excess: Nausea, bloating, cervical mucorrhea, polyposis, melasma, migraine headache, breast fullness or tenderness, edema, hypertension

Estrogen Deficiency: Early or midcycle breakthrough bleeding, increased spotting, hypomenorrhea

Progestin Excess: Increased appetite, weight gain, tiredness, fatigue, hypomenorrhea, acne, oily scalp*, hair loss, hirsutism*, depression, monilial vaginitis, breast regression

Progestin Deficiency: Late breakthrough bleeding, amenorrhea, hypermenorrhea

*Result of androgenic activity of progestins

Pharmacological effects of progestins used in oral contraceptives:

Norgestrel/levonorgestrel:

Progestin: Pronounced effect

Estrogen: No effect

Antiestrogen: Moderate effect

Androgen: Pronounced effect

Ethynodiol diacetate:

Progestin: Moderate effect

Estrogen: Slight effect*

Antiestrogen: Slight effect*

Androgen: Slight effect

Norethindrone acetate:

Progestin: Slight effect

Estrogen: Slight effect

Antiestrogen: Pronounced effect

Androgen: Slight effect

Norethindrone:

Progestin: Slight effect

Estrogen: Slight effect*

Antiestrogen +*

Androgen: Slight effect

Norethynodrel:

Progestin: Slight effect

Estrogen: Pronounced effect

Antiestrogen: No effect

Androgen: No effect

*Has estrogenic effect at low doses; may have antiestrogenic effect at higher doses.

Toxicity is unlikely following single exposures of excessive doses

Any treatment following emesis and charcoal administration should be supportive and symptomatic

Decreased effect:

Tetracyclines, penicillins, griseofulvin, rifampin, acetaminophen, barbiturates, hydantoins may increase contraceptive failures

Decreases acetaminophen, estrogen levels, and anticoagulants

Increased toxicity: Increases benzodiazepines, caffeine, metoprolol, theophyllines, and tricyclic antidepressants

Combination oral contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary. The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, oral contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Oral contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility.

Adults: Female: Oral:

One dose missed: Take as soon as remembered or take 2 tablets next day

Two doses missed: Take 2 tablets as soon as remembered or 2 tablets next 2 days

Three doses missed: Begin new compact of tablets starting on day 1 of next cycle

Should be administered with food at same time each day

May cause anxiety or depression

Hepatic metabolism of TCAs, benzodiazepines (oxidatively metabolized) and beta-blockers may be decreased by oral contraceptives; monitor increased/toxic effects; may increase the clearance of benzodiazepines (glucuronidation); barbiturates may increase the metabolism of oral contraceptives resulting in decreased effectiveness

No information available to require special precautions

When prescribing antibiotics, patients must be advised to use additional methods of birth control when taking oral contraceptives

Take exactly as directed; use additional method of birth control during first week of administration of first cycle; photosensitivity may occur

Women should be advised that if they miss one daily dose, they should take the tablet as soon as remembered. If 2 daily doses are missed, 2 tablets should be taken daily for 2 days and the regular schedule resumed. If 3 or more daily doses are missed, therapy should be discontinued. Therapy with a new cycle can be resumed in 7 or 8 days. When any doses are missed, alternative contraceptive methods should be used for the next 2 days or until 2 days into the new cycle.

Women should discontinue taking the medication if they suspect they are pregnant or become pregnant

Administer at bedtime to minimize occurrence of adverse effects

Tablet: Mestranol 0.05 mg and norethindrone 1 mg (21s and 28s)