Ethinyl Estradiol/Levonorgestrel (oral contraceptive)

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[edit] BRAND NAMES

[edit] STRUCTURE

[edit] MECHANISM OF ACTION

Combination oral contraceptives, containing both estrogen and progestins, act by suppression of gonadotropins (FSH and LH). Although the primary mechanism of this action is inhibition of ovulation, other alterations include changes in the cervical mucus (which increase the difficulty of sperm entry into the uterus) and the endometrium (which reduce the likelihood of implantation).

[edit] INDICATIONS

Ethinyl Estradiol/Levonorgestrel combination is indicated for use by women to prevent pregnancy

[edit] DOSAGE

  • 28-day regimen of tablets: The possibility of ovulation and conception prior to initiation of medication should be considered.
    The patient should be instructed to begin taking Ethinyl Estradiol/Levonorgestrel tablets on either Day 1 of menstruation (Day 1 Start) or the first Sunday after the onset of menstruation (Sunday Start).
    Patient should take one tablet in the order directed on the package at the same time every day, preferably after the evening meal or at bedtime. The failure rate may increase when pills are missed or taken incorrectly.
    During the first cycle of Ethinyl Estradiol/Levonorgestrel, when beginning on the first Sunday after the onset of menstrual period, Ethinyl Estradiol/Levonorgestrel should not be considered effective as a contraceptive until after the first 7 consecutive days of product administration. Patients should use a non-hormonal contraceptive as back-up during the first 7 days.
    Patients should begin the next and all subsequent 28-day regimens of Ethinyl_Estradiol/Levonorgestrel on the same day of the week that they began their first regimen, following the same schedule.
  • 21-day regimen of tablets: begin taking Ethinyl Estradiol/Levonorgestrel tablets on Day 1 of menstruation. The dosage is one tablet daily for 21 consecutive days per menstrual cycle, according to the prescribed schedule. Tablets are then discontinued for 7 days (three weeks on, one week off). It is recommended that Ethinyl Estradiol/Levonorgestrel Tablets be taken at the same time each day, preferably after the evening meal or at bedtime

[edit] CONTRAINDICATIONS

  • A history of, or current deep vein thrombosis, thrombophlebitis or thromboembolic disorders; thrombogenic valvulopathies or thrombogenic rhythm disorders. Hereditary or acquired predisposition for venous or arterial thrombosis.
  • Cerebrovascular or coronary artery disease
  • Hepatic adenomas or carcinomas, cholestatic jaundice of pregnancy, jaundice with prior combined oral contraceptive use or active liver disease, as long as liver function has not returned to normal.
  • Known or suspected carcinoma of the breast or other known or suspected oestrogendependent neoplasias.
  • Diabetes with vascular involvement.
  • Headaches with focal neurological symptoms (such as aura) including hemiplegic migraine.
  • Uncontrolled hypertension.
  • Undiagnosed vaginal bleeding.
  • Pancreatitis associated with severe hypertriglyceridaemia (current or history).
  • Known or suspected pregnancy.

[edit] WARNINGS AND PRECAUTIONS

  • Cigarette smoking increases the risk of serious cardiovascular side effects from oral contraceptive use. This risk increases with age and with the extent of smoking (in epidemiologic studies, 15 or more cigarettes per day was associated with a significantly increased risk) and is quite marked in women over 35 years of age. Women who use oral contraceptives should be strongly advised not to smoke.
  • Oral contraceptives does not protect against HIV infection (AIDS) and other sexually transmitted diseases
  • The use of oral contraceptives is associated with increased risk of several serious conditions including venous and arterial thrombotic and thromboembolic events (such as myocardial infarction, thromboembolism, and stroke), hepatic neoplasia, gallbladder disease, and hypertension, although the risk of serious morbidity or mortality is very small in healthy women without underlying risk factors. The risk of morbidity and mortality increases significantly in the presence of other underlying risk factors such as certain inherited thrombophilias, hypertension, hyperlipidemias, obesity and diabetes.
  • Headache: The onset or exacerbation of migraine or development of headache with a new pattern which is recurrent, persistent, or severe requires discontinuation of oral contraceptives and evaluation of the cause
  • Oral contraceptives may cause some degree of fluid retention. They should be prescribed with caution, and only with careful monitoring, in patients with conditions which might be aggravated by fluid retention.
  • Women with a history of depression should be carefully observed and the drug discontinued if depression recurs to a serious degree
  • Uterine bleeding: Breakthrough bleeding and spotting are sometimes encountered in patients on oral contraceptives, especially during the first three months of use. If bleeding persists or occurs after previously regular cycles check for causes such as pregnancy or malignancy. If pathology and pregnancy are excluded, bleeding irregularities may resolve over time or with a change to a different COC.

[edit] INTERACTIONS

  • Anti-infective agents and anticonvulsants: Contraceptive effectiveness may be reduced when hormonal contraceptives are coadministered with antibiotics, anticonvulsants, and other drugs that increase the metabolism of contraceptive steroids. This could result in unintended pregnancy or breakthrough bleeding and menstrual irregularities. Examples include: Rifampicin, Barbiturates, Phenylbutazone, Phenytoin, Carbamazepine, Felbamate, Oxcarbazepine, Topiramate, Griseofulvin , Ampicillin and other penicillins and tetracyclines (Certain antibiotics may decrease enterohepatic circulation of estrogens).
  • Anti-HIV Protease inhibitors: some protease inhibitors may decrease the plasma levels of the estrogen and progestin. The safety and efficacy of combination oral contraceptive products may be affected with coadministration of anti-HIV protease inhibitors. Refer to the label of the individual anti-HIV protease inhibitors for further drug-drug interaction information.
  • Herbal products: St. John’s Wort (hypericum perforatum) may induce hepatic enzymes (cytochrome P450) and p-glycoprotein transporter and may reduce the effectiveness of contraceptive steroids. This may also result in breakthrough bleeding.
  • Increase in plasma levels of estradiol associated with co-administered drugs:
  • Atorvastatin : Co-administration of atorvastatin and certain combination oral contraceptives containing ethinyl estradiol increase AUC values for ethinyl estradiol by approximately 20%.
  • Ascorbic acid and acetaminophen may increase plasma ethinyl estradiol levels, possibly by inhibition of conjugation.
  • CYP3A4 inhibitors such as itraconazole or ketoconazole may increase plasma hormone levels.
  • Combined hormonal contraceptives have been shown to significantly decrease plasma concentrations of lamotrigine when co-administered due to induction of lamotrigine glucuronidation. This may reduce seizure control; therefore, dosage adjustments of lamotrigine may be necessary.

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES