LOESTRIN ® 24 Fe

LOESTRIN ® 24 Fe

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LOESTRIN ® 24 Fe (norethindrone acetate and ethinyl estradiol tablets and ferrous fumarate tablets)

LOESTRIN 24 Fe is a combination oral contraceptive for oral administration consisting of active tablets containing norethindrone acetate, a progestin, and ethinyl estradiol, an estrogen, and placebo tablets containing ferrous fumarate, which serve no therapeutic purpose.

Each active white tablet contains 1 mg norethindrone acetate and 20 mcg ethinyl estradiol.

Inactive ingredients include acacia, lactose, magnesium stearate, starch, confectioner’s sugar,and talc.

Each placebo brown tablet contains 75 mg ferrous fumarate, microcrystalline cellulose, magnesium stearate, povidone, sodium starch glycolate, and compressible sugar. The ferrous fumarate tablets do not serve any therapeutic purpose. Ferrous fumarate tablets are not USP for dissolution and assay.

The chemical name of ethinyl estradiol is 19-nor-17a-pregna-1,3,5(10)-trien-20-yne-3,17-diol. The empirical formula of ethinyl estradiol is C20H24O2

The chemical name of norethindrone acetate is 17-hydroxy-19-nor-17a-pregn-4-en-20-yn-3-one acetate. The empirical formula of norethindrone acetate is C22H28O3

Mechanism of Action

CHCs prevent pregnancy primarily by suppressing ovulation.

Indications and usage

LOESTRIN 24 Fe is indicated for use by women to prevent pregnancy. The efficacy of LOESTRIN 24 Fe in women with a body mass index (BMI) of > 35 kg/m 2 has not been evaluated.

Dosage and administration

How to Start LOESTRIN 24 Fe

LOESTRIN 24 Fe is dispensed in a blister card. LOESTRIN 24 FE may be started using either a Day 1 start or a Sunday start. For the first cycle of a Sunday Start regimen, an additional method of contraception must be used until after the first 7 consecutive days of administration.

Table 1:Instructions for Administration of LOESTRIN 24 Fe

Starting COCs in women not currentlyusing hormonal contraception (Day 1Start or Sunday Start)

Important: Consider the possibility of ovulation andconception prior to initiation of this product. 

Tablet Color:LOESTRIN 24 Fe active tablets are white(Day 1 to Day 24). LOESTRIN 24 Fe inactive tablets arebrown (Day 25 to Day 28).
Day 1 Start: Take first white active tablet without regard to meals on the first day of menses. 

Take subsequent active tablets once daily at the same time each day for a total of 24 days. 

Take one brown inactive tablet daily for 4 days and at the same time of day that active tablets were taken. 

Begin each subsequent pack on the same day of the week as the first cycle pack (i.e., on the day after taking the last inactive tablet). 

Sunday Start: For each 28-day course, take in the following order: 

Take the white active tablet without regard to meals on the first Sunday after the onset of menses.

Due to the potential risk of becoming pregnant, use additional non-hormonal contraception (such as condoms and spermicide) for the first 7 days of the patient’s first cycle pack of LOESTRIN 24 Fe.  

Take subsequent active tablets once daily at the same time each day for a total of 24 days. 

Take one brown tablet (ferrous fumarate) daily for the following 4 days and at the same time of day that active tablets were taken.

A scheduled period should occur during the 4 days that the brown tablets are taken. 

Begin each subsequent pack on the same day of the week as the first cycle pack (i.e., on the Sunday after taking the last inactive tablet) and additional non-hormonal contraceptive is not needed.
Switching to LOESTRIN 24 Fe fromanother oral contraceptiveStart on the same day that a new pack of the previous oral contraceptive would have started.
Switching from another contraceptive method to LOESTRIN 24 FeStart LOESTRIN 24 Fe:
Transdermal patch On the day when next application wouldhave been scheduled.
Vaginal ring  On the day when next insertion would have been scheduled
Injection On the day when next injection would have been scheduled
Intrauterine contraceptive On the day of removal  

If the IUD is not removed on first day of the patient’s menstrual cycle, additional non-hormonal contraceptive (such as condoms and spermicide) is needed for the first seven days of the first cycle pack
ImplantOn the day of removal

Starting LOESTRIN 24 Fe after Abortion or Miscarriage

First-trimester

  • After a first-trimester abortion or miscarriage, LOESTRIN 24 Fe may be started immediately. An additional method of contraception is not needed if LOESTRIN 24 Fe is started immediately.
  • If LOESTRIN 24 Fe is not started within 5 days after termination of the pregnancy, the patient must use additional non-hormonal contraception (such as condoms and spermicide) for the first 7 days of her first 28-day course of LOESTRIN 24 Fe.

Second-trimester

  • Do not start until 4 weeks after a second-trimester abortion or miscarriage, due to the increased risk of thromboembolic disease. Start LOESTRIN 24 Fe following the instructions in Table 1 for Sunday start. Use additional non-hormonal contraception (such as condoms and spermicide) for the first 7 days of the patient’s first 28-day course of LOESTRIN 24 Fe

Starting LOESTRIN 24 Fe after Childbirth

  • Do not start until 4 weeks after delivery, due to the increased risk of thromboembolic disease. Start contraceptive therapy with LOESTRIN 24 Fe following the instructions in Table 1 for women not currently using hormonal contraception.
  • If the woman has not yet had a period postpartum, consider the possibility of ovulation and conception occurring prior to use of LOESTRIN 24 Fe

Table 2:Instructions for Missed LOESTRIN 24 Fe Tablets

If one active tablet is missed in Weeks 1, 2 or 3Take the tablet as soon as possible. Take the next pill at the regular time and continue taking one tablet a day until the pack is finished. Back-up contraception is not needed
If two consecutive active tablets are missed in Week 1 or Week 2 Take the two missed tablets as soon aspossible and the next two active tablets the next day. Continue taking one tablet a day until the pack is finished.  

Additional non-hormonal contraception (such as condoms and spermicide) must be used as back-up if the patient has sex within 7 days after missing tablets.
If two consecutive active tablets are missed in Week 3 or Week 4 or three or more consecutive active tablets are missed at any timeDay 1 Start: Throw out the rest of the pack and start a new pack that same day. 

Sunday Start: Continue taking one tablet a day until Sunday, then throw out the rest of the pack and start a new pack that same day. Additional non-hormonal contraception(such as condoms and spermicide) must be used as back-up if the patient has sex within 7 days after missing 3 tablets. 

Advice in Case of Gastrointestinal Disturbances

In case of severe vomiting or diarrhea, absorption may not be complete and additional contraceptive measures must be taken. If vomiting or diarrhea occurs within 3-4 hours after taking a white tablet, handle this as a missed tablet

CONTRAINDICATIONS

  • A high risk of arterial or venous thrombotic diseases. Examples include women who are known to:
  • Smoke, if over age 35
  • Have deep vein thrombosis or pulmonary embolism, now or in the past
  • Have inherited or acquired hypercoagulopathies
  • Have cerebrovascular disease
  • Have coronary artery disease
  • Have thrombogenic valvular or thrombogenic rhythm diseases of the heart (for example, subacute bacterial endocarditis with valvular disease, or atrial fibrillation)
  • Have uncontrolled hypertension
  • Have diabetes mellitus with vascular disease
  • Have headaches with focal neurological symptoms or have migraine headaches with aura
  • Women over age 35 with any migraine headaches
  • Liver tumors, benign or malignant, or liver disease
  • Undiagnosed abnormal uterine bleeding
  • Breast cancer or other estrogen- or progestin-sensitive cancer, now or in the past
  • Use of Hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, due to the potential for ALT elevations

WARNINGS AND PRECAUTIONS

Thrombotic Disorders and Other Vascular Problems

  • Stop LOESTRIN 24 Fe if an arterial thrombotic event or venous thromboembolic (VTE) event occurs.
  • Stop LOESTRIN 24 Fe if there is unexplained loss of vision, proptosis, diplopia, papilledema, or retinal vascular lesions. Evaluate for retinal vein thrombosis immediately
  • If feasible, stop LOESTRIN 24 Fe at least 4 weeks before and through 2 weeks after major surgery or other surgeries known to have an elevated risk of VTE as well as during the following prolonged immobilization.
  • Start LOESTRIN 24 Fe no earlier than 4 weeks after delivery, in women who are not breastfeeding. The risk of postpartum VTE decreases after the third postpartum week, whereas the risk of ovulation increases after the third postpartum week.
  • The use of COCs increases the risk of VTE. However, pregnancy increases the risk of VTE as much or more than the use of COCs. The risk of VTE in women using COCs is 3 to 9 cases per 10,000 woman-years. The risk of VTE is highest during the first year of use of a COCs and when restarting oral contraception after a break of 4 weeks or longer. The risk of thromboembolic disease due to COCs gradually disappears after COC use is discontinued.
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  • Use of COCs also increases the risk of arterial thromboses such as strokes and myocardial infarctions, especially in women with other risk factors for these events. COCs have been shown to increase both the relative and attributable risks of cerebrovascular events (thrombotic and hemorrhagic strokes). This risk increases with age, particularly in women over 35 years of age who smoke.
  • Use COCs with caution in women with cardiovascular disease risk factors.

Impaired Liver Function

Do not use LOESTRIN 24 Fe in women with liver disease, such as acute viral hepatitis or severe (decompensated) cirrhosis of liver. Acute or chronic disturbances of liver function may necessitate the discontinuation of COC use until markers of liver function return to normal and COC causation has been excluded. Discontinue LOESTRIN 24 Fe if jaundice develops.

Liver Tumors

LOESTRIN 24 Fe is contraindicated in women with benign and malignant liver tumors. Hepatic adenomas are associated with COC use. An estimate of the

attributable risk is 3.3 cases per 100,000 COC users. Rupture of hepatic adenomas may cause death through intra-abdominal hemorrhage.

Studies have shown an increased risk of developing hepatocellular carcinoma in long-term (>8 years) COC users. However, the risk of liver cancers in COC users is less than one case per million users.

Risk of Liver Enzyme Elevations with Concomitant Hepatitis C Treatment

During clinical trials with the Hepatitis C combination drug regimen that contains

ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, ALT elevations greater than 5 times the upper limit of normal (ULN), including some cases greater than 20 times the ULN, were significantly more frequent in women using ethinyl estradiol-containing medications, such as COCs. Discontinue LOESTRIN 24 Fe prior to starting therapy with the combination drug regimen ombitasvir/paritaprevir/ritonavir, with or without dasabuviR.

LOESTRIN 24 Fe can be restarted approximately 2 weeks following completion of treatment with the Hepatitis C combination drug regimen.

High Blood Pressure

LOESTRIN 24 Fe is contraindicated in women with uncontrolled hypertension or hypertension with vascular disease. For women with well-controlled hypertension, monitor blood pressure and stop LOESTRIN 24 Fe if blood pressure rises significantly.

Gallbladder Disease

Studies suggest a small increased relative risk of developing gallbladder disease among COC users. Use of COCs may worsen existing gallbladder disease. A past history of COC-related cholestasis predicts an increased risk with subsequent COC use. Women with a history of pregnancy-related cholestasis may be at an increased risk for COC related cholestasis.

Carbohydrate and Lipid Metabolic Effects

Carefully monitor prediabetic and diabetic women who are taking LOESTRIN 24 Fe. COCs may decrease glucose tolerance.

Consider alternative contraception for women with uncontrolled dyslipidemias. A small proportion of women will have adverse lipid changes while on COCs.

Women with hypertriglyceridemia, or a family history thereof, may be at an increased risk of pancreatitis when using COCs.

Headache

If a woman taking LOESTRIN 24 Fe develops new headaches that are recurrent, persistent, or severe, evaluate the cause and discontinue LOESTRIN 24 Fe if indicated.

Consider discontinuation of LOESTRIN 24 Fe in the case of increased frequency or severity of migraine during COC use (which may be prodromal of a cerebrovascular event).

Unscheduled Bleeding and Spotting

Unscheduled (breakthrough or intracyclic) bleeding and spotting sometimes occur in patients on COCs, 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 contraceptive product.

COC Use Before or During Early Pregnancy

Extensive epidemiologic studies have revealed no increased risk of birth defects in women who have used oral contraceptives prior to pregnancy. Studies also do not suggest a teratogenic effect, particularly in so far as cardiac anomalies and limb reduction defects are concerned, when oral contraceptives are taken inadvertently during early pregnancy. Discontinue LOESTRIN 24 Fe use if pregnancy is confirmed.

Depression

Carefully observe women with a history of depression and discontinue LOESTRIN 24 Fe if depression recurs to a serious degree.

Carcinoma of the Breast and Cervix

LOESTRIN 24 Fe is contraindicated in women who currently have or have had breast cancer because breast cancer is a hormonally-sensitive.

There is substantial evidence that COCs do not increase the incidence of breast cancer. Although some past studies have suggested that COCs might increase the incidence of breast cancer, more recent studies have not confirmed such findings.

Some studies suggest that COCs are associated with an increase in the risk of cervical cancer or intraepithelial neoplasia. However, there is controversy about the extent to which these findings may be due to differences in sexual behavior and other factors.

Effect on Binding Globulins

The estrogen component of COCs may raise the serum concentrations of thyroxine-binding globulin, sex hormone-binding globulin, and cortisol-binding globulin. The dose of replacement thyroid hormone or cortisol therapy may need to be increased.

Chloasma

Chloasma may occasionally occur, especially in women with a history of chloasma gravidarum. Women with a tendency to chloasma should avoid exposure to the sun or ultraviolet radiation while taking LOESTRIN 24 Fe.

ADVERSE REACTIONS

The following serious adverse reactions with the use of COCs are discussed elsewhere in the labeling:

  • Serious cardiovascular events and stroke
  • Vascular events
  • Liver disease

Adverse reactions commonly reported by COC users are:

  • Irregular uterine bleeding
  • Nausea
  • Breast tenderness
  • Headache

USE IN SPECIFIC POPULATIONS

Pregnancy: There is no use for contraception in pregnancy; therefore, LOESTRIN 24 Fe should be discontinued during pregnancy. Epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to CHCs before conception or during early pregnancy.

Lactation: Contraceptive hormones and/or metabolites are present in human milk. CHCs can reduce milk production in breastfeeding females. This reduction can occur at any time but is less likely to occur once breastfeeding is well-established.

When possible, advise the nursing female to use other methods of contraception until she discontinues breastfeeding. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for LOESTRIN 24 Fe and any potential adverse effects on the breastfed child from LOESTRIN 24 Fe or from the underlying maternal condition.

Pediatric Use: Safety and efficacy of LOESTRIN 24 Fe have been established in women of reproductive age. Efficacy is expected to be the same in postpubertal adolescents under the age of 18 years as for users 18 years and older. Use of this product before menarche is not indicated.

Geriatric Use: LOESTRIN 24 Fe has not been studied in postmenopausal women and is not indicated in this population.

Hepatic Impairment

The pharmacokinetics of LOESTRIN 24 Fe has not been studied in subjects with hepatic impairment. However, steroid hormones may be poorly metabolized in patients with hepatic impairment. Acute or chronic disturbances of liver function may necessitate the discontinuation of COC use until markers of liver function return to normal and COC causation has been excluded.

Renal Impairment

The pharmacokinetics of LOESTRIN 24 Fe has not been studied in women with renal impairment.

Body Mass Index

The safety and efficacy of LOESTRIN 24 Fe in women with a body mass index (BMI) > 35 kg/m 2 has not been evaluated

OVERDOSAGE

There have been no reports of serious ill effects from overdose of oral contraceptives, including ingestion by children. Overdosage may cause withdrawal bleeding in females and nausea.

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