Norgestrel Tablets USP 0.075mg Taj Pharma
Patients should be counseled that oral contraceptives do not protect against transmission of HIV (AIDS) and other sexually transmitted diseases (STDs) such as chlamydia, genital herpes, genital warts, gonorrhea, hepatitis B, and syphilis.
DESCRIPTION
Norgestrel, is a progestin medication which is used in birth control pills and in menopausal hormone therapy. It is available both in combination with an estrogen and alone. It is taken by mouth.
Side effects of norgestrel include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, acne, increased hair growth, and others.
Norgestrel is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic activity and no other important hormonal activity.
It was subsequently introduced for use in menopausal hormone therapy as well. Norgestrel is sometimes referred to as a “second-generation” progestin. It is marketed widely throughout the world.
COMPOSITION
Each Norgestrel tablet contains:
Norgestrel 0.075 mg
Excipients q.s.
INDICATIONS
Norgestrel Tablets are indicated for use by females of reproductive potential to prevent pregnancy.
Norgestrel Tablets are not for use as emergency contraception.
In eight US clinical studies with Norgestrel Tablets, 2,173 women completed at least one cycle and 648 completed at least 13 cycles providing a total of 21,856 28-day cycles of exposure in women aged from 15 to 49 years. The racial demographic was 53% Caucasian and 47% African-American. The pregnancy rate was approximately 2 per 100 women-years.
DOSAGE AND ADMINISTRATION
To achieve maximum contraceptive effectiveness, Norgestrel Tablets must be taken exactly as directed. The woman should take one tablet every day, at the same time. Administration is continuous, with no interruption between pill packs. See PATIENT LABELING for detailed instructions.
HOW SUPPLIED
Norgestrel Tablets (0.075 mg norgestrel) are available in a blister package of 28 tablets as follows.
Storage
Store at controlled room temperature between 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].
SIDE EFFECTS
An increased risk of the following adverse reactions has been reported with the use of progestin-only oral contraceptives (see WARNINGS section for additional information):
- Delayed follicular atresia/ovarian cysts
- Menstrual irregularity, changes in menstrual flow; breakthrough bleeding/spotting; amenorrhea, prolonged bleeding
The following adverse reactions were reported in ≥ 5% of subjects in the Norgestrel Tablet clinical studies:
- Headache
- Dizziness
- Nausea
- Increased appetite
- Abdominal pain, cramps and bloating
- Fatigue
- Vaginal discharge
- Dysmenorrhea
- Nervousness
- Backache
- Breast discomfort
- Acne
DRUG INTERACTIONS
- The effectiveness of progestin-only pills is reduced by hepatic enzyme-inducing drugs such as phenytoin, carbamazepine, barbiturates,rifampin, efavirenz, bosentan and herbal preparations containing St. John’s Wort (hypericum perforatum). This could result in unintended pregnancy or breakthrough bleeding.
During concomitant use of Norgestrel and substances that may affect its efficacy, it is recommended that a nonhormonal back-up method of contraception (such as condom) be used in addition to the regular intake of Norgestrel Tablets. Use of a nonhormonal back-up method is recommeded for 28 days after discontinuation of substances that have led to induction of hepatic microsomal enzymes. For women receiving long-term therapy with hepatic enzyme inducers, another method of contraception should be considered. - Effectiveness of progestin-containing hormonal contraceptives and emergency contraceptive ulipristal acetate may be decreased if progestin-containing hormonal contraceptives are used within five days after ulipristal acetate dosing.
If a woman wishes to use Norgestrel Tablets after using ulipristal acetate, she should do so no sooner than 5 days after the intake of ulipristal acetate and she should use a reliable barrier method for subsequent acts of intercourse until her next menstrual period. Consult the product information of concomitant medications/substances to identify potential interactions.
Gastrointestinal
Diarrhea and/or vomiting within 4 hours after taking a pill may reduce hormone absorption. Women should use of a nonhormonal back-up method of birth control (such as a condom or spermicide) during the next 48 hours.
Interactions With Laboratory Tests
The following endocrine tests may be affected by Norgestrel Tablets use:
- Sex hormone-binding globulin (SHBG) concentrations may be decreased.
- Total thyroxine concentrations may be decreased, due to a decrease in thyroid binding globulin (TBG). However, free thyroxine level should remain unchanged.
Norgestrel Tablets contains FD&C Yellow No.5 (tartrazine) which may cause allergic-type reactions (including bronchial asthma) in certain susceptible persons. Although the overall incidence of FD&C Yellow No. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity. (See CONTRAINDICATIONS)
Carbohydrate And Lipid Effects
Some Norgestrel Tablets users may experience slight changes in glucose tolerance with increases in plasma insulin, but women with diabetes mellitus who use progestin-only oral contraceptives do not generally experience changes in their insulin requirements.
Lipid metabolism is occasionally affected in that HDL1, HDL2, and apolipoprotein A-I and A-II may be decreased; hepatic lipase may be increased. There is usually no effect on total cholesterol, HDL3, LDL, or VLDL.
The effect of progestin-only oral contraceptives on carbohydrate and lipid metabolism is generally not clinically significant.
WARNINGS
Ectopic Pregnancy
The incidence of ectopic pregnancies for progestin-only oral contraceptive users is 5 per 1000 woman-years. Up to 10% of pregnancies reported in clinical studies of progestin-only oral contraceptive users are extrauterine. Health-care providers should be alert to the possibility of an ectopic pregnancy in women who become pregnant or complain of lower abdominal pain while on Norgestrel Tablets.
Delayed Follicular Atresia/Ovarian Cysts
If follicular development occurs, atresia of the follicle is sometimes delayed, and the follicle may continue to grow beyond the size it would attain in a normal cycle. Generally these enlarged follicles disappear spontaneously. Often they are asymptomatic; in some cases they are associated with mild abdominal pain, and rarely they may twist or rupture, requiring surgical intervention.
Bleeding Pattern Alterations
Irregular menstrual patterns are common among women using Norgestrel Tablets. Undiagnosed abnormal uterine bleeding should be evaluated before Norgestrel is prescribed (see CONTRAINDICATIONS). In the 8 U.S. clinical trials of Norgestrel Tablets, there were a total of 2,575 enrolled subjects, and approximately half of them experienced some menstrual changes. This was defined in the clinical studies as vaginal bleeding which, in the judgment of the subject, did not have the characteristics of her pre-treatment menstrual periods in duration, amount or appearance. Subjects experienced unscheduled (breakthrough) bleeding (48.6%) and spotting (47.3%) on Norgestrel Tablets. Amenorrhea occurred in 6.1% of subjects in their first cycle and 28.7% of all subjects during the studies. A total of 379 participants (17.4%) discontinued treatment due to side effects; 67.6% of all discontinuations were due to bleeding patterns. Overall, 6.4% of participants discontinued treatment due to breakthrough bleeding and 2.7% due to amenorrhea (n=2,173 subjects who completed at least one cycle).
If uterine bleeding together with the clinical history is suggestive of infection, malignancy, pregnancy, or other conditions, rule out these conditions. If amenorrhea occurs, consider the possibility of pregnancy.
Hepatic Neoplasia/Liver Disease
Discontinue Norgestrel Tablet use if jaundice or acute disturbances of liver function develop. Do not resume use until markers of liver function return to normal and Norgestrel Tablet causation has been excluded.
PRECAUTIONS
Migraine/Headache
The onset or exacerbation of migraine, or development of headache with a new pattern that is recurrent, persistent, or severe requires evaluation of the cause because women with migraine may be at increased risk of stroke.
Pregnancy
Norgestrel Tablets are contraindicated for use in pregnant women because there is no need for pregnancy prevention in a woman who is already pregnant [see CONTRAINDICATIONS]. Published studies report no harmful effects on fetal development associated with long-term use of contraceptive doses of oral progestins in pregnant women.
Discontinue Norgestrel Tablets if pregnancy is confirmed.
Nursing Mothers
Small amounts of progestin pass into the breast milk, resulting in steroid levels in infant plasma. No adverse effects have been reported on breastfeeding performance or infant health. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Norgestrel Tablets and any potential adverse effects on the breastfed infant from Norgestrel Tablets or from the underlying maternal condition.
Fertility Following Discontinuation
The limited available data do not indicate a significant delay in the return of normal ovulation and fertility following discontinuation of progestin-only oral contraceptives.
Pediatric Use
Safety and efficacy of Norgestrel Tablets have been established in women of reproductive age, including adolescents as young as 15 years of age, and almost 30% of subjects in the clinical trials who were under 20 years of age. Use of this product before menarche is not indicated.
Geriatric Use
Norgestrel Tablets has not been studied in postmenopausal women and is not indicated in this population.
Information For The Patient
Advise the patient to read the FDA-approved patient labeling (PATIENT INFORMATION).
- Before prescribing Norgestrel Tablets, advise the patient that:
- Norgestrel Tablets should be taken at the same time every day, including throughout all bleeding episodes.
- She should use a nonhormonal back-up method of contraception (such as condoms or spermicides) for the next 48 hours whenever Norgestrel Tablets are taken 3 or more hours late, or if she has vomiting or diarrhea within 4 hours after taking the pill.
- Use of Norgestrel Tablets may be associated with changes in their normal menstrual bleeding pattern. However, women who miss two periods (or have missed a single period but have missed doses of Norgestrel) or suspect they may be pregnant should take a pregnancy test.
- She should inform her healthcare provider if she develops repeated vaginal postcoital bleeding, prolonged episodes of bleeding, amenorrhea or development of severe abdominal pain.
- Norgestrel Tablets do not protect against HIV infection (AIDS) or other sexually transmitted infections (STIs).
OVERDOSE
Symptoms of oral contraceptive overdosage may include nausea, vomiting, breast tenderness, dizziness, somnolence (drowsiness/fatigue), and withdrawal bleeding in females. There is no specific antidote and further treatment of overdose, if necessary, is directed to the symptoms.
CONTRAINDICATIONS
Norgestrel Tablets is contraindicated for use by women who are known to have the following conditions:
- Known or suspected pregnancy
- Known or suspected carcinomaof the breast, or other progestin-sensitive cancer, now or in the past
- Undiagnosed abnormal uterine bleeding
- Hypersensitivity to any component of this product (see PRECAUTIONS, FD & C Yellow No. 5)
- Benignor malignant liver tumors
- Acute liver disease
CLINICAL PHARMACOLOGY
Mode Of Action
Progestin-only oral contraceptives such as Norgestrel Tablets prevent conception by suppressing ovulation in approximately half of the cycles in users, thickening the cervical mucus to inhibit sperm penetration, lowering the midcycle LH and FSH peaks, slowing the movement of the ovum through the fallopian tubes, and altering the endometrium.
Pharmacokinetics
Serum progestin levels peak about two hours after oral administration, followed by rapid distribution and elimination. By 24 hours after drug ingestion, serum levels are near baseline, making efficacy dependent upon rigid adherence to the dosing schedule. There are large variations in serum levels among individual users. Progestin-only administration results in lower steady-state progestin levels and a shorter elimination half-life than concomitant administration with estrogens.
MANUFACTURED IN INDIA BY:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com
