NEXT CHOICE

NEXT CHOICE — levonorgestrel tablet
Rebel Distributors Corp.

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PHYSICIAN LABELING

Levonorgestrel Tablets, 0.75 mg

Rx only for women age 17 and younger

This product is not approved for nonprescription use.

Levonorgestrel tablets are a prescription–only emergency contraceptive for women age 17 and younger. This product is not approved for nonprescription use. Levonorgestrel tablets are intended to prevent pregnancy after known or suspected contraceptive failure or unprotected intercourse. Emergency contraceptive pills (like all oral contraceptives) do not protect against infection with HIV (the virus that causes AIDS) and other sexually transmitted diseases.

DESCRIPTION

Emergency contraceptive tablet. Each levonorgestrel tablet contains 0.75 mg of a single active steroid ingredient, levonorgestrel [18,19-Dinorpregn-4-en-20-yn-3-one-13-ethyl-17-hydroxy-, (17α)-(-)-], a totally synthetic progestogen. The inactive ingredients present are colloidal silicon dioxide, corn starch, FD&C Yellow #6, magnesium stearate, povidone, and lactose monohydrate. Levonorgestrel has a molecular weight of 312.45, and the following structural and molecular formulas:

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C21 H28 O2

CLINICAL PHARMACOLOGY

Emergency contraceptives are not effective if the woman is already pregnant. Levonorgestrel tablets are believed to act as an emergency contraceptive principally by preventing ovulation or fertilization (by altering tubal transport of sperm and/or ova). In addition, they may inhibit implantation (by altering the endometrium). They are not effective once the process of implantation has begun.

Pharmacokinetics

Absorption

No specific investigation of the absolute bioavailability of levonorgestrel tablets in humans has been conducted. However, literature indicates that levonorgestrel is rapidly and completely absorbed after oral administration (bioavailability about 100%) and is not subject to first pass metabolism. After a single dose of levonorgestrel tablets (0.75 mg) administered to 16 women under fasting conditions, maximum serum concentrations of levonorgestrel are 14.1 ± 7.7 ng/mL (mean ± SD) at an average of 1.6 ± 0.7 hours. No formal study of the effect of food on the absorption of levonorgestrel has been undertaken.

Table 1 Pharmacokinetic Parameter Values Following Single Dose Administration of Levonorgestrel Tablets, 0.75 mg to Healthy Female Volunteers
Mean (± S.D.)
N Cmax (ng/mL) Tmax (h) CL(L/h) Vd (L) T1/2 (h) AUC0-∞ (ng/mL/h)
16 14.1 ± 7.7 1.6 ± 0.7 7.7 ± 2.7 260.0 24.4 ± 5.3 123.1 ± 50.1

Distribution

Levonorgestrel in serum is primarily protein bound. Approximately 50% is bound to albumin and 47.5% is bound to sex hormone binding globulin (SHBG).

Metabolism

Following a single oral dosage, levonorgestrel does not appear to be extensively metabolized by the liver. The primary metabolites are 3α,5β- and 3α,5α-tetrahydrolevonorgestrel with 16β-hydroxynorgestrel also identified. Together, these account for less than 10% of parent plasma levels. Urinary metabolites hydroxylated at the 2α and 16β positions have also been identified. Small amounts of the metabolites are present in plasma as sulfate and glucuronide conjugates.

Excretion

The elimination half-life of levonorgestrel following single dose administration as levonorgestrel tablets (0.75 mg) is 24.4 ± 5.3 hours. Excretion following single dose administration as emergency contraception is unknown, but based on chronic, low-dose contraceptive use, levonorgestrel and its metabolites are primarily excreted in the urine, with smaller amounts recovered in the feces.

SPECIAL POPULATIONS

Geriatric

This product is not intended for use in geriatric (age 65 years or older) populations and pharmacokinetic data are not available for this population.

Pediatric

This product is not intended for use in pediatric (premenarcheal) populations, and pharmacokinetic data are not available for this population.

Race

No formal studies have evaluated the effect of race. However, clinical trials demonstrated a higher pregnancy rate in the Chinese population with both levonorgestrel tablets and the Yuzpe regimen (another form of emergency contraception consisting of two doses of ethinyl estradiol 0.1 mg + levonorgestrel 0.5 mg). The reason for this apparent increase in the pregnancy rate of emergency contraceptives in Chinese women is unknown.

Hepatic Insufficiency and Renal Insufficiency

No formal studies have evaluated the effect of hepatic insufficiency or renal insufficiency on the disposition of emergency contraceptive tablets.

Drug-Drug Interactions

No formal studies of drug-drug interactions were conducted.

NEXT CHOICE Indications and Usage

Levonorgestrel tablets are a prescription-only emergency contraceptive, for women age 17 and younger, that can be used to prevent pregnancy following unprotected intercourse or a known or suspected contraceptive failure. This product is not approved for nonprescription use.

To obtain optimal efficacy, the first tablet should be taken as soon as possible within 72 hours of intercourse. The second tablet must be taken 12 hours later.

Clinical Studies

A double-blind, controlled clinical trial in 1,955 evaluable women compared the efficacy and safety of levonorgestrel tablets, (one 0.75 mg tablet of levonorgestrel taken within 72 hours of intercourse, and one tablet taken 12 hours later) to the Yuzpe regimen (two tablets of 0.25 mg levonorgestrel and 0.05 mg ethinyl estradiol, taken within 72 hours of intercourse, and two tablets taken 12 hours later). Levonorgestrel tablets, were at least as effective as the Yuzpe regimen in preventing pregnancy. After a single act of intercourse, the expected pregnancy rate of 8% (with no contraception) was reduced to approximately 1% with levonorgestrel tablets.

Emergency contraceptives are not as effective as routine contraception since their failure rate, while low based on a single use, would accumulate over time with repeated use (see WARNINGS). See Table 2 below.

Table 2 Percentage of women experiencing an unintended pregnancy during the first year of typical use and the first year of perfect use of contraception, and the percentage continuing use at the end of the first year, United States.
% of Women Experiencing an Unintended Pregnancy within the First Year of Use % of Women Continuing Use at One Year 3
Method (1) Tpical Use 1 (2) Perfect Use 2 (3) (4)
Source: Trussell J, Contraceptive efficacy. In Hatcher RA, Trussell J, Stewart F, Cates W, Stewart GK, Kowal D, Guest F, Contraceptive Technology: Seventeenth Revised Edition. New York, NY: Irvington Publishers, 1998.
1 Among typical couples who initiate use of a method (not necessarily for the first time), the percentage who experience an unintended pregnancy during the first year if they do not stop use for any other reason.
2 Among couples who initiate use of a method (not necessarily for the first time) and who use it perfectly (both consistently and correctly), the percentage who experience an unintended pregnancy during the first year if they do not stop use for any other reason.
3 Among couples attempting to avoid pregnancy, the percentage who continue to use a method for one year.
4 The percentages of women becoming pregnant in columns (2) and (3) are based on data from populations where contraception is not used and from women who cease using contraception in order to become pregnant. Among such populations, about 89% become pregnant within one year. This estimate was lowered slightly (to 85%) to represent the percentage who would become pregnant within one year among women now relying on reversible methods of contraception if they abandoned contraception altogether.
5 Foams, creams, gels, vaginal suppositories and vaginal film.
6 Cervical mucus (ovulation) method supplemented by calendar in the preovulatory and basal body temperature in the post-ovulatory phases.
7 With spermicidal cream or jelly.
8 Without spermicides.
9 The treatment schedule is one dose within 72 hours after unprotected intercourse and a second dose 12 hours after the first dose. The Food and Drug Administration has declared the following brands of oral contraceptives to be safe and effective for emergency contraception: Ovral®* (1 dose is 2 white pills), Alesse®* (1 dose is 5 pink pills), Nordette®* or Levlen®* (1 dose is 2 light-orange pills), Lo/Ovral®* (1 dose is 4 white pills), Triphasil®* or Tri-Levlen®* (1 dose is 4 yellow pills).
10 However, to maintain effective protection against pregnancy, another method of contraception must be used as soon as menstruation resumes, the frequency or duration of breastfeeds is reduced, bottle feeds are introduced or the baby reaches six months of age.
Chance4 85 85
Spermicide5 26 6 40
Periodic Abstinence 25 63
Calendar 9
Ovulation Method 3
Sympto-thermal6 2
Post-ovulation 1
Withdrawal 19 4
Cap7
Parous Women 40 26 42
Nulliparous Women 20 9 56
Sponge
Parous Women 40 20 42
Nulliparous Women 20 9 56
Diaphragm7 20 6 56
Condom8
Female (Reality®*) 21 5 56
Male 14 3 61
Pill 5 71
Progestin Only 0.5
Combined 0.1 0.1
IUD
Progesterone T 2.0 1.5 81
Copper T 380A 0.8 0.6 78
LNg 20 0.1 0.1 81
Depo-Provera®* 0.3 0.3 70
Norplant®* andNorplant-2®* 0.05 0.05 88
Female Sterilization 0.5 0.5 100
Male Sterilization 0.15 0.10 100
Emergency Contraceptive Pills: Treatment initiated within 72 hours after unprotected intercourse reduces the risk of pregnancy by at least 75%.9
Lactational Amenorrhea Method: LAM is a highly effective, temporary , method of contraception.10
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