HEATHER

HEATHER- norethindrone tablet
A-S Medication Solutions

Rx only

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

Each pale yellow HEATHER tablet provides a continuous oral contraceptive regimen of 0.35 mg norethindrone USP daily, and the inactive ingredients include corn starch, lactose monohydrate, magnesium stearate, povidone, talc, D&C Yellow No. 10 aluminum lake and FD&C Yellow No. 6 aluminium lake.

The chemical name for norethindrone USP is 17-Hydroxy-19-Nor-17α-pregn-4-en-20-yn-3-one. The structural formula follows:

Structure of Norethindrone

Norethindrone USP

Therapeutic class = oral contraceptive

CLINICAL PHARMACOLOGY

1. Mode of Action

HEATHER progestin-only oral contraceptives prevent conception by suppressing ovulation in approximately half of users, thickening the cervical mucus to inhibit sperm penetration, lowering the mid-cycle LH and FSH peaks, slowing the movement of the ovum through the fallopian tubes, and altering the endometrium.

2. Pharmacokinetics

Absorption:

Norethindrone is rapidly absorbed with maximum plasma concentrations occurring within 1 to 2 hours after HEATHER administration (see Table 1). Norethindrone appears to be completely absorbed following oral administration; however, it is subject to first pass metabolism resulting in an absolute bioavailability of approximately 65%.

figure 1
(click image for full-size original)

Figure 1: Mean ± SD Norethindrone Plasma Concentrations Following HEATHER Administration

Peak plasma concentrations occur approximately 1 hour after administration (mean T 1.2 hours). The mean (SD) C was 4816.8 (1532.6) pg/mL and generally occurred within 1 hour (mean) of tablet administration, ranging from 0.5 to 2 hours. The mean (SD) C was 885 (250) pg/mL, however, the mean concentration at 24 hrs was 130 (47) pg/mL. max max avg

Table 1 provides summary statistics of the pharmacokinetic parameters associated with single dose HEATHER administration.

Table 1: Mean ± SD Pharmacokinetic Parameters Following Single Dose Administration of HEATHER in 12 Healthy Female Subjects Under Fasting Conditions

Pharmacokinetic Parameter

Norethindrone 0.35 mg

T (hr) max

1.2 ± 0.5

C (pg/mL) max

4817 ± 1533

AUC (pg•h/mL) (0-48)

21233 ± 6002

t (h) 1/2

7.7 ± 0.5

The food effect on the rate and extent of norethindrone absorption after HEATHER administration has not been evaluated.

Distribution:

Following oral administration, norethindrone is 36% bound to sex hormone-binding globulin (SHBG) and 61% bound to albumin. Volume of distribution of norethindrone is approximately 4 L/kg.

Metabolism:

Norethindrone undergoes extensive biotransformation, primarily via reduction, followed by sulfate and glucuronide conjugation; less than 5% of a norethindrone dose is excreted unchanged; greater than 50% and 20-40% of a dose is excreted in urine and feces, respectively. The majority of metabolites in the circulation are sulfate, with glucuronides accounting for most of the urinary metabolites.

Excretion:

Plasma clearance rate for norethindrone has been estimated to be approximately 600 L/day. Norethindrone is excreted in both urine and feces, primarily as metabolites. The mean terminal elimination half-life of norethindrone following single dose administration of HEATHER is approximately 8 hours.

INDICATIONS AND USAGE

1. Indications

Progestin-only oral contraceptives are indicated for the prevention of pregnancy.

2. Efficacy

If used perfectly, the first-year failure rate for progestin-only oral contraceptives is 0.5%. However, the typical failure rate is estimated to be closer to 5%, due to late or omitted pills. The following table lists the pregnancy rates for users of all major methods of contraception.

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.
Treatment initiated within 72 hours after unprotected intercourse reduces the risk of pregnancy by at least 75%. LAM is a highly effective, temporary method of contraception. 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. Emergency Contraceptive Pill: *
Lactational Amenorrhea Method:
*
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 4 yellow pills). ® ® ® ®
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 6 months of age
Among couples attempting to avoid pregnancy, the percentage who continue to use a method for one year
§
Among couples who initiate use of a method (not necessarily for the first time), the percentage who experience an accidental pregnancy during the first year if they do not stop use for any reason. typical
Among couples who initiate use of a method (not necessarily for the first time), and who use it (both consistently and correctly), the percentage who experience an accidental pregnancy during the first year if they do not stop use for any other reason perfectly
#
The percentage of women becoming pregnant noted 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 that would become pregnant within one year among women now relying on reversible methods of contraception if they abandoned contraception altogether
Þ
Foams, creams, gels, vaginal suppositories, and vaginal film
ß
Cervical mucus (ovulation) method supplemented by calendar in the pre-ovulatory and basal body temperature in the post-ovulatory phases
à
With spermicidal cream or jelly
è
Without spermicides

% of Women Experiencing an Unintended Pregnancy within the First Year of Use

% of Women Continuing Use at One Year

Method

(1)

Typical Use §

(2)

Perfect Use

(3)

(4)

Chance #

85

85

Spermicides Þ

26

6

40

Periodic abstinence

25

63

Calendar

9

Ovulation Method

3

Sympto-Thermal ß

2

Post-Ovulation

1

Cap à

Parous Women

40

26

42

Nulliparous Women

20

9

56

Sponge

Parous Women

40

20

42

Nulliparous Women

20

9

56

Diaphragm à

20

6

56

Withdrawal

19

4

Condom è

Female (Reality)

21

5

56

Male

14

3

61

Pill

5

71

Progestin only

0.5

Combined

0.1

IUDs

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

Levonorgestrel Implants (Norplant ) ®

0.05

0.05

88

Female Sterilization

0.5

0.5

100

Male Sterilization

0.15

0.10

100

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