Norethindrone Acetate Tablets USP, 5 mg | Norethindrone Acetate

05:47 EDT 30th September 2014 | BioPortfolio
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Norethindrone acetate tablets USP - 5 mg oral tablets Norethindrone acetate USP, (17-hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one acetate), a synthetic, orally active progestin, is the acetic acid ester of norethindrone. It is a white, or creamy white, crystalline powder.

Norethindrone acetate tablets USP, 5 mg contain the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose and talc.

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Norethindrone acetate induces secretory changes in an estrogen-primed endometrium. On a weight basis, it is twice as potent as norethindrone.

Norethindrone acetate is completely and rapidly deacetylated to norethindrone (NET) after oral administration, and the disposition of norethindrone acetate is indistinguishable from that of orally administered norethindrone. Norethindrone acetate is rapidly absorbed from norethindrone acetate tablets, with maximum plasma concentration of norethindrone generally occurring at about 2 hours post-dose. The pharmacokinetic parameters of norethindrone following single oral administration of norethindrone acetate in 29 healthy female volunteers are summarized in Table 1.

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Table 1 Pharmacokinetic Parameters after a Single Dose of Norethindrone Acetate in Healthy Women
Norethindrone Acetate (n=29) Arithmetic Mean ± SD
Norethindrone (NET)
AUC (0-inf) (ng/ml*h) 166.90 ± 56.28
Cmax (ng/ml) 26.19 ± 6.19
tmax (h) 1.83 ± 0.58
t1/2 (h) 8.51 ± 2.19
AUC = area under the curve,
Cmax = maximum plasma concentration,
tmax = time at maximum plasma concentration,
t1/2 = half-life,
SD = standard deviation

The effect of food administration on the pharmacokinetics of norethindrone acetate has not been studied.

Norethindrone is 36% bound to sex hormone-binding globulin (SHBG) and 61% bound to albumin. Volume of distribution of norethindrone is about 4 L/kg.

Norethindrone undergoes extensive biotransformation, primarily via reduction, followed by sulfate and glucuronide conjugation. The majority of metabolites in the circulation are sulfates, with glucuronides accounting for most of the urinary metabolites.

Plasma clearance value for norethindrone is approximately 0.4 L/hr/kg. Norethindrone is excreted in both urine and feces, primarily as metabolites. The mean terminal elimination half- life of norethindrone following a single dose administration of norethindrone acetate is approximately 9 hours.

The effect of age on the pharmacokinetics of norethindrone after norethindrone acetate administration has not been evaluated.

The effect of race on the disposition of norethindrone after norethindrone acetate administration has not been evaluated.

The effect of renal disease on the disposition of norethindrone after norethindrone acetate administration has not been evaluated. In pre-menopausal women with chronic renal failure undergoing peritoneal dialysis who received multiple doses of an oral contraceptive containing ethinyl estradiol and norethindrone, plasma norethindrone concentration was unchanged compared to concentrations in pre-menopausal women with normal renal function.

The effect of hepatic disease on the disposition of norethindrone after norethindrone acetate administration has not been evaluated. However, norethindrone acetate is contraindicated in markedly impaired liver function or liver disease.

No pharmacokinetic drug interaction studies investigating any drug-drug interactions with norethindrone acetate have been conducted.

Norethindrone acetate is indicated for the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer. Norethindrone acetate is not intended, recommended or approved to be used with concomitant estrogen therapy in postmenopausal women for endometrial protection.

Patients with risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus) should be managed appropriately.

Discontinue medication pending examination if there is a sudden partial or complete loss of vision or if there is sudden onset of proptosis, diplopia, or migraine. If examination reveals papilledema or retinal vascular lesions, medication should be discontinued.

Healthcare providers are advised to discuss the PATIENT INFORMATION leaflet with patients for whom they prescribe norethindrone acetate.

The following laboratory test results may be altered by the use of estrogen/progestin combination drugs:

Some beagle dogs treated with medroxyprogesterone acetate developed mammary nodules. Although nodules occasionally appeared in control animals, they were intermittent in nature, whereas nodules in treated animals were larger and more numerous, and persisted. There is no general agreement as to whether the nodules are benign or malignant. Their significance with respect to humans has not been established.

Norethindrone acetate is contraindicated during pregnancy as it may cause fetal harm when administered to pregnant women. Several reports suggest an association between intrauterine exposure to progestational drugs in the first trimester of pregnancy and congenital abnormalities in male and female fetuses. Some progestational drugs induce mild virilization of the external genitalia of female fetuses.

Detectable amounts of progestins have been identified in the milk of mothers receiving them. Caution should be exercised when progestins are administered to a nursing woman.

Norethindrone acetate tablets are not indicated in children.

See WARNINGS and PRECAUTIONS The following adverse reactions have been observed in women taking progestins:

Therapy with norethindrone acetate must be adapted to the specific indications and therapeutic response of the individual patient.

2.5 to 10 mg norethindrone acetate may be given daily for 5 to 10 days to produce secretory transformation of an endometrium that has been adequately primed with either endogenous or exogenous estrogen.

Progestin withdrawal bleeding usually occurs within three to seven days after discontinuing norethindrone acetate therapy. Patients with a past history of recurrent episodes of abnormal uterine bleeding may benefit from planned menstrual cycling with norethindrone acetate.

Initial daily dosage of 5 mg norethindrone acetate for two weeks. Dosage should be increased by2.5 mg per day every two weeks until 15 mg per day of norethindrone acetate is reached. Therapy may be held at this level for six to nine months or until annoying breakthrough bleeding demands temporary termination.

Norethindrone acetate tablets USP are available as:

5 mg : White to off-white oval, flat faced beveled edged, uncoated tablets debossed with ‘G with breakline’ on one side and 304 on other side.

Available as follows:

Bottles of 50 NDC 68462-304-50Bottles of 500 NDC 68462-304-05

Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].

Manufactured by:

Glenmark Generics Ltd. Colvale-Bardez, Goa 403 513, India

Manufactured for:

Glenmark Generics Inc., USA Mahwah, NJ 07430

Questions? 1 (888)721-7115www.glenmarkgenerics.com

June 2009

Norethindrone acetate tablets USP, 5 mg

Read this PATIENT INFORMATION before you start taking norethindrone acetate tablets and read what you get each time you refill norethindrone acetate tablets. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition.

Norethindrone acetate is similar to the progesterone hormones naturally produced by the body. Your healthcare provider may provide norethindrone acetate as individual tablets.

Norethindrone acetate tablets are used for the treatment of secondary amenorrhea (absence of menstrual periods in women who have previously had a menstrual period who are not pregnant), the treatment of endometriosis, and the treatment of irregular menstrual periods due to hormone imbalance.

You should not tke norethindrone acetate tablets if you are postmenopausal, pregnant or breast-feeding.

You should not take norethindrone acetate tablets if you have the following conditions:

Call your healthcare provider right away if you get any of these warning signs, or any other unusual symptom that concerns you.

These are not all the possible side effects of progestin and/or estrogen therapy. For more information, ask your healthcare provider or pharmacist.

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not take norethindrone acetate tablets for conditions for which it was not prescribed. Do not give norethindrone acetate tablets to other people, even if they have the same symptoms you have. It may harm them.

Keep norethindrone acetate tablets out of the reach of children.

This leaflet provides a summary of the most important information about progestin and/or estrogen therapy. If you would like more information, talk with your healthcare provider or pharmacist. You can ask for information about norethindrone acetate that is written for health professionals.

Norethindrone acetate tablets contain the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose and talc.

Manufactured by:

Glenmark Generics Ltd. Colvale-Bardez, Goa 403 513, India

Manufactured for:

Glenmark Generics Inc., USA Mahwah, NJ 07430

Questions? 1 (888)721-7115www.glenmarkgenerics.com

June 2009

IMAGE d0a94321-eb60-4aa6-a429-f0156f9f8e01-05.jpg

Manufacturer

Glenmark Generics Inc., USA

Active Ingredients

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