1 Star2 Stars3 Stars4 Stars5 Stars (No Ratings Yet)
blankLoading...

Norethisterone

Drug Nomenclature

NorethisteroneSynonyms: Ethinylnortestosterone; NSC-9564; Norethindrone; Norethisteron; Norethisteronum; Noretisteron; Noretisterona; Noretisteronas; Noretisterone; Noretisteroni; Noretiszteron; Norpregneninolone
BAN: Norethisterone
INN: Norethisterone [pINN (en)]
INN: Noretisterona [pINN (es)]
INN: Noréthistérone [pINN (fr)]
INN: Norethisteronum [pINN (la)]
INN: Норэтистерон [pINN (ru)]
Chemical name: 17β-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one
Molecular formula: C20H26O2 =298.4
CAS: 68-22-4
ATC code: G03AC01; G03DC02
Read code: y00VA [Progestogen Oral Contraceptive]; y00XI [Malignancy]; y02bO; y07kF; y00V7 [Combined Oral Contraceptive]; y08DZ [Endocrine]

Pharmacopoeias. In China, Europe, International, Japan, and US.

European Pharmacopoeia, 6th ed. (Norethisterone). A white or yellowish-white crystalline powder. Practically insoluble in water sparingly soluble in dehydrated alcohol and in acetone soluble in dichlorometh-ane.

The United States Pharmacopeia 31, 2008 (Norethindrone). A white to creamy-white odourless crystalline powder. Practically insoluble in water sparingly soluble in alcohol soluble in chloroform and in dioxan slightly soluble in ether.

Norethisterone Acetate

Drug Nomenclature

Synonyms: Norethindrone Acetate; Norethisteron-acetát; Norethisteroni Acetas; Noretisterona, acetato de; Noretisteronacetat; Noretisteroniasetaatti; Noretisterono acetatas; Noretiszteron-acetát
BAN: Norethisterone Acetate [BANM]
INN: Norethisterone Acetate [pINNM (en)]
INN: Acetato de noretisterona [pINNM (es)]
INN: Noréthistérone, Acétate de [pINNM (fr)]
INN: Norethisteroni Acetas [pINNM (la)]
INN: Норэтистерона Ацетат [pINNM (ru)]
Chemical name: 17β-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one acetate; 3-Oxo-19-nor-17α-pregn-4-en-20-yn-17β-yl acetate
Molecular formula: C22H28O3 =340.5
CAS: 51-98-9
ATC code: G03AC01; G03DC02

Pharmacopoeias. In Europe, International, and US.

European Pharmacopoeia, 6th ed. (Norethisterone Acetate). A white or yellowish-white crystalline powder. It exhibits polymorphism. Practically insoluble in water soluble in alcohol freely soluble in dichloromethane. Protect from light.

The United States Pharmacopeia 31, 2008 (Noneth in drone Acetate). A white to creamy-white odourless crystalline powder. Practically insoluble in water soluble 1 in 10 of alcohol, 1 in less than 1 of chloroform, 1 in 2 of dioxan, and 1 in 18 of ether.

Norethisterone Enantate

Drug Nomenclature

Synonyms: Norethindrone Enanthate; Norethisterone Enanthate; Norethisterone Heptanoate; Noretisterona, enantato de
BAN: Norethisterone Enantate [BANM]
INN: Norethisterone Enantate [pINNM (en)]
INN: Enantato de noretisterona [pINNM (es)]
INN: Noréthistérone, Enantate de [pINNM (fr)]
INN: Norethisteroni Enantas [pINNM (la)]
INN: Норэтистерона Енантат [pINNM (ru)]
Chemical name: 17β-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one heptanoate
Molecular formula: C27H38O3 =410.6
CAS: 3836-23-5
ATC code: G03AC01; G03DC02
Read code: y00VB

Pharmacopoeias. In International

Adverse Effects and Precautions

As for progestogens in general (see Progesterone). See also under Hormonal Contraceptives.

Effects on the liver. There were 6 cases of jaundice among 107 patients with breast cancer treated with high-dose norethisterone acetate the jaundice was reversible and of an obstructive type. A retrospective analysis found that the use of norethisterone to prevent menstrual haemorrhage during the thrombocytopenic phase of allogeneic bone marrow transplantation was a significant risk factor for hepatic veno-occlusive disease.

Porphyria. Norethisterone has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.

Pregnancy. Abnormalities seen in the offspring of women given norethisterone during pregnancy (either alone or with ethinylestradiol) included: hypospadias, masculinisation of female infants, meningomyelocele or hydrocephalus, and neonatal choreoathetosis associated with oral contraceptive use. For reference to the fact that oral contraceptives have not generally been associated with teratogenicity, even when used inadvertently in pregnancy.

Venous thromboembolism. For mention that combined oral contraceptives containing older progestogens such as norethisterone appear to be associated with a lower incidence of venous thromboembolism than desogestrel- or gestodene-containing preparations.

Interactions

As for progestogens in general (see Progesterone). See also under Hormonal Contraceptives.

Pharmacokinetics

Norethisterone is absorbed from the gastrointestinal tract, undergoing first-pass hepatic metabolism, with peak plasma concentrations occurring 1 to 2 hours after an oral dose. It exhibits biphasic pharmacokinetics an initial distribution phase is followed by a prolonged elimination phase with a half-life of about 8 hours or more. Norethisterone is highly protein bound about 60% to albumin and 35% to sex hormone binding globulin. Use with an oestrogen increases the proportion bound to sex hormone binding globulin. It is metabolised in the liver with 50 to 80% of a dose being excreted in the urine and up to 40% appearing in the faeces.

Norethisterone acetate is rapidly hydrolysed to norethisterone, principally by intestinal tissue. After intramuscular injection of norethisterone enantate peak concentrations of norethisterone in plasma are not attained for several days.

Uses and Administration

Norethisterone and its acetate and enantate esters are progestogens (see Progesterone) derived from nortestosterone that have weak oestrogenic and andro-genic properties. They are commonly used as hormonal contraceptives. Norethisterone and norethisterone acetate are both given orally. Typical daily doses are 350 micrograms for norethisterone and 600 micrograms for norethisterone acetate when used alone, or 0.5 to 1 mg for norethisterone and 1 to 1.5 mg for norethisterone acetate when used with an oestrogen. Norethisterone enantate is given by intramuscular injection a dose of 200 mg provides contraception for 8 weeks. An intramuscular injection containing norethisterone enantate 50 mg with estradiol valerate 5 mg is given once each month.

Norethisterone and norethisterone acetate are used as the progestogen component of menopauasl HRT. Typical regimens have included either continuous daily doses of norethisterone 700 micrograms or norethisterone acetate 0.5 to 1 mg, or cyclical regimens of norethisterone or norethisterone acetate 1 mg daily for 10 to 12 days of a 28-day cycle. Norethisterone acetate is also available as transdermal patches supplying 140, 170, or 250 micrograms in 24 hours, that are applied twice weekly for 2 weeks of a 4-week cycle the lower strengths may also be applied twice weekly on a continuous basis.

Norethisterone and norethisterone acetate may be given orally, usually in divided doses, for the treatment of conditions such as menorrhagia (below) and endometriosis. In menorrhagia (dysfunctional uterine bleeding), norethisterone is given in usual doses of 10 to 15 mg daily and norethisterone acetate in doses of 2.5 to 10 mg daily, in a cyclical regimen. In endometriosis the dosage of norethisterone is 10 to 25 mg daily and of norethisterone acetate 5 to 15 mg daily. Treatment of endometriosis is usually continuous for 4 to 9 months.

Norethisterone has been used in daily doses of up to 15 mg orally in a cyclical regimen in the treatment of premenstrual syndrome. In breast cancer oral doses of up to 60 mg daily of norethisterone have been used.

Administration in children. Although unlicensed in the UK for use in children, the BNFC does include norethisterone for the management of delayed puberty in girls. It is added after 12 to 24 months of oestrogen therapy to establish a menstrual cycle and maintain sexual maturation, in an oral dose of 5 mg once daily for the last 7 days of a 28-day cycle.

Menorrhagia. Although cyclical norethisterone has been widely used for menorrhagia, it is of limited efficacy during ovulatory cycles being most effective for anovulatory bleeding, which occurs in a minority of women with menorrhagia.

Preparations

British Pharmacopoeia 2008: Estradiol and Norethisterone Acetate Tablets; Estradiol and Norethisterone Tablets; Norethisterone Tablets

The United States Pharmacopeia 31, 2008: Estradiol and Norethindrone Acetate Tablets; Norethindrone Acetate and Ethinyl Estradiol Tablets; Norethindrone Acetate Tablets; Norethindrone and Ethinyl Estradiol Tablets; Norethindrone and Nestranol Tablets; Norethindrone Tablets.

Proprietary Preparations

 

Argentina: Ginediol Primolut-Nor Selectan

Australia: Locilan Nicronor Noriday Primolut N

Austria: Duokliman Nicronovum Primolut-Nor

Belgium: Primolut-Nor

Brazil: Nicronor Norestin Primolut-Nor

Canada: Nicronor Norlutate

Chile: Primolut-Nor

Czech Republic: Primolut-Nor

Denmark: Mini-Pe

Finland: Mini-Pill Primolut N Primolut-Nor

France: Milligynon Primolut-Nor

Germany: Gestakadin Noristerat Primolut-Nor Sovel

Greece: Fortilut Primolut-Nor

Hong Kong: Norcolut Primolut N

Hungary: Norcolut

India: Cycloreg Noristerat Norlut Primolut N Styptin

Indonesia: Anore Norelut Primolut N Regumen

Ireland: Noriday Primolut N

Israel: Primolut-Nor

Italy: Primolut-Nor

Malaysia: Depocon Norcolut Noriday Noristerat Primolut N Sunolut Trisequens

Mexico: Noristerat Primolut-Nor

The Netherlands: Primolut N

Norway: Conluclag Primolut N

New Zealand: Noriday Primolut N

Philippines: Noristerat Primolut N

Poland: Primolut-Nor

Portugal: Primolut-Nor

Russia: Primolut-Nor

South Africa: Nicronovum Nur-Isterate Primolut N

Singapore: Norcolut Noristerat Primolut N

Spain: Primolut-Nor

Sweden: Nini-Pe Primolut-Nor

Switzerland: Nicronovum Primolut N

Thailand: Noristerat Primolut N Steron

Turkey: Primolut N

UK: Nicronor Nicronor HPT Noriday Noristerat Primolut N Utovlan

USA: Aygestin Jolivette Nor-QD Ortho Nicronor

 

Multi-ingredient

Argentina: Activelle Estalis Estalis Sequi Estracomb Estragest Evorel Conti Evorel Sequi Kliogest Nesigyna Trial Combi Trial Gest Trial Pack Trisequens

Australia: Brevinor Estalis Continuous Estalis Sequi Estracombi Improvil Kliogest Kliovance Norimin Norinyl-1 Synphasic Trisequens

Austria: Activelle Estalis Estalis Sequens Estracomb Fem-HRT Kliogest Nericomb Nerigest Novofem Ovysmen Perikliman Primosiston Trinovum Trisequens

Belgium: Activelle Estalis Estracombi Kliogest Minestril Novofem Ovysmen Trinovum Trisequens

Brazil: Activelle Biofim Ciclovulon Cliane Estalis Estalis SQ Estracomb Estragest Gineane Ginedisc 50 Plusf Kliogest Negestran Nericomb Nerigest Nesigyna Natifa Pro Noregyna Primosiston Suprema Systen Conti Systen Sequi Trinovum Trisequens

Canada: Brevicon Estalis Estalis Sequi Estracomb FemHRT Loestrin 1.5/30 Ninestrin Ortho 0.5/35 Ortho 1/35 Ortho 7/7/7 Ortho-Novum 1/50 Select 1/35 Synphasic

Chile: Activelle Cliane Enadiol Neta Estracomb Estragest Ginefolin Kliogest Nesigyna Primosiston Trisequens

Czech Republic: Activelle Estalis Estalis Sequi Estrace Plus Estrace-C Estracomb Estragest Kliane Kliogest Nenophase Non-Ovlon Novofem Pausogest Sequidot Systen Conti Systen Sequi Triaklim Trinovum Trisequens

Denmark: Activelle Econ Estracomb Evo-Conti Evo-Sequi Femanor Femasekvens Kliogest Novofem Ostranorm Trinorm Trinovum Trisekvens

Finland: Activelle Estalis Estalis Sekvens Estracomb Evorel Conti Evorel Sequi Kliogest Nericomb Nerigest Novofem Trisekvens

France: Activelle Kliogest Niniphase Novofemme Ortho-Novum 1/35 Triella Trisequens

Germany: Activelle Clionara Conceplan N Estalis Sequi Estracomb Estragest Eve Gynamon Kliogest N Nericomb Nerigest Non-Ovlon Nora-ratiopharm Novofem Ostro-Primolut Ovysmen Primosiston Prosiston Sequostat Sinovula Synphasec Trinovum Trisequens

Greece: Activelle Estalis Estracomb TTS Kliogest Systen Conti Systen Sequi Trisequens

Hong Kong: Activelle Brevinor Estracomb Kliogest Norimin Norinyl-1 Novofem Synphase Trinovum Trisequens

Hungary: Activelle Estracomb Estragest Kliogest Pausogest Triaklim Trisequens Tulita

Ireland: Activelle Brevinor Estalis Estalis Sequi Estracombi Estrapak Evorel Conti Kliogest Novofem Trisequens

Israel: Activelle Evorel Conti Evorel Sequi Kliogest Neno-Net Novofem Trisequens

Italy: Activelle Estalis Sequi Estracomb Kliogest Trisequens

Japan: Ortho 777

Malaysia: Activelle Kliogest

Mexico: Cliane Estalis Estracomb Evorel Conti Nesigyna Norace Norinyl Nostidyn Ortho-Novum 1/35 Ortho-Novum

The Netherlands: Activelle Estalis Estalis Sequi Estracomb Kliogest Nodicon Neocon Novofem Trinovum Trisequens

Norway: Activelle Estalis Estalis Sekvens Kliogest Novofem Synfase Trisekvens

New Zealand: Brevinor Cliane Estrapak Kliogest Kliovance Norimin Norinyl-1 Synphasic Trisequens

Philippines: Kliogest Nicropil

Poland: Activelle Estalis Estalis Sequi Estracomb Kliogest Novofem Systen Conti Systen Sequi Trinovum Trisequens

Portugal: Activelle Estalis Estalis Sequi Estracomb Kliogest Novofem Trisequens

Russia: Non-Ovlon Pausogest Triaklim Trisequens

South Africa: Activelle Brevinor Estracombi Estro-Pause N Evorel Conti Evorel Sequi Kliogest Norinyl-1/28 Novofem Trinovum Trisequens

Singapore: Activelle Estracomb Kliogest Trisequens

Spain: Absorlent Plus Activelle Duofemme Endomina Plus Estalis Estalis Sequi Estracomb Nerigest Nerigest Sequi Trisequens

Sweden: Activelle Estalis Estalis Sekvens Estracomb Evorel Nicronor Femanor Femasekvens Kliogest Novofem Orthonett Novum Synfase Trinovum Trisekvens

Switzerland: Activelle Estalis Estalis Sequi Estracomb Estragest Kliogest N Nericomb Nerigest Novofem Ovysmen Primosiston Systen Conti Systen Sequi Trinovum Trisequens

Thailand: Activelle Anamai

Turkey: Activelle Estracombi Kliogest Nesigyna Trisequens

UK: Binovum Brevinor Climagest Climesse Clinorette Elleste Duet Conti Elleste-Duet Estracombi Estrapak Evorel Conti Evorel Pak Evorel Sequi FemTab Continuous Kliofem Kliovance Loestrin Norimin Norinyl-1 Novofem Nuvelle Continuous Ovysmen Synphase Trinovum Trisequens

USA: Activella Aranelle Balziva Brevicon CombiPatch Estrostep Fe Estrostep Femcon Fe FemHRT Junel Fe Leena Loestrin Loestrin Fe Nodicon Necon 1/50 Necon 10/1 I Necon 0.5/35, 1/35 NEE 1/35 Norinyl I + 35 Norinyl I + 50 Ortho-Novum 1/35 Ortho-Novum 1/50 Ortho-Novum 10/11 Ortho-Novum 7/7/7 Ovcon 35 Ovcon 50 Tilia Fe Tri-Legest Tri-Norinyl Zenchent

Venezuela: Cliane Estracomb Estragest Nesigyna Primosiston-F.

Leave a Reply

  Subscribe  
Notify of