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Home , Nandrolone cypionate, Nandrolone propionate, Nomegestrol, Norethandrolone, Norethisterone, Norethisterone acetate

/ 2119 fluid retention or adverse effect on renal function or serum-lipids. Pharmacopoeias. In Eur. (see p.vii). Mex.: Evra; Neth.: Evra; Norw.: Evra; Philipp.: Evra; Pol.: Evra; Port.: In these reports, intramuscular doses of Ph. Eur. 6.2 ( ). A white or almost white Evra; Rus.: Evra (Евра); S.Afr.: Evra; Singapore: Evra; Spain: Evra; Swed.: have ranged from 100 mg once every 2 weeks4 up to 600 mg crystalline powder. Practically insoluble in water; soluble in al- Evra; Switz.: Evra; Thai.: Evra; UK: Evra; USA: Ortho Evra; Venez.: Evra. weekly,2 and treatment has generally been given for 12 to 24 cohol; freely soluble in acetone. Protect from light. weeks. Profile (BAN, rINN) ⊗ 1. Gold J, et al. Safety and efficacy of nandrolone decanoate for is a structurally related to pro- treatment of wasting in patients with HIV infection. AIDS 1996 17α-Ethyl-17β-hydroxyestr-4-en-3-one; 17β-Hydroxy-19-nor- 10: 745–52. gesterone (p.2125) that has been used in the treatment of men- 2. Sattler FR, et al. Effects of pharmacological doses of nandrolone strual disorders and as the progestogen component of menopau- 17α-pregn-4-en-3-one; Noretandrolona; Noréthandrolone; decanoate and progressive resistance training in immunodefi- sal HRT (p.2071). Typical oral doses are 5 mg daily for 10 to 14 Norethandrolonum. cient patients infected with human immunodeficiency virus. J days of a 28-day cycle. A subdermal implant is under investiga- Норэтандролон Clin Endocrinol Metab 1999; 84: 1268–76. tion as a long-acting progestogen-only contraceptive. C H O = 302.5. 3. Storer TW, et al. A randomized, placebo-controlled trial of nan- 20 30 2 drolone decanoate in human immunodeficiency virus-infected ◊ References. CAS — 52-78-8. ATC — A14AA09. men with mild to moderate weight loss with recombinant human 1. Coutinho EM, et al. Multicenter on the efficacy and growth as active reference treatment. J Clin Endocrinol acceptability of a single contraceptive implant of nomegestrol ATC Vet — QA14AA09. Metab 2005; 90: 4474–82. acetate, Uniplant. Contraception 1996; 53: 121–5. 4. Mulligan K, et al. Effect of nandrolone decanoate therapy on 2. Devoto L, et al. Hormonal profile, endometrial histology and weight and lean body mass in HIV-infected women with weight ovarian ultrasound assessment during 1 year of nomegestrol ac- OH loss: a randomized, double-blind, placebo-controlled, multicent- etate implant (Uniplant ). Hum Reprod 1997; 12: 708–13. H3C CH3 er trial. Arch Intern Med 2005; 165: 578–85. 3. Barbosa IC, et al. Carbohydrate in sickle pa- 5. Gold J, et al. Effects of nandrolone decanoate compared with tients using a subdermal implant containing nomegestrol acetate placebo or on HIV-associated wasting. HIV Med (Uniplant). Contraception 2001; 63: 263–5. H H 2006; 7: 146–55. 4. Arowojolu AO, Ladipo OA. Nonmenstrual adverse events asso- 6. Johansen KL, et al. Anabolic effects of nandrolone decanoate in ciated with subdermal contraceptive implants containing patients receiving dialysis: a randomized controlled trial. JAMA normegestrel [sic] and . Afr J Med Med Sci 2003; H H 1999; 281: 1275–81. 32: 27–31. 7. Johansen KL, et al. Effects of resistance exercise training and 5. Barbosa IC, et al. Effects of a single Silastic contraceptive im- O nandrolone decanoate on body composition and muscle function plant containing nomegestrol acetate (Uniplant) on endometrial among patients who receive hemodialysis: a randomized, con- morphology and ovarian function for 1 year. Contraception trolled trial. J Am Soc Nephrol 2006; 17: 2307–14. 2006; 74: 492–7. Adverse Effects and Precautions 8. Eiam-Ong S, et al. Nutritional effect of nandrolone decanoate in As for and anabolic in general (see Testoster- predialysis patients with chronic kidney disease. J Ren Nutr Preparations one, p.2130). As with other 17α-alkylated compounds, 2007; 17: 173–8. Proprietary Preparations (details are given in Part 3) norethandrolone may produce and function Male contraception. Preliminary findings showed that nan- Arg.: Lutenyl; Belg.: Lutenyl; Braz.: Lutenil; Chile: Lutenyl; Cz.: Lutenyl†; should be monitored. It should probably be avoided in patients 1-3 Hong Kong: Lutenyl; Indon.: Lutenyl; Ital.: Lutenyl; Mex.: Luvenyl; Mon.: with impaired liver function, and certainly if this is severe. drolone suppressed , suggesting potential as a Lutenyl; Pol.: Lutenyl; Port.: Lutenyl; Turk.: Lutenyl; Venez.: Lutenyl†. (p.2070), but later studies seem to have fa- Multi-ingredient: Ital.: Naemis; Mon.: Naemis; Neth.: Naemis; Port.: Uses and Administration voured other androgens. Naemis. Norethandrolone is an anabolic with some androgenic 1. Schürmeyer T, et al. Reversible azoospermia induced by the an- properties (see Testosterone, p.2131). It is given in the treatment abolic steroid 19-nortestosterone. Lancet 1984; i: 417–20. of aplastic anaemia in an oral dose of 0.25 to 2 mg/kg daily. 2. Knuth UA, et al. Combination of 19-nortestosterone-hexyloxy- phenyl-propionate (Anadur) and depot-- (BAN, USAN, rINN) Preparations acetate (Clinovir) for male contraception. Fertil Steril 1989; 51: Proprietary Preparations (details are given in Part 3) 1011–18. 17-Deacylnorgestimate; Norelgestromiini; Norelgestromina; Fr.: Nilevar. 3. WHO Task Force on Methods for the Regulation of Male Fertil- Norelgestromine; Norelgestrominum; RWJ-10553. 13-Ethyl-17- ity. Comparison of two androgens plus depot-medroxyprogester- hydroxy-18,19-dinor-17α-pregn-4-en-20-yn-3-one oxime. one acetate for suppression to azoospermia in Indonesian men. Fertil Steril 1993; 60: 1062–8. Норэльгестромин Norethisterone (BAN, pINN) Preparations C21H29NO2 = 327.5. CAS — 53016-31-2. BP 2008: Nandrolone Decanoate Injection; Nandrolone Phenylpropionate Ethinylnortestosterone; Etinil hidroxiestrona; Etinilnortestostero- Injection; na; Norethindrone; Norethisteron; Noréthistérone; Norethister- USP 31: Nandrolone Decanoate Injection; Nandrolone Phenpropionate onum; Noretindrona; Noretisteron; Noretisterona; Noretistero- H C OH CH Injection. 3 nas; Noretisterone; Noretisteroni; Noretiszteron; Noretysteron; Proprietary Preparations (details are given in Part 3) Norpregneninolona; Norpregneninolone; NSC-9564. 17β-Hy- Arg.: Deca-Durabolin; Keratyl†; Austral.: Deca-Durabolin; Austria: Deca- droxy-19-nor-17α-pregn-4-en-20-yn-3-one. Durabolin; Belg.: Deca-Durabolin; Braz.: Deca-Durabolin; Canad.: Deca- HH Durabolin; Chile: Anaprolina; Deca-Durabolin; Nandrosande; Cz.: Deca- Норэтистерон Durabolin†; Keratyl†; Superanabolon; Fin.: Deca-Durabolin; Fr.: Keratyl†; C H O = 298.4. Ger.: Deca-Durabolin; Keratyl†; Gr.: Anaboline Depot; Deca-Durabolin; 20 26 2 Extraboline; Nurezan†; Hong Kong: Deca-Durabolin; Hung.: Retabolil; HH CAS — 68-22-4. India: Deca-Durabolin; Decaneurabol†; Durabolin; Metabol; Metadec; HO ATC — G03AC01; G03DC02. Neurabol; Indon.: Deca-Durabolin; Ital.: Deca-Durabolin; Dynabolon†; N Malaysia: Deca-Durabolin; Mex.: Deca-Durabolin; Neth.: Deca-Durab- ATC Vet — QG03AC01; QG03DC02. olin; Durabolin; Norw.: Deca-Durabolin; NZ: Deca-Durabolin; Pol.: Deca- Profile Durabolin; Port.: Deca-Durabolin; Nandain†; Rus.: Retabolil (Ретаболил); S.Afr.: Deca-Durabolin; Singapore: Deca-Durabolin; Spain: Deca-Du- Norelgestromin is a progestogen (see , p.2125); it is OH H the primary active of (p.2121). Nore- rabolin; Swed.: Deca-Durabol; Switz.: Deca-Durabolin; Keratyl; Thai.: H3C Deca-Durabolin; Keratyl; UK: Deca-Durabolin; USA: Androlone-D; Deca- lgestromin is used as the progestogenic component of a com- Durabolin; Durabolin; Hybolin; Neo-Durabolic; Venez.: Deca-Durabolin. bined contraceptive . A dose of Multi-ingredient: Arg.: Dexatopic†; Indon.: Dexatopic; Neth.: Dexat- 150 micrograms of norelgestromin is released daily with ethi- H H opic†. nylestradiol. A new patch is applied each week for 3 weeks of a 4-week cycle. Norelgestromin exposure from such a patch may H H be greater than that resulting from a comparable oral contracep- Nomegestrol Acetate (BANM, rINNM) tive. O Acetato de nomegestrol; Nomegestrol acetát; Nomégestrol, ◊ References. Pharmacopoeias. In Chin., Eur. (see p.vii), Int., Jpn, and US. acétate de; Nomegestrol Asetat; Nomegestrolacetat; Nomeges- 1. Audet M-C, et al. Evaluation of contraceptive efficacy and cycle Ph. Eur. 6.2 (Norethisterone). A white or yellowish-white crys- troli acetas; Nomegestroliasetaatti; Nomegestrolio acetatas; No- control of a transdermal vs an oral contra- ceptive: a randomized controlled trial. JAMA 2001; 285: talline powder. Practically insoluble in water; sparingly soluble megesztrol-acetát. 17-Hydroxy-6-methyl-19-norpregna-4,6-di- 2347–54. in dehydrated alcohol and in acetone; soluble in dichlorometh- ene-3,20-dione acetate. 2. Abrams LS, et al. of norelgestromin and ethi- ane. Номегестрола Ацетат nyl from two consecutive contraceptive patches. J Clin USP 31 (Norethindrone). A white to creamy-white odourless Pharmacol 2001; 41: 1232–7. C23H30O4 = 370.5. 3. Abrams LS, et al. Pharmacokinetics of norelgestromin and ethi- crystalline powder. Practically insoluble in water; sparingly sol- CAS — 58691-88-6 (nomegestrol); 58652-20-3 (nomeg- nyl estradiol delivered by a contraceptive patch (Ortho uble in alcohol; soluble in chloroform and in dioxan; slightly sol- estrol acetate). Evra /Evra ) under conditions of heat, humidity, and exercise. uble in ether. ATC — G03DB04. J Clin Pharmacol 2001; 41: 1301–9. 4. Abrams LS, et al. Pharmacokinetics of a contraceptive patch ATC Vet — QG03DB04. (BANM, pINNM) (Evra /Ortho Evra ) containing norelgestromin and ethiny- loestradiol at four application sites. Br J Clin Pharmacol 2002; Acetato de noretisterona; Norethindrone Acetate; Norethister- 53: 141–6. on-acetát; Noréthistérone, acétate de; Norethisteroni acetas; OCH3 5. Burkman RT. The transdermal contraceptive system. Am J Ob- stet Gynecol 2004; 190 (suppl): S49–S53. Noretisteron Asetat; Noretisteronacetat; Noretisteroniasetaatti; H3C OH 6. Devineni D, et al. Pharmacokinetics and of Noretisterono acetatas; Noretiszteron-acetát. 17β-Hydroxy-19- a transdermal contraceptive patch and an oral contraceptive. J nor-17α-pregn-4-en-20-yn-3-one acetate; 3-Oxo-19-nor-17α- Clin Pharmacol 2007; 47: 497–509. pregn-4-en-20-yn-17β-yl acetate. HH 7. Jick S, et al. Further results on the risk of nonfatal venous throm- boembolism in users of the contraceptive transdermal patch Норэтистерона Ацетат compared to users of oral contraceptives containing norgesti- C22H28O3 = 340.5. H H mate and 35 μg of ethinyl estradiol. Contraception 2007; 76: CAS — 51-98-9. 4–7. ATC — G03AC01; G03DC02. O Preparations ATC Vet — QG03AC01; QG03DC02. CH3 Proprietary Preparations (details are given in Part 3) Pharmacopoeias. In Eur. (see p.vii), Int., and US. Ph. Eur. 6.2 (Norethisterone Acetate). A white or yellowish- Multi-ingredient: Arg.: Evra; Belg.: Evra; Braz.: Evra; Canad.: Evra; (nomegestrol) Chile: Evra; Cz.: Evra; Denm.: Evra; Fin.: Evra; Fr.: Evra; Ger.: Evra; Gr.: white crystalline powder. It exhibits polymorphism. Practically Evra; Hong Kong: Evra; Hung.: Evra; Irl.: Evra; Israel: Evra; Ital.: Evra; insoluble in water; soluble in alcohol; freely soluble in dichlo- The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii) 2120 Sex and their Modulators romethane. Protect from light. nortestosterone that have weak oestrogenic and andro- Activelle; Biofim†; Ciclovulon; Cliane; Estalis; Estalis SQ; Estracomb†; Estrag- USP 31 (Norethindrone Acetate). A white to creamy-white est; Gineane; Ginedisc 50 Plus†; Kliogest; Megestran†; Mericomb; Merigest; genic properties. They are commonly used as hormo- Mesigyna; Natifa Pro; Noregyna; Primosiston; Suprema; Systen Conti; Sys- odourless crystalline powder. Practically insoluble in water; sol- nal contraceptives (see p.2069). Norethisterone and ten Sequi; Trinovum†; Trisequens; Canad.: Brevicon; Estalis; Estalis Sequi; uble 1 in 10 of alcohol, 1 in less than 1 of chloroform, 1 in 2 of Estracomb; FemHRT; Loestrin 1.5/30; Minestrin; Ortho 0.5/35; Ortho 1/35; dioxan, and 1 in 18 of ether. norethisterone acetate are both given orally. Typical Ortho 7/7/7; Ortho-Novum 1/50†; Select 1/35; Synphasic; Chile: Activelle; daily doses are 350 micrograms for norethisterone and Cliane; Enadiol Neta; Estracomb; Estragest; Ginefolin; Kliogest; Mesigyna; Primosiston; Trisequens; Cz.: Activelle; Estalis; Estalis Sequi; Estrace Plus†; Norethisterone Enantate (BANM, pINNM) 600 micrograms for norethisterone acetate when used Estrace-C†; Estracomb†; Estragest†; Kliane; Kliogest; Menophase†; Non- alone, or 0.5 to 1 mg for norethisterone and 1 to 1.5 mg Ovlon†; Novofem; Pausogest; Sequidot; Systen Conti; Systen Sequi; Triak- Enantato de noretisterona; Norestisteron Enantat; Norethin- lim†; Trinovum; Trisequens; Denm.: Activelle; Econ†; Estracomb; Evo-Con- drone Enanthate; Noréthistérone, Enantate de; Norethisterone for norethisterone acetate when used with an oestro- ti; Evo-Sequi; Femanor; Femasekvens; Kliogest; Novofem; Ostranorm†; Tri- Enanthate; Norethisterone Heptanoate; Norethisteroni Enantas. gen. Norethisterone enantate is given by intramuscular norm†; Trinovum; Trisekvens; Fin.: Activelle; Estalis; Estalis Sekvens; Estracomb†; Evorel Conti; Evorel Sequi; Kliogest; Mericomb; Merigest; 17β-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one heptanoate. injection; a dose of 200 mg provides contraception for Novofem; Trisekvens; Fr.: Activelle; Kliogest; Miniphase; Novofemme; Or- Норэтистерона Энантат 8 weeks. An containing nore- tho-Novum 1/35; Triella; Trisequens; Ger.: Activelle; Clionara; Conceplan M; Estalis Sequi; Estracomb†; Estragest; Eve; Gynamon; Kliogest N; Meri- C27H38O3 = 410.6. thisterone enantate 50 mg with 5 mg comb; Merigest; Non-Ovlon†; Nora-ratiopharm†; Novofem; Ostro-Primo- CAS — 3836-23-5. is given once each month. lut†; Ovysmen†; Primosiston†; Prosiston†; Sequostat†; Sinovula†; Syn- ATC — G03AC01; G03DC02. phasec; Trinovum; Trisequens; Gr.: Activelle†; Estalis; Estracomb TTS; ATC Vet — QG03AC01; QG03DC02. Norethisterone and norethisterone acetate are used as Kliogest; Systen Conti; Systen Sequi; Trisequens; Hong Kong: Activelle; Brevinor; Estracomb; Kliogest; Norimin†; Norinyl-1; Novofem; Synphase†; Pharmacopoeias. In Int. the progestogen component of menopausal HRT (see Trinovum†; Trisequens; Hung.: Activelle; Estracomb; Estragest; Kliogest; p.2076). Typical regimens have included either contin- Pausogest; Triaklim; Trisequens; Tulita; Irl.: Activelle; Brevinor; Estalis; Estalis Sequi; Estracombi; Estrapak†; Evorel Conti; Kliogest; Novofem; Trisequens; Adverse Effects and Precautions uous daily doses of norethisterone 700 micrograms or Israel: Activelle; Evorel Conti; Evorel Sequi; Kliogest; Meno-Net†; As for in general (see Progesterone, norethisterone acetate 0.5 to 1 mg, or cyclical regimens Novofem; Trisequens; Ital.: Activelle; Estalis Sequi; Estracomb; Kliogest; Trisequens; Jpn: Ortho 777; Malaysia: Activelle; Kliogest†; Mex.: Cliane; p.2125). See also under Hormonal Contraceptives, of norethisterone or norethisterone acetate 1 mg daily Estalis; Estracomb; Evorel Conti; Mesigyna; Norace; Norinyl; Nostidyn; Or- p.2059. for 10 to 12 days of a 28-day cycle. Norethisterone ac- tho-Novum 1/35; Ortho-Novum†; Neth.: Activelle; Estalis; Estalis Sequi; etate is also available as transdermal patches supplying Estracomb; Kliogest; Modicon; Neocon; Novofem; Trinovum; Trisequens; Effects on the liver. There were 6 cases of among 107 Norw.: Activelle; Estalis; Estalis Sekvens; Kliogest; Novofem; Synfase; patients with cancer treated with high-dose norethisterone 140, 170, or 250 micrograms in 24 hours, that are ap- Tr isekvens; NZ: Brevinor; Cliane; Estrapak†; Kliogest; Kliovance; Norimin; 1 Norinyl-1; Synphasic; Trisequens; Philipp.: Kliogest; Micropil; Pol.: Activ- acetate; the jaundice was reversible and of an obstructive type. plied twice weekly for 2 weeks of a 4-week cycle; the elle; Estalis; Estalis Sequi; Estracomb; Kliogest; Novofem; Systen Conti; Sys- A retrospective analysis2 found that the use of norethisterone to lower strengths may also be applied twice weekly on a ten Sequi; Trinovum; Trisequens; Port.: Activelle; Estalis; Estalis Sequi; Estra- prevent menstrual haemorrhage during the thrombocytopenic continuous basis. comb; Kliogest; Novofem; Trisequens; Rus.: Non-Ovlon (Нон-овлон); phase of allogeneic bone marrow transplantation was a signifi- Pausogest (Паузогест); Triaklim (Триаклим); Trisequens (Трисеквенс); Norethisterone and norethisterone acetate may be giv- S.Afr.: Activelle; Brevinor†; Estracombi; Estro-Pause N; Evorel Conti; Evorel cant risk factor for hepatic veno-occlusive disease. Sequi; Kliogest; Norinyl-1/28; Novofem; Trinovum; Trisequens; Singapore: 1. Langlands AO, Martin WMC. Jaundice associated with norethis- en orally, usually in divided doses, for the treatment of Activelle; Estracomb; Kliogest; Trisequens; Spain: Absorlent Plus; Activelle; terone-acetate treatment of . Lancet 1975; i: 584–5. conditions such as menorrhagia (below) and en- Duofemme; Endomina Plus; Estalis; Estalis Sequi; Estracomb; Merigest; Mer- 2. Hägglund H, et al. Norethisterone treatment, a major risk-factor igest Sequi; Trisequens; Swed.: Activelle; Estalis; Estalis Sekvens; Estra- for veno-occlusive disease in the liver after allogeneic bone mar- dometriosis (p.2091). In menorrhagia (dysfunctional comb†; Evorel Micronor; Femanor; Femasekvens; Kliogest; Novofem; Or- row transplantation. Blood 1998; 92: 4568–72. uterine bleeding), norethisterone is given in usual dos- thonett Novum; Synfase; Trinovum; Trisekvens; Switz.: Activelle; Estalis; Estalis Sequi; Estracomb; Estragest; Kliogest N; Mericomb; Merigest; Porphyria. Norethisterone has been associated with acute at- es of 10 to 15 mg daily and norethisterone acetate in Novofem; Ovysmen; Primosiston; Systen Conti; Systen Sequi; Trinovum; tacks of porphyria and is considered unsafe in porphyric patients. doses of 2.5 to 10 mg daily, in a cyclical regimen. In Trisequens; Thai.: Activelle; Anamai†; Turk.: Activelle; Estracombi; Kliogest; Mesigyna; Trisequens; UK: Binovum; Brevinor; Climagest; Climesse; Clinor- . Abnormalities seen in the offspring of women giv- the dosage of norethisterone is 10 to ette; Elleste Duet Conti; Elleste-Duet; Estracombi; Estrapak†; Evorel Conti; en norethisterone during pregnancy (either alone or with ethi- 25 mg daily and of norethisterone acetate 5 to 15 mg Evorel Pak†; Evorel Sequi; FemTab Continuous†; Kliofem; Kliovance; Loestrin; Norimin; Norinyl-1; Novofem; Nuvelle Continuous; Ovysmen; nylestradiol) included: hypospadias,1 masculinisation of female daily. Treatment of endometriosis is usually continu- 2 3 Synphase; Trinovum; Trisequens; USA: Activella; Aranelle; Balziva; Brevicon; infants, meningomyelocele or hydrocephalus, and neonatal ous for 4 to 9 months. CombiPatch; Estrostep Fe; Estrostep†; Femcon Fe; FemHRT; Junel Fe; Lee- choreoathetosis associated with oral contraceptive use.4 For ref- na; Loestrin; Loestrin Fe; Modicon; Necon 1/50; Necon 10/11; Necon erence to the fact that oral contraceptives have not generally been Norethisterone has been used in daily doses of up to 0.5/35, 1/35; NEE 1/35; Norinyl 1 + 35; Norinyl 1 + 50; Ortho-Novum 1/35; Ortho-Novum 1/50; Ortho-Novum 10/11; Ortho-Novum 7/7/7; associated with teratogenicity, even when used inadvertently in 15 mg orally in a cyclical regimen in the treatment of Ovcon 35; Ovcon 50; Tilia Fe; Tri-Legest; Tri-Norinyl; Zenchent; Venez.: pregnancy, see p.2067. premenstrual syndrome (p.2099). Cliane; Estracomb†; Estragest; Mesigyna; Primosiston†. 1. Aarskog D. Clinical and cytogenetic studies in hypospadias. Acta Paediatr Scand 1970; (suppl 203): 1–62. In breast cancer (p.661) oral doses of up to 60 mg dai- 2. Wilkins L. Masculinization of female due to use of orally ly of norethisterone have been used. given progestins. JAMA 1960; 172: 1028–32. (BAN, rINN) 3. Gal I, et al. Hormonal pregnancy tests and congenital malforma- Administration in children. Although unlicensed in the UK tion. Nature 1967; 216: 83. for use in children, the BNFC does include norethisterone for the Norethynodrel (USAN); Noretinodrel; Noretynodreeli; Norétyn- 4. Profumo R, et al. Neonatal choreoathetosis following prenatal management of delayed puberty (p.2079) in girls. It is added af- odrel; Noretynodrelum; NSC-15432; SC-4642. 17β-Hydroxy- exposure to oral contraceptives. Pediatrics 1990; 86: 648–9. ter 12 to 24 months of oestrogen therapy to establish a menstrual 19-nor-17α-pregn-5(10)-en-20-yn-3-one. cycle and maintain sexual maturation, in an oral dose of 5 mg Venous thromboembolism. For mention that combined oral Норэтинодрел contraceptives containing older progestogens such as norethis- once daily for the last 7 days of a 28-day cycle. terone appear to be associated with a lower incidence of venous C20H26O2 = 298.4. Menorrhagia. Although cyclical norethisterone has been wide- CAS — 68-23-5. thromboembolism than - or -containing ly used for menorrhagia (p.2126), it is of limited efficacy during preparations, see p.2063. ovulatory cycles1 being most effective for anovulatory bleeding, which occurs in a minority of women with menorrhagia. OH CH Interactions 1. Lethaby A, et al. Cyclical progestogens for heavy menstrual H C As for progestogens in general (see Progesterone, bleeding. Available in The Cochrane Database of Systematic Re- 3 views; Issue 1. Chichester: John Wiley; 2008 (accessed p.2126). See also under Hormonal Contraceptives, 27/06/08). p.2067. H Preparations BP 2008: Estradiol and Norethisterone Acetate Tablets; Estradiol and H H Pharmacokinetics Norethisterone Tablets; Norethisterone Tablets; Norethisterone is absorbed from the gastrointestinal USP 31: Estradiol and Norethindrone Acetate Tablets; Norethindrone Ac- O etate and Ethinyl Estradiol Tablets; Norethindrone Acetate Tablets; Nore- tract, undergoing first-pass hepatic metabolism, with thindrone and Ethinyl Estradiol Tablets; Norethindrone and Tab- peak plasma concentrations occurring 1 to 2 hours after lets; Norethindrone Tablets. Pharmacopoeias. In US. an oral dose. It exhibits biphasic pharmacokinetics; an Proprietary Preparations (details are given in Part 3) USP 31 (Norethynodrel). A white or practically white, odour- initial distribution phase is followed by a prolonged Arg.: Ginediol; Primolut-Nor; Selectan; Austral.: Locilan; Micronor; Nori- less, crystalline powder. Very slightly soluble in water and in pe- day; Primolut N; Austria: Duokliman; Micronovum; Primolut-Nor; Belg.: troleum spirit; sparingly soluble in alcohol; soluble in acetone; elimination phase with a half-life of about 8 hours or Primolut-Nor; Braz.: Micronor; Norestin; Primolut-Nor; Canad.: Micro- freely soluble in chloroform. more. Norethisterone is highly protein bound; about nor; Norlutate†; Chile: Primolut-Nor; Cz.: Primolut-Nor†; Denm.: Mini- Pe; Fin.: Mini-Pill; Primolut N; Primolut-Nor; Fr.: Milligynon; Primolut-Nor; 60% to albumin and 35% to binding Profile Ger.: Gestakadin; Noristerat; Primolut-Nor; Sovel†; Gr.: Fortilut; Primolut- Noretynodrel is a progestogen (see Progesterone, p.2125) struc- globulin. Use with an oestrogen increases the propor- Nor; Hong Kong: Norcolut; Primolut N; Hung.: Norcolut; India: Cy- cloreg; Noristerat; Norlut; Primolut N; Styptin; Indon.: Anore; Norelut; Pri- turally related to norethisterone that has been given orally with tion bound to sex hormone binding globulin. It is me- molut N; Regumen; Irl.: Noriday; Primolut N; Israel: Primolut-Nor; Ital.: an oestrogen such as mestranol for the treatment of various men- tabolised in the liver with 50 to 80% of a dose being Primolut-Nor; Malaysia: Depocon; Norcolut; Noriday; Noristerat; Primo- strual disorders and endometriosis. lut N; Sunolut; Trisequens†; Mex.: Noristerat; Primolut-Nor; Neth.: Pri- excreted in the and up to 40% appearing in the molut N; Norw.: Conludag; Primolut N; NZ: Noriday; Primolut N; Breast feeding. About 1% of an oral dose of radiolabelled faeces. Philipp.: Noristerat; Primolut N; Pol.: Primolut-Nor; Port.: Primolut-Nor; noretynodrel was detected in in a study of 4 women.1 Rus.: Primolut-Nor (Примолют-нор); S.Afr.: Micronovum; Nur-Isterate; Norethisterone acetate is rapidly hydrolysed to nore- Primolut N; Singapore: Norcolut; Noristerat†; Primolut N; Spain: Primo- No adverse effects have been seen in breast-fed infants of moth- lut-Nor; Swed.: Mini-Pe; Primolut-Nor; Switz.: Micronovum; Primolut N; ers given noretynodrel, and the American Academy of Pediatrics thisterone, principally by intestinal tissue. Thai.: Noristerat†; Primolut N; Steron; Turk.: Primolut N; UK: Micronor; considers2 that it is therefore usually compatible with breast feed- After intramuscular injection of norethisterone enan- Micronor HRT†; Noriday; Noristerat; Primolut N; Utovlan; USA: Aygestin; ing. Jolivette; Nor-QD; Ortho Micronor. tate peak concentrations of norethisterone in plasma 1. Laumas KR, et al. Radioactivity in the breast milk of lactating Multi-ingredient: Arg.: Activelle; Estalis; Estalis Sequi; Estracomb; Estrag- women after oral administration of H-norethynodrel. Am J Ob- are not attained for several days. est; Evorel Conti; Evorel Sequi; Kliogest; Mesigyna; Trial Combi; Trial Gest; Trial Pack†; Trisequens; Austral.: Brevinor; Estalis Continuous; Estalis Sequi; stet Gynecol 1967; 98: 411–3. Estracombi; Improvil; Kliogest; Kliovance; Norimin; Norinyl-1; Synphasic; 2. American Academy of Pediatrics. The transfer of drugs and oth- Uses and Administration Trisequens; Austria: Activelle; Estalis; Estalis Sequens; Estracomb; Fem- er chemicals into human milk. Pediatrics 2001; 108: 776–89. Norethisterone and its acetate and enantate esters are HRT†; Kliogest; Mericomb; Merigest; Novofem; Ovysmen; Perikliman; Pri- Correction. ibid.; 1029. Also available at: mosiston; Trinovum; Trisequens; Belg.: Activelle; Estalis; Estracombi; Klio- http://aappolicy.aappublications.org/cgi/content/full/ progestogens (see Progesterone, p.2126) derived from gest; Minestril†; Novofem; Ovysmen; Trinovum; Trisequens; Braz.: pediatrics%3b108/3/776 (accessed 27/06/08)