Norethisterone

Has the properties of progesterone and is given orally for treating functional uterine haemorrhage. Norethisterone, 19-norelhisterone, m.p. 20I-206°C is one of the progestational steroids used in the contraceptive pill. 

Chemical Nama 17-hydroxy-19-nor-17o -pregn-4-en-20-yn-3-one Common Nama Norethisteron Structural Formula ... 

Norethisteron (Jenapharm) Primolut-Nor (Schering) Primosiston (Schering)-comb. 

C,4H2f,03 626-27-7) see Norethisterone enanthate Prasterone enanthate testosterone enanthate l.-ephedrine... 

CigH2402 1624-62-0) see Estriol Mestranol Methylestrenolone Norethisterone Noretynodrel Promegestone ethane-l,2-dithlol... 

FIGURE 2 Comparison of in vitro release profiles of phase II and phase III clinical batches of 90-day norethisterone microspheres. 

FIGURE 3 Batch-to-batch reproducibility of 90-day norethisterone microspheres as determined by in vitro release profiles. 

The earliest reports of controlled release steroids were those of Jackanicz (63), Yolles (64), Anderson (65), and Wise (66). Most of those early studies were based on poly[ (L+)-lactic acid). Implants and granular particles were fabricated with progesterone, norgestrel, and norethisterone. In vivo urinary excretion studies were conducted on [I Cjprogesterone beads (64). The reported results were somewhat questionable as only 20% of the original implanted drug could be accounted for. 

FIGURE 5 Scanning electron micrograph of 90-day norethisterone microspheres 45-90 pm in diameter and containing 47% by weight drug. 

The most commonly used oral progestogens are medroxyprogesterone acetate, micronized progesterone, and norethisterone acetate. 

Neven P, Lunde T, Benedetti-Panici P, Tiitinen A, Marinescu B, Villiers T, Hillard T, Cano A, Peer E, Quail D, Nickelsen T (2003) A multicentre randomised trial to compare uterine safety of raloxifene with a continuous combined hormone replacement therapy containing oestradiol and norethisterone acetate. Br J Obstet Gynaecol 110 157-167... 

The oral contraceptive norethisterone (norethindrone, 129) has been shown to produce the 4/ ,5/ -epoxide (130) over a 30 min irradiation at 300 nm in aqueous buffer at pH 7.4. The possibility that this reactive species is responsible for the non-dermatological side-effects of oral contraceptives containing norethisterone was noted. One serious systemic effect of the drug which could be caused... 

Hydroxylation ergotamine phenylalanine tyrosine norethisterone oestrone phenytoin phylloquinone... 

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