Sex Hormone Binding Globulin : The Carrier Protein For d-Norgestrel

Victor, Arne; Weiner, Erik; Johansson, Elof D. B.

doi:10.1210/jcem-43-1-244

Cited by 119 publications

(26 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This is explained by a higher concentration of SHBG during treatment with preparation 5049. Levonorgestrel binds to SHBG with an affinity between that of testosterone and estradiol [11], Ethinyl estradiol will induce an increased production of SHBG [11] while treatment with levonorgestrel will decrease the concentration of SHBG significantly [10],…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Ovarian Function during Treatment with High Ratio Levonorgestrel/Ethinyl Estradiol as Oral Contraceptives

Johansson¹,

Elamsson²,

Elmestedt³

1982

Gynecol Obstet Invest

View full text Add to dashboard Cite

Levonorgestrel 250 µg was combined with 30 or 20 µg of ethinyl estradiol and tested as an oral contraceptive for effects on the ovarian function and changes in sex hormone binding globulin (SHBG) in a random crossover study of 5 women. Both combinations inhibited ovulation but the 20 µg ethinyl estradiol combination allowed for development of follicles as judged by increasing estradiol concentrations in 3 out of 5 women. The concentration of SHBG was slightly decreased in the 250/20 preparation, probably a result of the SHBG lowering effect of levonorgestrel that was not enough counteracted by the SHBG raising effect of ethinyl estradiol.

show abstract

Section: Discussionmentioning

confidence: 99%

“…Progesterone in plasma was analyzed according to Bosu et al [1] and levonorgestrel according to Victor et al [10], The sex steroid binding globulin (SHBG) was analyzed according to Rosner [7] with minor modifications, Victor et al [11].…”

Section: Methodsmentioning

confidence: 99%

Ovarian Function during Treatment with High Ratio Levonorgestrel/Ethinyl Estradiol as Oral Contraceptives

Johansson¹,

Elamsson²,

Elmestedt³

1982

Gynecol Obstet Invest

View full text Add to dashboard Cite

show abstract

“…The binding capacity of SHBG for norethisterone and levonorgestrel is usually about 40-70 nmol 1-' (Back et al, 1978b;Victor et al, 1976) and this binding capacity can be enhanced by both ethinyloestradiol (Anderson, 1974;Odlind et al, 1980) and drugs such as phenobarbitone (Backstrom & Sodergard, 1977). There is a close correlation between the SHBG capacity and the plasma concentration of norethisterone (Back et al, 1978b) and levonorgestrel (Nilsson et al, 1977).…”

Section: Protein Binding Ofcontraceptive Steroidsmentioning

confidence: 99%

The third S.K. & F. Prize lecture, University of London, December 1981. The clinical pharmacology of oral contraceptive steroids.

Orme¹

1982

Brit J Clinical Pharma

View full text Add to dashboard Cite

Oral contraceptive steroids have been in regular use for some 20 years and are taken by about 50 million women worldwide. It is therefore surprising to find that information on the clinical pharmacology of such commonly used drugs is so lacking. There are a number of possible reasons for this state of affairs, but at least partly this is due to the fact that oral contraceptive steroids occupy a unique position in therapeutics in being given to a healthy group of women. In addition, oral contraceptive steroids were, for a long time, given in supratherapeutic doses. With the realisation that side effects were occurring, and that some of these were clearly dose related, the dose of steroid in the combined preparations was gradually reduced. As the dose has been reduced, the problems associated with interindividual variations in elimination have become apparent, thus highlighting our previous lack of knowledge. The first combination preparation to undergo large scale clinical trial was Enovid which contained 150 ,tg of oestrogen (mestranol) and 10 mg of progestogen (norethynodrel). Most combined preparations now contain 1 mg or less of progestogen and about 30 ,ug of the oestrogen (ethinyloestradiol). The latest triphasic preparations contain an even lower total dose of steroid.We are now at such a stage that it would be difficult to reduce the total dose level much further without impairing the contraceptive efficacy of the preparation. Any factor which interferes with the bioavailability of the contraceptive steroids is likely to cause failure of contraception and this is reflected in the increasing interest in drug interactions with the contraceptive steroids. Pharmacokinetics of contraceptive steroidsThere is a wide inter-individual range in the plasma concentrations of steroids, measured in blood samples taken 10-12 h after dosing in women on long term treatment. Figure 1 shows the plasma concentrations of ethinyloestradiol and levonorgestrel given at two dose levels to groups of women. There is a 20-30 fold variation in the steady state plasma concentration of each steroid.

show abstract

“…Levonorgestrel and norethisterone display significant SHBG binding [7][8][9] and there are data that also 3-ketodesogestrel, the active metabolite of desogestrel, is bound to SHBG with high affinity. Therefore, the affin ities of desogestrel, 3-keto-desogestrel, ethisterone, nore thisterone, levonorgestrel, medroxyprogesterone acetate and testosterone for SHBG binding were compared by the use of an equilibrium partition method.…”

Section: Introductionmentioning

confidence: 99%

Binding of Levonorgestrel, Norethisterone and Desogestrel to Human Sex Hormone Binding Globulin and Influence on Free Testosterone Levels

Nilsson

Schoultz²

1989

Gynecol Obstet Invest

View full text Add to dashboard Cite

The progestogens desogestrel, levonorgestrel, lynestrenol and norethisterone are known to display certain androgenic effects. Apart from direct androgen receptor interaction, binding to sex hormone binding globulin (SHBG) and displacement of testosterone could lead to an increase in free, metabolically active testosterone. The affinities for SHBG binding of some progestogens including levonorgestrel, norethisterone and the active metabolite of desogestrel, 3-keto-desogestrel, were compared using an equilibrium partition method, and the distribution between free and protein-bound testosterone during progestogen therapy was calculated with the use of a computer program. During treatment with desogestrel, levonorgestrel and norethisterone alone, testosterone displacement could account for a slight increase in free testosterone, though the decrease in serum SHBG following treatment was found to be more important in this respect. Also during treatment with combinations of ethinyl estradiol and levonorgestrel for oral contraception, testosterone displacement could theoretically have a slight influence on free testosterone levels. Combinations with ethinyl estradiol and desogestrel or norethisterone, on the other hand, cause an increase in SHBG concentration and as a result a fall in free testosterone which could not be compensated via testosterone displacement.

show abstract

Sex Hormone Binding Globulin : The Carrier Protein For d-Norgestrel

Cited by 119 publications

References 0 publications

Ovarian Function during Treatment with High Ratio Levonorgestrel/Ethinyl Estradiol as Oral Contraceptives

Ovarian Function during Treatment with High Ratio Levonorgestrel/Ethinyl Estradiol as Oral Contraceptives

The third S.K. & F. Prize lecture, University of London, December 1981. The clinical pharmacology of oral contraceptive steroids.

Binding of Levonorgestrel, Norethisterone and Desogestrel to Human Sex Hormone Binding Globulin and Influence on Free Testosterone Levels

Contact Info

Product

Resources

About