Gracial ProdMonograph_cover - epgonline.org

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Pharmacokinetics Conclusion Gracial contains the progestogen desogestrel, which is rapidly absorbed and transformed following oral administration to its active metabolite, etonogestrel. Etonogestrel is 96–99% bound to plasma proteins, mainly albumin and SHBG and is eliminated from the body in urine and feces. Ethinylestradiol is 98.5% bound to plasma proteins, mainly albumin. 9
3. Pharmacodynamics •Etonogestrel has a high selectivity index • The 22-day regimen of Gracial permits a very low progestogen dose in the first seven days of the cycle, without compromising contraceptive reliability •Gracial inhibits follicle development and ovulation 3.1 Receptor affinity Different progestogens have different hormonal profiles: in addition to the progestogenic activity required for the inhibition of ovulation, progestogens may also possess some degree of androgenic activity. This is neither required nor desirable in OCs because of adverse effects such as androgenic skin disorders. Desogestrel is derived, like levonorgestrel, gestodene and norgestimate, from 19-nortestosterone. Desogestrel is, however, differentiated from levonorgestrel and other progestogens by a methylene group at position 11, which interferes with the binding of desogestrel to androgen receptors. CH 3 H 2 C 11 12 CH 2 13 17 OH C CH 2 1 9 10 8 14 15 16 3 5 4 6 7 Fig. 6: Structure of desogestrel 10
Page 1 and 2: ® indicates trademark(s) registere
Page 3 and 4: © 2000 N.V. Organon All rights res
Page 5 and 6: Contents Page 8. SUMMARY 42 9. REFE
Page 7 and 8: Introduction Since all the current
Page 9 and 10: Introduction 1.1 Rationale for Grac
Page 11 and 12: 2. Pharmacokinetics • After oral
Page 13: Pharmacokinetics ENG mainly bound t
Page 17 and 18: Pharmacodynamics 40 30 20 10 0 nore
Page 19 and 20: Pharmacodynamics mIU/ml 7 6 5 4 3 2
Page 21 and 22: 4. Contraceptive efficacy • The P
Page 23 and 24: Acceptability Effect of Gracial on
Page 25 and 26: Acceptability % of women 35 30 25 2
Page 27 and 28: 6. Gracial and mild to moderate acn
Page 29 and 30: Gracial and mild to moderate acne G
Page 31 and 32: Gracial and mild to moderate acne R
Page 33 and 34: Safety aspects Gracial not included
Page 35 and 36: Safety aspects The incidence of VTE
Page 37 and 38: Safety aspects Table 5: Relative ri
Page 39 and 40: Safety aspects Oral contraceptives
Page 41 and 42: Safety aspects Stroke With regard t
Page 43 and 44: Safety aspects Influence of adjustm
Page 45 and 46: Safety aspects On balance, this stu
Page 47 and 48: 8. Summary The most recent area of
Page 49 and 50: References Falsetti L. Acne treatme
Page 51 and 52: References Lunsen HW van. Recent or
Page 53 and 54: 10. Summary of product characterist
Page 55 and 56: Summary of product characteristics

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