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Long-Acting Contraceptive Delivery Systems: Clinical Studies 39 CONTENTS ACCEPTABILITY OF LONG-ACTING CONTRACEPTION 1. Need for and Acceptability of Long-Acting Steroidal Contraception 1 Rochelle N. Shain, Malcolm Potts 2. Discussion: Acceptability of Long-Acting Contraception 20 Moderator: John J. Sciarra POLYMERIC DELIVERY SYSTEMS FOR CONTRACEPTION 3. Polymers and Drug Delivery Systems 23 Robert S. Langer 4. Novel Delivery Approaches for Enhancement of Therapeutic Activity of Steroids 33 Anwar A. Hussain 5. Capronor—A Biodegradable Delivery System for Levonorgestrel 48 Colin G. Pitt, Anton Schindler 6. Microencapsulation of Contraceptive Steroids 64 Elie S. Nuwayser, David L. Williams, James H. Kerrigan, William A. Nucefora, James C. Armstrong 7. Polymeric Considerations in the Design of Microencapsulation of Contraceptive Steroids 77 Danny H. Lewis, Thomas R. Tice 8. Development of Microencapsulated Norgestimate as a Long-Acting Contraceptive 96 Do Won Hahn, John L. McGuire, Robert M. Cohn, Lee R. Beck, Thomas R. Tice, Danny H. Lewis 9. Controlled Release of Contraceptive Agents from Poly(ortho esters) 113 Jorge Heller, Donald W. H. Penhale, Bruce K. Fritzinger, Steve Y. Ng http://d-nb.info/1012327442 x I Contents 10. Discussion: Polymeric Delivery Systems for Contraception 129 Moderator: Henry L. Gabelnick INJECT ABLE/IMPLANT ABLE LONG- ACTING CONTRACEPTIVE DELIVERY SYSTEMS 11. Implantable Levonorgestrel Rod Systems: In Vivo Release Rates and Clinical Effects 133 Dale N. Robertson 12. Biodegradable and Nonbiodegradable Fibrous Delivery Systems 145 Donald R. Cowsar, Richard L. Dunn 13. Preparation of Biodegradable Levonorgestrel Rods 164 Judith P. Kitchell, Stephen C. Crooker, Donald L. Wise, Lour ens J. D. Zaneveld 14. Microencapsulation of the Peptide Nafarelin Acetate for Controlled Release 169 John S. Kent, Lynda M. Sanders, Thomas R. Tice, Danny H. Lewis 15. In Vivo Assessment of Long-Acting Formulations of Luteinizing Hormone- Releasing Hormone Analogs 180 Brian H. Vickery, Georgia I. McRae, Lynda M. Sanders, John S. Kent, John J. Nestor, Jr 16. Development of Certain Levonorgestrel Esters as Long-Acting Injectable Contraceptives 190 Peter E. Hall, Gabriel Bialy, R. P. Blye, Pierre Crabbe 17. Discussion: Injectable/Implantable Long- Acting Contraceptive Delivery Systems 199 Moderator: Peter E. Hall Contents / xi LONG-ACTING VAGINAL CONTRACEPTIVE DELIVERY SYSTEMS 18. Vaginal Ring Steroid-Releasing Systems 201 Theodore M. Jackanicz 19. Some Pharmacokinetic and Pharmacodynamic Properties of Vaginal Delivery Systems That Release Small Amounts of Progestogens at a Near Zero- Order Rate 213 Egon Diczfalusy, Britt-Marie Landgren 20. Delivery of a New Vaginal Contraceptive 228 Brian H. Vickery, Jessie C. Goodpasture, Lih-Yang Wang Lin 21. Vaginal Absorption of Contraceptive Steroids 241 Arne Victor 22. Discussion: Long-Acting Vaginal Contraceptive Delivery Systems 246 Moderator: Elof D. B. Johansson 23. Tissue Response to Drug Delivery Systems: The Cage Implant System 248 James M. Anderson, Roger Marchant, Michael McClurken 24. External Scintigraphy in the Study of Long- Acting Contraceptive Delivery Systems 256 George A. Digenis, Michael Jay, Robert M. Beihn, Thomas R. Tice, Lee R. Beck 25. Effects of Progestogens on Cervical Secretion and Sperm—Cervical Mucus Interaction 265 Kamran S. Moghissi 26. Sex Steroids and Plasma Lipoprotein Metabolism With Special Reference to High- Density Lipoproteins 278 Bengt G. Johansson xii I Contents 27. Discussion: Metabolic Changes 287 Moderator: Egon Diczfalusy ENDOMETRIAL RESPONSE TO STEROIDS 28. Histopathology of the Endometrium During Continuous Use of Levonorgestrel 290 Hector D. Croxatto, Soledad Diaz, Margarita Pavez, Horacio B. Croxatto 29. Comparative Effects of Norgestimate, Norethisterone, and Medroxyprogesterone Acetate on the Microanatomy of Baboon Endometrium 296 Walter H. Wilborn, Barbara M. Hyde, Valerie Z. Pope, Lee R. Beck, Do Won Hahn, John McGuire, Robert Cohn 30. Endometrial Effects of Progestogens: Their Elusive Relationship to Ovarian Function and Intermenstrual Bleeding 316 Egon Diczfalusy, Elisabeth Johannisson 31. Discussion: Endometrial Response to Steroids 332 Moderator: Charles E. Flowers, Jr. FETAL AND CHILD DEVELOPMENT ISSUES 32. Mutagenicity and Teratogenicity of Inject able and Implantable Progestins: Probable Lack of Effect 334 Joe Leigh Simpson 33. Transfer of Contraceptive Steroids From Human Breast Milk to Infants; Effect of Steroids on Luteinizing Hormone and Testosterone Levels and Possible Biologic Activity 362 Villi S. Toddywalla, S. S. Betrabet, Badri N. Saxena Contents / xiii 34. Contraception With a Levonorgestrel- Releasing IUD: Effect on Lactation and Child Development 368 Matti Heikkild, Maija Haukkamaa, Tapani Luukkainen 35. Long-Term Study of Growth and Development of Children Breast-Fed by Mothers Receiving Depo-Provera (Medroxyprogesterone Acetate) During Lactation 378 Suporn Koetsawang, Vanpen Boonyaprakob, Sukanda Suvanichati, Sasithorn Paipeekul 36. Effect of DMPA on Lactation 388 Fouad Hefnawi, S. A. M. Hassanyn, M. M. Abdel-Kader, Abraham Risk, E. Hegazi 37. Effects of NORPLANT® Subdermal Implants on Lactation and Infant Growth 397 Soledad Diaz, Carmen Herreros, Gabriela Juez, Maria-Eugenia Casado, Ana-Maria Salvatierra, Patricia Miranda, Octavio Peralta, Horacio B. Croxatto 38. Discussion: Fetal and Child Development Issues 404 Moderator: Miriam H. Labbok LONG-ACTING CONTRACEPTIVE DELIVERY SYSTEMS: CLINICAL STUDIES 39. Poly ( d,l-lactide-co-glycolide ) /Norethisterone Microcapsules: Clinical Study 407 Lee R. Beck, Charles E. Flowers, Jr., Valerie Z. Pope, Thomas R. Tice, Richard L. Dunn, Richard M. Gilley 40. Norethisterone Microspheres 6-Month System: Clinical Results 418 Roberto Rivera, Consuelo Flores, Silvia Aldaba, Ana Hernandez xiv / Contents 41. Preparation, Properties, and Release Rate of Norethindrone (NET) From Subcutaneous Implants 425 Gopi N. Gupta, Brij B. Saxena, Robert Landesman, William J. Ledger 42. Clinical Evaluation of Subcutaneous Norethindrone (NET) Implants: Phase I Multicenter Clinical Studies 431 Ricardo H. Asch, Brij B. Saxena, Gopi N. Gupta, Jose P. Balmaceda, Roberto Rivera, Horacio B. Croxatto, Elsimar M. Coutinho, Robert Landesman 43. ST-1435: Development of an Implant 441 Viveca Odlind, Hans Lithell, Henri Kurunmdki, Pertti Ldhteenmdki, Juhani Toivonen, Tapani Luukkainen, ElofD. B. Johansson 44. Contraception With Single Implants and Mini-Implants of ST-1435 450 Elsimar M. Coutinho, A. R. da Silva, C. Carreira, lone Barbosa, V. Dourado-Silva, Irving Sivin 45. Discussion: Long-Acting Contraceptive Delivery Systems: Clinical Studies 456 Moderator: Alfredo Goldsmith LONG-ACTING CONTRACEPTIVE DELIVERY SYSTEMS: NORPLANT® 46. NORPLANT® Clinical Study in Thailand 459 Suporn Koetsawang, Somsak Varakamin, Suwanee Satayapan, Nikorn Dusitsin 47. NORPLANT® Clinical Studies—Egypt 471 Fouad Hefnawi, Mokhtar Toppozada, Mohamed Rizk, Mamdouh Shaaban, A. M. El Said, Ahmed F. M. Mustafa 48. Performance of NORPLANT® Subdermal Implants in Clinical Studies in Chile 482 Soledad Diaz, Margarita Pavez, Patricia Miranda, Irving Sivin, Horacio B. Croxatto Contents / xv 49. Findings in Phase III Studies of NORPLANT® Implants 488 Irving Sivin 50. Discussion: Long-Acting Contraceptive Delivery Systems—NORPLANT® 501 Moderator: James D. Shelton OTHER LONG-ACTING CONTRACEPTIVE SYSTEMS 51. Norethisterone (Norethindrone) Enanthate Clinical Studies 502 Mokhtar Toppozada 52. Clinical Trial of the Monthly Injectable Contraceptives Cycloprovera and HRP 102 515 Peter E. Hall 53. Cycloprovera 523 Giuseppe Benagiano, Francesco Maria Primiero 54. Monthly Injectables: NET and Estradiol Valerate/Cypionate 537 Indian Council of Medical Research Task Force on Hormonal Contraception: Badri N. Saxena (Presenter), Raj Baweja, Usha Krishna, Shyamli Data Chaudhury, Saroj K. Bhattacharya, Florence S. Philips, May Manual 55. Subdermal Progesterone Implants for Fertility Regulation in Nursing Women 543 Horacio B. Croxatto, Soledad Diaz, Octavio Peralta, Gabriela Juez, Carmen Herreros, Maria-Eugenia Casado, Ana-Maria Salvatierra, Patricia Miranda 56. Anordrin: Biologic Studies and Potential as a Long-Acting Contraceptive 550 Robert T. Chatterton, Jr., Rajeshwari R. Mehta, John M. Jenco, Liliana V. Gaynor, Duane L. Venton 57. Discussion: Other Long-Acting Contraceptive Delivery Systems 564 Moderator: Roberto Rivera xvi / Contents LONG-ACTING CONTRACEPTIVE DELIVERY SYSTEMS: ADDITIONAL CLINICAL STUDIES 58. Depot Medroxyprogesterone Acetate Update 566 Paul C. Schwallie 59. Vaginal Ring Clinical Studies: Update 581 Subir Roy, Daniel R. Mishell, Jr. 60. Development of Intracervical Steroid- Releasing System 595 Pekka Ld'hteenmdki, Henri Kurunmdki, Tapani Luukkainen, Pertti Ld'hteenmdki, Kari Ratsula, Juhani Toivonen 61. Intrauterine Release of Levonorgestrel 601 Tapani Luukkainen, Carl Gustaf Nilsson, Hannu Allonen, Maija Haukkamaa, Juhani Toivonen 62. Development of the Intrauterine Progesterone-Releasing System 613 Ramon Aznar, Juan Giner 63. Long-Acting Progestasert IUD Systems 621 David A. Edelman, Lynda Painter Cole, Ruben Apelo, Pablo Lavin 64. Discussion: Long-Acting Contraceptive Delivery Systems: Additional Clinical Studies 628 Moderator: Gerald I. Zatuchni Contributing Authors 631 Workshop Participants 641 Index 647.
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