Pharmacokinetic study to compare the absorption and tolerability of two doses of levonorgestrel following single vaginal administration of levonorgestrel in Carraguard® gel: a new formulation for "dual protection" contraception

Contraception

Volumn 75, Issue 6, 2007, Pages 454-460

  Sitruk Ware, Regine ^a   Brache, Vivian ^b   Maguire, Robin ^a   Croxatto, Horacio ^c   Kumar, Narender ^a   Kumar, Sushma ^a   Montero, Juan Carlos ^c   Salvatierra, Ana Maria ^c   Phillips, David ^a   Faundes, Anibal ^b  

^a POPULATION COUNCIL   (United States)

^b PROFAMILIA   (Dominican Republic)

^c Instituto Chileno de Medicina Reproductiva   (Chile)

Author keywords

Emergency contraception; Levonorgestrel; Microbicides; SHBG; Vaginal administration

Indexed keywords

CARRAGEENAN; ESTRADIOL; LEVONORGESTREL; LUTEINIZING HORMONE; PROGESTERONE; SEX HORMONE BINDING GLOBULIN;

ADULT; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG FORMULATION; DRUG MEGADOSE; DRUG TOLERABILITY; FEMALE; GEL; HORMONE BLOOD LEVEL; HUMAN; LOW DRUG DOSE; MAXIMUM ALLOWABLE CONCENTRATION; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL; SEXUALLY TRANSMITTED DISEASE; SINGLE DRUG DOSE; VAGINA CONTRACEPTION;

ADMINISTRATION, INTRAVAGINAL; ANTI-INFECTIVE AGENTS; AREA UNDER CURVE; CHEMISTRY, PHARMACEUTICAL; CHILE; CONTRACEPTIVES, POSTCOITAL, SYNTHETIC; DOMINICAN REPUBLIC; DOUBLE-BLIND METHOD; FEMALE; HUMANS; INTESTINAL ABSORPTION; LEVONORGESTREL; VAGINAL CREAMS, FOAMS, AND JELLIES;

EID: 34248548508     PISSN: 00107824     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.contraception.2007.02.003     Document Type: Article

References (44)

1. Baba M., Nakajima M., Schols D., Pauwels R., Balzarini J., and De Clercq E. Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro. Antiviral Res 9 (1988) 335-343
2. Pearce-Pratt R., and Phillips D.M. Sulfated polysaccharides inhibit lymphocyte-to-epithelial transmission of HIV-1. Biol Reprod 54 (1996) 173-182
3. Zacharopoulos V.R., and Phillips D.M. Vaginal formulations of carrageenan protect mice from herpes simplex virus infection. Clin Diagn Lab Immunol 4 (1997) 465-468
4. Jerse A.E. Experimental gonococcal genital tract infection and opacity protein expression in estradiol-treated mice. Infect Immun 67 (1999) 5699-5708
5. Maguire R., Bergman N., and Phillips D.M. Comparison of microbicides for efficacy in protecting mice against vaginal challenge with herpes simplex virus type 2, cytoxicity, antibacterial properties, and sperm immobilization. Sex Transm Dis 28 (2001) 259-265
6. Elias C.J., Coggins C., Alvarez F., et al. Colposcopic evaluation of a vaginal gel formulation of iota-carrageenan. Contraception 56 (1997) 387-389
7. Coggins C., Blanchard K., Alvarez F., et al. Preliminary safety and acceptability of a carrageenan gel for possible use as a vaginal microbicide. Sex Transm Inf 76 (2000) 480-483
8. Mishell D.J., Lumkin M., and Jackanicz T. Initial clinical studies of intravaginal rings containing norethindrone and norgestrel. Contraception 12 (1975) 253-260
9. Victor A., and Johansson E. Plasma levels of d-norgestrel and ovarian function in women using intravaginal rings impregnated with d-norgestrel for several cycles. Contraception 14 (1976) 215-226
10. Sivin I., Mishell D.R., Victor A., et al. A multicenter study of levonorgestrel-estradiol contraceptive vaginal rings. I - Use effectiveness. An international comparative trial. Contraception 24 (1981) 341-358
11. Landgren B.M., Aedo A.R., Johannisson E., and Cekan S.Z. Pharmacokinetic and pharmacodynamic effects of vaginal rings releasing levonorgestrel at a rate of 27 micrograms/24 hs: a pilot study. Contraception 49 (1994) 139-150
12. World Health Organization. Microdose intravaginal levonorgestrel contraception: a multicenter clinical trial: I. Contraceptive efficacy and side effects. Contraception 41 (1990) 105-124
13. Alvarez-Sanchez F., Brache V., Jackanicz T., and Faundes A. Evaluation of four different contraceptive vaginal rings: steroid serum levels, luteal activity, bleeding control and lipid profiles. Contraception 46 (1992) 387-397
14. Ballagh S., Mishell D.R., Jackanicz T., Lacarra M., and Eggena P. Dose-finding study of a contraceptive ring releasing norethindrone acetate/ethinyl estradiol. Contraception 50 (1994) 535-549
15. Stanczyk F.Z., Hiroi M., Goebelsmann U., Brenner P.F., Lumkin M.E., and Mishell D.R. Radioimmunoassay of serum d-norgestrel in women following oral and intravaginal administration. Contraception 12 (1975) 279-298
16. Brache V., Blumenthal P., Alvarez F., Dunson T., Cochon L., and Faundes A. Timing of onset of contraceptive effectiveness in Norplant implant users: II. Effect on the ovarian function in the first cycle of use. Contraception 59 (1999) 245-251
17. Von Hertzen H., Piaggio G., Ding J., et al. World Health Organization. Low dose mifepristone and two regimens of levonorgestrel for emergency contraception: a WHO multicentre randomised trial. Lancet 360 (2002) 1803-1810
18. World Health Organization and CONRAD. Manual for the standardization for the evaluation of vaginal products (2004), WHO and CONRAD, Geneva and Arlington (WHO/RHR/04.02 and CONRAD/2004.1)
19. Jick H., Hannan M.T., Stergachis A., Heidrich F., Perera D.R., and Rothman K.J. Vaginal spermicides and gonorrhea. JAMA 248 (1982) 1619-1621
20. Hicks D.R., Martin L.S., Getchell J.P., et al. Inactivation of HTLV III/LAV infected cultures of normal human lymphocytes by nonoxynol-9 in vitro. Lancet 2 (1985) 1422-1423
21. Louv W.C., Austin H., Alexander W.J., Stagno S., and Cheeks J. A clinical trial of nonoxynol-9 for preventing gonococcal and chlamydial infections. J Infect Dis 158 (1988) 518-523
22. Mauck C.K., Baker J.M., Barr S.P., Abercrombie T.J., and Archer D.F. A phase I comparative study of contraceptive vaginal films containing benzalkonium chloride and nonoxynol-9. Postcoital testing and colposcopy. Contraception 56 (1997) 89-96
23. Roddy R.E., Zekeng L., Ryan K.A., Tamoufe U., Weir S.S., and Wong E.L. A controlled trial of nonoxynol-9 film to reduce male to female transmission of sexual transmitted disease. N Engl J Med 339 (1998) 504-510
24. Bourinbaiar A.S., and Lee-Huang S. Comparative in vitro study of contraceptive agents with anti-HIV activity: gramicidin, nonoxynol-9, gossypol. Contraception 49 (1994) 131-137
25. Van Damme L., Ramjee G., Alary M., et al. Effectiveness of COL-1492, a nonoxynol-9 vaginal gel, on HIV-1 transmission in female sex workers: a randomized controlled trial. Lancet 360 (2002) 971-977
26. D'Cruz O.J., and Uckun F.M. Clinical development of microbicides for the prevention of HIV infection. Curr Pharm Des 10 (2004) 315-336
27. Smita J., Soma D., Beverly B., et al. Phase I safety study of 0.5% PRO 2000 vaginal gel among HIV un-infected women in Pune, India. AIDS Res Ther 3 (2006) 4
28. Van Damme L., Wright A., Depraetere K., et al. A phase I study of a novel potential intravaginal microbicide, PRO 2000, in healthy sexually inactive women. Sex Transm Infect 76 (2000) 126-130
29. Van De Wijgert J., Fullem A., Kelly C., et al. Phase 1 trial of the topical microbicide BufferGel: safety results from four international sites. J Acquir Immune Defic Syndr 26 (2001) 21-27
30. Malonza I.M., Mirembe F., Nakabiito C., et al. Expanded Phase I safety and acceptability study of 6% cellulose sulfate vaginal gel. AIDS 19 (2005) 2157-2163
31. Johansson E., Brache V., Alvarez F., et al. Pharmacokinetic study of different dosing regimens of levonorgestrel for emergency contraception in healthy women. Hum Reprod 17 (2002) 1472-1476
32. Tremblay D., Gainer E., and Ulmann A. The pharmacokinetics of 750 μg levonorgestrel after administration of one single dose or two doses at 12- or 24-h interval. Contraception 64 (2002) 327-331
33. Kook K., Gabelnick H., and Duncan G. Pharmacokinetics of levonorgestrel 0.75 mg tablets. Contraception 66 (2002) 73-76
34. Kives S., Hahn P., White E., Stanczyk F.Z., and Reid R. Bioavailability of the Yuzpe and levonorgestrel regimens of emergency contraception: vaginal vs. oral administration. Contraception 71 (2005) 197-201
35. Devoto L., Fuentes A., Palomino A., et al. Pharmacokinetics and endometrial tissue levels of levonorgestrel after administration of a single 1.5-mg dose by the oral and vaginal route. Fertil Steril 84 (2005) 46-51
36. Alvarez F., Faundes A., Johansson E., and Coutinho E. Blood levels of levonorgestrel in women following vaginal placement of contraceptive pills. Fertil Steril 40 (1983) 120-123
37. Timmer C.J., and Mulders T.M. Pharmacokinetics of etonogestrel and ethinylestradiol released from a combined contraceptive vaginal ring. Clin Pharmacokinet 39 (2000) 233-242
38. Alexander N.J., Baker E., Kaptein M., Karck U., Miller L., and Zampaglione E. Why consider vaginal drug administration?. Fertil Steril 82 (2004) 1-12
39. Croxatto H.B., Brache V., Pavez M., et al. Pituitary-ovarian function following the standard levonorgestrel emergency contraceptive dose or a single 0.75 mg dose given on the days preceding ovulation. Contraception 70 (2004) 442-450
40. Kesseru E., Lanrranaga A., and Parada J. Postcoital contraception with d-norgestrel. Contraception 7 (1973) 367-379
41. Kesseru E., Garmedndia F., Westphal N., and Parada J. The hormonal and peripheral effects of d-norgestrel in postcoital contraception. Contraception 10 (1974) 411-423
42. Brache V., Faundes A., Johansson E., and Alvarez F. Anovulation, inadequate luteal phase and poor sperm penetration in cervical mucus during prolonged use of Norplant implants. Contraception 31 (1985) 261-273
43. Croxatto H.B., Diaz S., Salvatierra A.M., Morales P., Ebensperger C., and Brandeis A. Treatment with Norplant subdermal implants inhibits sperm penetration through cervical mucus in vitro. Contraception 36 (1987) 193-201
44. Dunson T.R., Blumenthal P.D., Alvarez F., et al. Timing of onset of contraceptive effectiveness in Norplant implant users: Part I. Changes in cervical mucus. Fertil Steril 69 (1998) 258-266