TY - JOUR
T1 - Comparative pharmacokinetics and pharmacodynamics after subcutaneous and intramuscular administration of medroxyprogesterone acetate (25 mg) and estradiol cypionate (5 mg)
AU - Sierra-Ramírez, José Alfredo
AU - Lara-Ricalde, Roger
AU - Lujan, Miguel
AU - Velázquez-Ramírez, Norma
AU - Godínez-Victoria, Marycarmen
AU - Hernádez-Munguía, Ivonne Araceli
AU - Padilla, Agustin
AU - Garza-Flores, Josué
N1 - Funding Information:
The authors would like to thank nurses María Elena Guevara-Reyes and Isabel Muñoz-Lemus from the National Institute of Perinatology, México, for the efficient management of the subjects; Dr. Vicente Sanchez-Solis for carrying out the ultrasounds; Enrique Lopez for his contribution in the statistical analysis; Carlos Maria-Martinez for his valuable comments; Oscar Alberto Nolasco-Luna, Martha Irma Romero-Moreno and Martha Escudero for their contributions; and Importadora y Manufacturera Bruluart for financial support.
PY - 2011/12
Y1 - 2011/12
N2 - Background: The efficacy of contraceptives is affected by its route and ease of administration. Herein, both pharmacokinetics and pharmacodynamics of the once-a-month combined injectable contraceptive medroxyprogesterone acetate (MPA) plus estradiol cypionate (E 2-Cyp) were compared after intramuscular (IM) or subcutaneous (SC) injection in women of reproductive age. Study Design: Thirty women were randomly assigned to the SC (n=15) or IM (n=15) route of MPA 25 mg+E 2-Cyp 5 mg administration. Serum samples were obtained daily for 7 days and then three times a week for 40 days in order to quantify E 2, progesterone and MPA. In addition, three ultrasounds were performed on each subject to determine follicular development, and a daily record of the bleeding pattern and side effects was maintained. Results: A comparative analysis showed that the main pharmacokinetic (peak serum concentration, peak serum time, area under the serum concentration vs. time curve, absorption half-life and elimination half-life) and pharmacodynamic parameters, such as follicular development and ovulation, were similar in the SC vs. IM groups. Complete suppression in ovarian function was present in all women. The bleeding patterns and side effects were similar in both groups. Conclusions: The results presented herein demonstrate that the injection of 25 mg of MPA plus 5 mg of E 2-Cyp has similar efficacy and safety with either the SC or IM route of administration. The SC option can be considered a viable self-administered contraceptive option that might increase women's compliance to contraceptive use.
AB - Background: The efficacy of contraceptives is affected by its route and ease of administration. Herein, both pharmacokinetics and pharmacodynamics of the once-a-month combined injectable contraceptive medroxyprogesterone acetate (MPA) plus estradiol cypionate (E 2-Cyp) were compared after intramuscular (IM) or subcutaneous (SC) injection in women of reproductive age. Study Design: Thirty women were randomly assigned to the SC (n=15) or IM (n=15) route of MPA 25 mg+E 2-Cyp 5 mg administration. Serum samples were obtained daily for 7 days and then three times a week for 40 days in order to quantify E 2, progesterone and MPA. In addition, three ultrasounds were performed on each subject to determine follicular development, and a daily record of the bleeding pattern and side effects was maintained. Results: A comparative analysis showed that the main pharmacokinetic (peak serum concentration, peak serum time, area under the serum concentration vs. time curve, absorption half-life and elimination half-life) and pharmacodynamic parameters, such as follicular development and ovulation, were similar in the SC vs. IM groups. Complete suppression in ovarian function was present in all women. The bleeding patterns and side effects were similar in both groups. Conclusions: The results presented herein demonstrate that the injection of 25 mg of MPA plus 5 mg of E 2-Cyp has similar efficacy and safety with either the SC or IM route of administration. The SC option can be considered a viable self-administered contraceptive option that might increase women's compliance to contraceptive use.
KW - Estradiol Cypionate
KW - Intramuscular and subcutaneous
KW - Medroxyprogesterone acetate
KW - Pharmacodynamics
KW - Pharmacokinetics
UR - http://www.scopus.com/inward/record.url?scp=81155128598&partnerID=8YFLogxK
U2 - 10.1016/j.contraception.2011.03.014
DO - 10.1016/j.contraception.2011.03.014
M3 - Artículo
C2 - 22078184
SN - 0010-7824
VL - 84
SP - 565
EP - 570
JO - Contraception
JF - Contraception
IS - 6
ER -