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  • Title: Pharmacokinetics of medroxyprogesterone acetate after single and multiple injection of Cyclofem in Chinese women.
    Author: Zhou XF, Shao QX, Han XJ, Weng LJ, Sang GW.
    Journal: Contraception; 1998 Jun; 57(6):405-11. PubMed ID: 9693401.
    Abstract:
    To provide pharmacokinetic data for safety evaluation on prolonged treatment with Cyclofem, which contains 25 mg medroxyprogesterone acetate (MPA) and 5 mg estradiol cypionate in 0.5 mL microcrystalline aqueous suspension, the pharmacokinetic profiles of MPA after single and multiple administration of this monthly injectable contraceptive were investigated in Chinese women. Nine healthy fertile women received Cyclofem based on a once-a-month regiment for up to 1 year. Blood samples were collected immediately prior to drug administration and on days 1, 3, 5, 7, 14, 21, and 28 after injection. After the 1st, 6th, and 12th injection, the maximum serum concentrations (Cmax) of MPA were observed on days 3.4 +/- 0.9, 4.3 +/- 2.2, and 3.7 +/- 2.6, respectively. Cmax of serum MPA during the 1st, 6th, and 12th treatment cycles were 3.75 +/- 1.27, 5.54 +/- 1.79, and 5.55 +/- 1.80 nmol/L, whereas the areas under the curve (AUC0-28 days) were 55.84 +/- 28.15, 95.45 +/- 26.56, and 98.81 +/- 21.84 nmol/L.day, respectively. There was significant interindividual variation in the pharmacokinetics of MPA after intramuscular injection of Cyclofem. No significant change was demonstrated in mean residence time (MRT) of MPA after single and multiple injection. There was a tendency of increase in Cmax and AUC0-28 days of MPA during the first 6 months of treatment, whereas no further enhancement was found between the 6th and 12th injection (p > 0.05). Peak levels of estradiol (E2) observed in Cyclofem users were within the normal range of the preovulatory phase. Results of this long-term study suggest that no drug accumulation occurred after repeated administration of Cyclofem in the Chinese women. To provide pharmacokinetic data for a safety evaluation of long-term use of the monthly injectable Cyclofem (25 mg of medroxyprogesterone acetate (MPA) and 5 mg of estradiol cypionate), 9 fertile Chinese women 27-34 years of age were enrolled in a 12-month clinical study. Serum samples were collected immediately prior to drug administration and on days 1, 3, 5, 7, 14, 21, and 28 after monthly injection. After injections 1, 6, and 12, maximum serum MPA concentrations were observed on days 3.4 +or- 0.9, 4.3 +or- 2.2, and 3.7 +or- 2.6, respectively. Maximum concentrations of serum MPA during treatment cycles 1, 6, and 12 were 3.75 +or- 1.27, 5.54 +or- 1.79, and 5.55 +or- 1.80 nmol/l, respectively, while the corresponding areas under the curve were 55.84 +or- 28.15, 95.45 +or- 26.56, and 98.81 +or- 21.84 nmol/l per day. There was significant interindividual variation in the pharmacokinetics of MPA after intramuscular injection. No significant change was recorded in mean MPA residence time after single and multiple injection. Noted was a trend of increases in MPA maximum serum concentration and areas under the curve during the first 6 months of treatment, followed by no further enhancement in the last 6 months. Peak estradiol levels were within the normal range of the preovulatory phase. These findings suggest that long-term Cyclofem use is not associated with drug accumulation. As a safe, highly effective formulation, Cyclofem offers women around the world yet another contraceptive choice.
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