Chemistry, pharmacology and clinical pharmacology of oral contraceptives.
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Sex hormone binding globulin (SHBG) has been measured using an improved ammonium-precipitation method. SHBG has been measured in normal male and female subjects, and in hirsute subjects on and off combined oral contraceptives (OCs). SHBG concentrations in hirsute subjects were significantly lower than those of normal female subjects (P0.001). During treatment with OCs, SHBG concentrations rose significantly (P0.001). Among hirsute patients, there was no significant (P0.5) difference between the pretreatment SHBG concentrations of 'responders' and those of 'nonresponders.' During treatment, SHBG concentrations increased in both groups.
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Endocrinological changes due to the effect of treatment with mono-, bi- and three-phase contraceptive pills taking continuously and occasionally are reviewed. It is established that oral contraceptives based on ovulation inhibition are safe. Less side effects are produced by Ovidon tablets. Continuin and Postinor pills are not safe, and they can produce irregular bleeding. Beside their numerous advances extrauterine pregnancy frequently happens (6.4%). A three-phase preparation is expected to have a reversible effect and lack of a consequent functional infertility. This is improved by hormone level measurements.
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Changes in the level of inhibitors of the coagulation system, primarily of thrombin neutralizing factors have been studied during the prolonged use of four products of contraceptive preparations containing various amounts of oestrogens and progestogens, two fixed dose pills (Bisecurin, Ovidon), a low dose combination pill (Rigevidon) and a biphasic preparation (Anteovin). Thrombelastographic values referred to hypercoagulability while the results of other examinations indicating activation of the coagulation system did not show definite changes in comparison with the control. The activity and quantity of antithrombin III decreased but never below 80%. Except Anteovin all contraceptives significantly enhanced alpha 1-antitrypsin while alpha 2-macroglobulin levels, remained nearly the same as the control values. Attention is called to that the increased alpha 1-antitrypsin level may be a biochemical risk factor. The results showed that the increased coagulability and disposition to thromboembolic disorders caused by hormonal contraceptives may be attributed not only to the decrease of thrombin inhibitors but also to increased alpha 1-antitrypsin levels which may cause increased inhibition of the fibrinolytic system.
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We studied the effects of oral contraceptive pills (OCP) supplied by the Govt of India in its Family Welfare Campaign, on serum lipid levels of women. The OCP, containing 30 micrograms ethinyl estradiol and 1 mg of norethisterone acetate were administered to the women for six months continuously and serum lipid levels were estimated after three and six months of the treatment. There were no significant changes in serum cholesterol, high density lipoprotein (HDL), low density lipoprotein (LDL), serum triglycerides and very low density lipoprotein (VLDL). In a simultaneous study we also measured serum lipid levels at 3 and 6 months after withdrawal of the pills in women who had been receiving OCP containing 50 micrograms of ethinyl estradiol and 0.5 mg of one of the progesterones for the past 1 1/2 to 2 years continuously. Only serum LDL level fell significantly (P less than 0.01) on 3 months withdrawal period. It is concluded that 6 months of usage of the OCP marketed by the Govt. of India does not affect the serum lipid profile.
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