Summary
The effects over 1 year of an oestrogendominant oral contraceptive containing ethinylestradiol and levonorgestrel on serum high-density lipoprotein cholesterol, apolipoproteins A-I and A-II and liver microsomal enzyme activity assessed by antipyrine kinetics, were investigated in 21 healthy, young women. HDL cholesterol and apolipoprotein concentrations rose and hepatic microsomal enzyme activity fell during the first month of the treatment, and remained affected throughout the year. After discontinuation of treatment, the lipid and apolipoprotein concentrations and the microsomal enzyme activity returned to their pretreatment levels within 1 month. The drug, by reducing hepatic enzyme activity, may have influenced both the antipyrine elimination rate and the high-density lipoprotein concentration.
Similar content being viewed by others
References
Vessey MP (1980) Female hormones and vascular disease; an epidemiologic overview. Br J Fam Plann 6 [Suppl]: 1–12
Slone D, Shapiro S, Kaufman DW, Rosenberg L, Miettinen OS, Stolley PD (1981) Risk of myocardial infarction in relation to current and discontinued use of oral contraceptives. N Engl J Med 305: 420–4
Wynn V, Doar JWH, Mills GL, Stokes T (1969) Fasting serum triglyceride, cholesterol, and lipoprotein levels during oral contraceptive therapy. Lancet 2: 756–60
Wynn V, Adams PW, Godsland et al. (1979) Comparison of effects of different combined oral contraceptive formulations on carbohydrate and lipid metabolism. Lancet 1: 1045–9
Bradley DD, Wingerd J, Petitti DB, Krauss RM, Ramcharan S (1978) Serum high-density lipoprotein cholesterol in women using oral contraceptives, oestrogens and progestins. N Engl J Med 299: 17–20
Tikkanen MJ, Nikkilä EA, Kuusi T, Sipinen S (1982) High-density lipoprotein-2 and hepatic lipase: Reciprocal changes produced by oestrogen and norgestrel. J Endocrinol Metab 54: 1113–7
Luoma PV, Sotaniemi EA, Pelkonen RO, Myllylä VV (1980) Plasma high-density lipoprotein cholesterol and hepatic cytochrome P-450 concentrations in epileptics undergoing anti-convulsant treatment. Scand J Clin Lab Invest 40: 163–7
Luoma PV, Sotaniemi EA, Pelkonen RO, Savolainen MJ, Ehnholm C (1982) Induction and lipoproteins. Lancet 1: 625
O'Malley K, Stevenson IH, Crooks J (1972) Impairment of human drug metabolism by oral contraceptive steroids. Clin Pharmacol Ther 13: 552–7
Sotaniemi EA, Hynynen T, Ahlquist J, Ahokas JT, Puoskari U (1978) Effects of medroxyprogesterone on the liver function and drug metabolism of patients with primary biliary cirrhosis and chronic active hepatitis. J Med 9: 137–48
Sotaniemi EA, Ahlquist J, Pelkonen RO, Pirttiaho H, Luoma PV (1977) Histological changes in the liver and the indices of drug metabolism in alcoholics. Eur J Clin Pharmacol 11: 295–303
Finley PR, Schifman RB, Williams RJ, Lichti DA (1978) Cholesterol in high-density lipoprotein: Use of Mg/dextran sulfate in its enzymic measurement. Clin Chem 24: 931–3
Huttunen JK, Länsimies E, Voutilainen E et al. (1979) Effect of moderate physical exercise on serum lipoproteins. Circulation 60: 1220–9
Brodie BB, Axelrod J (1950) The fate of antipyrine in man. J Pharmacol Exp Ther 98: 97–104
Vesell ES (1979) Commentary: The antipyrine test in clinical pharmacology: conceptions and misconceptions. Clin Pharmacol Ther 26: 275–86
Prescott LF, Adjepon-Yamoak KK, Roberts E (1973) Rapid gasliquid chromatographic estimation of antipyrine in plasma. J Pharm Pharmacol 25: 205–7
Wallenstein S, Zucker CL, Fleiss JL (1980) Some statistical methods useful in circulation research. Circ Res 47: 1–9
Tephley TR, Mannering GJ (1968) Inhibition of drug metabolism by steroids. Mol Pharmacol 4: 10–4
Nikkilä EA (1978) Metabolic regulation of plasma high-density lipoprotein concentrations. Eur J Clin Invest 8: 111–3
Hamilton RL, Williams MC, Fielding CJ, Havel RJ (1976) Discoidal bilayer structure of nascent high density lipoprotein from perfused rat liver. J Clin Invest 58: 667–80
Conney AH (1967) Pharmacological implications of enzyme induction. Pharmacol Rev 19: 317–66
Chao Y-S, Pickett CB, Yamin T-T, Guo LSS, Alberts AW, Kroon PA (1985) Phenobarbital induces rat liver apolipoprotein A-I mRNA. Mol Pharmacol 27: 394–8
Luoma PV, Myllylä VV, Hokkanen E (1982) Relationship between plasma HDL cholesterol and anticonvulsant levels in epileptics. J Cardiovasc Pharmacol 4: 1024–7
Kuusi T, Nikkilä EA, Virtanen I, Kinnunen PKJ (1979) Localization of the heparin-releasable lipase in situ in the rat liver. Biochem J 181: 245–6
Shepherd J, Packard CJ (1984) High-density lipoprotein apolipoprotein metabolism. In: Miller NE, Miller GJ (eds) Clinical and metabolic aspects of high-density lipoproteins. Amsterdam, Elsevier, pp 247–74
Naito HK (1985) The association of serum lipids, lipoproteins and apolipoproteins with coronary artery disease assessed by coronary arteriography. Ann NY Acad Sci 454: 230–8
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Luoma, P.V., Heikkinen, J.E., Ehnholm, C. et al. One year study of effects of an oestrogen-dominant oral contraceptive on serum high-density lipoprotein cholesterol, apolipoproteins A-I and A-II and hepatic microsomal function. Eur J Clin Pharmacol 31, 563–567 (1987). https://doi.org/10.1007/BF00606631
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00606631