Long-acting contraceptive agents: design of the WHO Chemical Synthesis Programme

Steroids. 1983 Mar;41(3):243-53. doi: 10.1016/0039-128x(83)90095-8.

Abstract

The great demand for improved long-acting injectable steroid contraceptives, particularly in developing countries, and the relative lack of interest from the pharmaceutical industry to develop such products stimulated WHO to launch a synthetic and screening programme to find improved, safe and acceptable injectable preparations. More than 210 esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) and levonorgestrel (D-(-)-13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) have been prepared in university-based research laboratories situated mainly in developing countries, and then screened by NICHHD in animal models. The following three compounds, levonorgestrel butanoate, cyclopropylcarboxylate and cyclobutylcarboxylate, proved to be particularly long-acting when administered as microcrystalline suspensions. The overall strategy of this research and development programme is described.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Contraceptives, Oral / administration & dosage
  • Contraceptives, Oral / chemical synthesis*
  • Contraceptives, Oral, Combined / chemical synthesis
  • Delayed-Action Preparations
  • Female
  • Humans
  • Injections
  • Solutions
  • Suspensions
  • World Health Organization

Substances

  • Contraceptives, Oral
  • Contraceptives, Oral, Combined
  • Delayed-Action Preparations
  • Solutions
  • Suspensions