Safety and toxicity of nonoxynol-9 gel as a rectal microbicide

Sex Transm Dis. 1999 Nov;26(10):564-71. doi: 10.1097/00007435-199911000-00005.

Abstract

Background and objectives: Methods of HIV and STD prevention, which can be controlled by the receptive partner, are a high priority for research and development. Studies on the safety of Nonoxynol-9 (N-9) on the vaginal mucosa have yielded conflicting results. No Phase I study has evaluated the effect of N-9 on the rectal mucosa.

Goals: To assess the safety of 52.5 mg of N-9 in a 1.5-g gel when applied one to four applicators per day to the rectum and penis.

Study design: The study included 25 HIV-negative and 10 HIV-positive, monogamous gay male couples in which each partner was exclusively insertive or receptive while using N-9 gel. Each participant served as his own control during placebo gel use compared to during N-9 gel use. Receptive partners underwent anoscopic examination after 1 week of placebo use and after 2, 5, and 6 weeks of N-9 gel use, with rectal biopsies obtained after 1 week of placebo use and after 5 and 6 weeks of N-9 gel use. Insertive partners had safety monitoring after 1 week of placebo use and after 2, 5, and 6 weeks of N-9.

Results: No rectal ulcers were detected; superficial rectal erosions were noted in two HIV-negative participants. Abnormal or slightly abnormal histologic abnormalities of rectal biopsies were detected in 31 (89%) receptive participants after N-9 gel use compared to 24 (69%) participants after 1 week of placebo gel use. Meatal ulceration, not caused by herpes simplex virus, was detected in one HIV-negative participant.

Conclusion: Low-dose N-9 gel was not associated with macroscopic rectal and penile epithelial disruption or inflammation, but histologic abnormalities were commonly observed during N-9 gel as well as during placebo gel use.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Anti-Infective Agents / adverse effects
  • Anti-Infective Agents / pharmacology*
  • Epithelium / drug effects
  • HIV Infections / prevention & control*
  • Homosexuality, Male
  • Humans
  • Intestinal Mucosa / drug effects
  • Male
  • Middle Aged
  • Nonoxynol / adverse effects
  • Nonoxynol / pharmacology*
  • Penis / cytology
  • Penis / drug effects*
  • Rectum / drug effects*
  • Sexually Transmitted Diseases / prevention & control*

Substances

  • Anti-Infective Agents
  • Nonoxynol