Phase I prehysterectomy studies of the transcervical administration of quinacrine pellets.
To determine the safety of transcervical administration of quinacrine pellets as a method of voluntary female sterilization, three noncomparative Phase I clinical trials of the administration of 250 mg quinacrine were carried out in 21 women who were scheduled to undergo hysterectomy 24 h or one month later. Detailed results are presented for one of the trials using 10-min pellets. Six of 10 women had minor transitory complaints during the postinsertion 24-h follow-up period. Five women reported pelvic/abdominal cramping, one experienced headache, and one experienced dizziness. Blood chemistry values were not adversely influenced by the quinacrine. The average plasma level of quinacrine peaked at 3 h, 36.1 ng/ml, slightly lower than the value observed 4 h after oral administration of 200 mg in a previous study. An average of 27% of the administered dose was recovered in tampons. Quinacrine was detected in the plasma of two women at the four/six-week visit. Selected results are presented from two other trials that were halted because of slow recruitment. The transcervical administration of 250 mg of 10-min quinacrine pellets was well tolerated. However, based on recent mutagenicity testing and meetings with regulatory officials, it appears unlikely that the use of quinacrine for nonsurgical sterilization could be approved in the United States or Europe.
Laufe
L E
LE
University of Texas Health Science Center at San Antonio, USA.
Sokal
D C
DC
Cole
L P
LP
Shoupe
D
D
Schenken
R S
RS
D015746:Abdominal Pain / Q000139:chemically induced; D000282:Administration, Intravaginal; D000328:Adult; D015331:Cohort Studies; D004343:Drug Implants; D005260:Female; D006801:Humans; D007044:Hysterectomy; D011184:Postoperative Period; D011796:Quinacrine / Q000008:administration & dosage / Q000009:adverse effects / Q000032:analysis* / Q000493:pharmacokinetics*; D013630:Tampons, Surgical; D013997:Time Factors; D014592:Uterine Hemorrhage / Q000139:chemically induced; D014599:Uterus / Q000187:drug effects / Q000378:metabolism* / Q000503:physiopathology
D004343:Drug Implants; D011796:Quinacrine