The spermicidal and antitrichomonas activities of SSRI antidepressants.
The study investigated spermicidal and antitrichomonas activities of selective serotonin reuptake inhibitor (SSRI) antidepressants with a view to generate new lead for development of dual-function spermicidal microbicides, which is an urgent global need. Fluoxetine, Sertraline, and Fluvoxamine exhibited both spermicidal and anti-STI (antitrichomonas) activities in vitro, whereas Paroxetine and Citalopram showed only the spermicidal activity. Fluoxetine exhibited better activity profile than the other antidepressant drugs with its spermicidal and antitrichomonas activities being comparable to that of the OTC contraceptive Nonoxynol-9. The non-detergent nature of Fluoxetine and a much lower spermicidal ED50 value (than N-9) may add considerably to its merit as a candidate for microbicidal contraceptive. Thus, the antidepressants exhibiting both spermicidal and antitrichomonas activities might provide useful lead for the development of novel, dual-function spermicidal contraceptives.
Kumar
V S Kiran
VS
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow-226001, India.
Sharma
Vishnu Lal
VL
Tiwari
Pratibha
P
Singh
Divya
D
Maikhuri
Jagdamba Prasad
JP
Gupta
Gopal
G
Singh
Man Mohan
MM
D000818:Animals; D000928:Antidepressive Agents / Q000737:chemistry / Q000494:pharmacology*; D000994:Antitrichomonal Agents / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D005473:Fluoxetine / Q000737:chemistry / Q000494:pharmacology; D016666:Fluvoxamine / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D015394:Molecular Structure; D017367:Selective Serotonin Reuptake Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D020280:Sertraline / Q000737:chemistry / Q000494:pharmacology; D013089:Spermatocidal Agents / Q000737:chemistry / Q000494:pharmacology*; D013094:Spermatozoa / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects*
D000928:Antidepressive Agents; D000994:Antitrichomonal Agents; D005473:Fluoxetine; D016666:Fluvoxamine; D017367:Selective Serotonin Reuptake Inhibitors; D020280:Sertraline; D013089:Spermatocidal Agents