Orally administered ketoconazole rapidly appears in seminal plasma and suppresses sperm motility

Vickery, B. H.; Burns, Jaime; Zaneveld, L. J. D.; Goodpasture, Jessie C.; Bergstrom, K.K.

doi:10.1007/bf01849310

Cited by 16 publications

(12 citation statements)

References 39 publications

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“…Little is known so far about the effect of ketoconazole on dog semen. Vickery, Burns, Zaneveld, Goodpasture, and Bergström (1985) showed that administration of ketoconazole was associated with a decline in motility of sperm. We showed for first time that prolonged treatment with ketoconazole led to azoospermia.…”

Section: Discussionmentioning

confidence: 99%

Clinical and spermatological findings in male dogs with acquired infertility: A retrospective analysis

Domosławska

Zduńczyk

2020

Andrologia

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A variety of causative factors of infertility in male dogs has been reported. In this study, the results of clinical examination and semen evaluation of 61 infertile stud dogs are described. Infertility was defined as conception failure of at least three matings with different bitches. The dogs, belonged to various breeds, were 4–8 years old and had a history of prior normal fertility. The dogs were subjected to clinical examination including ultrasonography of the prostate and testes. The semen was evaluated using CASA and microscopically morphology and live‐dead spermatozoa. In all dogs, the semen parameters were outside the reference range, and mostly oligoastheno‐teratozoospermia was found. There were also three cases of azoospermia. Thirty dogs showed no clinical abnormalities of the genital organ and no signs of systemic diseases, and testicular degeneration was assumed as the possible cause of infertility. In 20 dogs, BPH was diagnosed. In three dogs, infertility was associated with hypothyroidism. Three dogs had a history of babesiosis, and one dog prolonged ketoconazole treatment. One case each of chronic prostatitis, prostatic adenocarcinoma, epididymitis and retrograde ejaculation was diagnosed. The cause of acquired infertility could not be identified in almost half of the dogs. In other, infertility was often associated with prostate diseases.

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Section: Discussionmentioning

confidence: 99%

Clinical and spermatological findings in male dogs with acquired infertility: A retrospective analysis

Domosławska

Zduńczyk

2020

Andrologia

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“…Ketoconazole is an inhibitor of cellular division and has been shown to exert spermatostatic effects in several species including the dog, rabbit, monkey and man (Kutzler and Wood, 2006).Its oral administration to adult male dogs @ 50-246 mg/kg was associated with a decline in motility of sperm in ejaculates within 4 hours of dosing (Vickery et al, 1985b). However, Heckman et al(1992) in their study with mice and rats observed lack of correlation between steroid levels and sperm immobilization, along with rapid in vivo and in vitro effects on sperm motility and they concluded that ketoconazole is probably not a viable approach to the development of a male contraceptive.…”

Section: Ketoconazolementioning

confidence: 99%

Chemical Control of Fertility in Male Dogs: A Review

Soni¹,

Pandey²

2018

Int.J.Curr.Microbiol.App.Sci

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“…For example, ketoconazole (11), alpha-chlorohydrin (12) and emblein (13) have been tested in animals. However, the suppression of spermatogenesis was incomplete and systemic toxicity was limiting (14).…”

Section: Introductionmentioning

confidence: 99%

Melphalan, alone or conjugated to an FSH-β peptide, kills murine testicular cells in vitro and transiently suppresses murine spermatogenesis in vivo

Amory¹,

Hong²,

Yu³

et al. 2014

Theriogenology

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New approaches to sterilizing male animals are needed to control captive and wild animal populations. We sought to develop a non-surgical method of permanent sterilization for male animals by administering the gonadotoxicant melphalan conjugated to peptides derived from the β-chain of follicle stimulating hormone (FSHβ). We hypothesized that conjugating melphalan to FSHβ peptides would magnify the gonadotoxic effects of melphalan while minimizing systemic toxicity. The ability of conjugates of melphalan and FSHβ peptides to kill murine testicular cells was first tested in vitro in a three-dimensional testicular cell co-culture system. In this system, melphalan caused considerable cell death as measured both by increases in LDH concentrations in the culture supernatant and direct visualization of the cultures. Of the conjugates tested, melphalan conjugated to a 20 amino acid peptide derived from human FSHβ consisting of amino acids 33-53 (FSHβ (33-53)-melphalan) was very potent, with cell cytotoxicity and LDH release roughly one-half that of melphalan. The effects of melphalan and FSHβ (33-53)-melphalan on spermatogenesis were then tested in vivo in mature C56Bl/6 male mice. Four weeks after intraperitoneal injection, all mice treated with either FSHβ (33-53)-melphalan or melphalan had ~75% reductions in testicular spermatid counts compared with control animals. Testicular histology revealed significant reduction in mature spermatids and spermatocytes in most tubules. However, 12 weeks after the injection, testicular spermatid counts and histology were similar to controls, except in one animal receiving FSHβ (33-53)-melphalan that had no apparent spermatogenesis. We conclude that melphalan and FSHβ (33-53)-melphalan are potent gonadotoxicants in male mice resulting in marked suppression of spermatogenesis 4 weeks after a single intraperitoneal injection. However, this effect is transient in most mice as spermatogenesis is similar to control animals 12 weeks after drug administration. Melphalan or FSHβ (33-53)-melphalan may be useful for the temporary control of fertility in male animals, but additional research will be needed to develop a single dose method of permanent sterilization for male animals.

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Orally administered ketoconazole rapidly appears in seminal plasma and suppresses sperm motility

Cited by 16 publications

References 39 publications

Clinical and spermatological findings in male dogs with acquired infertility: A retrospective analysis

Clinical and spermatological findings in male dogs with acquired infertility: A retrospective analysis

Chemical Control of Fertility in Male Dogs: A Review

Melphalan, alone or conjugated to an FSH-β peptide, kills murine testicular cells in vitro and transiently suppresses murine spermatogenesis in vivo

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