Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Gulati, Abhishek; Tiwary, Ashok K.; Jain, Subheet Kumar; Moudgil, Pranab; Gupta, Anshu

doi:10.1211/jpp.58.8.0017

Cited by 5 publications

(5 citation statements)

References 17 publications

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“…Therefore, the spermicidal action of these drugs could be ascribed to elevation of Ca 2+ is to a threshold level of 1100-1200 nm. This finding was in agreement with earlier reports on ejaculated human sperm (White et al 1995;Lee et al 1996;Patni et al 2001;Reddy et al 2001;Gupta et al 2003Gupta et al , 2004Gulati et al 2006).…”

Section: Effect Of Gbe Gle or Rge On Ca 2+supporting

confidence: 94%

“…is DBZ (2 mm) and MZE (0.01 mm) are reported to produce complete loss of sperm motility, accompanied by an increase in Ca 2+ is in ejaculated human sperm cells in 60 min (Patni et al 2001;Gulati et al 2006). These concentrations of DBZ and MZE were deliberately chosen so that the effect of their combination with other drugs on motility and Ca 2+ i could easily be discernible from their effect alone.…”

Section: Effect Of Drug Combinations: Potentiation Of Spermicidal Actmentioning

confidence: 99%

“…Hence, these channels can be targeted for modulating Ca 2+ is and the pharmacological agents acting on these channels can be exploited as contact spermicides. Pharmacological modulation of Ca 2+ is has been investigated by treating human ejaculated semen samples with propranolol (White et al 1995), chelating agents (Lee et al 1996), 2 4dichlorobenzamil hydrochloride (Patni et al 2001;Reddy et al 2001), membrane stabilizers (Moudgil et al 2002a, b), H 2 -receptor antagonists (Gupta et al 2003), H 1 -receptor antagonists (Gupta et al 2004), IP 3 modulators and Ca 2+ -ATPase inhibitors (Gulati et al 2006). These studies revealed that an elevation of Ca 2+ is to ∼ 1200 nm produced complete loss of viability of human ejaculated sperm cells.…”

Section: Introductionmentioning

confidence: 99%

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Spermicidal activity of sulfonylureas and meglitinide analogues: role of intrasperm Ca2+ elevation

Kumar

Jain

Gupta

et al. 2008

Journal of Pharmacy and Pharmacology

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Intrasperm calcium concentration ([Ca2+]is) is known to play a vital role in regulating motility and viability of ejaculated spermatozoa. K ATP channel blockers are reported to block K ATP channels, leading to depolarization of the cell membrane. This activates the voltage-gated calcium channels, resulting in enhanced Ca2+ influx, which eventually elevates the intracellular [Ca2+] level. Hence, it can be hypothesized that drugs acting on K ATP channels could possess the ability to elevate [Ca2+]is. Sulfonylureas such as glibenclamide or gliclazide, as well as meglitinide analogues such as repaglinide, produced a dose- and time-dependent decrease in viability, each requiring 7.5 mM, 10 mM and 6.5 mM, respectively, to produce death of all sperm cells immediately upon addition to ejaculated human semen samples. The reduction in sperm viability was accompanied by an elevation of [Ca2+]is and was affected by removal of extracellular Ca2+. Significantly (P < 0.05) less time was required to elevate [Ca2+](is) and produce complete loss of sperm viability when any of these drugs were added to sperm cells simultaneously with selected agents affecting Ca2+ homeostasis. Thus, the spermicidal activity of these drugs attributed to elevation of [Ca2+]is and their synergism can be potentially exploited for developing contact spermicidal formulations.

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Section: Effect Of Gbe Gle or Rge On Ca 2+supporting

confidence: 94%

Section: Effect Of Drug Combinations: Potentiation Of Spermicidal Actmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Spermicidal activity of sulfonylureas and meglitinide analogues: role of intrasperm Ca2+ elevation

Kumar

Jain

Gupta

et al. 2008

Journal of Pharmacy and Pharmacology

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“…The reduction in sperm viability was accompanied by an elevation of Ca 2+ is and was affected by removal of extracellular Ca 2+ . Studies conducted by Gulati et al [144] with Miconazole nitrate, clotrimazole and loperamide hydrochloride furnished similar results where enhanced spermicidal activity of miconazole, clotrimazole and loperamide appeared to be due to further mobilization of Ca 2+ from partially depleted intrasperm Ca 2+ stores. Synergism of spermicidal activity and intrasperm Ca 2+ elevation by miconazole or clotrimazole was observed when Ca 2+ efflux from spermcells was simultaneously inhibited by 20,40-dichlorobenzamil hydrochloride, a Na + -Ca 2+ exchange inhibitor.…”

Section: Major Possible Pathways By Which the Spermicides Work Changementioning

confidence: 63%

Insights of Spermicidal Research: An Update

Hazra¹

2014

JFIV Reprod Med Genet

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Spermicides came into existence as a method of contraception for over hundred years. Since then, investigations and developments in this field have led to more and more fruitful as well as promising results but still left enough scope for further studies. The titled article manifests a brief discussion on the development of spermicides from different natural and synthetic sources, a compilation of the promising molecules and even extracts and includes an outline of the basic physiology behind the bioactivity. Since spermicides are only one among several other methods of contraception adopted and practiced, an attempt has been made to probe the necessity and advantage of spermicides over other modes of contraception, emphasizing on the requirements and scope of future investigations in this field.

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“…The authors, in this well designed and performed study, highlighted the role of intrasperm calcium concentration in regulating motility and viability of ejaculated spermatozoa. In recent years, other reports concerning the impact of some drugs, such as miconazole, clotrimazole or loperamide, on viability of human spermatozoa have been reported (Gulati et al 2006). However, the impact of drugs on sperm quality and male fertility may be underestimated.…”

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confidence: 99%

A possible negative effect of co-administered amlodipine and atorvastatin on semen volume and spermatozoa in men

et al. 2008

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To the editor,We read with great interest the recent study of Kumar et al (2008) published in this journal, concerning the role of glibenclamide or gliclazide and repaglinide in decreasing sperm quality. The authors, in this well designed and performed study, highlighted the role of intrasperm calcium concentration in regulating motility and viability of ejaculated spermatozoa. In recent years, other reports concerning the impact of some drugs, such as miconazole, clotrimazole or loperamide, on viability of human spermatozoa have been reported (Gulati et al 2006). However, the impact of drugs on sperm quality and male fertility may be underestimated. We focused our attention on the co-administration of statins (or HMG-CoA reductase inhibitors) and calcium-channel antagonists. The co-administration of atorvastatin and amlodipine has been reported as well-tolerated treatment for coexisting hypertension and dyslipidaemia (Messerli et al 2006) and without demonstrating significant adverse pharmacodynamic interactions or effects (Preston et al 2007). No studies regarding the effect of the co-administration of atorvastatin and amlodipine on male fertility have been reported. On the other hand, the absence of influence of statins on testicular reproductive function has already been demonstrated by several authors (Bernini et al 1998;Dostal et al 2001). We have recently reviewed our outpatients urological database to evaluate the impact of the co-administration of atorvastatin and amlodipine on male fertility. From a total study population of 689 patients with coexisting hypertension and dyslipidaemia attending our department for all urological diseases (with the exception of infertility), we selected all those patients who had been treated with either atorvastatin or amlodipine or atorvastatin and amlodipine co-administration, with an age lower than 55 years. We finally enrolled 287 patients; 12 patients were excluded for lack of clinical information. Thus, data from 275 were analysed. Ninety-one out of 275 had been treated with atorvastatin, 87 with amlodipine and 97 co-administered atorvastatin and amlodipine. All patients (mean age 48.5 years) had been undergoing pharmacological treatments for at least 12 months. From each patient we obtained at least two consecutive semen parameter analyses (with a mean interval time of 13.3 months). Fisher's exact test or Chi-square test ( 2 ) were used to assess statistical significance with P 0.05 accepted as significant. The two groups of patients did not show any significant difference in terms of smoking or other drug use. The two groups of patients who had undergone atorvastatin or amlodipine treatment did not have significant changes in two consecutive semen characteristics analyses. On the other hand, the group of patients who had undergone co-administration with atorvastatin and amlodipine demonstrated significant differences in semen parameters in the two consecutive semen analyses. In particular, the semen volume was significantly different (3.4 mL vs 1.1 mL) between the...

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Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Cited by 5 publications

References 17 publications

Spermicidal activity of sulfonylureas and meglitinide analogues: role of intrasperm Ca2+ elevation

Spermicidal activity of sulfonylureas and meglitinide analogues: role of intrasperm Ca2+ elevation

Insights of Spermicidal Research: An Update

A possible negative effect of co-administered amlodipine and atorvastatin on semen volume and spermatozoa in men

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