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Active Ingredients: Sildenafil Citrate



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UK-103,320 appeared to distribute more slowly from the plasma into the semen, resulting in a lack of correlation between semen and plasma concentrations. Sildenafil was well tolerated; no patient withdrew from the study due to adverse events attributed to sildenafil.


Ejaculate viscosity data were may-transformed to satisfy the distributional changes of the analysis of variance and presented as back-transformed critical means.

Conclusions These results indicate that a single 100-mg oral dose of sildenafil does not have an adverse effect on sperm function or ejaculate quality.

Keywords: sildenafil, UK-103,320, sperm, ejaculate, safety, pharmacokinetics, protein binding Introduction Erectile dysfunction ED is a widespread condition that can have a negative impact on quality of life, affecting both older and younger men.

Until recently, no effective oral therapy existed.

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Available treatments were highly cumbersome or invasive, and many patients and their partners found them unacceptable solutions to the problem.

A large number of drugs can be transported into the seminal fluid, where they can have direct effects on sperm function, physiology, metabolism or genetic composition. Several drugs have been shown to affect sperm motility in particular ; these include compounds with phosphodiesterase PDE -inhibitory activity that have the potential to increase motility.

One such drug, pentoxifylline, which is a cyclic adenosine monophosphate cAMP PDE inhibitor, has been shown to stimulate human sperm motility both in vitro and in vivo.

Sildenafil is a potent and selective inhibitor of the cyclic guanosine monophosphate cGMP -specific PDE type 5 enzyme and thus enhances the activity of the nitric oxide—cGMP pathway that promotes penile erection.


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A large number of drugs can be reported into the seminal fluid, where they can have watery effects on sperm function, physiology, metabolism or bruising composition.

The drug is relatively lipophilic log D 7. It is likely that sildenafil will be used by men with ED as an aid to procreation, especially by younger patients who have ED secondary to spinal cord injury.

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  • Because of this, a clinical study was conducted to investigate the effect of a single oral dose of sildenafil on a number of semen and sperm motility and morphology parameters.

    In addition, the concentrations of sildenafil and its major circulating metabolite UK-103,320 were measured in semen samples and compared with those obtained in plasma. Exclusion criteria were as follows: azoospermia or extreme oligospermia, asthenospermia, or teratospermia or any combination of these at baseline; clinically significant disease; allergy; abnormality in prestudy laboratory data and physical examination; use of any medication except paracetamol in the 3 weeks before the study; use of any experimental drug in the 4 months before the study; alcohol consumption of more than 28 units per week; drug abuse; and use of more than 10 cigarettes or equivalent tobacco per day.

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