Pharmacokinetic and Pharmacodynamic Factors to Consider
In volume 97 of
BJU International, Karl-Erik Andersson, John P. Mulhall, and Michael G. Wyllie examine the pharmacokinetic and pharmacodynamic features of dapoxetine
( Priligy ™ )
. The drug was developed for the treatment of premature or rapid ejaculation, although it has not yet been approved by the Food and Drug Administration ( FDA ). Basically, pharmacokinetics is the study of how the human body reacts to or responds to a particular drug. Pharmacodynamics studies what a drug does to the body, taking into account dosages and concentrations of the drug.
One of the limitations of treating premature ejaculation ( PE ) is the fact that there is not a consistent definition used to diagnose the condition. Researchers contend that there are both physical and psychological factors in premature ejaculation, although not all studies point to the same factors with the same results. The majority of the studies use intravaginal ejaculatory latency time ( IELT ) as a marker of the physical characteristics. These studies generally use IELT of ≤2 minutes to define the condition. Psychological characteristics are much more difficult to quantify including: lack of perceived control over the ejaculatory process, sexual satisfaction of both the male and his partner, and the degree of personal distress that is caused by the condition.
( Priligy ™ )
is a selective serotonin reuptake inhibitor ( SSRI ), although it differs with long-acting SSRIs on the market today. Pharmacological studies demonstrate that dapoxetine
( Priligy ™ )
is effective on the neurotransmitter serotonin, making it similar to other SSRIs like clomipramine. It differs, however, from these SSRIs in that it is a non-halogenated compound (does not have halogen atoms). In addition, it metabolizes quickly in the body, generally peaking 60-90 minutes after ingestion. Other SSRIs usually peak 6 hours after ingestion.
Dapoxetine
( Priligy ™ )
is virtually untraceable in the body a few hours after administration, leaving only trace amounts 24 hours after ingestion. It does not appear to have cumulative effects unlike other SSRIs that require chronic dosing in order to be effective for both depression and premature ejaculation.
During Phase III studies, researchers recommended taking dapoxetine
( Priligy ™ )
1-3 hours prior to sexual intercourse. Other SSRIs require dosing on a daily basis for sometimes several weeks in order to achieve maximal effectiveness. As such, dapoxetine
( Priligy ™ )
works from the first dose and “on demand” unlike other medications that may claim to have “on demand” properties, yet require repeated dosing in order achieve maximum response levels. Even though patient satisfaction and perceived control over ejaculation is more difficult to measure objectively, patients using dapoxetine
( Priligy ™ )
reported increases in both of these areas.
The most important side to note is nausea. Patients taking both 30 and 60mg of dapoxetine noted nausea as the most prominent side effect. The nausea is short-term and related only to dapoxetine in the system. It abates as soon as the drug metabolizes in the system. Other SSRIs may cause additional sexual side effects the longer they are administered. For example, some patients report diminished libido after chronic dosing for premature ejaculation ( PE ). These same sexual side effects were not noted with dapoxetine.
Researchers note that “sexual intercourse is rarely premeditated,” and dapoxetine comes as close as possible to mimicking on-demand dosing while still offering maximum benefit. Side effects are few, limited to dosing of the drug and are not long-term. It is absorbed rapidly in the body, metabolized quickly, and leaves inactive compounds after it is metabolized.
Andersson, Karl-Erik; Mulhall, John P.; and Wyllie, Michael G. “Pharmacokinetic and Pharmacodynamic Features of Dapoxetine, a Novel Drug for ‘On-Demand’ Treatment of Premature Ejaculation.”
BJU International, (97), 2006, 311-315.
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