Tramadol is a centrally acting opioid analgesic used off-label to treat moderately severe pain and has shown promising efficacy for premature ejaculation. However, numerous side effects and the potential for addiction have prevented Tramadol from becoming a preferred treatment for PE. Zertane is a branded version of Tramadol by Vyrix Pharmaceuticals, a spin-off of Ampio Pharmaceuticals, targeted specifically for PE but not currently not available.
The way in which Tramadol delays ejaculation is not well understood. The general consensus is that tramadol delays ejaculation with a combination of effects including inhibiting the neuronal reuptake of serotonin, inhibiting the neuronal reuptake of noradrenaline, enhancing serotonin efflux, antinociceptive effects and inhibiting spinal somatosensory evoked potentials. In more understandable terms that a PE patient may understand, Tramadol may do the following:
· Acts as a SSRI similar to Dapoxetine / Priligy
· Numbs the entire nervous system to stimuli
Wong and Malde(1) reviewed five different studies and the data on Tramadol efficacy for PE varies dramatically. Only the multicenter study by Bar-Or et al was registered on the U.S. National Institutes of Health clinicaltrials.gov. The study showed about a 2.5 fold increase in IELT (intravaginal ejaculation latency time) which means that a man who normally lasts about 1 minute would be expected to last about 2.5 minutes. Tramadol must be taken at least 2 hours before sexual activity in order to be effective.
Tramadol has a half-life of approximately 6 hours which means that half the drug is still in the body after 6 hours and one-quarter after 12 hours. Side effects on average dissipate after about 10 hours. Low doses of Tramadol (25mg) appear to be tolerated well. However, a dose thought to be appropriate for the treatment of PE (75-100mg) has a significant side effect profile. Again, using the Bar-Or study, the rate of adverse effects in their study was 16.4% for the 89mg dose of Tramadol, expected to be the target Tramadol dose of Zertane. The most common side effects include: nausea, somnolence, erectile dysfunction, dyspepsia, headache, vomiting, and dizziness.
There is no market research data on the use of Tramadol for premature ejaculation. However, the trend appears to be that its use is decreasing. In addition to the inconvenience (planning two hours in advance) and side effects of Tramadol, many urologists are now using new topical medications with absorption technology. Such solutions have similar effectiveness with a much lower side effect profile and are available over-the-counter in the U.S.
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(1) Wong, BL and Malde, S. The use of tramadol "on-demand" for premature ejaculation: a systematic review. Urology 2013 Jan;81(1):98-103.
Zertane is a trademark of Ampio Pharmaceuticals