OP: "Hi all, just acquired some Tapentadol and wondered what it was like in not therapeutic doses? Got 100mg orange tablets.
I’ve tried Tramadol for pain but replaced with this and wondered if there was any experiences with Tapentadol?"
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Dosage Info from Psychonautwiki.org
Tapentadol has an oral bioavailability of about 32%. Tapentadol is metabolized by the Cytochrome P450 system in the liver and is excreted by the kidneys in urine as well as in feces. Unlike most opioids, tapentadol is also a norepinephrine reuptake inhibitor and also has weak serotonergic effects as well.
Tapentadol is an orally available, synthetic benzenoid that acts as an agonist for the mu-opioid receptor (MOR) and inhibits the reuptake of noradrenaline, with potential anti-nociceptive activity. Upon oral administration, tapentadol binds to the MOR which enhances MOR-mediated signaling, interferes with the sensation of pain and results in an analgesic effect. Tapentadol also inhibits the reuptake of noradrenaline, which increases the levels of noradrenaline (NA), activates the inhibitory alpha-2 receptors and results in an analgesic effect.
Tapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug.
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@deficiT 9/22
It is similar to
tramadol in its dual mechanism of action; namely, its ability to activate the mu opioid receptor and inhibit the reuptake of norepinephrine.
Unlike tramadol, it has only weak effects on the reuptake of serotonin and is a significantly more potent opioid with no known active metabolites.
Tapentadol is not a
pro-drug and therefore does not rely on metabolism to produce its therapeutic effects; this makes it a useful moderate-potency analgesic option for patients who do not respond adequately to more commonly used opioids due to genetic disposition (poor metabolizers of
CYP3A4and
CYP2D6), as well as providing a more consistent dosage-response range among the patient population.
The
potency of tapentadol is somewhere between that of tramadol and
morphine,
with an analgesic efficacy comparable to that of oxycodone despite a lower incidence of side effects.