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Testosterone Replacement, Low T, HCG, & Beyond
When Testosterone Is Not Enough
How to increase dopamine?
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<blockquote data-quote="Cataceous" data-source="post: 225587" data-attributes="member: 38109"><p>I don't know more than what the <a href="https://en.wikipedia.org/wiki/Selegiline#Pharmacokinetics" target="_blank">Wiki article</a> says:</p><p></p><p style="margin-left: 20px"><strong>Pharmacokinetics</strong></p> <p style="margin-left: 20px">Selegiline has an <u>oral bioavailability of about 10%</u>, which increases when ingested together with a fatty meal, as the molecule is fat soluble.[1][23] Selegiline and its metabolites bind extensively to plasma proteins (at a rate of 94%). They cross the blood–brain barrier and enter the brain, where they most concentrated at the thalamus, basal ganglia, midbrain, and cingulate gyrus.[6][9]</p> <p style="margin-left: 20px"></p> <p style="margin-left: 20px">Selegiline is mostly metabolized in the intestines and liver; it and its metabolites are excreted in the urine.[1]</p> <p style="margin-left: 20px"></p> <p style="margin-left: 20px">Buccal administration of selegiline results in 5-fold higher bioavailability, more reproducible blood concentration, and produces less amphetamine metabolites than the oral tablet form.[24]</p><p></p><p style="margin-left: 20px"><strong>Metabolism</strong></p> <p style="margin-left: 20px">Selegiline is metabolized by cytochrome P450 to L-desmethylselegiline and levomethamphetamine.[25][26] Desmethylselegiline has some activity against MAO-B, but much less than that of selegiline.[19][18] It is thought to be further metabolized by CYP2C19.[27] Levomethamphetamine (the less potent of the two enantiomers of methamphetamine) is converted to levoamphetamine (the less potent of the two enantiomers of amphetamine, with regards to psychological effects).</p> <p style="margin-left: 20px"></p> <p style="margin-left: 20px">Due to the presence of these metabolites, people taking selegiline may test positive for "amphetamine" or "methamphetamine" on drug screening tests.[28] While the amphetamine metabolites may contribute to selegiline's ability to inhibit reuptake of the neurotransmitters dopamine and norepinephrine, they have also been associated with orthostatic hypotension and hallucinations.[26][29][30] The amphetamine metabolites are hydroxylated and, in phase II, conjugated by glucuronyltransferase.</p> <p style="margin-left: 20px">...</p> <p style="margin-left: 20px"></p> <p style="margin-left: 20px"><strong>Patch</strong></p> <p style="margin-left: 20px">Following application of the patch to humans, an average of <u>25% to 30%</u> of the selegiline content is delivered systemically over 24 hours. Transdermal dosing results in significantly higher exposure to selegiline and lower exposure to all metabolites when compared to oral dosing; this is due to the extensive first-pass metabolism of the pill form and low first-pass metabolism of the patch form. ...</p></blockquote><p></p>
[QUOTE="Cataceous, post: 225587, member: 38109"] I don't know more than what the [URL='https://en.wikipedia.org/wiki/Selegiline#Pharmacokinetics']Wiki article[/URL] says: [INDENT][B]Pharmacokinetics[/B][/INDENT] [INDENT]Selegiline has an [U]oral bioavailability of about 10%[/U], which increases when ingested together with a fatty meal, as the molecule is fat soluble.[1][23] Selegiline and its metabolites bind extensively to plasma proteins (at a rate of 94%). They cross the blood–brain barrier and enter the brain, where they most concentrated at the thalamus, basal ganglia, midbrain, and cingulate gyrus.[6][9][/INDENT] [INDENT][/INDENT] [INDENT]Selegiline is mostly metabolized in the intestines and liver; it and its metabolites are excreted in the urine.[1][/INDENT] [INDENT][/INDENT] [INDENT]Buccal administration of selegiline results in 5-fold higher bioavailability, more reproducible blood concentration, and produces less amphetamine metabolites than the oral tablet form.[24][/INDENT] [INDENT][B]Metabolism[/B][/INDENT] [INDENT]Selegiline is metabolized by cytochrome P450 to L-desmethylselegiline and levomethamphetamine.[25][26] Desmethylselegiline has some activity against MAO-B, but much less than that of selegiline.[19][18] It is thought to be further metabolized by CYP2C19.[27] Levomethamphetamine (the less potent of the two enantiomers of methamphetamine) is converted to levoamphetamine (the less potent of the two enantiomers of amphetamine, with regards to psychological effects).[/INDENT] [INDENT][/INDENT] [INDENT]Due to the presence of these metabolites, people taking selegiline may test positive for "amphetamine" or "methamphetamine" on drug screening tests.[28] While the amphetamine metabolites may contribute to selegiline's ability to inhibit reuptake of the neurotransmitters dopamine and norepinephrine, they have also been associated with orthostatic hypotension and hallucinations.[26][29][30] The amphetamine metabolites are hydroxylated and, in phase II, conjugated by glucuronyltransferase.[/INDENT] [INDENT]...[/INDENT] [INDENT][/INDENT] [INDENT][B]Patch[/B][/INDENT] [INDENT]Following application of the patch to humans, an average of [U]25% to 30%[/U] of the selegiline content is delivered systemically over 24 hours. Transdermal dosing results in significantly higher exposure to selegiline and lower exposure to all metabolites when compared to oral dosing; this is due to the extensive first-pass metabolism of the pill form and low first-pass metabolism of the patch form. ...[/INDENT] [/QUOTE]
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Testosterone Replacement, Low T, HCG, & Beyond
When Testosterone Is Not Enough
How to increase dopamine?
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