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Clinical Use of Anabolics and Hormones
Clinical Use of Anabolics and Hormones
Oxandrolone via Troche to Bypass First Pass Metabolism. Effective?
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<blockquote data-quote="tareload" data-source="post: 143158"><p><em>I’d be interested in hearing others experience using oxandrolone troches instead of oral delivery (capsules) to bypass first-pass metabolism and reduce liver toxicity and lower minimum effective dose</em>. Since oxandrolone has excellent oral bioavailability (97-98%) and is actually metabolized partially by kidneys (haven’t looked at the original studies to support this assertion), I have a hard time believing that sublingual/buccal administration is going to do much to lower liver damage for same dosage (i,e, you end up swallowing most of the troche as it dissolves?). I’ve pulled 10-15 studies and most seem to show similar pharmacokinetics for oral and sublingual administration of drugs that are metabolized similarly (ie CYP 3A4). </p><p></p><p>Here’s an example with DHEA troche, similar result to oral administration (pill):</p><p><a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4607057/" target="_blank">Novel dehydroepiandrosterone troche supplementation improves the serum androgen profile of women undergoing in vitro fertilization</a></p><p><em></em></p><p><em>A few thoughts:</em></p><p>Seems like oxandrolone’s reputation for “mildness” is related to dosage and individual’s genetic response. 50-100 mg/day of oxandrolone probably ain’t gonna give the same result as 20 mg/day so just wanted to daylight the obvious. Caffeine or other CYP450 modulation also to be considered. Thanks for sharing your experiences on dosage experience Nelson. I don’t think anyone is doing histology on the kidneys while trial participants are running oxandrolone but perhaps that’s another place to look.</p><p></p><p><a href="https://www.physiology.org/doi/full/10.1152/japplphysiol.00808.2003" target="_blank">Treatment with oxandrolone and the durability of effects in older men</a></p><p></p><p>I was just genuinely curious why oxandrolone is dispensed from legitimate pharmacies via troche when its oral (delivery via digestive system) bioavailability is so high. Seems like a hammer in search of a nail. What am I missing? Hence I thought about avoiding liver damage. But, just because the drug doesn’t get delivered to liver/circulation via portal system doesn’t mean it can’t come back to the liver/kidney via serum for additional metabolism. Seems to me a troche’s strength is to get molecules (which have low oral bioavailability) into circulation by increasing bioavailability (avoid digestive system) and not to minimize end-organ metabolism damage. I can’t find an example of the latter in the literature.</p><p></p><p>Now, with regard to the delivery systems, would be an interesting experiment to test these different delivery modes on CMP/SHBG, lipids (hepatic lipase etc.). Appears to be a challenge for some to keep serum T levels reasonable (even with exogenous T usage) while also running oxandrolone since SHBG heads toward zero:</p><p></p><p><a href="https://www.ncbi.nlm.nih.gov/pubmed/17961146" target="_blank">Low sex hormone-binding globulin and testosterone levels in association with erectile dysfunction among human immunodeficiency virus-infected men receiving testosterone and oxandrolone.</a></p><p></p><p>On second thought, I probably need to correct myself. If you can get drug into systemic circulation (while avoiding first pass) where it presents at reduced systemic serum concentration (vs concentration upon introduction into portal vein) and metabolic clearance typically first order function of serum concentration, I can see where this concept has legs although effect may be quite minimal with highly bioavailable oxandrolone. Especially if most of the metabolic clearance is done in kidneys anyway. In short, dilution <em>may be</em> the solution.</p><p></p><p>Nice demonstration of the measurements and procedure you’d leverage clinically to study this with oral vs sublingual / rectal approaches:</p><p><a href="https://jpharmsci.org/article/S0022-3549(15)50414-0/pdf" target="_blank">Moment Analysis of Intestinal First-Pass Metabolism by Portal–Systemic Concentration Difference in Single Conscious Rat Using 5′-Deoxy-5-Fluorouridine and 5-Fluorouracil as Model Drug System</a></p><p></p><p>Thanks for sharing any experiences.</p></blockquote><p></p>
[QUOTE="tareload, post: 143158"] [I]I’d be interested in hearing others experience using oxandrolone troches instead of oral delivery (capsules) to bypass first-pass metabolism and reduce liver toxicity and lower minimum effective dose[/I]. Since oxandrolone has excellent oral bioavailability (97-98%) and is actually metabolized partially by kidneys (haven’t looked at the original studies to support this assertion), I have a hard time believing that sublingual/buccal administration is going to do much to lower liver damage for same dosage (i,e, you end up swallowing most of the troche as it dissolves?). I’ve pulled 10-15 studies and most seem to show similar pharmacokinetics for oral and sublingual administration of drugs that are metabolized similarly (ie CYP 3A4). Here’s an example with DHEA troche, similar result to oral administration (pill): [URL='https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4607057/']Novel dehydroepiandrosterone troche supplementation improves the serum androgen profile of women undergoing in vitro fertilization[/URL] [I] A few thoughts:[/I] Seems like oxandrolone’s reputation for “mildness” is related to dosage and individual’s genetic response. 50-100 mg/day of oxandrolone probably ain’t gonna give the same result as 20 mg/day so just wanted to daylight the obvious. Caffeine or other CYP450 modulation also to be considered. Thanks for sharing your experiences on dosage experience Nelson. I don’t think anyone is doing histology on the kidneys while trial participants are running oxandrolone but perhaps that’s another place to look. [URL='https://www.physiology.org/doi/full/10.1152/japplphysiol.00808.2003']Treatment with oxandrolone and the durability of effects in older men[/URL] I was just genuinely curious why oxandrolone is dispensed from legitimate pharmacies via troche when its oral (delivery via digestive system) bioavailability is so high. Seems like a hammer in search of a nail. What am I missing? Hence I thought about avoiding liver damage. But, just because the drug doesn’t get delivered to liver/circulation via portal system doesn’t mean it can’t come back to the liver/kidney via serum for additional metabolism. Seems to me a troche’s strength is to get molecules (which have low oral bioavailability) into circulation by increasing bioavailability (avoid digestive system) and not to minimize end-organ metabolism damage. I can’t find an example of the latter in the literature. Now, with regard to the delivery systems, would be an interesting experiment to test these different delivery modes on CMP/SHBG, lipids (hepatic lipase etc.). Appears to be a challenge for some to keep serum T levels reasonable (even with exogenous T usage) while also running oxandrolone since SHBG heads toward zero: [URL='https://www.ncbi.nlm.nih.gov/pubmed/17961146']Low sex hormone-binding globulin and testosterone levels in association with erectile dysfunction among human immunodeficiency virus-infected men receiving testosterone and oxandrolone.[/URL] On second thought, I probably need to correct myself. If you can get drug into systemic circulation (while avoiding first pass) where it presents at reduced systemic serum concentration (vs concentration upon introduction into portal vein) and metabolic clearance typically first order function of serum concentration, I can see where this concept has legs although effect may be quite minimal with highly bioavailable oxandrolone. Especially if most of the metabolic clearance is done in kidneys anyway. In short, dilution [I]may be[/I] the solution. Nice demonstration of the measurements and procedure you’d leverage clinically to study this with oral vs sublingual / rectal approaches: [URL='https://jpharmsci.org/article/S0022-3549(15)50414-0/pdf']Moment Analysis of Intestinal First-Pass Metabolism by Portal–Systemic Concentration Difference in Single Conscious Rat Using 5′-Deoxy-5-Fluorouridine and 5-Fluorouracil as Model Drug System[/URL] Thanks for sharing any experiences. [/QUOTE]
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Clinical Use of Anabolics and Hormones
Clinical Use of Anabolics and Hormones
Oxandrolone via Troche to Bypass First Pass Metabolism. Effective?
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