Wagner83

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I meant 4mg. This actually isn't a large dose. A typical starting dose of metergoline is 12 mg/day, and increases up to 24mg/day if needed. The package insert on the pharmaceutical preperation suggests 4mg on the first day, 8mg on the second day, and 12mg thereafter. Google "Liserdol", you may have to translate from German.

That being said, when this guinea pig gets around to restarting metergoline after this break, he's going to try microdosing 1 or 2 drops per day,
Damn Liserdol is cheaper, but it's like they filled the pill with as much crap as possible. If you are using this perhaps you are reacting to titanum dioxide, I don't know about the safety of the other ones.
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_________________________________________________

Effects of various serotonin receptor subtype-selective antagonists alone and on m-chlorophenylpiperazine-induced neuroendocrine changes in rats.
Aulakh CS1, Hill JL, Murphy DL.
Author information
Abstract

Administration of m-chlorophenylpiperazine [m-CPP, a serotonin (5-HT) agonist] to rats increases plasma concentrations of prolactin and corticosterone. Pretreatment with various doses of ritanserin (5-HT1C/5-HT2 antagonist), ICS 205-930 and MDL-72222 (5-HT3 antagonists), iodocyanopindolol or CG361A (beta adrenoceptor antagonists) and spiperone (5-HT1A/5-HT2 antagonist) did not attenuate m-CPP-induced increases in plasma concentrations of prolactin. In contrast, pretreatment with various doses of metergoline (5-HT1/5-HT2 antagonist), propranolol (beta adrenoceptor antagonist that also has binding affinity for 5-HT1A, 5-HT1B and 5-HT1C sites), mesulergine and mianserin (5-HT1C/5-HT2 antagonists) attenuated m-CPP-induced increases in plasma prolactin. On the other hand, m-CPP-induced increases in corticosterone concentrations were attenuated only by pretreatment with a low dose of mianserin and a high dose of spiperone. When administered without m-CPP, metergoline, mesulergine, ritanserin, ICS 205-930 and high doses of mianserin, spiperone and propranolol increased plasma corticosterone secretion. On the other hand, none of the antagonists used in the present study, except spiperone, had any significant effect on plasma prolactin secretion. These findings suggest that m-CPP-induced prolactin secretion is mediated by stimulation of 5-HT1C receptors while corticosterone secretion may be mediated either by an antagonistic effect at 5-HT3 receptor subtype or by nonserotonergic mechanisms. Alternatively, enhancement of corticosterone secretion by the 5-HT antagonists when administered alone may be responsible for their failure to block m-CPP-induced corticosterone secretion.(ABSTRACT TRUNCATED AT 250 WORDS).

@haidut
 
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Bluemustang

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Damn Liserdol is cheaper, but it's like they filled the pill with as much crap as possible. If you are using this perhaps you are reacting to titanum dioxide, I don't know about the safety of the other ones.
Hilfsstoffe
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  • Hypromellose
  • Povidon K25
  • Carmellose natrium
  • Maisstärke
  • Lactose-1-Wasser
  • Macrogol 6000
  • Dimeticon
  • Titandioxid

Yes it is quite cheap in Germany and Italy, but you do need a prescription. I've never understood myself the amount of excipients used in pills (and even supplement capsules), its so unnecessary.

I have both Idealabs and Rx Teofarma Metergoline, but am currently experimenting with Idealabs version.
 
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haidut

haidut

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Damn Liserdol is cheaper, but it's like they filled the pill with as much crap as possible. If you are using this perhaps you are reacting to titanum dioxide, I don't know about the safety of the other ones.
Hilfsstoffe
  • Magnesium stearat
  • Hypromellose
  • Povidon K25
  • Carmellose natrium
  • Maisstärke
  • Lactose-1-Wasser
  • Macrogol 6000
  • Dimeticon
  • Titandioxid
_________________________________________________

Effects of various serotonin receptor subtype-selective antagonists alone and on m-chlorophenylpiperazine-induced neuroendocrine changes in rats.
Aulakh CS1, Hill JL, Murphy DL.
Author information
Abstract

Administration of m-chlorophenylpiperazine [m-CPP, a serotonin (5-HT) agonist] to rats increases plasma concentrations of prolactin and corticosterone. Pretreatment with various doses of ritanserin (5-HT1C/5-HT2 antagonist), ICS 205-930 and MDL-72222 (5-HT3 antagonists), iodocyanopindolol or CG361A (beta adrenoceptor antagonists) and spiperone (5-HT1A/5-HT2 antagonist) did not attenuate m-CPP-induced increases in plasma concentrations of prolactin. In contrast, pretreatment with various doses of metergoline (5-HT1/5-HT2 antagonist), propranolol (beta adrenoceptor antagonist that also has binding affinity for 5-HT1A, 5-HT1B and 5-HT1C sites), mesulergine and mianserin (5-HT1C/5-HT2 antagonists) attenuated m-CPP-induced increases in plasma prolactin. On the other hand, m-CPP-induced increases in corticosterone concentrations were attenuated only by pretreatment with a low dose of mianserin and a high dose of spiperone. When administered without m-CPP, metergoline, mesulergine, ritanserin, ICS 205-930 and high doses of mianserin, spiperone and propranolol increased plasma corticosterone secretion. On the other hand, none of the antagonists used in the present study, except spiperone, had any significant effect on plasma prolactin secretion. These findings suggest that m-CPP-induced prolactin secretion is mediated by stimulation of 5-HT1C receptors while corticosterone secretion may be mediated either by an antagonistic effect at 5-HT3 receptor subtype or by nonserotonergic mechanisms. Alternatively, enhancement of corticosterone secretion by the 5-HT antagonists when administered alone may be responsible for their failure to block m-CPP-induced corticosterone secretion.(ABSTRACT TRUNCATED AT 250 WORDS).

@haidut

The human studies with metergoline show reductions in cortisol. Cyproheptadine does the same (also studied in humans) and this is why it is used for Cushing syndrome. Maybe rats have a different response to these chemicals than us.
 

Zpol

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Yes, that is one of the nicer things about metergoline - it does not seem to have activity on 5-HT3 and thus does not cause constipation. So, due to this lack of constipating activity it is used in some countries off-label to treat both IBS-C and IBS-D.

What's this now?!? It's used to treat IBS-C?! By what mechanism? I can't find any studies indicating how this works or anything at all relating to IBS-C. I see the studies showing it treats candida but IBS is moreso a dysbiosis of bacteria and archea. Can someone point out to me how to use this to treat IBS-C?
If the mechanism is antimicrobial in the gut, I assume it would have to be taken orally between meals and cycled so as to not cause resistance.
If the mechanism is reducing cortisol then I would take in the morning and afternoon only and theoretically would be best taken topically.
Would one have to quite taking Estroban if one were to take Metergoline (because of the Vit. E)?
 
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haidut

haidut

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What's this now?!? It's used to treat IBS-C?! By what mechanism? I can't find any studies indicating how this works or anything at all relating to IBS-C. I see the studies showing it treats candida but IBS is moreso a dysbiosis of bacteria and archea. Can someone point out to me how to use this to treat IBS-C?
If the mechanism is antimicrobial in the gut, I assume it would have to be taken orally between meals and cycled so as to not cause resistance.
If the mechanism is reducing cortisol then I would take in the morning and afternoon only and theoretically would be best taken topically.
Would one have to quite taking Estroban if one were to take Metergoline (because of the Vit. E)?

Anti-serotonin drugs are being tested right now for IBS. Just Google for "TPH inhibitor IBS". None of them are approved officially yet, but studies have talked about anti-serotonin drugs for IBS before. Here is one.
Management of functional abdominal pain and irritable bowel syndrome in children and adolescents

Peat also said in his articles that anti-serotonin drugs can probably successfully treat IBS. I said metergoline is used off-label, so you are not going to find studies about it for IBS. However, it is a non-selective antagonist just like cyproheptadine, so the usage makes perfect sense.
 

tomisonbottom

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This stuff is amazing.

Interesting how different each subject responds because some said it caused sleepiness, but in my subject 5 drops orally resulted in almost instant skyrocketing of energy, increased heartbeat (but not excessive) increased blood flow, and major dopamine boost; almost euphoric.

This is the 1st try with oral. Will see if results continue, or it's a 1 time thing.
 

Wagner83

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This stuff is amazing.

Interesting how different each subject responds because some said it caused sleepiness, but in my subject 5 drops orally resulted in almost instant skyrocketing of energy, increased heartbeat (but not excessive) increased blood flow, and major dopamine boost; almost euphoric.

This is the 1st try with oral. Will see if results continue, or it's a 1 time thing.
Remember the half-life is very long.
 
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haidut

haidut

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This stuff is amazing.

Interesting how different each subject responds because some said it caused sleepiness, but in my subject 5 drops orally resulted in almost instant skyrocketing of energy, increased heartbeat (but not excessive) increased blood flow, and major dopamine boost; almost euphoric.

This is the 1st try with oral. Will see if results continue, or it's a 1 time thing.

Awesome, thanks for the feedback!
 

ddjd

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I love metergolines initial effects and I only take about 4 drops once a week, but sometimes after a few hours I start feeling really weak, really tired, almost feverish but no actual fever, just weak all over.

What is that?
 

ddjd

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4mg for 3 days now.
First two days were rough - anxious fatigue, flu-like symptoms, foggy brain, a big depressed, uncomfortable digestion.

Today, pulse (finally!), has risen to 75 bpm after breakfast. Nothing else has made this happen. Nothing.
Extremely warm feet and hands (again, nothing else has helped this).
Positive mood, very calm and relaxed --digestion feeling strong.
Exact same thing happened to me. I feel weak all over and tited but can't stop fidgeting and can't sleep
 

Zpol

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Anti-serotonin drugs are being tested right now for IBS. Just Google for "TPH inhibitor IBS". None of them are approved officially yet, but studies have talked about anti-serotonin drugs for IBS before. Here is one.
Management of functional abdominal pain and irritable bowel syndrome in children and adolescents

Peat also said in his articles that anti-serotonin drugs can probably successfully treat IBS. I said metergoline is used off-label, so you are not going to find studies about it for IBS. However, it is a non-selective antagonist just like cyproheptadine, so the usage makes perfect sense.

Thank you. This info will be very helpful in my research.
 

Bluemustang

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Remember the half-life is very long.

What's interesting is that the half-life of Metergoline is only 50 minutes. Strangely it has receptor effects that persist much longer than its blood levels would suggest.

Another interesting thing is that 75% of Metergoline is removed in first-pass metabolism, so those taking it orally may have different experiences than those taking it sublingually or topically.

I've been taking it sublingually and its been rough. It seems a number of people having positive effects are taking it orally only. Perhaps the difference in the amount of Metergoline entering circulation is the difference, or perhaps one the metabolites is more responsible for the positive effects, with less negative effects?

Pharmacokinetics and bioavailability of metergoline in healthy volunteers after single i.v. and oral administration. - PubMed - NCBI

Abstract
Concentrations of unchanged metergoline and its main metabolite, 1-demethylmetergoline, were measured by HPLC and fluorescence detector in the plasma of 13 healthy male volunteers. The subjects received on various occasions the following single-dose metergoline treatments: 4 mg by i.v. infusion (n = 7), 8 mg orally as aqueous solution (n = 7) and 8 mg orally as two different formulations of film-coated tablets (Formulation A, n = 12; Formulation B, n = 12). The mean plasma t 1/2 of metergoline and of 1-demethylmetergoline were about 50 min and 100 min, respectively, independent of the route of administration. A considerable first-pass effect was evident from the data, with about 75% of metergoline being metabolized by the liver before reaching the systemic circulation. However, the availability of the drug in terms of 1-demethylmetergoline was similar for the i.v. and oral routes of administration indicating a complete absorption of the solution from the gastrointestinal tract. Very low plasma levels of another metabolite (12-hydroxymetergoline) were detected in some patients. The bioavailability of film-coated tablets in Formulation B was slightly better than for Formulation A with regard to both relative absorption (A vs B = 82%) and lower interpatient variation. Compared with oral solution, the absorption of Formulation B was slightly slower but practically complete.
 

Wagner83

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THanks for the link that's what I was referring to (so, it wasn't about half-life). With metergoline (and many supps) less may be more both in terms of frequency and quantity. Such saturation reported nausea with more than 2 drops daily I think, others reported 0 effect, others had effects from oral but not topical, Andman reported changing his life with two weekly doses.. So who knows what to do, experimenting sounds more like it.
 

Bluemustang

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THanks for the link that's what I was referring to (so, it wasn't about half-life). With metergoline (and many supps) less may be more both in terms of frequency and quantity. Such saturation reported nausea with more than 2 drops daily I think, others reported 0 effect, others had effects from oral but not topical, Andman reported changing his life with two weekly doses.. So who knows what to do, experimenting sounds more like it.

Yes! This is what I have begun to notice as well. Several posters who have been using higher doses have had no effect or negative effects. A number of posters using very small oral doses have had good to profound effects, just like you said.

Time to approach this a little differently...
 

Luckytype

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Yes! This is what I have begun to notice as well. Several posters who have been using higher doses have had no effect or negative effects. A number of posters using very small oral doses have had good to profound effects, just like you said.

Time to approach this a little differently...

I am ordering lisuride to use in conjuction with cypro. I feel like due to limited anecdotal it may be similar with lisuride as well.

What were some of the differences you noticed upon changing your dosing of metegoline?
 

Bluemustang

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I am ordering lisuride to use in conjuction with cypro. I feel like due to limited anecdotal it may be similar with lisuride as well.

What were some of the differences you noticed upon changing your dosing of metegoline?

My experiment is on pause after stopping the higher dose, and I haven't restarted at a lower dose yet. Going to wait a couple more weeks and start with a clean slate.
 

Waynish

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Interesting how different each subject responds because some said it caused sleepiness, but in my subject 5 drops orally resulted in almost instant skyrocketing of energy, increased heartbeat (but not excessive) increased blood flow, and major dopamine boost; almost euphoric.

Yep, and different effects on the same subject based on their current state - reminds me of LSD. While I could never sleep while on LSD, I find it easy to sleep on any of these similar substances.
 

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