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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 14 of 14. This is the beginning of the thread.
Posted by willyeee on August 31, 2009, at 14:18:21
This is a tiny bit technical.ok some meds have there metabolites made into a med themselves.Its been argued that parnates metabolite is that close to a amphetamine,which makes sense since a metabolite shows up when the drug is leaving hence the insomia.Also however with the insomnia i notice my mood does actualy improve,just to damn late for any of this.
So to make this short,i i looked and looked,could not find any hard info on what the parnate metabolite is,only that parnate holds a 2.5 half life,my thinking is can we look at using the metabolite as a med as other drugs have done since we see how it acts so strongly.
Hope this makes sense thanks.
Posted by bulldog2 on August 31, 2009, at 14:46:53
In reply to Parnate technical, posted by willyeee on August 31, 2009, at 14:18:21
> This is a tiny bit technical.ok some meds have there metabolites made into a med themselves.Its been argued that parnates metabolite is that close to a amphetamine,which makes sense since a metabolite shows up when the drug is leaving hence the insomia.Also however with the insomnia i notice my mood does actualy improve,just to damn late for any of this.
>
> So to make this short,i i looked and looked,could not find any hard info on what the parnate metabolite is,only that parnate holds a 2.5 half life,my thinking is can we look at using the metabolite as a med as other drugs have done since we see how it acts so strongly.
>
> Hope this makes sense thanks.Yes I noticed a ritalin like feeling after each parnate dose.This feeling lasted a couple of hours and was actually quite nice.
I was on parnate for eight weeks and had brought up the dose to 60 mg. After each dose increase I felt well for a few days and that would subside.I went up to 60 mg and was on that for maybe 10 days to two weeks. After that I stopped because my p-doc and I had decided on 60 mg as a top dose.
I think aborting my trial may have been premature.I may retry the med. Maybe add nortriptyline. also possibly go higher than 60 mg.also once I get to a therapeutic range stay at least three weeks at that range before I move up.
Posted by SLS on August 31, 2009, at 15:42:46
In reply to Parnate technical, posted by willyeee on August 31, 2009, at 14:18:21
> This is a tiny bit technical.ok some meds have there metabolites made into a med themselves.Its been argued that parnates metabolite is that close to a amphetamine,which makes sense since a metabolite shows up when the drug is leaving hence the insomia.Also however with the insomnia i notice my mood does actualy improve,just to damn late for any of this.
>
> So to make this short,i i looked and looked,could not find any hard info on what the parnate metabolite is,only that parnate holds a 2.5 half life,my thinking is can we look at using the metabolite as a med as other drugs have done since we see how it acts so strongly.
>
> Hope this makes sense thanks.Post-mortem studies of Parnate overdose victims have not tested positive for amphetamine or metabolites.
- Scott
*************************************************81: J Anal Toxicol. 1996 Sep;20(5):301-4.Links
One fatal and one nonfatal intoxication with tranylcypromine. Absence of amphetamines as metabolites.
Iwersen S, Schmoldt A.Department of Legal Medicine, University of Hamburg, Germany.
Two very different cases of overdose with tranylcypromine are presented. One clinical case involving the ingestion of 400 mg tranylcypromine with suicidal intention and one fatality with a suspicion of possible tranylcypromine overdose were examined. Both cases showed similar blood concentrations (0.5 and 0.7 mg/L, respectively), but the clinical case exhibited only mild symptoms of intoxication. The fatality showed no other drugs that could provide an explanation for the death of a 40-year-old male except tranylcypromine. Consideration of the drug concentrations in the fatality in relation to the case findings and other reported data indicates the tranylcypromine overdose as the probable cause of death, despite the low blood concentration. In addition, we looked for evidence of amphetamine as a putative metabolite in both cases. No amphetamines were detected in the overdose cases reported here.
Posted by SLS on August 31, 2009, at 15:49:33
In reply to Re: Parnate technical, posted by SLS on August 31, 2009, at 15:42:46
More:
http://cat.inist.fr/?aModele=afficheN&cpsidt=823081
Titre du document / Document title
Failure to detect amphetamine or 1-amino-3-phenlypropane in humans or rats receiving the MAO inhibitor tranylcypromine
Auteur(s) / Author(s)
SHERRY R. L (1) ; RAUW G. (1) ; MCKENNA K. F. (1) ; PAETSCH P. R. (1) ; COUTTS R. T. (1) ; BAKER G. B. (1) ;
Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)
(1) Neurochemical Research Unit, Department of Psychiatry, University of Alberta, Edmonton, AB, T6G 2R7, CANADA
Résumé / Abstract
Background: There have been conflicting reports in the literature about whether or not tranylcypromine is metabolized to amphetamine. In the current report, we investigated this possible route of metabolism in both rats and humans. Body fluid samples from patients and rats and brain, liver and heart samples from rats were analyzed for levels of amphetamine and 1-amino-3-phenylpropane, another potential product of cleavage of the cyclopropyl ring of tranylcypromine after administration of tranylcypromine. Extracted samples were reacted with pentofluorobenzenesulfonyl chloride and analyzed using electron-capture gas chromatography. Results: Amphetamine or 1-amino-3-phenylpropane were not found in any of the samples, indicating that opening of the cyclopropyl ring of tranylcypromine is not a significant route of metabolism for this drug at usual doses. Limitations: The assay procedure did not permit analysis of 1-amino-2-phenylpropane (another possible product of cleavage of the cyclopropyl ring of tranylcypromine) or of N-methylamphetamine. Conclusions: These studies support the growing body of evidence indicating that opening of the cyclopropyl ring of tranylcypromine to form amphetamine, a drug of abuse, is not significant at usual doses of tranylcypromine.
Revue / Journal Title
Journal of affective disorders ISSN 0165-0327 CODEN JADID7
Posted by SLS on August 31, 2009, at 15:53:28
In reply to Re: Parnate technical, posted by SLS on August 31, 2009, at 15:49:33
The Parnate (tranylcypromine) molecule itself acts like amphetamine in that it produces an increased release of norepinephrine and possibly an inhibition of reuptake:
Am J Psychiatry 126:925-931, January 1970
doi: 10.1176/appi.ajp.126.7.925
© 1970 American Psychiatric AssociationTranylcypromine: Effects on Norepinephrine Metabolism in Rat Brain
JOSEPH J. SCHILDKRAUT M.D.11 Neuropsychopharmacology laboratory, Massachusetts Mental Health Center, 74 Fenwood Rd., Boston, Mass. 02115, assistant professor of psychiatry, Harvard Medical School
This investigation examines the effects of tranylcypromine on the uptake, release, and metabolism of intracisternally administered tritiated norepinephrine (norepinephrine-H3) in rat brain. The findings suggest that, in addition to being a potent inhibitor of the enzyme monoamine oxidase, tranylcypromine discharges norepinephrine extraneuronally onto receptors and possibly also inhibits the neuronal reuptake of this amine. These neuropharmacological effects of tranylcypromine may possibly account for the greater clinical efficacy of tranylcypromine in the treatment of some depressed patients and the higher incidence of hypertensive cerebrovascular reactions when this drug is compared with other monoamine oxidase inhibitors.
Posted by linkadge on August 31, 2009, at 16:53:45
In reply to Re: Parnate technical, posted by SLS on August 31, 2009, at 15:53:28
I wonder if parante also increases the release of dopamine. I havn't taken nardil so I can't compare, but parnate can definately produce a transient buzz upon initial administration.
Insomnia is a common effect of monoamine oxidase inhibitors. In animal models too MAO inhibitors can produce dramatic shifts in the circadian rythem.
Linkadge
Posted by Maxime on August 31, 2009, at 16:55:09
In reply to Re: Parnate technical, posted by SLS on August 31, 2009, at 15:42:46
I once overdosed on over 400mg of Parnate and I went totally psychotic. I was found on the street trying to chew my arm off. Not one of my best moments. I even ate a lot of forbidden food with the overdose. I am still here to talk about it. It didn't feel like an amphetamine to me at that dosage.
Posted by Phillipa on August 31, 2009, at 16:59:38
In reply to Re: Parnate technical » SLS, posted by Maxime on August 31, 2009, at 16:55:09
Maxie that's horrible thankfully you survived. Phillipa
Posted by Maxime on August 31, 2009, at 18:18:59
In reply to Re: Parnate technical » Maxime, posted by Phillipa on August 31, 2009, at 16:59:38
> Maxie that's horrible thankfully you survived. Phillipa
Actually it is. I just recalculated how much I took and it was 4800 mg! It was two months worth at 80mg a day. I am surprised that I didn't have a stroke!
Posted by viper1431 on September 1, 2009, at 1:05:03
In reply to Parnate technical, posted by willyeee on August 31, 2009, at 14:18:21
Parnate puts me to sleep, it was a great sleeping pill, better than benzos. Certainly didn't feel any amphetamine like feeling.
Posted by katamnesis on September 2, 2009, at 8:44:36
In reply to Parnate technical, posted by willyeee on August 31, 2009, at 14:18:21
I remember you! This is tygereyes/halcyondaze, the other high dose Parnate responder.
Parnate is a racemic mix of + and - tranylcypromine isomers. One is involved in neurotransmitter release/reuptake and the other in MAO inhibition. They were evaluated as separate ADs in clinical trials decades ago with the release/reuptake isomer exhibiting positive results but nothing ever came of it, unfortunately.
Posted by willyeee on September 3, 2009, at 16:15:10
In reply to Parnate is racemic, posted by katamnesis on September 2, 2009, at 8:44:36
> I remember you! This is tygereyes/halcyondaze, the other high dose Parnate responder.
>
> Parnate is a racemic mix of + and - tranylcypromine isomers. One is involved in neurotransmitter release/reuptake and the other in MAO inhibition. They were evaluated as separate ADs in clinical trials decades ago with the release/reuptake isomer exhibiting positive results but nothing ever came of it, unfortunately.Sounds familiar i read this clip,thanks for sharing
Posted by djmmm on September 4, 2009, at 18:41:26
In reply to Parnate technical, posted by willyeee on August 31, 2009, at 14:18:21
some additional info on Parnate
Insights into the mechanisms of action of the MAO inhibitors phenelzine and tranylcypromine: a review.
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=1188458Monoamine Oxidase: Basic and Clinical Perspectives
http://www.acnp.org/g4/GN401000046/CH046.htmlMetabolism of Tranylcypromine-C14 and dl-Amphetamine-C14 in the Rat
http://pubs.acs.org/doi/abs/10.1021/jm00342a001also, I believe the metabolites of tranylcypromine are N-acetytranylcypromine, and hydroxylated N-acetyltranylcypromine
Posted by willyeee on September 6, 2009, at 15:13:43
In reply to Re: Parnate technical, posted by djmmm on September 4, 2009, at 18:41:26
.....and just when you think you know how to find everything on the net,...great articles lots of good precise reading thanks!!!!
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