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Desyrel (Trazodone)

splenda

Bluelighter
Joined
Jun 18, 2005
Messages
651
Anyone tried this for sleep and sleep only (trying to negate the 5-HT2a effects/5-HT effects in general?)

More interestingly... I'm interested in how Trazodone metabolises in vivo into mCPP. Anyone have experience also with how the long-half life affects the next day/etc.?

I noticed last night that although it doesn't knock me out, 50mg causes some sedation that helps to ease into sleep... although I slept for 7 hours and didn't wake up sedated, I did feel a bit drowsy earlier today (a transient drowsiness though.)

Also I'm wondering, since trazodone has minor norepinephrine uptake inhibitory properties, how this would negatively affect cardiovascular function?

This is a bout of insomnia induced by stress and lots of me being "on the run" busy these days helping family and friends. Possibly anxiety related, although I'm trying to stay away from sedative/hypnotics or benzodiazepines for sleep. I don't want to/plan to take trazodone for an extended period of time. Melatonin and melatonin-agonists (Rozerem) makes me depressed the next day, even at a .25mg dose of melatonin, so that's out of the picture.

Side effects so far today from the Trazodone:
Minor agitation
Minor dysthimia
Slight increase in stress (but this could be due to my current state of stress.)
Reduced anxiety/strong anxiolysis (but not a "pleasant" anxiolysis like say benzodiazepines would cause)
Slight cognitive slowness/psychomotor retardation
--

DESYREL (trazodone hydrochloride) is an antidepressant chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. Trazodone hydrochloride is a triazolopyridine derivative designated as 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one hydrochloride. It is a white odorless crystalline powder which is freely soluble in water. Its molecular weight is 408.3. The empirical formula is C19H22ClN5O • HCl

CLINICAL PHARMACOLOGY

The mechanism of DESYREL’s antidepressant action in man is not fully understood. In animals, DESYREL selectively inhibits serotonin uptake by brain synaptosomes and potentiates the behavioral changes induced by the serotonin precursor, 5-hydroxytryptophan. Cardiac conduction effects of DESYREL in the anesthetized dog are qualitatively dissimilar and quantitatively less pronounced than those seen with tricyclic antidepressants. DESYREL is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system.
--

Anyone have a bigger idea on trazodone's pharmacology?
 
I took trazodone a few times; the last time resulted in a priapism. This was, well, very unpleasant.

Avoid this drug if possible. As mentioned, the priapism did not occur the first few times, so exercise caution...
 
side effects are aweful on this...next day dry mouth...almost hangover effects...stick to somethin like amiltriplimine...(sp)
 
I personally did not feel any side effects at 50 mg, then again Trazadone was nowhere near as effective as 2 mg Xanax. :\

Both meds used for sleep (the Xanax of course had a pleasant euphoric effect as well).
 
I once took trazodone, forgot what dose, and it made me sleep ok. It was less effective in inducing sleep than Amitryptilin, which itself is less effective than gabaergics. You do the math ;).

Of note though, is that I woke up feeling VERY good.
 
trazodone is also a quite strong alpha1-adrenoceptor-antagonist (or rather thats its main target), which explains its sedative effects.
 
well, i've extracted the ki-values of trazodone from pdsp now.
they are (in descending order):
alpha1: ~30nM
5-ht2a: ~40nM
5-ht2b: ~80nM
5-ht1a: ~100nM
alpha2: ~200nM
5-ht2c: ~230nM
5-ht-uptake-transporter: ~250nM

all other values are in the micromolar range.

maybe that helps you @threadstarter :)
 
I was up to 400mgs a night, but after a few months it stoped working as a sleep aid. It wasent a very good one to begin with. I didnt feel any side affects at all really.
 
splenda said:
Anyone tried this for sleep and sleep only (trying to negate the 5-HT2a effects/5-HT effects in general?)

More interestingly... I'm interested in how Trazodone metabolises in vivo into mCPP. Anyone have experience also with how the long-half life affects the next day/etc.?

I noticed last night that although it doesn't knock me out, 50mg causes some sedation that helps to ease into sleep... although I slept for 7 hours and didn't wake up sedated, I did feel a bit drowsy earlier today (a transient drowsiness though.)

Also I'm wondering, since trazodone has minor norepinephrine uptake inhibitory properties, how this would negatively affect cardiovascular function?

This is a bout of insomnia induced by stress and lots of me being "on the run" busy these days helping family and friends. Possibly anxiety related, although I'm trying to stay away from sedative/hypnotics or benzodiazepines for sleep. I don't want to/plan to take trazodone for an extended period of time. Melatonin and melatonin-agonists (Rozerem) makes me depressed the next day, even at a .25mg dose of melatonin, so that's out of the picture.

Side effects so far today from the Trazodone:
Minor agitation
Minor dysthimia
Slight increase in stress (but this could be due to my current state of stress.)
Reduced anxiety/strong anxiolysis (but not a "pleasant" anxiolysis like say benzodiazepines would cause)
Slight cognitive slowness/psychomotor retardation
--

DESYREL (trazodone hydrochloride) is an antidepressant chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. Trazodone hydrochloride is a triazolopyridine derivative designated as 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one hydrochloride. It is a white odorless crystalline powder which is freely soluble in water. Its molecular weight is 408.3. The empirical formula is C19H22ClN5O • HCl

CLINICAL PHARMACOLOGY

The mechanism of DESYREL’s antidepressant action in man is not fully understood. In animals, DESYREL selectively inhibits serotonin uptake by brain synaptosomes and potentiates the behavioral changes induced by the serotonin precursor, 5-hydroxytryptophan. Cardiac conduction effects of DESYREL in the anesthetized dog are qualitatively dissimilar and quantitatively less pronounced than those seen with tricyclic antidepressants. DESYREL is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system.
--

Anyone have a bigger idea on trazodone's pharmacology?

Don't know heavy chemistry but I can tell you that I took Desyrel and it had sedative effects which I did not care for in the least. No other noticiable side effects. But I will not take a psych drug with sedative effects. The methadone is more than sufficient for sleep.8)
 
splenda: a dose of st. john's wort in the morning after will induce CYP3A4 and speed excretion of the trazodone, which will help with hangover. It works for a few people I've talked to, to the point of eliminating symptoms entirely, though obviously taking SJW can come with its own considerations.
 
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