SpunkySkunk347
Bluelighter
- Joined
- Jan 15, 2006
- Messages
- 1,717
OP: "Anyone had any experiences with this stuff?
It's a direct 5-HT2 antagonist with anti-depressant and sedative effects.
I love it. I was given a trial of it and actually requested it over benzos, I would say it almost feels like sedating MDMA.
You constantly laugh at anything and everything. All anxiety diminshes and you are left with a simple yet satisfying euphoria.
I made a short list of effects I've noticed.
Positive:
-Light Euphoria
-Anxiolytic
-Sedating
-Mood Lift and Uncontrollable Laughter
Neutral:
-Loss of Motor Skills
-Increased feeling of gravity (feels like your limbs are being pulled down to the ground)
-Visual Distortions
Negative:
-Headache
-Possibility of Priapism (a never ending erection that requires going to a hospital to reverse)
-Nausea
-Dizzyness
-Delerious mind-set (aural hallucinations, not fun)
-Overwhelming feeling of uncontrollable sedation (not comparable to anything else I've ever tried, although slightly similar to the "overwhelming" feeling you get from DXM.)
-Amnesia"
___________________________________________
Pharmacokinetic data
Bioavailability
By mouth: 65%
Protein binding
89–95%
Metabolism
Liver (CYP3A4, CYP2D6, CYP1A2?)
Metabolites
mCPP
Onset of action
By mouth: 1 hour (Tmax)
Elimination half-life
• Trazodone (IR): 4–15 hours
• Trazodone (ER): 9–13 hours
• mCPP: 3–16 hours
Excretion
Urine: 70–75%
Feces: 21%
Identifiers
IUPAC name
2-{3-[4-(3-Chlorophenyl)piperazin-1-yl]propyl}[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one
Pharmacology
Trazodone is a mixed agonist and antagonist of various serotonin receptors, antagonist of adrenergic receptors, weak histamine H1 receptor antagonist, and weak serotonin reuptake inhibitor. More specifically, it is an antagonist of 5-HT2A and 5-HT2B receptors, a partial agonist of the 5-HT1A receptor, and an antagonist of the α1- and α2-adrenergic receptors. It is also a ligand of the 5-HT2C receptor with lower affinity than for the 5-HT2A receptor. However, it is unknown whether trazodone acts as a full agonist, partial agonist, or antagonist of the 5-HT2C receptor. Trazodone is a 5-HT1A receptor partial agonist similarly to buspirone and tandospirone but with comparatively greater intrinsic activity. A range of weak affinities (Ki) have been reported for trazodone at the human histamine H1 receptor, including 220 nM, 350 nM, 500 nM, and 1,100 nM.
Priapism Warning!!!!
A relatively rare side effect associated with trazodone is priapism, likely due to its antagonism at α-adrenergic receptors. More than 200 cases have been reported, and the manufacturer estimated that the incidence of any abnormal erectile function is about one in 6,000 male patients treated with trazodone. The risk for this side effect appears to be greatest during the first month of treatment at low dosages (i.e. <150 mg/day). Early recognition of any abnormal erectile function is important, including prolonged or inappropriate erections, and should prompt discontinuation of trazodone treatment. Spontaneous orgasms have also been reported with trazodone in men.
Clinical reports have described trazodone-associated psychosexual side effects in women as well, including increased libido, priapism of the clitoris, and spontaneous orgasms.
- @deficiT
It's a direct 5-HT2 antagonist with anti-depressant and sedative effects.
I love it. I was given a trial of it and actually requested it over benzos, I would say it almost feels like sedating MDMA.
You constantly laugh at anything and everything. All anxiety diminshes and you are left with a simple yet satisfying euphoria.
I made a short list of effects I've noticed.
Positive:
-Light Euphoria
-Anxiolytic
-Sedating
-Mood Lift and Uncontrollable Laughter
Neutral:
-Loss of Motor Skills
-Increased feeling of gravity (feels like your limbs are being pulled down to the ground)
-Visual Distortions
Negative:
-Headache
-Possibility of Priapism (a never ending erection that requires going to a hospital to reverse)
-Nausea
-Dizzyness
-Delerious mind-set (aural hallucinations, not fun)
-Overwhelming feeling of uncontrollable sedation (not comparable to anything else I've ever tried, although slightly similar to the "overwhelming" feeling you get from DXM.)
-Amnesia"
___________________________________________
Pharmacokinetic data
Bioavailability
By mouth: 65%
Protein binding
89–95%
Metabolism
Liver (CYP3A4, CYP2D6, CYP1A2?)
Metabolites
mCPP
Onset of action
By mouth: 1 hour (Tmax)
Elimination half-life
• Trazodone (IR): 4–15 hours
• Trazodone (ER): 9–13 hours
• mCPP: 3–16 hours
Excretion
Urine: 70–75%
Feces: 21%
Identifiers
IUPAC name
2-{3-[4-(3-Chlorophenyl)piperazin-1-yl]propyl}[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one
Pharmacology
Trazodone is a mixed agonist and antagonist of various serotonin receptors, antagonist of adrenergic receptors, weak histamine H1 receptor antagonist, and weak serotonin reuptake inhibitor. More specifically, it is an antagonist of 5-HT2A and 5-HT2B receptors, a partial agonist of the 5-HT1A receptor, and an antagonist of the α1- and α2-adrenergic receptors. It is also a ligand of the 5-HT2C receptor with lower affinity than for the 5-HT2A receptor. However, it is unknown whether trazodone acts as a full agonist, partial agonist, or antagonist of the 5-HT2C receptor. Trazodone is a 5-HT1A receptor partial agonist similarly to buspirone and tandospirone but with comparatively greater intrinsic activity. A range of weak affinities (Ki) have been reported for trazodone at the human histamine H1 receptor, including 220 nM, 350 nM, 500 nM, and 1,100 nM.
Priapism Warning!!!!
A relatively rare side effect associated with trazodone is priapism, likely due to its antagonism at α-adrenergic receptors. More than 200 cases have been reported, and the manufacturer estimated that the incidence of any abnormal erectile function is about one in 6,000 male patients treated with trazodone. The risk for this side effect appears to be greatest during the first month of treatment at low dosages (i.e. <150 mg/day). Early recognition of any abnormal erectile function is important, including prolonged or inappropriate erections, and should prompt discontinuation of trazodone treatment. Spontaneous orgasms have also been reported with trazodone in men.
Clinical reports have described trazodone-associated psychosexual side effects in women as well, including increased libido, priapism of the clitoris, and spontaneous orgasms.
- @deficiT
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