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Cyclazodone
Revision as of 18:22, 1 March 2024 by >Scrumptious(Added some additional information, and updated wording!)
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Cyclazodone was developed by the American Cyanamid Company in the 1960s for use as an appetite suppressant and an antidepressant. Its non-clinical use has only found recent attention as a research chemical study aid. The lack of pharmacological data and limited human usage history raise concerns about its long-term use as a stimulant substitute.
Cyclazodone had no documented history of recreational human usage prior to its appearance on the online research chemical market in 2017. However, discussions about it on various forums date back as early as 2002[1]. Concerns persist about potential hepatotoxic and other yet-to-be-discovered toxic properties, but there have been no reported cases of hepatotoxicity attributed to cyclazodone thus far.
Cyclazodone is a phenyl 4-oxazolidinone that differs from the parent pemoline by an N-cyclopropyl group. Compounds like cyclazodone of the 4-oxazolidinone class can be considered as 4-oxy derivatives of the 2-amino-5-aryloxazoline class including aminorex, fluminorex, and 4-methylaminorex, conformationally restricted analogues of phenethylamines and amphetamines.
Cyclazodone is structurally most closely related, not to pemoline, but rather to two N-substituted derivatives of pemoline — fenozolone (N-ethyl pemoline) and thozalinone (N,N-dimethyl pemoline).
Pharmacology
Cyclazodone is a more potent N-cyclopropyl derivative of pemoline. Pemoline is considered to be dopaminergic, yet its precise mechanism of action remained elusive during its market presence.[2]
Pemoline's mild sympathomimetic side effects and weaker anorectic effects suggest limited affinity for noradrenaline and potentially serotonin receptors compared to other central nervous system stimulants. This characteristic appears to be shared with cyclazodone, as demonstrated by the limited sympathomimetic effects observed in dogs following administration, , evidenced by limited sympathomimetic effects observed in dogs following administration.
According to the patent filed by the inventors, cyclazodone demonstrated significant central nervous system stimulation and antidepressant properties, and relative potency greater than both pemoline and various other N-lower-alkyl-substituted pemoline derivatives. At the time cyclazodone also offered a much more favorable therapeutic index and margin of safety than pemoline and other N-lower-alkyl-substituted pemoline derivatives.[3]
In animal models, cyclazodone exhibits central nervous system stimulant and antidepressant efficacy and potency at least equal to that of dextro-amphetamine. The duration of maximum activity spanned 180 minutes, and the total duration of excitation was in excess of 6 hours.[3] Furthermore, according to the inventor's patents, cyclazodone also possessed anorexic efficacy and potency at least equal to that of dextro-amphetamine in animal models, yet the toxicity of cyclazodone was found to be low in comparison with the activity thereof.[3]
The related compound N-Methyl-Cyclazodone seems to function as a pro-drug for cyclazodone, leading to the presence of significant amounts of cyclazodone in urine after consumption.[4]
The stimulant effects of cyclazodone have been compared to those of amphetamine, but with the addition of a low to moderate affinity for serotonin release comparable to that of methamphetamine and 3-FMA. Additionally, it is noticeably less euphoric than amphetamine and appears to have less sympathomimetic activation.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical euphoria - This effect is dose dependent and tends only to be present at higher doses. Cyclazodone is reported to lack the body glow associated with amphetamine at typical doses.
The visual effects of cyclazodone are usually less consistent and only mildly noticeable at higher dosages. They may manifest as a brightening of colors and areas of light appearing brighter than that of their surrounding.
Distortions
Drifting(breathing and morphing) - This effect is usually subtle and barely noticeable and only occurs at higher dosages or when combined with cannabis.
Brightness alteration - Cyclazodone can make spaces seem brighter as a result of its pupil dilating effects.
Hallucinatory states
Transformations - This effect occurs very rarely, and typically only when the user has taken high doses, is coming down, or has been awake for unusually long periods. It is usually very mild when it does occur.
Anxiety & Paranoia - This effect is dose dependent and typically occurs with overly high doses or after redosing and staying awake for extended periods of time.
Anxiety suppression - Common to moderately high doses, when used infrequently, will tend to result in a complete loss of all anxiety symptoms.
Cognitive euphoria - This effect is dose dependent; a low dose will tend to produce only that of a slight mood lift and moderate to high doses are typically reported to be on par with that of amphetamine though less than that of methamphetamine, 3-FMA, and 4-methylaminorex. It is the strongest when used infrequently at moderate doses, and binges often result in a loss of this effect.
Empathy, affection, and sociability enhancement - Cyclazodone has been reported to produce moderately strong prosocial and entactogenic effects which, although much weaker than that of traditional entactogens such as MDMA, surpass that of amphetamine. As with most amphetamine-like stimulants, this effect rapidly fades with prolonged use.
Ego inflation - Cyclazodone, at moderate doses, has been reported to substantially increase confidence and self-esteem. Higher doses, however, can result in complete self-absorption and ego mania.
Time distortion - This can be described as the experience of time speeding up and passing much quicker than it usually would when sober.
After effects
The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. Its effects commonly include:
There are currently 0 experience reports which describe the effects of this substance in our experience index.
Toxicity and harm potential
The long-term health effects of recreational cyclazodone use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because cyclazodone has a very limited history of human usage.
One adult presented with moderate intoxication after the consumption of 5,000 mg of N-Methyl-Cyclazodone over the course of five days. N-Methyl-Cyclazodone appears to act as a pro-drug for cyclazodone, with detectable levels found in urine, as detailed in the same toxicological report. [4]
Another structurally related compound, 4-methylaminorex, is associated with pulmonary hypertension[8]; though, it is reported to induce far stronger stimulation than that of cyclazodone.
The structurally related compound pemoline was withdrawn from the market in 2005 due to concerns about its potential to cause spontaneous serious liver damage in children.[9]
In rodents and primates, sufficiently high doses of monoamine releasing agents cause dopaminergic neurotoxicity, or damage to dopamine neurons, which is characterized by reduced transporter and receptor function. There is no evidence that releasing agents are directly neurotoxic in humans. However, large doses of releasing agents may cause indirect neurotoxicity as a result of increased oxidative stress from reactive oxygen species and autoxidation of dopamine.[citation needed]
Cyclazodone has demonstrated LD50 values of 81 mg/kg (intraperitoneal) and 142 mg/kg (subcutaneous) in rats.
Addiction is a serious risk with heavy recreational stimulant use but is unlikely to arise from typical long-term medical use at therapeutic doses. Notably, the structurally related compound pemoline fails to demonstrate a potential for self-administration in primates and is considered to have reduced risk of dependence relative to those more typical dopaminergic stimulants. Caution is nonetheless advised, as with other monoamine releasing agents.
Tolerance to many of the effects of cyclazodone tends to develop with prolonged or repeated use::develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Cyclazodone presents cross-tolerance with [[Cross-tolerance::all dopaminergicstimulants]], meaning that after the consumption of cyclazodone all stimulants may have a reduced effect.
Based on its pharmacological similarity to other stimulants, it is likely that misuse of this compound can result in state of psychosis marked by a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[10][11] A review on the treatment for amphetamine and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[11][12] The same review asserts that based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[11] Psychosis very rarely arises from therapeutic use. The combination of the prolonged use of high doses combined with sleep deprivation significantly increases the risk of stimulant psychosis.[citation needed]
Dangerous interactions
Warning:Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).
Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
"[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] & "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 25x compounds are highly stimulating and physically straining. Combinations with Cyclazodone should be strictly avoided due to the risk of excessive stimulation and heart strain. This can result in increased blood pressure, vasoconstriction, panic attacks, thought loops, seizures, and heart failure in extreme cases.
"[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Combining alcohol with stimulants can be dangerous due to the risk of accidental over-intoxication. Stimulants mask alcohol's depressant effects, which is what most people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects will be left unopposed, which can result in blackouts and severe respiratory depression. If mixing, the user should strictly limit themselves to only drinking a certain amount of alcohol per hour.
"[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Combinations with DXM should be avoided due to its inhibiting effects on serotonin and norepinephrine reuptake. There is an increased risk of panic attacks and hypertensive crisis, or serotonin syndrome with serotonin releasers (MDMA, methylone, mephedrone, etc.). Monitor blood pressure carefully and avoid strenuous physical activity.
"[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Any neurotoxic effects of MDMA are likely to be increased when other stimulants are present. There is also a risk of excessive blood pressure and heart strain (cardiotoxicity).
"[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Some reports suggest combinations with MXE may dangerously increase blood pressure and increase the risk of mania and psychosis.
"[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Both classes carry a risk of delusions, mania and psychosis, and these risk may be multiplied when combined.
"[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Cyclazodone may be dangerous to combine with other stimulants like cocaine as they can increase one's heart rate and blood pressure to dangerous levels.
"[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Tramadol is known to lower the seizure threshold[13] and combinations with stimulants may further increase this risk.
Legal status
Cyclazodone is currently a gray area compound within all parts of the world, meaning its regulation lies in a legal gray area and that it is not known to be specifically illegal ("scheduled") within any country. However, people may still be charged for its possession under certain circumstances such as under analogue laws and with intent to sell or consume. It is a banned stimulant under the World Anti-Doping Agency prohibited list.
Germany: Cyclazodone is not a controlled substance under the BtMG (Narcotics Act)[14] or the NpSG (New Psychoactive Substances Act).[15] According to §2 AMG (Medicines Act) it would fall under the definition of a medicine because it induces pharmacological effect.[16] By a decision of the European Court of Justice, this definition was declared ineffective because it was not compatible with EU law.[17] Cyclazodone can be considered legal.
Switzerland: Cyclazodone is not controlled under Buchstabe A, B, C and D. It could be considered legal.[18]
United States: Cyclazodone being an analogue of pemoline, a Schedule IV controlled substance in the US, may fall under Federal Analogue Act, 21 U.S.C. § 813[19] when intended for human consumption.
Sweden: Cyclazodone is not a classified or controlled substance in Sweden. However, the related compound N-Methyl-Cyclazodone was subject to investigation in Sweden in 2018. Despite this, authorities chose not to proceed with classification, ultimately resulting in the discontinuation of the investigation, and it has remained legal. [20]
Segal, D. S., Cox Jr, R. H., Stern, W. C., & Maickel, R. P. (1967). Stimulatory effects of pemoline and cyclopropylpemoline on continuous avoidance behavior: similarity to effects of D-amphetamine. Life Sciences, 6(23), 2567-2572. https://doi.org/10.1016/0024-3205(67)90322-0
↑Gaine, S. P., Rubin, L. J., Kmetzo, J. J., Palevsky, H. I., Traill, T. A. (November 2000). "Recreational use of aminorex and pulmonary hypertension". Chest. 118 (5): 1496–1497. doi:10.1378/chest.118.5.1496. ISSN0012-3692.
↑Hofmann, F. G. (1983). A handbook on drug and alcohol abuse: the biomedical aspects (2nd ed ed.). Oxford University Press. ISBN9780195030563.CS1 maint: Extra text (link)
↑Talaie, H.; Panahandeh, R.; Fayaznouri, M. R.; Asadi, Z.; Abdollahi, M. (2009). "Dose-independent occurrence of seizure with tramadol". Journal of Medical Toxicology. 5 (2): 63–67. doi:10.1007/BF03161089. eISSN1937-6995. ISSN1556-9039. OCLC163567183.
