Mirtazapine

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Summary sheet: Mirtazapine
Mirtazapine
Mirtazapine.svg
Chemical Nomenclature
Common names Avanza, Axit, Mirtaz, Mirtazon, Remeron, Zispin
Substitutive name Mirtazapine
Systematic name (±)-2-Methyl-1,2,3,4,10,14b-hexahydropyrazino[2,1-a]pyrido[2,3-c][2]benzazepine
Class Membership
Psychoactive class Deliriant / Depressant
Chemical class Piperazinoazepine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Bioavailability 50%[1]
Threshold 3.5 mg
Light 70 - 130 mg
Common 130 - 190 mg
Strong 190 - 250 mg
Heavy 250 mg +
Duration
Total 14 - 24 hours
Onset 15 - 30 minutes
Peak 90 - 180 minutes
Offset 2 - 6 hours
After effects up to 24 hours









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.

Interactions
Antidepressants

Mirtazapine (trade name Remeron, among others) is an antidepressant substance of the piperazinoazepine class. At high doses, it has been reported to act as an atypical psychedelic and sedative. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).[citation needed]

Mirtazapine was developed in the Netherlands and introduced in the United States in 1996.[2] Its patent expired in 2004 and generic versions have been widely available since.[3] It is used primarily in the treatment of major depressive disorder and other mood disorders.[4][5] It has also been prescribed off-label for the treatment of generalized anxiety disorder,[6] social anxiety disorder,[7][8] obsessive-compulsive disorder,[7][9] panic disorder,[7][10] post-traumatic stress disorder,[7] low appetite,[11][12][13] insomnia,[14][15] nausea/vomiting,[16][17][18] itching,[19][20] and headaches and migraines.[17][21][22]

Higher doses of mirtazapine (that exceed the recommended prescription dose) are reported to produce an unusual mixture of psychedelic and sedative effects. Subjective effects include sedation and mild-moderate versions of open and closed-eye visuals, conceptual thinking, and euphoria. Mirtazapines has potential paradoxical effects concerning it's sedative effects. Anecdotal reports and studies suggest it's Sedation decreases as the dose increases. (7.5mg is more sedating than 15mg.) One theory suggests it has minor Stimulant effects that overpowers it's sedative effects.[citation needed]

The toxicity and health risks of recreational mirtazapine use is not known. It is highly advised to use harm reduction practices if using this substance.

Chemistry

Mirtazapine is a synthetic tetrahedral molecule of the piperazino-azepine and phenethylamine group of compounds. It is comprised of a fusion of pyridine, benzene, azepine, and piperazine rings. It is a tetracyclic antidepressant, named so because of their four-ring structure. Mirtazapine is the 6-aza analog of mianserin, which is pharmacologically similar in function.

Mirtazapine enhances central adrenergic and serotonergic transmission, possibly by acting as an antagonist at central presynaptic alpha 2 adrenergic inhibitory autoreceptors and heteroreceptors. This agent is a potent antagonist of 5-hydroxytryptamine type 2 (5-HT2), 5-HT3, and histamine 1 (H1) receptors, and a moderate antagonist of peripheral alpha 1 adrenergic and muscarinic receptors.[23]

Pharmacology

Mirtazapine acts as an antagonist/inverse agonist upon the following receptors:[24][25]

While mirtazapine has some affinity for the 5-HT2A receptor, it acts as an antagonist[6] thus it is unlikely that this mechanism is responsible for its psychedelic and deliriant effects.

Additionally, Mirtazapine has also been observed to indirectly agonize the following GCPR in humans:

Mirtazapine has also been found to modulate the κ3 opioid receptor, supporting the claim that mirtazapine causes pain relief[32] and adds to the sedative and hallucinogenic effects of mirtazapine[33][34]. This even may explain mirtazapine's withdrawal/discontinuation effects as well as its promotion of diuresis and a possible increase in food intake (usually resulting in weight gain).

It should be noted that although some of these effects are observed in those who take mirtazapine recreationally (or one off dosing) most neurophysiological effects are observed in those with on-going use (15, 30 and 45 mg daily prescribed for depression, etc) due to a maintained level of mirtazapine in the body.

The oral bioavailability of mirtazapine is about 50%. It is found mostly bound to plasma proteins, about 85%. It is metabolized primarily in the liver by demethylation and hydroxylation via cytochrome P450 enzymes, CYP1A2, CYP2D6, CYP3A4.[6] One of its major metabolites is desmethylmirtazapine. The overall elimination half-life is 20–40 hours. It is conjugated in the kidney for excretion in the urine, where 75% of the drug is excreted,[35] and about 15% is eliminated in feces.[36]

Subjective effects

Although mirtazapine exhibits almost exclusively psychedelic effects, the hallucinations that accompany it do have distinctively deliriant-like effects. For example, they are often delirious in their believability and rarely comprised of condensed visual geometry. Instead they tend to be solid and extremely realistic in appearance.

The mental processes, thought patterns and general head space experienced during a high dose mirtazapine experience is one that is typically described to be completely devoid of insight. In contrast to many other substances with hallucinogenic properties, it produces no introspection, personal problem solving or creativity enhancing effects; for this reason it is generally reported that mirtazapine holds no therapeutic potential when used as a hallucinogen.

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 PsychonautWiki contributors. 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 effects
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Cognitive effects
User.svg

Visual effects
Eye.svg


Combination effects

  • Cannabis - When mirtazapine is combined with cannabis, the euphoric and visual effects are greatly potentiated.
  • Psychedelics - Due to mirtazapines action as a 5-HT2A antagonist, it can help reduce the intensity or "abort" a bad trip

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

Additional experience reports can be found here:

Toxicity and harm potential

This document, provided with prescription mirtazapine, contains detailed information regrading its toxicity and harm potential.

Mirtazapine is not known to cause brain damage, and has extremely low toxicity relative to dose. Similar to other psychedelic drugs, there are relatively few physical side effects associated with mirtazapine exposure. Various studies have shown that in reasonable doses in a careful context, it presents no negative cognitive, psychiatric or toxic physical consequences of any sort.

Dependence and abuse potential

Mirtazapine is not habit-forming when used as a hallucinogen and the desire to use it can actually decrease with use. It is most often self-regulating.

Tolerance to the effects of mirtazapine are built almost immediately after ingestion. After that, it takes about 3 days for the tolerance to be reduced to half and 7 days to be back at baseline (in the absence of further consumption).

Overdose

Mirtazapine is considered to be relatively safe in the event of an overdose,[38] although it is considered slightly more toxic in overdose than most of the SSRIs (except citalopram).[39] Unlike the TCAs, mirtazapine showed no significant cardiovascular adverse effects at 7 to 22 times the maximum recommended dose.[40] Case reports of overdose with as much as 30 to 50 times the standard dose described the drug as relatively nontoxic, compared to TCAs.[41][42]

Twelve reported fatalities have been attributed to mirtazapine overdose.[43][44] The fatal toxicity index (deaths per million prescriptions) for mirtazapine is 3.1 (95% CI: 0.1 to 17.2). This is similar to that observed with SSRIs.[45]

It is strongly recommended that one use harm reduction practices when using this substance.

Dangerous interactions

    • Antidepressants - Different types of antidepressants can cause adverse effects as well as possible serotonin syndrome when mixed.

Legal status

Handcuffs-300px.png

This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

Mirtazapine is legally approved for medical purposes worldwide. However, it is illegal to sell and possess in most countries without a prescription.

  • Switzerland: Mirtazapine is listed as a "Abgabekategorie B" pharmaceutical, which generally requires a prescription.[citation needed]
  • Turkey: Mirtazapine is classed as anti-depressant so it is prescription only drug[citation needed] but the law is often unenforced.
  • United Kingdom: Mirtazapine is a licensed prescription-only medicine (POM) in the United Kingdom.[46] It is not a criminal offence to possess this medicine without a valid prescription. This medicine can legally be obtained with a valid prescription or through legal import of the medicine for personal use as outlined in Section 13 of the Medicines Act 1968.[47]

See also

External links

Discussion

References

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