Also known as
Remeron, Remeron SolTab, avanza, zispin, axit, mirtaz, mirtazon
Classification
Antidepressant, hallucinogen
Overview
Mirtazapine is an antidepressant introduced by Organon International in 1996 used for the treatment of moderate to severe depression. Mirtazapine has a tetracyclic chemical structure and is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). It is the only tetracyclic antidepressant that has been approved by the FDAUS Food and Drug Administration to treat depression 1.
Medical usage
Used to treat depression 2.
What does it look like?
Tablets
Dosage
Therapeutic
- For oral dosage forms (orally disintegrating tablets, tablets) –
- For depression –
- Adults – at first, 15 milligrams once a day, preferably in the evening just before sleep. Your doctor may adjust your dose if needed. However, the dose is usually not more than 45 mg per day 2.
Abuse
Oral
- threshold 50 – 70 mg,
- light 80 – 130 mg,
- common 140 – 90 mg,
- strong 190 – 240 mg,
- heavy 250 mg + 3.
What are the different forms?
Mirtazapine is available as regular and oral disintegrating tablets of 15, 30 and 45 mg in multiple generic forms and under the brand name Remeron 4.
How long do its effects last?
Onset of effects
- 15 – 30 minutes 3.
Peak
- 90 – 180 minutes 3.
Offset
- 2 – 6 hours 3.
After-effects
- Up to 12 hours 3.
Pharmacology
Pharmacodynamics
Mirtazapine, an antidepressant of the piperazinoazepine class, is a tetracyclic compound with an anxiolyticDrugs that relieve medically-diagnosed anxiety. More effect. Mirtazapine has fewer ADRs than tricyclic antidepressants and is better tolerated. Selective blockade of specific serotonin receptorsnerve endings that sense changes in the body More by mirtazapine likey minimises side-effects typical of other antidepressants 1.
Absorption
Rapid and complete, but, due to first-pass metabolism, absolute bioavailability is 50% 1.
Bioavailability
50% 1.
Metabolism
Mirtazapine is extensively metabolised by demethylation and hydroxylation followed by glucuronide conjugation. Cytochrome P450 2D6 and cytochrome P450 1A2 are involved in formation of the 8-hydroxy metabolite of mirtazapine, and cytochrome P450 3A4 is responsible for the formation of the N-desmethyl and N-oxide metabolites. Several metabolites possess pharmacological activity, but plasma levels are very low 1.
Half-life
20 – 40 hours 1.
Elimination
Lethal dosage
Tolerance
Tolerancethis is the process by which the receptors in your brain become habituated to the action of a drug. When tolerance is reached, more of the drug is required to achieve the same effect. With benzodiazepines, and probably with many other classes of drugs as well, tolerance is virtually always associated with some degree of physical dependence. If you find that you are experiencing tolerance, this is a clear warning sign that you may have formed a dependence. More to the effects of mirtazapine are built almost immediately after ingestion. After that, it takes about 3 days for the tolerancethis is the process by which the receptors in your brain become habituated to the action of a drug. When tolerance is reached, more of the drug is required to achieve the same effect. With benzodiazepines, and probably with many other classes of drugs as well, tolerance is virtually always associated with some degree of physical dependence. If you find that you are experiencing tolerance, this is a clear warning sign that you may have formed a dependence. More to be reduced to half and 7 days to be back at baseline (in the absence of further consumption). Mirtazapine presents cross-tolerance with all psychedelics, meaning that after the consumption of mirtazapine all psychedelics will have a reduced effect 3.
Mechanism of action
Mirtazapine acts as an antagonist at central pre-synaptic alpha(2)-receptors, inhibiting negative feedback to the presynaptic nerve and causing an increase in NE release. Blockade of heteroreceptors, alpha(2)-receptors contained in serotenergic neurons, enhances the release of 5-HT, increasing the interactions between 5-HT and 5-HT1 receptorsnerve endings that sense changes in the body More and contributing to the anxiolyticDrugs that relieve medically-diagnosed anxiety. More effects of mirtazapine. Mirtazapine also acts as a weak antagonist at 5-HT1 receptorsnerve endings that sense changes in the body More and as a potent antagonist at 5-HT2 (particularly subtypes 2A and 2C) and 5-HT3 receptorsnerve endings that sense changes in the body More. Blockade of these receptorsnerve endings that sense changes in the body More may explain the lower incidence of adverse effects such as anxiety, insomniadifficulty in going to sleep or in getting enough sleep, and nausea. Mirtazapine also exhibits significant antagonism at H1-receptors, resulting in sedationthe state of being relaxed or sleepy because of a drug More. Mirtazapine has no effects on the reuptake of either NE or 5-HT and has only minimal activity at dopaminergic and muscarinic receptorsnerve endings that sense changes in the body More 1.
Effects
Physical effects
- changes in gravitycan be described as feelings of gravity shifting in its direction. For example, during this state one may feel as if they are flying forwards, backwards, upwards, downwards, in multiple directions at once, or in a singular direction that doesn't make sense More,
- spontaneous tactile sensationsthese can be described as the physical experience of an activation of nerve endings across the body occurring without any obvious or immediate physical trigger. The experience of this results in feelings of distinct random tactile input and general tingling sensations. Depending on the psychoactive substance consumed, these vary greatly in their alternative styles of sensation, but can be broken down into three basic levels of intensity. These are described and listed here - 1. Mild - The lowest level of the sensation can be described as light and fleeting tingling sensations across the body that do not impair physical motor control and can essentially be ignored if one wishes to do so, and - 2. Distinct - At this level, the sensation becomes impossible to ignore. It can be described as distinct tingling sensations which are intense enough to partially impair a person’s motor control and cause a significant portion of mental focus to be directed towards these sensations, and - 3. Overwhelming - The highest level occurs when the tingling sensations have increased enough to become a powerful, uncontrollable focus point of attention. This feels completely overwhelming and impairs a person's motor control, consistently leaving them either lying or sitting down, incapable of standing up, or writhing in the all-encompassing sensations More,
- tactile hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind,
- appetite enhancement,
- motor control loss,
- sedationthe state of being relaxed or sleepy because of a drug More,
- constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More,
- dizziness 3.
Cognitive effects
- conceptual thinking,
- time distortion,
- dream potentiationcan be described as a cognitive component which increases the intensity, vividness and frequency of sleeping dream states. This effect also creates higher detail and definition within dreams alongside of an increase in the likelihood of one's dreams becoming lucid. More,
- immersion enhancementThis is an effect which can be described as a pronounced increase in one's ability to become fully engulfed within external visual or auditory stimuli such as music, movies, video games and various other forms of media. More,
- increased music appreciation,
- amnesiainability to remember,
- information processing suppressioncan be described as a partial to complete suppression of a person's ability to process information and logically analyse a situation in an understandable and linear fashion. This is something which can result in states of stupor, indecisiveness, confusion and even irrational behaviour or delirium. More,
- thought deceleration 3.
Auditory effects
- auditory distortion,
- auditory enhancement,
- auditory hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind 3.
Visual effects
- tracers,
- geometrybest described as the experience of a person's field of vision being partially or completely encompassed by fast-moving, colourful and indescribably complex geometric patterns, form constants, phosphenes, shapes, fractals, structures and colour. These geometric forms can also become structured and organised in a way that presents genuine information to the person experiencing it far beyond the perception of meaningless, although complex, shapes and colours. This happens through the experience of innately understood geometric representations that feel as though they depict specific concepts and neurological components that exist within the brain in a manner that is extremely detailed. More,
- autonomous entities,
- external hallucinationsbest described as the experience of perceiving imagined visual concepts and occurrences which display themselves seamlessly into the external environment as if they were actually happening. More,
- internal hallucinationsbest described as the perception of imagery and scenes which are experienced exclusively within a layer in front of one's open or closed eye vision and not seamlessly within the external environment around oneself. At lower levels, internal hallucinations begin with imagery which does not take up the entirety of one's visual field and is distinctively separate from its background. These can be described as spontaneous moving or still images of scenes, concepts, places, and anything one could imagine. They are manifested in varying levels of detail, ranging from ill-defined and cartoon-like in nature to completely realistic and beyond realism through seemingly impossible, non-euclidean geometric forms. They rarely hold their form for more than a few seconds before fading or shifting into another image. More,
- perspective alterations,
- scenarios and plots,
- settings, sceneries, and landscapes 3.
Minor effects
More common
- constipationmeans that you're not passing stools regularly or you're unable to completely empty your bowels. More,
- dizziness,
- drowsiness,
- dry mouth,
- increased appetite,
- weight gain 2.
Less common
- abdominal or stomach pain,
- abnormal dreams,
- back pain,
- dizziness or fainting when getting up suddenly from a lying or sitting position,
- increased need to urinate,
- increased sensitivity to touch,
- increased thirst,
- low blood pressure,
- muscle pain,
- nausea,
- sense of constant movement of self or surroundings,
- trembling or shaking,
- vomiting,
- weakness 2.
Major effects
Less common
- decreased or increased movement,
- mood or mental changes, including abnormal thinking, agitation, anxiety, confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation, and feelings of not caring,
- shortness of breath,
- skin rash,
- swelling 2.
Rare
- change in menstrual cycle,
- convulsionswhen your body shakes violently without you meaning it to,
- decreased sexual ability,
- menstrual pain,
- mood or mental changes, including anger, feelings of being outside the body, hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind, mood swings, and unusual excitement,
- mouth sores,
- sore throat, chills, or fever 2.
History
Originally introduced by Organon International in the United States in 1990. Its patent expired in 2004 and hence generic versions are now available 3.
Footnotes:
Mirtazapine, 2017, https://www.drugbank.ca/drugs/DB00370
Mirtazapine, 2017, https://www.drugs.com/mirtazapine.html
Mirtazapine, 2017, https://psychonautwiki.org/wiki/Mirtazapine
Mirtazapine, 2017, https://livertox.nlm.nih.gov//Mirtazapine.htm
Mirtazapine, 2017, https://en.wikipedia.org/wiki/Mirtazapine