Mianserin

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Mianserin
200px
Systematic (IUPAC) name
(±)-2-methyl-1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine
Identifiers
CAS Number 24219-97-4
ATC code N06AX03 (WHO)
PubChem CID 4184
IUPHAR/BPS 135
Chemical data
Formula C18H20N2
Molar mass 264.365[[Script error: No such module "String".]]
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Mianserin (Bolvidon, Norval, Tolvon) is a psychoactive drug of the tetracyclic antidepressant (TeCA) chemical class which is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine effects. It was previously available internationally, however in most markets it has been phased out in favor of its analogue and successor mirtazapine (Remeron).

An interesting finding is that upon administration, mianserin has been shown to increase the life span of the nematode Caenorhabditis elegans by as much as 30% via dietary restriction caused by modulation of serotonin receptors in the species.[1] But if the animals are kept in a high-food environment mianserin increases obesity and actually decreases the lifespan.[2]

Pharmacology

Mianserin is an antagonist at the H1, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, and also acts as a norepinephrine reuptake inhibitor (NRI) via blockade of the norepinephrine transporter (NET).[3] As a high affinity H1 receptor antagonist, mianserin has strong antihistamine effects; however, it has negligible affinity for the muscarinic acetylcholine receptors, and therefore lacks any anticholinergic properties.

Blockade of the H1 receptor has sedative and anxiolytic effects, while antagonism of the 5-HT2A and α1-adrenergic receptors inhibits activation of intracellular phospholipase C (PLC), which seems to be common target for several different classes of antidepressants.[4] By antagonizing the somatodendritic and presynaptic α2-adrenergic receptors which function predominantly as inhibitory autoreceptors and heteroreceptors, mianserin disinhibits the release of norepinephrine, dopamine, serotonin, and acetylcholine in various areas of the brain and body.

Side effects

Common side effects of mianserin may include dizziness, blurred vision, sedation, drowsiness or somnolence, increased appetite or hyperphagia and subsequent weight gain, dry mouth or xerostomia, and constipation, among others. Potentially serious adverse reactions may include allergic reaction, fainting or syncope, seizures or convulsions, and white blood cell reduction or agranulocytosis.

Discontinuation

Abrupt or rapid discontinuation of mianserin may provoke a withdrawal, the effects of which may include depression, anxiety, panic attacks,[5] decreased appetite or anorexia, insomnia, diarrhea, nausea and vomiting, and flu-like symptoms, such as allergies or pruritus, among others.

Enantioselectivity

File:Smianserin.png
(S)-mianserin

(S)-(+)-Mianserin is approximately 200-300 times more active than its antipode (R)-(–)-mianserin.

References

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Further reading

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External links


GABAA PAMs
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc, drug(N5A/5B/5C/6A/6B/6D)

5-HT3 Antagonists
CB1 Agonists (Cannabinoids)
D2/D3 Antagonists
H1 Antagonists (Antihistamines)
mACh Antagonists (Anticholinergics)
NK1 Antagonists
Others
GABAA receptor
Ultrashort-acting
Short/intermediate-
acting
Long-acting
Ungrouped
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Long-acting
Dialkylphenols
Alpha-2 adrenergic
receptor
Melatonin receptor
Histamine receptor &
Acetylcholine receptor
5-HT2A &
α1-adrenergic
Selective 5-HT2A & α1-adrenergic antagonists
GABAB receptor /
GHB receptor
GHB Type
Orexin receptors
Orexin antagonists
Other receptors/
ungrouped
Other

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc, drug(N5A/5B/5C/6A/6B/6D)

Classes
Antidepressants
7-OH-Amoxapine • Amezepine • Amineptine • Amitriptyline • Amitriptylinoxide • Amoxapine • Aptazapine • Azepindole • Azipramine • Butriptyline • Cianopramine • Ciclazindol • Ciclopramine • Clomipramine • Cotriptyline • Cyanodothiepin • Demexiptiline • Depramine/Balipramine • Desipramine • Dibenzepine • Dimetacrine • Dosulepin/Dothiepin • Doxepin • Enprazepine • Esmirtazapine • Fluotracen • Hepzidine • Homopipramol • Imipramine • Imipraminoxide • Intriptyline • Iprindole • Ketipramine • Litracen • Lofepramine • Losindole • Loxapine • Maprotiline • Mariptiline • Mazindol • Melitracen • Metapramine • Mezepine • Mianserin • Mirtazapine • Naranol • Nitroxazepine • Nortriptyline • Noxiptiline • Octriptyline • Opipramol • Oxaprotiline • Pipofezine • Pirandamine • Propizepine • Protriptyline • Quinupramine • Setiptiline/Teciptiline • Tandamine • Tampramine • Tianeptine • Tienopramine • Trimipramine
Antihistamines
Antipsychotics
Acetophenazine • Amoxapine • Asenapine • Butaclamol • Butaperazine • Carphenazine • Carpipramine • Chlorpromazine • Chlorprothixene • Ciclindole • Clocapramine • Clomacran • Clotiapine • Clozapine • Flucindole • Fluotracen • Flupentixol • Fluphenazine • Gevotroline • Homopipramol • Levomepromazine/Methotrimeprazine • Loxapine • Maroxepin • Mesoridazine • Metitepine/Methiothepin • Metoxepin • Mosapramine • Naranol • Olanzapine • Perazine • Perphenazine • Periciazine • Piperacetazine • Pipotiazine • Piquindone • Prochlorperazine • Promazine • Prothipendyl • Quetiapine • Sulforidazine • Thiethylperazine • Thiopropazate • Thioridazine • Thiothixene • Trifluoperazine • Triflupromazine • Zotepine • Zuclopenthixol
Others
de:Mianserin

fr:Miansérine hu:Mianszerin ja:ミアンセリン pl:Mianseryna pt:Mianserina sv:Mianserin

zh:米塞林
  1. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. ↑ Zarse K, Ristow M (2008). "Antidepressants of the serotonin-antagonist type increase body fat and decrease lifespan of adult Caenorhabditis elegans". PLoS ONE. 3 (12): e4062. doi:10.1371/journal.pone.0004062. PMC 2605556 Freely accessible. PMID 19112515. 
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