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Mianserin
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
PubChem 4184
Chemical data
Formula C 18H20N2  
Mol. mass 264.365
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?
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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 scientific fact 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]

Contents

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 and 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

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

(S)-mianserin

References

  1. ^ Petrascheck M, Ye X, Buck LB (November 2007). "An antidepressant that extends lifespan in adult Caenorhabditis elegans". Nature 450 (7169): 553–6. doi:10.1038/nature05991. PMID 18033297.  
  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. PMID 19112515.  
  3. ^ Leonard, B; Richelson H (2000). "Synaptic Effects of Antidepressants: Relationship to Their Therapeutic and Adverse Effects.". in Buckley. Schizophrenia and Mood Disorders: The New Drug Therapies in Clinical Practice.. Oxford: Butterworth-Heinemann. ISBN 978-0-7506-4096-1.  
  4. ^ Dwivedi, Y; Agrawal AK, Rizavi HS, Pandey GN (December 2002). "Antidepressants Reduce Phosphoinositide-Specific Phospholipase C (PI-PLC) Activity and the mRNA and Protein Expression of Selective PLC β1 Isozyme in Rat Brain.". Neuropharmacology (Elsevier) 43 (8): 1269–1279. doi:10.1016/S0028-3908(02)00253-8. PMID 12527476.  
  5. ^ Kuniyoshi, M; Arikawa K, Miura C, Inanaga K (June 1989). "Panic Anxiety after Abrupt Discontinuation of Mianserin". Psychiatry and Clinical Neurosciences (Wiley InterScience) 43 (2): 155–159. doi:10.1111/j.1440-1819.1989.tb02564.x. PMID 2796025.  

Further reading

External links








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