The Wayback Machine - https://web.archive.org/web/20120223233714/https://en.wikipedia.org/wiki/Mianserin

Mianserin

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Mianserin
Systematic (IUPAC) name
(±)-2-methyl-1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 24219-97-4 YesY
ATC code N06AX03
PubChem CID 4184
IUPHAR ligand 135
DrugBank DB06148
ChemSpider 4040 YesY
UNII 250PJI13LM YesY
KEGG D08216 YesY
ChEBI CHEBI:51137 N
ChEMBL CHEMBL6437 YesY
Chemical data
Formula C18H20N2 
Mol. mass 264.365
SMILES eMolecules & PubChem
 N(what is this?)  (verify)
Mianserin

Mianserin (Bolvidon, Depnon, 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]

Contents

[edit] Therapeutic uses

Mianserin is used in the treatment of depression, such as depression associated with agitation or anxiety and has similar efficacy to the antidepressant drug moclobemide.[3]

[edit] 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).[4] 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.

In addition, mianserin also appears to be a potent antagonist of the neuronal octopamine receptor.[5] What implications this may have on mood are currently unknown, however octopamine has been implicated in the regulation of sleep, appetite and insulin production and therefore may theoretically contribute to the overall side effect profile of mianserin.[6][7]

Blockade of the H1 and α1-adrenergic receptors has sedative and anxiolytic effects,[8] 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.[9] 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.

[edit] 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.

[edit] Discontinuation

Abrupt or rapid discontinuation of mianserin may provoke a withdrawal, the effects of which may include depression, anxiety, panic attacks,[10] decreased appetite or anorexia, insomnia, diarrhea, nausea and vomiting, and flu-like symptoms, such as allergies or pruritus, among others.

[edit] Enantioselectivity

(S)-mianserin

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

[edit] 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). Chapouthier, Georges. ed. "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. PMID 19112515. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2605556. 
  3. ^ Delini-Stula A, Mikkelsen H, Angst J (October 1995). "Therapeutic efficacy of antidepressants in agitated anxious depression--a meta-analysis of moclobemide studies". J Affect Disord 35 (1-2): 21–30. PMID 8557884. 
  4. ^ Leonard, B; Richelson H (2000). "Synaptic Effects of Antidepressants: Relationship to Their Therapeutic and Adverse Effects.". In Buckley, Peter F.. Schizophrenia and Mood Disorders: The New Drug Therapies in Clinical Practice.. Oxford: Butterworth-Heinemann. ISBN 978-0-7506-4096-1. 
  5. ^ Roeder, T (November 1990). "High-affinity antagonists of the locust neuronal octopamine receptor". European journal of pharmacology (Elsevier) 191 (2): 221–4. doi:10.1016/0014-2999(90)94151-M. PMID 2086239. 
  6. ^ Crocker, A; Sehgal A (September 2008). "Octopamine Regulates Sleep in Drosophila through PKA Dependent Mechanisms". Journal of neuroscience 28 (38): 9377–85. doi:10.1523/JNEUROSCI.3072-08a.2008. PMC 2742176. PMID 18799671. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2742176. 
  7. ^ Bour, S; Visentin V, Prévot D, Carpéné C. (September 2003). "Moderate weight-lowering effect of octopamine treatment in obese Zucker rats". Journal of physiology and biochemistry 59 (3): 175–82. doi:10.1007/BF03179913. PMID 15000448. 
  8. ^ http://www.medicines.org.au/files/shptolvo.pdf
  9. ^ 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. 
  10. ^ 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. 

[edit] Further reading

[edit] 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(eval/thrp), 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 agonists/PAMs
Barbiturates: Allobarbital • Amobarbital • Aprobarbital • Barbital • Butabarbital • Butobarbital • Cyclobarbital • Ethallobarbital • Heptabarb • Hexobarbital • Mephobarbital • Methohexital • Pentobarbital • Phenobarbital • Proxibarbal • Reposal • Secobarbital • Talbutal • Thiamylal • Thiopental • Vinbarbital • Vinylbital
Benzodiazepines: Brotizolam • Clonazepam • Cinolazepam • Climazolam • Doxefazepam • Estazolam • Flunitrazepam • Flurazepam • Flutoprazepam • Haloxazolam • Loprazolam • Lorazepam •Lormetazepam • Midazolam • Nimetazepam • Nitrazepam • Quazepam • Temazepam • Triazolam
Carbamates: Carisoprodol • Ethinamate • Hexapropymate • Meprobamate • Methocarbamol • Procymate • Tybamate
Neuroactive Steroids: Acebrochol • Allopregnanolone • Alphadolone • Alphaxolone • Eltanolone • Ganaxolone • Hydroxydione • Minaxolone • Org 20599 • Org 21465 • Tetrahydrodeoxycorticosterone
Nonbenzodiazepines: CL-218,872 • Eszopiclone • Indiplon • JM-1232 • Lirequinil • Necopidem • Pazinaclone • ROD-188 • Saripidem • Suproclone • Suriclone • SX-3228 • U-89843A • U-90042 • Zaleplon • Zolpidem • Zopiclone
Phenols: Fospropofol • Propofol
Piperidinediones: Glutethimide • Methyprylon • Pyrithyldione • Piperidione
Quinazolinones: Afloqualone • Cloroqualone • Diproqualone • Etaqualone • Mebroqualone • Mecloqualone • Methaqualone • Methylmethaqualone • Nitromethaqualone
Volatiles/gases: 2-Methyl-2-butanol • Acetophenone • Acetylglycinamide chloral hydrate • Centalun • Chloral hydrate • Ethanol (Alcohol) • Paraldehyde • Trichloroethanol
Others: Bromide (Lithium bromide, Potassium bromide, Sodium bromide) • Chloralose • Chloralodol • Clomethiazole • Dichloralphenazone • Ethchlorvynol • Etomidate • Gaboxadol • Loreclezole • Methylpentynol • Metomidate • Org 25435 • Petrichloral • Sulfonmethane • Triclofos • Valerenic acid (Valerian)
GABAB agonists
1,4-Butanediol • Aceburic acid • GABOB • GHB (Sodium oxybate) • GBL • GVL
H1 inverse agonists
α1-Adrenergic antagonists
α2-Adrenergic agonists
5-HT2A antagonists
Melatonin agonists
Orexin antagonists
Others
Classes
Antidepressants
Antihistamines
Antipsychotics
Others
Retrieved from "http://en.wikipedia.org/w/index.php?title=Mianserin&oldid=468072439"
Personal tools
Namespaces
Variants
Actions
Navigation
Interaction
Toolbox
Print/export
Languages
Morty Proxy This is a proxified and sanitized view of the page, visit original site.