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Tandospirone

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Tandospirone
Clinical data
Trade namesSediel
Other namesMetanopirone
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life2–3 hours (3–5 hours for metabolite 1-PPTooltip 1-(2-pyrimidinyl)piperazine)
ExcretionUrine (70%; 0.1% as unchanged drug)
Identifiers
  • (1R,2R,6S,7S)-4-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-4-azatricyclo[5.2.1.02,6]decane-3,5-dione
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.210.461 Edit this at Wikidata
Chemical and physical data
FormulaC21H29N5O2
Molar mass383.487 g/mol g·mol−1
3D model (JSmol)
  • O=C1N(C(=O)[C@H]3[C@@H]1[C@@H]2CC[C@H]3C2)CCCCN5CCN(c4ncccn4)CC5
  • InChI=1S/C21H29N5O2/c27-19-17-15-4-5-16(14-15)18(17)20(28)26(19)9-2-1-8-24-10-12-25(13-11-24)21-22-6-3-7-23-21/h3,6-7,15-18H,1-2,4-5,8-14H2/t15-,16+,17+,18- checkY
  • Key:CEIJFEGBUDEYSX-FZDBZEDMSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Tandospirone (brand name Sediel) is an anxiolytic and antidepressant drug used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma. It is a member of the azapirone class of drugs and is closely related to other azapirones like buspirone and gepirone.

Medical uses

Anxiety and depression

Tandospirone is most commonly used as a treatment for anxiety and depressive disorders, such as generalised anxiety disorder and dysthymia respectively.[1] For both indications it usually takes a couple of weeks for therapeutic effects to be start being seen,[1] although at higher doses more rapid anxiolytic responses have been seen.[2] It has also been used successfully as a treatment for bruxism.[3]

Other uses

Tandospirone has also been tried, successfully, as an adjunctive treatment for cognitive symptoms in schizophrenic individuals.[4]

Side effects

Common adverse effects include:[1]

  • Dizziness
  • Drowsiness
  • Insomnia
  • Headache
  • Gastrointestinal disorders
  • Dry mouth
  • Negative influence on explicit memory function [1]

Adverse effects with unknown frequency include:[1]

It is not believed to be addictive but it is known to produce mild withdrawal effects (e.g. anorexia) after abrupt discontinuation.[1]

Pharmacology

Tandospirone acts as a potent and selective 5-HT1A receptor partial agonist, with a Ki affinity value of 27 ± 5 nM[5] and approximately 55 to 85% intrinsic activity.[6][7] It has weak and clinically negligible affinity for the 5-HT2A (1,300 ± 200), 5-HT2C (2,600 ± 60), α1-adrenergic (1,600 ± 80), α2-adrenergic (1,900 ± 400), D1 (41,000 ± 10,000), and D2 (1,700 ± 300) receptors, and is essentially inactive at the 5-HT1B, 5-HT1D, β-adrenergic, and muscarinic acetylcholine receptors, serotonin transporter, and benzodiazepine allosteric site of the GABAA receptor (all of which are > 100,000).[5] There is evidence of tandospirone having low but significant antagonistic activity at the α2-adrenergic receptor through its active metabolite 1-(2-pyrimidinyl)piperazine (1-PP), however.[8][9]

Research

In February of 2018, a study was conducted by researchers at the Queensland University of Technology and published in the journal Scientific Reports. Researchers found that tandospirone helped reverse brain deficits caused by chronic alcohol exposure in mice.[10] The study was the first of its kind and brought interest in the drug for possible treatment of alcohol withdrawal symptoms.[11]

Society and culture

Name

Tandospirone has also been known as metanopirone.

References

  1. ^ a b c d e f Barradell, LB; Fitton, A (February 1996). "Tandospirone". CNS Drugs. 5 (2): 147–153. doi:10.2165/00023210-199605020-00006. {{cite journal}}: |format= requires |url= (help)
  2. ^ Nishitsuji; To, H; Murakami, Y; Kodama, K; Kobayashi, D; Yamada, T; Kubo, C; Mine, K (2004). "Tandospirone in the treatment of generalised anxiety disorder and mixed anxiety-depression : results of a comparatively high dosage trial". Clinical drug investigation. 24 (2): 121–6. doi:10.2165/00044011-200424020-00007. PMID 17516698. {{cite journal}}: |format= requires |url= (help)
  3. ^ Tandospirone. The Royal Pharmaceutical Society of Great Britain. 23 September 2011. Retrieved 14 November 2013. {{cite book}}: |work= ignored (help)
  4. ^ Sumiyoshi, T; Matsui, M; Nohara, S; Yamashita, I; Kurachi, M; Sumiyoshi, C; Jayathilake, K; Meltzer, HY (October 2001). "Enhancement of cognitive performance in schizophrenia by addition of tandospirone to neuroleptic treatment" (PDF). The American Journal of Psychiatry. 158 (10): 1722–1725. doi:10.1176/appi.ajp.158.10.1722. PMID 11579010.
  5. ^ a b Hamik; Oksenberg, D; Fischette, C; Peroutka, SJ (1990). "Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites". Biological Psychiatry. 28 (2): 99–109. doi:10.1016/0006-3223(90)90627-E. PMID 1974152.
  6. ^ Tanaka; Tatsuno, T; Shimizu, H; Hirose, A; Kumasaka, Y; Nakamura, M (1995). "Effects of tandospirone on second messenger systems and neurotransmitter release in the rat brain". General pharmacology. 26 (8): 1765–72. doi:10.1016/0306-3623(95)00077-1. PMID 8745167.
  7. ^ Yabuuchi, Kazuki; Tagashira, Rie; Ohno, Yukihiro (2004). "Effects of tandospirone, a novel anxiolytic agent, on human 5-HT1A receptors expressed in Chinese hamster ovary cells (CHO cells)". Biogenic Amines. 18 (3): 319. doi:10.1163/1569391041501933.
  8. ^ Blier; Curet, O; Chaput, Y; De Montigny, C (1991). "Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine--II. Effects of acute administration of 1-PP and long-term administration of tandospirone on noradrenergic neurotransmission". Neuropharmacology. 30 (7): 691–701. doi:10.1016/0028-3908(91)90176-C. PMID 1681447.
  9. ^ Miller; Thompson, ML; Byrnes, JJ; Greenblatt, DJ; Shemer, A (1992). "Kinetics, brain uptake, and receptor binding of tandospirone and its metabolite 1-(2-pyrimidinyl)-piperazine". Journal of Clinical Psychopharmacology. 12 (5): 341–5. doi:10.1097/00004714-199210000-00009. PMID 1362206.
  10. ^ "5-HT1A receptor-dependent modulation of emotional and neurogenic deficits elicited by prolonged consumption of alcohol". Scientific Reports. 2018. doi:10.1038/s41598-018-20504-z.
  11. ^ "New drug could reverses binge drinking effects on brain, help alcoholics: scientists". ABC.net.au. Retrieved 8 February 2018.


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