Zotepine

Zotepine


Zotepine (brand names: Losizopilon (JP), Lodopin (ID, JP), Setous (JP), Zoleptil (CZ, PT, TR, UK†); where † indicates a formulation that has been discontinued) is an atypical antipsychotic drug indicated for acute and chronic schizophrenia. It has been used in Germany since 1990 (although it has been discontinued in Germany) and Japan since 1982.

Zotepine is not approved for use in the United States, United Kingdom, Australia, Canada or New Zealand.[1]

Contents

  • Description 1
  • Taxonomy 2
  • Distribution 3
  • References 4
  • External links 5

Medical Uses

Zotepine's primary use is as a treatment for schizophrenia[2] although clinical trials have been conducted (with positive results) into its efficacy as an antimanic agent in patients with acute bipolar mania.[3][5][7]

Side effects

Common[8][2]
Unknown Frequency[8][2]
Rare[8][2]

Pharmacology

The antipsychotic effect of zotepine is thought to be mediated through antagonist activity at dopamine and serotonin receptors. Zotepine has a high affinity for the D1 and D2 receptors. It also affects the 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors.[13] In addition, its active metabolite, norzotepine, serves as a potent norepinephrine reuptake inhibitor.[15]
Macromolecule (Receptor or transporter protein) Ki [nM][13]
SERT 151
NET 530
DAT 3621
5-HT1A 470.5
5-HT1B 59.5
5-HT1D 119
5-HT1E 700
5-HT2A 2.7
5-HT2C 2.6
5-HT3 472
5-HT5A 29
5-HT6 6
5-HT7 12
α1A 7
α1B 5
α2A 180
α2B 5.35
α2C 106
M1 18
M2 140
M3 73
M4 77
M5 260
D1 71
D2 25
D2S 5.4
D2L 11
D3 6.4
D4 18
D5 248
H1 3.21
H2 500
H4 1977

Dosing

The most common dosage used is 150 mg daily. It is suggested that zotepine therapy starts at 75 mg to 150 mg divided into three daily doses. Some people may need to have their dosage increased to 300 mg.[1]

50 mg Lodopin® pills

See also

References

  1. ^
  2. ^ a b c
  3. ^ a b c
  4. ^
  5. ^ a b c
  6. ^
  7. ^ a b , abstract (in French and English)
  8. ^
  9. ^
  10. ^
  • http://www.priory.com/focus11.htm
  • http://www.nyrdtc.nhs.uk/docs/nde/Zotepine.pdf -
  • LOSIZOPILON SUGAR-COATED TABLETS & FINE GRANULES (PDF)
  • ロドピン(ゾテピン) 1982年 精神神経学雑誌