Mr. Ibrahem/Loxapine
Clinical data
Trade namesLoxitane, Adasuve, others
AHFS/Drugs.comMonograph
MedlinePlusa682311
License data
Routes of
administration
By mouth, powder for inhalation
Drug classTypical antipsychotic[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic data
Protein binding96.8%[2]
MetabolismExtensive hepatic; active metabolites include amoxapine and 8-hydroxyloxapine. Inhibits P-gp and is a substrate of CYP1A2, CYP3A4 and CYP2D6[2]
Elimination half-life4 hours (oral); 7.61 hours (inhalation)[2]
ExcretionMajority are excreted within 24 hours, main route through urine (conjugated metabolites), small amounts through the feces (unconjugated metabolites)
Identifiers
  • 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine
Chemical and physical data
FormulaC18H18ClN3O
Molar mass327.81 g·mol−1
3D model (JSmol)
Melting point109 to 110 °C (228 to 230 °F)
  • Clc2ccc1Oc4c(/N=C(\c1c2)N3CCN(C)CC3)cccc4
  • InChI=1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3 checkY
  • Key:XJGVXQDUIWGIRW-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Loxapine, sold under the brand names Loxitane among others, is a typical antipsychotic used to treat psychosis including schizophrenia and for agitation.[1][3] Benefit in people with intellectual disability is unclear.[1] It is taken by mouth or inhaled.[1][3]

Common side effects include movement disorders, sleepiness, dry mouth, blurry vision, low blood pressure with standing, and fast heart rate.[1] Other side effects may include milk production, seizures, sunburns, neuroleptic malignant syndrome, and increased risk of death in those with dementia.[1] It is believed to work by blocking dopamine D2 and 5-HT2A receptors.[3]

Loxapine was approved for medical use in the United States in 1975.[1] In the United States 60 pills of 50 mg costs about 38 USD as of 2021.[4]

References edit

  1. ^ a b c d e f g h i j "Loxapine Monograph for Professionals". Drugs.com. Archived from the original on 27 January 2021. Retrieved 24 November 2021.
  2. ^ a b c Truven Health Analytics, Inc. DrugPoint System (Internet) [cited 2013 Sep 21]. Greenwood Village, CO: Thomsen Healthcare; 2013.
  3. ^ a b c BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 407. ISBN 978-0857114105.
  4. ^ "Loxapine Prices, Coupons & Savings Tips". GoodRx. Archived from the original on 11 December 2021. Retrieved 24 November 2021.