thiothixene (Navane, Tiotixene)

Introduction

Tradename: Navane. (thiothixene hydrochloride)

Indications

• symptomatic management of psychotic disorders

Contraindications

• narrow-angle glaucoma
• bone marrow suprression
• severe liver disease
• severe cardiac disease

Caution:

• safety & efficacy in children < 6 months of age is not established
• seizures

pregnancy category = c

safety in lactation = ?

Dosage

4 mg IM every 6-12 hours

• start 2 mg PO TID, max 60 mg/day.

Tabs: 1, 2, 5, 10, 20 mg.

Liquid: 5 mg/5 mL.

Pharmacokinetics

• oral dose is well absorbed from GI tract
• widely distributed throughout body tissues
• metabolized by the liver
• excreted unchanged in the feces
• elimination 1/2life is 30 hours
• residual drug remains in body for several weeks

elimination via liver

elimination via kidney

1/2life = 34 hours

Adverse effects

• common (> 10%)
  • pseudoparkinsonism, akathisia, dystonia, hypotension, pigmentary retinopathy, persistent tardive dyskinesia, constipation, decreased sweating, dizziness, orthostatic hypotension, nasal congestion
• less common (1-10%)
  • difficulty urinating, photosensitivity, rash, changes in menstrual cycle, sexual dysfunction, breast pain, weight gain, nausea/vomiting, epigastric pain, trembling of fingers
• uncommon (< 1%)
  • agranulocytosis, cholestatic jaundice, neuroleptic malignant syndrome, priapism, blue-gray discoloration of skin, impairment of temperature regulation, galactorrhea, leukopenia, hepatotoxicity, changes in the cornea & lens, pigmentary retinopathy
• other
  • low sedation, anticholinergic effects & orthostatic hypotension
  • high incidence of extrapyramidal effects
    • tardive dyskinesia
      • pseudoparkinsonism
      • dystonias
      • akathisia
  • neuroleptic malignant syndrome (rare)
  • prolongation of the QT interval
  • elevated serum transaminases
  • lowering of seizure threshold

• drug adverse effects of antipsychotic agents
• drug adverse effects of psychotropic agents

Drug interactions

(see chlorpromazine)

• drug interaction(s) of antipsychotics & dopamine receptor agonists
• drug interaction(s) of antipsycotics with benzodiazepines

Laboratory

• specimen: serum
• methods: color, fluorometry, GC-MS, HPLC
• interferences: color & fluorometric methods lack specificity

Mechanism of action

• high potency antipsychotic agent (see chlorpromazine)

More general terms

• thioxanthene
• antipsychotic agent

Additional terms

• chlorpromazine (Thorazine, Ormazine, Propaphenin, Sonazine, Chloractil)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5454
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=941650
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=941651
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=64754
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=64755