Suvarna Garge (Editor)

Loxapine

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AHFS/Drugs.com
  
Monograph

CAS ID
  
1977-10-2

Protein binding
  
96.8%

MedlinePlus
  
a682311

Molar mass
  
327.808 g/mol

Loxapine

Trade names
  
Several trade names worldwide

License data
  
EU EMA: Adasuve US DailyMed: 50e11732-7387-452d-b3e6-db3a431d5c4a US FDA: Loxapine

Pregnancy category
  
US: C (Risk not ruled out)

Routes of administration
  
Oral, powder for inhalation

Loxapine (several trade names worldwide) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines). Several researchers have argued that loxapine may behave as an atypical antipsychotic.

Contents

Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant.

Therapeutic uses and dosages

The typical starting dosage is 10 mg twice daily; usual dose range 30–50 mg twice daily; maximum recommended dosage is 250 mg per day. The US Food and Drug Administration (FDA) has approved loxapine inhalation powder 10 mg (Adasuve, Alexza Pharmaceuticals) for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults.

A brief review of loxapine found no conclusive evidence that it was particularly effective in patients with paranoid schizophrenia. A subsequent systematic review considered that the limited evidence did not indicate a clear difference in its effects from other antipsychotics.

Precautions

This drug is unrelated to the habit-forming benzodiazepines, and misuse is rare. The risks and side effect profile are comparable to other antipsychotics.

Side effects

Note: Percentages given after possible adverse effects refer to the incidence of said adverse effects, according to DrugPoint.

Common side effects of loxapine (≥1% incidence) when inhaled include
  • Taste sense altered (14%)
  • Sedated (12%)
  • Pharyngitis (3%)
  • Common side effects of orally-administered loxapine include
  • Constipation
  • Dry mouth
  • Akathisia
  • Dizziness
  • Intense Sleeping (Highest Percentage)
  • Blurred Speech
  • Extrapyramidal disease (dose-dependent. At lower dosages its propensity for causing extrapyramidal side effects appears to be similar to that of atypical antipsychotics
  • Blurred vision
  • Urinary retention
  • Somnolence (which appears to be moderate in severity compared to other antipsychotic drugs)
  • Dyspnoea
  • Nasal congestion
  • Rare side effects include
  • Paralytic ileus
  • Agranulocytosis
  • Leukopenia
  • Thrombocytopenia
  • Hepatocellular liver damage
  • Neuroleptic malignant syndrome
  • Seizure
  • Tardive dyskinesia
  • Stroke
  • Transient ischaemic attack
  • Death
  • Pharmacology

    The data in the following table was obtained from the PDSP Ki database and they are for binding towards human cloned proteins (receptor and transporter) unless otherwise specified.

    References

    Loxapine Wikipedia