Loxapine

Loxapine Brand Names

ADASUVE | Loxitane | Loxitane C

What is Loxapine

Loxapine is a conventional dibenzoxazepine antipsychotic used in the treatment of psychotic disorders such as schizophrenia.

Loxapine is metabolized to several active metabolites including amoxapine, a commercially available tetracyclic antidepressant.

Loxapine is considered an intermediate potency antipsychotic. Anticholinergic effects and other adverse reactions such as orthostatic hypotension and sedation are less likely to occur with loxapine than low potency antipsychotics such as chlorpromazine.

Additionally, extrapyramidal symptoms are generally less frequent with loxapine than high potency antipsychotics such as haloperidol.

Oral loxapine was initially approved by the FDA in 1975 as an oral formulation for the treatment of schizophrenia.

In December 2012, an oral inhalational formulation (Adasuve) was approved by the FDA for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults.

Due to the risk of bronchospasm, which may result in respiratory distress or respiratory arrest, inhalational loxapine is only available through the Adasuve Risk Evaluation and Mitigation Strategy (ADASUVE REMS) program and must be administered by a healthcare professional.

Healthcare facilities where Adasuve is administered must be enrolled in and fulfill the requirements of the REMS program.

Indications

  1. agitation
  2. autistic disorder
  3. behavioral or psychological symptoms of dementia
  4. schizophrenia

For the treatment of schizophrenia

Side Effects

  1. agitation
  2. agranulocytosis
  3. akathisia
  4. akinesia
  5. alopecia
  6. amenorrhea
  7. aplastic anemia
  8. asthenia
  9. blurred vision
  10. bronchospasm
  11. confusion
  12. constipation
  13. cough
  14. dizziness
  15. drowsiness
  16. dysarthria
  17. dysgeusia
  18. dysphagia
  19. dyspnea
  20. dystonic reaction
  21. edema
  22. elevated hepatic enzymes
  23. eosinophilia
  24. fever
  25. flushing
  26. galactorrhea
  27. gynecomastia
  28. hemolytic anemia
  29. hepatitis
  30. hyperprolactinemia
  31. hypertension
  32. hyperthermia
  33. hyponatremia
  34. hypotension
  35. hypothermia
  36. ileus
  37. insomnia
  38. jaundice
  39. leukopenia
  40. menstrual irregularity
  41. nasal congestion
  42. nausea
  43. neuroleptic malignant syndrome
  44. neutropenia
  45. orthostatic hypotension
  46. pancytopenia
  47. photosensitivity
  48. polydipsia
  49. pruritus
  50. pseudoparkinsonism
  51. ptosis
  52. purpura
  53. rash
  54. respiratory arrest
  55. retinopathy
  56. seborrhea
  57. seizures
  58. SIADH
  59. sinus tachycardia
  60. skin hyperpigmentation
  61. stroke
  62. syncope
  63. tardive dyskinesia
  64. throat irritation
  65. thrombocytopenia
  66. tremor
  67. urinary retention
  68. visual impairment
  69. vomiting
  70. water intoxication
  71. weight gain
  72. weight loss
  73. wheezing
  74. xerostomia

Monitoring Parameters

  • AIMS assessment
  • blood pressure
  • CBC
  • ophthalmologic exam
  • thyroid function tests (TFTs)

Contraindications

  • acute bronchospasm
  • agranulocytosis
  • ambient temperature increase
  • anticholinergic medications
  • asthma
  • breast cancer
  • breast-feeding
  • cardiac disease
  • cerebrovascular disease
  • children
  • chronic obstructive pulmonary disease (COPD)
  • closed-angle glaucoma
  • CNS depression
  • coadministration with other CNS depressants
  • coma
  • dehydration
  • dementia
  • driving or operating machinery
  • dysphagia
  • emphysema
  • ethanol ingestion
  • ethanol intoxication
  • geriatric
  • heart failure
  • hepatic disease
  • hyperprolactinemia
  • hyperthermia
  • hypotension
  • hypothermia
  • hypovolemia
  • infants
  • infertility
  • leukopenia
  • myocardial infarction
  • neonates
  • neurological disease
  • neutropenia
  • orthostatic hypotension
  • overdose
  • Parkinson’s disease
  • pregnancy
  • pregnancy testing
  • prostatic hypertrophy
  • pulmonary disease
  • requires a specialized care setting
  • seizure disorder
  • seizures
  • strenuous exercise
  • stroke
  • syncope
  • tardive dyskinesia
  • urinary retention

Loxapine is contraindicated in patients with a hypersensitivity to loxapine or other dibenzoxazepines (e.g., amoxapine)

Interactions

  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Guaifenesin; Phenylephrine
  • Acetaminophen; Tramadol
  • Acrivastine; Pseudoephedrine
  • Aldesleukin, IL-2
  • Alprazolam
  • Amifampridine
  • Amoxapine
  • Amphetamine
  • Amphetamine; Dextroamphetamine
  • Amphetamine; Dextroamphetamine Salts
  • Anticholinergics
  • Aripiprazole
  • Articaine; Epinephrine
  • Asenapine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Atropine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Edrophonium
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Baclofen
  • Barbiturates
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Benzphetamine
  • Benztropine
  • Brexpiprazole
  • Bromocriptine
  • Brompheniramine
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Dextromethorphan; Phenylephrine
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Bupropion
  • Bupropion; Naltrexone
  • Buspirone
  • Cabergoline
  • Cannabidiol
  • Capsaicin; Metaxalone
  • Carbamazepine
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Guaifenesin; Phenylephrine
  • Carbetapentane; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pyrilamine
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Cariprazine
  • Carisoprodol
  • Cenobamate
  • Cetirizine
  • Cetirizine; Pseudoephedrine
  • Cetrorelix
  • Chlophedianol; Dexbrompheniramine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chlophedianol; Guaifenesin; Phenylephrine
  • Chlorcyclizine
  • Chlordiazepoxide; Clidinium
  • Chlorpheniramine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorpromazine
  • Clemastine
  • Clobazam
  • Clozapine
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • COMT inhibitors
  • Cyclizine
  • Cyclobenzaprine
  • Cyproheptadine
  • Dantrolene
  • Degarelix
  • Deutetrabenazine
  • Dexchlorpheniramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmethylphenidate
  • Dextroamphetamine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Guaifenesin; Phenylephrine
  • Dextromethorphan; Promethazine
  • Dicyclomine
  • Dimenhydrinate
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Disopyramide
  • Dopamine
  • dopamine agonists
  • Doxylamine
  • Doxylamine; Pyridoxine
  • Ephedrine
  • Epinephrine
  • Esketamine
  • Eszopiclone
  • Ethanol
  • Ethosuximide
  • Fenfluramine
  • Flavoxate
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • food
  • Gabapentin
  • Ganirelix
  • General anesthetics
  • Glycopyrrolate
  • Glycopyrrolate; Formoterol
  • Goserelin
  • Guaifenesin; Phenylephrine
  • Haloperidol
  • Histrelin
  • Homatropine; Hydrocodone
  • Hydantoins
  • Hydrocodone; Phenylephrine
  • Hydroxyzine
  • Hyoscyamine
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Iloperidone
  • Indacaterol; Glycopyrrolate
  • Isocarboxazid
  • Lasmiditan
  • Leuprolide
  • Leuprolide; Norethindrone
  • Levocetirizine
  • Levodopa
  • Lithium
  • Lofexidine
  • Lorazepam
  • Lumateperone
  • Lurasidone
  • Maprotiline
  • Meclizine
  • Mepenzolate
  • Meperidine; Promethazine
  • Meprobamate
  • Mesoridazine
  • Metaxalone
  • Methamphetamine
  • Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
  • Methscopolamine
  • Methylphenidate
  • Metoclopramide
  • Molindone
  • Monoamine oxidase inhibitors
  • Nafarelin
  • Non-Ionic Contrast Media
  • Norepinephrine
  • Olanzapine
  • Opiate Agonists
  • Orphenadrine
  • Oxybutynin
  • Paliperidone
  • Paroxetine
  • Pemoline
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenylephrine
  • Phenylephrine; Promethazine
  • Pimozide
  • Pregabalin
  • Prilocaine; Epinephrine
  • Prochlorperazine
  • Promethazine
  • Propantheline
  • Quazepam
  • Quetiapine
  • Rasagiline
  • Risperidone
  • Rotigotine
  • Safinamide
  • Scopolamine
  • Sedating H1-blockers
  • Selegiline
  • Sodium picosulfate; Magnesium oxide; Anhydrous citric acid
  • Tetrabenazine
  • Thalidomide
  • Thioridazine
  • Thiothixene
  • Tizanidine
  • tobacco
  • Tramadol
  • Tranylcypromine
  • Tricyclic antidepressants
  • Trifluoperazine
  • Trihexyphenidyl
  • Triprolidine
  • Triptorelin
  • Valproic Acid, Divalproex Sodium
  • Vigabatrin
  • Zaleplon
  • Ziprasidone
  • Zolpidem
  • Zonisamide
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