Classes
DEA Class; Rx
Common Brand Names; Loxitane, Adasuve
- Antipsychotics, 1st Generation;
Description
Oral formulation approved for the treatment of schizophrenia
Inhalational formulation approved for treating agitation associated with schizophrenia or bipolar I disorder
Inhalational loxapine is only available through a REMS program due to the risk of bronchospasm, which may result in respiratory distress or respiratory arrest
Indications
Indicated for the treatment of schizophrenia
Contraindications
Documented hypersensitivity; severe CNS depression; severe liver or cardiac disease, bone marrow suppression; narrow-angle glaucoma
CNS depression (including coma), neuroleptic malignant syndrome (NMS), poorly controlled seizure disorder
Adverse Effects
Common
Hypotension, orthostatic hypotension
Akathisia, dizziness, drug-induced tardive dystonia, dystonia, extrapyramidal disease, parkinsonian, somnolence, tardive dyskinesia
Diminished sweating
Constipation, xerostomia
Blurred vision
Urinary retention
Nasal congestion
Serious
Prolonged QT interval, torsades de pointes
Ineffective thermoregulation, heatstroke or hypothermia (rare), neuroleptic malignant syndrome (rare), seizure (rare)
Paralytic ileus (rare)
Agranulocytosis (rare), disorder of hematopoietic structure (rare), leukopenia (rare), thrombocytopenia (rare)
Cholestatic jaundice syndrome (rare)
Drug-induced lupus erythematosus, systemic (rare)
Priapism (rare)
Warnings
Use with extreme caution in patients with a history of convulsive disorders since it lowers convulsive threshold; seizures have been reported in patients receiving drug at antipsychotic dose levels, and may occur in epileptic patients even with maintenance of routine anticonvulsant drug therapy
The drug has an antiemetic effect in animals; since this effect may also occur in man, therapy may mask signs of overdosage of toxic drugs and may obscure conditions such as intestinal obstruction and brain tumor
Use with caution in patients with cardiovascular disease; increased pulse rates reported in majority of patients receiving antipsychotic doses; transient hypotension has been reported
Watch for hypotension if administering IM; in the presence of severe hypotension requiring vasopressor therapy, the preferred drugs may be norepinephrine or angiotensin; usual doses of epinephrine may be ineffective because of inhibition of its vasopressor effect by the drug
The possibility of ocular toxicity from therapy cannot be excluded; careful observation should be made for pigmentary retinopathy and lenticular pigmentation since these have been observed in some patients receiving certain other antipsychotic drugs for prolonged periods
Because of possible anticholinergic action, the drug should be used cautiously in patients with glaucoma or a tendency to urinary retention, particularly with concomitant administration of anticholinergic-type antiparkinson medication
Experience to date indicates the possibility of a slightly higher incidence of extrapyramidal effects following intramuscular administration than normally anticipated with oral formulations; increase may be attributable to higher plasma levels following intramuscular injection
Antipsychotic drugs elevate prolactin levels; the elevation persists during chronic administration; tissue culture experiments indicate that approximately one-third of human breast cancers are prolactin-dependent in vitro, a factor of potential importance if the prescription of these drugs is contemplated in a patient with a previously detected breast cancer
Pregnancy and Lactation
Pregnancy Category: C
Neonates exposed to antipsychotic drugs during the 3rd trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery
These complications vary in severity; in some cases, symptoms have been self-limited, while in other cases neonates have required intensive care unit support and prolonged hospitalization
Lactation: avoid in breastfeeding
Maximum Dosage
100 mg/day PO. 20 mg/day IM of haloperidol lactate. Clinical experience with haloperidol decanoate doses greater than 450 mg/month IM is limited.
100 mg/day PO. 20 mg/day IM of haloperidol lactate. Clinical experience with haloperidol decanoate doses greater than 450 mg/month IM is limited.
Weighing more than 40 kg: 15 mg/day PO for Tourette’s syndrome; there is no stated maximum dosage for adolescents with other indications; dosages exceeding 15 mg/day PO are rarely needed in adults but severely disturbed psychotic adults may require higher dosages; adult dosages up to 100 mg/day PO have been used in severe refractory cases. Safe and effective use of haloperidol injections has not been established (adult haloperidol lactate Max: 20 mg/day IM).
Weighing 40 kg or less: 0.15 mg/kg/day PO for most indications; severely psychotic patients may require higher doses (suggested Max: 6 mg/day PO for non-psychotic behaviors); 15 mg/day PO for Tourette’s syndrome. Safe and effective use of haloperidol injections has not been established (adult haloperidol lactate Max: 20 mg/day IM).
3 to 12 years and weighing 15 to 40 kg: 0.15 mg/kg/day PO for most indications; severely psychotic children may require higher doses (suggested Max: 6 mg/day PO for non-psychotic behaviors); 15 mg/day PO for Tourette’s syndrome. Safe and effective use of haloperidol injections has not been established (adult haloperidol lactate Max: 20 mg/day IM).
1 to 2 years or weighing less than 15 kg: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Loxapine
capsule
- 5mg
- 10mg
- 25mg
- 50mg
powder for oral inhalation
- 10mg/single-use inhaler
