Dosing & Uses
Dosage Forms & Strengths
capsule
- 5mg
- 10mg
- 25mg
- 50mg
Schizophrenia
Initial: 10-25 mg PO q12hr
Maintenance: 60-100 mg/day divided q6-12hr; not to exceed 250 mg/day
Not recommended
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
Frequency Not Defined
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)
Postmarketing Reports
Falls
Warnings
Black Box Warnings
Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature.
This drug is not approved for the treatment of patients with dementia-related psychosis.
Bronchospasm
- Can cause bronchospasm with potential to lead to respiratory distress and respiratory arrest
- Available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the ADASUVE REMS
- Administer only in an enrolled healthcare facility that has immediate access on site to supplies and personnel trained to manage acute bronchospasm, and ready access to emergency response services; facilities must have short-acting bronchodilator, including a nebulizer and inhalation solution, for immediate treatment of bronchospasm
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
Cautions
Caution in patients with cardiovascular disease or seizures; watch for hypotension if administering IM; in patients taking benzodiazepines, loxapine should be preceded by stopping benzodiazepine therapy for 2 weeks to avoid drug interactions capable of respiratory depression
May cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls and, consequently, fractures or other injuries; perform complete fall risk assessments when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy
FDA Warning regarding off-label use for dementia in elderly
Can cause bronchospasm that has potential to lead to respiratory distress and respiratory arrest (See BBW)
REMS to Mitigate Bronchospasm
- Available only through restricted program under a REMS called the ADASUVE REMS
- Healthcare facilities that dispense and administer therapy must be enrolled and comply with REMS requirements; certified healthcare facilities must be able to provide immediate access on site to supplies and personnel trained to manage acute bronchospasm, and ready access to emergency response services
- Facilities must have a short-acting bronchodilator (e.g., albuterol), including nebulizers and inhalation solutions, for immediate treatment of bronchospasm
- Wholesalers and distributors must distribute only to enrolled healthcare facilities
Pregnancy & 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
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Dibenzoxazepine antipsychotic; blocks mesolimbic D1 and D2 receptors in the brain; also has anti-serotonin 5HT2 activity
Pharmacokinetics
Half-Life: 4-12 hr
Duration: 12 hr
Onset: 20-30 min
Peak plasma time: 1-2 hr (PO); 5 hr (IM)
Peak plasma concentration: 0.006-0.013 mcg/mL
Metabolism: Aromatic hydroxylation, N-demethylation, N-oxidation
Metabolites: 8-hydroxyloxapine, 7-hydroxyloxapine
Excretion: Urine (56-70%), feces
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
