for signs and symptoms of bronchospasm following administration; perform a physical exam, including chest auscultation at least q15min for at least 1 hr after the dose Increased mortality in elderly patients with demential-related psychosis (see Black Box Warnings) Antipsychotic drugs can cause neuroleptic malignant syndrome; symptoms include hyperpyrexia, muscle rigidity, altered mental status, and autonomic instability; associated findings include increased CPK, rhabdomyolysis, increased urine and serum myoglobin, and renal failure May cause hypotension, orthostatic hypotension, and syncope Lowers seizure threshold; use caution in patients with history of seizures May cause cognitive and motor impairment May cause sedation and somnolence; use caution when driving or operating machinery and when coadministered with other drugs known to cause CNS depression May cause anticholinergic adverse reactions, including exacerbation of glaucoma and urinary retention; caution when coadministered with other drugs that elicit anticholinergic effects Increased incidence of stroke and transient ischemic attack in elderly patients with dementia-related psychosis treated with antipsychotic drugs Pregnancy There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to atypical antipsychotics during pregnancy; healthcare providers are encouraged to register patients by contacting the National Pregnancy Registry for Atypical Antipsychotics at 1-866- 961-2388 or online at http://womensmentalhealth.org/ clinical-and-researchprograms/pregnancyregistry/ Neonates exposed to antipsychotic drugs, during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms following delivery The available data from published case reports and pharmacovigilance cases with loxapine in pregnant women are insufficient to determine a drug-associated risk for major birth defects, miscarriage or adverse maternal or fetal outcomes There are risks to mother associated with untreated schizophrenia or bipolar I disorder and with exposure to antipsychotics, including loxapine during pregnancy Extrapyramidal and/or withdrawal symptoms, including agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder reported in neonates exposed to antipsychotic drugs, including loxapine, during third trimester of pregnancy; these symptoms have varied in severity Monitor neonates for extrapyramidal and/or withdrawal symptoms and manage symptoms appropriately; some neonates recovered within hours or days without specific treatment; others required prolonged hospitalization Animal data In animal reproduction studies, increased embryofetal toxicity and death in rat fetuses and offspring were observed when pregnant rats were orally administered loxapine, during period of organogenesis, at doses approximately less or equal to maximum recommended human dose (MRHD) based on mg/m2 body surface area Lactation There is no available information on presence of loxapine in human milk, effects on breastfed infant, or on milk production The drug is present in milk of lactating dogs; when a drug is present in animal milk, it is likely that the drug will be present in human milk The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from therapy or from underlying maternal conditionPregnancy 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. Mechanism of Action Typical antipsychotic (dibenzoxazepine subclass of tricyclic antipsychotic agents); mechanism of action is unknown, but is theorized to antagonize central dopamine D2 and serotonin 5-HT2a receptors Absorption Peak Plasma Time: 2 minutes Peak Plasma Concentration: 257 ng/mL AUC: 66 ng•h/mL (0-2 hr); 188 ng•h/mL (infinity) Distribution Protein Bound: 96.6% Metabolism Metabolized extensively in the liver by hydroxylation; forms 8-OH-loxapine by CYP1A2 and forms 7-OH-loxapine by CYP3A4 and CYP2D6 Metabolized by N-oxidation to form loxapine N-oxide by flavanoid monoamine oxidases Demethylated to form amoxapine Because there are multiple metabolic pathways, the risk of metabolic interactions caused by an effect on an individual isoform is minimal Because there are multiple metabolic pathways, the risk of metabolic interactions caused by an effect on an individual isoform is minimal Elimination Half-life: 7.16 hr (range 6-8 hr) Excretion: feces (unconjugated metabolites); urine (conjugated metabolites) No images available for this drug. No images available for this drug.A Patient Handout is not currently available for this monograph.Print FormularyPatient DiscountsAdding 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.Create Your List of PlansAdding 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. The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information. View explanations for tiers and restrictions Tier Description 1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs. 2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs. 3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs. 4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. 5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. 6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. NC NOT COVERED – Drugs that are not covered by the plan. Code Definition PA Prior Authorization Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription. QL Quantity Limits Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered. ST Step Therapy Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription. OR Other Restrictions Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription. 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