[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [First-generation antipsychotics](https://durgical.com/en/pharmacology/classes/first-generation-antipsychotics/) › Loxapine # Loxapine ## First-generation antipsychotics? First-generation antipsychotics A dibenzoxazepine antipsychotic of the first generation for schizophrenia. An inhaled form exists for acute agitation. It lowers the seizure threshold. Updated Nov 1, 2026 ## Quick facts **Group** [First-generation antipsychotics](https://durgical.com/en/pharmacology/classes/first-generation-antipsychotics/) **Target** Dopamine D2 receptor (antagonist) **Used for** Schizophrenia · Acute agitation **Key effects** Sedation · Dry mouth · Raised prolactin **Monitor** Abnormal movements · Seizures in people with epilepsy **ATC** N05AH01 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action Loxapine is a tricyclic dibenzoxazepine antipsychotic, chemically distinct from phenothiazines and butyrophenones. Like other first-generation agents its antipsychotic effect is linked to dopamine D2 blockade, and it has modest extrapyramidal effects. It calms quickly: sedation starts within half an hour by mouth. It also has anticholinergic actions. - Loxapine blocks dopamine D2 receptors - Less mesolimbic dopamine signal: less psychosis - Sedation within half an hour - Anticholinergic effects and a lower seizure threshold ## Indications - Schizophrenia [Schizophrenia →](https://durgical.com/en/conditions/schizophrenia/) - Acute agitation (inhaled form) ## Adverse effects ### Common - Sedation, unsteadiness and faintness - Dry mouth, blurred vision, constipation, difficulty urinating - Restlessness and abnormal movements - Raised prolactin: breast milk, breast enlargement, missed periods ### Serious (rare, important) - Higher mortality in older people with dementia-related psychosis (boxed warning) - Neuroleptic malignant syndrome; tardive dyskinesia - Seizures, even in people with epilepsy on treatment - Respiratory depression, stupor or hypotension reported with lorazepam ## Contraindications - Coma or severe drug-induced CNS depression (alcohol, barbiturates, opioids) - Hypersensitivity to dibenzoxazepines ## Key interactions **Lorazepam** Rare reports of significant respiratory depression, stupor or hypotension **Anticholinergic antiparkinson drugs** Added anticholinergic effects: caution in glaucoma or urinary retention **Alcohol and other CNS depressants** Added sedation ## What is monitored - Abnormal movements - Seizures in people with epilepsy - Weight - Signs of neuroleptic malignant syndrome ## Administration and safety - Oral capsules and the inhaled powder are different products used in different settings - Caution in glaucoma and urinary retention because of anticholinergic effects ## Pregnancy and breastfeeding Newborns exposed in the third trimester may have extrapyramidal or withdrawal symptoms; use weighs benefit and risk. ## Nursing care - Watches for sedation, dizziness and falls, especially in older patients - Looks for stiffness, tremor, restlessness and worm-like tongue movements - Watches breathing and level of consciousness if lorazepam is also given - Asks about urination and constipation ## Pharmacokinetics **Absorption** Capsules by mouth; an inhaled powder acts within minutes **Metabolism** Extensive liver metabolism; metabolites are excreted mainly in the first 24 hours **Onset and duration** Sedation within 20 to 30 minutes by mouth, most marked at 1.5 to 3 hours and lasting about 12 hours ## Memory aid «LOX = Low threshold for seizures, OX for oxazepine»: a tricyclic first-generation D2 blocker with an inhaled option for agitation. ## Test yourself Think of the answer, then tap the question to see it. ## To which chemical group does loxapine belong? Dibenzoxazepines, a tricyclic subclass of first-generation antipsychotics. ## Which neurological risk is a specific warning for loxapine? It lowers the seizure threshold; seizures can occur even in treated epilepsy. ## Which combination has caused respiratory depression and stupor? Loxapine with lorazepam. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/loxapine/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## Connections ## Related drugs 2 - [Haloperidol](https://durgical.com/en/pharmacology/haloperidol/) - [Chlorpromazine](https://durgical.com/en/pharmacology/chlorpromazine/) ## Related conditions 1 - [Schizophrenia](https://durgical.com/en/conditions/schizophrenia/) [← Back to the class: First-generation antipsychotics](https://durgical.com/en/pharmacology/classes/first-generation-antipsychotics/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [DailyMed - LOXAPINE capsule](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ce8c5a31-7600-4525-a0c7-b3adc9ec2977) (DailyMed (U.S. National Library of Medicine), 2026); [Loxapine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a682311.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N05AH01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/loxapine/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/loxapine/