Description: Loxapine, a dibenzoxazepine antipsychotic, antagonizes central dopaminergic action by blocking postsynaptic mesolimbic D1 and D2 receptors in the brain.


Absorption: Absorbed readily from the GI tract; peak plasma concentrations within 1-2 hr.

Distribution: Widely distributed; crosses the placenta and distributes into breast milk.

Metabolism: Very rapidly and extensively hepatic. Major metabolites: 7- and 8-hydroxyloxapine.

Excretion: Mainly via urine (as conjugated metabolites); via faeces (small amounts as unconjugated metabolites). 12-19 hr (terminal elimination half-life).

Loxapine is used to treat certain mental/mood disorders (such as schizophrenia) that helps you to think more clearly, feel less nervous, and take part in everyday life. It can decrease aggression and hallucinations (such as hearing/seeing things that are not there). Loxapine is a psychiatric medication (antipsychotic type) that works by helping to restore the balance of certain natural substances (such as dopamine) in the brain.

How to use loxapine

Take this medication by mouth, usually 2 to 4 times daily with or without food or exactly as directed by your doctor.

If you are using the liquid form of this medication, carefully measure the dose using a special measuring device/dropper and mix it in liquid or soft food (such as applesauce, pudding) just before taking. Do not use a household spoon because you may not get the correct dose.

Dosage is based on your medical condition and response to treatment. To reduce your risk of side effects such as drowsiness and shaking (tremor), your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor’s directions carefully.

Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day.

Although you may notice some improvement in your symptoms soon after starting this medication, it may take several weeks to months before you get the full benefit of this drug.

Do not stop taking this medication without consulting your doctor. Some conditions may become worse when this drug is suddenly stopped. Also, you may experience symptoms such as uncontrolled movements. To prevent these symptoms while you are stopping treatment with this drug, your doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details. Report any new or worsening symptoms immediately.

Tell your doctor if your condition does not improve or if it worsens.

There may be a slightly increased risk of serious, possibly fatal side effects (such as heart failure, fast/irregular heartbeat, pneumonia) when this medication is used by older adults with dementia.

This medication is not approved for the treatment of dementia-related behavior problems.

Tell your doctor or pharmacist promptly if any of these effects persist or worsen:

  • Drowsiness
  • Dizziness
  • Constipation
  • dry mouth
  • weight gain
  • blurred vision

This drug may cause muscle/nervous system problems (extrapyramidal symptoms-EPS). Therefore, tell your doctor right away if you notice any of the following side effects:

  • stiff muscles
  • restlessness/constant need to move
  • shaking (tremor)
  • slow/shuffling walk
  • drooling/trouble swallowing
  • mask-like expression of the face
  • severe muscle spasms/cramping (such as twisting neck, arching back, eyes rolling up)

Tell your doctor right away if you have any serious side effects, including:

  • easy bruising/bleeding
  • fainting
  • depression/suicidal thoughts
  • difficulty urinating
  • signs of infection (such as fever, persistent sore throat)
  • seizures
  • severe stomach/abdominal pain

This medication may cause a condition known as tardive dyskinesia. Tell your doctor right away if you develop any involuntary/repetitive muscle movements such as lip smacking/puckering, tongue thrusting, chewing, or finger/toe movements.

For females, increase in prolactin due to loxapine may result in unwanted breast milk, missed/stopped periods, or difficulty becoming pregnant. For males, it may result in decreased sexual ability, inability to produce sperm, or enlarged breasts. These are rare cases that may occur.

This medication may rarely cause a very serious condition called neuroleptic malignant syndrome (NMS). Get medical help right away if you have any of the following symptoms:

  • Fever
  • muscle stiffness/pain/tenderness/weakness
  • severe tiredness
  • severe confusion
  • sweating
  • fast/irregular heartbeat
  • dark urine
  • change in the amount of urine

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including:

  • Rash
  • itching/swelling (especially of the face/tongue/throat)
  • severe dizziness
  • trouble breathing

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

  • Allergic reaction from this medication
  • Patients with medical history of:
  • blood problems (such as low red/white/platelet blood cell counts)
  • a certain eye condition (glaucoma)
  • heart problems (such as fast/irregular heartbeat, low blood pressure)
  • liver disease
  • a brain disorder/tumor/injury
  • drug/alcohol/substance abuse
  • breast cancer
  • Parkinson’s disease
  • Seizures
  • a certain severe reaction to other antipsychotic-type medications (neuroleptic malignant syndrome-NMS)
  • difficulty urinating (such as due to prostate problems)
  • This drug may make you dizzy or drowsy or cause blurred vision.
  • This medication may rarely make you more sensitive to the sun.
  • Tell your doctor or dentist that you are using this medication before having surgery or imaging procedures (such as certain X-rays, CT scans) requiring the use of contrast dye (such as metrizamide)
  • This medication may make more likely to get heat stroke
  • Older adults may be more sensitive to dizziness, extrapyramidal symptoms (EPS), and tardive dyskinesia (TD) from the drug
  • This medication should be used only when clearly needed during pregnancy
  • Do not stop taking this medication unless directed by your doctor
  • Discuss the risk and benefits with your doctor before breast-feeding

Consult your doctor regarding the precautions mentioned above.



Metoclopramide and certain drugs used for Parkinson’s disease (such as bromocriptine, levodopa, pergolide) may interact with this drug.

Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as codeine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

If overdose is suspected, contact a poison control center or emergency room immediately.


Do not share this medication with others.

Laboratory and/or medical tests (such as eye examinations, complete blood count) may be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

Missed Dose

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.


Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.



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