Chemical Name

Loxapine

 

Ingredients

Active Ingredients: Loxapine

Non-Active Ingredients: blue 1, gelatin, lactose, magnesium stearate, titanium dioxide, and yellow 10. 

 

Indications

Loxitane is indicated for the treatment of schizophrenic patients who fail to respond adequately to standard drug treatment for schizophrenia.

 

How It Works

Loxapine is a tricyclic antipsychotic. It works as a tranquilizer for which the exact mode of action has not been established. However, changes in the level of excitability of sub-cortical inhibitory areas have been observed.

 

Dosage

Tablets (10 mg or 25 mg) 

 

Loxitane is usually taken in divided doses 2-4 times per day. An initial dosage of 10mg twice daily is recommended, this dosage can be raised over the next 7-10 days until an optimal dosage is achieved. The usual therapeutic and maintenance dose range is 60 to 100mg per day. In severely schizophrenic or aggressive patients an initial dosage of up to 50mg daily may be desirable. Daily doses of more than 250mg are not recommended.

 

Precautions

Loxitane is contraindicated in patients with a previous hypersensitivity to loxapine or any other component of this drug, in patients with myeloproliferative disorders, uncontrolled epilepsy or other seizure disorder, a history of low white blood cell (WBC) counts, glaucoma, urination problems, heart disease, a history of breast cancer, paralytic ileus, or a history of Loxitane induced agranulocytosis or severe granulocytopenia. If you have a history of any of the above you may not be able to take Loxitane or you may require a reduced or tailored dosage. As with more typical antipsychotic drugs, Loxitane is contraindicated in severe central nervous system depression or comatose states from any cause.

 

Among elderly patients with dementia-related psychosis, treatment with loxapine is associated with an increased risk of heart failure, sudden death, or pneumonia. Loxapine is not approved for use in dementia-related psychosis.

 

Seizures have occurred in approximately one out of every 20 to 30 persons receiving loxapine. Patients receiving higher doses seem to be at higher risk. Loxapine may cause a severe reduction in white blood cell count. White blood cells fight infections. If there is a severe reduction in white blood cells, it can result in severe infections. Early detection may avoid fatality. Therefore, the white blood cell count should be measured.

There are no adequate studies of loxapine in pregnant women. If you are pregnant or thinking about becoming pregnant, talk your doctor to see if the benefit outweighs the adverse effects. It is not recommended to breastfeed while on this medication.

 

Loxapine also may cause sudden, often jerky, uncontrollable motions of the body and eyes. The risk of such reactions appears to be lower with loxapine than with older anti-psychotics, perhaps due to its weaker effects on dopamine type-2 receptors. Patients ought to be tested during treatment for elevated blood-sugars. In addition, patients with risk factors for diabetes, including obesity or a family history of diabetes, should have their fasting levels of blood sugar tested before they start treatment and periodically throughout treatment to detect the onset of diabetes. Any patient developing symptoms that suggest diabetes during treatment should be tested for diabetes.

 

Loxapine is eliminated from the body by enzymes P450 in the liver. Many medications can increase or decrease the activities of these enzymes leading to low (potentially ineffective) or highly toxic levels of loxapine in the blood.  When used with these medications, the dose of loxapine may need to be reduced or increased.

 

The possibility of increased hazardous seizures and other adverse reactions at higher dosages, patients should ordinarily be given adequate time to respond to any given dosage before increasing the allocated dosage.

 

Patients should be advised to report immediately the appearance of lethargy, weakness, fever, sore throat or any other signs of infection occurring at any time during Loxitane (loxapine) therapy. Such patients should have a WBC count and ANC performed promptly. 

Hyperglycemia, in some cases extreme and associated with ketoacidosis or coma or death, has been reported in patients treated with atypicalantipsychotics including Loxitane. A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported with antipsychotic drugs. This syndrome manifests as muscle rigidity, altered mental status and evidence of autonomic instability.

 

A syndrome consisting of potentially irreversible, involuntary, dyskinetic movements may also develop in patients treated with antipsychotic drugs, although the prevalence of the syndrome appears to be highest among the elderly - especially elderly women.

 

If signs and symptoms of tardive dyskinesia appear in a patient on Loxapine, drug discontinuation should be considered.

 

Gradual reduction in dosage is recommended over a one-to-two week period. However, should a patient's medical condition require abrupt discontinuation (leukopenia), the patient should be carefully observed for the recurrence of psychotic symptoms and symptoms related tocholinergic rebound such as headache, nausea, vomiting, and diarrhea. If you are pregnant or thinking about becoming pregnant, do not take this drug without speaking to a physician first.

Drug Interactions

Loxapine should not be taken concurrently with Lorazepam as there have been rare reports of significant respiratory depression, stupor and/or hypotension with the concomitant use of these two drugs.

 

Enzymes may decrease the plasma levels of loxapine. Phenytoin, tobacco, and rifampin may decrease Loxitane plasma levels, resulting in a decrease in effectiveness of a previously effective Loxitane dose. Cimetidine, caffeine, citalopram, ciprofloxacin, and erythromycin may increase plasma levels of Loxitane.

 

Fluvoxamine, debrisoquin, dextromethorphan, and tricyclic antidepressants may interact. In addition, certain drugs that are metabolized by this isozyme, including many antidepressants (loxapine, selective serotonin reuptake inhibitors, and others), may inhibit the activity of this isozyme, requiring lower doses than usually prescribed for either loxapine or the other drug. Therefore, co-administration of loxapine with other drugs that are metabolized by this isozyme, which include antidepressants, phenothiazines, carbamazepine, and Type 1c antiarrhythmics, propafenone, flecainide,  encainide, or that inhibit this enzyme like quinidine, should be approached with caution.

 

Risperidone (Risperdal) may cause an increase in the amount of loxapine in the blood. This could lead to an increased risk of side effects from loxapine. Always tell you doctor about your medical history and about any drugs or supplements you may be taking.

 

Adverse/Side Effects

The most common side effect of loxapine is drowsiness. Central nervous system complaints, including drowsiness/sedation, dizziness/vertigo, headache and tremor, autonomic nervous system complaints, including salivation, sweating, dry mouth along with the possibility of visual disturbances; cardiovascular findings, including tachycardia, hypotension and syncope; and gastrointestinal complaints, including constipation and nausea; and fever are all potential side effects. Complaints of drowsiness/sedation tend to subside with continued therapy or dose reduction. Salivation may be profuse, especially during sleep, but may be diminished with dose reduction.

 

Tell your doctor immediately if you experience any of the following serious side effects: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, easy bruising or bleeding, unusual weakness, fever, chills, body aches, flu symptoms, feeling like you might pass out, restless muscle movements in your eyes, tongue, jaw, or neck, tremor (uncontrolled shaking), trouble swallowing, seizure (convulsions), vision changes, severe constipation or urinating less than usual or not at all.

 

Other less serious side effects include: dizziness or drowsiness, blurred vision, puffiness in your face, feeling restless or agitated, sleep problems (insomnia), breast swelling or discharge, changes in your menstrual periods, nausea, vomiting, constipation, changes in weight, dry mouth, stuffy nose or mild skin rash, itching, or flaking.

 

Other rare side effects that may occur include: edema, acute pancreatitis, dysphagia, fecal impaction, intestinal obstruction/paralytic ileus, inability of bile to flow from liver, hapitits, jaunice, acute interstitial nephritis, inability of penis or clitori to return to facid state, photosensitivity, inflammatory destruction of blood cells, superficial microvasculature of the skin, hypercholesterolemia, new onset diabetes, myasthenic syndrome, rhabdomyolysis, aspiration, pleural effusion, and pneumonia and lower respiratory tract infection which may be fatal, deep vein thrombosis, elevated hemoglobin/hematocrit, ESR increase, pulmonary embolism sepsis, thrombocytosis, thrombocytopnia, narrow angle glaucoma, CPK elevation, hyperglycemia, hyperuricemia, hypoartemia and weight loss. If any of these side effects occur immediately consult your doctor.

 

Overdose

In case of overdose contact local poison control or emergency room. Symptoms of Loxitane overdose include: decreased urination, difficulty breathing, involuntary, uncontrolled muscle movements, loss of consciousness, seizures, severe or persistent dizziness.

 

Storage Instructions

Store at room temperature, away from moisture and light, and out of reach of children and pets.