loxapine

ROUTE	ONSET	PEAK	DURATION
PO	30 min	1.5–3 hr	12 hr
Inhaln	2 min	Unknown	Unknown

Contraindicated in:

Hypersensitivity or intolerance to loxapine or amoxapine;
Coma;
CNS depression;
Asthma, COPD, or other bronchospastic disease or use of medications to treat such disorders (inhalation only);
Acute respiratory signs/symptoms (inhalation only);
History of loxapine-induced bronchospasm (inhalation only);

Use Cautiously in:

Glaucoma;
Intestinal obstruction;
History of seizures;
Alcohol use disorder;
Cardiovascular disease;
Hepatic impairment;
Patients at risk for falls;
Older male adults or men with prostatic hyperplasia (more prone to urinary retention);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults are more susceptible to adverse reactions; ↑ risk of mortality in older adults patients treated for dementia-related psychosis.

Adv. Reactions/Side Effects ⬆ ⬇

CV: orthostatic hypotension, tachycardia

Derm: dermatitis, edema, facial photosensitivity, pigment changes, rash, seborrhea

EENT: blurred vision, lens opacities, nasal congestion

Endo: galactorrhea

GI: constipation, drug-induced hepatitis, dry mouth, ileus, nausea, vomiting

GU: urinary retention

Hemat: AGRANULOCYTOSIS

Neuro: confusion, dizziness, drowsiness, ataxia, extrapyramidal reactions, headache, insomnia, NEUROLEPTIC MALIGNANT SYNDROME, sedation, SEIZURES, syncope, tardive dyskinesia, weakness

Resp: BRONCHOSPASM (INHALATION)

Misc: allergic reactions

Interactions ⬆ ⬇

Drug-drug:

Blocks the alpha-adrenergic effects of epinephrine (may result in hypotension and tachycardia).
Additive CNS depression with other CNS depressants, including alcohol, antihistamines, opioid analgesics, and sedative/hypnotics.
Antacids or adsorbent antidiarrheals may ↓ absorption.
Use with antidepressants or MAO inhibitors may result in prolonged CNS depression and ↑ anticholinergic effects.

Drug-Natural Products:

Concomitant use of kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.

Route/Dosage ⬆ ⬇

PO (Adults ): 10 mg twice daily, may ↑ gradually over the first 7–10 days as needed and tolerated. Usual maintenance dose is 60–100 mg/day.
IM (Adults ): 12.5–50 mg every 4–6 hr or longer (some patients may respond to twice daily dosing).
Inhaln (Adults ): 10 mg as a single dose (one dose within a 24-hr period).

Availability ⬆ ⬇

(Generic available)

Tablets: 2.5 mg; 5 mg; 10 mg; 25 mg; 50 mg
Capsules: 5 mg; 10 mg; 25 mg; 50 mg
Powder for oral inhalation: 10 mg/inhaler (single-use inhaler)
Solution for injection: 50 mg/mL

Assessment ⬆ ⬇

Monitor patient’s mental status (orientation, mood, behavior) before and periodically during therapy.
Assess positive (delusions, hallucinations, agitation) and negative (social withdrawal) symptoms of schizophrenia.
Assess weight and BMI initially and throughout therapy. Refer as appropriate for nutritional/weight management and medical management.
Monitor BP (sitting, standing, lying) and pulse rate before and frequently during dose adjustment.
Observe patient carefully when administering medication to ensure that medication is actually taken and not hoarded or cheeked.
Monitor patient for onset of akathisia (restlessness or desire to keep moving) and extrapyramidal side effects (parkinsonian: difficulty speaking or swallowing, loss of balance control, pill rolling of hands, mask-like face, shuffling gait, rigidity, tremors; and.dystonic: muscle spasms, twisting motions, twitching, inability to move eyes, weakness of arms or legs) every 2 mo during therapy and 8–12 wk after therapy has been discontinued. Report these symptoms; reduction in dosage or discontinuation of medication may be necessary. Trihexyphenidyl, diphenhydramine, or benztropine may be used to control symptoms. Benzodiazepines may alleviate akathisia.
Monitor for tardive dyskinesia (uncontrolled rhythmic movement of mouth, face, and extremities; lip smacking or puckering; puffing of cheeks; uncontrolled chewing; rapid or worm-like movements of tongue, excessive eye blinking). Tardive dyskinesia is dose related initially but may increase with cumulative dose. Report immediately; may be irreversible.
Monitor frequency and consistency of bowel movements. Increasing bulk and fluids in the diet may help minimize constipation.
Loxapine lowers the seizure threshold. Institute seizure precautions for patients with history of seizures.
Monitor for symptoms related to hyperprolactinemia (menstrual abnormalities, galactorrhea, sexual dysfunction).
Monitor for development of neuroleptic malignant syndrome (fever, respiratory distress, tachycardia, convulsions, diaphoresis, hypertension or hypotension, pallor, tiredness, severe muscle stiffness, loss of bladder control). Report symptoms immediately.
Assess for falls risk. Drowsiness, orthostatic hypotension, and motor and sensory instability increase risk. Institute prevention if indicated.
Inhaln: May cause severe bronchospasm. Assess for history of pulmonary disease (asthma, COPD) and examine with auscultation for respiratory abnormalities including wheezing.
- Monitor for signs and symptoms of bronchospasm every 15 min for at least 1 hr after inhalation.

Lab Test Considerations:

Monitor CBC and differential before and periodically throughout therapy.
- Obtain fasting blood glucose and cholesterol levels initially and periodically during therapy.
- Monitor liver function studies and urine bilirubin and bile concentrations if patient develops jaundice.

Toxicity and Overdose:

Antiemetic effects of loxapine may block the action of ipecac. Overdose is treated by gastric lavage, barbiturates to control seizures, and supportive care for fluctuations in body temperature. Hypotension may be corrected by use of IV fluids, norepinephrine, or phenylephrine. Avoid use of epinephrine, as it may worsen hypotension.

Implementation ⬆ ⬇

REMS: Adasuve is only available through a restricted program, Adasuve REMS. Facilities must have a short-acting bronchodilator (albuterol), delivered by inhaler (with spacer) or nebulizer, for the immediate treatment of bronchospasm. Can only be administered in an enrolled facility with immediate on-site access to equipment and personnel trained to treat acute bronchospasm, including intubation and mechanical ventilation.
PO: Administer tablets and capsules with food or milk to decrease gastric irritation.
- Do not administer antacids or antidiarrheals within 2 hr of loxapine.
Inhaln: Must be administered by a health care professional. Use a single dose inhaler no more than once/24 hrs. Pull tab from rear of inhaler to turn on green light indicating inhaler ready for use. Must use within 15 min or will deactivate. Discard after use.

Patient/Family Teaching ⬆ ⬇

Inform patient of possibility of extrapyramidal symptoms and tardive dyskinesia. Instruct patient to report these symptoms immediately to health care professional.
Advise patient to change positions slowly to minimize orthostatic hypotension. Protect from falls.
May cause drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to the medication is known.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially alcohol and CNS depressants.
Instruct patient to use frequent mouth rinses, good oral hygiene, and sugarless gum or candy to minimize dry mouth. Consult health care professional if dry mouth continues for >2 wk.
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Instruct patient to notify health care professional promptly if sore throat, fever, unusual bleeding or bruising, rash, weakness, tremors, visual disturbances, dark-colored urine, or clay-colored stools occur.
Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Monitor neonates for extrapyramidal and/or withdrawal symptoms and manage symptoms appropriately. Recovery may occur within hrs or days without specific treatment; or require prolonged hospitalization. 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 1-866961-2388 or online at http://womensmentalhealth.org/clinical-and-researchprograms/pregnancyregistry/.
Advise patient of need for continued medical follow-up for psychotherapy, eye exams, and laboratory tests, and to detect side effects.
PO: Instruct patient on need to take loxapine as directed. Take missed doses as soon as remembered, up to 1 hr before next scheduled dose. Patients on long-term high-dose therapy may need to discontinue gradually to avoid withdrawal symptoms (dyskinesia, tremors, dizziness, nausea, and vomiting).
Inhaln: Inform patient that inhaler may produce a flash or light, a clicking sound, and may become warm; all are normal. Instruct patient to hold inhaler away from mouth and exhale, then place inhaler in mouth, close lips, and inhale a steady deep breath. Make sure green light turns off indicating dose was delivered. Hold breath as long as possible up to 10 seconds. If green light does not turn off, dose was not delivered; repeat up to twice more. If green light is still on, discard and get a new inhaler.
- Advise patient to notify healthcare professional immediately if bronchospasm occurs.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇