LOXAPINE HYDROCHLORIDE (lox'a-peen)
Loxitane C, Loxitane IM LOXAPINE SUCCINATE Loxitane, Loxapac  Classifications: psychotherapeutic; antipsychotic; Therapeutic: antipsychotic Prototype: Chlorpromazine Pregnancy Category: C
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Availability
5 mg, 10 mg, 25 mg, 50 mg capsules; 25 mg/mL oral solution; 50 mg/mL injection
Action
This antipsychotic blocks postsynaptic dopamine receptors in limbic system and increases dopamine turnover by blockade of
D2-receptors in that region. After approximately 12 wk of chronic therapy, depolarization blockade of dopamine occurs, decreasing
dopamine neurotransmission, correlating with its antipsychotic effects. D2-receptor blockade is also responsible for the potent extrapyramidal effects observed with use of this drug. Dopamine blockade
in the chemoreceptor trigger zone is responsible for antiemetic effects of the drug.
Therapeutic Effect
Stabilizes emotional component of schizophrenia by acting on subcortical level of CNS.
Uses
Manifestations of psychotic disorders.
Unlabeled Uses
Anxiety associated with mental depression.
Contraindications
Severe drug-induced CNS depression; Parkinson's disease; comatose states, children <16 y; pregnancy (category C), lactation.
Cautious Use
Glaucoma, prostatic hypertrophy, urinary retention, history of convulsive disorders, cardiovascular disease; alcoholism;
brain tumor; older adults; hematologic disease; hepatic disease; peptic ulcer disease; renal impairment; thyroid disease.
Route & Dosage
Psychosis Adult: PO Start with 10 mg b.i.d. and rapidly increase to maintenance levels of 60100 mg/d in 24 divided doses (max: 250
mg/d) IM 12.550 mg q46h
Dementia Behavior Geriatric: PO 510 mg 12 times/d, may increase q47d (max: 125 mg/d)
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Administration
Oral
- Give with food, milk, or water to reduce possibility of stomach irritation.
- Dilute oral concentrate in about 23 oz (6090 mL) water or orange or grapefruit juice shortly before administration.
Measure concentrate with calibrated dropper dispensed with drug. Do not store diluted solution.
Intramuscular
- Use only with acute psychosis or when oral route not feasible.
- Reduce dosage gradually over period of several days when therapy is to be terminated.
- Protect from light and freezing. Intensification of straw color to light amber is acceptable. Discard if solution is noticeably
discolored.
Adverse Effects (≥1%)
CNS: Drowsiness, sedation, dizziness, syncope, EEG changes, paresthesias, staggering gait, muscle weakness,
extrapyramidal effects, akathisia,
tardive dyskinesia, neuroleptic malignant syndrome. CV: Orthostatic hypotension, hypertension, tachycardia.
Special Senses: Nasal congestion, tinnitus; blurred vision, ptosis.
GI: Constipation, dry mouth.
Skin: Dermatitis, facial edema, pruritus, photosensitivity.
Urogenital: Urinary retention, menstrual irregularities.
Body as a Whole: Polydipsia, weight gain or loss, hyperpyrexia, transient leukopenia.
Interactions
Drug: Alcohol and other
cns depressants potentiate
CNS depression; will inhibit vasopressor effects of
epinephrine.
Pharmacokinetics
Absorption: Readily absorbed from GI tract.
Onset: 2030 min.
Peak: 1.53 h.
Duration: 12 h.
Distribution: Widely distributed; crosses placenta; distributed into breast milk.
Metabolism: In liver.
Elimination: 50% in urine, 50% in feces.
Half-Life: 19 h.
Nursing Implications
Assessment & Drug Effects
- Monitor baseline BP pattern prior and during therapy; both hypotension and hypertension have been reported as adverse reactions.
- Observe carefully for extrapyramidal effects such as acute dystonia (see Appendix F) during early therapy. Most symptoms
disappear with dose adjustment or with antiparkinsonism drug therapy.
- Discontinue therapy and report promptly to physician the first signs of impending tardive dyskinesia (fine vermicular movements
of the tongue) when patient is on long-term treatment.
- Monitor I&O and bowel elimination patterns and check for bladder distention. Depressed patients often fails to report urinary
retention or constipation.
- Risk of seizures is increased in those with history of convulsive disorders.
Patient & Family Education
- Do NOT change dosage regimen in any way without physician approval.
- Avoid self-dosing with OTC drugs unless approved by the physician.
- Drowsiness usually decreases with continued therapy. If it persists and interferes with daily activities, consult physician.
A change in time of administration or dose may help.
- Avoid potentially hazardous activity until response to drug is known.
- Learn measures to relieve dry mouth; rinse mouth frequently with water, suck hard candy. Avoid commercial products that may
contain alcohol and enhance drying and irritation.
- Notify physician of blurred or colored vision.
- Do not take drug dose and notify physician of following: Light-colored stools, bruising, unexplained bleeding, prolonged
constipation, tremor, restlessness and excitement, sore throat and fever, rash.
- Stay out of bright sun; cover exposed skin with sunscreen.