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loxapine (Loxitane, Dibenzoazepine, Cloxazepin)
Tradename: Loxitane.
Indications:
1) symptomatic management of psychotic disorders
2) may be preferred for paranoid patients
Contraindications:
1) narrow-angle glaucoma
2) bone marrow depression
3) severe liver disease
4) severe cardiac disease
5) severe CNS depression or coma
Dosage:
1) 12.5-50 mg IM every 4-6 hours, PRN.
2) start 10 mg PO BID
3) usual effective dose: 60-100 mg//day divided BID-QID
4) max 250 mg/day
Tabs: 5, 10, 25, 50 mg.
Liquid: 25 mg/mL.
Pharmacokinetics:
1) metabolized by liver to many active metabolites
2) metabolites excreted in the urine & feces
3) elimination 1/2life is 4-5 hours
Adverse effects:
1) common (> 10%)
- drowsiness
- extrapyramidal symptoms are moderate
- tardive dyskinesia (persistent)
- pseudoparkinsonism
- dystonias
- akathisia
3) low anticholinergic & orthostatic hypotensive effects
- blurred vision, dry mouth, confusion
2) less common (1-10%)
- constipation, skin rash, breast enlargement, nausea/vomiting
3) uncommon (< 1%)
- tachycardia, arrhythmias, abnormal T-waves with prolonged ventricular repolarization, sedation, restlessness, anxiety, altered central temperature regulation, hyperpigmentation, pruritus, rash, amenorrhea, galactorrhea, gynecomastia, weight gain, adynamic ileus, agranulocytosis*, leukopenia#, retinal pigmentation, urinary retention, overflow incontinence, sexual dysfunction, photosensitivity,
4) other
- moderate sedation profile
- neuroleptic malignant syndrome is rare
- QT prolongation
- direct myocardial depression
- seizures (rare)
- increased mortality in elderly
* Most frequent in women in 4th-10th week of therapy
# Usually after large doses for prolonged periods
Drug interactions: (see chlorpromazine)
Mechanism of action:
1) intermediate/high potency antipsychotic
2) has antidepressant properties
3) see chorpromazine
Interactions
drug interactions
drug adverse effects (more general classes)
Related
chlorpromazine (Thorazine, Ormazine, Propaphenin, Sonazine, Chloractil)
General
antipsychotic agent
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Schneeweiss S et al,
Risk of death with use of conventional versus atypical
antipsychotic drugs among elderly patients.
CMAJ 2007, 176:627
PMID: 17325327