Relation of plasma prolactin to clinical response in schizophrenic patients.

It has been suggested that, if dopamine antagonism is a necessary condition for the antischizophrenic action of neuroleptics, the prolactin response, as an index of dopamine blockade, would correlate with clinical response. Morning prolactin and clinical symptomatology were measured in 15 schizophrenic patients before neuroleptic therapy, and after three and six weeks of high-dose butaperazine or loxapine treatment. Prolactin levels were transiently elevated during the unmedicated admission period, probably reflecting a normal stress response. Prolactin increased in all patients during neuroleptic therapy. There was, however, no correlation between magnitude of prolactin changes and clinical response, probably because the prolactin response achieved a maximum at relatively low doses of neuroleptics.

Fluradoline and aspirin for orthopedic postoperative pain.

Fluradoline (150 or 300 mg), a novel tricyclic with both antidepressant and analgesic properties in animals, was compared with aspirin, 650 mg, and placebo when given orally for postoperative orthopedic pain in a double-blind, single-dose, parallel-group study. Analgesic measurements were made by two trained nurse observers using standard verbal rating and visual analogue scales. Aspirin was statistically superior to placebo on all analgesic measures, demonstrating assay sensitivity. Fluradoline, 300 mg, was distinguished from placebo and fluradoline, 150 mg, but not from aspirin, 650 mg. Overall, fluradoline, 300 mg, was equivalent to aspirin, 650 mg. Fluradoline, 300 mg, produced a significant elevation in mood score. Neither aspirin, 650 mg, nor fluradoline caused untoward side effects, but fluradoline, 300 mg, increased blood pressure.

Successful treatment of obsessive-compulsive disorder with loxapine.

The authors describe a 21-year-old man with severe, incapacitating obsessive-compulsive symptoms who was treated successfully with loxapine. The patient's response to the drug was rapid, dramatic, and sustained.

Amoxapine and imipramine in the treatment of depressed outpatients: a controlled study.

In a double-blind, controlled study 158 outpatients with unipolar depression were treated for six weeks with amoxapine, imipramine, or placebo to assess the antidepressant effects of the new dibenzooxazepine compound, amoxapine. Forty-five amoxapine, 43 imipramine, and 27 placebo patients completed at least four weeks of treatment. Active drugs produced significantly more improvement at treatment endpoint, according to several physician-rated measures, but patient-rated measures failed to differentiate among treatments. Both active drugs at daily doses up to 200 mg produced an equal amount of moderate and marked global improvement, and both produced significantly more side effects than did placebo.

Efficacy of antipsychotic medications in behaviorally disturbed dementia patients.

This study compared the therapeutic efficacy of thioridazine, loxapine, and a placebo in the treatment of behavioral disturbances in nursing home patients with dementia. Antipsychotic medications were effective for the specific behavioral problems of anxiety, excitement, emotional lability, and uncooperativeness. Subjects with the most severe symptoms at baseline assessment derived the greatest benefit from treatment. Sedation, extrapyramidal symptoms, and decreased blood pressure were common side effects among patients treated with the antipsychotic drugs. The authors conclude that antipsychotic medication has a definite but limited therapeutic role in the treatment of behavioral disturbances in nursing home patients with dementia.

Is loxapine more effective than chlorpromazine in paranoid schizophrenia?

The authors compared loxapine with chlorpromazine in inpatients with paranoid schizophrenia and found no difference in clinical efficacy. Thus a previous finding, based on retrospective analyses, that loxapine was superior to other neuroleptics in the treatment of paranoid schizophrenia was not verified in this prospective study.

Loxapine as an alternative to phenothiazines in a case of oculocutaneous skin pigmentation.

The authors describe a patient with changes in oculocutaneous pigmentation that cleared after chlorpromazine was discontinued. They suggest that loxapine may be a suitable alternative to phenothiazines when skin pigmentation and ocular involvement occur, although the patient must be carefully monitored for ocular problems.

Amoxapine versus amitriptyline combined with perphenazine in the treatment of psychotic depression.

In a double-blind study lasting for 4 weeks, the authors compared the effectiveness of amoxapine, an antidepressant with potential antipsychotic properties, with a combination of amitriptyline plus perphenazine in the treatment of 38 patients who had the diagnosis of major depression with psychotic features (psychotic or delusional depression). Patients in each group showed similar improvement in depression and psychosis. There was a tendency for the patients treated with amitriptyline plus perphenazine to have higher global response rates. However, the patients given amoxapine had significantly fewer extrapyramidal side effects.

Efficacy of amoxapine in psychotic depression.

Psychotic depression is a distinct clinical entity in that its response to tricyclic antidepressants is poor but its response to tricyclic antidepressant-antipsychotics is better. The authors report the favorable outcome of four patients with psychotic depression treated with amoxapine, a derivative of the antipsychotic loxapine. The elevation of serum prolactin during treatment in three patients suggests that postsynaptic dopamine blockade occurs with amoxapine treatment. This might account for the efficacy of amoxapine in psychotic depression.

Imipramine reduces experimental pain.

In a homogeneous sample of 20 healthy male students, the analgesic effects of the tricyclic antidepressant imipramine (100 mg) were compared to those of the narcotic meperidine (150 mg) and a further tricyclic compound with assumed analgesic properties (fluradoline, 450 mg). Drugs were orally administered, using a placebo controlled, double-blind repeated measures Latin Square design. Phasic pain was induced by intracutaneous electrical shocks with random intensities and interstimulus intervals. Each stimulus block consisted of 80 stimuli and lasted for 20 min. Pain estimates, somatosensory evoked cerebral potentials (SSEPs) and power spectral density of the electroencephalogram (EEG) were measured under each drug condition. Under placebo, pain ratings and SSEP amplitudes were constant within the entire session lasting for approximately 4 h. Meperidine analgesia was evident within 30 min of drug application, reaching a maximum after about 90 min. Imipramine produced a comparable degree of pain reduction, however, with a delay of 2 h. Under both drugs, the decrease in pain ratings was accompanied by decreased amplitudes of the late components of the SSEP, as well as by a reduction in alpha activity and an enhancement of slow EEG waves. Effects of fluradoline on experimental pain could not be affirmed. These findings are discussed in terms of pain relief and decrease in vigilance.

Suppression of tardive dyskinesia with amoxapine: case report.

Evidence of the neuroleptic potency of amoxapine is rapidly accumulating. A case history is presented which complements the growing literature in this area. A depressed patient with persistent orofacial dyskinesia was placed on amoxapine and experienced a suppression of her involuntary movements. The therapeutic implications of this observation are discussed.

A critical appraisal of amoxapine.

The authors provide a literature review and assess amoxapine's clinical pharmacology, therapeutic efficacy and side effects. They conclude that Amoxapine is indicated for use in moderate to severe depressions, has a favorable side effect profile and probably has an earlier onset of action than other tricyclic antidepressants.

A comparison of the onset of action and therapeutic efficacy of amoxapine and amitriptyline.

A total of 61 moderately to severely depressed outpatients were treated for four weeks with either amoxapine (a dibenzoxapine tricyclic) or amitriptyline. This double blind study showed that amoxapine was as effective as amitriptyline and had an earlier onset of action. Maximum doses used were 300 mg of amoxapine and 150 mg of amitriptyline. Side effects were similar for the two drugs, except for impotence or loss of libido in eight male amoxapine, as against three amitriptyline patients. Laboratory, EKG, and vital signs findings showed no pathological trends.

Treatment of depression in outpatients: a controlled comparison of the onset of action of amoxapine and maprotiline.

In a 4-week double-blind study, amoxapine and maprotiline were compared in the treatment of 76 outpatients with moderate to severe depressive illness. Mean maximum daily dosages were 230 mg for amoxapine and 165 mg for maprotiline. The data suggest that in these dosages amoxapine and maprotiline are equally effective overall. However, significant differences favored amoxapine at Days 4 and 7, in agreement with other studies showing early onset of therapeutic action of amoxapine.

Amoxapine and amitriptyline in the outpatient treatment of endogenous depression.

This double-blind investigation compared onset of action, efficacy, and safety of amoxapine and amitriptyline in 46 endogenously depressed outpatients. Statistical analysis demonstrated relatively few significant differences in improvement between the two groups. Most of the differences favored amoxapine, however, and on all measures there were clear trends favoring amoxapine for more rapid onset of action or greater overall efficacy or both.

A comparison of parenteral loxapine and haloperidol in hostile and aggressive acutely schizophrenic patients.

In a parallel groups, double-blind study, 54 acutely psychotic schizophrenics were given loxapine or haloperidol parenterally for 24 to 72 hours, then orally for a total study period of up to 10 days. Dosage ratios of loxapine to haloperidol ranged from a minimum of 2.7:1 to a maximum of 4.4:1. Both groups showed significant and rapid improvement from baseline. Forty-eight percent of the loxapine patients and 33% of the haloperidol patients achieved and maintained a global severity of illness rating of mild or better. By the end of the study, 84% of the loxapine patients and 63% of the haloperidol patients had achieved an improvement rating of moderate or marked. This difference approached significance (p less than .10). The most frequently reported adverse experiences were dystonic reactions and akathisia. The number and severity of adverse experiences did not differ significantly between drug groups. Intramuscular loxapine was at least as effective as haloperidol in the initial management of hostile and aggressive schizophrenic patients. The maintenance of therapeutic response after conversion to oral concentrate was comparable with the two drugs.

Onset of action of amoxapine and doxepin in outpatients with "mixed anxiety/depression".

In a parallel-group double-blind study, 142 outpatients with "mixed anxiety/depression" were treated with amoxapine or doxepin for 4 weeks in mean maximum daily dosages of 260 mg and 130 mg, respectively. Patients in both groups improved significantly during treatment as shown by changes in the Hamilton, Zung, Patient Self-Evaluation, and Clinical Global Impressions scales. From 24 to 31 of the 71 subjects receiving amoxapine and 16 to 24 of the 71 receiving doxepin were rated as "unquestionably improved" at the end of the treatment period on these scales. The time to achieve this degree of response was significantly shorter with amoxapine on both the CGI (p = .018) and Hamilton (p = .005) scales. Side effects were roughly comparable with two exceptions: doxepin-treated patients experienced more daytime drowsiness (p less than or equal to .05) and amoxapine-treated patients experienced more constipation (p less than or equal to .01).

Double-blind comparison of amoxapine and imipramine in the treatment of depressed patients.

A 5-week double-blind study compared amoxapine to imipramine (2:1 dosage ratio) in the treatment of depressed outpatients. The two agents were similar in anti-depressant efficacy and rapidity of action. The most common adverse reactions to both drugs were anticholinergic effects and sedation; cardiovascular effects were minimal. A few amoxapine-treated patients developed adverse effects typical of neuroleptic drugs: some experienced extrapyramidal signs, one developed galactorrhea, and most showed elevated plasma prolactin concentrations. Amoxapine was associated with significant neuroleptic activity in plasma. No correlation was found between blood levels of either drug and therapeutic response.

Loxapine versus chlorpromazine in paranoid schizophrenia: a double-blind study.

Newly admitted paranoid schizophrenic patients (N = 68) were treated with either loxapine or chlorpromazine for up to 4 weeks. Mean maximum dosages were 84 mg/day of loxapine and 820 mg/day of chlorpromazine. Loxapine showed efficacy superior to that of chlorpromazine, confirming earlier retrospective findings. Adverse reactions were also less troublesome with loxapine.

Tricyclic antidepressant use in a patient with bundle branch blocks and ventricular ectopy.

Amoxapine, a dibenzoxapine tricyclic antidepressant, was used successfully to treat a depressed elderly woman with left anterior hemiblock, right bundle branch block, and ventricular ectopy. This case highlights the importance of serial electrocardiographic monitoring in depressed patients with cardiac abnormalities treated with tricyclic antidepressants. The apparent reduction of ectopy in this case indicates a possible quinidine-like action of amoxapine.